Guggulsterone inhibits melanogenesis in B16 murine melanoma cells by             downregulating tyrosinase expression.
In the present study, we investigated the effect of guggulsterone on melanogenesis             in B16 melanoma cells and elucidated its possible mechanism of action. The effects             of guggulsterone on melanogenesis were determined by assaying melanin synthesis             and cellular tyrosinase activity in B16/F10 mouse melanoma cells. Guggulsterone             dose-dependently inhibited isobutylmethylxanthine (IBMX)-induced melanogenesis             and cellular tyrosinase activity with no cytotoxicity. Decreased melanin biosynthesis             was accompanied by the reduced expression of melanogenesis-related genes, such             as tyrosinase, microphthalmia-associated transcription factor, tyrosinase-related             protein (TRP)-1 and TRP-2. Guggulsterone also inhibited α-melanocyte stimulating             hormone- or forskolin-induced increases in melanogenesis, suggesting an action             on the cAMP-dependent melanogenic pathway. Co-incubation with chenodeoxycholic             acid, a well-known farnesoid-X receptor agonist, did not affect IBMX-induced melanogenesis.             These results suggest that guggulsterone exerts a melanogenic inhibitory effect             through the downregulation of tyrosinase expression.
Department of Biochemistry, Chonbuk National University Medical                     School, Jeonju, Jeonbuk 561-756, Republic of Korea.
Jeung-Hyun
JH
Koo
Kyoung-Suk
KS
Rhee
Hyoung-Won
HW
Koh
Hyun-Young
HY
Jang
Byung-Hyun
BH
Park
Jin-Woo
JW
Park
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D045744:Cell Line, Tumor; D029744:Commiphora / Q000737:chemistry; D000242:Cyclic AMP / Q000378:metabolism; D015536:Down-Regulation / Q000187:drug effects*; D008543:Melanins / Q000378:metabolism*; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000235:genetics* / Q000378:metabolism; D051379:Mice; D014442:Monophenol Monooxygenase / Q000235:genetics* / Q000378:metabolism; D011282:Pregnenediones / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D008543:Melanins; D011282:Pregnenediones; C023617:pregna-4,17-diene-3,16-dione; D000242:Cyclic AMP; D014442:Monophenol Monooxygenase