Search results for "Biflavonoids"
showing 7 items of 7 documents
Natural products as inhibitors of recombinant cathepsin L of Leishmania mexicana.
2015
Cysteine proteinases (cathepsins) from Leishmania spp. are promising molecular targets against leishmaniasis. Leishmania mexicana cathepsin L is essential in the parasite life cycle and a pivotal in virulence factor in mammals. Natural products that have been shown to display antileishmanial activity were screened as part of our ongoing efforts to design inhibitors against the L. mexicana cathepsin L-like rCPB2.8. Among them, agathisflavone (1), tetrahydrorobustaflavone (2), 3-oxo-urs-12-en-28-oic acid (3), and quercetin (4) showed significant inhibitory activity on rCPB2.8 with IC50 values ranging from 0.43 to 18.03 µM. The mechanisms of inhibition for compounds 1–3, which showed Ki values…
Modulation of lipid metabolism and colonic microbial diversity of high-fat-diet C57BL/6 mice by inulin with different chain lengths
2019
Abstract The physicochemical properties, biological functions and microbial degradation of inulins differ according to their degree of polymerization. However, the relationship between inulin activities and its effect on gut microbiota remains unknown. In this study, high fat diet with inulin (1 or 5 g/kg·bw), either with short or long chains groups were administered to different groups of mice (n = 10) for 10 weeks in order to investigate the effect of inulin on the microbial diversity of the animals. Litchi pericarp procyanidins (LPPC) were used for comparison purposes. Furthermore, the lipid metabolism and key regulator genes in mice were determined. The results indicated that natural in…
Direct and indirect measurements of enhanced phenolic bioavailability from litchi pericarp procyanidins by Lactobacillus casei-01
2017
Litchi pericarp procyanidins (LPP) are dietary supplements with high antioxidant activity, but poor oral bioavailability and efficacy. Lactobacillus casei (L. casei-01) can transform flavan-3-ols from litchi pericarp and increase their antioxidant ability; thus, L. casei-01 with LPP was administered to rats for four and eight weeks to study the effect of such a combination on metabolic parameters and on phase II metabolism and detoxification pathways in the liver as an indirect measure for phenolic bioavailability. Our data indicated that the T-AOC of the plasma, the liver GSH-Px and GSH-ST activity, and the expression of UGT and SULT isoforms in the liver of the rats were all enhanced afte…
A hypotensive procyanidin-glycoside from Rhamnus lycioides ssp. lycioides.
1990
A lyophilized hot water extract of the aerial parts of Rhamnus lycioides L. (Rhamnaceae) produced a lowering of systemic arterial blood pressure in normotensive anaesthetized Wistar rats. An activity-guided fractionation of the methanolic extract led to the isolation of a tetrameric procyanidin-glycoside which produced a clear dose-dependent hypotensive response (1.5-6 mg/kg i.v.). This principle was characterized using acid hydrolysis, thiolytic degradation and spectroscopic methods. It consisted of four flavanol units with a 2,3-cis configuration and with a O-beta-d-glucosylpyranoside function on the epicatechin terminal unit. The interflavan linkage was (4-8).
Cytotoxicity of isoflavones and biflavonoids from Ormocarpum kirkii towards multi-factorial drug resistant cancer.
2019
Abstract Background While incidences of cancer are continuously increasing, drug resistance of malignant cells is observed towards almost all pharmaceuticals. Several isoflavonoids and flavonoids are known for their cytotoxicity towards various cancer cells. Purpose The aim of this study was to determine the cytotoxicity of isoflavones: osajin (1), 5,7-dihydroxy-4ˈ-methoxy-6,8-diprenylisoflavone (2) and biflavonoids: chamaejasmin (3), 7,7″-di-O-methylchamaejasmin (4) and campylospermone A (5), a dimeric chromene [diphysin(6)] and an ester of ferullic acid with long alkyl chain [erythrinasinate (7)] isolated from the stem bark and roots of the Kenyan medicinal plant, Ormocarpum kirkii. The m…
COLORECTAL CANCER AND INFLAMMATORY BOWEL DISEASES: EFFECTS ON DIET AND ANTIOXIDANTS
2017
It is well established that oxidative stress is common in inflammatory bowel diseases (IBDs). Accordingly, antioxidants are recommended for treatment. The aim of this study is to compare the effects of antioxidants contained in the various types of tea on symptoms and evolution of IBD and colorectal cancer (CRC). Analysis of the literature revealed that the theaflavin-3, 30-digallate (TFDG) contained in black tea, and epigallocatechin-3-O-gallate (EGCG) contained in green tea have protective effects against oxidative stress. Moreover, these substances are involved in many biochemical processes responsible for inflammation and proliferation of cancer cells. It is documented that both TFDG an…
Morelloflavone, a novel biflavonoid inhibitor of human secretory phospholipase A2 with anti-inflammatory activity
1997
Abstract The flavanonylflavone morelloflavone inhibited secretory phospholipase A 2 (PLA 2 ) in vitro , with a high potency on the human recombinant synovial and bee venom enzymes ( IC 50 = 0.9 and 0.6 μM, respectively). The inhibition was apparently irreversible. In contrast, the compound was inactive on cytosolic PLA 2 activity from human monocytes. Morelloflavone scavenged reactive oxygen species generated by human neutrophils ( IC 50 = 2.7 and 1.8 μM for luminol and lucigenin, respectively) but did not modify cellular responses such as degranulation or eicosanoid release. This biflavonoid exerted anti-inflammatory effects in animal models, with a potent inhibition of 12-O-tetradecanoylp…