scholarly journals Melatonin - A Cutaneous Perspective

2021 ◽  
Vol 19 (2) ◽  
pp. 3-12
Author(s):  
Tapan Dhali ◽  
Mona Sharma ◽  
Priyanka Hemrajani
Keyword(s):  
Biological Activities ◽  
Hair Follicles ◽  
Melatonin Receptors ◽  
Skin Cell ◽  
Specific Selectivity ◽  
Range Of Functions ◽  
Radiation Induced ◽  
Anti Inflammatory ◽  
Independent Effects ◽  
High Level

Melatonin (MLT) is an endogenous hormone secreted from the pineal gland, located deep in the brain in the epithalamus associated with numerous biological activities. The primary function of melatonin is to regulate sleep-wake cycles. However, research over the last few years has enlightened a range of functions associated with this molecule, including anti-inflammatory, direct and indirect antioxidant activity, regenerative tissue benefits, and preservation of mitochondrial function. Melatonin’s anti-inflammatory and antioxidant support, coupled with its mitochondrial modulation, makes it a vital molecule to use for skin health homeostasis. The cutaneous melatoninergic system’s widespread expression and pleiotropic activity provides for a high level of cell-specific selectivity. Several skin cells, including normal and malignant keratinocytes, melanocytes, fibroblasts and hair follicles, express melatonin receptors. Melatonin also has receptor-independent effects that protect against oxidative stress and can reduce ultraviolet radiation-induced damage. Several functions of melatonin in the skin have been experimentally implicated such as hair growth cycling, fur pigmentation, melanoma control, suppression of ultraviolet-induced damage to the skin cell. Melatonin may play a role in treating several dermatoses e.g., atopic eczema, psoriasis, melasma, ulcer healing, and malignant melanoma. There is a plethora of functional melatonin properties, which still await to be fully appreciated by dermatologists. The current review emphasizes few of the established uses and few emerging potentialities that render melatonin a promising candidate for managing several diseases.

scholarly journals Herbal Formulation for the Treatment of Acne Vulgaris

2019 ◽  
Vol 2 (4) ◽  
Keyword(s):  
Wheat Germ ◽  
Acne Vulgaris ◽  
Hair Follicles ◽  
Wheat Germ Oil ◽  
Skin Cell ◽  
Anti Oxidant ◽  
Inflammatory Skin Disorder ◽  
Anti Inflammatory ◽  
Anti Fungal

The main objective of the present article is to avoid the adverse effect of the existing synthetic acne cream by formulating an herbal acne cream for treatment of acne vulgaris. Acne vulgaris is a long term skin disease that occurs when hair follicles were blocked with dead skin cell and oil from the skin. Acne vulgaris is the most common bacteria causing chronic inflammatory skin disorder. Propioni bacterium and staphylococcus aureus are common pus forming microbes responsible for acne vulgaris. Various herbs used for the treatment of acne vulgaris such as wheat germ oil used as anti-oxidant and it is a great sources of vitamin-e, haldi helps to reduce the inflammation of acne and it act as anti-inflammatory agent, neem helps in clearing acne, scars and pigmentation, raspberry used as anti-oxidant and it is a source of vitamin c, kesar act as anti-inflammatory, anti-fungal and antioxidant. Natural herbal extracts in combination effectively utilized for the treatment of acne. Use of such products far better than the use of synthetic cream for the control of acne. Wheat germ oil which is extracted from kernel of wheat grains, haldi is extracted from rhizome; neem is extracted from leaf, raspberry (seed), kesar extracted from the stigmas of the flower part.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Comparative Analysis of In-Vitro Biological Activities of Methyl Eugenol Rich Cymbopogon khasianus Hack., Leaf Essential Oil with Pure Methyl Eugenol Compound

2020 ◽  
Vol 21 (10) ◽  
pp. 927-938 ◽  
Author(s):  
Roktim Gogoi ◽  
Rikraj Loying ◽  
Neelav Sarma ◽  
Twahira Begum ◽  
Sudin K. Pandey ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Biological Activities ◽  
Methyl Eugenol ◽  
Dpph Assay ◽  
Pure Compound ◽  
Allium Cepa Assay ◽  
Anti Inflammatory ◽  
Lemongrass Essential Oil

Background: The essential oil of methyl eugenol rich Cymbopogon khasianus Hack. was evaluated and its bioactivities were compared with pure methyl eugenol. So far, methyl eugenol rich essential oil of lemongrass was not studied for any biological activities; hence, the present study was conducted. Objective: This study examined the chemical composition of essential oil of methyl eugenol rich Cymbopogon khasianus Hack., and evaluated its antioxidant, anti-inflammatory, antimicrobial, and herbicidal properties and genotoxicity, which were compared with pure compound, methyl eugenol. Material and Methods: Methyl eugenol rich variety of Cymbopogon khasianus Hack., with registration no. INGR18037 (c.v. Jor Lab L-9) was collected from experimental farm CSIR-NEIST, Jorhat, Assam (26.7378°N, 94.1570°E). The essential oil wasobtained by hydro-distillation using a Clevenger apparatus. The chemical composition of the essential oil was evaluated using GC/MS analysis and its antioxidant (DPPH assay, reducing power assay), anti-inflammatory (Egg albumin denaturation assay), and antimicrobial (Disc diffusion assay, MIC) properties, seed germination effect and genotoxicity (Allium cepa assay) were studied and compared with pure Methyl Eugenol compound (ME). Results: Major components detected in the Essential Oil (EO) through Gas chromatography/mass spectroscopy analysis were methyl eugenol (73.17%) and β-myrcene (8.58%). A total of 35components were detected with a total identified area percentage of 98.34%. DPPH assay revealed considerable antioxidant activity of methyl eugenol rich lemongrass essential oil (IC50= 2.263 μg/mL), which is lower than standard ascorbic acid (IC50 2.58 μg/mL), and higher than standard Methyl Eugenol (ME) (IC50 2.253 μg/mL). Methyl eugenol rich lemongrass EO showed IC50 38.00 μg/mL, ME 36.44 μg/mL, and sodium diclofenac 22.76 μg/mL, in in-vitro anti-inflammatory test. Moderate antimicrobial activity towards the 8 tested microbes was shown by methyl eugenol rich lemongrass essential oil whose effectiveness against the microbes was less as compared to pure ME standard. Seed germination assay further revealed the herbicidal properties of methyl eugenol rich essential oil. Moreover, Allium cepa assay revealed moderate genotoxicity of the essential oil. Conclusion: This paper compared the antioxidant, anti-inflammatory, antimicrobial, genotoxicity and herbicidal activities of methyl eugenol rich lemongrass with pure methyl eugenol. This methyl eugenol rich lemongrass variety can be used as an alternative of methyl eugenol pure compound. Hence, the essential oil of this variety has the potential of developing cost-effective, easily available antioxidative/ antimicrobial drugs but its use should be under the safety range of methyl eugenol and needs further clinical trials.

