Publications by authors named "Gokhan Zengin"

266 Publications

Comparative Investigation of Composition, Antifungal, and Anti-Inflammatory Effects of the Essential Oil from Three Industrial Hemp Varieties from Italian Cultivation.

Antibiotics (Basel) 2021 Mar 22;10(3). Epub 2021 Mar 22.

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

Industrial hemp is characterized by a huge amount of by-products, such as inflorescences, that may represent high-quality sources of biomolecules with pharmaceutical interest. In the present study, we have evaluated the phytochemical profile, including terpene and terpenophenolic compounds, of the essential oils (EOs) of , and hemp varieties. The EOs were also tested for antifungal properties toward and . In parallel, we investigated the inhibitory effects of the EOs against tyrosinase, and the production of prostaglandin E in isolated mouse skin exposed to hydrogen peroxide. In human H1299 lung adenocarcinoma cells, we also evaluated the influence of the EOs on the gene expression of angiotensin-converting enzyme 2 (ACE2) and transmembrane protease serine 2 (TMPRSS2), which are involved in SARS-CoV-2 entry in human host. -caryophyllene and α-pinene were the prominent terpenes in the EOs, whereas the cannabidiolic acid was the terpenophenol present at higher concentration. The EOs inhibited the growth of all tested dermatophytes species. In isolated skin specimens, EOs prevented the hydrogen-peroxide-induced synthesis of prostaglandin E, consistent with the intrinsic antityrosinase activity. Finally, in H1299 cells, all tested EOs reduced the gene expression of ACE-2 and TMPRSS2, as well. Therefore, the present findings highlight the rationale for the use of the present EOs against infectious diseases.
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http://dx.doi.org/10.3390/antibiotics10030334DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8005080PMC
March 2021

Health Potential of Clery Strawberries: Enzymatic Inhibition and Anti- Activity Evaluation.

Molecules 2021 Mar 19;26(6). Epub 2021 Mar 19.

Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma "La Sapienza", Piazzale Aldo Moro 5, 00185 Roma, Italy.

Strawberries, belonging to cultivar Clery ( × Duchesne ex Weston) and to a graft obtained by crossing Clery and L., were chosen for a study on their health potential, with regard to the prevention of chronic and degenerative diseases. Selected samples, coming from fresh and defrosted berries, submitted to different homogenization techniques combined with thermal and microwave treatments, had been previously analyzed in their polyphenolic content and antioxidant capacity. In the present work, these homogenates were evaluated in relation to their enzymatic inhibition activity towards acetylcholinesterase and butyrylcholinesterase, α-amylase, α-glucosidase and tyrosinase. All these enzymes, involved in the onset of diabetes, and neurodegenerative and other chronic diseases, were modulated by the tested samples. The inhibitory effect on tyrosinase and cholinesterase was the most valuable. Antifungal activity against , recently shown to play a crucial role in human gut diseases as well as diabetes, rheumatoid arthritis and Alzheimer's disease, was also shown in vitro and confirmed by the in vivo text on . Overall, the obtained results confirm once again the health potential of strawberries; however, the efficacy is dependent on high quality products submitted to correct processing flow charts.
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http://dx.doi.org/10.3390/molecules26061731DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003815PMC
March 2021

Exploring the Genetic Conception of Obesity via the Dual Role of FoxO.

Int J Mol Sci 2021 Mar 20;22(6). Epub 2021 Mar 20.

Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 410028 Oradea, Romania.

Obesity or overweight are not superficial problems, constituting a pressing issue. The obesity index has almost tripled since 1975, which is an alarming state. Most of the individuals are currently becoming overweight or have inappropriate body mass index (BMI) conditions. Obesity is characterized by increased fat accumulation and thus poses a higher health risk. There is increased size and volume of fat cells in the body, which usually accounts for obesity. Many investigations have been carried out in this area, such as behavioral improvements, dietary changes, chemical involvements, etc., but presently no such goals are established to manage these health concerns. Based on previous literature reports and our interpretation, the current review indicates the involvement of various transcriptional and transporter functions in modifying the above-mentioned health conditions. Various transcriptional factors such as Forkhead box O1 (FoxO1) impart a significant effect on the physiology and pathology of metabolic dysfunction such as obesity. FoxO1 plays a dual role whether in the progression or suppression of metabolic processes depending on its targets. Thus, in the current study, will be discussed the dual role of FoxO1 in metabolic conditions (such as obesity), also summarizing the role of various other transcriptional factors involved in obesity.
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http://dx.doi.org/10.3390/ijms22063179DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003860PMC
March 2021

Evaluation of Antioxidant and Enzyme Inhibition Properties of L'Hér. Extracts Obtained with Different Solvents.

