文献类型：期刊文献

英文题名：Tyrosinase inhibitory effects and inhibition mechanisms of nobiletin and hesperidin from citrus peel crude extracts

作者：Zhang, Chongwei; Lu, Yanhua; Tao, Lin; Tao, Xinyi; Su, Xiaochun; Wei, Dongzhi

机构：[1]E China Univ Sci & Technol, New World Inst Biotechnol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China

年份：2007

卷号：22

期号：1

起止页码：91

外文期刊名：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000245098100014)】；

语种：英文

外文关键词：citrus unshiu Marc.; nobiletin; hesperidin; B16 mouse melanoma; crude extract; tyrosinase inhibitor; melanin; Traditional Chinese Medicine; SAR

摘要：The inhibitory effects of nobiletin and hesperidin from citrus peel crude extracts on tyrosinase diphenolase activity have been evaluated. IC50 of nobiletin and hesperidin were 1.49mM and 16.08mM, respectively and their inhibition mechanisms are competitive type with inhibition constant (K-i) 2.82mM and noncompetitive type with K-i 9.16mM, respectively. Crude extracts from citrus peel (C. unshiu Marc.) were extracted with 95% ethanol and fractionated by petroleum ether (PCPE). The ethanol phase (ECPE) was further desorbed from macroporous adsorption resin (FGRE). Their IC50 values were 8.09 mg/mL, 7.53 mg/mL and 4.80 mg/mL, respectively. Their inhibition of melanogenesis in B16 mouse melanoma cells was also evaluated. FGRE showed a significant inhibition (42.48% at 31.25 mu g/mL, p < 0.01) while hesperidin showed almost no inhibition. Nobiletin and PCPE gave efficacious antiproliferation effects on the B16 mouse melanoma cell with IC50 values 88.6 mu M and 62.96 mu g/mL, respectively, through the MTT test. Hesperidin and other crude extracts showed very low cytotoxity to the B16 cell.