Antimicrobial and cytotoxic activities of several ammonium derivatives of diterpenoids steviol and isosteviol have been investigated in vitro. The results have showed that these compounds possess high antibacterial activity against MRSA strains and cytotoxic effect against cancer cell lines MCF-7, M−HeLa, A-549, PC3, HepG2, T98G. Lead compounds 4 and 5 were detected, which, in the case of the MCF-7 cell line (human breast adenocarcinoma), showed IC₅₀ at the doxorubicin level with a selectivity index of 5.0–5.2. Flow cytometry and laser confocal microscopy analysis demonstrated that the mechanism of cytotoxic effects of the tested compounds on MCF-7 cells could be associated with the induction of apoptosis along the mitochondrial pathway. At the same time, they did not cause hemolysis and showed only slight cytotoxicity with respect to normal human cells of embryonic lung (Wi-38).

The obtained results allow us to consider the studied compounds as promising scaffolds for the design of new effective antibacterial drugs and anticancer agents targeting mitochondria.

体外研究了二萜类甜菊醇和异甜菊醇的几种铵衍生物的抗菌和细胞毒活性。结果表明，这些化合物对 MRSA 菌株具有高抗菌活性，对癌细胞系 MCF-7、M-HeLa、A-549、PC3、HepG2、T98G 具有细胞毒作用。检测到先导化合物4和5，在 MCF-7 细胞系（人乳腺癌）的情况下，其 IC ₅₀在多柔比星水平，选择性指数为 5.0-5.2。流式细胞术和激光共聚焦显微镜分析表明，受试化合物对 MCF-7 细胞的细胞毒性作用机制可能与沿线粒体途径诱导细胞凋亡有关。同时，它们不会引起溶血，并且对胚胎肺（Wi-38）的正常人细胞仅显示出轻微的细胞毒性。

获得的结果使我们能够将所研究的化合物视为设计新的有效抗菌药物和靶向线粒体的抗癌剂的有前途的支架。