scholarly journals In Silico Prediction of Tyrosinase and Adenylyl Cyclase Inhibitors from Natural Compounds

2014 ◽  
Vol 9 (2) ◽  
pp. 1934578X1400900
Author(s):  
Pedro Fong ◽  
Henry H. Y. Tong ◽  
Chi M. Chao
Keyword(s):  
Adenylyl Cyclase ◽  
Skin Irritation ◽  
Herbal Medicines ◽  
Skin Permeability ◽  
Pharmacophore Mapping ◽  
Topical Formulation ◽  
Melanin Production ◽  
Skin Whitening

Although many herbal medicines are effective in the treatment of hyperpigmentation, the potency of different constituents remains unknown. In this work, more than 20,000 herbal ingredients from 453 herbs were docked into the crystal structures of adenylyl cyclase and a human homology tyrosinase model using Surflex-Dock. These two enzymes are responsible for melanin production and inhibition of them may attain a skin-whitening effect superior to currently available agents. The essential drug properties for topical formulation of the herbal ingredients, including skin permeability, sensitization, irritation, corrosive and carcinogenic properties were predicted by Dermwin, Skin Sensitization Alerts (SSA), Skin Irritation Corrosion Rules Estimation Tool (SICRET) and Benigni/Bossa rulebase module of Toxtree. Moreover, similarity ensemble and pharmacophore mapping approaches were used to forecast other potential targets for these herbal compounds by the software, SEArch and PharmMapper. Overall, this study predicted seven compounds to have advanced drug-like properties over the well-known effective tyrosinase inhibitors, arbutin and kojic acid. These seven compounds have the highest potential for further in vitro and in vivo investigation with the aim of developing safe and high-efficacy skin-whitening agents.

scholarly journals Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers

2021 ◽  
Vol 14 (12) ◽  
pp. 1233
Author(s):  
Quoc Lam Vu ◽  
Chih-Wun Fang ◽  
Muhammad Suhail ◽  
Pao-Chu Wu
Keyword(s):  
Drug Delivery ◽  
Skin Irritation ◽  
Topical Administration ◽  
Skin Whitening ◽  
Drug Delivery Carrier ◽  
In Vitro Permeation ◽  
Topical Bioavailability ◽  
The Mean

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm2·h up to 20.00 μg/cm2·h and 4.90 up to 53.52 μg/cm2, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.

Traditional Herbal Medicines, Newer Herbs and Other Novel Approaches Integrated in Herbal Medicine for Atopic Dermatitis-A Narrative Review

2020 ◽  
Vol 15 (3) ◽  
pp. 194-208
Author(s):  
Pravin Kumar ◽  
Dinesh Kumar Sharma ◽  
Mahendra Singh Ashawat
Keyword(s):  
Atopic Dermatitis ◽  
Herbal Medicines ◽  
Developed Countries ◽  
Skin Lesions ◽  
Scientific Data ◽  
Herbal Drugs ◽  
Biological Drugs ◽  
Alternative Treatment Option

Atopic Dermatitis (AD) is a prolonged reverting skin ailment with characteristically distributed skin lesions. In the previous decades, researchers had shown a marked interest in AD due to its increased prevalence in developed countries. Although different strategies including biological and immune modulators are available for the treatment of AD, each has certain limitations. The researchers had shown considerable interest in the management of AD with herbal medicines. The establishment of herbal drugs for AD might eliminate local as well as systemic adverse effects associated with long term use of corticosteroids and also higher cost of therapy with biological drugs. The present review discusses the traditional East Asian herbal medicines and scientific data related to newer herbal extracts or compositions for the treatment of AD. In vivo animal models and in vitro cell cultures, investigated with herbal medicines to establish a possible role in AD treatment, have also been discussed in the paper. The paper also highlights the role of certain new approaches, i.e. pharmacopuncture, a combination of allopathic and herbal medicines; and novel carriers (liposomes, cubosomes) for herbal drugs on atopic skin. In conclusion, herbal medicines can be a better and safe, complementary and alternative treatment option for AD.

