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Expert Opin Ther Pat. 2016 Jun;26(6):643-55. doi: 10.1080/13543776.2016.1182988. Epub 2016 May 10.

Oleanolic acid derivatives for pharmaceutical use: a patent review.

Author information

1
a Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease and State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , China.

Abstract

INTRODUCTION:

Oleanolic acid belongs to the pentacyclic triterpene family. In China, oleanolic acid has been used as an over the counter (OTC) hepatoprotective drug for decades. Oleanolic acid and its derivatives present a wide variety of biological activities, supporting their pharmaceutical uses for multiple diseases.

AREAS COVERED:

Representative patent publications (1971-2015) covering the preparation, pharmaceutical compositions, and medical uses of oleanolic acid and its derivatives are analyzed, with focus on their anticancer, anti-osteoporosis, anti-obesity, anti-diabetic, lipid-lowering, anti-inflammatory, antioxidant, immune-regulatory, and hepatoprotective effects. A large number of Chinese patents have been given particular attention in this review.

EXPERT OPINION:

Detailed efficacy studies are highly worth doing to undoubtedly confirm the clinical potential of oleanolic acid and its derivatives. Based on that, it would be critical to identify the key protein targets of the drugs so as to promote drug development and search for new lead compounds. Together, there is a huge potential for drug-repositioning of oleanolic acid, particularly in the areas of metabolic disease and immunological disorders.

KEYWORDS:

Oleanolic acid; anti-cancer; anti-diabetes; anti-inflammation; anti-osteoporosis; anti-psoriasis; hepatoprotection; hypolipidemic

PMID:
27113324
DOI:
10.1080/13543776.2016.1182988
[Indexed for MEDLINE]

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