Publications by authors named "Hesham R El-Seedi"

97 Publications

Cyanobacteria-From the Oceans to the Potential Biotechnological and Biomedical Applications.

Mar Drugs 2021 Apr 24;19(5). Epub 2021 Apr 24.

Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom 32512, Egypt.

Cyanobacteria are photosynthetic prokaryotic organisms which represent a significant source of novel, bioactive, secondary metabolites, and they are also considered an abundant source of bioactive compounds/drugs, such as dolastatin, cryptophycin 1, curacin toyocamycin, phytoalexin, cyanovirin-N and phycocyanin. Some of these compounds have displayed promising results in successful Phase I, II, III and IV clinical trials. Additionally, the cyanobacterial compounds applied to medical research have demonstrated an exciting future with great potential to be developed into new medicines. Most of these compounds have exhibited strong pharmacological activities, including neurotoxicity, cytotoxicity and antiviral activity against HCMV, HSV-1, HHV-6 and HIV-1, so these metabolites could be promising candidates for COVID-19 treatment. Therefore, the effective large-scale production of natural marine products through synthesis is important for resolving the existing issues associated with chemical isolation, including small yields, and may be necessary to better investigate their biological activities. Herein, we highlight the total synthesized and stereochemical determinations of the cyanobacterial bioactive compounds. Furthermore, this review primarily focuses on the biotechnological applications of cyanobacteria, including applications as cosmetics, food supplements, and the nanobiotechnological applications of cyanobacterial bioactive compounds in potential medicinal applications for various human diseases are discussed.
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http://dx.doi.org/10.3390/md19050241DOI Listing
April 2021

Guaianolide Sesquiterpene Lactones from .

Molecules 2021 Apr 3;26(7). Epub 2021 Apr 3.

National Research Centre, Chemistry of Medicinal Plants Department, 33 El-Bohouth St., Dokki, Giza 12622, Egypt.

(family Asteraceae), is a leafy shrub indigenous to the southwestern Arabian Peninsula. With a paucity of phytochemical data on this species, we set out to chemically characterize the plant. From the aerial parts, two newly identified guaianolides were isolated: 3β-hydroxy-4α(acetoxy)-4β(hydroxymethyl)-8α-(4-hydroxy methacrylate)-1α,5α, 6α-gual-10(14),11(13)-dien-6,12-olide () and 15-descarboxy picrolide A (). Seven previously reported compounds were also isolated: 3β, 4α, 8α-trihydroxy-4-(hydroxymethyl)-lα, 5α, 6β, 7α-guai-10(14),11(13)-dien-6,12-olide (), chlorohyssopifolin B (), cynaropikrin (), hydroxyjanerin (), chlorojanerin (), isorhamnetin (), and quercetagetin-3,6-dimethyl ether-4'--β-d-pyranoglucoside (). Chemical structures were elucidated using spectroscopic techniques, including High Resolution Fast Atom Bombardment Mass Spectrometry (HR-FAB-MS), 1D NMR; H, C NMR, Distortionless Enhancement by Polarization Transfer (DEPT), and 2D NMR (H-H COSY, HMQC, HMBC) analyses. In addition, a biosynthetic pathway for compounds - is proposed. The chemotaxonomic significance of the reported sesquiterpenoids and flavonoids considering reports from other species is examined.
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http://dx.doi.org/10.3390/molecules26072055DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8038342PMC
April 2021

In Silico Mining of Terpenes from Red-Sea Invertebrates for SARS-CoV-2 Main Protease (M) Inhibitors.

Molecules 2021 Apr 5;26(7). Epub 2021 Apr 5.

Chemistry of Medicinal Plants Department, National Research Centre, 33 El-Bohouth St., Dokki, Giza 12622, Egypt.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent for the COVID-19 pandemic, which generated more than 1.82 million deaths in 2020 alone, in addition to 83.8 million infections. Currently, there is no antiviral medication to treat COVID-19. In the search for drug leads, marine-derived metabolites are reported here as prospective SARS-CoV-2 inhibitors. Two hundred and twenty-seven terpene natural products isolated from the biodiverse Red-Sea ecosystem were screened for inhibitor activity against the SARS-CoV-2 main protease (M) using molecular docking and molecular dynamics (MD) simulations combined with molecular mechanics/generalized Born surface area binding energy calculations. On the basis of analyses, six terpenes demonstrated high potency as M inhibitors with Δ ≤ -40.0 kcal/mol. The stability and binding affinity of the most potent metabolite, erylosides B, were compared to the human immunodeficiency virus protease inhibitor, lopinavir. Erylosides B showed greater binding affinity towards SARS-CoV-2 M than lopinavir over 100 ns with Δ values of -51.9 vs. -33.6 kcal/mol, respectively. Protein-protein interactions indicate that erylosides B biochemical signaling shares gene components that mediate severe acute respiratory syndrome diseases, including the cytokine- and immune-signaling components , , and . Pathway enrichment analysis and Boolean network modeling were performed towards a deep dissection and mining of the erylosides B target-function interactions. The current study identifies erylosides B as a promising anti-COVID-19 drug lead that warrants further and testing.
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http://dx.doi.org/10.3390/molecules26072082DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8038614PMC
April 2021

Wasp Venom Biochemical Components and Their Potential in Biological Applications and Nanotechnological Interventions.

Toxins (Basel) 2021 03 12;13(3). Epub 2021 Mar 12.

Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom 32512, Egypt.

Wasps, members of the order Hymenoptera, are distributed in different parts of the world, including Brazil, Thailand, Japan, Korea, and Argentina. The lifestyles of the wasps are solitary and social. Social wasps use venom as a defensive measure to protect their colonies, whereas solitary wasps use their venom to capture prey. Chemically, wasp venom possesses a wide variety of enzymes, proteins, peptides, volatile compounds, and bioactive constituents, which include phospholipase A2, antigen 5, mastoparan, and decoralin. The bioactive constituents have anticancer, antimicrobial, and anti-inflammatory effects. However, the limited quantities of wasp venom and the scarcity of advanced strategies for the synthesis of wasp venom's bioactive compounds remain a challenge facing the effective usage of wasp venom. Solid-phase peptide synthesis is currently used to prepare wasp venom peptides and their analogs such as mastoparan, anoplin, decoralin, polybia-CP, and polydim-I. The goal of the current review is to highlight the medicinal value of the wasp venom compounds, as well as limitations and possibilities. Wasp venom could be a potential and novel natural source to develop innovative pharmaceuticals and new agents for drug discovery.
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http://dx.doi.org/10.3390/toxins13030206DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8000949PMC
March 2021

Comparative Study on the Essential Oils from Five Wild Egyptian Species: Effective Extraction Techniques, Antimicrobial Activity and In-Silico Analyses.

