Publications by authors named "Gunes Ak"

42 Publications

and as Sources of Antioxidants and Multi-Target Bioactive Compounds: A Comprehensive Characterization Combining Bioassays and Integrated NMR and LC-MS Characterization by Using a Multivariate Approach.

Front Pharmacol 2021 26;12:660735. Epub 2021 Mar 26.

Department of Biology, Science Faculty, Selcuk University, Konya, Turkey.

and were evaluated for their phytochemical content and bioactivity. NMR analyses were performed on the methanol extract of the aerial parts of to establish the main classes of phytoconstituents. Then, LC-DAD-MS analyses were performed in order to compare the composition of aerial parts and roots extracts of both species, obtained using either methanol or water as solvents. Results, processed using multivariate data analysis, showed a significantly higher phenolic content of methanol extracts compared to water extracts, while minor qualitative differences were observed between the two. Distinctive flavonoid and PAC patterns were observed for and , and specific compounds were exclusively detected in one or the other species. Specifically, the phloroglucinols 7-epiclusianone, hyperfirin and hyperforin were present only in while hyperforin was detected only in Extracts were assayed using different tests to evaluate their antioxidant properties and their inhibitory activity against several enzymes, showing significant antioxidant and metal chelating activities. Furthermore, inhibitory properties against acetylcholinesterase, butyrylcholinesterase and tyrosinase were observed. Multivariate approaches were used to correlate biological data with the phytochemical composition of the different extracts. The results, showing positive correlations between specific chemical constituents and the measured bioactivities, represent preliminary data that could guide future studies aimed at isolating bioactive constituents from and for further pharmacological evaluations.
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http://dx.doi.org/10.3389/fphar.2021.660735DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8033251PMC
March 2021

Chemical Composition and Pharmacological Evaluation and of Toddalia asiatica (Rutaceae) Extracts and Essential Oil by in Vitro and in Silico Approaches.

Chem Biodivers 2021 Mar 19. Epub 2021 Mar 19.

Department of Health Sciences, Faculty of Medicine and Health Sciences, University of Mauritius, Moka, Réduit, 80837, Mauritius.

Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Despite its frequent use in traditional medicine, there is still a paucity of scientific information on T. asiatica growing on the tropical island of Mauritius. Therefore, the present study was designed to appraise the pharmacological and phytochemical profile of extracts (methanol, ethyl acetate and water) and essential oil obtained from aerial parts of T. asiatica. Biological investigation involved the evaluation of in vitro antioxidant and enzyme inhibitory potentials. The chemical profile of the EO was determined using gas chromatography coupled to mass spectrometry (GC/MS) analysis, while for the extracts, the total phenolic (TPC) and flavonoid content were quantified as well as their individual phenolic compounds by LC/MS/MS. Quinic acid, fumaric acid, chlorogenic acid, quercitrin and isoquercitrin were the main compounds in the extracts. Highest total phenolic (82.5±0.94 mg gallic acid equivalent (GAE/g)) and flavonoid (43.8±0.31 mg rutin equivalent (RE/g)) content were observed for the methanol extract. The GC/MS analysis has shown the presence of 26 compounds with linalool (30.9 %), linalyl acetate (20.9 %) and β-phellandrene (7.9 %) being most abundant components in the EO. The extracts and EO showed notable antioxidant properties, with the methanol extract proved to be superior source of antioxidant compounds. Noteworthy anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE) effects were recorded for the tested samples, while only the methanol and ethyl acetate extracts were active against tyrosinase. With respect to antidiabetic effects, the extracts and EO were potent inhibitors of α-glucosidase, while modest activity was recorded against α-amylase. Docking results showed that linalyl acetate has the highest affinity to interact with the active site of BChE with docking score of -6.25 kcal/mol. The findings amassed herein act as a stimulus for further investigations of this plant as a potential source of bioactive compounds which can be exploited as phyto-therapeutics.
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http://dx.doi.org/10.1002/cbdv.202000999DOI Listing
March 2021

Chemical composition, biological properties and bioinformatics analysis of two Caesalpina species: A new light in the road from nature to pharmacy shelf.

J Pharm Biomed Anal 2021 May 9;198:114018. Epub 2021 Mar 9.

Department of Virology with SARS Laboratory, Medical University of Lublin, Chodzki 1, 20-059, Lublin, Poland.

Caesalpinia bonduc and C. decapeleta var. japonica have great importance in traditional medicine systems but scientific information's are still lacking for their potentials. To explore their bioactivity, we assessed the antioxidant, enzyme inhibitory abilities of the dichloromethane (DCM), ethyl acetate, methanol, and water extracts prepared from the leaves and bark. The cytotoxicity and anticancer properties of the extracts were also assessed in vitro. The water extract of C. decapeleta leaves possessed highest phenolic content (108.16 mg gallic acid equivalent (GAE)/g extract), while the highest flavonoid content was recorded for the C. bonduc leaf methanolic extract (27.89 mg rutin equivalent (RE)/g extract). In general, C. decapeleta extracts possessed higher radical scavenging potential compared to C. bonduc extracts. C. decapeleta DCM leaves extract (10.20 mg galantamine equivalent (GALAE)/g extract) showed highest inhibition against butyrylcholinesterase. The cytotoxicity of the most potent methanolic and aqueous extracts were assessed against four cell lines. The chemical profiles of both species appeared to be different. C. bonduc was abundant in organic and phenolic acids as well as their esters. Flavonoid glycosides, bonducellin and its derivatives and caesalminaxins were identified. Whereas, C. decalpetala possessed many galloylated compounds. The cytotoxicity of C. bonduc and C. decapetala extracts was tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) based assay on VERO (kidney of an adult African Green monkey cells), HeLa (human cervical adenocarcinoma cells), RKO (human colon carcinoma cells), FaDu (human hypopharyngeal squamous carcinoma cells) cell lines. C. bonduc bark water extract exhibited the highest cytotoxicity towards HeLa (50 % cytotoxic concentration (CC): 28.5 μg/mL) cancer cell line, as compared to normal VERO cells (CC:35.87 μg/mL). For C. decapetala, the highest cytotoxicity was found for bark methanol extract on the HeLa cells with CC of 46.08 μg/mL and selectivity index of 3.33. In the gene ontology analysis, prostate cancer, nuclear factor kappa B (NF-kappa B) signaling, proteoglycans in cancer pathways might support the results of the cytotoxic assays. These results showed that the tested Caesalpinia species, showing potent inhibitory action against butyrylcholinesterase, might represent novel phytotherapeutic avenues for the management of Alzheimer's disease.
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http://dx.doi.org/10.1016/j.jpba.2021.114018DOI Listing
May 2021

Conditioning Regimens for Relapsed/Refractory Lymphoma Patients Undergoing Autologous Stem Cell Transplantation: BEAM Versus High Dose ICE.

Indian J Hematol Blood Transfus 2021 Jan 8;37(1):82-89. Epub 2020 Jul 8.

Department of Hematology and Bone Marrow Transplantation, Ankara City Hospital, Universiteler Avenue Bilkent Street. No:1, 06800 Çankaya, Ankara, Turkey.