Molecules 2021 Mar 28;26(7). Epub 2021 Mar 28.

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

L'Hér methanol extract was studied by NMR and two different LC-DAD-MS using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol--[arabinosil(1-6) glucoside] (133 mg/g), dihydro β ionol--[arabinosil(1-6) glucoside] (80 mg/g), β-sitosterol (49 mg/g), and isorhamnetin-3--rutinoside (26 mg/g). was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest as a novel source of bioactive phytochemicals with potential for commercial development.
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http://dx.doi.org/10.3390/molecules26071902DOI Listing
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

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

Metabolomic insight into the profile, in vitro bioaccessibility and bioactive properties of polyphenols and glucosinolates from four Brassicaceae microgreens.

Food Res Int 2021 Feb 8;140:110039. Epub 2021 Jan 8.

Department for Sustainable Food Process, Università Cattolica del Sacro Cuore, Via Emilia Parmense 84, 29122 Piacenza, Italy.

In this study, four Brassicaceae microgreens species, namely kale, red cabbage, kohlrabi, and radish, were evaluated for their phytochemical compositions using spectrophotometric assays and untargeted metabolomics before and after in vitro gastrointestinal digestion. According to the in vitro spectrophotometric results, significant amounts of phenolics could be detected in each studied species, thus supporting the total antioxidant capacities recorded. Overall, metabolomics allowed annotating a total of 470 phytochemicals across the four Brassicaceae microgreens, either fresh or digested. Among polyphenols, flavonoids were the most represented class (180 compounds, including anthocyanins, flavones, flavonols, and other flavonoids), followed by phenolic acids (68 compounds, mainly hydroxycinnamic and hydroxybenzoic acids), non-flavonoid or phenolic acid-based structures (i.e., alkyl- and alkylmethoxy-phenols and tyrosol derivatives), and lignans. Also, 22 glucosinolates were annotated, including gluconapin glucoraphanin, glucobrassicin, and 4-hydroxyglucobrassicin. Noteworthy, significant differences could be observed in terms of bioaccessibility as a function of the phenolic class and the species considered. Overall, lignans exhibited the highest bioaccessibility values (14%), followed by tyrosol derivatives and flavonoids (on average, 9% and 8%, respectively). However, differences could be evidenced as a function of the species, with red cabbage having comparatively lower bioaccessibility values irrespective of the chemical class of bioactive considered. Similarly, bioaccessibility of glucosinolates significantly differed across species, ranging from 2% in kale to 43% in kohlrabi microgreens.
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http://dx.doi.org/10.1016/j.foodres.2020.110039DOI Listing
February 2021

Volatile and phenolic profiling of a traditional medicinal plant, Hypericum empetrifolium with in vitro biological activities.

J Ethnopharmacol 2021 May 15;272:113933. Epub 2021 Feb 15.

Department of Biology, Faculty of Science, Selçuk University, 42250, Konya, Turkey.

Ethnopharmacological Relevance: Hypericum empetrifolium Willd is a member of the Hypericaceae family, mainly known in southern Greece, and western Turkey. Being a centuries-old medicinal plant, the aerial parts of the plant have been used for the treatment of herpes, kidney stones, gastric ulcer, and also for their anti-helminthic, and diuretic purposes traditionally.

Aim Of The Study: The current study aimed to investigate the phytochemical profiles of the essential oil, and two ethanol extracts prepared from the aerial parts (H. empetrifolium aerial parts extract - HEA), and roots of the plant (H. empetrifolium roots extract - HER), and to provide data on antioxidant, anticholinesterase, antityrosinase, antiurease, cytotoxic, and antimicrobial activities of the extracts.

Materials And Methods: In this study, volatile and phenolic compounds of the HEA and HER were analyzed by GC-MS and LC-MS/MS, respectively. Antioxidant potential of the extracts was clarified by using DPPH radical scavenging assay, ABTS cation radical assay, and the CUPRAC assay. Acetylcholinesterase, butyrylcholinesterase, urease, and tyrosinase inhibitory activity assays were used to determine enzyme inhibition capacity of the extracts. Cytotoxic activity of the extracts was established by using XTT assay. The antimicrobial activity of the extracts was determined by the microbroth dilution technique.

