Protective Effects of a Polyphenolic Phytochemical Quercetin against Oxidative Dysfunctions in Rats.

Background: Quercetin hastraditionally been used in various oxidative and urinary tract dysfunctions. Thecurrent project is consequently set to evaluate the defensive efficacy ofQuercetin against potassium bromate (KBrO3) induced testiculartissue oxidative dysfunctions through biochemical, hormonal, and genotoxicmarkers. Methods: To observe theprotective efficacy of Quercetin against urinogenital oxidative dysfunction inrats, thirty six albino male rats were divided into six groups. Protectiveefficacies of Quercetin were checked on reproductive hormonal levels,antioxidant enzyme activities, lipids peroxidation (LP), and DNA damages. Results: Potassium bromate exposure in experimentalanimals caused a reduction in the activities of antioxidant enzymes and disturbedhormonal secretions while enhancing the peroxidation of lipids andfragmentations of DNA. Cotreatment of Quercetin considerably (P<0.01)reversed these abnormalities with admiration to levels of hormones, antioxidantenzymes activities, and peroxidations of lipids secure to those seen inuntreated rats. (P < 0.01). Conclusion: The findings of the current project revealedthat various doses of Quercetin are able to keep the testicular organ fromabnormal free radical dysfunctions. These improvements might be due to theantioxidant ability of polyphenolic bioactive constituent, i.e., Quercetin.

Carduus edelbergii Rech. f. Mediated Fabrication of Gold Nanoparticles; Characterization and Evaluation of Antimicrobial, Antioxidant and Antidiabetic Potency of the Synthesized AuNPs.

Background: Due to the high expense, less effectiveness and more side effects of available synthetic medicine, the researchers and communities are focusing on phyto-based natural bioactive compounds, which are considered safer for the treatment of syndromes and chronic diseases. Aim: The current project was aimed to determine the phytochemicals constituents available in the aerial parts of methanol extract of Carduus edelbergii via GC-MS, fabrication of AuNPs mediated with the mentioned extract; characterization and evaluation of antimicrobial, antioxidant and antidiabetic potency of the synthesized AuNPs. Methods: Confirmation of green synthesis of AuNPs, functional groups responsible for the reduction in Au+, size and crystallinity, morphology and quantity of gold (Au) were carried out by Ultraviolet-Visible (UV-Vis) spectroscopy, Transform Infrared (FTIR) spectroscopy, Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD) and dispersive X-ray (EDX), respectively, whereas in vitro antioxidant characteristics were assessed by DPPH and ABTS assays. Wistar albino rats were used to test the anti-diabetic properties of the methanol extract and AuNPs. Results: GC-MS revealed that the diluted methanol extract of Carduus edelbergii consists of about 19 chemical constituents. Among the identified compounds, the 13-Docosenoic acid, methyl ester, (Z)­has the highest concentration (38.16%), followed by 9-Octadecenoic acid, methyl ester, (E)­(15.72%) and n-Hexadecanoic acid (15.07%). Methanol extract and its fabricated nanoparticles showed significant antioxidant and antimicrobial activities. In vivo antidiabetic study revealed a noteworthy (p < 0.05) decline in body weight and HDL and elevated concentration of blood glucose, bilirubin, creatinine, urea, triglyceride, VLDL, LDL, ALP, ALT and AST in diabetic control. The said changes were recovered significantly (p < 0.05) by treatment of diabetic rats with methanol extract (150 and 300 mg/Kg BW) and AuNPs of Carduus edelbergii (5 and 10 mg/Kg BW). Conclusion: The green synthesized AuNPs exhibit significant antioxidant, antimicrobial and antidiabetic characteristics.

Isolation, Characterization and In Silico Studies of Secondary Metabolites from the Whole Plant of Polygala inexpectata Pesmen & Erik.

Polygala species are frequently used worldwide in the treatment of various diseases, such as inflammatory and autoimmune disorders as well as metabolic and neurodegenerative diseases, due to the large number of secondary metabolites they contain. The present study was performed on Polygala inexpectata, which is a narrow endemic species for the flora of Turkey, and resulted in the isolation of nine known compounds, 6,3'-disinapoyl-sucrose (1), 6-O-sinapoyl,3'-O-trimethoxy-cinnamoyl-sucrose (tenuifoliside C) (2), 3'-O-(O-methyl-feruloyl)-sucrose (3), 3'-O-(sinapoyl)-sucrose (4), 3'-O-trimethoxy-cinnamoyl-sucrose (glomeratose) (5), 3'-O-feruloyl-sucrose (sibiricose A5) (6), sinapyl alcohol 4-O-glucoside (syringin or eleutheroside B) (7), liriodendrin (8), and 7,4'-di-O-methylquercetin-3-O-ß-rutinoside (ombuin 3-O-rutinoside or ombuoside) (9). The structures of the compounds were determined by the spectroscopic methods including 1D-NMR (1H NMR, 13C NMR, DEPT-135), 2D-NMR (COSY, NOESY, HSQC, HMBC), and HRMS. The isolated compounds were shown in an in silico setting to be accommodated well within the inhibitor-binding pockets of myeloperoxidase and inducible nitric oxide synthase and anchored mainly through hydrogen-bonding interactions and π-effects. It is therefore plausible to suggest that the previously established anti-inflammatory properties of some Polygala-derived phytochemicals may be due, in part, to the modulation of pro-inflammatory enzyme activities.

