Inhibition Effects of Mangosenone F from Garcinia mangostana on Melanin Formation in B16F10 Cells

Abstract

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.

Inhibition of cell proliferation, migration and invasion of B16-F10 melanoma cells by α-mangostin

“…Hamid and colleagues [26] have demonstrated the melanogenic potential of mangosteen leaf extract in B16-F1 melanoma cells. Conversely, mangostenone F was found to inhibit melanin production [27]. Since terminal differentiation is a part of apoptotic process [28] we also investigate the effect of a-M on cell cycle distribution.…”

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

“…Xanthone derivative mangostenone F 79, isolated from the fruit case of Garcinia mangostana, was tested for their inhibitory activity against a range of enzymes. Thus, against aglucosidase activity (from Saccharomyces cerevisiae) showed an IC 50 ¼ 21.0 ± 0.8 mM (positive control 1-deoxynorjirimycin, IC 50 ¼ 39.5 ± 0.5 mM) [44,68] and against b-glucosidase activity (from almond) presented an IC 50 ¼ 212 ± 18 mM, being not active to inhibit the action of enzymes such as a-mannosidase (from jack been), a-galactosidase (from green coffee bean), b-galactosidase (from bovine liver), a-rhamnosidase (from Penicillium decumbens) and a-amylase (from porcine pancreas) [68].…”

A tocotrienol quinone dimer and xanthones from the leaf extract of Garcinia nigrolineata

“…xanthones and benzophenones were the most common compounds isolated from this genus [5][6][7][8][9][10][11]. These types of compounds have displayed a wide range of biological activities such as anti-bacterial, cytotoxic, anti-HIV, α-glucosidase inhibitory, antioxidant, antiinflammatory, antimalarial, and anti-pyretic activities [12][13][14][15][16][17][18][19]. G. nigrolineata is a small to medium sized tree widely distributed throughout Malaysia, Thailand and Myanmar.…”