Functionality study of santalin as tyrosinase inhibitor: A potential depigmentation agent

Hemachandran, Hridya; Anantharaman, Amrita; Mohan, Sankari; Gopalakrishnan, Mohan; D, Thirumal Kumar; Doss, George Priya; Siva, Ramamoorthy

doi:10.1016/j.ijbiomac.2016.01.098

Cited by 51 publications

(28 citation statements)

References 37 publications

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“…At transcriptional level, our findings showed that both FLA and FLB significantly suppressed the melanogenic master regulator of Mitf gene expression which in turn suggesting the down-regulation of other melanogenic-related genes including Tyr, Trp-1 and Trp-2 [55]. The successful suppression of Mitf determines the effectiveness of FLA and FLB as potent depigmenting agents since Mitf is essential in melanin-bearing pigment cells across species and tissue types [55,56]. The outcome has suggested the implication of FLA and FLB in mechanistic inhibition on cAMP/α-MSH mechanism pathway.…”

Section: Discussionmentioning

confidence: 76%

Melanogenic Inhibition and Toxicity Assessment of Flavokawain A and B on B16/F10 Melanoma Cells and Zebrafish (Danio rerio)

et al. 2020

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Excessive production of melanin implicates hyperpigmentation disorders. Flavokawain A (FLA) and flavokawain B (FLB) have been reported with anti-melanogenic activity, but their melanogenic inhibition and toxicity effects on the vertebrate model of zebrafish are still unknown. In the present study, cytotoxic as well as melanogenic effects of FLA and FLB on cellular melanin content and tyrosinase activity were evaluated in α-MSH-induced B16/F10 cells. Master regulator of microphthalmia-associated transcription factor (Mitf) and the other downstream melanogenic-related genes were verified via quantitative real time PCR (qPCR). Toxicity assessment and melanogenesis inhibition on zebrafish model was further observed. FLA and FLB significantly reduced the specific cellular melanin content by 4.3-fold and 9.6-fold decrement, respectively in α-MSH-induced B16/F10 cells. Concomitantly, FLA significantly reduced the specific cellular tyrosinase activity by 7-fold whilst FLB by 9-fold. The decrement of melanin production and tyrosinase activity were correlated with the mRNA suppression of Mitf which in turn down-regulate Tyr, Trp-1 and Trp-2. FLA and FLB exhibited non-toxic effects on the zebrafish model at 25 and 6.25 µM, respectively. Further experiments on the zebrafish model demonstrated successful phenotype-based depigmenting activity of FLA and FLB under induced melanogenesis. To sum up, our findings provide an important first key step for both of the chalcone derivatives to be further studied and developed as potent depigmenting agents.

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Section: Discussionmentioning

confidence: 76%

Melanogenic Inhibition and Toxicity Assessment of Flavokawain A and B on B16/F10 Melanoma Cells and Zebrafish (Danio rerio)

et al. 2020

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“…Kinetic analysis revealed that these components inhibit tyrosinase via competitive inhibition [56]. Similarly, studies of Hridya et al [57] and Hridya et al [58] demonstrated that brazilein isolated from Caesalpinia sappan and santalin isolated from Pterocarpus santalinus have been found to reversibly inhibit tyrosinase in a mixed-type manner. Both the compounds inhibited tyrosinase activity dose dependently.…”

Section: Inhibition Of Tyrosinase Activitymentioning

confidence: 90%

On the Intricacies of Facial Hyperpigmentation and the Use of Herbal Ingredients as a Boon for Its Treatment: Cosmeceutical Significance, Current Challenges and Future Perspectives

Parveen¹,

Ali²,

Ali³

2019

Depigmentation

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Facial hyperpigmentation is the term used to express areas on irregular pigmentation in the skin. It appears as darkened patches on the face that make the facial skin look uneven. Facial hyperpigmentation is not physically debilitating but has been associated with enhanced psychosocial complications including anger, depression and frustration. These psychosocial burdens, in turn, have inference on quality of life and self-esteem. So, the treatment of facial hyperpigmentation seems to be a growing concern to the dermatologists today and they have been practising several treatment modalities including chemical peeling, laser therapy, dermabrasion, etc. But, those are found to be associated with various after-effects. Hence, the use of plants and its products is highly recommended as they are reported with either none or fewer after-effects. The present chapter draws attention to the forms of facial hyperpigmentation with their aetiologies and available treatment options for them with associated side effects. Furthermore, we have discussed about the other side of treatment with herbal ingredients which are safe and have less or no side effects. This chapter will be of value to the dermatologists who are searching for naturally derived ingredients for treating facial hyperpigmentation, in line with consumer expectations and preferences.

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“…Consequently, tyrosinase plays a pivotal role in melanin formation, which is an important component responsible for skin pigmentation in humans. Although melanin produced in skin melanocytes provides protection from UV radiation, excessive accumulation of melanin may cause cosmetic flaws such as age spots, freckles, senile lentigines, solar lentigo, and melasma in humans (Germanò et al, 2012;Hridya et al, 2016;Soares et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

Inhibition of Tyrosinase by Mercury Chloride: Spectroscopic and Docking Studies

Chen

Ran

et al. 2020

Front. Pharmacol.

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Inorganic mercury compounds have been used in skin-lightening products since ancient times. Although a previous study demonstrated that mercury impeded the transfer of Cu 2+ to the apotyrosinase, the effect of mercury on tyrosinase is still unclear. In the present study, the mechanism of mercury chloride (HgCl 2) induced inactivation of tyrosinase was investigated for the first time. The IC 50 values were 29.97 and 77.93 mmol/L for monophenolase and diphenolase, respectively. A kinetic analysis revealed that HgCl 2 inhibited tyrosinase activity in an irreversible non-competitive manner. The strong intrinsic fluorescence quenching suggested that the formation of the HgCl 2-tyrosinase complex induced conformational changes of the enzyme, and HgCl 2 had only one single binding site or a single class of binding site on tyrosinase. The molecular docking and further experiments demonstrated that HgCl 2 bound to the amino residuals (His) in the catalytic center of tyrosinase. To our knowledge, these findings presented in this paper were the first evidence of the direct interactions between HgCl 2 and tyrosinase, which provided a deep understanding of the inhibition mechanism of mercury on tyrosinase.

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Functionality study of santalin as tyrosinase inhibitor: A potential depigmentation agent

Cited by 51 publications

References 37 publications

Melanogenic Inhibition and Toxicity Assessment of Flavokawain A and B on B16/F10 Melanoma Cells and Zebrafish (Danio rerio)

Melanogenic Inhibition and Toxicity Assessment of Flavokawain A and B on B16/F10 Melanoma Cells and Zebrafish (Danio rerio)

On the Intricacies of Facial Hyperpigmentation and the Use of Herbal Ingredients as a Boon for Its Treatment: Cosmeceutical Significance, Current Challenges and Future Perspectives

Inhibition of Tyrosinase by Mercury Chloride: Spectroscopic and Docking Studies

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