试图从 gambogic 酸和它的衍生物发现有势力 apoptosis inducer。gambogic 酸的八新不捐赠的衍生物作为潜在的反肿瘤被综合的方法在 HT-29, Bel-7402, BGC-823,和 A549 房间线上带混合物和他们的禁止的活动被 MTT 试金在 vitro 评估。在这些混合物之中的结果, 4 通过 MTT 房间试金,词法变化的观察,和 Annexin-V/PI 作为 SKOV3 房间 apoptosis inducer 与在 gambogic 酸一半的 C35 的一个氢氧根组一起被识别两倍染色的试金。在导致 apoptosis 和力量的结论化合物 4 显示出的重要效果为新 anticancer 药的发现用作潜在的铅混合物。
AIM: To find a potent apoptosis inducer from gambogic acid and its derivatives. METHODS: Eight new NO-donating derivatives of gambogic acid were synthesized as potential anti-tumor lead compounds and their inhibitory activity on the HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by the MTF assay. RESULTS: Among these compounds, 4 with a hydroxyl group at C35 of the gambogic acid moiety was identified as a SKOV3 cell apoptosis inducer through the MTF cell assay, observations of morphological changes, and Annexin-V/PI double staining assay. CONCLUSION: Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for the discovery of new anticancer drugs.