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1.
Mini Rev Med Chem ; 19(10): 796-808, 2019.
Article in English | MEDLINE | ID: mdl-31244414

ABSTRACT

Cutaneous pigmentation plays critical role in determining the color of skin along with photo protection of skin from dreadful effects of ultraviolet radiations. Conversely, abnormal accumulation of melanin is responsible for hyper pigmentary disorders such as melasma, senile lentigines and freckles. Because of the visible nature of dermatologic diseases, they have a considerable psychosomatic effect on affected patients. Tyrosinase inhibitors are molecules that interrelate in some way with the enzyme to prevent it from working in the normal manner. Past many decades witnessed the quest for the development of natural tyrosinase inhibitors due to imperative role played by tyrosinase in the process of melanogenesis and fungi or fruit enzymatic browning. Mechanism of pigmentation is characterized by the intact process of the synthesis of specialized black pigment within melanosomes. Melanin is synthesized by a cascade of enzymatic and chemical reactions. For this reason, melanin production is mainly controlled by the expression and activation of tyrosinase. In the current article, we discussed tyrosinase inhibitors from the natural sources, which can be an essential constituent of cosmetics products and depigmenting agents for the treatment of hyperpigmentory disorders.


Subject(s)
Biological Products/pharmacology , Enzyme Inhibitors/pharmacology , Hyperpigmentation/drug therapy , Melanins/biosynthesis , Monophenol Monooxygenase/antagonists & inhibitors , Phytotherapy , Skin Lightening Preparations/pharmacology , Skin Pigmentation/drug effects , Animals , Biological Products/chemical synthesis , Biological Products/chemistry , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Humans , Molecular Structure , Monophenol Monooxygenase/metabolism , Skin Lightening Preparations/chemical synthesis , Skin Lightening Preparations/chemistry
2.
Int J Health Sci (Qassim) ; 12(1): 69-76, 2018.
Article in English | MEDLINE | ID: mdl-29623021

ABSTRACT

Skin color in animals is richer than human beings and is determined by different types of pigments. Melanin is the key pigment responsible for the diverse pigmentation found in animal and human skin, hair, and eyes. Melanin pigment is synthesized by melanocytes and is consecutively transferred to adjacent keratinocytes; here, it acts as an internal sunscreen to defend from ultraviolet (UV) damage. Any defect in the process of melanocytes development and/or melanin synthesis results in esthetic problem of abnormal pigmentation. Clinically, abnormal pigmentation displays distinct increased or reduced pigment levels, known as hyperpigmentation or hypopigmentation. These defects affect either the melanocyte number or its function. Herein, we discuss the fundamental aspects of melanocytes/melanin biology taken together the underlying cause of pigmentary disorders. The current chapter also gives an insight into the melanocyte stem cells biology, which in turn can facilitate the development of novel treatment regimens for dermatological disorders.

3.
Mini Rev Med Chem ; 17(9): 785-798, 2017.
Article in English | MEDLINE | ID: mdl-28019642

ABSTRACT

BACKGROUND: Skin pigmentation is a broadly appearing phenomenon in nature which plays an important task of determining the appearance and biology of all vertebrates including human beings. Skin color is a crucial attribute, determined by the synthesis of melanin pigment within melanocytes by the process of melanogenesis and is regulated by many extrinsic as well as intrinsic factors. Tyrosinase catalyzes the key step of melanogenesis, dysfunction of tyrosinase leads to reduce melanin production which results in severe clinical and aesthetical problems of hypopigmentation. Therefore, the regulation of melanin production is an important strategy in the treatment of abnormal skin pigmentation for cosmetic and medicinal purpose. METHOD: The present review covers the various aspects of mammalian melanocyte biology which will help in the identification of key regulators of melanogenesis from pharmaceutical and pharmacological point of view. Further sections of the review focus on the dysfunctions of melanogenic pathways, which result in severe clinical and aesthetical problems of hypopigmentation. CONCLUSION: We have also attempted to highlight the ability of available scientifically validated plant extracts to naturally enhance melanin synthesis in order to cure hypopigmentation.