There are different drug combinations and conditioning regimens in lymphoma transplants. However, no randomized data is available to demonstrate the superiority of any regimen and the optimal choice is unknown. In this analysis, we compared the efficacy, toxicity and the survival outcomes of the BEAM and the high dose ICE (hdICE) conditioning regimens in relapsed NHL and relapsed/refractory Hodgkin Lymphoma patients undergoing auto-SCT. 83 patients with relapsed/refractory HL or relapsed NHL who were treated with Auto-SCT between 2006 and 2016, were analyzed retrospectively. 52 patients (62.7%) received BEAM, while 31 patients (37.3%) received hdICE. Between two groups there is no significant difference in age, gender, diagnosis, disease stage, chemosensitivity, ECOG performance status, time from diagnosis to transplant, salvage regimens and previous lines of chemotherapy. After a median of 59-month follow-up, PFS and OS rates of both groups were similar (5-year PFS was 51.6% in BEAM group, 48.8% in hdICE group,  = 0.71; 5-year OS was 58% in BEAM group, 54.8% in hdICE group,  = 0.93). The median neutrophil (11 vs. 10 days,  = 0.06) and platelet engraftment (13 vs. 11 days,  = 0.01) was faster and demand of transfusions were lesser in hdICE group ( = 0.03). However, severe renal toxicity was significantly higher in hdICE group in our study ( = 0.01). hdICE conditioning regimen may be used as an alternative to BEAM, with similar survival outcomes and toxicity profile, especially transplant centers that experience some difficulties in the availability of the carmustine.
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http://dx.doi.org/10.1007/s12288-020-01317-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7900376PMC
January 2021

Phytochemical Investigations and In Vitro Bioactivity Screening on Melia azedarach L. Leaves Extract from Nepal.

Chem Biodivers 2021 Mar 8. Epub 2021 Mar 8.

Central Department of Botany, Tribhuvan University, 44613, Kirtipur, Kathmandu, Nepal.

Melia azedarach is a common tree used in the traditional medicine of Nepal. In this work, leaves were considered as source of bioactive constituents and composition of methanol extract was evaluated and compared with starting plant material. Flavonoid glycosides and limonoids were identified and quantified by HPLC-DAD-MS approaches in dried leaves and methanolic extract, while HPLC-APCI-MS and GC/MS analysis were used to study phytosterol and lipid compositions. β-Sitosterol and rutin were the most abundant constituents. HPLC-APCI-MS and HPLC-DAD-MS analysis revealed high levels of phytosterols and flavonoids in methanolic extract accounting 9.6 and 7.5 % on the dried weight, respectively. On the other hand, HPLC/MS data revealed that limonoid constituents were in minor amount in the extract <0.1 %, compared with leaves (0.7 %) indicating that degradation occurred during extraction or concentration procedures. The methanol extract was subjected to different bioassays, and antioxidant activity was evaluated. Limited inhibitory activity on acetyl and butyryl cholinesterase, as well as on amylase were detected. Moreover, tyrosinase inhibition was significant resulting in 131.57±0.51 mg kojic acid equivalents/g of dried methanol extract, suggesting possible use of this M. azedarach extract in skin hyperpigmentation conditions. Moderate cytotoxic activity, with IC of 26.4 μg/mL was observed against human ovarian cancer cell lines (2008 cells). Our findings indicate that the Nepalese M. azedarach leaves can be considered as valuable starting material for the extraction of phenolics and phytosterols, yielding extracts with possible cosmetic and pharmaceutical applications.
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http://dx.doi.org/10.1002/cbdv.202001070DOI Listing
March 2021

Chemical and Bioinformatics Analyses of the Anti-Leishmanial and Anti-Oxidant Activities of Hemp Essential Oil.

Biomolecules 2021 Feb 12;11(2). Epub 2021 Feb 12.

Department of Pharmacy, University of Lahore, Islamabad Campus, Islamabad 54590, Pakistan.

Industrial hemp is a multiuse crop that has been widely cultivated to produce fibers and nutrients. The capability of the essential oil (EO) from inflorescences as antimicrobial agent has been reported. However, literature data are still lacking about the hemp EO antiprotozoal efficacy in vivo. The present study aims to unravel this concern through the evaluation of the efficacy of hemp EOs (2.5 mL/kg, intraperitoneally) of three different cultivars, namely , and , in mice intraperitoneally infected with . A detailed description of EO composition and targets-components analysis is reported. Myrcene, α-pinene and -caryophyllene were the main components of the EOs, as indicated by the gas-chromatographic analysis. However, a prominent position in the scenario of the theoretical interactions underlying the bio-pharmacological activity was also occupied by selina-3,7(11)-diene, which displayed affinities in the micromolar range (5.4-28.9) towards proliferator-activated receptor α, cannabinoid CB2 receptor and acetylcholinesterase. The content of this compound was higher in and , in accordance with their higher scavenging/reducing properties and efficacy against the tissue wound, induced by . Overall, the present study recommends hemp female inflorescences, as sources of biomolecules with potential pharmacological applications, especially towards infective diseases.
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http://dx.doi.org/10.3390/biom11020272DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7917915PMC
February 2021

Pharmacological Potential and Chemical Characterization of Benth.-A Native Tropical African Medicinal Plant.

Antibiotics (Basel) 2021 Feb 23;10(2). Epub 2021 Feb 23.

Department of Life Sciences and Biotechnology (SVeB), UR7 Terra&Acqua Tech, University of Ferrara, 44121 Ferrara, Italy.

To avail the possible pharmacological actions of Benth., the present investigation was designed to quantitatively analyze the total flavonoid and phenolic contents and assess the various antioxidant and enzyme inhibition properties of leaf and stem bark extracts (ethyl acetate, water and methanolic) of Anti-proliferative effect was also investigated against human colon cancer cells (HCT116) as well as the antimicrobial potential against multiple bacterial and fungal (yeasts and dermatophytes) strains. The methanolic and water extracts of the stem bark demonstrated the highest phenolic content (193.58 ± 0.98 and 187.84 ± 1.88 mg/g, respectively), while the leaf extracts showed comparatively higher flavonoid contents (24.37-42.31 mg/g). Overall, the methanolic extracts were found to possess the most significant antioxidant potency. Compared to the other extracts, methanolic extracts of the were revealed to be most potent inhibitors of acetyl- and butyryl-cholinesterases, tyrosinase -amylase, except -glucosidase. Only the ethyl acetate extracts were found to inhibit glucosidase. Additionally, the stem bark methanolic extract also showed potent inhibitory activity against and gram-positive bacteria (MIC (minimum inhibitory concentration): 2.48-62.99 µg/mL), as well as all the tested fungi (MIC: 4.96-62.99 µg/mL). In conclusion, can be regarded as a promising source of bioactive compounds displaying multifunctional pharmacological activities and thus is a potential candidate for further investigations in the endeavor to develop botanical formulations for pharmaceutical and cosmeceutical industries.
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http://dx.doi.org/10.3390/antibiotics10020223DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7926895PMC
February 2021

A comprehensive evaluation of the chemical profiles and biological properties of six geophytes from Turkey: Sources of bioactive compounds for novel nutraceuticals.

