本文合成了9种含有由天然D(+)-樟脑衍生的1R，3S-1，2，2-三甲基-1，3-环戊二胺(A)为配体的铂(Ⅱ)配合物[Pt(ⅡHx]{其中，X=(CH2)，C(COO-)2(1，1-环丁烷二羧酸根)，2CH3OCH2COO-，2CH3CH2OCH2COO-，2CH，(CH2)3OCH2COO-，[OCH(CH3)COO]2-(乳酸根)，(OCH2COO)2-(乙醇酸根)，2CH3OCH2CH2OCH2COO-，2CH3CH2OCH2CH2OCH2COO-和2CH3(CH2)30CH2CH2OCH2COO-1。通过元素分析、热重分析、红外光谱、1H核磁共振谱和电喷雾质谱等对配合物进行了表征。体外生物活性测试表明，部分配合物对A549人肺癌细胞和HCT-116人结肠癌细胞具有较强的抗肿瘤活性。

AIM: To study the inhibitory effect of general gambogic acids (GGA) on transplantation tumor SMMC-7721 in experimental animal model and SMMC-7721 cells in vitro. METHODS: Anti-tumor activity of GGA in the experimental transplantation tumor SMMC-7721 was evaluated by relative tumor growth ratio. Cell morphology was observed with inverted microscope and electron microscope. Cell proliferation was measured by MTT assay and the telomerase activity was determined by PCR. RESULTS: In vivo study indicated that GGA (2, 4, and 8mg/kg, iv, 3 times per week for 3 weeks) displayed an inhibitory effect on the growth of transplantation tumor SMMC-7721 in nude mice compared with the normal saline group (P<0.01). At the concentrations of 0.625-5.0mg/L, GGA remarkably inhibited the proliferation of SMMC-7721 cells in vitro. GGA 2 mg/L dramatically changed morphology of SMMC-7721 cells and inhibited the telomerase activity in SMMC-7721 cells. CONCLUSION: GGA had inhibitory effect on the growth of SMMC-7721, which might be related to its inhibition of telomerase activity.

本文综述了非经典铂类抗肿瘤药物的发展概况，介绍了具有口服活性的铂（Ⅳ）配合物，具有空间位阻的铂（Ⅱ）配合物，反式铂（Ⅱ、Ⅳ）配合物，多核铂（Ⅱ）配合物和含有铂2硫键的铂（Ⅱ）配合物，并总结了这几类新型铂配合物的抗肿瘤机理，克服顺铂的耐药性机理及其临床进展。