瑞香狼毒提取物尼地吗啉的抗癌活性

THE ANTITUMOR ACTIVITIES 0F GNIDIMACRIN IS0LATED FR0M STELLERA CHAMAEJASME L

从中药瑞香狼毒（ＳｔｅｌｌｅｒａｃｈａｍａｅｊａｓｍｅＬ．）的甲醇提取物中分离到的二萜化合物尼地吗啉（ｇｎｉｄｉｍａｃｒｉｎ），以０．０２～０．０３ｍｇ／ｋｇ腹腔注射，可使小鼠白血病Ｐ－３８８和Ｌ－１２１０腹水型的生命延长７０％和８０％。以０．０１～０．０２ｍｇ／ｋｇ腹腔注射，可使小鼠实体瘤Ｌｅｗｉｓ肺癌、黑色素瘤Ｂ－１６和结肠癌２６的生命延长４０％、４９％和４１％。应用ＭＴＴ法和克隆形成法，观察了尼地吗啉对体外培养的人白血病Ｋ５６２和胃癌Ｋａｔｏ－Ⅲ、ＭＫＮ－２８、ＭＫＮ－４５及小鼠Ｌ－１２１０的细胞生长和克隆形成抑制作用，其ＩＣ＿５０在０．００７～０．０００１２μｇ／ｍｌ范围。这表明尼地吗啉具有较强的抗癌活性，是瑞香狼毒抗癌作用的主要成分。

Abstract Gnidimacrin ,a diterpene compound,isolated from the methanol extract of Stellera chamaejasmeL,showed significant antitumor activities against mouse leukemia P-388 and L-1210 in vivo.At thedosages of 0.02-0.03mg/kg ip,the in increase in life span(ILS)was 70% and 80%,respectively.Gnidimacrin was also active against murine solid tumors in vivo, such as Lewis lung carcinoma ,B-16melanoma and colon cancer 26.It showed ILSs of 40%,49%and 41%at the dosages of0.01-0.02mg/kg ip, respectively.Gnidimacrin strongly inhibited cell proliferation of human cancercell lines such as leukemia K 562,stomach cancers Kato-Ⅲ,MKN-28,MKN-45, and mouse L-1210 bythe MTT assay and colony forming assay in vitro The IC_50 of gnidimacrin was 0.007-0.00012μg/ml.It is concluded that gnidimacrin is the principal antitumor element in Stellera chamaejasme L.withstrong antitumor activities.