Results: The major compounds of the essential oil were revealed as alloaromodendrene (24.7%), α-pinene (14.7%), β-pinene (10.7%), and α-terpineol (7.7%) by the GC-MS analysis. According to the LC-MS/MS analysis results, quinic acid was the most abundant constituent in both extracts with 20612.42 ± 169.02 μg/g extract in HEA extract, and with 2254.34 ± 18.49 μg/g extract in HER extract, respectively. The HEA extract was also found to be rich in terms of chlorogenic acid (5583.14 ± 38.52 μg/g extract), isoquercitrin (3076.77 ± 40.92 μg/g extract), and malic acid (2822.90 ± 31.90 μg/g extract). HEA extract exhibited a significant antioxidant effect with an IC value of 11.98 ± 0.22 μg/mL according to the DPPH radical scavenging assay. Similar results were obtained with the ABTS cation radical assay, and the CUPRAC assay. HER extract showed a strong butyrylcholinesterase inhibitory effect with 88.69 ± 0.62% at 200 μg/mL concentration. Both extracts were considered to have moderate anti-tyrosinase activity compared to the standard at 200 μg/mL. The best antimicrobial activity was obtained for HEA against C. parapsilosis with an MIC value of 4.88 μg/mL. HEA also exhibited antifungal activity against C. tropicalis with 19.53 μg/mL. Only HER exhibited low cytotoxicity on A498 renal cell lines with 60.6% cell viability.

Conclusion: Unquestionably, H. empetrifolium Willd has ethnopharmacological importance according to these results, and further investigations are required to evaluate other therapeutic properties of the plant.
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http://dx.doi.org/10.1016/j.jep.2021.113933DOI Listing
May 2021

GC/MS Profiling, In Vitro and In Silico Pharmacological Screening and Principal Component Analysis of Essential Oils from Three Exotic and Two Endemic Plants from Mauritius.

Chem Biodivers 2021 Mar 17;18(3):e2000921. Epub 2021 Feb 17.

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

The chemical and pharmacological profiles of essential oils (EOs) hydrodistilled in yields of 0.03-0.77 % (w/w) from three exotic (Cinnamomum camphora, Petroselinum crispum, and Syzygium samarangense) and two endemic (Pittosporum senacia subsp. senacia and Syzygium coriaceum) medicinal plants were studied. GC-MS/GC-FID analysis of the EOs identified the most dominant components to be myristicin (40.3 %), myrcene (62.2 %), 1,8-cineole (54.0 %), β-pinene (21.3 %) and (E)-β-ocimene (24.4 %) in P. crispum, P. senacia and C. camphora, S. samarangense and S. coriaceum EOs, respectively. All EOs were found to possess anti-amylase (0.70-1.50 mM ACAE/g EO) and anti-tyrosinase (109.35-158.23 mg KAE/g) properties, whereas no glucosidase inhibition was displayed. Only Syzygium EOs acted as dual inhibitors of both acetyl- and butyryl-cholinesterases, while P. senacia and C. camphora EOs inhibited acetylcholinesterase selectively and P. crispum EO was inactive (AChE: 4.64-4.96 mg GALAE/g; BChE: 5.96 and 7.10 mg GALAE/g). Molecular docking revealed 1,8-cineole to present the best binding affinities with butyrylcholinesterase, amylase and tyrosinase, while both myristicin and β-pinene with acetylcholinesterase and finally β-pinene with glucosidase. In vitro antioxidant potency was also demonstrated in different assays (DPPH: 13.52-53.91 mg TE/g, ABTS: 5.49-75.62 mg TE/g; CUPRAC: 45.38-243.21 mg TE/g, FRAP: 42.49-110.64 mg TE/g; and phosphomolybdenum assay: 82.61-160.93 mM TE/g). Principal component analysis revealed the EOs to differ greatly in their bioactivities due to their chemodiversity. This study has unveiled some interesting preliminary pharmacological profiles of the EOs that could be explored for their potential applications as phytotherapeutics.
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http://dx.doi.org/10.1002/cbdv.202000921DOI 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

Investigation of phytochemical composition and enzyme inhibitory potential of L.

Nat Prod Res 2021 Feb 8:1-6. Epub 2021 Feb 8.

