环阿尔廷烷和葫芦烷糖苷的酪氨酸酶抑制研究及其构效关系
Tyrosinase inhibition studies of cycloartane and cucurbitane glycosides and their structure-activity relationships.
作者信息
Khan Mahmud Tareq Hassan, Choudhary M Iqbal, Mamedova Reyhan P, Agzamova Manzura A, Sultankhodzhaev Mukhlis N, Isaev Mahamed I
机构信息
Pharmacology Research Laboratory, Faculty of Pharmaceutical Sciences, University of Science and Technology, Chittagong, Bangladesh.
出版信息
Bioorg Med Chem. 2006 Sep 1;14(17):6085-8. doi: 10.1016/j.bmc.2006.05.002. Epub 2006 May 23.
In the present paper, tyrosinase inhibition studies and structure-activity relationship of eight cycloartane glycosides and one cucurbitane glycoside and its genin, which were isolated from Astragalus (Leguminoseae) and Bryonia (Cucurbitaceae) plants, have been discussed. The activities are compared with two reference tyrosinase inhibitors, kojic acid and l-mimosine. These studies and the SAR showed that the askendoside B which exhibited highly potent (IC50 =13.95 microM) tyrosinase inhibition could be a possible lead molecule for the development of new medications of several skin diseases related with the over-expression of the enzyme tyrosinase, like hyperpigmentation. The molecule also may be interesting for the cosmetic industries as a skin whitening agent.
本文讨论了从黄芪（豆科）和白蔹（葫芦科）植物中分离得到的8种环阿尔廷烷糖苷、1种葫芦烷糖苷及其苷元的酪氨酸酶抑制研究和构效关系。将这些活性与两种参考酪氨酸酶抑制剂曲酸和L-含羞草碱进行了比较。这些研究和构效关系表明，表现出高效（IC50 = 13.95 microM）酪氨酸酶抑制作用的紫花黄芪苷B可能是开发与酪氨酸酶过度表达相关的几种皮肤病新药物的潜在先导分子，如色素沉着过度。该分子作为皮肤美白剂对化妆品行业也可能具有吸引力。
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