Ursolic acid derivatives for pharmaceutical use: a patent review (2012-2016)

Expert Opin Ther Pat. 2017 Jun 30:1-12. doi: 10.1080/13543776.2017.1344219. [Epub ahead of print] Hussain H1,2, Green IR3, Ali I4, Khan IA5, Ali Z5, Al-Sadi AM6, Ahmed I7. Author information 1 a UoN Chair of Oman's Medicinal Plants and Marine Natural Products , University of Nizwa , Nizwa , Sultanate of Oman. 2 b Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography , University of California , San Diego , CA , USA. 3 c Department of Chemistry and Polymer Science , University of Stellenbosch , Stellenbosch , South Africa. 4 d Department of Chemistry , Karakoram International University , Gilgit-Baltistan , Pakistan. 5 e National Center for Natural Products Research , University of Mississippi , Oxford , MS , USA. 6 f Department of Crop Sciences, College of Agricultural and Marine Sciences , Sultan Qaboos University , Al Khod , Oman. 7 g DFG Centre for Functional Nanostructures , Karlsruhe Institute of Technology (KIT) , Karlsruhe , Germany. Abstract INTRODUCTION: Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012-2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson's disease, Alzheimer's disease, hepatitis B, hepatitis C and AIDS to mention but a few. Areas covered: This review covers patents on therapeutic activities of ursolic acid (UA) and its synthetic derivatives published during the four year period 2012-2016. A discussion about structure-activity relationships (SAR) of these analogs is also included. Expert opinion: Ursolic acid and its synthetic derivatives demonstrated excellent anticancer, antidiabetic, antiarrhythmic, anti-hyperlipidemic, antimicrobial, anti-hypercholesterolemic, and anti-cardiovascular properties. Additionally, various ursolic acid analogues have been synthesized through modification at positions C2-OH, C3-OH and C17-CO2H. It is noteworthy that the C-17 amide and amino analogs of UA possessed better anticancer activity compared to the parent compound (UA). Most importantly, UA has the potential to conjugate with other anticancer drugs or be transformed into its halo derivatives since this will greatly facilitate scientists to get lead compounds in cancer drug discovery. KEYWORDS: Ursolic acid; anti-inflammatory; anticancer; diabetes; in vitro; in vivo PMID: 28637397 DOI: 10.1080/13543776.2017.1344219 Share on FacebookShare on TwitterShare on Google+