School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan, Malaysia.

L. commonly known as 'Scarlet Pimpernel' has been used in folklore as natural remedy for treating common ailments. The present research is aimed to explore the phytochemical composition and enzyme inhibition potential of methanol and dichloromethane (DCM) extracts of aerial and root parts. The phytochemical composition was established HPLC-PDA polyphenolic quantification and UHPLC-MS analysis, while the inhibition potential against amylase and tyrosinase enzymes were assessed using standard protocols. The HPLC-PDA polyphenolic quantification revealed the presence of important compounds including catechin, gallic acid, chlorogenic acid, and ferulic acid, whereas 34 different secondary metabolites were tentatively identified by UHPLC-MS of both the DCM extracts. All the extracts showed moderate tyrosinase and a weak amylase inhibition activity. The aerial-DCM extract showed comparatively higher tyrosinase and amylase enzyme inhibition potential, which may be due to the presence of secondary metabolites as tentatively identified by its UHPLC-MS profiling.
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http://dx.doi.org/10.1080/14786419.2021.1880404DOI Listing
February 2021

Editorial: Application of Plant Secondary Metabolites to Pain Neuromodulation.

Front Pharmacol 2020 14;11:623399. Epub 2021 Jan 14.

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

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http://dx.doi.org/10.3389/fphar.2020.623399DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7841409PMC
January 2021

Essential Oils as Natural Sources of Fragrance Compounds for Cosmetics and Cosmeceuticals.

Molecules 2021 Jan 27;26(3). Epub 2021 Jan 27.

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

Fragrance is an integral part of cosmetic products and is often regarded as an overriding factor in the selection of cosmetics among consumers. Fragrances also play a considerable role in masking undesirable smells arising from fatty acids, oils and surfactants that are commonly used in cosmetic formulations. Essential oils are vital assets in the cosmetic industry, as along with imparting pleasant aromas in different products, they are able to act as preservatives and active agents and, simultaneously, offer various benefits to the skin. Moreover, the stimulating demand for natural ingredients has contributed massively to a renewed interest in cosmetic and wellness industries in plant derivatives, especially essential oils. This has led popular cosmetic companies to endorse natural fragrances and opt for minimally processed natural ingredients, given the potentially adverse health risks associated with artificial fragrance chemicals, which are major elements of cosmetics. Among the high-valued essential oils used as fragrances are citrus, lavender, eucalyptus, tea tree and other floral oils, among others, while linalool, geraniol, limonene, citronellol, and citral are much-appreciated fragrance components used in different cosmetics. Thus, this review aimed to highlight the enormous versatility of essential oils as significant sources of natural fragrances in cosmetics and cosmeceuticals. Moreover, a special focus will be laid on the different aspects related to essential oils such as their sources, market demand, chemistry, fragrance classification, aroma profile, authenticity and safety.
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http://dx.doi.org/10.3390/molecules26030666DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7865210PMC
January 2021

Bioactivity assays, chemical characterization, ADMET predictions and network analysis of Khaya senegalensis A. Juss (Meliaceae) extracts.

Food Res Int 2021 Jan 8;139:109970. Epub 2020 Dec 8.

Department of Analytical Chemistry, University of Granada, C/Fuentenueva s/n, 18071 Granada, Spain; Research and Development of Functional Food Centre (CIDAF), PTS Granada, Avda. Del Conocimiento s/n., Edificio BioRegion, 18016 Granada, Spain.

Khaya senegalensis A. Juss (Meliaceae) is a popular medicinal plant, widely used in the management of various ailments in the African traditional medicine. This study attempts to investigate into the different extraction methods (homogenizer-assisted extraction (HAE), maceration (MAC), infusion and Soxhlet (SE) extraction) on the pharmacological properties and chemical profiles of K. senegalensis. Antioxidant properties and inhibitory potential against key enzymes were assessed and bioinformatics analysis was conducted on selected limonoids to predict putative pharmacokinetics and protein targets underlying the pharmacological effects. Overall, the leaf extracts showed notable flavonoid (20.59-104.43 mg RE/g) content and the stem barks extracts displayed the highest total phenolic (87.69-46.28 mg GAE/g), phenolic acid (62.96-107.22 mg CE/g), flavanol (3.60-135.40 mg CAE/g) contents. All extracts showed remarkable antioxidant activities, with the MAC-Water leaf extract being most active in all the assays. Regarding stem bark, the MAC-MeOH extract exerted the highest free radical scavenging abilities, while HAE and MAC extracts were better sources of reducing agent and metal chelators. The HAE-MeOH, MAC-Water, and SE extracts showed noteworthy inhibitory activity against AChE, BChE (only stem barks), tyrosinase and α-glucosidase (only stem barks). All extracts displayed moderate inhibitory activities against α-amylase. The bioinformatics approach showed that khayanoside A and C interacted with multiple isoforms of metalloproteinase, while humilin B and khayanone interacted with opioid receptors. To sum up, the chemical profiles and biological activities of K. senegalensis were closely dependent on the extraction methods. Results amassed from this study showed that K. senegalensis is a potent source of bioactive compounds which could be explored as a functional food.
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http://dx.doi.org/10.1016/j.foodres.2020.109970DOI Listing
January 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

