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Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao
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Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao
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Journal Article
Antitumor and Antibacterial Derivatives of Oridonin: A Main Composition of Dong-Ling-Cao
2016
Overview
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.
Publisher
MDPI AG,MDPI
Subject
Anti-Bacterial Agents - isolation & purification
/ Anti-Bacterial Agents - pharmacology
/ Antineoplastic Agents, Phytogenic - isolation & purification
/ Antineoplastic Agents, Phytogenic - pharmacology
/ Cancer
/ Cell Proliferation - drug effects
/ Diterpenes, Kaurane - chemistry
/ Diterpenes, Kaurane - pharmacology
/ Drug Screening Assays, Antitumor
/ E coli
/ Humans
/ oridonin