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

Chemistry of Medicinal Plants Department, National Research Centre, 33 El-Bohouth St., Dokki, Giza 12622, Egypt.

The genus is recognized in folk medicine for anti-inflammatory, anti-itch, antitussive, purgative, astringent, and tonic activities. To study the chemical determinant for antimicrobial activity essential oils (EOs), five species were analyzed including: , , , and . Conventional hydro-distillation (HD) and microwave-assisted extraction (MAE), as new green technologies, were compared for the extraction of essential oils. GC/MS analysis identified 120 EOs including mostly terpenoid except from and in which nonterpenoids were the major constituents. Major terpenoids included spathulenol, caryophyllene oxide and alloaromadendrene oxide-2. To probe antibacterial activity, potential EO inhibitors of a bacterial type II DNA topoisomerase, DNA gyrase B were screened via an in silico molecular docking approach. Spathulenol and alloaromadendrene oxide-2 possessed the best binding affinity in the ATP- binding pocket of Gyrase B enzyme. Principal component analysis and agglomerative hierarchical clustering were used for sample classification and revealed that sesquiterpenes contributed the most for accessions classification. In vitro antimicrobial activity against , and for all EOs were also evaluated. EOs from , and exhibited significant MIC against with an MIC value of 31.25 µg/mL.
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http://dx.doi.org/10.3390/antibiotics10030252DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8000757PMC
March 2021

Potential Role of Curcumin and Its Nanoformulations to Treat Various Types of Cancers.

Biomolecules 2021 Mar 7;11(3). Epub 2021 Mar 7.

Pharmacology Department, Faculty of Veterinary Medicine, Suez Canal University, Ismailia 41522, Egypt.

Cancer is a major burden of disease globally. Each year, tens of millions of people are diagnosed with cancer worldwide, and more than half of the patients eventually die from it. Significant advances have been noticed in cancer treatment, but the mortality and incidence rates of cancers are still high. Thus, there is a growing research interest in developing more effective and less toxic cancer treatment approaches. Curcumin (CUR), the major active component of turmeric ( L.), has gained great research interest as an antioxidant, anticancer, and anti-inflammatory agent. This natural compound shows its anticancer effect through several pathways including interfering with multiple cellular mechanisms and inhibiting/inducing the generation of multiple cytokines, enzymes, or growth factors including IκB kinase β (IκKβ), tumor necrosis factor-alpha (TNF-α), signal transducer, and activator of transcription 3 (STAT3), cyclooxygenase II (COX-2), protein kinase D1 (PKD1), nuclear factor-kappa B (NF-κB), epidermal growth factor, and mitogen-activated protein kinase (MAPK). Interestingly, the anticancer activity of CUR has been limited primarily due to its poor water solubility, which can lead to low chemical stability, low oral bioavailability, and low cellular uptake. Delivering drugs at a controlled rate, slow delivery, and targeted delivery are other very attractive methods and have been pursued vigorously. Multiple CUR nanoformulations have also been developed so far to ameliorate solubility and bioavailability of CUR and to provide protection to CUR against hydrolysis inactivation. In this review, we have summarized the anticancer activity of CUR against several cancers, for example, gastrointestinal, head and neck, brain, pancreatic, colorectal, breast, and prostate cancers. In addition, we have also focused on the findings obtained from multiple experimental and clinical studies regarding the anticancer effect of CUR in animal models, human subjects, and cancer cell lines.
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http://dx.doi.org/10.3390/biom11030392DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001478PMC
March 2021

Determination of perchlorate in tea using SERS with a superhydrophobically treated cysteine modified silver film/polydimethylsiloxane substrate.

Anal Methods 2021 04 18;13(13):1625-1634. Epub 2021 Mar 18.

School of Food and Biological Engineering, Jiangsu University, Zhenjiang 212013, China.

Perchlorate is a new type of persistent pollutant, which interferes with the synthesis and secretion of thyroxine and affects human health. The EU's limit for perchlorate in tea is 750 μg kg. The surface-enhanced Raman scattering (SERS) technique has the characteristics of a simple pretreatment method, rapid detection, high sensitivity, high specificity and great stability in the detection of perchlorate. This study proposed a novel superhydrophobic SERS substrate, which can be used to detect perchlorate in tea. Firstly, a chemical deposition method was used to deposit a silver film on the surface of a thin layer of polydimethylsiloxane. After drying, the substrate was immersed in 1H,1H,2H,2H-perfluorodecyltriethoxysilane aqueous solution for 15 hours to make the surface of the substrate superhydrophobic. Then cysteine molecules were deposited on the surface of the silver film/polydimethylsiloxane by incubation. The superhydrophobic surface has a unique enrichment effect on the highly diluted solution, and perchlorate has a strong affinity for the amino group of cysteine. We collected the Raman spectra of 9 gradient concentrations (1-100 μmol L) of perchlorate-spiked tea samples on the hydrophobic substrate, and a linear model of the relationship between the SERS spectral intensity and the concentrations of perchlorate in tea was established. This method reached a good limit of detection of 0.0067 μmol L (0.82 μg kg) in tea, which showed that the developed sensor has high sensitivity and could be used as a fast and simple technique for quantitative detection of perchlorate based on SERS technology.
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http://dx.doi.org/10.1039/d1ay00215eDOI Listing
April 2021

Intelligent evaluation of taste constituents and polyphenols-to-amino acids ratio in matcha tea powder using near infrared spectroscopy.

Food Chem 2021 Mar 8;353:129372. Epub 2021 Mar 8.

School of Food and Biological Engineering, Jiangsu University, Zhenjiang 212013, China.

Matcha tea is rich in taste and bioactive constituents, quality evaluation of matcha tea is important to ensure flavor and efficacy. Near-infrared spectroscopy (NIR) in combination with variable selection algorithms was proposed as a fast and non-destructive method for the quality evaluation of matcha tea. Total polyphenols (TP), free amino acids (FAA), and polyphenols-to-amino acids ratio (TP/FAA) were assessed as the taste quality indicators. Successive projections algorithm (SPA), genetic algorithm (GA), and simulated annealing (SA) were subsequently developed from the synergy interval partial least squares (SiPLS). The overall results revealed that SiPLS-SPA and SiPLS-SA models combined with NIR exhibited higher predictive capabilities for the effective determination of TP, FAA and TP/FAA with correlation coefficient in the prediction set (R) of R > 0.97, R > 0.98 and R > 0.98 respectively. Therefore, this simple and efficient technique could be practically exploited for tea quality control assessment.
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http://dx.doi.org/10.1016/j.foodchem.2021.129372DOI Listing
March 2021

Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer's Disease Therapy.

