Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis

European Journal of Medicinal Chemistry - Tập 231 - Trang 114147 - 2022
Romeo Romagnoli1, Paola Oliva1, Filippo Prencipe1, Stefano Manfredini2, Maria Paola Germanò3, Laura De Luca3, Federico Ricci3, Diana Corallo4, Sanja Aveic4, Elena Mariotto5, Giampietro Viola5,4, Roberta Bortolozzi5
1Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, 44121, Ferrara, Italy
2Department of Life Sciences and Biotechnology, University of Ferrara, 44121 Ferrara, Italy
3Department of Chemical Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy
4Istituto di Ricerca Pediatrica (IRP), Fondazione Città della Speranza, 35128, Padova, Italy
5Department of Woman's and Child's Health, Hemato-oncology Lab, University of Padova, 35131, Padova, Italy

Tóm tắt

Từ khóa


Tài liệu tham khảo

Park, 2009, Cellular mechanisms regulating human melanogenesis, Cell. Mol. Life Sci., 66, 1493, 10.1007/s00018-009-8703-8

Hearing, 1989, Analysis of mammalian pigmentation at the molecular level, Pigm. Cell Res., 2, 75, 10.1111/j.1600-0749.1989.tb00166.x

Mort, 2015, The melanocyte lineage in development and disease, Development, 142, 620, 10.1242/dev.106567

White, 2008, Melanocytes in development, regeneration and cancer, Cell Stem Cell, 11, 242, 10.1016/j.stem.2008.08.005

Kondo, 2011, Update on the regulation of mammalian melanocyte function and skin pigmentation, Expet Rev. Dermatol., 6, 97, 10.1586/edm.10.70

Brenner, 2008, The protective role of melanin against UV damage in human skin, Photochem. Photobiol., 84, 539, 10.1111/j.1751-1097.2007.00226.x

Herrling, 2008, The role of melanin as protector against free radicals in skin and its role as free radical indicator in hair, Spectrochim. Acta Mol. Biomol. Spectrosc., 69, 1429, 10.1016/j.saa.2007.09.030

Rinnerthaler, 2015, Oxidative stress in aging human skin, Biomolecules, 5, 545, 10.3390/biom5020545

Dorga, 2014, Pigmentary disorders: an insight, Pigment Int., 1, 5, 10.4103/2349-5847.135429

Speeckaert, 2014, The biology of hyperpigmentation syndromes, Pigment Cell Melanoma Res., 27, 512, 10.1111/pcmr.12235

Maymone, 2017, The impact of skin hyperpigmentation and hyperchromia on quality of life: a crosssectional study, J. Am. Acad. Dermatol., 77, 775, 10.1016/j.jaad.2017.05.009

Liu, 2014, Developmental pathways activated in melanocytes and melanoma, Arch. Biochem. Biophys., 563, 13, 10.1016/j.abb.2014.07.023

Slominski, 2015, The role of melanin pigment in melanoma, Exp. Dermatol., 24, 258, 10.1111/exd.12618

Schadendorf, 2018, Lancet, 392, 971, 10.1016/S0140-6736(18)31559-9

Bose, 2018, Parkinson's disease and melanoma: co-occurrence and mechanisms, J. Parkinsons Dis., 8, 385, 10.3233/JPD-171263

Greco, 2014, Neuromelanin and Parkinson's disease, 913

B Roberts, 2015, The pigment in alkaptonuria relationship to melanin and other coloured substances: a review of metabolism, composition and chemical analysis, JIMD Rep., 24, 51, 10.1007/8904_2015_453

Rittiè, 2015, Natural and sun-induced aging of human skin, Cold Spring Harb. Perspect. Med., 5

Imokawa, 2015, Biological mechanisms underlying the ultraviolet radiation-induced formation of skin wrinkling and sagging II: over-expression of neprilysin plays an essential role, Int. J. Mol. Sci., 16, 7776, 10.3390/ijms16047776

Farage, 2008, Intrinsic and extrinsic factors in skin ageing: a review, Int. J. Cosmet. Sci., 30, 87, 10.1111/j.1468-2494.2007.00415.x

Lai, 2018, Structure and function of human tyrosinase and tyrosinase-related proteins, Chem. Eur J., 24, 47, 10.1002/chem.201704410

Prota, 1993, Regulatory mechanisms of melanogenesis: beyond the tyrosinase concept, J. Invest. Dermatol., 100, S156, 10.1038/jid.1993.69

Hearing, 2011, Determination of melanin synthetic pathways, J. Invest. Dermatol., 131, E8, 10.1038/skinbio.2011.4

