柑橘皮粗提物中川陈皮素和橙皮苷的酪氨酸酶抑制作用及抑制机制

Tyrosinase inhibitory effects and inhibition mechanisms of nobiletin and hesperidin from citrus peel crude extracts.

作者信息

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

机构信息

State Key Laboratory of Bioreactor Engineering, New World Institute of Biotechnology, East China University of Science and Technology, Shanghai, China.

出版信息

J Enzyme Inhib Med Chem. 2007 Feb;22(1):83-90. doi: 10.1080/14756360600953876.

DOI:10.1080/14756360600953876

PMID:17373552

Abstract

The inhibitory effects of nobiletin and hesperidin from citrus peel crude extracts on tyrosinase diphenolase activity are evaluated. IC50 of nobiletin and hesperidin is 1.49 mM and 16.08mM, respectively and their inhibition mechanism is competitive type with Ki = 2.82 mM and noncompetitive with Ki = 9.16 mM, 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 on melanogenesis in B16 mouse melanoma cells was also evaluated. FGRE showed a significant inhibition (42.5% at 31.25 microg/mL, p < 0.01) while hesperidin showed almost no inhibition. Nobiletin and PCPE give efficacious antiproliferation effects on B16 mouse melanoma cell with IC50 values 88.6 microM and 62.96 microg/mL, respectively, by the MTT test. Hesperidin and other crude extracts showed very low cytotoxity to the B16 cell.

摘要

评估了柑橘皮粗提物中川陈皮素和橙皮苷对酪氨酸酶双酚酶活性的抑制作用。川陈皮素和橙皮苷的IC50分别为1.49 mM和16.08 mM，其抑制机制分别为竞争性（Ki = 2.82 mM）和非竞争性（Ki = 9.16 mM）。用95%乙醇提取柑橘皮（温州蜜柑）粗提物，并用石油醚（PCPE）进行分离。乙醇相（ECPE）进一步从大孔吸附树脂上解吸（FGRE）。它们的IC50值分别为8.09 mg/mL、7.53 mg/mL和4.80 mg/mL。还评估了它们对B16小鼠黑色素瘤细胞黑色素生成的抑制作用。FGRE显示出显著抑制作用（31.25 μg/mL时为42.5%，p < 0.01），而橙皮苷几乎没有抑制作用。通过MTT试验，川陈皮素和PCPE对B16小鼠黑色素瘤细胞具有有效的抗增殖作用，IC50值分别为88.6 μM和62.96 μg/mL。橙皮苷和其他粗提物对B16细胞的细胞毒性非常低。