Biomolecules 2021 Feb 25;11(3). Epub 2021 Feb 25.

Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana-124001, India.

Alzheimer's disease (AD) is a gradually growing irreversible illness of the brain that almost affects every fifth person (aged > 80 years) in the world. World Health Organization (WHO) also revealed that the prevalence of this disease will enhance (upto double) significantly upto 2030. The poor cholinergic transmission at the synapse is considered to be one of the main reasons behind the progression and occurrence of this disorder. Natural inhibitors of acetylcholine (ACh) such as galanthamine and rivastigmine are used commercially in the treatmentof AD. The biomolecules such assesquiterpenes, possess a great structural diversity and are responsible for a plethora of pharmacological properties. The potential of various sesquiterpenes as anticholinesterase has been reviewed in this article. For this purpose, the various databases, mainly PubMed, Scopus, and Web of Science were investigatedwith different keywords such as "sesquiterpenes+acetylcholinesterase" and "sesquiterpenes+cholinesterase+inhibitors" in the surveyed time frame (2010-2020). A vast literature was evident in the last decade, which affirms the potential of various sesquiterpenes in the improvement of cholinergic transmission by inhibiting the AChE. After data analysis, it was found that 12 compounds out of a total of 58 sesquiterpenes were reported to possess IC < 9μM and can be considered as potential candidates for the improvement of learning and memory. Sesquiterpene is an important category of terpenoids, found to possess a large spectrum of biological activities. The outcome of the review clearly states that sesquiterpenes (such as amberboin, lipidiol,etc) from herbs could offer fresh, functional compounds for possible prevention and treatment of AD.
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http://dx.doi.org/10.3390/biom11030350DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7996600PMC
February 2021

Angiotensinogen Gene Missense Polymorphisms (rs699 and rs4762): The Association of End-Stage Renal Failure Risk with Type 2 Diabetes and Hypertension in Egyptians.

Genes (Basel) 2021 Feb 25;12(3). Epub 2021 Feb 25.

Department of Public Health and Community Medicine, Faculty of Medicine, Menoufia University, Menoufia 32511, Egypt.

Type 2 diabetes mellitus (T2DM) and hypertension are common chronic diseases mainly associated with the development and progression of end-stage renal disease (ESRD) leading to morbidity and mortality. Gene polymorphisms linked to the renin-angiotensin ()-aldosterone system (RAAS) were broadly inspected in patients with diabetic nephropathy (DN) and hypertension. This study aimed to investigate the association of gene polymorphisms (rs699 and rs4762) with ESRD in T2DM hypertensive Egyptian patients. Genotyping of rs699 and rs4762 was conducted using the tetra-primers amplification refractory mutation system (ARMS-PCR). The allelic distribution analysis was performed on 103 healthy control subjects, 97 non-ESRD patients, and 104 patients with ESRD. The allelic frequencies of gene polymorphisms (rs4762 and rs699) in all study participants were assessed. For the non-ESRD group, the frequencies of the alleles of -rs4762 ( = 31.88, < 0.001, OR = 5.17, CI 95%: 2.81-9.51) and -rs699 ( = 4.85, = 0.027, OR = 1.56, CI 95%: 1.05-2.33) were significantly associated with the non-ESRD group. However, for the ESRD group, the T allele was significantly higher than that in the controls ( = 24.97, < 0.001, odds ratio (OR) = 4.35, CI 95%: 2.36-8.02). Moreover, (rs699) genotypes showed no significant difference between the ESRD group and controls. In conclusion, gene polymorphisms rs699 and rs4762 were associated with non-ESRD versus controls, without any significant risk observed in all patient groups. However, the (rs4762) variant showed a significant risk in the ESRD group in comparison to controls in Egyptians.
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http://dx.doi.org/10.3390/genes12030339DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7996594PMC
February 2021

Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid.

Molecules 2021 Feb 26;26(5). Epub 2021 Feb 26.

Third World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

In search of anti-inflammatory compounds, novel scaffolds containing isonicotinoyl motif were synthesized via an efficient strategy. The compounds were screened for their in vitro anti-inflammatory activity. Remarkably high activities were observed for isonicotinates - and -. The compound exhibits an exceptional IC value (1.42 ± 0.1 µg/mL) with 95.9% inhibition at 25 µg/mL, which is eight folds better than the standard drug ibuprofen (11.2 ± 1.9 µg/mL). To gain an insight into the mode of action of anti-inflammatory compounds, molecular docking studies were also performed. Decisively, further development and fine tuning of these isonicotinates based scaffolds for the treatment of various aberrations is still a wide-open field of research.
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http://dx.doi.org/10.3390/molecules26051272DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7956706PMC
February 2021

Synthesis, X-ray, Hirshfeld surface analysis, exploration of DNA binding, urease enzyme inhibition and anticancer activities of novel adamantane-naphthyl thiourea conjugate.

Bioorg Chem 2021 Apr 9;109:104707. Epub 2021 Feb 9.

Hacettepe University, Department of Physics, 06800 Beytepe-Ankara, Turkey.

1-(adamantane-1-carbonyl-3-(1-naphthyl)) thiourea (CHNOS (4), was synthesized by the reaction of freshly prepared adamantane-1-carbonyl chloride from corresponding acid (3) with ammonium thiocyanate in 1:1 M ratio in dry acetone to afford the adamantane-1-carbonyl isothiocyanate (2) in situ followed by treatment with 1-naphthyl amine (3). The structure was established by elemental analyses, FTIR, H, C NMR and mass spectroscopy. The molecular and crystal structure were determined by single crystal X-ray analysis. It belongs to triclinic system P - 1 space group with a = 6.7832(5) Å, b = 11.1810(8) Å, c = 13.6660(10) Å, α = 105.941(6)°, β = 103.730(6)°, γ = 104.562(6)°, Z = 2, V = 910.82(11) Å. The naphthyl group is almost planar. In the crystal structure, intermolecular CH···O hydrogen bonds link the molecules into centrosymmetric dimers, enclosing R(14) ring motifs, while the intramolecular NH···O hydrogen bonds enclose S(6) ring motifs, in which they may be effective in the stabilization of the structure. The Hirshfeld surface analysis of the crystal structure indicates that the most important contributions for the crystal packing are from H … H (59.3%), H … C/C … H (19.8%) and H … S/S … H (10.1%) interactions. Hydrogen bonding and van der Waals interactions are the dominant interactions in the crystal packing. DFT, molecular docking and urease inhibition studies revealed stability and electron withdrawing nature of 4 as compared to DNA base pairs and residues of urease. The DNA binding results from docking, UV- visible spectroscopy, and viscosity studies indicated significant binding of 4 with the DNA via intercalation and groove binding. Further investigation of the compound was done on hepatocellular carcinoma; Huh-7 cell line as well as normal human embryonic kidney; Hek-293 cell line. The compound showed significant cytotoxic activity against Huh-7 cells in comparison to normal Hek-293 cells indicating selective cytotoxicity towards cancer cells.
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http://dx.doi.org/10.1016/j.bioorg.2021.104707DOI Listing
April 2021

The Ameliorative Role of Gum against the Oxidative Stress and Genotoxicity Induced by the Radiographic Contrast Medium (Ioxitalamate) in Albino Rats.