Food Res Int 2021 Feb 25;140:110068. Epub 2020 Dec 25.

Department of Pharmaceutical Sciences, Section of Food Science and Nutrition, University of Perugia, via San Costanzo 1, 06126 Perugia, Italy. Electronic address:

Geophytes are gaining interest as sources of natural ingredients in nutraceutical and pharmaceutical area. In this sense, six bulbous plant species from Turkey are investigated, namely Hyacinthella campanulata K.Perss. & Wendelbo, Muscari neglectum Guss. ex Ten., Tulipa humilis herb., Iris stenophylla Hausskn. ex Baker, Galanthus elwesii Hook. f. and Crocus danfordiae Maw. with the aim to highlight their chemical compositions and biological properties. Polyphenolic profiles of the different plant parts (flower, bulb and leaf) of the six genotypes were evaluated using colorimetric methods as well LC-MS/MS. The antioxidant properties and enzymes inhibitory potential (α-amylase, α-glucosidase, tyrosinase and cholinesterases) of the extracts were determined. Overall, highest total phenolic content and total flavonoid content were observed in the leaf extracts of the studied species, except for M. neglectum (flower extract) and T. humilis (flower extract). LC-MS/MS analysis revealed the abundance of some phenolic compounds including quinic acid, hesperidin and chlorogenic acid in selective extracts. The extracts showed significant antioxidant potentials, with leaf extract of the I. stenophylla being more potent, which is linked to its high phenolic contents. All the extracts displayed notable anti-acetylcholinesterase (1.77 - 2.53 mg GALAE/g) and tyrosinase (54.9-67.20 mg KAE/g). Selective extracts have showed activity against butyrylcholinesterase, with bulb extract of M. neglectum (2.99 mg GALAE/g), I. stenophylla (2.53 mg GALAE/g) and G. elwesii (2.52 mg GALAE/g) showing highest activity. Modest activity was observed against α-amylase and α-glucosidase. The experimental data gathered herein is the first report on the phytochemical and biological attributes of these bulbous plant species which project them as potential sources of biologically active compounds for phytomedicines and nutraceuticals development.
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http://dx.doi.org/10.1016/j.foodres.2020.110068DOI Listing
February 2021

Clinical and molecular findings in children and young adults with persistent low alkaline phosphatase concentrations.

Ann Clin Biochem 2021 Mar 18:45632211000102. Epub 2021 Mar 18.

Subdivision of Pediatric Genetics, Department of Pediatrics, Faculty of Medicine, Ege University, Izmir, Turkey.

Background: Hypophosphatasia is a rare inherited metabolic disease resulted by gene mutations. It is characterized by defective bone and teeth mineralization. The phenotypic spectrum is highly variable ranging from lethal perinatal form to mild forms which are only diagnosed in adulthood or remain undiagnosed despite persistently low concentrations of ALP. The aim of this study is to evaluate the clinical phenotype and frequency of mutations in a group of patient with hypophosphatasaemia.

Methods: Thirty individuals with alkaline phosphatase values below 40 IU/L in at least two assessments and having no alternative explanation for their low ALP concentrations were included in the study. The clinical features and radiological data of the study group were re-investigated for hypophosphatasia-related findings. sequence analysis was performed using Sanger sequencing.

Results: No patient in the study group had severe symptoms, nor had they initially been diagnosed as having hypophosphatasia. Four different heterozygous mutations (c.542C>T, c.648 + 1G>A, c.657G>T and c.862 + 1G>C) were found in four patients. One splice site mutation (c.862 + 1G>C) was reported for the first time in this study.

Conclusion: sequence analysis may help to diagnosing genetic defects in individuals with persistently low ALP concentrations and provide to take preventive measures before symptoms appear. As in the other populations, HPP displays allelic heterogeneity in our population.
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http://dx.doi.org/10.1177/00045632211000102DOI Listing
March 2021

Phytochemical profile, enzyme inhibition activity and molecular docking analysis of O. Berg.

J Enzyme Inhib Med Chem 2021 Dec;36(1):618-626

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

leaves and fruits have been investigated as a source of diverse bioactive metabolites. Extract and eight metabolites isolated from leaves were evaluated for their enzymatic inhibitory activity against α-glucosidase, amylase, tyrosinase, acetylcholinestrerase and butyrylcholinesterase both and . leaves' extract showed strong antioxidant activity and variable levels of inhibitions against target enzymes with a strong anti-tyrosinase activity (115.85 mg Kojic acid equivalent/g). Additionally, α-tocopherol emerged as a potent inhibitor of AChE and BChE (5.40 & 10.38 mmol galantamine equivalent/g, respectively). Which was further investigated through molecular docking and found to develop key enzymatic interactions in AChE and BChE active sites. Also, primetin showed good anti BChE (11.70 mmol galantamine equivalent/g) and anti-tyrosinase inhibition (90.06 mmol Kojic acid equivalent/g) which was also investigated by molecular docking studies. Highlights Isolation of eight bioactive constituents from leaves. assays using different enzymatic drug targets were investigated. study was performed to define compound interactions with target proteins. leaf is an excellent source of anti-AChE and antityrosinase bioactives.
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http://dx.doi.org/10.1080/14756366.2021.1880397DOI Listing
December 2021

Deeper Insights on (Schumach. & Thonn.) Müll.Arg Extracts: Chemical Profiles, Biological Abilities, Network Analysis and Molecular Docking.

Biomolecules 2021 Feb 4;11(2). Epub 2021 Feb 4.

Physiology and Biochemistry Research Laboratory, Department of Biology, Science Faculty, Selcuk University, Konya 42130, Turkey.

(Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38-213.12 mg GAE/g and TFC: 9.66-57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents.
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http://dx.doi.org/10.3390/biom11020219DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7913913PMC
February 2021

Phytochemical Profile and Biological Activities of Crude and Purified Extracts.

Plants (Basel) 2021 Jan 21;10(2). Epub 2021 Jan 21.

School of Pharmacy, University of Camerino, via Sant'Agostino 1, I-62032 Camerino, Italy.

L. (Lamiaceae) is a perennial herb distributed in Asia and Southeastern Europe and has been used in traditional medicine since antiquity for its role against cardiac and gynecological disorders. The polar extracts obtained from aerial parts contain several compounds among which alkaloids, iridoids, labdane diterpenes, and phenylethanoid glycosides play a major role in conferring protection against the aforementioned diseases. On the other hand, the antioxidant activities and the enzyme inhibitory properties of these extracts have not yet been deeply studied. On the above, in the present study, crude and purified extracts were prepared from the aerial parts of and have been chemically characterized by spectrophotometric assays and HPLC-DAD-MS analyses. Notably, the content of twelve secondary metabolites, namely phenolic acids (chlorogenic, caffeic, caffeoylmalic and -ferulic acids), flavonoids (rutin and quercetin), phenylethanoid glycosides (verbascoside and lavandulifolioside), guanidine pseudoalkaloids (leonurine), iridoids (harpagide), diterpenes (forskolin), and triterpenes (ursolic acid), has been determined. Furthermore, the extracts were tested for their antioxidant capabilities (phosphomolybdenum, DPPH, ABTS, FRAP, CUPRAC, and ferrous chelating assays) and enzyme inhibitory properties against cholinesterase, tyrosinase, amylase, and glucosidase. The purified extracts contained higher phytochemical content than the crude ones, with caffeoylmalic acid and verbascoside as the most abundant compounds. A linear correlation between total phenolics, radical scavenging activity, and reducing power of extracts has been found. Notably, quercetin, caffeic acid, lavandulifolioside, verbascoside, chlorogenic acid, rutin, and ursolic acid influenced the main variations in the bioactivities found in extracts. Our findings provide further insights into the chemico-biological traits of and a scientific basis for the development of nutraceuticals and food supplements.
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http://dx.doi.org/10.3390/plants10020195DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7911824PMC
January 2021

Metabolomic Profile and Antioxidant/Anti-Inflammatory Effects of Industrial Hemp Water Extract in Fibroblasts, Keratinocytes and Isolated Mouse Skin Specimens.

