3971-27-5Relevant articles and documents
POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC BODY
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Paragraph 0160; 0162, (2021/02/19)
To provide a polymerizable compound giving such properties when added to a solution comprising a polymerizable composition that the resultant polymerizable composition has high storage stability and can induce a liquid crystal phase alignment in a short t
Inhibitors of mammalian melanocyte tyrosinase: In vitro comparisons of alkyl esters of gentisic acid with other putative inhibitors
Curto, Ernest V.,Kwong, Cecil,Hermersdoerfer, Heino,Glatt, Hansruedi,Santis, Chie,Virador, Victoria,Hearing Jr, Vincent J.,Dooley, Thomas P.
, p. 663 - 672 (2008/04/18)
To discover safe and effective topical skin-lightening agents, we have evaluated alkyl esters of the natural product gentisic acid (GA), which is related to our lead compound methyl gentisate (MG), and four putative tyrosinase inhibitors, utilizing mammalian melanocyte cell cultures and cell-free extracts. Desirable characteristics include the ability to inhibit melanogenesis in cells (ic50 50 ~ 11 and 20 μg/mL, respectively). For comparison, hydroquinone (HQ), a commercial skin 'bleaching' agent, was a less effective enzyme inhibitor (ic50 ~ 72 μg/mL), and was highly cytotoxic to melanocytes in vitro at concentrations substantially lower than the ic50 for enzymatic inhibition. Kojic acid was a potent inhibitor of the mammalian enzyme (ic50 ~ 6 μg/mL), but did not reduce pigmentation in cells. Both arbutin and magnesium ascorbyl phosphate were ineffective in the cell-free and cell-based assays. MG at 100 μg/mL exhibited a minimal inhibitory effect on DHICA oxidase (TRP-1) and no effect on DOPAchrome tautomerase (TRP-2), suggesting that MG inhibits melanogenesis primarily via tyrosinase inhibition. MG and GA were non-mutagenic at the hprt locus in V79 Chinese hamster cells, whereas HQ was highly mutagenic and cytotoxic. The properties of MG in vitro, including (1) pigmentation inhibition in melanocytes, (2) tyrosinase inhibition and selectivity, (3) reduced cytotoxicity relative to HQ, and (4) lack of mutagenic potential in mammalian cells, establish MG as a superior candidate skin-lightening agent. Copyright (C) 1999 Elsevier Science Inc.