Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao

摘要

Isodon rubescens has been used as a traditional green tea for more than 1000 years and many medicinal functions of I. rubescens are also very useful, such as its well-known antitumor and antibacterial activities. Oridonin, a bioactive ent-kaurane diterpenoid, is the major ingredient of this medicinal tea. Herein, 22 novel oridonin derivatives were designed and synthesized. The antibacterial activity was evaluated for the first time. Compound >12 was the most promising one with MIC of 2.0 μg/mL against B. subtilis, which was nearly 3-fold stronger than positive control chloromycetin. The antiproliferative property was also assayed and compound >19 showed stronger activity than taxol. The apoptosis-inducing ability, cell cycle arrest effect at S phase and influence of mitochondrial membrane potential by >19 in CaEs-17 cancer cells were first disclosed. Based on the above results, the cell apoptosis induced by compound >19 in CaEs-17 cells was most probably involved in the intrinsic apoptotic pathway.