Antioxidants (Basel) 2021 Jan 1;10(1). Epub 2021 Jan 1.

Department of Pharmacy, Università Degli Studi "Gabriele d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.

Industrial hemp is a multiuse crop whose phytocomplex includes terpenophenolics and flavonoids. In the present study, the phenolic and terpenophenolic compounds were assayed in the water extract of the hemp variety Futura 75. Protective effects were also investigated in human fibroblast and keratinocytes and isolate mouse skin specimens, which were exposed to hydrogen peroxide and/or to the extract (1-500 µg/mL). The results of phytochemical analysis suggested the cannabidiol, cannabidiolic acid and rutin as the prominent phytocompounds. In the in vitro system represented by human keratinocytes and fibroblasts, the hemp extract was found to be able to protect cells from cytotoxicity and apoptosis induced by oxidative stress. Moreover, modulatory effects on IL-6, a key mediator in skin proliferation, were found. In isolated rat skin, the extract reduced hydrogen peroxide-induced l-dopa turnover, prostaglandin-E2 production and the ratio kynurenine/tryptpophan, thus corroborating anti-inflammatory/antioxidant effects. The in silico docking studies also highlighted the putative interactions between cannabidiol, cannabidiolic acid and rutin with tyrosinase and indoleamine-2,3-dioxygenase, involved in l-dopa turnover and tryptophan conversion in kynurenine, respectively. In conclusion, the present findings showed the efficacy of hemp water extract as a skin protective agent. This could be partly related to the extract content in cannabidiol, cannabidiolic acid and rutin.
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http://dx.doi.org/10.3390/antiox10010044DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7823476PMC
January 2021

Anti-Inflammatory and Neuromodulatory Effects Induced by Water Extract: Results from In Silico, In Vitro and Ex Vivo Studies.

Molecules 2020 Dec 23;26(1). Epub 2020 Dec 23.

Department of Pharmacy, Università degli Studi "Gabriele d'Annunzio", via dei Vestini 31, 66100 Chieti, Italy.

(feverfew) has traditionally been employed as a phytotherapeutic remedy in the treatment of migraine. In this study, a commercial water extract was investigated to explore its anti-inflammatory and neuromodulatory effects. Isolated mouse cortexes were exposed to a K 60 mM Krebs-Ringer buffer and treated with water extract. The prostaglandin E (PGE) level, brain-derived neurotrophic factor (BDNF), interleukin-10 (IL-10), and IL-1β gene expression were evaluated in the cortex. The effects on dopamine (DA) release and dopamine transporter (DAT) gene expression were assayed in hypothalamic HypoE22 cells. A bioinformatics analysis was conducted to further investigate the mechanism of action. The extract was effective in reducing cortex PGE release and IL-1β gene expression. In the same experimental system, IL-10 and BDNF gene expressions increased, and in HypoE22 cells, the extract decreased the extracellular dopamine level and increased the DAT gene expression due to the direct interaction of parthenolide with the DAT. Overall, the present findings highlight the efficacy of water extract in controlling the inflammatory pathways that occur during cortical-spreading depression. Additionally, the inhibition of the hypothalamic DA release observed in this study further supports the role of dopaminergic pathways as key targets for novel pharmacological approaches in the management of migraine attacks.
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http://dx.doi.org/10.3390/molecules26010022DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7793142PMC
December 2020

The Follow-Up of Biomarkers Better Predicts the Poor Outcome in COVID-19 Patients.

Ann Clin Lab Sci 2020 Nov;50(6):848-851

Department of Chest Diseases, Ege University Faculty of Medicine.

Objective: To investigate the course of biomarkers on admission and follow-up in order to identify early predictors for poor outcome in COVID-19 patients.

Methods: In this study, 132 COVID-19 patients were classified as good outcome (n=62) and poor outcome (n=70) groups. Laboratory parameters were evaluated on admission and within 5-7 days after hospitalization.

Results: Baseline levels of neutrophil-lymphocyte ratio, CRP, procalcitonin, ferritin, D-dimer and LDH were higher (<0.01); lymphocyte count was lower in the poor outcome patients. During follow-up there was a larger decrease in lymphocyte count and more prominent increases in other biomarkers (<0.001). In ROC analysis, the AUCs strongly indicated the poor outcome on days 5-7 of the hospitalization.

Conclusions: This study suggests that the follow-up measurements of the biomarkers better predict the poor outcome in COVID-19 pneumonia.
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November 2020

Chemical characterization, antioxidant and enzyme inhibitory effects of Mitracarpus hirtus extracts.

J Pharm Biomed Anal 2021 Feb 26;194:113799. Epub 2020 Nov 26.

Department of Biology, Science Faculty, Selcuk University, Campus, Konya, Turkey. Electronic address:

Mitracarpus hirtus (L.) DC. (Family: Rubiaceae) is a tropical annual herb commonly found in America and Mexico. In the present study, the methanol, ethyl acetate, dichloromethane and aqueous extracts of the plant were tested for total phenolic (TPC) and flavonoid content (TFC) and antioxidant activities were evaluated using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. The phytochemical profile was obtained using liquid chromatography-diode array detection-electrospray ionization-mass spectrometry (LC-DAD-ESI-MS), liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry (LC-APCI-MS) and nuclear magnetic resonance (NMR) experiments. Results showed that the dichloromethane and ethyl acetate extracts yielded the highest TPC (29.10 ± 0.07 mg gallic acid equivalent/g) and TFC (38.14 ± 0.91 mg rutin equivalent/g), respectively. Aqueous extract showed weak activity against tested enzymes but demonstrated the strongest ABTS scavenging activity (59.39 ± 1.19 mg trolox equivalent/g) and is the strongest Fe reducer (59.42 ± 0.59 mg trolox equivalent/g). Phytochemical analysis revealed the presence of phenolics, pyrrolizidine alkaloids and triterpene acid. This is the first report gathering scientific data on antioxidant, enzyme inhibitory activities and phytochemical composition of M. hirtus and the obtained results can be used as starting point for further investigation on this traditional medicinal herb.
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http://dx.doi.org/10.1016/j.jpba.2020.113799DOI Listing
February 2021

Chromatographic Separation of (Dennst.) Alston Bark, Fruit and Leaf Constituents from Bioactive Extracts.