Jeon, 2005, Inhibitory effects on L-dopa oxidation of tyrosinase by skin-whitening agents, Bull. Kor. Chem. Soc., 26, 1135, 10.5012/bkcs.2005.26.7.1135

Gillbro, 2011, The melanogenesis and mechanisms of skin-lightning agents-existing and new approaches, Int. J. Cosmet. Sci., 33, 210, 10.1111/j.1468-2494.2010.00616.x

Lin, 2008, Natural products with skin-whitening effects, J. Food Drug Anal., 16, 1

Pillaiyar, 2017, Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 32, 403, 10.1080/14756366.2016.1256882

Smit, 2009, The hunt for natural skin whitening agents, Int. J. Mol. Sci., 10, 5326, 10.3390/ijms10125326

Solano, 2006, Hypopigmenting agents: an updated review on biological, chemical and clinical aspects, Pigm. Cell Res., 19, 550, 10.1111/j.1600-0749.2006.00334.x

Pillaiyar, 2017, Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 32, 403, 10.1080/14756366.2016.1256882

Sanchez-Ferrer, 1995, Tyrosinase: a comprehensive review of its mechanism, Biochim. Biophys. Acta, 1247, 1, 10.1016/0167-4838(94)00204-T

Olivares, 2009, New insights into the active site structure and catalytic mechanism of tyrosinase and its related proteins, Pigment Cell Melanoma Res., 22, 750, 10.1111/j.1755-148X.2009.00636.x

Hearing, 1980, Mammalin tyrosinase. Stoichiometry and measurement of reaction products, Biochim. Biophys. Acta, 611, 251, 10.1016/0005-2744(80)90061-3

Korner, 1982, Mammalian tyrosinase catalyzes three reactions in the biosynthesis of melanin, Science, 217, 1163, 10.1126/science.6810464

Kanteev, 2015, Structure-function correlations in tyrosinases, Protein Sci., 24, 1360, 10.1002/pro.2734

Lai, 2018, Structure and function of human tyrosinase and tyrosinase-related proteins, Chemistry, 24, 47, 10.1002/chem.201704410

Buitrago, 2016, Are human tyrosinase and related proteins suitable targets for melanoma therapy?, Curr. Top. Med. Chem., 16, 3033, 10.2174/1568026616666160216160112

Chang, 2012, Natural melanogenesis inhibitors acting through the down-regulation of tyrosinase activity, Materials, 5, 1661, 10.3390/ma5091661

Wu, 2014, Tyrosinase inhibitors from terrestrial and marine resources, Curr. Top. Med. Chem., 14, 1425, 10.2174/1568026614666140523115357

Khan, 2012, Novel tyrosinase inhibitors from natural resources-their computational studies, Curr. Med. Chem., 19, 2262, 10.2174/092986712800229041

Saruno, 1979, Kojic acid, a tyrosinase inhibitor from Aspergillus albus, Agric. Biol. Chem., 43, 1337

Maeda, 1996, Arbutin: mechanism of its depigmenting action in human melanocyte culture, J. Pharmacol. Exp. Therapeut., 276, 765

Westerhof, 2005, Hydroquinone and its analogues in dermatology-a potential health risk, J. Cosmet. Dermatol., 4, 55, 10.1111/j.1473-2165.2005.40202.x

Likhitwitayawuid, 2008, Stilbenes with tyrosinase inhibitory activity, Curr. Sci., 94, 44

Tu, 2012, Curcumin inhibits melanogenesis in human melanocytes, Phytother Res., 26, 174, 10.1002/ptr.3517

Orhan, 2014, Flavonoid derivatives as potent tyrosinase inhibitors-a survey of recent findings between 2008-2013, Curr. Top. Med. Chem., 14, 1486, 10.2174/1568026614666140523120741

Arroo, 2020, Flavones as tyrosinase inhibitors: kinetic studies in vitro and in silico, Phytochem. Anal., 31, 314, 10.1002/pca.2897

Shimizu, 2000, Inhibition of tyrosinase by flavonoids, stilbenes and related 4-substituted resorcinols: structure-activity investigations, Planta Med., 66, 11, 10.1055/s-2000-11113

Monteiro, 2013, A comparative study of the efficacy of 4% hydroquinone vs 0.75% kojic acid cream in the treatment of facial melasma, Indian J. Dermatol., 58, 157, 10.4103/0019-5154.108070

Andersen, 2010, Final amended safety assessment of hydroquinone as used in cosmetics, Int. J. Toxicol., 29, 274S, 10.1177/1091581810385957

