We evaluated the vasorelaxation effects of formononetin, an isoflavone/phytoestrogen found abundantly in Astragalus mongholicus Bunge, on rat isolated aorta and the underlying mechanisms involved. Cumulative administration of formononetin, genistein, daidzein and biochanin A relaxed phenylephrine-preconstricted aorta. Formononetin and biochanin A caused a similar magnitude of relaxation whereas daidzein was least potent. Mechanical removal of endothelium, L-NAME (100 microM) and methylene blue (10 microM) suppressed formononetin-induced relaxation. Formononetin increased endothelial nitric oxide (NO) synthase (eNOS), but not inducible NO synthase, activity with an up-regulation of eNOS mRNA and p-eNOS(Ser1177) protein expression. In endothelium-denuded preparations, formononetin-induced vasorelaxation was significantly reduced by glibenclamide (3 microM) and iberiotoxin (100 nM), and a combination of glibenclamide (3 microM) plus iberiotoxin (100 nM) abolished the relaxation. In contrast, formononetin-elicited endothelium-independent relaxation was not altered by ICI 182,780 (10 microM, an estrogen receptor (ER alpha/ER beta) antagonist) or mifepristone (10 microM, a progesterone receptor antagonist). In single aortic smooth muscle cells, formononetin caused opening of iberiotoxin-sensitive Ca(2+)-activated K(+) (BK(Ca)) channels and glibenclamide-sensitive adenosine triphosphate (ATP)-dependent K(+) (K(ATP)) channels. Thus, our results suggest that formononetin caused vascular relaxation via endothelium/NO-dependent mechanism and endothelium-independent mechanism which involves the activation of BK(Ca) and K(ATP) channels.
Chinese medicated diet is an everyday practice in China. In this study, 16 commonly used soup making tonic Chinese medicinal herbs were selected for antioxidative capacities by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and ferric reducing antioxidant power (FRAP), and the total phenolic contents of these herbal extracts were measured by the Folin-Ciocalteu method. It confirmed that drinking tonic soups could supplement total antioxidants intake. Amongst the tested herbal extracts, extracts of Canarium album Raeusch., Flos caryophylli and Fructus amomi were found to have the highest antioxidative activities in both DPPH and FRAP assays. Their antioxidative activities were comparable to ascorbic acid and butylated hydroxytoluene. Thus, these herbs are safe and inexpensive sources of natural antioxidants. A significant relationship between the antioxidative effects and total phenolic contents were found, indicating phenolic compounds are the major contributor of antioxidative capacities of these herbs. In addition, a strong correlation between DPPH assay and FRAP assay implied that antioxidants in these herbs were capable of scavenging free radicals and reducing oxidants.
This suggests that the water extract of Da Huang exerts potential anticancer activity through growth inhibition and apoptosis on MCF-7 and A549 cells lines.
Lobeliae chinensis Herba (''ban bian lian''), Rheum officinale Baill. (''da huang''), Sanguisorba officinalis Linn. (''di yu''), Agrimonia pilosa Ledeb. (''xian he cao''), and Paris polyphylla Smith (''zhi hua tou'') are well-known traditional Chinese medicines. They are commonly used in traditional Chinese medicine formulae against cancer. In this study, the antioxidant and anticancer effects of water extracts of these herbs were investigated. In the antioxidant and anticancer studies, water extracts of di yu, xian he cao, and da huang were show to be the most antioxidative and had the highest growth inhibitory effect on human lung adenocarcinoma A549 cell and human breast cancer MCF-7 cell. By comparing their percentage free radical scavenging capacity (SR%) and percentage growth inhibition on A549 and MCF-7 cells, a positive linear relationship between antioxidant activity and anticancer effect of the five herbal water extracts was found. This suggested that the antioxidants of the herbal water extracts might contribute to their anticancer effects on A549 and MCF-7 cells.
Hypercholesterolemia is a major risk factor for the development and progression of cardiovascular diseases including atherosclerosis. A major active ingredient scutellarin, from the plant Erigeron breviscapus was investigated for its hypocholesterolemic and atheroscleroprotective effects (30 and 100 mg/kg/day, p.o.). The serum lipid profile (total cholesterol, triglycerides, high density lipoprotein cholesterol and low density lipoprotein cholesterol) was monitored and aortic functions in Sprague-Dawley rats fed with normal diet, atherogenic diet or atherogenic diet plus oral administration of either scutellarin or simvastatin (a positive control) were tested. It was found that scutellarin markedly attenuated the increased serum total cholesterol induced by atherogenic diet. It caused a significant reduction in the atherogenic index. In addition, scutellarin administration could significantly enhance acetylcholine-induced nitrate/nitrite production, increase the gene expression of endothelial nitric oxide synthase and improve acetylcholine-induced endothelium-dependent vasorelaxation in rat isolated aortas. These data revealed that scutellarin could reduce the atherogenic properties of dietary cholesterol in rats. However, whether scutellarin's atheroscleroprotective potential targets endothelial function directly or indirectly on its antioxidative activity remains to be determined.
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