Molecules 2020 Nov 25;25(23). Epub 2020 Nov 25.

Department of Biology, Science Faculty, Selcuk University, 42130 Konya, Turkey.

(Dennst.) Alston (also known as Cup Saucer plant) is a food plant with wide applications in traditional medicine, particularly in Ayurveda. Extracts obtained with four solvents (dichloromethane, methanol, ethyl acetate and water), from three plant parts, (fruit, leaf and bark) were obtained. Extracts were tested for total phenolic, flavonoid content and antioxidant activities using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. Results showed that the methanolic bark extract exhibited significant radical scavenging activity (DPPH: 202.09 ± 0.15; ABTS: 490.12 ± 0.18 mg Trolox equivalent (TE)/g), reducing potential (FRAP: 325.86 ± 4.36: CUPRAC: 661.82 ± 0.40 mg TE/g) and possessed the highest TAC (3.33 ± 0.13 mmol TE/g). The methanolic extracts were subjected to LC-DAD-MS and NMR analysis. A two-column LC method was developed to separate constituents, allowing to identify and quantify forty-four and fifteen constituents in bark and fruits, respectively. Main compound in bark was epicatechin-3--sulphate and isolation of compound was performed to confirm its identity. Bark extract contained catechins, procyanidins, gallic acid derivatives and the sulfur containing spiroketal named breynins. Aerial parts mostly contained flavonoid glycosides. Considering the bioassays, the methanolic bark extract resulted a potent tyrosinase (152.79 ± 0.27 mg kojic acid equivalent/g), α-amylase (0.99 ± 0.01 mmol acarbose equivalent ACAE/g) and α-glucosidase (2.16 ± 0.01 mmol ACAE/g) inhibitor. In conclusion, methanol is able to extract the efficiently the phytoconstituents of and the bark is the most valuable source of compounds.
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http://dx.doi.org/10.3390/molecules25235537DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7728322PMC
November 2020

Comprehensive bioactivity and chemical characterization of the endemic plant Scorzonera hieraciifolia Hayek extracts: A promising source of bioactive compounds.

Food Res Int 2020 11 3;137:109371. Epub 2020 Jun 3.

Department of Health Sciences, Faculty of Science, University of Mauritius, 230 Réduit, Mauritius.

Members of Scorzonera genus are known for their potential application in both food and pharmaceutical industries. The present study reports the chemical component and bioactivity of the dichloromethane, ethyl acetate, hexane, methanol and infused extracts of Scorzonera hieraciifolia Hayek aerial parts and roots. The methanolic extracts of both aerial parts and roots were good sources of total phenolic and flavonoid content. For the aerial parts, the infused and methanolic extracts showed highest (p < 0.05) free radical scavenging (2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS)), reducing (cupric reducing antioxidant capacity (CUPRAC))and ferric reducing antioxidant power (FRAP)) and metal chelating capacities. Whilst, for the root extracts, overall most remarkable free scavenging and reducing activity was observed for the methanolic extracts (p < 0.05) while the hexane extracts showed highest metal chelating activity. The inhibitory activity of the extracts was evaluated against key enzymes. Overall, the hexane extracts of both aerial parts (acetylcholinesterase (AChE): 2.27 ± 0.04 and butyrlcholinesterase (BChE): 5.75 ± 0.48 mg galantamine equivalent (GALAE)/g) and roots (AChE: 2.44 ± 0.35 and BChE: 53.17 ± 0.22 mg GALAE/g) were most potent against AChE and BChE, suggesting a role for the more lipophilic compounds in this regard. The highest inhibitory activity against tyrosinase was displayed by methanolic extracts of aerial parts (64.70 ± 0.26 mg kojic acid equivalent (KAE)/g) and roots (63.63 ± 0.20 mg KAE/g). Modest activity was observed against α-amylase and α-glucosidase, two major enzymes implicated in the pathology of diabetes. Liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) analysis showed the presence of 40 compounds such as caffeic, ursolic, betulinic and oleanolic acid and their derivatives in the studied extracts. Multivariate analysis showed that the biological activities were dependent on the plant parts used as well as on the type of solvent used. Overall, the results showed that S. hieraciifolia is a valuable source of phytochemicals for both the nutraceutical and pharmaceutical sectors.
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http://dx.doi.org/10.1016/j.foodres.2020.109371DOI Listing
November 2020

Screening of Bioactive Metabolites and Biological Activities of Calli, Shoots, and Seedlings of (L.) Gray.

Plants (Basel) 2020 Nov 12;9(11). Epub 2020 Nov 12.

Department of Bioresources and Food Science, Institute of Natural Science and Agriculture, Konkuk University, Seoul 05029, Korea.

(L.) Gray is threatened with extinction owing to climate change, poor seed germination, and ocean warming. In vitro explant-culture is used for ex situ preservation and plantlet massive production. In vitro cell and organ cultures serve as an alternative plant material source to investigate the biological activities and phytochemical profiles of rare plants. We aimed to develop an efficient callus and shoot production protocol and investigate bioactive metabolites, antioxidants, and enzyme inhibitory potential of calli, shoots, and in vivo seedlings. The effects of combinations of different plant growth regulators, 6-BA (N-benzyladenine), 6-KN (Kinetin), TDZ (Thidiazuron), and NAA (1-Naphthylacetic acid), in MS (Murashige and Skoog) nutrient medium were studied. The highest callus proliferation was obtained after 5-week cultivation over a 16-h photoperiod on growth medium MS enriched with 4 µM each of 6-BA and NAA. The medium with 2 µM 6-BA and 4 µM 6-KN had the best shoot induction rate (91.1%) with a mean of 13.4 shoots. The combination of two cytokinins (6-BA and 6-KN) was found to be effective in shoot regeneration. The rooting frequency was 100% in ½ MS with Indole-3-butyric acid (IBA 2 µM). The number of detected compounds and chemical composition in the shoots and seedlings extracts were similar. The total amount of phenolics in the shoots was 216.4% and 369.5% higher than in seedlings and calli, respectively. The total amount of flavonoids in the shoots was 241.1% and 429.3% higher than in seedlings and calli, respectively. The best antioxidant activity was obtained in the shoots, followed by seedlings and calli. However, the order was seedlings > calli > shoots regarding metal chelating ability. The strongest acetylcholinesterase inhibition properties were obtained in the calli, followed by seedlings and shoots. However, the tested samples can be ranked as seedlings > shoots > calli in butylcholinestrase inhibition assay. This study is the first report on the enzyme inhibitory effects of extracts, providing valuable contributions to the scientific community.
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http://dx.doi.org/10.3390/plants9111551DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7697918PMC
November 2020

Phenolic Content and Antimicrobial and Anti-Inflammatory Effects of , , , , and Extracts.

Antibiotics (Basel) 2020 Nov 6;9(11). Epub 2020 Nov 6.

Department of Pharmacy, Università degli Studi "Gabriele d'Annunzio", via dei Vestini 31, 66100 Chieti, Italy.

