杜鹃兰化学成分及其生物活性研究

目的 研究杜鹃兰化学成分，发现其抗肿瘤活性成分。方法 杜鹃兰经95%乙醇提取、硅胶柱层析、半制备HPLC和Sephadex LH-20柱层析进行分离纯化，波谱分析（核磁共振氢谱、碳谱、和质谱）确定结构；应用MTT法，对部分化合物进行体外抗肿瘤活性筛选。结果 从杜鹃兰分离鉴定12个化合物，分别为bisbenzopyran (1),(22E)-ergosta-6, 22-dien-3β, 5α, 8α-triol (2), 3β-hydroxycholesta-5-ene (3), β-sistosterol (4),pinoresinol (5),5,4′-dihydroxy-7-(4-hydroxybenzoyl)-3′-methoxyflavone (6),4-methoxy-2,3,7-trihydroxyphenanthrene(7), 2-hydroxy-4, 7-dimethoxyphenanthrene(8), 4, 4′-dimethoxy-[1, 1′-biphenanthrene]-2,2′，7,7′-tetrol (9),4,7,4′，9′-tetramethoxy...

Chemical Compounds Isolated from Cremastra Appendiculata and Their Bioactive Activity

  Objective  To study the chemical compounds from the medicinal plants of Cremastra appendiculata and find its antitumor bioactive compounds.   Methods  The compounds were extracted by alcohol （95%） and isolated by column chromatography on silica gel and Sephadex LH-20. Their structures were identified by spectroscopic analysis （1H NMR, 13CNMR and EIMS）. The antitumor activity of the compounds was studied by MTT assay in vitro.   Results  Twelve compounds were obtained and identified as bisbenzopyran （1）, （22E）-ergosta-6, 22-dien-3β, 5α, 8α-triol （2）, 3β-hydroxycholesta-5-ene （3）, β-sistosterol （4）, pinoresinol （5）, 5, 4′-dihydroxy-7- （4-hydroxybenzoyl） -3′- methoxyflavone （6）, 4-methoxy-2, 3, 7- trihydroxyphenanthrene （7）, 2-hydroxy-4, 7-dimethoxyphenanthrene （8）, 4, 4′-dimethoxy-[1, 1′-biphenanthrene]- 2, 2′, 7, 7′-tetrol （9）, 4, 7, 4′, 9′-tetramethoxy-[1, 1′-biphenanthrene] 2, 2′, 7, 7′-tetrol （10）, Bavachinine （11）, 3-hydroxyphenpropionic acid- （2′-methoxy-4′- carboxy-phenol） ester （12）; . The results of anti-tumor activity test of compounds 7～12 showed that 9 and 10 showed good inhibitory activity on MCF-7/S cell line.  Conclusions   Compounds 2, 3, 5, 7, 10 and 12 were isolated from this plant for the first time. IC₅₀ of 9 and 10 on MCF-7/S cell lines were 2.16 and 5.09 respectively μmol/L.