Westerhof, 2005, Hydroquinone and its analogues in dermatology-a potential health risk, J. Cosmet. Dermatol., 4, 55, 10.1111/j.1473-2165.2005.40202.x

Ogiwara, 2015, Evaluation of the repeated-dose liver, bone marrow and peripheral blood micronucleus and comet assays using kojic acid, Mutat. Res. Genet. Toxicol. Environ. Mutagen, 780, 111, 10.1016/j.mrgentox.2015.01.004

Burnett, 2010, Final report of the safety assessment of Kojic acid as used in cosmetics, Int. J. Toxicol., 29, 244S, 10.1177/1091581810385956

Lee, 2016, Natural, semisynthetic and synthetic tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 31, 1, 10.3109/14756366.2015.1004058

Yang, 1999, Effects of 4-tertiary butylphenol on the tyrosinase activity in human melanocytes, Pigm. Cell Res., 12, 237, 10.1111/j.1600-0749.1999.tb00756.x

Yamazaki, 2010, N-(3,5-Dihydroxybenzoyl)-6-hydroxytryptamine as a novel human tyrosinase inhibitor that inactivates the enzyme in cooperation with L-3,4-dihydroxyphenylalanine, Chem. Pharm. Bull., 58, 1536, 10.1248/cpb.58.1536

Gaskell, 2005, Genotoxicity of the benzene metabolites para-benzoquinone and hydroquinone, Chem. Biol. Interact., 153, 267, 10.1016/j.cbi.2005.03.034

Dubois, 2012, Versatile effect of aurone structure on mushroom tyrosinase activity, Chembiochem, 13, 559, 10.1002/cbic.201100716

Haudecoeur, 2017, 2-Hydroxypyridine-N-oxide-embedded aurones as potent human tyrosinase inhibitors, ACS Med. Chem. Lett., 8, 55, 10.1021/acsmedchemlett.6b00369

Arrowitz, 2019, Effective tyrosinase inhibition by thiamidol results in significant improvement of mild to moderate melasma, J. Invest. Dermatol., 139, 1691, 10.1016/j.jid.2019.02.013

Philipp-Dormston, 2020, Thiamidol containing treatment regimens in facial hyperpigmentation: an international multi-center approach consisting of a double-blind, controlled, split-face study and of an open label, real-world study, Int. J. Cosmet. Sci., 42, 377, 10.1111/ics.12626

Roulier, 2020, Advances in the design of genuine human tyrosinase inhibitors for targeting melanogenesis and related pigmentations, J. Med. Chem., 63, 13428, 10.1021/acs.jmedchem.0c00994

Zolghadri, 2019, A comprehensive review on tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 34, 279, 10.1080/14756366.2018.1545767

Lee, 2016, Natural, semisynthetic and synthetic tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 3, 1, 10.3109/14756366.2015.1004058

Abbas, 2017, Development of highly potent melanogenesis inhibitor by in vitro, in vivo and computational studies, Drug Des. Dev. Ther., 11, 2029, 10.2147/DDDT.S137550

Ullah, 2016, Tyrosinase inhibitors: a patent review (2011-2015), Expert Opin. Ther. Pat., 26, 347, 10.1517/13543776.2016.1146253

Nazir, 2020, Hydroxyl substituted benzoic acid/cinnamic acid derivatives: tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies, Bioorg. Med. Chem. Lett, 30, 10.1016/j.bmcl.2019.126722

Garcia-Jimenez, 2018, Catalysis and inhibition of tyrosinase in the presence of cinnamic acid and some of its derivatives, Int. J. Biol. Macromol., 119, 548, 10.1016/j.ijbiomac.2018.07.173

Lee, 2019, Inhibitory effects of N-(acryloyl) benzamide derivatives on tyrosinase and melanogenesis, Bioorg. Med. Chem., 27, 3929, 10.1016/j.bmc.2019.07.034

Ullah, 2019, Tyrosinase inhibition and anti-melanin generation effect of cinnamamide analogues, Bioorg. Chem., 87, 43, 10.1016/j.bioorg.2019.03.001

Ullah, 2019, Synthesis of cinnamic amide derivatives and their anti-melanogenic effect in α-MSH-stimulated B16F10 melanoma cells, Eur. J. Med. Chem., 161, 78, 10.1016/j.ejmech.2018.10.025

Ullah, 2018, Design, synthesis and anti-melanogenic effect of cinnamamide derivatives, Bioorg. Med. Chem., 26, 5672, 10.1016/j.bmc.2018.10.014

Takahashi, 2010, Tyrosinase inhibitory activities of cinnamic acid analogues, Pharmazie, 65, 913

