Targeting tyrosinase in hyperpigmentation: Current status, limitations and future promises

Zolghadri, Samaneh; Beygi, M H Miran; Mohammad, Tasneem F.; Alijanianzadeh, Mahdi; Pillaiyar, Thanigaimalai; García-Molina, Pablo; Garcı́a-Cánovas, Francisco; Muñoz‐Muñoz, José Luis; Saboury, Ali Akbar

doi:10.1016/j.bcp.2023.115574

Cited by 30 publications

(12 citation statements)

References 199 publications

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“…Indeed, the communication between melanocytes as pigmentary cells and other adjacent types of aged skin cells such as senescent fibroblasts contribute to the aged-skin-associated pigmentation. Our results show that the presence of F. lutea essential oils decreases melanin, probably due to the inhibitory effect on tyrosinase, a key player in melanin production [39]. Our study is the first addressing the depigmenting properties of extracts obtained from plants from the genus Ferulago.…”

Section: Discussionmentioning

confidence: 68%

Effect of Ferulago lutea (Poir.) Grande Essential Oil on Molecular Hallmarks of Skin Aging

Alves-Silva,

Moreira,

Cavaleiro

et al. 2023

Plants

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With the increase in global life expectancy, maintaining health into old age becomes a challenge, and research has thus concentrated on various strategies which aimed to mitigate the effects of skin aging. Aromatic plants stand out as promising sources of anti-aging compounds due to their secondary metabolites, particularly essential oils (EOs). The aim of this study was to ascribe to Ferulago lutea EO several biological activities that could be useful in the context of skin aging. The EO was obtained using hydrodistillation and characterized by gas chromatography–mass spectrometry (GC/MS). The anti-inflammatory potential was assessed using lipopolysaccharide (LPS)-stimulated macrophages. The effect on cell migration was disclosed using scratch wound assay. Lipogenesis was induced using T0901317, hyperpigmentation with 3-isobutyl-1-methylxantine (IBMX) and senescence with etoposide. Our results show that the EO was characterized mainly by α-pinene and limonene. The EO was able to decrease nitric oxide (NO) release as well as iNOS and pro-IL-1β protein levels. The EO promoted wound healing while decreasing lipogenesis and having depigmenting effects. The EO also reduced senescence-associated β-galactosidase, p21/p53 protein levels and the nuclear accumulation of γH2AX. Overall, our study highlights the properties of F. lutea EO that make it a compelling candidate for dermocosmetics applications.

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Section: Discussionmentioning

confidence: 68%

Effect of Ferulago lutea (Poir.) Grande Essential Oil on Molecular Hallmarks of Skin Aging

Alves-Silva,

Moreira,

Cavaleiro

et al. 2023

Plants

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“…29 Inhibiting TYR has been widely recognized as an effective approach for reducing pigmentation and achieving skin whitening. 30 In clinical practice, commonly utilized TYR inhibitors, including hydroquinone, kojic acid, arbutin, azelaic acid, and L-ascorbic acid, possess certain inhibitory activity and whitening effects. However, they are characterized by inherent drawbacks such as high water solubility, poor penetration, and inadequate stability, which can potentially result in adverse reactions like skin irritation, allergies, and toxicity.…”

Section: ■ Introductionmentioning

confidence: 99%

“…TYR exhibits dual catalytic activities known as the monophenolase and diphenolase catalytic cycles, with the key distinction between them being the presence of bridging water or hydroxyl molecules between the copper centers (Figure A). , As the subsequent steps in melanin synthesis after dopaquinone are mainly non-enzymatic, TYR plays a pivotal role as the rate-limiting enzyme . Inhibiting TYR has been widely recognized as an effective approach for reducing pigmentation and achieving skin whitening …”

Section: Introductionmentioning

confidence: 99%

Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound

Cai,

Chen,

Jiang

et al. 2024

J. Med. Chem.

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Artificial intelligence (AI) de novo molecular generation is a highly promising strategy in the drug discovery, with deep reinforcement learning (RL) models emerging as powerful tools. This study introduces a fragment-by-fragment growth RL forward molecular generation and optimization strategy based on a low activity lead compound. This process integrates fragment growth-based reaction templates, while target docking and drug-likeness prediction were simultaneously performed. This comprehensive approach considers molecular similarity, internal diversity, synthesizability, and effectiveness, thereby enhancing the quality and efficiency of molecular generation. Finally, a series of tyrosinase inhibitors were generated and synthesized. Most compounds exhibited more improved activity than lead, with an optimal candidate compound surpassing the effects of kojic acid and demonstrating significant antipigmentation activity in a zebrafish model. Furthermore, metabolic stability studies indicated susceptibility to hepatic metabolism. The proposed AI structural optimization strategies will play a promising role in accelerating the drug discovery and improving traditional efficiency.

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“…However, the use of existing whitening functional materials, including hydroquinone, kojic acid, and arbutin, are associated with a number of safety and economic limitations; therefore, research on new whitening materials is necessary. To date, various attempts have been made to inhibit melanogenesis, such as the inhibition of tyrosinase activity, degradation of melanocytes, and reduction and decomposition of melanin, and research on natural products with lower toxicities and fewer side effects is being actively conducted [ 10 - 15 ].…”

Section: Introductionmentioning

confidence: 99%

Melanin Inhibitory Effect of Tuber himalayense Isolated in Incheon, Korea

Choi,

Kim,

Hong

et al. 2024

J. Microbiol. Biotechnol.

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There has been a growing interest in skin beauty and antimelanogenic products. Melanogenesis is the process of melanin synthesis whereby melanocytes are activated by UV light or hormone stimulation to produce melanin. Melanogenesis is mediated by several enzymes, such as tyrosinase (TYR), microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1 (TRP-1), and TRP-2. In this study, we investigated the effect of Tuber himalayense extract on melanin synthesis in α-melanocyte-stimulating hormone (α-MSH)-treated B16F10 melanoma cells. We confirmed that T. himalayense extract was not toxic to α-MSH-treated B16F10 melanoma cells and exhibited a significant inhibitory effect on melanin synthesis at concentrations of 25, 50, and 100 μg/ml. Additionally, the T. himalayense extract inhibited melanin, TRP-1, TRP-2, tyrosinase, and MITF, which are enzymes involved in melanin synthesis, in a concentration-dependent manner. Furthermore, T. himalayense extract inhibited the mitogen-activated protein kinase (MAPK) pathways, such as extracellular signal-regulated kinase-1/2 (ERK), c-Jun N-terminal kinase (JNK), and p38. Therefore, we hypothesized that various components of T. himalayense extract affect multiple factors involved in melanogenesis in B16F10 cells. Our results indicate that T. himalayense extract could potentially be used as a new material for preparing whitening cosmetics.

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Targeting tyrosinase in hyperpigmentation: Current status, limitations and future promises

Cited by 30 publications

References 199 publications

Effect of Ferulago lutea (Poir.) Grande Essential Oil on Molecular Hallmarks of Skin Aging

Effect of Ferulago lutea (Poir.) Grande Essential Oil on Molecular Hallmarks of Skin Aging

Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound

Melanin Inhibitory Effect of Tuber himalayense Isolated in Incheon, Korea

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