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The Cytotoxic Constituents from Marine-derived Streptomyces 3320^#
作者姓名:REN  Hong  GU  Qianqun  CUI  Chengbin  ZHU  Weiming
作者单位:[1]Key Laboratory of Marine Drug Chinese Ministry of Education, Institute of Marine Drug and Food, Ocean University of China, Qingdao 266003, P. R. China Science and Technology College of Chemistry and Biology, Yantai University, Yantai 264005, P.R. China [2]Science and Technology College of Chemistry and Biology, Yantai University, Yantai 264005, P. R. China [3]Beijing Institute of Pharmacology and Toxicology, AMMS, Beijing 100850, P.R. China
基金项目:中国科学院资助项目;教育部科学技术研究项目;山东省青岛市自然科学基金
摘    要:The present work studies the chemical constituents from marine-derived streptomyces 3320^# and their antitumor activities. The n-BuOH extract of the ferment broth of 3320^# was chromatographed on silica gel, Sephadex LH-20, ODS columns and HPLC to separate the compounds with antitoumor activities. Their structures were identified using IR, UV, NMR, MS spectroscopic techniques and compared with published data. The antitumor activities of the isolates were assayed using SRB method and flow cytometry assay, accompanied with the morphological observation of the cells under light micro- scope against mammalian tsFT210 cells. Ten compounds, cyclo-(Ala-Leu) 1, cyclo-(Ala-Ile) 2, cyclo-(Ala-Val) 3, cyclo- (Phe-Pro) 4, cyclo-(Phe-Gly)5, cyclo-(Leu-Pro)6, 1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid 7, N-(4- hydroxyphenethyl) acetamide 8, 4-methyoxy-l-(2-hydroxy) ethylbenzene 9 and uridine 10, were isolated from the ferment broth of streptomyces 3320^# . Among them, compounds 6, 7, 8 and 10 showed potent cytotoxicity against the tsFT210 cell with the IC50 values of 3.6, 7.2, 5.2 and 1.6 mmol L-1, respectively. Compounds 8, 10 also exhibited apoptosis inducing activity under 2.0 mmol L-1. Compounds 6, 7, 8 and 10 are the principle bioactive constituents responsible for the antitumor activities of marine streptomyces 3320^#. Compound 7 was isolated from this species for the first time.

关 键 词:链霉菌  代谢物  结构识别  生物量  分馏
收稿时间:2005-03-11
修稿时间:2005-11-04

The cytotoxic constituents from marine-derived streptomyces 3320#
REN Hong GU Qianqun CUI Chengbin ZHU Weiming.The Cytotoxic Constituents from Marine-derived Streptomyces 3320^#[J].Journal of Ocean University of China,2006,5(1):75-81.
Authors:Ren Hong  Gu Qianqun  Cui Chengbin  Zhu Weiming
Institution:1. Key Laboratory of Marine Drug Chinese Ministry of Education, Institute of Marine Drug and Food, Ocean University of China, Qingdao 266003, P .R .China;Science and Technology College of Chemistry and Biology, Yantai University,Yantai 264005, P .R .China
2. Key Laboratory of Marine Drug Chinese Ministry of Education, Institute of Marine Drug and Food, Ocean University of China, Qingdao 266003, P .R .China
3. Key Laboratory of Marine Drug Chinese Ministry of Education, Institute of Marine Drug and Food, Ocean University of China, Qingdao 266003, P .R .China;Beijing Institute of Pharmacology and Toxicology, AMMS, Beijing 100850, P .R .China
Abstract:The present work studies the chemical constituents from marine-derived streptomyces 3320# and their antitumor activities. Then-BuOH extract of the ferment broth of 3320# was chromatographed on silica gel, Sephadex LH-20, ODS columns and HPLC to separate the compounds with antitoumor activities. Their structures were identified using IR, UV, NMR, MS spectroscopic techniques and compared with published data. The antitumor activities of the isolates were assayed using SRB method and flow cytometry assay, accompanied with the morphological observation of the cells under light microscope against mammalian tsFT210 cells. Ten compounds, cyclo-(Ala-Leu) 1, cyclo-(Ala-Ile) 2, cyclo-(Ala-Val) 3, cyclo-(Phe- Pro) 4, cyclo-(Phe-Gly) 5, cyclo-(Leu-Pro) 6, 1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid 7, N-(4-hydroxyphenethyl) acetamide 8, 4-methyoxy-1-(2-hydroxy) ethylbenzene 9 and uridine 10, were isolated from the ferment broth of streptomyces 3320#. Among them, compounds 6, 7, 8 and 10 showed potent cytotoxicity against the tsFT210 cell with the IC50 values of 3.6, 7.2, 5.2 and 1.6 mmol L−1, respectively. Compounds 8, 10 also exhibited apoptosis inducing activity under 2.0 mmol L−1. Compounds 6, 7, 8 and 10 are the principle bioactive constituents responsible for the antitumor activities of marine streptomyces 3320#. Compound 7 was isolated from this species for the first time.
Keywords:marine-derived streptomyces  secondary metabolites  structural identify  bioassay-guided fractionation  antitumor activity
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