Antioxidants (Basel) 2021 Feb 2;10(2). Epub 2021 Feb 2.

Basic Science Center, Department of Biology, Misr University for Science and Technology, Giza 12511, Egypt.

Arabic gum (, AG) is proven effective antioxidant and cytoprotective agent. The present study was designed to test this notion by investigating the possible role of AG against the radiographic contrast medium (Ioxitalamate, Telebrix-35, TBX)-induced oxidative stress and genotoxicity. Albino rats were divided into four groups and supplied with either; distilled water, daily 10% (/) AG, an intravenous dose of TBX (1600 mg I/kg b.wt) and co-administration of TBX and AG. Rats were sacrificed and blood samples were collected to assess the genotoxicity employing the peripheral blood leucocytes fluorescent double staining; namely the acridine orange/ethidium bromide (AO/EB) staining and alkaline comet assay. Further, chromosomal analyses were done in bone marrow cells. Serum urea and creatinine levels, in addition to malondialdehyde (MDA), nitric oxide (NO), catalase (CAT) and glutathione (GSH) levels in kidney tissues were measured. Liquid chromatography-mass spectrophotometry (LC-MS-MS) was performed to identify the chemical composition of AG extract. Kidney functions, single/double-stranded DNA damage, chromosomal aberrations, mitotic index, MDA and NO levels were significantly ( < 0.001) increased in TBX-treated group compared to the control and AG-treated one. Meanwhile, CAT and GSH activities were significantly diminished and the AG supplementation significantly ( < 0.001) ameliorated these effects compared with the control and AG-treated groups. Five compounds have been identified using GNPS networking including 7,3',4'-Trihydroxyisoflavone, Noscapine, Tetrahydropapaveroline, Costunolide, Hesperidin. In conclusion, results of the present study suggest that AG exerted a protective role against TBX-induced oxidative stress and genotoxicity which may be attributed to the active metabolites in the gum.
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http://dx.doi.org/10.3390/antiox10020221DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7912984PMC
February 2021

Acrylamide-induced peripheral neuropathy: manifestations, mechanisms, and potential treatment modalities.

Environ Sci Pollut Res Int 2021 Mar 23;28(11):13031-13046. Epub 2021 Jan 23.

Pharmacology Department, Faculty of Veterinary Medicine, Suez Canal University, Ismailia, 41522, Egypt.

Acrylamide is a chemical monomer; its polymer compounds are used in the manufacture of plastic, papers, adhesive tapes, dyes, and food packaging. Lately, scientists found that cooking (mainly roasting, baking, and frying) yields acrylamide. In addition to fried/baked potatoes, coffee and bakery products still contain substantial amounts of acrylamide. Acrylamide has toxic effects on different body systems include genitourinary, reproductive, nervous system, along with being a carcinogenic substance. The neurotoxicity of acrylamide includes central and peripheral neuropathy. In humans, the clinical manifestations include sensory or motor peripheral neuropathy, drowsiness, or cerebellar ataxia. Likewise, it presents with skeletal muscle weakness, hindlimb dysfunction, ataxia, and weight loss in animals. The suggested mechanisms for acrylamide neurotoxicity include direct inhibition of neurotransmission, cellular changes, inhibition of key cellular enzymes, and bonding of kinesin-based fast axonal transport. Moreover, it is suggested that acrylamide's molecular effect on SNARE core kinetics is carried out through the adduction of NSF and/or SNARE proteins. Lately, scientists showed disruption of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2) cell signaling pathways in human differentiating neuroblastoma SH-SY5Y cells, exposed to acrylamide. Different treatment modalities have been revealed to shield against or hasten recovery from acrylamide-induced neuropathy in preclinical studies, including phytochemical, biological, and vitamin-based compounds. Still, additional studies are needed to elucidate the pathogenesis and to identify the best treatment modality.
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http://dx.doi.org/10.1007/s11356-020-12287-6DOI Listing
March 2021

Resveratrol and Neuroprotection: Impact and Its Therapeutic Potential in Alzheimer's Disease.

Front Pharmacol 2020 30;11:619024. Epub 2020 Dec 30.

Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.

Alzheimer's disease (AD) is a progressive cortex and hippocampal neurodegenerative disease which ultimately causes cognitively impaired decline in patients. The AD pathogen is a very complex process, including aggregation of Aβ (β-amyloid peptides), phosphorylation of tau-proteins, and chronic inflammation. Exactly, resveratrol, a polyphenol present in red wine, and many plants are indicated to show the neuroprotective effect on mechanisms mostly above. Resveratrol plays an important role in promotion of non-amyloidogenic cleavage of the amyloid precursor protein. It also enhances the clearance of amyloid beta-peptides and reduces the damage of neurons. Most experimental research on AD and resveratrol has been performed in many species, both and , during the last few years. Nevertheless, resveratrol's effects are restricted by its bioavailability in the reservoir. Therefore, scientists have tried to improve its efficiency by using different methods. This review focuses on recent work done on the cell and animal cultures and also focuses on the neuroprotective molecular mechanisms of resveratrol. It also discusses about the therapeutic potential onto the treatment of AD.
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http://dx.doi.org/10.3389/fphar.2020.619024DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7804889PMC
December 2020

Identification of novel C-2 symmetric Bis-Azo-Azamethine molecules as competitive inhibitors of mushroom tyrosinase and free radical scavengers: synthesis, kinetics, and molecular docking studies.

J Biomol Struct Dyn 2020 Dec 20:1-10. Epub 2020 Dec 20.

International Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang, China.

