云南红豆杉抗肿瘤活性成分的研究

STUDIES ON THE CHEMICAL CONSTITUENTS OF TAXUS YUNNANENSIS

云南红豆杉(Taxus yunnanensis Cheng et L.K.Fu)树皮的乙醇提取物显示较强的抗肿瘤活性,从中分离得到8个紫杉烷类二萜及其生物碱。经光谱分析和化学反应鉴定7个已知物为taxinine E(1),taxinine J(2),1-acetoxy-5-deacetvl baccatin Ⅰ(4),baccatin Ⅲ(5),taxol(6),cephalomannine(7)和7-xylosyl-10-deacetyl taxol(8)。化合物3命名为云南红豆杉甲素(ymlnanxane),为一新的紫杉烷二萜化合物,其结构为taxa-4(20),11-diene-2α,5α,10β,14β-tetraol-2α,5α,10β-triacetate-14β-αmethyl-β-hydroxyl butyrate,并通过X-射线单晶衍射予以证实.经体外筛迭化合物3具有抗肿瘤活性。

The ethanolic extract of the bark of Taxus yunnanensis Cheng et L.K. Fu. showed significant antineoplastic effect on the transplantable tumors in mice. The life survival ofP388 leukemic bearing mice was increased (84%)and the growth of B_(16) melanoma in mice was inhibited (53%).From this extract eight taxane diterpenoids and taxane alkaloids have been isolated.Seven of them have been identified as taxinine E(1), taxinine J(2), 1-acetoxy-5-deacetyl baccatin Ⅰ(4 ), baccatin Ⅲ(5), taxol (6), cephalomannine (7), 7 -xylosyl - 10 -deacetyl taxol (8)from their physical and spectroscopic properties. A new taxane diterpenoid, named yunnanxanc (3) was elucidated as taxa-4 (20), 11 - diene- 2α, 5α, 10β,14β- tetraoln2α,5α,10β- triacetaten - 14β-α - methyl-β- hydroxylbutyratebyhighfield ~1H NMR, ^(13)C NMR, ~1H-~1HCOSY, ^(13)C-~1HCOSY, ^(13)C-~1HCOLOC and X-ray analysis. It showed the inhibitory effect on A_(2780) DDP, KB and HCT-8 cell line in vitro. All of the eight compounds were isolated from this species for the first time.