In vitro cytotoxicity assay, mushroom tyrosinase inhibitory activity and release analysis of kojic monooleate nanodelivery system and in silico molecular docking study against 2Y9X target enzyme
Tyrosinase is the main enzyme that catalyzes the browning of fruits, fungi and vegetables, and melanogenesis process in mammals. Kojic monooleate (KMO) is an ester produced via esterification of kojic acid (KA) with oleic acid and has the potential as a tyrosinase inhibitor. Previously, we have repo...
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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English English |
| Published: |
Editions de Sante
2021
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| Subjects: | |
| Online Access: | http://irep.iium.edu.my/94194/7/94194_In%20vitro%20cytotoxicity%20assay_Scopus.pdf http://irep.iium.edu.my/94194/8/94194_In%20vitro%20cytotoxicity%20assay%2C%20mushroom%20tyrosinase%20inhibitory%20activity%20and%20release%20analysis%20of%20kojic%20monooleate%20nanodelivery%20system.pdf http://irep.iium.edu.my/94194/ https://www.sciencedirect.com/science/article/abs/pii/S1773224721004445?via%3Dihub |
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| Summary: | Tyrosinase is the main enzyme that catalyzes the browning of fruits, fungi and vegetables, and melanogenesis process in mammals. Kojic monooleate (KMO) is an ester produced via esterification of kojic acid (KA) with oleic acid and has the potential as a tyrosinase inhibitor. Previously, we have reported the optimization study of the KMO nanoemulsion using Mixture Experimental Design and Response Surface Methodology. This study aims to investigate the in vitro cytotoxicity, tyrosinase inhibitory and release activities of KMO and KMO nanoemulsion. Our study found that both the KMO and KMO nanoemulsion was not cytotoxic against 3T3 mouse embryonic fibroblast cell line with the IC50 > 500 μg/mL. The tyrosinase inhibition assay conducted by using 3,4-dihydroxy phenyl l-alanine (l-DOPA) substrate revealed a significant potency of KMO (IC50 = 85.98 μM) and its nano-emulsified system (IC50 = 68.20 μg/mL), when compared to KA with the IC50 = 124.28 μM. From Franz cell release study, up to 45.94 ± 0.03% of KMO was released from the nanoemulsion system and diffuses across the cellulose acetate membrane after 8 h of study time, and the kinetic mechanism analysis revealed that the data was most fitted with the zeroth-order model. Moreover, in silico molecular docking was applied to determine binding energy and predict the interaction of mushroom tyrosinase (PDB ID: 2Y9X) with KMO. The binding energy of the KMO against 2Y9X was −5.70 kcal/mol. The best docked complex was mostly interacted via hydrophobic interaction involving His61, His85, Glu256, His259, Asn260, His263, Phe264, Met280, Gly281, Ser282, Val283, Ala286 residues. Based on the results obtained, the KMO nanoemulsion was suggested to be suitable for use in cosmeceuticals field, and further study through in vivo approach should be carried out to clarify the efficacy and safety of the KMO nanoemulsion. |
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