Tyrosinase is a multi-copper enzyme found in plants, animals and microorganisms, plays a critical role in the melanogenesis and browning process critical to cosmetics and food industries. Many natural, semi-synthetic and synthetic inhibitors have been discovered. To this end, a small library of symmetrical Bis-Azo-Azamethine hybrids was synthesized and characterized through spectroscopic and analytical data and explored for mushroom tyrosinase and free radical scavenging activity. All of the molecules explicated better potential compared to the standard Kojic acid. On the whole, compound having IC value 0.002 ± 0.004 µM was found to be the most potent derivative. The Kinetic studies were performed for and indicating the mode of inhibition in a competitive manner. Structure Activity Relationship (SAR) analysis and docking studies were carried out. Thus compound bearing bulky naphthyl groups was most potent and, The molecular docking indicated formation of two hydrogen bonds with Arg268 and one hydrophobic interaction with Glu322. The carbonyl oxygen of interacts with Arg268 and form two hydrogen bonds having lengths 2.44 and 2.62 Å, respectively. In the same way, compounds were appraised for DPPH free radical scavenging ability and five of them , , , and were found to exhibit higher % scavenging potency compared with vitamin C, as the standard. Interesting compound was again the most potent in the series. The current investigation points towards the role of naphthyl group in design of new inhibitors of melanogenesis and the antioxidants with improved efficacy. Communicated by Ramaswamy H. Sarma.
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http://dx.doi.org/10.1080/07391102.2020.1857841DOI Listing
December 2020

Characterization of -Glucosidase Inhibitors from Jack Leaves Extract Using LC-MS-Based Multivariate Data Analysis and In-Silico Molecular Docking.

Molecules 2020 Dec 12;25(24). Epub 2020 Dec 12.

Pharmacognosy Group, Department of Pharmaceutical Biosciences, BMC, Uppsala University, SE-751 23 Uppsala, Sweden.

Jack has traditionally been used to treat diabetes. Despite its potential, the scientific proof in relation to this plant is still lacking. Thus, the present study aimed to investigate the -glucosidase inhibitors in leaf extracts using a metabolomics approach and to elucidate the ligand-protein interactions through in silico techniques. The plant leaves were extracted with methanol and water at five various ratios (100, 75, 50, 25 and 0% ; water-methanol). Each extract was tested for -glucosidase inhibition, followed by analysis using liquid chromatography tandem to mass spectrometry. The data were further subjected to multivariate data analysis by means of an orthogonal partial least square in order to correlate the chemical profile and the bioactivity. The loading plots revealed that the signals correspond to the activity of -glucosidase inhibitors, which led to the identification of three putative bioactive compounds, namely 5'-hydroxymethyl-1'-(1, 2, 3, 9-tetrahydro-pyrrolo (2, 1-) quinazolin-1-yl)-heptan-1'-one (), -terpinyl--glucoside (), and machaeridiol-A (). Molecular docking of the identified inhibitors was performed using Auto Dock Vina software against the crystal structure of isomaltase (Protein Data Bank code: 3A4A). Four hydrogen bonds were detected in the docked complex, involving several residues, namely ASP352, ARG213, ARG442, GLU277, GLN279, HIE280, and GLU411. Compound , , and showed binding affinity values of -8.3, -7.6, and -10.0 kcal/mol, respectively, which indicate the good binding ability of the compounds towards the enzyme when compared to that of quercetin, a known -glucosidase inhibitor. The three identified compounds that showed potential binding affinity towards the enzymatic protein in molecular docking interactions could be the bioactive compounds associated with the traditional use of this plant.
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http://dx.doi.org/10.3390/molecules25245885DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763559PMC
December 2020

Label-free surface enhanced Raman scattering spectroscopy for discrimination and detection of dominant apple spoilage fungus.

Int J Food Microbiol 2021 Jan 27;338:108990. Epub 2020 Nov 27.

School of Food and Biological Engineering, Jiangsu University, Zhenjiang 212013, China.

Fungal infection is one of the main causes of apple corruption. The main dominant spoilage fungi in causing apple spoilage are storage mainly include Penicillium Paecilomyces paecilomyces (P. paecilomyces), penicillium chrysanthemum (P. chrysogenum), expanded Penicillium expansum (P. expansum), Aspergillus niger (Asp. niger) and Alternaria. In this study, surface-enhanced Raman spectroscopy (SERS) based on gold nanorod (AuNRs) substrate method was developed to collect and examine the Raman fingerprints of dominant apple spoilage fungus spores. Standard normal variable (SNV) was used to pretreat the obtained spectra to improve signal-to-noise ratio. Principal component analysis (PCA) was applied to extract useful spectral information. Linear discriminant analysis (LDA) and non-linear pattern recognition methods including K nearest neighbor (KNN), Support vector machine (SVM) and back propagation artificial neural networks (BPANN) were used to identify fungal species. As the comparison of modeling results shown, the BPANN model established based on the characteristic spectra variables have achieved the satisfactory result with discrimination accuracy of 98.23%; while the PCA-LDA model built using principal component variables achieved the best distinguish result with discrimination accuracy of 98.31%. It was concluded that SERS has the potential to be an inexpensive, rapid and effective method to detect and identify fungal species.
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http://dx.doi.org/10.1016/j.ijfoodmicro.2020.108990DOI Listing
January 2021

Evaluation of cytotoxicity of areca nut and its commercial products on normal human gingival fibroblast and oral squamous cell carcinoma cell lines.

J Hazard Mater 2021 02 8;403:123872. Epub 2020 Sep 8.

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan; Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan. Electronic address:

Consumption of areca nut products is the most common cause of oral cancers, particularly in South Asian countries. This study evaluates the cytotoxic and necrotizing effects of areca nut and its formulations on normal human gingival fibroblasts (HGF-1) and oral squamous cell carcinoma (OSCC, CAL-27) cell lines. Identification of various carcinogens and adulterants using LC-HR-ESI-MS/MS analysis was performed in the extracts of areca nut and its products. Apart from alkaloids and flavonoids, a major adulterant, saccharin was found in all the samples of chalia (one of the most common chewing products of areca nut) in the ranges between 1.697-7.170 mg/g of the sample. Cytotoxic studies showed that most of the areca nut products were found cytotoxic to HGF-1 cells while being relatively non-cytotoxic against CAL-27 cells, rather they promote the growth of cancer cells. Our findings revealed that the components of areca nut and its products were injurious to HGF-1 cells and caused necrosis, which may attenuate HGF-1 protection toward oral epithelial cells. Moreover, the non-cytotoxic effect of these products on cancer cell lines suggests further predisposal of the habitual chewers for developing oral carcinomas. This study will give a better understanding of the hazardous effects of areca nut products.
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http://dx.doi.org/10.1016/j.jhazmat.2020.123872DOI Listing
February 2021

Exploring natural products-based cancer therapeutics derived from egyptian flora.

J Ethnopharmacol 2021 Apr 25;269:113626. Epub 2020 Nov 25.

Natural Products Laboratory, IBL, Leiden University PO Box 9505, 2300RA, Leiden, the Netherlands.

