Inhibition effects of mangosenone F from Garcinia mangostana on melanin formation in B16F10 cells.
Melanogenesis can be controlled by tyrosinase inhibition or by blocking the maturation processes of tyrosinase and its related proteins. Mangostenone F was isolated from the seedcases of Garcinia mangostana . Mangostenone F was shown to be inactive against tyrosinase (IC50 > 200 μM) but was a potent α-glucosidase inhibitor in vitro (IC50 = 21.0 μM). Mangostenone F was found to inhibit production of melanin in the mouse melanoma cell line B16F10. Importantly, unlike most glycosidase inhibitors, mangostenone F displayed very low cytotoxicity (EC50 > 200 μM). The Western blot for expression levels of proteins involved in melanogenesis showed that mangostenone F down-regulated tyrosinase and TRP-2 expression. Treating B16F10 cells with mangostenone F significantly increased the susceptibility of tyrosinase to endoglycosidase H digestion, indicating that tyrosinase was unable to mature fully and pass to the trans-golgi apparatus. Consistent with these data, in lysate assays, mangostenone F was shown to be a better inhibitor of α-glucosidases than deoxynojirimycin, a representative glycosidase inhibitor.
Division of Applied Life Science (BK21 Program), IALS, Graduate School of Gyeongsang National University , Jinju 660-701, Republic of Korea.
Hyung Won
HW
Ryu
Seong Hun
SH
Jeong
Marcus J
MJ
Curtis-Long
Sunin
S
Jung
Ji Won
JW
Lee
Hyun Sim
HS
Woo
Jung Keun
JK
Cho
Ki Hun
KH
Park
D000818:Animals; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D029762:Garcinia mangostana / Q000737:chemistry*; D065089:Glycoside Hydrolase Inhibitors; D020128:Inhibitory Concentration 50; D019746:Intramolecular Oxidoreductases / Q000378:metabolism; D017038:Mannosyl-Glycoprotein Endo-beta-N-Acetylglucosaminidase / Q000378:metabolism; D008543:Melanins / Q000378:metabolism*; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000378:metabolism; D051379:Mice; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors; D044004:Xanthones / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D008543:Melanins; D044004:Xanthones; C000590991:mangostenone F; D014442:Monophenol Monooxygenase; D017038:Mannosyl-Glycoprotein Endo-beta-N-Acetylglucosaminidase; D019746:Intramolecular Oxidoreductases; C042501:dopachrome isomerase