GC-MS Based Identification of the Volatile Components of Six Species from Uzbekistan and Their Biological Activity.

Plants (Basel) 2021 Jan 8;10(1). Epub 2021 Jan 8.

Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, 11566 Cairo 11566, Egypt.

The compositions of volatile components in the aerial parts of six species, namely (), (), (), (), () and (), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of , , , , and whole oils, respectively. Sylvestrene was the most predominant component in and , with highest concentration in (64.64%). In addition, ()-2-hexenal was present in a high percentage in both and (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all species and a high correlation between the and species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), α- amylase, α-glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, exhibited the maximum activity (24.12 ± 2.24 mg TE/g sample), and the volatiles from exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both and showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for (138.42 mg KAE/g). Accordingly, species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer's disease, diabetes mellitus and oxidative stress-related diseases.
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http://dx.doi.org/10.3390/plants10010124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7827139PMC
January 2021

Chemical profiling, antimicrobial, anti-enzymatic, and cytotoxic properties of Phlomis fruticosa L.

J Pharm Biomed Anal 2021 Feb 30;195:113884. Epub 2020 Dec 30.

Department of Plant Physiology, Institute for Biological Research "Siniša Stanković" - National Institute of Republic of Serbia, University of Belgrade, Bulevar despota Stefana 142, 11000 Belgrade, Serbia. Electronic address:

Structural diversity of biologically active compounds identified in plants after many years of storage is rarely reported in literature. Herein, we studied chemical profile and biological activities of Phlomis fruticosa L. after plant material storage for 20 years. Chemical analyzes were performed by UHPLC-LTQ-Orbitrap/MS, and revealed presence of 44 compounds: including 13 phenolic acids, 9 phenylethanoids, 20 flavonoids and 2 phenolic related compounds (a phenolic acid derivative and an aliphatic alcohol). The extract showed antimicrobial activity, being the most potent against Aspergillus fumigatus with minimum inhibitory concentration of 0.31 mg/mL. Also, the extract was able to inhibit biofilm formed by Candida species and to inhibit biofilm formation by Staphylococcus aureus. Obtained results revealed that the extract has potential to interfere with the cell membrane permeability of Candida albicans and to suppress production of virulence factor staphyloxanthin in S. aureus. Furthermore, the extract inhibited the activity of α-amylase which is one of the therapeutic targets for diabetes type II. Also, the antiproliferative effect of the extract was demonstrated on human cancer cell lines, while the extract did not exhibit any cytotoxic effect on primary human cells. Based on the obtained results, P. fruticosa could be an interesting source of biologically active compounds even after long term storage.
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http://dx.doi.org/10.1016/j.jpba.2020.113884DOI Listing
February 2021

RP-UHPLC-MS Chemical Profiling, Biological and In Silico Docking Studies to Unravel the Therapeutic Potential of Desf. as a Novel Source of Neuroprotective Bioactive Compounds.

Biomolecules 2021 Jan 4;11(1). Epub 2021 Jan 4.

