新型染料木素磺酸酯的合成及对小鼠血吸虫病肝肉芽肿的影响

Synthesis of genistein sulfonate and its therapeutic effect on mice schistosomiasis

为寻找抗血吸虫病的新候选化合物,通过正交实验,高选择性、高产率地合成了染料木素的磺酸酯衍生物。结果表明:小鼠感染血吸虫病,经过衍生物治疗后,由血吸虫导致的肉芽肿面积有不同程度的降低,其中低剂量组降低到23.2%,与溶剂组比较,差异显著(P<0.05),优于原药的27.1%及阳性对照组秋水仙碱的27.0%。说明该化合物对血吸虫导致的肉芽肿有一定抑制作用,该化合物有进一步研究价值。

Genistein sulfonic acid ester derivative was synthesized in high yield and high selectivity through the orthogonal experiment to seek new candidate compounds for schistosomiasis. After the mice that infected with schistosomiasis were treated by the derivative,the granuloma area in mice that were led by schistosome decreased in different degrees.Among them,the low dosage group reduced to 23.2%,significant difference compared with the solvent group（ P0.05）,） better than the parent drug 27.1% and the positive control group 27%. This compound had a certain inhibitory effect on granuloma in mice that was caused by schistosoma. The mechanism may be the liver functions of mice should be improved after drug treatment.