Herbs Carry The Board Owned By A Preliminary Study Of Anti-hbv And Hepatoprotective Activity

At present the number of hepatitis B patients and carriers increases year-by-year in the world especially in our country. However human beings have not yet found highly effective anti-HBV drugs after half a century. For the shortcomings of first-line clinical anti-HBV drugs such as side effects , drug resistance and expensive and so on, researchers have tried to find a new generation of anti-HBV drugs or leading compounds from natural medicines and traditional Chinese herbs, which have high efficiency and low toxicity, new structures and multi-target points.In the complex pathogenesis of hepatitis B virus, immunological liver injury occupies a decisive position. When the immune system is unable to get rid of HBV, the strong cellular immune response, humoral immune response will lead to immune hepatic injury. Therefore we need to consider impacts when new anti-HBV drugs act on the host's immune system.Polygonum perfoliatum L.is the potential one with anti-HBV activity which we screened out from 24 kinds Chinese medicines. During literature investigation, it is often used to treat diseases like mastitis, whooping cough, prostate cancer et al. Modern pharmacological researchs indicate that it has activities of antiviral, anti-tumor and so on. In order to better research this phant, we will preliminary study the following three aspects: chemical compositions which can anti-HBV and protect liver and lower enzymes, pharmacology effects , the immune regular functions.(1)The 70% ethanol extract of Polygonum perfoliatum L. was isolated by chromatography on silica gel and Sephadex LH-20, recrystallization. The structures of compounds were identified by physicochemical properties and spectral analyses(MS and NMR). Eighteen compounds were isolated and Fourteen compounds identified as quercetin(1), isorhamnetin(2), hyperoside(3), quercitrin(4), protocatechuic acid(5), gallic acid(6), ellagic acid(7), 3,3′-di-O-methyl ellagic acid(8), 1-O-galloyl-β-D-gluc- ose(9), mucic acid dimethyl ester-2-O-gallate (10), ethyl caffeate(11),β-sitosterol (12),β-daucosterol (13), mucic acid dimethyl ester(14). Compounds 10 and 14 were isolated from the genus Polygonum for the first time. Compounds 2,3,7,8,9,11 were obtained from the plant for the first time.(2)Choose HepG2 2.2.15 cell as model and the secretive changes of HBeAg and HBsAg as the activity-evaluating marker in vitro. The experimental results show that the ethanol, n-butanol and water extracts of Polygonum perfoliatum L. can significantly inhibited the secretion of HBeAg. In non-toxic concentration the inhibition rates were 74.02±11.58%, 88.21±1.30%, 73.66±3.86%. Separated by chemical methods, the active ingredient continuously enriched and enhanced efficacy, reduced cytotoxicity. Gallic acid and 1-O-galloyl-β-D-glucose have a certain inhibitory effect on the secretion of HBeAg with an excellent dose-dependent relationship. Flavonoids and phenolic compounds were high concentration especially 1-O-galloyl-β-D-glucose with more than 1.26%. So these two type compounds could be the basis materials of anti-HBV activity.(3)We have successfully established a ConA-induced mouse model of immune hepatic injury. At the same time we study Polygonum perfoliatum L. protective effect of acute liver injury. The results showed that it can reduce Con A-induced ALT and AST in mice serum. Comparing the model group histopathology observation of liver injury significantly reduced. Polygonum perfoliatum L.ethanol extract of high-dose group can be very good to reduce TNF-αproduction and releasing, remission of acute liver inflammation.Chemical compositions in anti-viral traditional Chinese herbal medicines are very complex and diverse. They often play the role of efficacy through multiple targets or a variety of ways at the same time. It's the first time that we found Polygonum perfoliatum L. 's activity which can anti-HBV and protect liver and lower enzyme.After the study of chemical composition we infer that the material basis for its activity contain flavonoids and gallic acid acylation of phenol compounds. And the mechanism of Polygonum perfoliatum L. may be closely related to these two types of strong antioxidant substances.Make use of knowledge and experiments about immunology, phytochemistry and pharmacology, we preliminary studied the chemical compositions which can anti-HBV and protect liver. Experimental studies lay the foundation for the development of Polygonum perfoliatum L..