假衛矛屬植物化學成分及其細胞毒殺之研究

Chemical Constituents and Cytotoxicity of Microtropis Species

陳怡曉(I-Hsiao Chen)

指導教授 ： 吳永昌

共同指導教授 ： 張芳榮(Fang-Rong Chang)

高雄醫學大學/藥學院/天然藥物研究所碩士班/博士(2009年)

摘要

本研究進行台灣衛矛科植物(Celastraceae)-福建賽衛矛(M. fokienensis)葉部、莖部和日本賽衛矛(M. japonica)莖部化學成分分離及活性之研究。從福建賽衛矛葉部得到十四個化合物，分別為七個ursane-type triterpenoids、二個oleanane-type triterpenoids、二個lupane-type triterpenoids、二個phenols及一個benzenoid；從莖部得到三十三個化合物，分別為十個ursane-type triterpenoids、九個oleanane-type triterpenoids、十三個lupane-type triterpenoids及一個agarofuran sesquiterpenoid。從日本賽衛矛莖部得到十五個化合物，分別為八個ursane-type triterpenoids、一個oleanane-type triterpenoid和六個agarofuran sesquiterpenoids。本研究共分離得到二十七個新化合物。
將化合物進行細胞毒殺活性篩選測試，其中活性化合物FL-3對於HepG2和Hep3B等細胞株具有明顯的細胞毒殺活性，其IC50值分別為3.8和4.5 ug/mL；FL-5對於HepG2細胞株也顯示細胞毒殺作用，其IC50值為4.6 ug/mL；FS-2對於HepG2、Hep3B、MDA-MB-231、MCF7、A549及HL 60具有顯著的細胞毒殺作用，其IC50值分別3.1、1.7、3.5、4.0、2.8和2.0 ug/mL；FS-6對於Hep3B、MCF7、Ca9-22及HL 60細胞株其細胞毒殺作用之IC50值分別為4.7、2.9、1.4和1.6 ug/mL。此外，進一步研究活性化合物FS-6 (28-hydroxy-3-oxo-lup-20(29)-en-30-al)針對HL 60細胞毒殺作用機轉。

關鍵字

衛矛科 ； 福建賽衛矛 ； 日本賽衛矛 ； 三萜類 ； HDAC

並列摘要

In this study for bioactive compounds from Celastraceous plants, the extracts of the leaves and stems of M. fokienensis, as well as the stems of M. japonica were found to be cytotoxic and selected for fractionation. Up to now, 14 compounds were isolated form the leaves of M. fokienensis, including seven ursane-type triterpenoids, two oleanane-type triterpenoids, two lupane-type triterpenoids, two flavonoids and one benzenoid; 33 compounds were isolated form the stems of M. fokienensis, including ten ursane-type triterpenoids, nine oleanane-type triterpenoids, thirteen lupane-type triterpenoids and one agarofuran sesquiterpenoid; 15 compounds were isolated form the stems of M. japonica, including eight ursane-type triterpenoids, one oleanane-type triterpenoid, and six agarofuran sesquiterpenoids. Among them, 27 new compounds were isolated.
All triterpenoids were evaluated for their in vitro cytotoxicity toward human cancer cell lines. Among these compounds, FL-3 was found to be the most active toward the HepG2 and Hep3B cancer cell lines with IC50 of values 3.8 and 4.5 ug/mL, respectively; FL-5 was found to be active toward the HepG2 cancer cell lines with IC50 of values 4.6 ug/mL; FS-2 was found to be active toward the HepG2, Hep3B, MDA-MB-231, MCF7, A549 and HL 60 cancer cell lines with IC50 of values 3.1, 1.7, 3.5, 4.0, 2.8 and 2.0 ug/mL；FS-6 was found to be active toward the Hep3B、MCF7、Ca9-22 and HL 60 cancer cell lines with IC50 of values 4.7, 2.9, 1.4 and 1.6 ug/mL. The active compound, 28-hydroxy-3-oxo-lup-20(29)-en-30-al (FS-6), was selected for further mechanic investigation of survival suppression and proliferation of HL60 cells.

並列關鍵字

Celastraceae ； Microtropis fokienensis ； Microtropis japonica ； triterpenes ； HDAC

參考文獻

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