基于人体等效剂量的蟾酥量—效关系探讨

目的：探讨中药材蟾酥的量—效/毒关系。方法：引用相关整体动物有效剂量的文献数据,根据体表面积法换算药材蟾酥的人体等效剂量（HED）。结果：折算蟾酥抗炎的HED为9.8-39.2 mg/日,抗肿瘤HED为53.7-104.7 mg/日,毒性HED为162-585.4 mg/日。结论：蟾酥用于炎症治疗的HED较小,接近甚至低于药典推荐用量（15-30 mg/日）,提示其临床用量具有一定科学、合理性;但分析显示抗肿瘤的HED较高,其上限与蟾酥中毒的HED接近,提示中药材蟾酥用于肿瘤的中医处方剂量需谨慎设计。

A new bufadienolide with cytotoxic activity from the Chinese traditional drug Ch'an Su

AIM: To study the bufadienolides in the Chinese traditional drug "Ch'an Su" and their cytotoxic activity. METHOD: Various chromatographic techniques were used to isolate the constituents, and their structures were elucidated through physical and spectroscopic data. RESULTS: Twenty compounds were isolated, and eighteen were evaluated in vitro for their cytotoxic activity against A-549 and K-562 cells. CONCLUSION: Compound 1(bufalin 3β-acrylic ester) was a new bufadienolide and exhibited the most potent activity against the two tumor cell lines with IC50 values of 7.16 and 6.83 nmol·L–1. The relationships between structure and activity are discussed.