Elucidating the Role of Santalol as a Potent Inhibitor of Tyrosinase: In Vitro and In Silico Approaches

Abstract

This research work focuses on the potential application of an organic compound, santalol, obtained from santalum album, in the inhibition of the enzyme tyrosinase, which is actively involved in the biosynthesis of melanin pigment. Over-production of melanin causes undesirable pigmentation in humans as well as other organisms and significantly downgrades their aesthetic value. The study is designed to explain the purification of tyrosinase from the mushroom Agaricus bisporus, followed by activity assays and enzyme kinetics to give insight into the santalol-modulated tyrosinase inhibition in a dose-dependent manner. The multi-spectroscopic techniques such as UV-vis, fluorescence, and isothermal calorimetry are employed to deduce the efficiency of santalol as a potential candidate against tyrosinase enzyme activity. Experimental results are further verified by molecular docking. Santalol, derived from the essential oils of santalum album, has been widely used as a remedy for skin disorders and a potion for a fair complexion since ancient times. Based on enzyme kinetics and biophysical characterization, this is the first scientific evidence where santalol inhibits tyrosinase, and santalol may be employed in the agriculture, food, and cosmetic industries to prevent excess melanin formation or browning.

Molecular understanding of the therapeutic potential of melanin inhibiting natural products

“…As a result, the pathway of melanin synthesis is blocked, leading to a decrease in melanin synthesis. 23…”

“…As a result, the pathway of melanin synthesis is blocked, leading to a decrease in melanin synthesis. 23 Zerumbone (ZER) (10), a potent inhibitor of melanin, was found in Zingiber officinale Roscoe. It was observed to inhibit melanogenesis in both α-MSH and SCF-stimulated B16F10 mouse melanoma cells and G361 human melanoma cells.…”

“…PLS may inhibit melanin production by suppressing the IBMX-activated cAMP-PKA signaling pathway, resulting in down-regulation of the expression of tyrosinase genes and MITF. PLS also contained puerarin (22) and daidzin (23), which significantly inhibited mushroom tyrosinase activity (with IC 50 values of 478.5 μM and 17.50 μM, respectively). Molecular docking studies have revealed that puerarin (22) and daidzin (23) exhibit high binding affinity to human tyrosinase.…”

“…PLS also contained puerarin (22) and daidzin (23), which significantly inhibited mushroom tyrosinase activity (with IC 50 values of 478.5 μM and 17.50 μM, respectively). Molecular docking studies have revealed that puerarin (22) and daidzin (23) exhibit high binding affinity to human tyrosinase. 34,35 Li-Ying Team conducted a study on the melanininhibiting properties of tectorigenin from Puerariae flos, which refers to the flower of Pueraria montana var.…”