title: Functionality study of santalin as tyrosinase inhibitor: A potential depigmentation agent.
abstract: Excessive melanin production leads to hyperpigmentation disorders which results in distressing aesthetic values. Though there are some synthetic depigmentation agents available it has been reported to possess cytotoxic and mutagenic effects. Hence there is a need for the development of safe and non toxic natural tyrosinase inhibitors. Here we report the role of santalin, the chief constituent of Pterocarpus santalinus in inhibition of tyrosinase and melanin synthesis. Santalin inhibited tyrosinase activity dose dependently. Inhibitory kinetic studies revealed mixed type of inhibition with reversible mechanism. Santalin was found to interact with the fluorophore amino acid residue of tyrosinase. Analysis of circular dichroism spectra showed the binding of santalin to tyrosinase which induced the loss of secondary helical structure. Molecular docking result suggested that santalin interact with the catalytic core of tyrosinase through strong hydrogen and hydrophobic bonding. The results of in vitro studies showed santalin inhibited melanogenesis through down regulation of MITF, tyrosinase, TRP-1 and TRP-2 without any cytotoxic effects towards B16F0 melanoma cells. Therefore, our results suggested that santalin possesses anti-tyrosinase activity, which could be utilized as a safe depigmentation agent in the cosmetic field for the treatment of hyperpigmentation disorder.
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: Hemachandran
authors.initials: H
authors.lastname: Hridya
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: Anantharaman
authors.initials: A
authors.lastname: Amrita
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: Sankari
authors.initials: S
authors.lastname: Mohan
authors.affiliation: School of Advanced Sciences, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: Mohan
authors.initials: M
authors.lastname: Gopalakrishnan
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: Thirumal Kumar
authors.initials: TK
authors.lastname: Dakshinamurthy
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors.forename: George Priya
authors.initials: GP
authors.lastname: Doss
authors.affiliation: School of Bio Sciences and Technology, VIT University, Vellore 632014, Tamil Nadu, India. Electronic address: rsiva77in@rediffmail.com.
authors.forename: Ramamoorthy
authors.initials: R
authors.lastname: Siva
mesh_terms: D000818:Animals; D001578:Benzopyrans / Q000378:metabolism / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects; D007700:Kinetics; D008543:Melanins / Q000378:metabolism; D051379:Mice; D051739:Microphthalmia-Associated Transcription Factor / Q000235:genetics; D062105:Molecular Docking Simulation; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D011487:Protein Conformation / Q000187:drug effects; D062327:Skin Lightening Preparations / Q000378:metabolism / Q000494:pharmacology*; D014966:Xanthenes
chemical_list: D001578:Benzopyrans; D004791:Enzyme Inhibitors; D008543:Melanins; D051739:Microphthalmia-Associated Transcription Factor; D014442:Monophenol Monooxygenase; D062327:Skin Lightening Preparations; C030275:Santalin; D014966:Xanthenes
keywords: Hyperpigmentation; Santalin; Tyrosinase