Subject(s)
Hypopigmentation/drug therapy , Melanins/pharmacology , Melanocytes/drug effects , Skin Diseases/drug therapy , Animals , Dose-Response Relationship, Drug , Humans , Hypopigmentation/pathology , Melanins/biosynthesis , Melanins/chemistry , Molecular Structure , Skin Diseases/pathology , Structure-Activity Relationship
4.
J Microsc Ultrastruct ; 3(4): 210-219, 2015.
Article in English | MEDLINE | ID: mdl-30023201

ABSTRACT

Berberine is an active compound of Berberis vulgaris (Daruhaldi) with known multiple pharmacological activities, including antimicrobial, antiviral, anti-inflammatory, cholesterol-lowering, and anticancer effects. The present work aimed to study the ultrastructural effects of berberine to determine its skin-darkening potential using Bufo melanostictus melanophores, which has not been done to date. Light and electron microscopic analysis of isolated dorsal skin melanophores of B. melanostictus has been done after treatment with various concentrations of berberine, along with specific antagonists and agonists of ß-adrenoceptors in order to explore the mechanism of action of berberine-induced skin darkening. The results showed that the number of melanophores with melanin-loaded dendrites increased in the subepidermal layer significantly in berberine-treated skin pieces in a dose-dependent manner leading to skin darkening. Highly electron-dense melanosomes of Stage IV increased considerably due to the enhanced process of melanization. These effects were found to be antagonized by propranolol, and were also found to be highly potentiated by isoprenaline, which is a specific ß-adrenoceptor agonist. The findings show that berberine possesses a skin-darkening potential and could be used as a safe melanogenic agent for the treatment of hypopigmentation disorders or vitiligo.

5.
Biochem Res Int ; 2014: 854687, 2014.
Article in English | MEDLINE | ID: mdl-24895537

ABSTRACT

Tyrosinase is a natural enzyme and is often purified to only a low degree and it is involved in a variety of functions which mainly catalyse the o-hydroxylation of monophenols into their corresponding o-diphenols and the oxidation of o-diphenols to o-quinones using molecular oxygen, which then polymerizes to form brown or black pigments. The synthesis of o-diphenols is a potentially valuable catalytic ability and thus tyrosinase has attracted a lot of attention with respect to industrial applications. In environmental technology it is used for the detoxification of phenol-containing wastewaters and contaminated soils, as biosensors for phenol monitoring, and for the production of L-DOPA in pharmaceutical industries, and is also used in cosmetic and food industries as important catalytic enzyme. Melanin pigment synthesized by tyrosinase has found applications for protection against radiation cation exchangers, drug carriers, antioxidants, antiviral agents, or immunogen. The recombinant V. spinosum tryosinase protein can be used to produce tailor-made melanin and other polyphenolic materials using various phenols and catechols as starting materials. This review compiles the recent data on biochemical and molecular properties of microbial tyrosinases, underlining their importance in the industrial use of these enzymes. After that, their most promising applications in pharmaceutical, food processing, and environmental fields are presented.

6.
J Recept Signal Transduct Res ; 34(1): 15-20, 2014 Feb.
Article in English | MEDLINE | ID: mdl-24099619

ABSTRACT

Reduced production of melanin by decreased or the absence of melanocytes leads to various hypopigmentation disorders, and the development of melanogenetic agents for photoprotection and hypopigmentation disorders is one of the top priority areas of research. Hence, the present study was carried out to elucidate the ability of berberine, a principal active ingredient present in the roots of the herb Berberis vulgaris to stimulate pigment dispersion in the isolated skin melanophores of the toad Bufo melanostictus. In the present study, mean melanophore size index of the isolated skin melanophores of B. melanostictus was assayed after treating with various concentrations of berberine. A marked melanin dispersion response leading to skin darkening was observed in the isolated melanophores of toad in response to berberine, which was found to be mediated through beta-2 adrenergic receptors. The physiologically significant dose-related melanin dispersion effects of berberine per se were found to be completely abolished by propranolol, which is a specific beta-2 adrenergic receptor blocker. These per se melanin dispersal effects were also found to be markedly potentiated by isoprenaline, which is a specific beta-adrenoceptor agonist. The results indicate that berberine causes a tremendous, dose-dependent, physiologically significant pigment dispersing in the isolated skin melanophores of B. melanostictus.


Subject(s)
Berberine/administration & dosage , Melanins/biosynthesis , Receptors, Adrenergic, beta-2/biosynthesis , Vasodilation/genetics , Animals , Atropine/administration & dosage , Bufonidae , Melanophores/drug effects , Melanophores/metabolism , Phosphoric Diester Hydrolases/metabolism , Pigmentation Disorders , Receptors, Adrenergic, beta-2/metabolism , Scopolamine/administration & dosage
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