Department for Management of Science and Technology Development, Ton Duc Thang University, Ho Chi Minh City 70000, Vietnam.

is one of the most important plant genera to have conventional folklore importance, and hence is a potential source of bioactive compounds. Thus, the present study was designed to explore the therapeutic potential of Desf., a relatively under-explored medicinal plant species. Methanolic extracts prepared from a whole plant of were studied for phytochemical composition and possible in vitro and in silico biological properties. Antioxidant potential was assessed via six different assays, and enzyme inhibition potential against key clinical enzymes involved in neurodegenerative diseases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), diabetes (α-amylase and α-glucosidase), and skin problems (tyrosinase) was assayed. Phytochemical composition was established via determination of the total bioactive contents and reverse phase ultra-high performance liquid chromatography mass spectrometry (RP-UHPLC-MS) analysis. Chemical profiling revealed the tentative presence of 50 secondary metabolites. The plant extract exhibited significant inhibition against AChE and BChE enzymes, with values of 3.80 and 3.44 mg GALAE/g extract, respectively. Further, the extract displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 43.19 and 41.80 mg TE/g extract, respectively. In addition, the selected compounds were then docked against the tested enzymes, which have shown high inhibition affinity. To conclude, was found to harbor bioactive compounds and showed potent biological activities which could be further explored for potential uses in nutraceutical and pharmaceutical industries, particularly as a neuroprotective agent.
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http://dx.doi.org/10.3390/biom11010053DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7824284PMC
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 Lipid Paradox as a Metabolic Checkpoint and Its Therapeutic Significance in Ameliorating the Associated Cardiovascular Risks in Rheumatoid Arthritis Patients.

Int J Mol Sci 2020 Dec 14;21(24). Epub 2020 Dec 14.

Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 410028 Oradea, Romania.

While the most common manifestations associated with rheumatoid arthritis (RA) are synovial damage and inflammation, the systemic effects of this autoimmune disorder are life-threatening, and are prevalent in 0.5-1% of the population, mainly associated with cardiovascular disorders (CVDs). Such effects have been instigated by an altered lipid profile in RA patients, which has been reported to correlate with CV risks. Altered lipid paradox is related to inflammatory burden in RA patients. The review highlights general lipid pathways (exogenous and endogenous), along with the changes in different forms of lipids and lipoproteins in RA conditions, which further contribute to elevated risks of CVDs like ischemic heart disease, atherosclerosis, myocardial infarction etc. The authors provide a deep insight on altered levels of low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C) and triglycerides (TGs) in RA patients and their consequence on the cardiovascular health of the patient. This is followed by a detailed description of the impact of anti-rheumatoid therapy on the lipid profile in RA patients, comprising DMARDs, corticosteroids, anti-TNF agents, anti-IL-6 agents, JAK inhibitors and statins. Furthermore, this review elaborates on the prospects to be considered to optimize future investigation on management of RA and treatment therapies targeting altered lipid paradigms in patients.
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http://dx.doi.org/10.3390/ijms21249505DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7764917PMC
December 2020

Understanding the role of Inflammasome in Angina Pectoris.

Curr Protein Pept Sci 2020 Dec 8. Epub 2020 Dec 8.

Chitkara College of Pharmacy, Chitkara University, Punjab,. India.

Angina pectoris, associated with coronary artery disease, a cardiovascular disease where, pain is caused by adverse oxygen supply in myocardium, resulting in contractility and discomfort in chest. Inflammasomes, triggered by stimuli due to infection and cellular stress have identified to play a vital role in the progression of cardiovascular disorders and thus, causing various symptoms like angina pectoris. Nlrp3 inflammasome, a key contributor in the pathogenesis of angina pectoris, requires activation and primary signaling for the commencement of inflammation. Nlrp3 inflammasome elicit out an inflammatory response by emission of pro inflammatory cytokines by ROS (reactive oxygen species) production, mobilization of K+ efflux and Ca2+ and by activation of lysosome destabilization that eventually causes pyroptosis, a programmed cell death process. Thus, inflammasome are considered to be one of the factors involved in the progression of coronary artery diseases and have an intricate role in development of angina pectoris.
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http://dx.doi.org/10.2174/1389203721999201208200242DOI Listing
December 2020

Deciphering the Neuroprotective Role of Glucagon-like peptide-1 Agonists in Diabetic Neuropathy: Current Perspective and Future Directions.

Curr Protein Pept Sci 2020 Dec 8. Epub 2020 Dec 8.

Chitkara College of Pharmacy, Chitkara University, Punjab,. India.