Gas chromatography-mass spectrometry metabolic profiling, molecular simulation and dynamics of diverse phytochemicals of Punica granatum L. leaves against estrogen receptor.

Introduction: Breast cancer is the most common type of cancer globally and its treatment with many FDA-approved synthetic drugs manifests various side effects. Alternatively, phytochemicals are natural reserves of novel drugs for cancer therapy. Punica granatum commonly known as pomegranate is a rich source of phytopharmaceuticals. Methods: The phytoconstituents of Punica granatum leaves were profiled using GC-MS/MS in the present work. Cytoscape-assisted network pharmacology of principal and prognostic biomarkers, which are immunohistochemically tested in breast cancer tissue, was carried out for the identification of protein target. Followed by, rigorous virtual screening of 145 phytoconstituents against the three ER isoforms (α, ß and γ) was performed using Discovery Studio. The docked complexes were further evaluated for their flexibility and stability using GROMACS2016 through 50 ns long molecular dynamic simulations. Results: In the current study, we report the precise and systematic GC-MS/MS profiling of phytoconstituents (19 novel metabolites out of 145) of hydromethanolic extract of Punica granatum L. (pomegranate) leaves. These phytocompounds are various types of fatty acids, terpenes, heterocyclic compounds and flavonoids. 4-coumaric acid methyl ester was identified as the best inhibitor of ER isoforms with drug-likeness and no toxicity from ADMET screening. γ-ligand binding domain complex showed the best interactions with minimum RMSD, constant Rg, and the maximum number of hydrogen bonds. Conclusion: We conclude that 4-coumaric acid methyl ester exhibits favourable drug-like properties comparable to tamoxifen, an FDA-approved breast cancer drug and can be tested further in preclinical studies.

Phytochemical Analysis of Anvillea garcinii Leaves: Identification of Garcinamines F-H and Their Antiproliferative Activities.

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lung and liver diseases, digestive problems, and as an antidiabetic agent. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of three undescribed guaiane sesquiterpene derivatives, named garcinamines F-H, characterized by the presence of an amino acid unit, along with five known sesquiterpene lactones (garcinamines B-E and 9ß-hydroxyparthenolide). The structures of the new compounds were established using spectroscopic (1D and 2D NMR) and spectrometric methods (ESIMS). Garcinamine H possesses a double bond at the Δ1,10 position, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antiproliferative activity of the isolated sesquiterpenes was screened against three different cancer cell lines, and 9ß-hydroxyparthenolide and garcinamines C and D displayed significant effects against lung carcinoma (A549), colon carcinoma (LoVo), and breast carcinoma (MCF7) cell lines.

Development and validation of a high-performance thin-layer chromatographic method for the quantitative analysis of vitexin in Passiflora foetida herbal formulations.

The aim of this study is the development of validated HPTLC method for the quantification of vitexin from Passiflora foetida commercial herbal formulations. The developed method was validated, in accordance with ICH guidelines for precision, accuracy, specificity and robustness. The plate was developed using ethyl acetate:methanol:water:formic acid 30:4:2:1(%, v/v/v/v) on 20 × 10 cm glass coated silica gel 60 F254 plates and the developed plate was scanned and quantified densitometrically at λ = 340 nm. Linear regression analysis revealed a good linear relationship between peak area and amount of vitexin in the range of 100-700 ng/spot. The amount of vitexin in nine commercial herbal formulations was successfully quantified by the developed HPTLC method. The developed and validated high performance thin layer chromatographic method offers a new sensitive and reliable tool for quantification of vitexinin in various herbal formulations containing Passiflora foetida.

Antimicrobial guaianolide sesquiterpenoids from leaves of the Saudi Arabian plant Anvillea garcinii.

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lungs and liver diseases, digestive problems, and as an anti-diabetic. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of two undescribed guaiane sesquiterpene lactones (1-2), along with four known germacranolides (3-6). The structures of the new compounds were established using spectroscopic (1D, 2D NMR) and spectrometric methods (ESIMS). Compounds 1 and 2 were shown to possess hydroxyl substituents at position 9, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antimicrobial activity of 1-6 was screened against five different gram-positive/negative bacteria and the fungi Candida albicans and C. parapsilosis. Compounds 1 and 2 displayed remarkable antifungal effect against C. albicans and C. parapsilosis and potent antibacterial activities against Staphylococcus aureus.

HPTLC method for simultaneous determination of ascorbic acid and gallic acid biomarker from freeze dry pomegranate juice and herbal formulation.

