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Antitumor Principle Constituents of <i>Myrica rubra </i>Var. <i>acuminata</i>

Lingling YangGraduate Institute of Pharmacognosy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan, Republic of China, and Graduate Institute of Biopharmaceutics, National Chiayi University, 300 University Road, Chiayi 600, Taiwan, Republic of ChinaChia‐Chen ChangGraduate Institute of Pharmacognosy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan, Republic of China, and Graduate Institute of Biopharmaceutics, National Chiayi University, 300 University Road, Chiayi 600, Taiwan, Republic of ChinaLih-Geeng ChenGraduate Institute of Pharmacognosy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan, Republic of China, and Graduate Institute of Biopharmaceutics, National Chiayi University, 300 University Road, Chiayi 600, Taiwan, Republic of ChinaChing‐Chiung WangGraduate Institute of Pharmacognosy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan, Republic of China, and Graduate Institute of Biopharmaceutics, National Chiayi University, 300 University Road, Chiayi 600, Taiwan, Republic of China
2003en
ABI

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Myrica rubra var. acuminata is a native shrub widely distributed and used as folk medicine in Taiwan for stomach disorders and diarrhea. Column chromatography combined with cytotoxic bioassay-guided fractionation was performed to isolate the antitumor principles from fresh leaves of M. rubravar. acuminata. The 20% MeOH eluate fraction of M. rubra var. acuminata inhibited the viability of HeLa and P-388 cells in an in vitro assay and an in vivo P-388 tumor-bearing CDF(1) mouse model. The percent increase in life span (%ILS) of 20% MeOH eluate fraction was greater than 125%. (-)-Epigallocatechin 3-O-gallate (1) and prodelphinidin A-2,3'-O-gallate (2) were isolated from D-20 as the antitumor principle components. Both compounds can inhibit the growth of HeLa cells, but 1 had lower cytotoxic effects in normal cervical fibroblasts than did 2. Moreover, pretreatment with a caspase-3 specific inhibitor prevented 1- and 2-induced poly(ADP-ribose) polymerase cleavage. In view of these results, we suggest that 1 and 2 can induce apoptosis in HeLa cells and that activation of caspase-3 may provide a mechanistic explanation for their cytotoxic effects. Therefore, we suggest that the 20% MeOH eluate fraction extract is good for health and that M. rubra var. acuminata is an economically valuable plant.

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