Study On The Chemical Constituents And Antitumor Mechanism Of The Chloroform Fraction Of Acitnidia Eriantha Benth

At present, as a high death rate of the disease, cancer is seriously harmful to human health.Along with the modernized development of research techniques, the use of new technology andmethod to study anticancer activity and anticancer mechanisms of Chinese herbal medicine hasbecome a hot spot in the research of anticancer drugs. It is playing an irreplaceable role in newdrugs and drug lead compound discovery process.This research selects the long-term use of traditional she medicine Actinidia eriantha Benth.,which has antitumor effect as research object. On the basis of our laboratory，s previous research,we separate the chemical constituents and further study the antitumor mechanism of itschloroform fraction.Studies on isolation and structure identification of chemical constituents, we use methanolextracts from the root of Actinidia eriantha Benth.. Using solvent method, thin layer chromate--graphy, qualitative chemical color reaction and high-performance liquid chromatographymethod, we separated7kinds of compounds from chloroform layer. Using1H-NMR,¹³C-NMR,and mass spectrometry, we can analysis of compound structures in Actinidia eriantha Benth..The results showed that the compound1is2,3,24-trihydroxyurs-12-en-28-oic acid; thecompound2is2β,3β-dihydroxy-23-oxo-urs-12-en-28-oic acid; the compound3is2,3-dihydroxy-23-methoxy-12-en-28-oic acid; the compound6is an unsaturated fatty acid.We examined the anti-cancer activity of the above extracts through MTT assay and growthcurve, the results showed the chloroform fraction has significant antitumor activity in vitro. Theproliferation of the chloroform fraction is in a dose-dependent manner, the IC50value was114.8μg·mL^-1. Through the observation of cell morphology, Hoechst33258and AO/EB cell stainingexperiments, we can preliminarily conclude that the chloroform fraction may inhibit tumor cellthrough a necrotic pathway. This inhibition has a close relation with concentration, and lowconcentrations can selectively inhibit the proliferation of tumor cells and have small toxicity tonormal cells.We examined antitumor activity in vivo. After setting up the animal model of H22, theantitumor effects of chloroform fraction were investigated by detecting tumor inhibitory rate, the result showed that the75mg/kg low dose groups of H22hepatoma mice shows significantinhibition, the tumor inhibition rate was37.34%. While the dosage was150or300mg/kg, theeffect is not obvious. And the experiment suggested the chloroform fraction have certain toxicity,compared with normal group and model group.We investigated the chemical constituents and antitumor activity in this study. These resultsprovided experimental basis for Actinidia eriantha Benth. as clinical antitumor drugs. Also, theresults provided effective information for later chemical synthesis of antitumor drugs and leadcompounds.