Chemical Constituents In Root Of Actinidia Chinensis

The dried roots of Actinidia chinensis Planch., also called Tengligen, which belong to Actinidiaceae and Actinidia Lindl., have the effects of promoting blood circulation and reduction of swelling, relieving internal heat and diuresis,alleviating rheumatism, radiating and hemostasis, and they are used to treat diseases of gastric cancer and breast cancer, hepatitis,edema, bruises, rheumatoid arthritis, dysentery, filariasis, etal. It is widely distributed in the eastern of China and it is mainly distributed Shanxi, Jiangxi, Hunan, Hubei, Zhejiang and Anhui. Pharmacological studies on this plant have shown that it has antitumor effect, anti-bacterial effect,anti-inflammatory effect,anti-viral effect, immunomodulatory effect, anti-oxidant and liver protection effect, etal. The main constituents of Actinidia chinensis Planch. are triterpenes, flavanoids,anthraquinones,carbohydrate, sterols and essential oils.Objectives: To study the chemical constitutes of the root of Actinidia chinensis Planch. and the primary pharmacological effect on anti-tumor of the constitutes of high quantity.Methods: The dried root of Actinidia chinensis Planch. were percolated with 95% EtOH and partitioned with petroleum ether, ethyl acetate, n-butyl alcohol fractionally. Constituents were isolated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography, TLC preparation and recrystallization. Their structures were identified on the basis of their chemical and physical properties as well as the spectra data of IR, ESI-MS, 1~H-NMR and (13)~C-NMR etal. The inhibition effect of 2α,3α,24-trihydroxyurs-12-en-28-oic acid on sarcoma 180 tumor ( S180 )-bearing mice was observed at dosages of 200, 100 and 50 mg/kg by systematically to measure the S180 tumor inhibition rate.Results: Fifteen compounds were isolated from Actinidia chinensis Planch. and were determined as follows: (n)-tetracosanoic-acid ( I ),β-sitosterol ( II ), stearyl-β-D-gluco pyranoside( III ), stearic acid( IV ), ursolic acid( V ), 3-epi-corosolicacid( VI ), 2α,3α,24-trihydroxyurs-12-en-28-oic acid ( VII ), daucosterol ( VIII ), formononetin ( IX ), biochanin A ( X ), ( - )-epi-catechin ( XI ), r-quinide ( XII ), n-butyl-β-D-fructopyranoside ( XIII ), sucrose( XIV ), glucose ( XV ). The pharmacological studies have shown that 2α,3α,24-trihydroxyurs-12-en-28-oic acid at dosages of 200 mg/kg have some antitumor activity, and there was a dose-effect relationship.Conclusions: Fifteen compounds were isolated from Actinidia chinensis Planch.. Among them, Compounds I,III,IV,IX,X,XII and XIII were isolated from Actinidia chinensis Planch. for the first time. Compounds XII was isolated for the first time as natural substance. The investigation on antitumor effect of Actinidia chinensis Planch. indicated that the compound showed antitumor activity. It provides the evidence for the further utilization and research.