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Oridonin, a Promising ent-Kaurane Diterpenoid Lead Compound

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China
Department of Medicinal Chemistry and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical College, Xuzhou 221004, China
State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, and School of Chemistry and Pharmacy, Guangxi Normal University, Guilin 541004, China
Authors to whom correspondence should be addressed.
Academic Editor: Chang Won Choi
Int. J. Mol. Sci. 2016, 17(9), 1395;
Received: 24 June 2016 / Revised: 15 August 2016 / Accepted: 18 August 2016 / Published: 24 August 2016
(This article belongs to the Section Bioactives and Nutraceuticals)
PDF [3870 KB, uploaded 24 August 2016]


Oridonin belongs to ent-kaurane tetracyclic diterpenoid and was first isolated from Isodon species. It exhibits inhibitory activities against a variety of tumor cells, and pharmacological study shows that oridonin could inhibit cell proliferation, DNA, RNA and protein synthesis of cancer cells, induce apoptosis and exhibit an antimutagenic effect. In addition, the large amount of the commercially-available supply is also very important for the natural lead oridonin. Moreover, the good stability, suitable molecular weight and drug-like property guarantee its further generation of a natural-like compound library. Oridonin has become the hot molecule in recent years, and from the year 2010, more than 200 publications can be found. In this review, we summarize the synthetic medicinal chemistry work of oridonin from the first publication 40 years ago and share our research experience of oridonin for about 10 years, which may provide useful information to those who are interested in this research field. View Full-Text
Keywords: oridonin; ent-kaurane; medicinal chemistry; structural modification; biological activity oridonin; ent-kaurane; medicinal chemistry; structural modification; biological activity

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Li, D.; Han, T.; Liao, J.; Hu, X.; Xu, S.; Tian, K.; Gu, X.; Cheng, K.; Li, Z.; Hua, H.; Xu, J. Oridonin, a Promising ent-Kaurane Diterpenoid Lead Compound. Int. J. Mol. Sci. 2016, 17, 1395.

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