Ethnopharmacological Relevance: Egyptian plants are a rich source of natural molecules, representing considerable biodiversity due to climate variations between the Northern, Southern, Eastern and Western regions of the country. Sinai is considered a precious nature reserves preserving flora, fauna, marine organisms, and historical habitats with ancient origins. Here, traditional medicinal approaches have been used for hundreds of years. Healthy lifestyles, low levels of stress and microbial infections, and a dependence on flora and herbal medicine might in combination explain why the burden of cancer is lower in some regions than in others.

Aim Of The Study: The primary aim of this review is to document the plants and natural products that are used as foods and medicines in Egypt, in general, and in Sinai, in particular, with a focus on those with demonstrated anticancer activities. The documented traditional uses of these plants are described, together with their chemical and pharmacological activities and the reported outcomes of clinical trials against cancer.

Materials And Methods: A literature search was performed to identify texts describing the medicinal plants that are cultivated and grown in Egypt, including information found in textbooks, published articles, the plant list website (http://www.theplantlist.org/), the medicinal plant names services website (http://mpns.kew.org/mpns-portal/), and web databases (PubMed, Science Direct, and Google Scholar).

Results And Discussion: We collected data for most of the plants cultivated or grown in Egypt that have been previously investigated for anticancer effects and reported their identified bioactive elements. Several plant species, belonging to different families and associated with 67 bioactive compounds, were investigated as potential anticancer agents (in vitro studies). The most potent cytotoxic activities were identified for the families Asteraceae, Lamiaceae, Chenopodiaceae, Apocynaceae, Asclepiadaceae, Euphorbiaceae, Gramineae, and Liliaceae. The anticancer activities of some species, such as Punica granatum L., Nerium oleander L., Olea europea L., Matricaria chamomilla L., Cassia acutifolia L., Nigella sativa L., Capsicum frutescens L., Withania somnifera L., and Zingiber officinale Roscoe, have been examined in clinical trials. Among the various Egyptian plant habitats, we found that most of these plants are grown in the North Sinai, New-Delta, and Giza Governorates.

Conclusion: In this review, we highlight the role played by Egyptian flora in current medicinal therapies and the possibility that these plants may be examined in further studies for the development of anticancer drugs. These bioactive plant extracts form the basis for the isolation of phytochemicals with demonstrated anticancer activities. Some active components derived from these plants have been applied to preclinical and clinical settings, including resveratrol, quercetin, isoquercetin, and rutin.
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http://dx.doi.org/10.1016/j.jep.2020.113626DOI Listing
April 2021

Natural isocoumarins: Structural styles and biological activities, the revelations carry on ….

Phytochemistry 2021 Jan 7;181:112568. Epub 2020 Nov 7.

College of Food and Biological Engineering, Jiangsu University, Zhenjiang, 212013, China; Al-Rayan Colleges, Medina, 42541, Saudi Arabia.

Isocoumarins and dihydroisocoumarins are lactonic phytochemicals plentiful in microbes and higher plants. These are an amazing small scaffolds consecrated with all types of pharmacological applications. Our previous review covered the period 2000-2016, documenting the then known natural products of this class; the current article is a critical account of discovery of known as well as undescribed structural types and pharmacological activities reported in the course of 2016-2020. The classification revealed in our previous review based on the biogenetic origin is further buttressed by discovery of new members of each class and some new structural types hitherto unknown have also been identified. Similarly, the biological activities and SAR conclusions identified were found to be valid as well, nonetheless with new accompaniments. The most recent available literature on the structural diversity and biological activity of these natural products has been included. The information documented in this article are collected from scientific journals, books, electronic search engines and scientific databases.
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http://dx.doi.org/10.1016/j.phytochem.2020.112568DOI Listing
January 2021

Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.

Eur J Med Chem 2021 Jan 28;210:112957. Epub 2020 Oct 28.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

The marine environment with its vast biological diversity encompasses many organisms that produce bioactive natural products. Marine microorganisms are rich sources of compounds from many structural classes with a multitude of biological activities. The biosynthesis of microbial natural products depends on a variety of biotic and abiotic factors in the marine environment, including temperature, nutrients, salinity and interaction with other microorganisms. Terpenoids, as one of the most important groups of natural products in terrestrial microorganisms are important metabolites for marine microorganisms. Here, we have reviewed the chemistry, biosynthesis and pharmacological activities of terpenoids, extracted from marine microbes, and then survey their potential applications in drug development. We also discussed the different habitats in which marine microorganisms are found including sediments, the flora, such as seaweeds, sea grasses, and mangroves as well as the fauna like sponges and corals. Amongst these habitats, marine sediments are the major source for terpenoids producing microorganisms. The marine bacteria produce mostly meroterpenoids, while the fungi are well known for production of isoprenoids. Interestingly, marine-derived microbial terpenoids have some structural characteristics such as halogenation, which are catalyzed by specific enzymes with distinct substrate specificity. These compounds have anticancer, antibacterial, antifungal, antimalarial and anti-inflammatory properties. The information collected here might provide useful clues for developing new medications.
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http://dx.doi.org/10.1016/j.ejmech.2020.112957DOI Listing
January 2021

Antioxidant, Anti-Inflammatory, and Anti-Apoptotic Effects of Ethanolic Extract against Lead-Induced Hepatotoxicity in Rats.

Antioxidants (Basel) 2020 Oct 19;9(10). Epub 2020 Oct 19.

Department of Biochemistry and Chemistry of Nutrition, Faculty of Veterinary Medicine, Menoufia University, Shebin El-Kom, Menoufia 32512, Egypt.

The current study investigated the protective potential of ethanolic extract (APE) against lead-induced hepatotoxicity in rats. Sixty male Wistar albino rats were randomly allocated into six groups (n = 10). The control group was orally administrated with saline. The second group received lead acetate (100 mg/kg body weight (BW) orally for 60 days). The third group was fed with APE (10 mg/kg BW orally for 60 days). The fourth group was administrated with lead acetate like the second group and APE like the third group, concomitantly, for 60 days. The fifth group was administrated with APE like the third group for 30 days, then orally administrated with the lead acetate like the second group for another 30 days. The sixth group was administrated with lead acetate like the second group for 30 days, then with APE like the third group for a further 30 days. Phytochemical analysis of APE indicated the presence of peonidin 3--glucoside cation, vitexin, rutin, thiamine, choline, tamarixetin, hyperoside, astragalin, and quercetin. The latter has been elucidated using one- and two-dimensional nuclear magnetic resonance (1D and 2D NMR) and liquid chromatography-mass spectrometry (LC-MS-MS). Lead acetate increased the serum levels of alanine and aspartate aminotransferases and that of urea, creatinine, tumor necrosis factor alpha, and interleukin 1, hepatic tissue malondialdehyde contents, and caspase 3 protein expression, as well as altering the hepatic tissue architecture. However, it decreased the serum levels of interleukin 10 and glutathione (GSH) contents, and the activities of catalase and superoxide dismutase in hepatic tissue. In contrast, the administration of APE ameliorated the lead-induced alterations in liver function and structure, exemplifying the benefits of 's phytochemical contents. Collectively, extract is a protective and curative agent against lead-induced hepatotoxicity via its antioxidant, anti-inflammatory, and anti-apoptotic impacts.
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http://dx.doi.org/10.3390/antiox9101014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7603163PMC
October 2020

Screening for natural and derived bio-active compounds in preclinical and clinical studies: One of the frontlines of fighting the coronaviruses pandemic.