Arylpyrazoles: Heterocyclic Scaffold of Immense Therapeutic Application

2020 ◽  
Vol 24 (14) ◽  
pp. 1555-1581
Author(s):  
Garima Tripathi ◽  
Anil Kumar Singh ◽  
Abhijeet Kumar
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Pyrazole Derivatives ◽  
Therapeutic Application ◽  
Diverse Range ◽  
Major Class ◽  
Anti Inflammatory

Among the major class of heterocycles, the N-heterocycles, such as pyrazoles, are scaffolds of vast medicinal values. Various drugs and other biologically active molecules are known to contain these N-heterocycles as core motifs. Specifically, arylpyrazoles have exhibited a diverse range of biological activities, including anti-inflammatory, anticancerous, antimicrobial and various others. For instance, arylpyrazoles are present as core moieties in various insecticides, fungicides and drugs such as Celebrex and Trocoxil. The present review will be highlighting the significant therapeutic importance of pyrazole derivatives developed in the last few years.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

Advances in Synthesis and Medicinal Applications of Compounds Derived from Phthalimide

2020 ◽  
Vol 17 (4) ◽  
pp. 252-270
Author(s):  
Marcel L. Almeida ◽  
Maria C.V.A. Oliveira ◽  
Ivan R. Pitta ◽  
Marina G.R. Pitta
Keyword(s):  
Chemical Synthesis ◽  
Biological Activities ◽  
Sedative Effects ◽  
Phthalimide Derivative ◽  
Anti Inflammatory

Phthalimide derivatives have been presenting several promising biological activities in the literature, such as anti-inflammatory, analgesic, antitumor, antimicrobial and anticonvulsant. The most well-known and studied phthalimide derivative (isoindoline-1,3-dione) is thalidomide: this compound initially presented important sedative effects, but it is now known that thalidomide has effectiveness against a wide variety of diseases, including inflammation and cancer. This review approaches some of the recent and efficient chemical synthesis pathways to obtain phthalimide analogues and also presents a summary of the main biological activities of these derivatives found in the literature. Therefore, this review describes the chemical and therapeutic aspects of phthalimide derivatives.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

Natural Sesquiterpene Lactones in the Prevention and Treatment of Inflammatory Disorders and cancer: A Systematic Study of this Emerging Therapeutic Approach based on Chemical and Pharmacological Aspect

2020 ◽  
Vol 17 (9) ◽  
pp. 1102-1116
Author(s):  
Sudip Kumar Mandal ◽  
Utsab Debnath ◽  
Amresh Kumar ◽  
Sabu Thomas ◽  
Subhash Chandra Mandal ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Structural Diversity ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Anti Cancer ◽  
Drug Discovery Program ◽  
Anti Inflammatory ◽  
Family Based

Background and Introduction: Sesquiterpene lactones are a class of secondary metabolite that contains sesquiterpenoids and lactone ring as pharmacophore moiety. A large group of bioactive secondary metabolites such as phytopharmaceuticals belong to this category. From the Asteraceae family-based medicinal plants, more than 5,000 sesquiterpene lactones have been reported so far. Sesquiterpene lactone-based pharmacophore moieties hold promise for broad-spectrum biological activities against cancer, inflammation, parasitic, bacterial, fungal, viral infection and other functional disorders. Moreover, these moiety based phytocompounds have been highlighted with a new dimension in the natural drug discovery program worldwide after the 2015 Medicine Nobel Prize achieved by the Artemisinin researchers. Objective: These bitter substances often contain an α, β-unsaturated-γ-lactone as a major structural backbone, which in recent studies has been explored to be associated with anti-tumor, cytotoxic, and anti-inflammatory action. Recently, the use of sesquiterpene lactones as phytomedicine has been increased. This study will review the prospect of sesquiterpene lactones against inflammation and cancer. Methods: Hence, we emphasized on the different features of this moiety by incorporating its structural diversity on biological activities to explore structure-activity relationships (SAR) against inflammation and cancer. Results: How the dual mode of action such as anti-inflammatory and anti-cancer has been exhibitedby these phytopharmaceuticals will be forecasted in this study. Furthermore, the correlation of anti-inflammatory and anti-cancer activity executed by the sesquiterpene lactones for fruitful phytotherapy will also be revealed in the present review in the milieu of pharmacophore activity relation and pharmacodynamics study as well. Conclusion: So, these metabolites are paramount in phytopharmacological aspects. The present discussion on the future prospect of this moiety based on the reported literature could be a guide for anti-inflammatory and anti-cancer drug discovery programs for the upcoming researchers.

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