A new acylated flavone glycoside, in vitro antioxidant and antimicrobial activities from Saudi Diospyros mespiliformis Hochst. ex A. DC (Ebenaceae) leaves.

Phytochemical investigation of Diospyros mespiliformis leaves resulted in the isolation of new acylated flavone isoscutellarein 7-O-(4'''-O-acetyl)-ß-allopyranosyl(1''' â†’ 2'')-ß-glucopyranoside (1), along with eight known flavonoid metabolites, luteolin 3',4',6,8-tetramethyl ether (2), luteolin 4'-O-ß-neohesperidoside (3), luteolin 7-O-ß-glucoside (4), luteolin (5), quercetin (6), quercetin 3-O-ß-glucoside (7), quercetin 3-O-α-rhamnoside (8), and rutin (9). Their structures were identified by analysis of spectroscopic (UV, NMR, and MS) data, as well as by acid hydrolysis for the isolated glycosides. The antioxidant activity of D. mespiliformis metabolites was determined by the DPPH radical-scavenging assay. The new acylated flavone (1) and flavonol O-rhamnoside (8) displayed the highest antioxidant activities with IC50 values 15.46 and 12.32 µg/mL, respectively, with respect to the antioxidant ascorbic acid (IC50 value 10.62 µg/mL). In addition, the isolated flavonoids were evaluated against four human pathogenic bacteria where the methylated flavone (2) exhibited potent activity against Escherichia coli with inhibition zone 34 mm, and mild activity of flavonol O-rhamnoside (8) against Staphylococcus aureus with MIC value 9.77 µg/mL. According to the MBC/MIC ratio, the antibacterial activity of the isolated flavonoids was considered flavonoid 2 is bactericidal nature against S. aureus, and flavonoids 3 and 4 are bactericidal against E. coli.

Phytochemical constituents and protective efficacy of Schefflera arboricola L. leaves extract against thioacetamide-induced hepatic encephalopathy in rats.

CONTEXT: Hepatic encephalopathy (HE) is a severe neuropsychiatric syndrome resulting from liver failure. OBJECTIVE: To evaluate the protective effect of Schefflera arboricola L. leaves methanol extract against thioacetamide (TAA) induced HE in rats. MATERIALS AND METHODS: GC/MS, LC-ESI-MS, and the total phenolic and flavonoid contents were determined. The methanol extract was orally administrated (100 and 200 mg/kg body weight) for 21 days. TAA (200 mg/kg body weight) was given intraperitoneally on day 19 and continued for three days. The evaluation was done by measuring alanine aminotransferase (ALT), alkaline phosphatase (ALP), ammonia, reduced glutathione (GSH), malondialdehyde (MDA), nitric oxide (NO), tumour necrosis factor-alpha (TNF-α), toll-like receptor 4 (TLR4), interleukin-1 beta (IL-1ß), interlukin-6 (IL-6), cyclooxygenase 2 (COX2), B cell lymphoma 2 (BCL2), alpha-smooth muscle actin (α-SMA), and the cluster of differentiation 163 (CD163). The histological features of the liver and brain were conducted. RESULTS: Forty-five compounds were identified from the n-hexane fraction, while twenty-nine phenolic compounds were determined from the methanol extract. Pre-treatment with the plant extract returned most of the measurements under investigation to nearly normal. CONCLUSION: Due to its richness with bioactive compounds, Schefflera arboricola L. leaves methanolic extract succeeded to exert anti-fibrotic, anti-inflammatory, and antioxidants properties in TAA-induced HE in rats with more efficacy to its high protective dose.

Bioactive compounds from Matricaria chamomilla: structure identification, in vitro antiproliferative, antimigratory, antiangiogenic, and antiadenoviral activities.

