Natural Tyrosinase Inhibitors: Role of Herbals in the Treatment of Hyperpigmentary Disorders

Zaidi, Kamal Uddin; Ali, Sharique A.; Ali, Ayesha; Naaz, Ishrat

doi:10.2174/1389557519666190116101039

Cited by 29 publications

(26 citation statements)

References 69 publications

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“…Overall, the total alkaloids characterizing C. szovitsii roots were found to be highly (p < 0.01) correlated to ABTS (0.97), AChE inhibition (0.95), tyrosinase inhibition (0.96), and amylase inhibition (0.95) values. These findings were also supported by several researchers, who reported that alkaloids were the main players against cholinesterase [37,38] and tyrosinase [39,40]. Looking to polyphenols characterizing the root extracts, the most significant correlations (p < 0.01) were observed between anthocyanins and CUPRAC values (0.86), flavanols and tyrosinase inhibition (−0.99), flavones and CUPRAC values (0.85), phenolic acids and FRAP values (−0.87), tyrosols and tyrosinase inhibition (0.97), and stilbenes and DPPH values (0.93).…”

Section: Correlationssupporting

confidence: 80%

Chemical Profiling and Biological Properties of Extracts from Different Parts of Colchicum Szovitsii Subsp. Szovitsii

et al. 2019

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Like other members of the Colchicum genus, C. szovitsii subsp. szovitsii is also of medicinal importance in Turkish traditional medicine. However, its biological properties have not been fully investigated. Herein, we focused on the evaluation of the in vitro antioxidant and enzyme inhibitory effects of flower, root and leaf extracts, obtained using different extraction methods. In addition, a comprehensive (poly)-phenolic and alkaloid profiling of the different extracts was undertaken. In this regard, ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) allowed us to putatively annotate 195 polyphenols and 87 alkaloids. The most abundant polyphenols were flavonoids (83 compounds), whilst colchicine and 2-demethylcolchicine were some of the most widespread alkaloids in each extract analyzed. However, our findings showed that C. szovitsii leaf extracts were a superior source of both total polyphenols and total alkaloids (being, on average 24.00 and 2.50 mg/g, respectively). Overall, methanolic leaf extracts showed the highest (p < 0.05) ferric reducing antioxidant power (FRAP) reducing power (on average 109.52 mgTE/g) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging (on average 90.98 mgTE/g). Interestingly, each C. szovitsii methanolic extract was more active than the water extracts when considering enzymatic inhibition such as against tyrosinase, glucosidase, and acetylcholinesterase (AChE). Strong correlations (p < 0.01) were also observed between polyphenols/alkaloids and the biological activities determined. Multivariate statistics based on supervised orthogonal projections to latent structures discriminant analysis (OPLS-DA) allowed for the detection of those compounds most affected by the different extraction methods. Therefore, this is the first detailed evidence showing that C. szovitsii subsp. szovitsii might provide beneficial effects against oxidative stress and the associated chronic diseases. Nevertheless, the detailed mechanisms of action need to be further investigated.

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Section: Correlationssupporting

confidence: 80%

Chemical Profiling and Biological Properties of Extracts from Different Parts of Colchicum Szovitsii Subsp. Szovitsii

et al. 2019

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“…The first rate‐limiting step of melanogenesis is the oxidation of tyrosine to dopaquinone by tyrosinase [6,7]. Therefore, tyrosinase inhibitors are in the focus of the research for the treatment of hyperpigmentation [7‐10]. Acting immediately and reversibly, they are considered safer than, for example hydroquinone [11] which is not allowed in the EU for cosmetic use [12].…”

Section: Introductionmentioning

confidence: 99%

Thiamidol containing treatment regimens in facial hyperpigmentation: An international multi‐centre approach consisting of a double‐blind, controlled, split‐face study and of an open‐label, real‐world study