Phytomedicine 2021 May 29;85:153311. Epub 2020 Aug 29.

Department of Molecular Biosciences, The Wenner-Gren Institute, Stockholm University, S-106 91, Stockholm, Sweden; Department of Chemistry, Faculty of Science, Menoufia University, 32512 Shebin El-Kom, Egypt; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan; International Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang 212013, China. Electronic address:

Background: Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge.

Methods: A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar).

Results: Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Hér.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARS-CoV. Out of the listed compound Lycorine, emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4`-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab.

Conclusion: Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.
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http://dx.doi.org/10.1016/j.phymed.2020.153311DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7455571PMC
May 2021

In silico drug discovery of major metabolites from spices as SARS-CoV-2 main protease inhibitors.

Comput Biol Med 2020 11 8;126:104046. Epub 2020 Oct 8.

Chemistry of Medicinal Plants Department, National Research Centre, 33 El-Bohouth St., Dokki, Giza, 12622, Egypt; Department of Pharmaceutical Biology, Institute of Pharmaceutical and Biomedical Sciences, Johannes Gutenberg University, Staudinger Weg 5, 55128, Mainz, Germany. Electronic address:

Coronavirus Disease 2019 (COVID-19) is an infectious illness caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), originally identified in Wuhan, China (December 2019) and has since expanded into a pandemic. Here, we investigate metabolites present in several common spices as possible inhibitors of COVID-19. Specifically, 32 compounds isolated from 14 cooking seasonings were examined as inhibitors for SARS-CoV-2 main protease (M), which is required for viral multiplication. Using a drug discovery approach to identify possible antiviral leads, in silico molecular docking studies were performed. Docking calculations revealed a high potency of salvianolic acid A and curcumin as M inhibitors with binding energies of -9.7 and -9.2 kcal/mol, respectively. Binding mode analysis demonstrated the ability of salvianolic acid A and curcumin to form nine and six hydrogen bonds, respectively with amino acids proximal to M's active site. Stabilities and binding affinities of the two identified natural spices were calculated over 40 ns molecular dynamics simulations and compared to an antiviral protease inhibitor (lopinavir). Molecular mechanics-generalized Born surface area energy calculations revealed greater salvianolic acid A affinity for the enzyme over curcumin and lopinavir with energies of -44.8, -34.2 and -34.8 kcal/mol, respectively. Using a STRING database, protein-protein interactions were identified for salvianolic acid A included the biochemical signaling genes ACE, MAPK14 and ESR1; and for curcumin, EGFR and TNF. This study establishes salvianolic acid A as an in silico natural product inhibitor against the SARS-CoV-2 main protease and provides a promising inhibitor lead for in vitro enzyme testing.
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http://dx.doi.org/10.1016/j.compbiomed.2020.104046DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7543985PMC
November 2020

Alpha-Glucosidase Inhibitory Effect of Jack Leaf: A Rapid Analysis Using Infrared Fingerprinting.

Molecules 2020 Sep 11;25(18). Epub 2020 Sep 11.

Department of Molecular Biosciences, The Wenner-Gren Institute, Stockholm University, SE-106 91 Stockholm, Sweden.

The plant Jack belongs to the Rubiaceae family and is known in Malaysia as "meroyan sakat/salung". A rapid analytical technique to facilitate the evaluation of the leaves' quality has not been well-established yet. This work aimed therefore to develop a validated analytical technique in order to predict the alpha-glucosidase inhibitory action (AGI) of leaves, applying a Fourier Transform Infrared Spectroscopy (FTIR) fingerprint and utilizing an orthogonal partial least square (OPLS). The dried leaf extracts were prepared by sonication of different ratios of methanol-water solvent (0, 25, 50, 75, and 100% /) prior to the assessment of alpha-glucosidase inhibition (AGI) and the following infrared spectroscopy. The correlation between the biological activity and the spectral data was evaluated using multivariate data analysis (MVDA). The 100% methanol extract possessed the highest inhibitory activity against the alpha-glucosidase (IC 2.83 ± 0.32 μg/mL). Different bioactive functional groups, including hydroxyl (O-H), alkenyl (C=C), methylene (C-H), carbonyl (C=O), and secondary amine (N-H) groups, were detected by the multivariate analysis. These functional groups actively induced the alpha-glucosidase inhibition effect. This finding demonstrated the spectrum profile of the FTIR for the natural herb Jack, further confirming its medicinal value. The developed validated model can be used to predict the AGI of , which will be useful as a tool in the plant's quality control.
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http://dx.doi.org/10.3390/molecules25184161DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7570612PMC
September 2020

Characterization of the structure and analysis of the anti-oxidant effect of microalga Spirulina platensis polysaccharide on Caenorhabditis elegans mediated by modulating microRNAs and gut microbiota.

Int J Biol Macromol 2020 Nov 12;163:2295-2305. Epub 2020 Sep 12.

