Oleanolic acid derivatives for pharmaceutical use: a patent review.
BACKGROUND
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.


METHODS
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.


CONCLUSIONS
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.
a Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease and State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , China.
Chao
C
Lin
a Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease and State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , China.
Xiaoan
X
Wen
a Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease and State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , China.
Hongbin
H
Sun
D000818:Animals; D002681:China; D015195:Drug Design; D006801:Humans; D004366:Nonprescription Drugs / Q000494:pharmacology / Q000627:therapeutic use; D009828:Oleanolic Acid / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D010330:Patents as Topic; D011506:Proteins / Q000378:metabolism*
D004366:Nonprescription Drugs; D011506:Proteins; D009828:Oleanolic Acid
Oleanolic acid; anti-cancer; anti-diabetes; anti-inflammation; anti-osteoporosis; anti-psoriasis; hepatoprotection; hypolipidemic