Journal
MOLECULES
Volume 21, Issue 5, Pages -Publisher
MDPI AG
DOI: 10.3390/molecules21050575
Keywords
Isodon rubescens; medicinal tea; diterpenoid; oridonin; medicinal chemistry
Funding
- National Natural Science Foundation of China [81373280, 21502121]
- China Post-Doctoral Science Foundation [2015M570258]
- General Scientific Research Projects of Department of Education in Liaoning Province [L2014382]
- Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University)
- Ministry of Education of China [CMEMR2015-B07]
- Career Development Support Plan for Young and Middle-aged Teachers in Shenyang Pharmaceutical University
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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 mu g/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.
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