Abstract
This study evaluated bioactivity-guided fractionation as a means to identify therapeutic phytochemicals from Pyracantha angustifolia that can attenuate melanogenesis and oxidation. Seven compounds with inhibitory effects on melanin production and tyrosinase (TYR) activity, and ABTS and DPPH radical-scavenging activities, which have not been reported as whitening materials, were isolated from the n-butanol fraction from P. angustifolia leaves (PAL). Among the seven compounds, p-hydroxybenzoic acid β-d-glucosylester (HG), and cimidahurinine (CH) had strong inhibitory effects on melanin production and TYR activity, as well as ABTS and DPPH radical-scavenging activities. Western blot analysis showed that HG and CH suppressed tyrosinase-related protein (TYRP)-1 and TYRP-2 expression. Moreover, HG and CH inhibited reactive oxygen species (ROS) generation in tert-butyl hydroperoxide (t-BHP)-treated B16F10 cells. These results suggest that P. angustifolia containing active compounds, such as HG and CH, is a potent therapeutic candidate for the development of hypopigmenting agents.
Highlights
Melanogenesis involves the production of melanin pigments in melanosomes produced by melanocytes [1,2]
This study examined the anti-melanogenesis and antioxidant activities of each part of the extracts from
This study evaluated the applicability of P. angustifolia by bioactivity-guided fractionation to find natural therapeutic products that can reduce hyperpigmentation
Summary
Melanogenesis involves the production of melanin pigments in melanosomes produced by melanocytes [1,2]. Melanogenesis is enhanced by the activation of tyrosinase (TYR), the key enzyme of melanogenesis. TYR is an enzyme that determines the color of mammalian skin and hair in the melanogenesis of mammals and browning of fruits and fungi [8]. Tyrosine is hydrozylated to 3,4-dihydroxyphenylalanin (DOPA) in melanin synthesis with TYR as a catalyst, which is a copper-containing enzyme present in melanosomes, and oxidized to dopaquinone by TYR [9]. Mammalian melanogenic enzymes are similar metalloproteins, such as TYR, tyrosinase-related protein 1 (TYRP-1), and TYRP-2. TYRP-1 and TYRP-2 are present in melanosomes and catalyze eumelanin-producing reactions. TYRP-1 increases the eumelanin: pheomelanin ratio and protects against oxidative stress through its peroxidase activity [10]. TYRP-2 is the enzyme dopachrome tautomerase (DCT), which facilitates the Antioxidants 2020, 9, 258; doi:10.3390/antiox9030258 www.mdpi.com/journal/antioxidants
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