Bedir E, Khan I A, Walker L A
National Center for Natural Products Research, University of Mississippi, USA.
Pharmazie. 2002 Jul;57(7):491-3.
The steroidal saponin constituents obtained from Tribulus terrestris were tested for their antimicrobial and cytotoxic effects. The spirostanol-based steroidal saponins 1-3 exhibited remarkable activity against fungal organisms (Candida albicans and Cryptococcus neoformans) and cancer cell lines [human malignant melanoma (SK-MEL), human oral epidermoid carcinoma (KB), human breast ductal carcinoma (BT-549), and human ovary carcinoma (SK-OV-3)], while none of the compounds possessing the furostanol framework 4-7 showed activity. The most active spirostanol glycoside, compound 3 exhibited a broad range of anticancer activity against cell lines, SK-MEL, KB, BT-549 and SK-OV-3 at IC50s of 6.0, 7.0, 6.0 and 8.2 micrograms/ml, respectively, while compounds 1 and 2 showed selective cytotoxicity against SK-MEL at 6.7 and 9.1 micrograms/ml, respectively. The minimum inhibitory concentrations (MIC) in antifungal bioassay for compounds 1-3 varied from 1.5 to 6.2 micrograms/ml, which prompted to conclude certain structural features are required for these bioactivities.
对从刺蒺藜中获得的甾体皂苷成分进行了抗菌和细胞毒性作用测试。基于螺甾烷醇的甾体皂苷1-3对真菌生物体（白色念珠菌和新型隐球菌）和癌细胞系[人类恶性黑色素瘤（SK-MEL）、人类口腔表皮样癌（KB）、人类乳腺导管癌（BT-549）和人类卵巢癌（SK-OV-3）]表现出显著活性，而具有呋甾烷醇骨架的化合物4-7均无活性。活性最高的螺甾烷醇糖苷化合物3对细胞系SK-MEL、KB、BT-549和SK-OV-3表现出广泛的抗癌活性，其IC50分别为6.0、7.0、6.0和8.2微克/毫升，而化合物1和2分别对SK-MEL表现出选择性细胞毒性，IC50分别为6.7和9.1微克/毫升。化合物1-3在抗真菌生物测定中的最低抑菌浓度（MIC）为1.5至6.2微克/毫升，这促使得出结论，这些生物活性需要某些结构特征。
