4‐n‐butylresorcinol enhances proteolytic degradation of tyrosinase in B16F10 melanoma cells

Lee, Seok‐Jin; Son, Young Hoon; Lee, Ki Back; Lee, Jin-Haeng; Kim, Hyo-Jun; Jeong, Eui Man; Park, Sang Chul; Kim, In‐Gyu

doi:10.1111/ics.12368

Cited by 19 publications

(20 citation statements)

References 40 publications

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“…Sample preparation and SDS-PAGE were performed as previously described. 49 The following primary antibodies were used: anti- β -actin (Sigma-Aldrich, A5441), TG2, 50 p65 (Santa Cruz Biotechnology, Santa Cruz, CA, USA, sc-8008), p-p65 Ser536 (Cell Signaling Technology, Beverly, MA, USA, #3031) and I κ B α (Cell Signaling Technology, sc-847). After the reaction with horseradish peroxidase-conjugated secondary antibody (Santa Cruz Biotechnology, sc-2004 or sc-2005), immunoreactive proteins were visualized by using a SuperSignal West Pico Chemiluminescent Substrate (Thermo Fisher Scientific Inc.).…”

Section: Methodsmentioning

confidence: 99%

Transglutaminase 2 mediates UV-induced skin inflammation by enhancing inflammatory cytokine production

Lee

Son

et al. 2017

Cell Death Dis

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UV irradiation elicits acute inflammation in the skin by increasing proinflammatory cytokine production in keratinocytes. However, the downstream protein target(s) that link UV radiation to the activation of signaling pathways responsible for cytokine expression have not been fully elucidated. In this study, we report a novel role of transglutaminase 2 (TG2), a member of the TG enzyme family whose activities are critical for cornified envelope formation, in mediating UV-induced inflammation. Our results showed that TG2-deficient mice exhibited reduced inflammatory responses to UV irradiation, including reduced erythema, edema, dilation of blood vessels, inflammatory cell infiltration, and levels of inflammatory cytokines. Using primary mouse keratinocytes and HaCaT cells, we found that UV irradiation-induced cytokine production by activating TG2, but not by upregulating TG2 expression, and that ER calcium release triggered by the UV-induced activation of phospholipase C was required for TG2 activation. Moreover, TG2 activity enhanced p65 phosphorylation, leading to an increase in NF-κB transcriptional activity. These results indicate that TG2 is a critical mediator of cytokine expression in the UV-induced inflammatory response of keratinocytes, and suggest that TG2 inhibition might be useful for preventing UV-related skin disorders, such as photoaging and skin cancer caused by chronic UV exposure.

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Section: Methodsmentioning

confidence: 99%

Transglutaminase 2 mediates UV-induced skin inflammation by enhancing inflammatory cytokine production

Lee

Son

et al. 2017

Cell Death Dis

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“…Inhibitory effect of arctigenin from Fructus arctii extract on tyrosinase gene expression was analysed by Park et al [23] using real time qPCR. Similarly Lee et al [24] elucidate the inhibitory effect of 4-n-butylresorcinol on tyrosinase mRNA expression in B16F10 melanoma cells through real time PCR. Reverse transcription PCR have also been extensively used for estimation of gene expression.…”

Section: Pcrmentioning

confidence: 99%

Microarray as High Throughput Tool for Tyrosinase Gene Expression Analysis

Parveen

Zaidi

Ali

et al. 2017

MOJPB

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Hyper pigmentary problems, including post inflammatory hyper pigmentation, solar lentigos, and melasma, occur widely in the human population and are thus of broad interest for control. Tyrosinase is the key enzyme of melanogenesis and it's over expression results in hyper pigmentation. Tyrosinase is not only liable to human pigmentation, but also responsible for the undesirable enzymatic browning of fruits and vegetables, which is of economic importance. So in order to get rid of the problem, inhibitors of the enzyme tyrosinase have been concerned. Advances in genomics and proteomics have opened up new possibilities for the rapid functional assignment and global characterization of proteins and DNA. Organized collection of molecules on arrays have provided a vigorous platform for rapid screening, lead discovery and eradication of molecular characterization. Nowadays, it is used for the discovery of tyrosinase inhibitor. It involves microarrays of immobilized distinct small molecules or DNA or RNA of cells treated with molecules to be tested and binding of tyrosinase proteins or TYR gene respectively. Compound is then screened and the respective compound is identified as a new small-molecule binder to tyrosinase and used it as potential tyrosinase inhibitor. Its actual binding and inhibitory effects on tyrosinase is also validated using an enzyme-based inhibition assay or other binding assays. As a rapidly maturing technology, high-throughput proteomic and genomic pave the way forward in the treatment of skin hyper pigmentation. Hence in the present review we have focused on the use of microarray technique over the conventional strategies for the elucidation of tyrosinase inhibitors.

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“…4nBRE has already been applied in the synthesis of hydroxyacetophenone derivatives [1], derivatives with benzenepropanoic acid [2], new benzopyrones with bacteriostatic activity [3], naturally occurring 6-acyl-7-methoxycoumarins [4], and pyrazole analogues of isoflavones [5]. Applications of 4nBRE in cosmetology show it to be an effective inhibitor of tyrosinase activity and melanin production for the treatment of hyperpigmentation [6][7][8][9][10]. Additionally, published laboratory studies show much higher effectiveness of 4nBRE when compared to arbutin (ARB) and hydroquinone [9] regarding depigmentation effects.…”

Section: Introductionmentioning

confidence: 99%

4-n-Butylresorcinol-Based Linear and Graft Polymethacrylates for Arbutin and Vitamins Delivery by Micellar Systems

2020

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A novel initiator, bromoester modified 4-n-butylresorcinol (4nBREBr2), was prepared and utilized in controlled atom transfer radical polymerization (ATRP) to obtain three series of amphiphilic copolymers. The V-shaped copolymers of methyl methacrylate (MMA), 2-hydroxyethyl methacrylate (HEMA), and poly(ethylene glycol) methyl ether methacrylate (MPEGMA), abbreviated to P(HEMA–co–MMA), P(HEMA–co–MPEGMA), and P(MMA–co–MPEGMA), were synthesized. Moreover, P((HEMA–graft–PEG)–co–MMA) graft copolymers were prepared by combining the pre-polymerization modification of HEMA and a “click” reaction using a “grafting onto” approach. All copolymers could form micelles with encapsulated active substances (vitamin C (VitC), vitamin E (VitE), arbutin (ARB)), which are used in cosmetology. In vitro studies carried out in a PBS solution (pH 7.4) demonstrates that in most cases the maximum release of active substance was after 1 h. The polymeric systems presenting satisfactory encapsulation characteristics and release profiles are attractive micellar carriers of cosmetic substances, which show a positive effect on the skin condition.

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4‐n‐butylresorcinol enhances proteolytic degradation of tyrosinase in B16F10 melanoma cells

Abstract: 4-n-butylresorcinol inhibits melanogenesis by enhancing proteolytic degradation of tyrosinase as well as competitive binding to tyrosinase. These findings will help to develop new, effective and safe chemicals for the treatment of hyperpigmentation disorders.

Cited by 19 publications

References 40 publications

Transglutaminase 2 mediates UV-induced skin inflammation by enhancing inflammatory cytokine production

Transglutaminase 2 mediates UV-induced skin inflammation by enhancing inflammatory cytokine production

Microarray as High Throughput Tool for Tyrosinase Gene Expression Analysis

4-n-Butylresorcinol-Based Linear and Graft Polymethacrylates for Arbutin and Vitamins Delivery by Micellar Systems

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