腺花香茶菜地下部分抗血吸虫活性研究

Anti-schistosome activity of the underground part of Isodon adenantha

目的:研究腺花香茶菜(Isodon adenantha)地下根茎的抗血吸虫活性作用。方法:用70%丙酮对腺花香茶菜地下根茎进行冷浸提取,采用体外抗血吸虫药敏实验测试腺花香茶菜地下根茎提取物及其中化合物的抗血吸虫活性。结果:腺花香茶菜粗提物、正丁醇部位和水部位的高浓度组(2 mg·mL-1)给药24 h后即起效,48 h后成虫死亡;中浓度组(0.5 mg·mL-1)给药48 h后未见成虫死亡;乙酸乙酯部位高浓度组(2 mg·mL-1)给药6 h后即起效,24 h后成虫死亡;中浓度组(0.5 mg·mL-1)给药6 h后即起效,48 h后成虫死亡;给药24 h后,化合物1高浓度组(200μg·mL-1)成虫全部死亡,显示出显著的杀虫活性;药物作用36 h后,化合物2高浓度组成虫全部死亡。结论:腺花香茶菜70%丙酮粗提物、乙酸乙酯部位、正丁醇部位、水部位以及单体化合物1和2均具有一定的体外抗血吸虫活性。本研究为深入了解腺花香茶菜的生物活性效果及可能的应用范围、开发植物来源的新型抗血吸虫天然产物提供了一定的参考。

Objective：To determine the anti-schistosome activity of the underground part of Isodon adenantha.Methods：The rhizomes of Isodon adenantha were extracted by 70% acetone cold soak extraction.Anti-schistosome activities of the cruder extracts,fractions,and compounds from Isodon adenantha were screened by in vitro anti-schistosome experiments.Results：Acetone extract,n-butanol fraction,and water fraction at a high concentration（2 mg·mL^- 1） showed schistosomicidal activities within 24 h in the durg-containing RPMI 1640 medium,and dead worms were observed in 48 h.However,at a low concentration（0.5 mg·mL^- 1） dead worms were not observed within 48 h.Both concentrations（2 and 0.5 mg·mL^- 1） of EtOAc fraction showed schistosomicidal activities within 6 h,and dead worms were observed within 24 and 48 h,respectively.Two ent-kaurane-diterpenoids,compounds 1 and 2,caused death of all the tested worms within 24 and 36 h periods at concentration of 200 μg·mL^- 1.Conclusion：Acetone extract,ethyl acetate fraction,n-butanol fraction,water fraction,and compounds 1 and 2 have potential anti-schistosome activities.This study could be useful for the better understand of the biological activities and applicability of Isodon adenantha,as well as for the development of new antischistosomal drugs from natural products in the future.