scholarly journals FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

2019 ◽  
pp. 156-163
Author(s):  
AMOL SHETE ◽  
PRIYANKA THORAT ◽  
RAJENDRA DOIJAD ◽  
SACHIN SAJANE
Keyword(s):  
Phase Separation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Separation Method ◽  
Gelling Agent ◽  
In Vivo Evaluation ◽  
Skin Delivery ◽  
Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

scholarly journals Non-invasive skin sampling of tryptophan/kynurenine ratio in vitro towards a skin cancer biomarker

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Skaidre Jankovskaja ◽  
Johan Engblom ◽  
Melinda Rezeli ◽  
György Marko-Varga ◽  
Tautgirdas Ruzgas ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Relative Increase ◽  
Cancer Biomarker ◽  
Cancer Diagnostics ◽  
Sampling Time ◽  
Skin Permeability ◽  
Experimental Conditions ◽  
Non Invasive

AbstractThe tryptophan to kynurenine ratio (Trp/Kyn) has been proposed as a cancer biomarker. Non-invasive topical sampling of Trp/Kyn can therefore serve as a promising concept for skin cancer diagnostics. By performing in vitro pig skin permeability studies, we conclude that non-invasive topical sampling of Trp and Kyn is feasible. We explore the influence of different experimental conditions, which are relevant for the clinical in vivo setting, such as pH variations, sampling time, and microbial degradation of Trp and Kyn. The permeabilities of Trp and Kyn are overall similar. However, the permeated Trp/Kyn ratio is generally higher than unity due to endogenous Trp, which should be taken into account to obtain a non-biased Trp/Kyn ratio accurately reflecting systemic concentrations. Additionally, prolonged sampling time is associated with bacterial Trp and Kyn degradation and should be considered in a clinical setting. Finally, the experimental results are supported by the four permeation pathways model, predicting that the hydrophilic Trp and Kyn molecules mainly permeate through lipid defects (i.e., the porous pathway). However, the hydrophobic indole ring of Trp is suggested to result in a small but noticeable relative increase of Trp diffusion via pathways across the SC lipid lamellae, while the shunt pathway is proposed to slightly favor permeation of Kyn relative to Trp.

scholarly journals The Genus Lagochilus (Lamiaceae): A Review of Its Diversity, Ethnobotany, Phytochemistry, and Pharmacology

Plants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 132
Author(s):  
Nilufar Z. Mamadalieva ◽  
Davlat Kh. Akramov ◽  
Ludger A. Wessjohann ◽  
Hidayat Hussain ◽  
Chunlin Long ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
Herbal Medicines ◽  
Future Research ◽  
South Central ◽  
Pharmacological Studies ◽  
Central South

The genus Lagochilus (Lamiaceae) is native to Central, South-Central, and Eastern Asia. It comprises 44 species, which have been commonly used as herbal medicines for the treatments of various ailments for thousands of years, especially in Asian countries. This review aims to summarize the chemical constituents and pharmacological activities of species from the genus Lagochilus to unveil opportunities for future research. In addition, we provide some information about their traditional uses, botany, and diversity. More than 150 secondary metabolites have been reported from Lagochilus, including diterpenes, flavonoids, phenolic compounds, triterpenoids, iridoid glycosides, lignans, steroids, alkaloids, polysaccharides, volatile, non-volatile and aromatic compounds, lipids, carbohydrates, minerals, vitamins, and other secondary metabolites. In vitro and in vivo pharmacological studies on the crude extracts, fractions, and isolated compounds from Lagochilus species showed hemostatic, antibacterial, anti-inflammatory, anti-allergic, cytotoxic, enzyme inhibitory, antispasmodic, hypotensive, sedative, psychoactive, and other activities.

Diagnostic and Experimental Methods Skin irritation: tests in vivo and in vitro

1990 ◽  
Vol 23 (4) ◽  
pp. 287-287
Author(s):  
D. P. Bruynzeel ◽  
B. A. M. Gerritsen ◽  
P. De Haan ◽  
E. M. De Boer
Keyword(s):  
Skin Irritation ◽  
Experimental Methods

scholarly journals Determination of in Vivo Biological Activities of Dodonaea Viscosa Flowers Against CCL4 Toxicity in Albino Mice With Bioactive Compound Detection