Song, 2011, Comparison of the antimelanogenic effects of p-coumaric acid and its methyl ester and their skin permeabilities, J. Dermatol. Sci., 63, 17, 10.1016/j.jdermsci.2011.03.012

Kwak, 2015, Ascorbyl coumarates as multifunctional cosmeceutical agents that inhibit melanogenesis and enhance collagen synthesis, Arch. Dermatol. Res., 307, 635, 10.1007/s00403-015-1583-x

Micillo, 2018, Conjugation with dihydrolipoic acid imparts caffeic acid ester potent inhibitory effect on dopa oxidase activity of human tyrosinase, Int. J. Mol. Sci., 19, 2156, 10.3390/ijms19082156

Leoty-Okombi, 2013, In vitro melanogenesis inhibitory effects of N-feruloyldopamine, J. Cosmet. Sci., 64, 133

Ashraf, 2015, Synthesis, kinetic mechanism and docking studies of vanillin derivatives as inhibitors of mushroom tyrosinase, Bioorg. Med. Chem, 23, 5870, 10.1016/j.bmc.2015.06.068

Song, 2012, Discovery of small molecules that inhibit melanogenesis via regulation of tyrosinase expression, Bioorg. Med. Chem. Lett, 22, 6943, 10.1016/j.bmcl.2012.09.003

Raza, 2020, Molecular docking, dynamic simulations, kinetic mechanism, cytotoxicity evaluation of N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl}butanamides as tyrosinase and melanin inhibitors: in vitro, in vivo and in silico approaches, Bioorg. Chem., 94, 10.1016/j.bioorg.2019.103445

Vittorio, 2020, 4-Fluorobenzylpiperazine-Containing derivatives as efficient inhibitors of mushroom tyrosinase, ChemMedChem, 15, 1757, 10.1002/cmdc.202000125

Ielo, 2019, Exploiting the 1-(4-fluorobenzyl)piperazine fragment for the development of novel tyrosinase inhibitors as anti-melanogenic agents: design, synthesis, structural insights and biological profile, Eur. J. Med. Chem., 178, 380, 10.1016/j.ejmech.2019.06.019

Gür, 2019, Novel piperazine amides of cinnamic acid derivatives as tyrosinase inhibitors, Lett. Drug Des. Discov., 16, 36, 10.2174/1570180815666180420105652

For the preparation of 1-(4-fluoro-3-chlorophenyl)piperazine (20f) see: D.J. O'Neill, E. Saiah, S.W.A. Kang, A. Brearley, J. Bentley. Pyrrole mTORC Inhibitors and Uses Thereof. WO/2018/089493.

Banziger, 2003, Tetrahedron: Asymmetry, 14, 3469, 10.1016/j.tetasy.2003.07.024

Kwak, 2020, Synthesis and evaluation of sulfonyl piperazine LpxH inhibitors, Bioorg. Chem., 102, 10.1016/j.bioorg.2020.104055

Cao, 2018, Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D3 receptor agonists, MedChemComm, 9, 1457, 10.1039/C8MD00237A

Vanitha, 2017, Isolation and characterisation of mushroom tyrosinase and screening of herbal extracts for anti-tyrosinase activity, Int. J. ChemTech. Res., 10, 1156

Jones, 1997, J. Mol. Biol., 267, 727, 10.1006/jmbi.1996.0897

2016

MacRae, 2015, Zebrafish as tools for drug discovery, Nat. Rev. Drug Discov., 14, 721, 10.1038/nrd4627

Cassar, 2020, Use of zebrafish in drug discovery toxicology, Chem. Res. Toxicol., 33, 95, 10.1021/acs.chemrestox.9b00335

Ferro, 2016, Searching for indole derivatives as potential mushroom tyrosinase inhibitors, J. Enzym. Inhib. Med. Chem., 31, 398

Ismaya, 2011, Crystal structure of Agaricus bisporus mushroom tyrosinase: identity of the tetramer subunits and interaction with tropolone, Biochemistry, 50, 5477, 10.1021/bi200395t

De Luca, 2020, Discovery of a new potent inhibitor of mushroom tyrosinase (Agaricus bisporus) containing 4-(4-hydroxyphenyl)piperazin-1-yl moiety, Bioorg. Med. Chem., 28, 115497, 10.1016/j.bmc.2020.115497

Baytas, 2014, Biological evaluation and molecular docking studies of trans-indole-3-acryl amide derivatives as tubulin polymerization inhibitors Bioorg, Med. Chem., 22, 3096

Westerfield, 2000