Prostatitis is an inflammatory condition that is related to multiple infectious agents, including bacteria and fungi. Traditional herbal extracts proved efficacious in controlling clinical symptoms associated with prostatitis. In this context, the aim of the present study was to explore the efficacy of extracts from , , , and against bacterial () and fungi strains () involved in prostatitis. Additionally, anti-mycotic effects were tested against multiple species of dermatophytes (, and ). Antioxidant effects were also evaluated in isolated rat prostates challenged with lipopolysaccharide (LPS), and phytochemical analyses were conducted to identify and quantify selected phenolic compounds, in the extracts. Finally, a bioinformatics analysis was conducted to predict putative human and microbial enzymes targeted by extracts' phytocompounds and underlying the observed bio-pharmacological effects. The phytochemical analysis highlighted that rutin levels could be crucial for explaining the highest antibacterial activity of extract, especially against and . On the other hand, in the extract, catechin concentration could partially explain the highest efficacy of this extract in reducing lipid peroxidation, in isolated rat prostates stimulated with LPS. Concluding, the results of the present study showed moderate antimicrobial and anti-inflammatory effects induced by water extracts of , and that could be related, at least partially, to the phenolic composition of the phytocomplex.
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http://dx.doi.org/10.3390/antibiotics9110783DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7694769PMC
November 2020

HPLC-FRAP methodology and biological activities of different stem bark extracts of Cajanus cajan (L.) Millsp.

J Pharm Biomed Anal 2021 Jan 12;192:113678. Epub 2020 Oct 12.

Department of Biology, Science Faculty, Selcuk University, Campus, Konya, Turkey. Electronic address:

Cajanus cajan. (L.) Millsp. (C. cajan) (Family: Fabaceae) also known as pigeon pea, is a famous food and cover/forage crop bearing a high amount of key amino acids (methionine, lysine and tryptophan). This study investigated into the total phenolic (TPC), flavonoid content (TFC), antioxidant [2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2 -azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating] activities and enzyme [α-amylase, α-glucosidase, tyrosinase, acetyl-(AChE), butyryl-(BChE) cholinesterase] inhibitory effects of four extracts (methanol, hexane, ethyl acetate, aqueous) prepared from C. cajan stem bark. Direct identification of antioxidants was also conducted using the high performance liquid chromatography-ferric reducing antioxidant power (HPLC-FRAP) system. The highest TPC and TFC were recorded with the methanolic (23.22 ± 0.17 mg GAE/g) and ethyl acetate extracts (19.43 ± 0.24 mg RE/g), respectively. The methanolic extract exhibited important antioxidant activity with DPPH (38.41 ± 0.05 mg Trolox equivalent (TE)/g), ABTS (70.49 ± 3.62 mg TE/g), CUPRAC (81.86 ± 2.40 mg TE/g), FRAP (42.96 ± 0.59 mg TE/g) and metal chelating (17.00 ± 1.26 mg ethylenediaminetetraacetic acid equivalent/g). p-coumaric and caffeic acid were the predominant antioxidants in the samples. Results from enzymatic assays showed the potential abilities of hexane extract in inhibiting the AChE, BChE, α-amylase and α-glucosidase enzymes. From the results obtained in this study, it can be concluded that C. cajan can be considered as a promising source of antioxidants and key enzyme inhibitors that can be exploited for future bioproduct development.
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http://dx.doi.org/10.1016/j.jpba.2020.113678DOI Listing
January 2021

Phytochemical Composition, Antioxidant Capacity, and Enzyme Inhibitory Activity in Callus, Somaclonal Variant, and Normal Green Shoot Tissues of (L) G. Don.

Molecules 2020 Oct 26;25(21). Epub 2020 Oct 26.

Department of Bioresources and Food Science, Institute of Natural Science and Agriculture, Konkuk University, Seoul 05029, Korea.

This study aimed to investigate the impact of plant growth regulators, sucrose concentration, and the number of subcultures on axillary shoot multiplication, in vitro flowering, and somaclonal variation and to assess the phytochemical composition, antioxidant capacity, and enzyme inhibitory potential of in vitro-established callus, somaclonal variant, and normal green shoots of . The highest shoot induction rate (95.8%) and highest number of shoots (23.6), with a mean length of 4.5 cm, were attained when the nodal explants (0.6-1 cm in length) were cultivated in Murashige and Skoog (MS) medium with 2 µM thidiazuron, 1 µM 2-(1-naphthyl) acetic acid (NAA), and 4% sucrose. The in vitro flowering of was affected by sucrose, and the number of subcultures had a significant effect on shoot multiplication and somaclonal variation. The highest levels of phenolics and flavonoids were found in normal green shoots, followed by those in somaclonal variant shoots and callus. The phytochemicals in extracts were qualified using liquid chromatography-tandem mass spectrometry. A total of 39, 55, and 59 compounds were identified in the callus, somaclonal variant shoot, and normal green shoot tissues, respectively. The normal green shoot extracts exhibited the best free radical scavenging ability and reducing power activity. The strongest acetylcholinesterase inhibitory effects were found in the callus, with an IC50 of 0.65 mg/mL.
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http://dx.doi.org/10.3390/molecules25214945DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7663286PMC
October 2020

Network analysis, chemical characterization, antioxidant and enzyme inhibitory effects of foxglove (Digitalis cariensis Boiss. ex Jaub. & Spach): A novel raw material for pharmaceutical applications.

J Pharm Biomed Anal 2020 Nov 16;191:113614. Epub 2020 Sep 16.

Department of Pharmacy, "G. d'Annunzio University" Chieti-Pescara, Via dei Vestini n. 31, 66100 Chieti, Italy.

The present study outlines the phenolic composition and pharmacological properties of different extracts of Digitalis cariensis Boiss. ex Jaub. & Spach root and aerial parts. The metabolic profiles of the studied extracts were characterized by UHPLC-MS. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were determined. Bioinformatics and docking investigations were also conducted to support the enzyme inhibition test and predict putative targets for potential pharmacological applications. Overall, the methanolic extract followed by the water extract of the D. cariensis root were found to be superior source of antioxidant compounds except for metal chelating ability, in which the water extract of the root (26.34 ± 1.54 mg EDTAE/g) and aerial parts (16.47 ± 0.88 mg EDTAE/g) have showed the highest activity. The tested extracts were potent against AChE (9.11 ± 0.27-9.79 ± 0.28 mg GEs/g extract), α-amylase (0.12 ± 0.01- 0.50 ± 0.01 mmol ACEs/g extract) and α-glucosidase (0.28 ± 0.01-17.29 ± 0.24 mmol ACEs/ g extract). Notable activity against tyrosinase was displayed by the methanolic extracts (Root-MeOH: 123.71 ± 2.70 and aerial parts - MeOH: 137.96 ± 1.07 mg KAE/g extract), while none of the extracts were potent against BChE. According to docking investigations, the observed anti-tyrosinase effect could be related, at least partially, to the presence of luteolin, rosmarinic acid and kaempferol in the extracts. Results amassed herein is the first report on the biological attributes of D. cariensis, which validate the pharmacological uses of this plant.
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http://dx.doi.org/10.1016/j.jpba.2020.113614DOI Listing
November 2020

Antimicrobial, Antioxidant, and Antiproliferative Effects of : An Unexplored Botanical Species.

Antibiotics (Basel) 2020 Sep 17;9(9). Epub 2020 Sep 17.

Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, 66100 Chieti, Italy.

species, belonging to the genus (Fabaceae), have long been used in traditional medicine for treating cold, diabetes, pain, and as cardiotonics. The goal of the present study was to explore the phytochemical composition and pharmaco-toxicological properties of In this regard, phenolic content, scavenging/reducing properties and antimicrobial activity toward pathogen bacterial (, , , ) and fungal strains (, , and ) were investigated. Extract effects on human colon cancer HCT116 cell viability were also assayed. Finally, a bioinformatics approach was conducted with the aim to identify putative microbial and human protein targets underlying antibacterial, antimycotic, and antiproliferative effects. Phytochemical investigation suggested that water extract is richer in terms of total flavonoid and phenol content, whereas the hydroalcoholic extract was revealed to be more potent as antioxidant agent. According to bioinformatics analysis, the antibacterial activity of the hydroalcoholic extract could be related to its content in resveratrol. The presence of resveratrol could also explain the hydroalcoholic extract efficacy in reducing HCT116 cell viability. In conclusion, the present study represents the first phytochemical and bio-pharmacological investigation about . Like other plants belonging to the Fabaceae family, revealed a good source of resveratrol, which could explain, albeit partially, the efficacy of the hydroalcoholic extract as antimicrobial, antioxidant, and antiproliferative agent.
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http://dx.doi.org/10.3390/antibiotics9090611DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7560210PMC
September 2020

Identification of bioactive compounds from Rhaponticoides iconiensis extracts and their bioactivities: An endemic plant to Turkey flora.

J Pharm Biomed Anal 2020 Oct 22;190:113537. Epub 2020 Aug 22.

Department of Pharmacognosy, Faculty of Pharmacy, Medical University-Sofia, Sofia, Bulgaria.

Rhaponticoides iconiensis (Hub.-Mor.) M.V.Agab. & Greuter. (Asteraceae) is an endemic species spread in several small populations in the province of Konya (Turkey). It is critically endangered with an extremely high risk of extinction. Recently, based on the molecular phylogenetic and eco geographical studies on Cardueae-Centaureinae, the genus Rhaponticoides Vaill. was separated from Centaurea L. Antioxidant properties and enzyme inhibition, as well as the phenolic and flavonoid contents, of the methanol (Soxhlet extraction and maceration) and water (infusion) extracts of R. iconiensis leaves, roots, and flower heads were determined. The methanol extracts of R. iconiensis leaves contained the highest amount of phenolic (52.37 and 54.37 mg gallic acid equivalent/g) and flavonoids (74.13 and 80.75 mg rutin equivalent/g). Accordingly, the leaves methanol extracts showed the highest antioxidant potential. Interestingly, the roots methanol extracts were the most potent acetylcholinesterase (4.75 mg galantamine equivalent/g) and butyrylcholinesterase inhibitors (5.26 and 5.14 mg galantamine equivalent/g). The leaves and roots methanol extracts exhibited high α-glucosidase (2.48-3.08 mmol acarbose equivalent/g) and α-amylase (0.17-0.70 mmol acarbose equivalent/g) inhibition. The highest tyrosinase inhibition was recorded for leaves methanol extracts (138.79 and 140.34 mg kojic acid equivalent/g). 87 natural products (including hydroxybenzoic, hydroxycinnamic and acylquinic acids, flavones, flavonols, flavanones and anthocyanins) were unambiguously identified or tentatively annotated in the studied extracts. Findings presented in the present study appraise the bioactivity of R. iconiensis, an understudied species.
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http://dx.doi.org/10.1016/j.jpba.2020.113537DOI Listing
October 2020

The Strength of the Nutrient Solution Modulates the Functional Profile of Hydroponically Grown Lettuce in a Genotype-Dependent Manner.

Foods 2020 Aug 21;9(9). Epub 2020 Aug 21.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

Considering that functional components of plant foods are mainly secondary-metabolism products, we investigated the shaping of health-promoting compounds in hydroponically grown butterhead lettuce ( L. var. ) as a function of the strength of the nutrient solution utilized. To this aim, untargeted metabolomics profiling, in vitro antioxidant capacity (total phenolics, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), and ferric reducing antioxidant power (FRAP) assays), and the inhibition of selected enzyme activities were investigated in two butterhead lettuce cultivars with different pigmentation, i.e., green and red Salanova. Full-strength nutrition, together with half- and quarter-strength solutions of macronutrients, was tested. Our results indicate that by reducing the nutrients strength, we could elicit a distinctive shaping of the phenolic profile of lettuce. It is noteworthy that only specific classes of phenolics (namely, lignans and phenolic acids, followed by flavones and anthocyanins) were modulated by the induction of nutritional eustress (fold-change values in the range between -5 and +11). This indicates that specific responses, rather than a generalized induction of phenolic compounds, could be observed. Nonetheless, a genotype-dependent response could be observed, with the red cultivar being much more responsive to nutritional deprivation than the green Salanova lettuce. Indeed, analysis of variance (ANOVA) confirmed a genotype x nutrition interaction in red Salanova ( < 0.001). As a consequence of the changes in phenolic composition, also the antioxidant capacity ( < 0.001) and amylase inhibition ( < 0.001) properties were affected by the growing conditions. However, the effect on cholinesterase and tyrosinase inhibition was poorly affected by the nutritional strength. Provided that yields are not compromised, the application of a controlled nutritional eustress in hydroponically cultivated lettuce may represent a valuable strategy to produce food with tailored functional features in a sustainable manner.
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http://dx.doi.org/10.3390/foods9091156DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7555578PMC
August 2020

Evaluation of Antioxidant, Antimicrobial and Tyrosinase Inhibitory Activities of Extracts from an Edible Wild Mushroom.

Antibiotics (Basel) 2020 Aug 13;9(8). Epub 2020 Aug 13.

Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, 66100 Chieti, Italy.

(Bres.) Guzmán ex T.J. Baroni is an excellent edible mushroom whose compounds and biological properties are still unknown. In this study, n-hexane, ethyl acetate and methanol extracts from fruiting bodies and liquid-cultured mycelia were compared for the analysis of phenolic compounds, the evaluation of scavenger (DPPH, ABTS) and reducing (CUPRAC, FRAP) activities, and the enzyme inhibition of α-amylase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase. Additionally, extracts were evaluated for antibacterial and antimycotic activities against Gram+ and Gram- bacteria, and clinical yeast and fungal dermatophytes. Finally, based on the extract content in phenolic compounds, in silico studies, including the docking approach, were conducted to predict the putative targets (namely tyrosinase, lanosterol-14-α-demethylase, the multidrug efflux system transporters of (mdtK) and (pmpM), and β-lactamase (ORF259)) underlying the observed bio-pharmacological and microbiological effects. The methanolic extract from mycelia was the richest in gallic acid, whereas the ethyl acetate extract from fruiting bodies was the sole extract to show levels of catechin. Specifically, docking runs demonstrated an affinity of catechin towards all docked proteins, in the micromolar range. These in silico data are consistent, at least in part, with the highest activity of ethyl acetate extract as an antimicrobial and anti-tyrosinase (554.30 mg KAE/g for fruiting bodies and 412.81 mg KAE/g for mycelia) agent. The ethyl acetate extracts were also noted as being the most active (2.97 mmol ACAE/g for fruiting bodies and 2.25 mmol ACAE/g for mycelia) on α-amylase. BChE inhibitory activities varied from 2.61 to 26.78 mg GALAE/g, while the tested extracts were not active on AChE. In conclusion, all mushroom extracts tested in this study had potent antimicrobial activities. Particularly, among the tested extracts, the ethyl acetate extract showed the highest efficacy as both an antimicrobial and anti-tyrosinase agent. This could be related, albeit partially, to its content of catechin. In this regard, the bioinformatics analyses showed interactions of catechin with tyrosinase and specific microbial proteins involved in the resistance to chemotherapeutic drugs, thus suggesting innovative pharmacological applications of extracts.
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http://dx.doi.org/10.3390/antibiotics9080513DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7460263PMC
August 2020