2021 ◽  
Author(s):  
Hina Gul ◽  
Muhammad Awais ◽  
Salina Saddick ◽  
Falak Sher Khan ◽  
Muhammad Gulfraz ◽  
...  
Keyword(s):  
Protective Effect ◽  
Biological Activities ◽  
Hematological Parameters ◽  
Octadecenoic Acid ◽  
Radical Scavenging ◽  
Herbal Medicines ◽  
Bioactive Compound ◽  
Dodonaea Viscosa

Abstract Dodonaea viscosa L. Jacq. is an evergreen shrub and native to Asia, Africa and Australia. It has been used as traditional medicine in different countries. The foremost objective of the current study was to discover protective potential of D. Viscosa flowers Methanol (DVM) and Chloroform (DVC) extracts against CCL4 induced toxicity in mice. This study was intended to identify phytochemicals through HPLC, GCMS and FT-IR as well as in vitro antioxidant and in vitro antituberculosis activity. Our comprehensive findings indicate that Dodonaea viscosa is valuable and widespread herbal medicines through therapeutic potentials for curing various ailments. Dodonaea viscosa flowers are found to have protective effect against oxidative stress produced by CCL4 in liver, kidney and spleen. The level of hepatic enzymes (ALP, AST ALT and Direct bilirubin), hematological parameters (RBCs, WBCs and Platelets), total protein and liver antioxidant enzymes (SOD, GPx and CAT) were restored by the intake of DV extracts after decline in levels by CCL4. Histopathological results discovered the defensive effect of 300mg/kg of DVM extract against CCL4 induced damage, thus having improved protective effect as compared to DVC and control. As a result of analysis total flavonoids and total phenolics were also revealed. Phytochemical investigation by HPLC identified gallic acid, epicatechin, cumeric acid, flavonoids while Oleic acid (Octadecenoic acid) (C18H34O2), Stearic acid (C18H36O2), Ricinoleic acid (C18H34O3) and Cedrol (C15H26O) was estimated by GCMS. DVM extract exhibited resistance against in vitro Mycobacterium tuberculosis strains. This study proposed that protective effect of DV against oxidative damage induced in Liver, Kidney and Spleen can possibly be correlated to their antioxidant as well as free radical scavenging property.

scholarly journals Potent Natural Inhibitors of Alpha-Glucosidase and Alpha-Amylase against Hyperglycemia in Vitro and in Vivo

2017 ◽  
Author(s):  
Jirawat Riyaphan ◽  
Chien-Hung Jhong ◽  
May-Jwan Tsai ◽  
Der-Nan Lee ◽  
Max K. Leong ◽  
...  
Keyword(s):  
Type Ii Diabetes ◽  
Herbal Medicines ◽  
Alpha Amylase ◽  
Type Ii ◽  
Reference Drug ◽  
Significant Difference ◽  
Natural Inhibitors ◽  
Alpha Glucosidase

The inhibition of alpha-glucosidase and alpha-amylase is one of clinic strategies for remedy the type II diabetes. Herbal medicines are reported to alleviate hyperglycemia. However, the constituents from those sources whether are targeted to the alpha-glucosidase and alpha-amylase still unexplored. This study attempted to select the compounds for efficacy of hypoglycemia via cellular and mouse levels. The results illustrated that the cytotoxicity in all tested compounds at various concentrations except the concentration of 16-hydroxy-cleroda-3,13-dine-16,15-olide (HCD) at 30 µM were not significant difference (p > 0.05) when compared with the untreated control. Acarbose (reference drug), Antroquinonol, Catechin, Quercetin, Actinodaphnine, Curcumin, HCD, Docosanol, Tetracosanol, Berberine, and Rutin could effectively inhibit the alpha-glucosidase activity of Caco-2 cells when compared with the control (maltose). The compounds (Curcumin, HCD, Tetracosanol, Antroquinonol, Berberine, Catechin, Actinodaphnine, and Rutin) could reduce blood sugar level at 30 min in tested mice. The effects of tested compounds on area under curve (AUC) were significant (p < 0.05) among Acarbose, Tetracosanol, Antroquinonol, Catechin, Actinodaphnine, and Rutin along with Berberine and Quercetin. In in vitro (alpha-glucosidase) with in vivo (alpha-amylase) experiments suggest that bioactive compounds can be a potential inhibitor candidate of alpha-glucosidase and alpha-amylase for the alleviation of type II diabetes.