Diabetic neuropathy is referred as subsequential and debilitating complication belonging to type 1 and type 2 diabetes mellitus. It is a heterogeneous group of disorder with particularly complex pathophysiology and also includes multiple forms, ranging from normal discomfort to death. The evaluation of diabetic neuropathy is associated with hyperglycemic responses, resulting in alteration in various metabolic pathways including protein kinase C pathway, polyol pathway and hexosamine pathway in sachwann and glial cells of neurons. The essential source of neuronal destruction is analogous to these respective metabolic pathways, thus identified as potential therapeutic targets. These pathways regulating therapeutic medications may be used for diabetic neuropathy, however, only target specific drugs could have partial therapeutic activity. Various antidiabetic medications have been approved and marketed, which possess therapeutic ability to control hyperglycemia and ameliorate the prevalence of diabetic neuropathy. Among all antidiabetic medications, incretin therapy, including Glucagon- like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors, are the most favorable medications for the management of diabetes mellitus and associated peripheral neuropathic complications. Besides enhancing glucose-evoked insulin release from pancreatic β-cells, these therapeutic agents also play a vital role to facilitate neurite outgrowth and nerve conduction velocity in dorsal root ganglion. Furthermore, incretin therapy also activates cAMP and ERK signalling pathways, resulting in nerve regeneration and repairing. These effects are evidently supported by a series of preclinical data and investigations associated with these medications. However, the literature lacks an adequate clinical trials outcome related to these novel antidiabetic medications. The manuscript emphasizes on the pathogenesis, current pharmacological approaches and vivid description of preclinical and clinical data for the effective management of diabetic neuropathy.
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http://dx.doi.org/10.2174/1389203721999201208195901DOI Listing
December 2020

Exploring the Multifaceted Therapeutic Potential of Withaferin A and Its Derivatives.

Biomedicines 2020 Dec 6;8(12). Epub 2020 Dec 6.

Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 410028 Oradea, Romania.

Withaferin A (WA), a manifold studied, C28-steroidal lactone withanolide found in . Given its unique beneficial effects, it has gathered attention in the era of modern science. Cancer, being considered a "hopeless case and the leading cause of death worldwide, and the available conventional therapies have many lacunae in the form of side effects. The poly pharmaceutical natural compound, WA treatment, displayed attenuation of various cancer hallmarks by altering oxidative stress, promoting apoptosis, and autophagy, inhibiting cell proliferation, reducing angiogenesis, and metastasis progression. The cellular proteins associated with antitumor pathways were also discussed. WA structural modifications attack multiple signal transduction pathways and enhance the therapeutic outcomes in various diseases. Moreover, it has shown validated pharmacological effects against multiple neurodegenerative diseases by inhibiting acetylcholesterinases and butyrylcholinesterases enzyme activity, antidiabetic activity by upregulating adiponectin and preventing the phosphorylation of peroxisome proliferator-activated receptors (PPARγ), cardioprotective activity by AMP-activated protein kinase (AMPK) activation and suppressing mitochondrial apoptosis. The current review is an extensive survey of various WA associated disease targets, its pharmacokinetics, synergistic combination, modifications, and biological activities.
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http://dx.doi.org/10.3390/biomedicines8120571DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7762146PMC
December 2020

Anti-Inflammatory, Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia).

Chem Biodivers 2021 Feb 29;18(2):e2000828. Epub 2020 Dec 29.

Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Trg D. Obradovića 2, 21000, Novi Sad, Serbia.

The aim of this research work was to study the bioactivity potentials (antioxidant, anti-inflammatory, and enzyme inhibitory) of ethanol (EtOH), water (H O) and chloroform (CHCl ) extracts of G. applanatum, G. lucidum, G. pfeifferi and G. resinaceum as well as their mycochemical profile: the total content of phenolics (TP) and sugars (TS) and LC/MS/MS detection of phenolics. LC/MS/MS profile showed that p-hydroxybenzoic and protocatechuic acids were mostly found. The highest ABTS and DPPH activities were detected in polar G. applanatum extracts (159.84±0.59 mg TE/g d.w., IC =0.85±0.30 μg/mL, respectively), while G. resinaceum CHCl extract was the most potent in NO assay (IC =41.21±0.18-81.89±0.81 μg/mL). The highest TP and TS were generally determined in G. applanatum EtOH extracts. Enzyme inhibitory effects were determined in H O extracts. Generally, CHCl extracts showed the most powerful anti-inflammatory potential. These results suggest that analyzed species are a promising source of bioactive compounds and may be considered as candidates for new food supplements or drug formulations.
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http://dx.doi.org/10.1002/cbdv.202000828DOI Listing
February 2021