Ghada Ahmed Fawzy

Antioxidant and urease inhibitory C-glycosylflavonoids from Celtis africana.

Two new C-glycosylflavonoids celtisides A (1) and B (2) have been isolated from n-butanol-soluble fraction of Celtis africana, along with five known C-glycosylflavonoids vitexin (3), orientin (4), isoswertiajaponin (5), isoswertisin (6), and 2″-O-rhamnosyl vitexin (7) reported for the first time from this species. Their structures were assigned from 1D and 2D NMR spectra. These compounds were investigated for biological activities and showed significant antioxidant and urease inhibitory activities.

Antidiabetic and Antioxidant Activities of Major Flavonoids of Cynanchum acutum L. (Asclepiadaceae) Growing in Egypt

Seven flavonoids were isolated from the butanol fraction of the methanolic extract of the aerial parts of Cynanchum acutum L. (Asclepiadaceae). All of which have been isolated for the first time from the genus Cynanchum. Their structures were established as quercetin 3-O-β-galacturonopyranoside (1), quercetin 7-O-β-glucopyranoside (2), tamarixtin 3-O-β-galacturonopyranoside (3), kaempferol 3-O-β-galacturonopyranoside (4), 8-hydroxyquercetin 3-O-β-galactopyranoside (5), tamarixtin 3-O-α-rhamnopyranoside (6), and tamarixtin 7-O-α-arabinopyranoside (7) on the basis of their chromatographic properties, chemical and spectroscopic data. The major isolated flavonoids 1, 2 and 3 were found to exhibit significant antioxidant and antidiabetic activities (by measuring blood glucose and insulin levels). This is the first report about the antioxidant and antidiabetic activities of compounds 1 - 3.

Chemical composition and biological evaluation of essential oils of Pulicaria jaubertii.

Background: The present study reports and compares the results of Gas Chromatographic-Mass analyses of Pulicaria jaubertii leaf (P-1) and root (P-2) essential oils, as well as their in vitro antimicrobial and cytotoxic activities. Materials and Methods: The chemical composition of P-1 and P-2 essential oils of P. jaubertii, was investigated by GC-MS. Moreover, the essential oils were evaluated for their antimicrobial activity using the broth micro-dilution assay for minimum inhibitory concentrations (MIC). The crystal violet staining method (CVS) was used for evaluation of their cytotoxic activity on HEPG-2 and MCF-7 human cell lines. Results: This investigation led to the identification of 16 constituents in P-1, and 23 constituents in P-2, representing 99.92% and 94.74% of the oils respectively. Oxygenated monoterpenes were found to be the major group in both P-1 (99.47%) and P-2 (89.88%). P-1 consists almost entirely of p-Menth-6-en-2-one (Carvotanacetone, 98.59%). P-2 is characterized by high contents of each of Dimethoxydurene (38.48%), Durenol (26.89%) and 2’,4’-Dimethoxy-3’-methylacetophenone (20.52%). Both oils showed moderate antimicrobial activity against the Gram-positive strains and C. albicans. However, no activity was shown against Gram-negative bacteria. P-1 showed a significant cytotoxic activity against both MCF-7 and HEPG-2 (IC50 = 3.8 and 5.1 μg/ml, respectively), while P-2 showed selective cytotoxic activity against MCF-7 cell line (IC50 = 9.3 μg/ml). Conclusion: The potent cytotoxic and moderate antimicrobial activities of P-1 may be attributed to its high content of Carvotanacetone.

Determination of Luteolin and Apigenin in Herbs by Capillary Electrophoresis with Diode Array Detection

Capillary electrophoresis with a diode array detector was employed for the determination of luteolin and apigenin in plant extracts. The experimental factors affecting the elution of the analytes were carefully optimized. The final analysis was achieved utilizing a fused silica capillary (58 cm effective length, 75 μm ID) and a background electrolyte solution consisting of borax buffer (20 mM, pH 10.0) and methanol (90: 10, v/v) with a 23 kV driving voltage and detection at 210 nm. The method was fully validated as per the guidelines of the International Conference on Harmonization for Analytical Procedures. The relationship between peak area and concentration was linear between 3 and 800 μg/mL for both compounds with detection limits of 1.05 for luteolin and 0.53 μg/mL for apigenin. The method was employed for the determination of the analytes in extracts of thyme and parsley. Both compounds were resolved from interfering peaks that were present in the extracts. Recovery studies were performed by fortifying the extracts with standards and demonstrated good accuracy with recovery values between 97.29 and 104.88% for luteolin and 96.89 and 105.18% for apigenin. Thyme and parsley were shown to contain high concentrations of luteolin and apigenin.

