2013
DOI: 10.4062/biomolther.2013.032
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Hesperidin Suppresses Melanosome Transport by Blocking the Interaction of Rab27A-Melanophilin

Abstract: We investigated the inhibitory effects of hesperidin on melanogenesis. To find melanosome transport inhibitor from natural products, we collected the structural information of natural products from Korea Food and Drug Administration (KFDA) and performed pharmacophore-based in silico screening for Rab27A and melanophilin (MLPH). Hesperidin did not inhibit melanin production in B16F10 murine melanoma cells stimulated with α-melanocyte stimulating hormone (α-MSH), and also did not affect the catalytic activity of… Show more

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Cited by 26 publications
(33 citation statements)
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“…Equally, by sequestering metal ions or the effects on the expression of endogenous protein tissue inhibitors of metalloproteinase (TIMPs) [ 9 ], flavonoids can act protectively. Flavonoids’ skin whitening activity relates to their modulation of tyrosinase activity, through their chelating of calcium(II), in the formation of L-dopaquinone, which is a part of the melanogenesis process [ 56 ]. This ability is common to quercetin, cyanidin, and kaempferol, while their glycoside forms have not shown this capability [ 3 ].…”
Section: Discussionmentioning
confidence: 99%
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“…Equally, by sequestering metal ions or the effects on the expression of endogenous protein tissue inhibitors of metalloproteinase (TIMPs) [ 9 ], flavonoids can act protectively. Flavonoids’ skin whitening activity relates to their modulation of tyrosinase activity, through their chelating of calcium(II), in the formation of L-dopaquinone, which is a part of the melanogenesis process [ 56 ]. This ability is common to quercetin, cyanidin, and kaempferol, while their glycoside forms have not shown this capability [ 3 ].…”
Section: Discussionmentioning
confidence: 99%
“…Daily topical applications of HSD microemulsion have shown a significant skin whitening effect, reduction in trans-epidermal water loss, and inhibition of irritation effect after exposure to UV rays after four weeks. In their study, Kim et al [ 56 ] showed that HSD had a depigmentation effect by blocking the melanophilin, a tripartite protein complex which is a response for transport of the melanosome into the melanocytes. This was proven by melanosome aggregation tests in cells.…”
Section: Discussionmentioning
confidence: 99%
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“…Hesperidin that is a major component of our CPE neither inhibit melanin production in B16F10 murine melanoma cells stimulated with α-melanocyte stimulating hormone nor affect the catalytic activity of tyrosinase. Instead, hesperidin inhibited melanosome transport in melanocytes and exerted a skin lightening effect in a pigmented reconstructed epidermis model [13].…”
Section: Subjective Efficacymentioning
confidence: 97%
“…According to a recent study, Rab27a-Mlph and Mlph-Myo5a interactions are very important for melanosome transport. For example, hesperidin blocks the Rab27a-Mlph interaction and therefore causes melanosome aggregation in melanocytes [8]. Also, manassantin B causes melanosome aggregation in melanocytes by blocking the Mlph-Myo5a interaction [9].…”
Section: Introductionmentioning
confidence: 99%