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Molecules 2016, 21(5), 575; doi:10.3390/molecules21050575

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

1
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China
2
State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
3
State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Processes, National Post-Doctoral Research Workstation, Jiangsu Kanion Pharmaceutical Co. Ltd., Lianyungang 222001, China
4
State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, Guilin 541004, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 March 2016 / Revised: 26 April 2016 / Accepted: 27 April 2016 / Published: 30 April 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2091 KB, uploaded 30 April 2016]   |  

Abstract

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. View Full-Text
Keywords: Isodon rubescens; medicinal tea; diterpenoid; oridonin; medicinal chemistry Isodon rubescens; medicinal tea; diterpenoid; oridonin; medicinal chemistry
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Li, D.; Han, T.; Xu, S.; Zhou, T.; Tian, K.; Hu, X.; Cheng, K.; Li, Z.; Hua, H.; Xu, J. Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao. Molecules 2016, 21, 575.

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