A new rapid, simple, sensitive and high performance thin layer chromatography (HPTLC) has been established for the simultaneous determination of ascorbic acid and gallic acid in the freeze-dried pomegranate fruit juice and herbal formulation. HPTLC method was carried out using ethyl acetate: acetone: water: formic acid, 10:6:2:2 (%, v/v/v/v)) on 20 × 10 cm glass coated silica gel 60 F254 plates and scanned at 254 nm for ascorbic acid and gallic acid. Ascorbic acid and gallic acid in the freeze-dried pomegranate fruit juice were identified by comparing their single spot at Rf = 0.54 ±â€¯0.02 and Rf = 0.83 ±â€¯0.01 respectively. The value of regression equation (r2 ≥ 0.9992) revealed a good linear relationship between peak area and amount of ascorbic acid and gallic acid in the range of 100-800 ng/band. The method was validated for precision, accuracy, robustness LOD and LOQ. The method proposed can be useful for routine determination of ascorbic acid and gallic acid in various crude as well as herbal formulations as a quality control tool.

Hepatoprotective and cytotoxic activities of Anvillea garcinii and isolation of four new secondary metabolites.

Anvillea garcinii is a medicinal plant traditionally used for the treatment of dysentery, gastrointestinal troubles, hepatitis, lung disease, colds, digestive problems and pulmonary affections and in liver diseases. Four new sesquiterpene lactones, garcinamines A-D, along with seven known compounds, were isolated from the leaves of A. garcinii. This is the first report of the isolation of amino acid analogues of parthenolide-type sesquiterpene lactones from the family Asteraceae. Total ethanol extract of leaves as well as the chloroform and n-butanol fractions were tested for their hepatoprotective effect using the carbon tetrachloride liver toxicity model. The chloroform fraction, at a dose of 400 mg/kg, demonstrated a significant hepatoprotective effect comparable to silymarin in all serum and tissue parameters. The cytotoxicity of all extracts and compounds were evaluated against five human cancer cell lines: MCF-7, HCT-116, HepG2, Hela and A-549. The results indicated that the chloroform and n-butanol fractions and compounds 3, 4, 7 and 8 displayed significant cytotoxic activity against these cell lines.

Rhanterium epapposum Oliv. essential oil: Chemical composition and antimicrobial, insect-repellent and anticholinesterase activities.

The essential oil (EO) of the aerial parts of Rhanterium epapposum Oliv. (Asteraceae), was obtained by hydrodistillation. The oil was subsequently analyzed by both GC-FID and GC-MS, simultaneously. Forty-five components representing 99.2% of the oil composition were identified. The most abundant compounds were camphene (38.5%), myrcene (17.5%), limonene (10.1%) and α-pinene (8.7%). Referring to the ethnobotanical utilization, an insecticidal assay was performed, where the oil repelled the yellow fever mosquito Aedes aegypti L. at a minimum effective dose (MED of 0.035 ± 0.010 mg/cm2) compared to the positive control DEET (MED of 0.015 ± 0.004 mg/cm2). Additionally, the in vitro antimicrobial activity against a panel of pathogens was determined using a microdilution method. The acetyl- and butyrylcholine esterase inhibitory activities were measured using the colorimetric Ellman method. The bioassay results showed that the oil was rather moderate in antimicrobial and cholinesterase inhibitions when compared to the standard compounds.

Comparative anti-inflammatory and hepatoprotective activities of Astragalus gummifer Labill herb and roots in rats.

BACKGROUND: The Astragalus gummifer (F. Fabaceae), herb and roots were studied for anti-inflammatory and hepatoprotective activities. MATERIALS AND METHOD: The alcoholic extracts of Astragalus gummifer (F. Fabaceae), herb (AGHE), and roots (AGRE), were used for anti-inflammatory and hepatoprotective activities in Wister rats. The effects of AGHE and AGRE were compared with the standard drugs Phenylbutazone and silymarin, for anti-inflammatory and hepatoprotective activities respectively. RESULT: Both extracts showed significant anti-inflammatory activity (P< 0.001). AGRE showed comparatively more significant hepatoprotective activity (P< 0.001), than AGHE (P< 0.05); at doses of 250 and 500 mg/kg body weight as manifested by lowering the serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), gamma-glutamyl transpeptidase (GGT), alkaline phosphatase (ALP), and total bilirubin. The hepatoprotective activity was, also, supported by total protein (TP), malondialdehyde (MDA), nonprotein sulfhydryls (NP-SH), and histo-pathological studies of liver tissue. DISCUSSION: To the best of our knowledge, this is the first report of the anti-inflammatory and hepatoprotective activities of Astragalus gummifer. The results of present studies indicated that both AGHE and AGRE can be used in inflammatory conditions, while investigation supports the use of AGRE in cases that hepatoprotection are required in the hepatotoxic conditions. More supportive studies are required before clinical recommendation.