Studies On The Active Constituents Of Actinidia Chinensis Planch. And Actinidia Valvata Dunn

As traditional Chinese herbs, the roots of Actinidia chinensis Planch (Actinidiaceae), which was called Tengligen, and the roots of Actinidia valvata Dunn, which was called Maorenseng, are used to treat tumors of the alimentary canal widely in clinic, such as gastric cancer, esophagus cancer and liver cancer et al. As a part of a continuing study on the antitumor activity constituents of Actinidia species, we have systematically investigated the roots of A. chinensis and A. valvata. This dissertation describes the chemical and pharmacology studies of the plants. Some structures had been tested for the activity of anti-tumor in vitro and the effects on the activities of the enzymes. Moreover, the method of the quality control of the species had also been established.From the roots of A. chinensis, we isolated twenty-eight compounds, elucidated as 12?-chloro-2?, 3?, 13?, 23-tetrahydroxyolean-28-oic acid-13-lactone (T-1), 2?, 3?, 19?, 23, 24-pentahydroxyurs-12-en-28-oic acid (T-2), 4, 4'-dihydroxyl- dihydrochalcone-2'-O-β-D-glucopyranoside (T-3), ursolic acid (T-4), pseudo-taraxasterol (T-5), 2?, 3?-dihydroxyolean-12-en-28-oic acid (T-6), 2?, 3?-dihydroxyurs-12-en-28-oic acid (T-7), 2?, 3?, 24-trihydroxyurs-12-en-28-oic acid (T-8), 2?, 3?, 24-trihydroxyolean-12-en-28-oic acid (T-9), 2?, 3?, 23-trihydroxyurs-12-en-28-oic acid (T-10), 2?, 3?, 23-trihydroxyurs-12-en-28-oic acid (T-11), 2?, 3?, 24-trihydroxyurs-12-en-28-oic acid (T-12), 2?, 3?, 19?, 24-tetrahydroxyurs-12-en-28-oic acid (T-13), 2?, 3?, 19?, 23-tetrahydroxyurs-12-en-28-oic acid (T-14), 2?, 3?, 24-trihydroxyurs-12, 20(30)-dien-28-oic acid (T-15), 2?, 3?, 19?, 24-tetrahydroxyurs-12-en-28-oic acid 28-O-?-D-glucopyranoside (T-16), 2?, 3?, 19?, 23-tetrahydroxyurs-12-en-28-oic acid 28-O-?-D-glucopyranoside (T-17), 2?, 3?, 23-trihydroxyurs-12, 20(30)-dien-28-oic acid (T-18), 2?, 3?, 23, 24-tetrahydroxyurs-12-en-28-oic acid (T-19), 2, 3, 4, 6 tetraacetyl-(19?-hydroxy-2?, 3?, 24-triacetoxyurs-12-en-28-oyl)- ?-D-glucopyranoside (T-20), 2?, 3?, 23-trihydroxyurs-13 (18)-en-28-oic acid (T-21), 1?, 2?, 3?, 19?, 23-pentahydroxyurs-12-en-28-oic acid (T-22), Actinidin A (T-23), Actinidin B (T-24), 3?-hydroxystigmast-5-en-7-one (T-25), ?-sitosterol (T-26), daucosterol (T-27), n-dotriacontanic acid (T-28). Among them, T-1, T-2, T-21 are new compounds and T-3,T-5,T-6,T-7,T-9,T-11,T-12,T-14,T-15,T-16,T-17,T-18,T-19,T-22,T-23,T-24,T-25,T-28 are the first report of the occurrence in this plant. From the roots of A. valvata, we isolated twelve compounds, elucidated as 2?, 3?, 24-trihydroxyurs-12-en-28-oic acid (M-1), 2?, 3?, 23-trihydroxyurs-12-en-28-oic acid (M-2), 2?, 3?-dihydroxyurs-12-en-28-oic acid (M-3), 2?, 3?, 23, 24-tetrahydroxyurs -12-en-28-oic acid (M-4), 2?, 3?, 13?, 24-tetrahydroxyurs-11-en-28-oic acid-13-lactone (M-5), 2?, 3?, 24-trihydroxyolean-12-en-28-oic acid (M-6), 2?, 3?, 19?, 24-tetrahydroxyurs-12-en-28-oic acid (M-7), 2?, 3?, 24-trihydroxyurs-12-en-28-oic acid (M-8), 2?, 3?, 24-trihydroxyurs-12, 20(30)-dien-28-oic acid (M-9), 2?, 3?, 23,24-tetrahydroxyurs-2,3-glycol-dioxyphene-12-en-28-oic acid (M-10), olean acid (M-11), ?-sitosterol (M-12). Among them, M-3,M-4,M-5,M-6,M-7,M-9 and M-10 are the first report in this plant.The cytotoxic activity of thirteen compounds (T-1,T-5,T-6,T-7,T-8,T-10,T-11,T-13,T-16,T-17,T-19,T-24,T-27) against A549, LOVO and HepG2 cell lines were evaluated. T-7 showed positive cytotoxic activity against LOVO (IC50 2.9?g/ml) and HepG2 (IC50 9.2?g/ml) cell lines, compared to DOX as a positive control (IC50 0.37 and 0.78 ?g/ml, respectively). T-6 showed weakly active against LOVO (IC50 6.0?g/ml) cell lines. The bioassay results indicated that the cytotoxic activity decreased when the water-solubility of the compounds increased, which was in accordance with the results of the reported.Crude extracts and six compounds (T-1,T-3,T-7,T-8,T-9,T-10) showed different inhibiting effect on the activities of the enzymes (CYP1A2,CYP2C9,CYP2C19,CYP2D6,CYP3A4).Besides, the contents of two mutual constituents were analysis by HPLC-UV method to make distinction between the roots and the rhizome gathered at different season in Zhejiang province.