Hussain Hidayat, Green Ivan R, Ali Iftikhar, Khan Ikhlas A, Ali Zulfiqar, Al-Sadi Abdullah M, Ahmed Ishtiaq
a UoN Chair of Oman's Medicinal Plants and Marine Natural Products , University of Nizwa , Nizwa , Sultanate of Oman.
b Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography , University of California , San Diego , CA , USA.
Expert Opin Ther Pat. 2017 Sep;27(9):1061-1072. doi: 10.1080/13543776.2017.1344219. Epub 2017 Jun 30.
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 C-OH, C-OH and CCOH. 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.
熊果酸（UA）属于五环三萜类化合物，已知具有一些非常有趣的生物学特性。人们已经开发出了合成具有生物活性的UA类似物的方法，这使得在2012年至2016年期间合成了大量熊果酸类似物。熊果酸及其类似物可用于治疗多种癌症、炎症性疾病、糖尿病、帕金森病、阿尔茨海默病、乙型肝炎、丙型肝炎和艾滋病等等。涵盖领域：本综述涵盖了2012年至2016年这四年期间发表的关于熊果酸（UA）及其合成衍生物治疗活性的专利。还包括对这些类似物的构效关系（SAR）的讨论。专家观点：熊果酸及其合成衍生物表现出优异的抗癌、抗糖尿病、抗心律失常、抗高血脂、抗菌、抗高胆固醇血症和抗心血管特性。此外，通过对C-OH、C-OH和CCOH位置进行修饰合成了各种熊果酸类似物。值得注意的是，与母体化合物（UA）相比，UA的C-17酰胺和氨基类似物具有更好的抗癌活性。最重要的是，UA有可能与其他抗癌药物缀合或转化为其卤代衍生物，因为这将极大地促进科学家在癌症药物发现中获得先导化合物。
