Inhibitors of Melanogenesis: An Updated Review

Pillaiyar, Thanigaimalai; Namasivayam, Vigneshwaran; Manickam, Manoj; Jung, Sang‐Hun

doi:10.1021/acs.jmedchem.7b00967

Cited by 238 publications

(184 citation statements)

References 209 publications

Supporting

Mentioning

181

Contrasting

Unclassified

Order By: Relevance

“…The quest for skin lighteners and agents capable of controlling hyperpigmentation disorders is growing at a sustained pace particularly in Asian countries. Most of the strategies explored so far focus on the control of the activity of tyrosinase, which is the main, rate-limiting enzyme involved in the biosynthesis of melanins, the pigments responsible for skin pigmentation in mammals [1][2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

2019

View full text Add to dashboard Cite

One of the most common approaches for control of skin pigmentation involves the inhibition of tyrosinase, a copper-containing enzyme which catalyzes the key steps of melanogenesis. This review focuses on the tyrosinase inhibition properties of a series of natural and synthetic, bioinspired phenolic compounds that have appeared in the literature in the last five years. Both mushroom and human tyrosinase inhibitors have been considered. Among the first class, flavonoids, in particular chalcones, occupy a prominent role as natural inhibitors, followed by hydroxystilbenes (mainly resveratrol derivatives). A series of more complex phenolic compounds from a variety of sources, first of all belonging to the Moraceae family, have also been described as potent tyrosinase inhibitors. As to the synthetic compounds, hydroxycinnamic acids and chalcones again appear as the most exploited scaffolds. Several inhibition mechanisms have been reported for the described inhibitors, pointing to copper chelating and/or hydrophobic moieties as key structural requirements to achieve good inhibition properties. Emerging trends in the search for novel skin depigmenting agents, including the development of assays that could distinguish between inhibitors and potentially toxic substrates of the enzyme as well as of formulations aimed at improving the bioavailability and hence the effectiveness of well-known inhibitors, have also been addressed.

show abstract

Section: Introductionmentioning

confidence: 99%

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

2019

View full text Add to dashboard Cite

show abstract

“…In such a way endophytic fungi Aspergillus flavus influence prominent role in finding novel bioactive metabolites and they require very small quantity of substance from plants. In some tropical areas, maximum exposure of skin to sunlight can result in an elevated risk that leads to skin cancer, oxidative stress, and sunburn 21 . To prevent the hazardous cause of ultraviolet rays, kojic acid isolated from fungi has been used in many cosmetic creams, lotions, and soaps because they prevent hyperpigmentation and tyrosinase inactivity, it is also used to avoid food browning 22 .…”

Section: Introductionmentioning

confidence: 99%

An In vitro Approach for Evaluating Antimicrobial Activity and Production of Kojic Acid by Aspergillus flavus Isolated from Karwar Region

Sanjotha¹,

Shivasharana²,

Manawadi³

2019

J Pure Appl Microbiol

View full text Add to dashboard Cite

“…It inhibited tyrosinase activity with a K i value of 52 µM. In addition to that, two other thiopurine drugs such as mercaptopurine (17) and azathioprine (18) were discovered as tyrosinase inhibitors, and among them, drug 17 showed stronger K i value (K i 52 µM) than the drug 16. Azathioprine (18) exhibited a poor tyrosinase inhibition.…”

Section: Introductionmentioning

confidence: 99%

“…Melanogenesis, a process of synthesis of melanin, is a complex enzymatic and biochemical catalyzed reactions, in which tyrosinase plays a rate-limiting step: hydroxylation of L-tyrosine to L-3,4-dihydroxyphenylalanine (L-DOPA) followed by the oxidation of L-DOPA to Ldopaquinone, which serves as a substrate for the production of melanin [18]. Therefore, targeting tyrosinase has been recognized as a potential approach for controlling the abnormal production of melanin.…”

Section: Introductionmentioning

confidence: 99%

A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery

Pillaiyar

Meenakshisundaram²,

Manickam

et al. 2020

European Journal of Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

Drug repurposing is a strategy consisting of finding new indications for already known marketed drugs used in various clinical settings or highly characterized compounds despite they can be failed drugs. Recently, it emerges as an alternative approach for the rapid identification and development of new pharmaceuticals for various rare and complex diseases for which lack the effective drug treatments. The success rate of drugs repurposing approach accounts for approximately 30% of new FDA approved drugs and vaccines in recent years.This review focuses on the status of drugs repurposing approach for various diseases including skin diseases, infective, inflammatory, cancer, and neurodegenerative diseases.Efforts have been made to provide structural features and mode of actions of drugs.Keywords: Cancer, drug repositioning, drug reprofiling, recycling of drugs, drug discovery, inflammation, neurodegenerative diseases, skin diseases. since clinical and pre-clinical studies of the re-purposed candidates are already being documented in the original indication(s). Thus, it reduces the time and cost needed to reach the market and risk intrinsic to any research and development program. Moreover, the risk of clinical failure is also low. As an added advantage, this approach gives a possibility to widen the market and to prolong the application of the patent life of a drug. There are mainly two ways to proceed drug-repositioning approach such as experimental strategies and computational strategies.Experimental repurposing strategies include binding assays and phenotypic screening methods, which can be to find binding interactions of drug molecules to assay components and to identify lead compounds from a vide range of compound libraries, respectively [10].Computational approaches are categorized into target-/mechanism based, knowledge-based, pathway-and network-based approaches. These approaches are proven economic in discovering novel therapeutic ligands. Most notably, computational methods augment the drug discovery process by effectively utilizing cheminformatics, bioinformatics, network biology and systems biology. More specifically, these methods exploit known targets, drugs, disease biomarkers or pathways to establish novel methods and accelerate the planning of crucial clinical trials [11].In this perspective, we focused on the status of drugs repurposing approaches for various diseases including skin diseases, infective, inflammatory, cancer, and neurodegenerative diseases. Efforts have been made to provide structural features, and modes of action of drugs, which are exclusively small molecules, peptidomimetics, and macrocyclic compounds.Antibodies, vaccines, and any other biological drugs are not discussed. Drugs repositioning for skin whitening activity.Melanin is a collection of natural pigments that primarily determine the skin, hair and hair color of the human. Melanocytes, which are found in the basal layer of the epidermis, produce melanin by the process called melanogenesis upon the skin exposure to the ultra...

show abstract

Inhibitors of Melanogenesis: An Updated Review

Cited by 238 publications

References 209 publications

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

An In vitro Approach for Evaluating Antimicrobial Activity and Production of Kojic Acid by Aspergillus flavus Isolated from Karwar Region

A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery

Contact Info

Product

Resources

About