Evaluation of the predictive role of neutrophil/lymphocyte ratio in the diagnosis of lymphoma in patients with asymptomatic and ısolated cervical lymphadenopathy.

Braz J Otorhinolaryngol 2020 Aug 1. Epub 2020 Aug 1.

Mersin City Training and Research Hospital, Department of Otorhinolaryngology, Mersin, Turkey. Electronic address:

Introduction: The diagnostic approach to patients with isolated asymptomatic cervical lymphadenopathy varies between excisional biopsy and follow-up. When the anamnesis, physical examination, laboratory and imaging findings are not sufficient to identify the etiology, an excisional biopsy is performed for the differential diagnosis between early-stage lymphoma and infectious or reactive causes. If the excisional biopsy, which may have some complications, is not performed, it may delay the diagnosis of lymphoma. This diagnostic challenge could be avoided by predictive markers.

Objectives: This study was planned to determine the predictive value of neutrophil/lymphocyte ratio in the diagnosis of Hodgkin and non-Hodgkin limphoma in patients with asymptomatic, isolated cervical limphadenopathy and underwent excisional biopsy.

Methods: A total of 90 patients between the years 2016-2019 admitted to our clinics due to asymptomatic isolated cervical lymphadenopathy, present in at least 4 weeks with lympho nodes in pathological dimensions persisting in the cervical region, were included to our study. An excisional lympho node biopsy was performed in all 90 patients.

Results: Of the 90 patients who underwent excisional biopsy; 34 were diagnosed as reactive lymphadenopathy 30 were non-Hodgkin linphoma, and 26 were Hodgkin linphoma. A total of 56 (62.2%) patients were diagnosed as lymphoma, either Hodgkin or non-Hodgkin, while 34 patients (38.8%) were diagnosed as reactive lymphadenopathy. The median age, total whiteblood count, neutrophil count of the lymphoma groups were significantly higher than reactive lymphadenopathy group, whereas the lymphocyte count was significantly lower in the lymphoma patients. The median neutrophil/ lymphocyte ratio was 1.7 in the reactive lymphadenopathy group, 3.5 in the non-Hodgkin limphoma group, and 3.0 in the Hodgkin limphoma group (p< 0.001).

Conclusion: According to the results of our study, neutrophil/lymphocyte ratio was significantly higher in patients who were admitted with isolated asymptomatic lymphadenopathy and were diagnosed with lymphoma, and who were diagnosed with early-stage Hodgkin and non- Hodgkin lymphoma compared to those who were found to have reactive lymphadenopathy. Neutrophil/lymphocyte ratio, which is a low-cost, fast and easy-to-access test, has a predictive value in the diagnosis of lymphoma in patients with asymptomatic lymphadenopathy.
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http://dx.doi.org/10.1016/j.bjorl.2020.06.012DOI Listing
August 2020

Antioxidant and enzyme-inhibitory activity of peppermint extracts and essential oils obtained by conventional and emerging extraction techniques.

Food Chem 2021 Feb 2;338:127724. Epub 2020 Aug 2.

University of Novi Sad, Faculty of Technology, Blvd. cara Lazara 1, 21000 Novi Sad, Serbia. Electronic address:

Peppermint is widely used medicinal plant with distinguished bioactive potential, therefore, the aim of present work was to develop novel peppermint extracts with high activity by application of traditional and emerging separation techniques. Conventional hydrodistillation and microwave-assisted hydrodistillation (MWHD) were applied for recovery of essential oil (EO), while organic solvent extraction using Soxhlet apparatus, microwave-assisted and ultrasound-assisted process and supercritical fluid extraction (SFE) were applied for non-selective recovery of peppermint lipophilic extracts. Extracts were characterized in terms of terpenoids profile with special emphasis on content of major compounds (mentol, menthone, isomenthol and eucalyptol). Antioxidant activity (DPPH, ABTS, CUPRAC, FRAP, chelating and phosphomolybdenum assay) and enzyme-inhibitory assays (acetylcholinesterase, butyrylcholinesterase, tyrosinase, amylase and glucosidase inhibition) were used for screening of peppermint bioactivity. MWHD was recognized as alternative for traditional process in EO recovery, while SFE extracts were useful for green production of solvent-free peppermint extracts rich in terpenoids and other lipophilic bioactives.
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http://dx.doi.org/10.1016/j.foodchem.2020.127724DOI Listing
February 2021

Classical Hodgkin lymphoma-like post-transplant lymphoproliferative disease after allogeneic stem cell transplantation for primary myelofibrosis is successfully treated with nivolumab: A case report.

J Oncol Pharm Pract 2021 Mar 6;27(2):509-512. Epub 2020 Aug 6.

Department of Hematology, Gaziantep University School of Medicine, Gaziantep, Turkey.

Introduction: Post-transplant lymphoproliferative disease (PTLD), a lymphoid proliferation observed after the solid organ transplantation or allogeneic stem cell transplant, is an important and mortal complication that can occur during the post-transplant period. Classical Hodgkin lymphoma-like PTLD is the least form of PTLD. We are presenting an adult case of classical Hodgkin lymphoma-like PTLD which was successfully treated with nivolumab.

Case Report: A 31-year-old female was diagnosed with primary myelofibrosis and we performed allogeneic stem cell transplantation from her HLA fully matched brother in 2015. Two years after transplant, classical Hodgkin lymphoma-like PTLD was diagnosed. The patient was resistant to six cycles of ABVD chemotherapy and four cycles of brentuximab vedotin.

Management And Outcome: After the failure of ABVD and brentuximab vedotin, we started nivolumab therapy at a dose of 3 mg/kg every 2 weeks. After six cycles, we achieved a PET negative complete remission. After 10 cycles of nivolumab, the patient is still followed with a complete remission. Still, there is no evidence of acute or chronic GvHD, and therefore no need for immunosuppressive treatment. No auto-immune complication was observed. It is planned to give nivolumab treatment to the patient until the progression.

Discussion: Our case has depicted that the classical Hodgkin lymphoma type PTLD may be resistant to the conventional treatments and anti-CD30 brentuximab vedotine. In such cases, nivolumab may be an effective and worth assessing agent in terms of both activity and safety profile.
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http://dx.doi.org/10.1177/1078155220946462DOI Listing
March 2021