Recent advances in medicinal chemistry of oleanolic acid derivatives.

Yi-Hui Yang, Si-Yang Dai, Fu-Hua Deng, Li-Huan Peng, Chang Li, Yue-Hu Pei

Journal: Phytochemistry 2022;203():113397

PMID: 36029846

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Abstract

Oleanolic acid (OA), a ubiquitous pentacyclic oleanane-type triterpene isolated from edible and medicinal plants, exhibits a wide spectrum of pharmacological activities and tremendous therapeutic potential. However, the undesirable pharmacokinetic properties limit its application and development. Numerous researches on structural modifications of OA have been carried out to overcome this limitation and improve its pharmacokinetic and therapeutic properties. This review aims to compile and summarize the recent progresses in the medicinal chemistry of OA derivatives, especially on structure-activity relationship in the last few years (2010-2021). It gives insights into the rational design of bioactive derivatives from OA scaffold as promising therapeutic agents.

Address: Department of Medicinal Chemistry and Natural Medicine Chemistry, College of Pharmacy, Harbin Medical University, Harbin, 150081, PR China.; Department of Medicinal Chemistry and Natural Medicine Chemistry, College of Pharmacy, Harbin Medical University, Harbin, 150081, PR China. Electronic address: [email protected].; Department of Medicinal Chemistry and Natural Medicine Chemistry, College of Pharmacy, Harbin Medical University, Harbin, 150081, PR China. Electronic address: [email protected].

DOI: 10.1016/j.phytochem.2022.113397

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MeSH Terms: Chemistry, Pharmaceutical, Oleanolic Acid, Plants, Medicinal, Structure-Activity Relationship, Triterpenes