scholarly journals THE EFFECT OF ESSENTIAL OILS ON MICROORGANISMS CAUSING CARIES AND PERIODONTITIS

2020 ◽  
Vol 20 (2) ◽  
pp. 253-259
Author(s):  
N.M. Devyatkina ◽  
N.O. Bobrova ◽  
E.M. Vazhnichaya
Keyword(s):  
Essential Oils ◽  
Dental Treatment ◽  
Therapeutic Potential ◽  
Oral Care ◽  
Antibacterial Properties ◽  
Herbal Medicines ◽  
Oral Streptococci ◽  
Tea Tree

The oral cavity contains a large number of bacteria, some of which are involved in the development of caries and periodontitis (S. mutans, S. sobrinus, Lactobacilli spp, P. intermedia, P. gingivalis, and T. forythus). The disadvantages of existing antiseptics used in dentistry necessitate the study of antibacterial properties of herbal medicines, and, in particular, of essential oils. The aim of this review is to provide the analysis of literature sources from PubMed and Google Scholar databases related to the effects of essential oils of cloves, mint, thyme, eucalyptus, tea tree and their components on cariogenic and periodontopathic microflora. It was found out that the most in vitro studies evaluated the effects of essential oils or isolated compounds (eugenol, menthol, thymol, carvacrol, eucalyptol, and terpinene-4-ol) on S. mutans, which is considered to be the most cariogenic of oral streptococci, and the researchers limited to defining the susceptibility of the microorganism and effects on biofilm formation. Only in a few studies, the effects of essential oils on the virulence factors of oral pathogens, in particular glycosyl transferase, are represented. Clinical trials of essential oils, their components and combinations confirm the therapeutic potential of these agents in vivo, but raise the question of their effectiveness, taking into account the short-term action, which does not exceed the potency of chlorhexidine. Essential oils of cloves, mint, thyme, eucalyptus, tea tree and their components should be used for treating caries and periodontitis. They are also promising when used as agents of the oral care products, preservatives of the dental medicinal forms, and as remedies for halitosis. With a rational prescription, essential oils can be useful in improving the quality of dental treatment and preventive procedures.

Analysis of the function of the 70-kilodalton cyclase-associated protein (CAP) by using mutants of yeast adenylyl cyclase defective in CAP binding

1993 ◽  
Vol 13 (7) ◽  
pp. 4087-4097
Author(s):  
J Wang ◽  
N Suzuki ◽  
Y Nishida ◽  
T Kataoka
Keyword(s):  
Heat Shock ◽  
Adenylyl Cyclase ◽  
Gene Replacement ◽  
Yeast Cells ◽  
Cyclase Activity ◽  
In Vitro Mutagenesis ◽  
Wild Type ◽  
Adenylyl Cyclase Activity

In Saccharomyces cerevisiae, adenylyl cyclase forms a complex with the 70-kDa cyclase-associated protein (CAP). By in vitro mutagenesis, we assigned a CAP-binding site of adenylyl cyclase to a small segment near its C terminus and created mutants which lost the ability to bind CAP. CAP binding was assessed first by observing the ability of the overproduced C-terminal 150 residues of adenylyl cyclase to sequester CAP, thereby suppressing the heat shock sensitivity of yeast cells bearing the activated RAS2 gene (RAS2Val-19), and then by immunoprecipitability of adenylyl cyclase activity with anti-CAP antibody and by direct measurement of the amount of CAP bound. Yeast cells whose chromosomal adenylyl cyclase genes were replaced by the CAP-nonbinding mutants possessed adenylyl cyclase activity fully responsive to RAS2 protein in vitro. However, they did not exhibit sensitivity to heat shock in the RAS2Val-19 background. When glucose-induced accumulation of cyclic AMP (cAMP) was measured in these mutants carrying RAS2Val-19, a rapid transient rise indistinguishable from that of wild-type cells was observed and a high peak level and following persistent elevation of the cAMP concentration characteristic of RAS2Val-19 were abolished. In contrast, in the wild-type RAS2 background, similar cyclase gene replacement did not affect the glucose-induced cAMP response. These results suggest that the association with CAP, although not involved in the in vivo response to the wild-type RAS2 protein, is somehow required for the exaggerated response of adenylyl cyclase to activated RAS2.

Sign in / Sign up

Export Citation Format

Share Document