Tyrosinase inhibitory effect and inhibitory mechanism of tiliroside from raspberry.
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.
Lu
Yan-hua
YH
State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, PR China. luyanhua@ecust.edu.cn
Chen
Juan
J
Wei
Dong-zhi
DZ
Wang
Zheng-tao
ZT
Tao
Xin-yi
XY
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*
D005419:Flavonoids; D008543:Melanins; D010936:Plant Extracts; C052083:tiliroside; D013722:Teprotide; D014442:Monophenol Monooxygenase