东北红豆杉中三种紫杉烷类化合物体外抗癌活性研究

Effects of 3 taxanes from Taxus cuspidate on inhibiting proliferation of cultured breast cancer cells in vitro

目的:通过观察东北红豆杉中三种紫杉烷二萜类化合物2,9-diacetyl-5-cinnamoyl-phototaxicinⅡ(1)、5-acetyltaxuspineW(2)及10-acetyltaxuspineB(3)对人乳腺癌细胞生长的影响,探讨这三种紫杉烷类化合物的抗癌作用及各化合物结构与活性之间的构效关系。方法:以人乳腺癌细胞为研究对象,采用MTT法检测3种紫杉烷类化合物对乳腺癌细胞生长的抑制率。结果:上述三个化合物对乳腺癌细胞均有不同程度的抑制作用,其中2,9-diacetyl-5-cinnamoyl-phototaxicinⅡ(1)及10-acetyltaxuspineB(3)的作用优于5-acetyltaxuspineW(2);前两者有效浓度范围是20μmol/L-100μmol/L,后者的有效浓度为60μmol/L-100μmol/L。结论:从东北红豆杉中得到的三种紫杉烷类化合物2,9-diacetyl-5-cinnamoyl-phototaxicinⅡ(1)、5-acetyltaxuspineW(2)及10-acetyltaxuspineB(3)对人乳腺癌细胞具有较强的体外抗肿瘤活性,侧链肉桂酰基可能是有效基团之一。

Object： To study the effects of 3 taxanes （ 2,9-diacetyl-5-cinnamoyl-phototaxicinⅡ （ 1 ） ,5-acetyhaxuspineW（ 2 ） and 10-acctyhaxuspineB （3）） from Taxus cuspidate on inhibiting proliferation of cultured breast cancer cells in vitro. Methods： MTT was used to observe the effects of inhibiting proliferation of breast cancer cells cultured in vitro with the 3 taxanes of different concentration in it for 36h . Results： It was found that compounds （ 1 ） and （ 3 ） had the effects on inhibiting proliferation of breast cancer cells cultured for 36 h at doses ranging from 20μmol/L - 100μmol/L, and for compound （2） ,60μmol/L - 100μmol/L were effective. Compounds （ 1 ） and （3） were more effective than compound （2）. This result maybe partly due to the existence of cinnamoyl group. Conclusion： The 3 Taxanes, 2,9-diacetyl-5-cinnamoyl- phototaxicinⅡ（ 1 ）,5-acetyhaxuspineW （2） and 10-acetyhaxuspineB （3）, had the effects on inhibiting the proliferation of cultured breast cancer cells in vitro.