Hepatoprotective constituents of Torilis radiata Moench (Apiaceae)

An investigation of the aqueous ethanolic extract (AE) of the aerial parts of Torilis radiata Moench yielded two triterpenes (lupeol acetate (1) and α-amyrin (2)), a sterol (spinasterol (3)) from its n-hexane fraction (HF), a flavone (acacetin (4)), a coumarin (scopoletin (5)), a phenolic acid (ferulic acid (6)) from the chloroform fraction (CF) and a flavone glycoside (luteolin-7-O-glucoside (7)) from the n-butanol fraction (BF). The hepatoprotection of the AE and its fractions was assessed in terms of the reduction in histological damage, accompanied by restoration of the liver enzymes (alanine amino transferase (ALT), aspartate amino transferase (AST), lactate dehydrogenase (LDH)), a reduction in the inflammatory markers (tumour necrosis-α (TNF-α), nitric oxide (NO), N-acetyl-β-D-glucosaminidase (NAG) and myloperoxidase (MPO) in serum) and restoration of the oxidant balance by decreasing the serum and hepatic malondialdehyde (MDA) levels, along with increasing the activity of hepatic catalase (CAT), glutathione peroxidase (GSHPx) and the non-enzymatic antioxidant glutathione (GSH).

New flavonol glycosides from the leaves of Caragana brachyantha

Two new flavonol glycosides, brachysides C and D, together with three known flavonol glycosides, were isolated from the leaves of Caragana brachyantha. The structures of brachysides C and D were elucidated on the basis of detailed spectroscopic analysis as quercetin 5-O-[α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranoside]-7-O-[α-l-rhamnopyranoside] and quercetin 5-O-[α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranoside]-7-O-[α-l-rhamnopyranoside]-4′-O-[α-l-rhamnopyranoside], respectively. The presence of flavonol tetra- and triglycosides bearing a sugar moiety at position 5 was the first report from this genus Caragana.

Bioactivity and chemical characterization of Acalypha fruticosa Forssk. growing in Saudi Arabia

Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely 2-methyl-5,7-dihydroxychromone 5-O-β-d-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect.

Anticancer activity of flavane gallates isolated from Plicosepalus curviflorus.

Background: Previous investigation of the methanol extract of Plicosepalus curviflorus leaves led to the isolation of two new flavane gallates (1, 2), together with other compounds including quercetin (3). The stems of P. curviflorus are used traditionally for the treatment of cancer in Yemen. Objective: The aim of this study was to evaluate the anticancer activity of the plant methanol extract as well as isolated compounds (1-3). Materials and Methods: The human cancer cell lines used were; MCF-7, HepG-2, HCT-116, Hep-2, HeLa and normal, Vero cell line using the Crystal Violet Staining method (CVS). Results: Quercetin (3) possessed the highest anticancer effect against all five cell lines (IC50 ranging from 3.6 to 16.2 μg/ml). It was followed by 2S, 3R-3, 3′, 4′, 5, 7-pentahydroxyflavane-5-O-gallate (1), with IC50 ranging from 11.6 to 38.8 μg/ml. The weakest anticancer activity was given by 2S, 3R-3,3′,4′,5,5′,7-hexahydroxyflavane-3′,5-di-O-gallate (2) with IC50 ranging from 39.8 to above 50 μg/ml, compared to vinblastine sulphate as reference drug. Colon, liver and breast cell lines seemed to be more sensitive to the tested compounds than the cervical and laryngeal cell lines. Concerning the cytotoxic effect on Vero cell line, the pentahydroxyflavane-5-O-gallate (1) showed the highest IC50 ( 138.2 μg/ml), while quercetin exhibited the lowest IC50 to Vero cells (30.5 μg/ml), compared to vinblastine sulphate as reference drug (IC50: 39.7 μg/ml). Conclusion: The results suggest the possible use of compounds 1 and 3 as anticancer drugs especially against colon and liver cancers.