During our exploring the anticancer activity of some medicinal plants and their major metabolites, the aerial parts of the Egyptian Matricaria chamomilla (flowers and stems) were studied. GC-MS analysis of the organic soluble extracts of the flowers and stems fractions revealed the presence of 43 and 45 compounds, respectively. Individual chromatographic purification of the flowers and stems' extracts afforded three major compounds. Structures of these compounds were identified by 1D- and 2D-NMR and HRESI-MS spectroscopic data as bisabolol oxide A (1) and (E)-tonghaosu (2) (as mixture of ratio 2:1) from the flowers extract, meanwhile apigenin-7-ß-d-glucoside (3) from the stems fraction. Biologically, the chamomile extracts announced significant antiproliferative activities exceeded in potency by ∼1.5 fold in case of the stem, recording GI50 13.16 and 17.04 µg/mL against Caco-2 and MCF-7, respectively. Both fractions were approximately equipotent against the migration of the same cell type down to 10 µg/mL together, compounds 1, 2 but not 3, showed considerable growth inhibition of the same cells at GI50 13.36 and 11.83 µg/mL, respectively. Interestingly, they were able to suppress Caco-2 colon cancer cells migration at 5.8 µg/mL and potently inactivate the VEGFR2 angiogenic enzyme (1.5-fold relative to sorafenib. The obtained compounds and corresponding chamomile extracts were evaluated against Adeno-7 virus, revealing that both chamomiles' extracts (flowers and stems) and their corresponding obtained compounds (1-3) were potent in their depletion to the Adeno 7 infectivity titer, however, the flower extract and compounds 1-2 were more effective than those of the stem extract and its end-product (3).

Bioactive compounds and therapeutic role of Brassica oleracea L. seeds in rheumatoid arthritis rats via regulating inflammatory signalling pathways and antagonizing interleukin-1 receptor action.

CONTEXT: Rheumatoid arthritis (RA) is a chronic, progressive autoimmune disease characterized by aggressive and systematic polyarthritis. OBJECTIVE: The present study aimed to isolate and identify the phenolic constituents in Brassica oleracea L. (Brassicaceae) seeds methanolic extract and evaluates its effect against rheumatoid arthritis in rats referring to the new therapy; interleukin-1 receptor antagonist (IL-1RA). MATERIALS AND METHODS: The GC/MS profiling of the plant was determined. Arthritis induction was done using complete Freund's adjuvant. Arthritis severity was assessed by percentage of edema and arthritis index. IL-1 receptor type I gene expression, interleukin-1ß (IL-1ß), oxidative stress markers, protein content, inflammatory mediators, prostaglandin-E2 (PGE2), genetic abnormalities and the histopathological features of ankle joint were evaluated. RESULTS: For the first time twelve phenolic compounds had been isolated from the seeds extract. Treatment with extract and IL-1RA improved the tested parameters by variable degrees. CONCLUSIONS: RA is an irreversible disease, where its severity increases with the time of induction. Brassica oleracea L. seeds extract is considered as a promising anti-arthritis agent. IL-1 RA may be considered as an unusual therapeutic agent for RA disease. More studies are needed to consider the seeds extract as a nutraceutical agent and to recommend IL-1RA as a new RA drug.

Phytochemical investigation and biological studies of Bombax malabaricum flowers.

In this study, extracts of the flowers of the folk medicinal plant Bombax malabaricum DC were biologically and chemically screened. Chemical constituents in the n-hexane fraction from the flowers of B. malabaricum DC were investigated using gas-liquid chromatography (GLC) analysis, affording 14 compounds, including cholesterol, stigmasterol, campesterol and α-amyrin, while the residual 10 compounds are hydrocarbons. GLC analysis of the fatty acid (FA) esters established the majority abundance of the saturated FA over their unsaturated analogues. The polar methanol fraction afforded seven flavones: vicenin 2 (1), linarin (2), saponarin (3), cosmetin (4), isovitexin (5), xanthomicrol (6) and apigenin (7). Structures 1-7 were established by intensive studies of various spectral data (H-NMR, mass spectroscopy and UV) and comparison with authentic samples. Compounds 1-7 are described here for the first time from this plant. Extracts of n-hexane and methanol exhibited significant antioxidant and antimicrobial activities.