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目的研究双四氢呋喃型番荔枝内酯的体内抗肿瘤作用。方法以紫杉醇为阳性对照,观察4个双四氢呋喃型番荔枝内酯单体番荔枝塔亭戊(squamostatin-E,1)、番荔枝塔亭甲(squamostatin-A,2)、去乙酰紫玉盘素(desacetyluvaricin,3)、泡番荔枝辛(bullatacin,4)对移植性肝癌Heps和肉瘤S180荷瘤小鼠的抑瘤作用及对小鼠体质量与肝、胸腺和脾指数的影响。结果与模型组比较,化合物1高剂量(60μg/kg)、化合物3和4低剂量(15μg/kg)对移植性肝癌Heps荷瘤小鼠肿瘤有极显著抑制作用(P<0.01),抑制率分别为51.6%、32.5%、63.4%;化合物2和3高剂量(60μg/kg)对移植性肝癌Heps荷瘤小鼠肿瘤有显著抑制作用(P<0.05),抑制率分别为31.2%、70.9%;紫杉醇40μg/kg的抑瘤率为62.2%。化合物3高剂量对移植性肉瘤S180荷瘤小鼠肿瘤有极显著抑制作用(P<0.01),抑制率为63.9%;紫杉醇40μg/kg的抑瘤率为48.9%。结论化合物1～4对移植性肝癌Heps荷瘤小鼠、肉瘤S180荷瘤小鼠均有明显抗肿瘤作用,部分化合物的抗肿瘤活性强于紫杉醇。
Objective To study the anti-tumor effect of biotanylated annona in vivo. Methods paclitaxel was used as a positive control to observe the effects of four bis-tetrahydrofurane type annatto lactone squamostatin-E (1), squamostatin-A (2) The effect of desacetyluvaricin (3) and bullatacin (4) on tumor-bearing mice with transplanted hepatocarcinoma Heps and sarcoma S180 tumor and its effect on body weight, liver, thymus and spleen index of mice. Results Compared with the model group, compound 1 high dose (60μg / kg) and compound 3 and 4 low dose (15μg / kg) had significant inhibitory effect on the tumor of Heps tumor-bearing mice (P <0.01) (51.6%, 32.5% and 63.4% respectively). High doses of compound 2 and 3 (60μg / kg) significantly inhibited tumor growth in Heps mice bearing transplanted hepatocarcinoma (P <0.05), with inhibitory rates of 31.2% and 70.9 %; Paclitaxel 40μg / kg inhibition rate of 62.2%. The high dose of compound 3 had a significant inhibitory effect on the tumor of S180 tumor-bearing mice (P <0.01), the inhibition rate was 63.9%, and the inhibition rate of paclitaxel 40μg / kg was 48.9%. Conclusion Compounds 1 to 4 have obvious antitumor effects on Heps tumor-bearing mice and sarcoma S180 tumor-bearing mice of transplanted hepatocarcinoma. Some of the compounds have stronger anti-tumor activity than paclitaxel.