Nepeta deflersiana attenuates isoproterenol-induced myocardial injuries in rats: Possible involvement of oxidative stress, apoptosis, inflammation through nuclear factor (NF)-κB downregulation

BACKGROUND Nepeta deflersiana (Lamiaceae) is a perennial herb used in the Saudi and Yemeni folk medicine as an anti-inflammatory, carminative, and antirheumatic agent. PURPOSE This study explores the phytochemistry of the plant and the cardioprotective effect of N. deflersiana ethanolic extract (NDEE) against isoproterenol (ISP)-induced myocardial injury in rats. DESIGN/METHODS Cardiac function, serum cardiac enzymes, myocardial antioxidants, inflammatory, and apoptotic biomarkers, and histopathological parameters were studied in ISP-injured Wistar rat heart tissues. RESULTS To the best of our knowledge, this is the first study to report the isolation of nine secondary metabolites from this plant: 1α-hydroxy-7α,14α,18-triacetoxy-isopimara-8,15-diene (1), β-sitosterol (2), lupeol (3), ursolic acid (4), 2,3-dihydroxy ursolic acid (5), caffeic acid (6), methyl rosmarinate (7), rosmarinic acid (8), and an irridoid glucoside 8-epi-7-deoxyloganic acid (9). To explain the mechanisms underlying the cardioprotective effect of NDEE, we evaluated the redox-sensitivity of NDEE in ISP-induced cardiac injury. The oral administration of NDEE (50 and 100 mg/kg b.w) prevented the depletion of endogenous antioxidants (CAT, SOD, NP-SH, and NO) and myocyte injury marker enzymes and inhibited lipid peroxidation (MDA, MPO). Moreover, NDEE downregulated the expression of pro-inflammatory cytokines (TNFα, IL-6, and IL-10) and apoptotic markers (caspase-3 and Bax) and upregulated the anti-apoptotic protein Bcl2. Furthermore, NDEE pretreatment significantly downregulated cardiac NF-κB (p65) expression, NF-κB-DNA binding activity, and MPO activity. Histological data showed that NDEE pretreatment reduced myonecrosis, edema, and infiltration of inflammatory cells and restored the architecture of cardiomyocytes. CONCLUSION NDEE demonstrated strong antioxidant, cardioprotective, anti-inflammatory, and anti-apoptotic potential against myocardial damage. This further endorses the use of N. deflersiana in Yemeni folk medicine against cardiovascular diseases.

Antidiarrheal and Antispasmodic Activities of Buddleja polystachya are Mediated Through Dual Inhibition of Ca(++) Influx and Phosphodiesterase Enzyme.

This study describes the antidiarrheal and antispasmodic activities of the hydro‐alcoholic extract of Buddleja polystachya (Bp.Cr) with possible mode of action explored along with activity‐directed fractionation. Bp.Cr and its aqueous (Bp.Aq) and organic fractions, petroleum ether (Bp.Pet), dichloromethane (Bp.DCM), ethylacetate (Bp.EtAc) and butanol (Bp.But), were tested using the in‐vivo and in‐vitro assays. The crude extract (100–300 mg/kg) showed 20 and 60% protection of castor oil‐induced diarrhea in mice. In isolated rabbit jejunum, Bp.Cr like papaverine inhibited spontaneous and high K+ (80 mM)‐induced contractions equi‐potently. In guinea‐pig ileum, Bp.Cr showed a moderate spasmogenic effect. The activity‐directed fractionation revealed that the spasmolytic activity was concentrated in the organic fractions and spasmogenic component in the aqueous fraction. Amongst the organic fractions, BP.DCM and Bp.Pet inhibited spontaneous and high K+‐induced contractions equi‐potently, while Bp.But, like verapamil was more potent against high K+. The crude extract and its organic fractions caused rightward shift in the Ca++‐concentration response curves (CRCs), similar to verapamil, and all except Bp.But potentiated the isoprenaline‐inhibitory CRCs to the left, similar to papaverine. The results of this study indicate that the crude extract of B. polystachya possesses antidiarrheal and antispasmodic activities, mediated possibly through dual inhibition of Ca++ influx and phospodiesterase enzyme. Copyright