Philipp‐Dormston

Echagüe²,

Damonte³

et al. 2020

Intern J of Cosmetic Sci

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OBJECTIVE: Tyrosinase is the rate-limiting enzyme in melanogenesis. Thiamidol is the most potent inhibitor of human tyrosinase out of 50 000 tested compounds. In clinical studies, it was shown to improve facial hyperpigmentation, post-inflammatory hyperpigmentation and age spots significantly. To identify the optimal number of daily Thiamidol applications, we conducted a split-face study comparing the efficacy and tolerability of four-times with two-times daily application. Subsequently, we evaluated the efficacy and tolerability of a typical face care regimen containing Thiamidol in a real-world study. METHODS: The split-face study was double-blind, randomized, controlled, including two Thiamidol containing products (serum and day care SPF 30). The serum was applied twice daily on one half of the face and the day care SPF30 twice-daily on the whole face. The real-world study was open-label, observational, including three Thiamidol containing products (day care SPF 30 in the morning, serum and night care in the evening). In both studies, subjects with mild-to-moderate facial hyperpigmentation applied the products over 12 weeks. Assessments included clinical and subjective grading of hyperpigmentation, skin condition, hemi-/modified MASI, chromameter and clinical photography. RESULTS: In the split-face study (n = 34), hyperpigmentation, skin roughness and hMASI improved all significantly (P < 0.001) versus baseline, with first visible results after two weeks of twice-daily application. The four-times daily application led to significant improvement versus the two-times daily application. In the real-world study (n = 83), all evaluated parameters, including skin condition and chromametry (n = 30), improved significantly (P < 0.001) in comparison with baseline and the corresponding preceding visits. The subjects judged the cosmetic properties of the products positively. In both studies, the products were well tolerated. CONCLUSION: Four-times daily Thiamidol improves facial hyperpigmentation significantly more than two-times daily and is well tolerated by the subjects. The real-world study with a typical face care regimen containing Thiamidol shows improvement of facial hyperpigmentation and confirms tolerability. Furthermore, the data provide evidence for the suitability of this three-product Thiamidol regimen for day-today life.

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“…It is reported that approximately 15% of the world’s population invests in skin-whitening cosmetics, and global industry analysis forecasts predict that the global market for skin-whitening agents will reach $23 billion by 2020 [ 54 ]. Since tyrosinase catalyzes the rate-limiting step in melanogenesis, most of the pertinent research has focused on developing specific inhibitors against tyrosinase [ 55 , 56 ]. Indeed, most commercially available skin-lightening agents (e.g., arbutin, hydroquinone, kojic acid, and tranexamic acid) are tyrosinase inhibitors.…”

Section: Discussionmentioning

confidence: 99%

Jeju Magma-Seawater Inhibits α-MSH-Induced Melanogenesis via CaMKKβ-AMPK Signaling Pathways in B16F10 Melanoma Cells

Song

Lee²,

Kim

et al. 2020

Marine Drugs

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Melanin protects skin from ultraviolet radiation, toxic drugs, and chemicals. Its synthesis is sophisticatedly regulated by multiple mechanisms, including transcriptional and enzymatic controls. However, uncontrolled excessive production of melanin can cause serious dermatological disorders, such as freckles, melasma, solar lentigo, and cancer. Moreover, melanogenesis disorders are also linked to neurodegenerative diseases. Therefore, there is a huge demand for safer and more potent inhibitors of melanogenesis. In the present study, we report novel inhibitory effects of Jeju magma-seawater (JMS) on melanogenesis induced by α-melanocyte stimulating hormone (α-MSH) in B16F10 melanoma cells. JMS is the abundant underground seawater found in Jeju Island, a volcanic island of Korea. Research into the physiological effects of JMS is rapidly increasing due to its high contents of various minerals that are essential to human health. However, little is known about the effects of JMS on melanogenesis. Here, we demonstrate that JMS safely and effectively inhibits α-MSH-induced melanogenesis via the CaMKKβ (calcium/calmodulin-dependent protein kinase β)-AMPK (5′ adenosine monophosphate-activated protein kinase) signaling pathway. We further demonstrate that AMPK inhibits the signaling pathways of protein kinase A and MAPKs (mitogen-activated protein kinase), which are critical for melanogenesis-related gene expression. Our results highlight the potential of JMS as a novel therapeutic agent for ameliorating skin pigmentation-related disorders.

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Natural Tyrosinase Inhibitors: Role of Herbals in the Treatment of Hyperpigmentary Disorders

Cited by 29 publications

References 69 publications

Chemical Profiling and Biological Properties of Extracts from Different Parts of Colchicum Szovitsii Subsp. Szovitsii

Chemical Profiling and Biological Properties of Extracts from Different Parts of Colchicum Szovitsii Subsp. Szovitsii

Thiamidol containing treatment regimens in facial hyperpigmentation: An international multi‐centre approach consisting of a double‐blind, controlled, split‐face study and of an open‐label, real‐world study

Jeju Magma-Seawater Inhibits α-MSH-Induced Melanogenesis via CaMKKβ-AMPK Signaling Pathways in B16F10 Melanoma Cells

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