Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 3 de 3
Filter
Add more filters











Database
Language
Publication year range
1.
J Nat Med ; 74(3): 612, 2020 06.
Article in English | MEDLINE | ID: mdl-32274681

ABSTRACT

The article Cycloartane triterpenoid (23R, 24E)-23-acetoxymangiferonic acid inhibited proliferation and migration in B16-F10 melanoma via MITF downregulation caused by inhibition of both ß-catenin.

2.
J Nat Med ; 73(1): 47-58, 2019 Jan.
Article in English | MEDLINE | ID: mdl-30084054

ABSTRACT

We recently reported that (23R, 24E)-23-acetoxymangiferonic acid (23R-AMA), a cycloartane triterpenoid isolated by activity-guided separation from a methanol extract of Garcinia sp. bark, inhibited melanin production via inhibition of tyrosinase (TYR) expression in the B16-F10 melanoma cell line. Since 23R-AMA also inhibited microphthalmia-associated transcription factor (MITF) expression, an upstream factor of TYR, these features of 23R-AMA were thought to be appropriate for development of whitening cosmetics. However, 23R-AMA exhibited growth inhibition other than inhibition of melanin production in B16-F10 cells. Therefore, we investigated biological activities of 23R-AMA in detail, focused on its application as an anti-melanoma compound. In this study, we demonstrated that 23R-AMA inhibited cell proliferation and basic FGF (bFGF)-induced migration in B16-F10 cells. Furthermore, 23R-AMA promoted ser45/thr41 phosphorylation of ß-catenin and suppressed its intranuclear accumulation, which was suggested to be related to inhibition of MITF expression. The transcriptional activity of MITF is known to be regulated by phosphorylation via activated ERK. Further investigation revealed that 23R-AMA inhibited phosphorylation of c-Raf, MEK-1, and ERK, and also that of upstream molecules including FAK and c-Src. These results suggested that 23R-AMA inhibited growth and migration of B16-F10 melanoma by regulating both MITF expression and its activity. The activities of 23R-AMA reported in this study are new aspects of cycloartane triterpenoids.


Subject(s)
Garcinia/chemistry , Melanoma, Experimental/drug therapy , Microphthalmia-Associated Transcription Factor/genetics , beta Catenin/metabolism , raf Kinases/metabolism , Cell Line, Tumor , Cell Movement , Cell Proliferation , Down-Regulation , Humans , Phosphorylation , Signal Transduction
3.
J Nat Med ; 70(4): 702-7, 2016 Oct.
Article in English | MEDLINE | ID: mdl-27357963

ABSTRACT

The ceramicines, a series of limonoids from Chisocheton ceramicus (Meliaceae), were evaluated for anti-melanin deposition activity on α-melanocyte stimulating hormone (α-MSH) and 3-isobutyl-1-methylxanthine (IBMX)-treated B16-F10 melanoma cell, and several ceramicines were found to be active. The structure-activity relationship of ceramicines as anti-melanin deposition inhibitors was deduced. Furthermore, the mechanism of anti-melanin deposition activity of ceramicine B, a major constituent of C. ceramicus that showed potent anti-melanin deposition activity, was investigated. Tyrosinase enzymatic activity and tyrosinase mRNA expression were not affected by ceramicine B. The anti-melanin deposition activity of ceramicine B was shown to be related to the downregulation of tyrosinase protein expression. These results suggest that ceramicines have potential to be used as depigmentation agents.


Subject(s)
Limonins/pharmacology , Melanins/metabolism , Melanoma, Experimental/metabolism , Meliaceae/chemistry , Monophenol Monooxygenase/metabolism , Plant Extracts/pharmacology , Animals , Cell Line, Tumor , Down-Regulation/drug effects , Melanins/biosynthesis , Mice , Pigmentation/drug effects , Structure-Activity Relationship
SELECTION OF CITATIONS
SEARCH DETAIL