Engineering Research Centre of Fujian-Taiwan Special Marine Food Processing and Nutrition, Ministry of Education, Fuzhou, Fujian 350002, China; College of Food Science, Fujian Agriculture and Forestry University, Fuzhou 350002, China; Fujian Province Key Laboratory for the Development of Bioactive Material from Marine Algae, Quanzhou Normal University, Quanzhou 362000, China; Key Laboratory of Marine Biotechnology of Fujian Province, Institute of Oceanology, Fujian Agriculture and Forestry University, Fuzhou 350002, China. Electronic address:

The antioxidant activity of Spirulina platensis polysaccharide (SPP) was investigated in Caenorhabditis elegans. Nuclear magnetic resonance, Fourier-transform infrared, multi-angle laser light scattering, and GC-MS were used to identify the structural characteristics of SPP. It was composed of the →2)-α-L-Rhap-(1→, →4)-β-D-Manp-(1→, →6)-β-D-Glcp-(1→, →4)-β-Xylp-(1→, →3)-β-L-Araf-(1→, and →2)-β-L-Fucp-(1→, respectively. The modulation of gut microbiota in C. elegans was determined using 16S rRNA gene high-throughput sequencing. The malondialdehyde (MDA) content was significantly decreased, while the total superoxide dismutase (T-SOD) and reactive oxygen species (ROS) levels were improved after SPP supplementation. The cellular mitochondrial content and apoptosis were significantly down-regulated. The obvious increased levels of the DAF-16 and SKN-1 mRNAs were observed in the SPP-treated group, while the levels of miR-48 and miR-51 were significantly reduced. Moreover, SPP administration significantly increased the abundance of Flavobacterium, Achromobacter, Empedobacter, Anaerolinea, and Pseudoalteromonas of the intestinal flora. Based on these results, S. platensis polysaccharides may be used as a functional food to ameliorate diseases related to oxidative stress.
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http://dx.doi.org/10.1016/j.ijbiomac.2020.09.041DOI Listing
November 2020

Novel Insight into Utilization of Flavonoid Glycosides and Biological Properties of Saffron ( L.) Flower Byproducts.

J Agric Food Chem 2020 Sep 22;68(39):10685-10696. Epub 2020 Sep 22.

Laboratory of Medicinal Plant Biotechnology, College of Pharmacy, Zhejiang Chinese Medical University, Hangzhou, Zhejiang 310053, China.

Saffron ( L.) byproducts are considered as a cheap source of bioactive polyphenolics endowed with potential antioxidant effects. The saffron biowaste is utilized for extraction of flavonoid glycosides and their potential biological properties. The total amount of polyphenolics and polysaccharides was found to be higher in the tepal than in the stamen. The bioactive compounds quercetin-3--sophoroside (Q-3-sop) and kaempferol-3--sophoroside (K-3-sop) were analyzed using high-performance liquid chromatography equipped with a photodiode array detector (HPLC-PDA) and identified by high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). The antioxidant effects were studied using 2,2 diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), ferric ion reducing antioxidant power (FRAP), and oxygen radical absorbance capacity (ORAC); Q-3-sop showed stronger antioxidant effects compared to K-3-sop, crocin-I, and crocin-II. Furthermore, Q-3-sop also inhibited cell apoptosis caused by HO by reducing the levels of cellular reactive oxygen species (ROS). In terms of cytogenetic effects, Q-3-sop revealed no cytogenic effects on onion root meristem cells but chromosomal aberration was observed at the highest dose (200 ppm). Thus, saffron byproducts and its flavonoids could be utilized as natural antioxidant agents with no cytogenetic effects.
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http://dx.doi.org/10.1021/acs.jafc.0c04076DOI Listing
September 2020

A newly isolated strain of Halomonas sp. (HA1) exerts anticancer potential via induction of apoptosis and G/M arrest in hepatocellular carcinoma (HepG2) cell line.

Sci Rep 2020 08 21;10(1):14076. Epub 2020 Aug 21.

Department of Chemistry, Faculty of Science, Menoufia University, Menoufia, 32511, Egypt.

Marine bacterial strains are of great interest for their ability to produce secondary metabolites with anticancer potentials. Isolation, identification, characterization and anticancer activities of isolated bacteria from El-Hamra Lake, Wadi El-Natrun (Egypt) were the objectives of this study. The isolated bacteria were identified as a moderately halophilic alkaliphilic strain. Ethyl acetate extraction was performed and identified by liquid chromatography-mass spectrophotometry (LC-MS-MS) and nuclear magnetic resonance analysis (NMR). Cytotoxicity of the extract was assessed on the HepG2 cell line and normal human peripheral lymphocytes (HPBL) in vitro. Halomonas sp. HA1 extract analyses revealed anticancer potential. Many compounds have been identified including cyclo-(Leu-Leu), cyclo-(Pro-Phe), C17-sphinganine, hexanedioic acid, bis (2-ethylhexyl) ester, surfactin C14 and C15. The extract exhibited an IC of 68 ± 1.8 μg/mL and caused marked morphological changes in treated HepG2 cells. For mechanistic anticancer evaluation, 20 and 40 µg/mL of bacterial extract were examined. The up-regulation of apoptosis-related genes' expression, P53, CASP-3, and BAX/BCL-2 at mRNA and protein levels proved the involvement of P53-dependant mitochondrial apoptotic pathway. The anti-proliferative properties were confirmed by significant G/M cell cycle arrest and PCNA down-regulation in the treated cells. Low cytotoxicity was observed in HPBL compared to HepG2 cells. In conclusion, results suggest that the apoptotic and anti-proliferative effects of Halomonas sp. HA1 extract on HepG2 cells can provide it as a candidate for future pharmaceutical industries.
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http://dx.doi.org/10.1038/s41598-020-70945-8DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7443142PMC
August 2020

Revisiting the Amyloid Cascade Hypothesis: From Anti-Aβ Therapeutics to Auspicious New Ways for Alzheimer's Disease.

Int J Mol Sci 2020 Aug 14;21(16). Epub 2020 Aug 14.

Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

Alzheimer's disease (AD) is the most prevalent neurodegenerative disorder related to age, characterized by the cerebral deposition of fibrils, which are made from the amyloid-β (Aβ), a peptide of 40-42 amino acids. The conversion of Aβ into neurotoxic oligomeric, fibrillar, and protofibrillar assemblies is supposed to be the main pathological event in AD. After Aβ accumulation, the clinical symptoms fall out predominantly due to the deficient brain clearance of the peptide. For several years, researchers have attempted to decline the Aβ monomer, oligomer, and aggregate levels, as well as plaques, employing agents that facilitate the reduction of Aβ and antagonize Aβ aggregation, or raise Aβ clearance from brain. Unluckily, broad clinical trials with mild to moderate AD participants have shown that these approaches were unsuccessful. Several clinical trials are running involving patients whose disease is at an early stage, but the preliminary outcomes are not clinically impressive. Many studies have been conducted against oligomers of Aβ which are the utmost neurotoxic molecular species. Trials with monoclonal antibodies directed against Aβ oligomers have exhibited exciting findings. Nevertheless, Aβ oligomers maintain equivalent states in both monomeric and aggregation forms; so, previously administered drugs that precisely decrease Aβ monomer or Aβ plaques ought to have displayed valuable clinical benefits. In this article, Aβ-based therapeutic strategies are discussed and several promising new ways to fight against AD are appraised.
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http://dx.doi.org/10.3390/ijms21165858DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7461598PMC
August 2020