title: Tyrosinase inhibitory effect and inhibitory mechanism of tiliroside from raspberry.
abstract: Tiliroside was found to inhibit both monophenolase and diphenolase activity of mushroom tyrosinase. The lag time of tyrosine oxidation catalyzed by mushroom tyrosinase was obviously lengthened; 0.337 mM of tiliroside resulted in the lag time extension from 46.7 s to 435.1 s. A kinetic analysis shown that tiliroside was a competitive inhibitor for monophenolase and diphenolase with K(i) values of 0.052 mM and 0.26 mM, respectively. Furthermore, tiliroside showed 34.5% (p < 0.05) inhibition of intracellular tyrosinase activity and 54.1% (p < 0.05) inhibition of melanin production with low cytotoxicity on B16 mouse melanoma cells at 0.168 mM. In contrast, arbutin displayed 9.1% inhibition of cellular tyrosinase activity and 29.5% inhibition of melanin production at the same concentration. These results suggested that tiliroside was a potent tyrosinase inhibitor and might be used as a skin-whitening agent and pigmentation medicine.
authors.affiliation: State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, PR China. luyanhua@ecust.edu.cn
authors.forename: Yan-hua
authors.initials: YH
authors.lastname: Lu
authors.forename: Juan
authors.initials: J
authors.lastname: Chen
authors.forename: Dong-zhi
authors.initials: DZ
authors.lastname: Wei
authors.forename: Zheng-tao
authors.initials: ZT
authors.lastname: Wang
authors.forename: Xin-yi
authors.initials: XY
authors.lastname: Tao
mesh_terms: D000363:Agaricales / Q000201:enzymology; D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival; D004789:Enzyme Activation / Q000187:drug effects*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects; D008543:Melanins / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D010936:Plant Extracts / Q000494:pharmacology; D027824:Rosaceae / Q000737:chemistry*; D013722:Teprotide / Q000494:pharmacology*
chemical_list: D005419:Flavonoids; D008543:Melanins; D010936:Plant Extracts; C052083:tiliroside; D013722:Teprotide; D014442:Monophenol Monooxygenase