scholarly journals A Face Serum Containing Bakuchiol, Palmitoyl Tripeptide-38, Hydrolyzed Hyaluronic Acid and a Polyherbal and Vitamin Blend Improves Skin Quality in Human Volunteers and Protects Skin Structure In vitro

2021 ◽  
Author(s):  
Brett J West ◽  
Ifedayo Alabi ◽  
Shixin Deng
Keyword(s):  
Patch Test ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Quality Parameters ◽  
Biologically Active ◽  
Efficacy Trial ◽  
Dermatological Examination ◽  
The Face ◽  
Skin Quality

A face serum composed of a combination of biologically active compounds was evaluated for safety and efficacy in vitro, in a repeat insult patch test and in a human clinical efficacy trial. The serum inhibited tyrosinase activity modestly, decreased collagenase activity and exhibited notable free radical scavenging activity in vitro. It is gentle to the skin, as the serum did not irritate the skin or produce symptoms of allergic contact dermatitis in the 55 healthy adults that participated in the repeat insult patch test. In the efficacy trial, daily application of the face serum for 30 days significantly increased skin hydration, with all 35 volunteers experiencing improvement. Substantial improvements in skin elasticity, roughness (fine lines and wrinkles), and brightness also occurred during the trial. Dermatological examination also revealed a trend for reduced comedone count with use of the serum. Self-assessment responses revealed that all volunteers experienced improvements in multiple skin quality parameters and that participant perceptions are consistent with the results of the instrumental analyses. These findings indicated that the measured improvements in skin quality are not only statistically significant but are also clinically relevant as they were great enough for users of the face serum to feel and recognize.

Synthesis, Characterization and Biological Evaluation of Indole-Pyrazole Amalgamated α-Cyano Substituted Chalcones

2021 ◽  
Vol 21 ◽  
Author(s):  
Pravin S. Bhale ◽  
Sadanand N. Shringare ◽  
Amol B. Khade ◽  
Hemant V. Chavan
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Safety Margin ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Monkey Cell ◽  
Mcf 7

Background: Indole and pyrazole constitute a major class of biologically active scaffolds. The amalgamation of two or more pharmacophores would generate novel molecular templates that are likely to unveil remarkable biological properties. Objective: An efficient and high yielding synthesis of indole-pyrazole integrated α-cyano substituted chalcones and their in vitro antibreast cancer and antioxidant evaluation. Methods: The synthesis of a series of indole-pyrazole amalgamated α-cyano substituted chalcones (6a-o) was achieved by reacting substituted 3-cyanoacetyl indole 2 with substituted pyrazole aldehyde 5 in the presence of piperidine. All the newly synthesized compounds have been characterized by IR, 1H NMR and HRMS spectroscopy. Results: Anti-breast cancer evaluation of the synthesized compounds in vitro against MCF-7 cell line revealed high anti-breast cancer activities. Amongst the compounds screened 6f, 6g, 6h, 6c, 6d, 6e, 6i and 6k unveiled excellent activity against breast carcinoma (GI50 <0.1µM) as good as adriamycin (GI50 <0.1µM). The compounds were also screened against the normal Vero monkey cell line and the results demonstrated more selectivity against MCF-7. In other hand, compounds, 6b, 6c, 6d, 6h and 6i have shown moderate DPPH and NO radical scavenging activity. Conclusion: Most of the synthesized compounds exhibited significant antitumor activities. These results further support its safety margin by studying the activity on normal Vero monkey cell line. These results acclaim the possible use of these compounds for the design and development of potent anti-breast cancer agents.

scholarly journals Protective effect of Aurelia aurita against free radicals and streptozotocin-induced diabetes

2018 ◽  
Vol 13 (3) ◽  
pp. 287 ◽  
Author(s):  
Mallikarjuna Rao Talluri ◽  
Alekhya Ketha ◽  
Ganga Rao Battu ◽  
Rajananda Swamy Tadi ◽  
Vinay Bharadwaj Tatipamula
Keyword(s):  
Free Radicals ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Aurelia Aurita ◽  
Biologically Active ◽  
Chemical Profiling ◽  
Streptozotocin Induced Diabetes ◽  
Anti Oxidant ◽  
Profiling Analysis

<p class="Abstract">The present work was carried out to identify the anti-oxidant and anti-diabetic activities of Aurelia aurita. The chemical profiling analysis showed that it possess different biologically active secondary metabolites like phenols, alakoids, steroids etc. The methanolic extract showed different free radical scavenging activity as ascorbic acid with  IC<sub>50</sub> values 202, 205, 153 µg on DPPH, hydroxyl and superoxide free radicals. The extract significantly reduced the hyperglycemic conditions with percentage of reduction 18.7 ± 1.3 to 53.5 ±1.5 of streptozotocin-induced animals and the positive result of in-vitro aldose reductase enzyme inhibition with IC<sub>50</sub> value 163 µg suggests that A. aurita have potential to cure the diabetic complications.</p>

scholarly journals Synthesis, Characterization and Biological Evaluation of Novel Triazole Linked Chromone Biheterocycle Analogs

2021 ◽  
Vol 34 (1) ◽  
pp. 53-59
Author(s):  
Jilla Soujanya ◽  
D. Ravisankar Reddy ◽  
Gade Kalyani
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biological Properties ◽  
Protective Role ◽  
Biological Evaluation ◽  
Biologically Active ◽  
The Novel ◽  
Spectral Techniques ◽  
Physico Chemical

The current work focused on the synthesis of novel chromone biheterocycle analogs followed by its characterization through physico-chemical and spectral techniques like FTIR, mass and NMR spectroscopy. The basic triazole heterocycle and its analogs have different biological properties. At the point when one biological active molecule is connected to another, the resultant shows improved potency (biheterocycles). Chromone and triazole are selected in this study to develop new efficient, simple, economically viable and biologically active synthetic compounds. All the novel derivatives of triazole linked chromone biheterocycles were synthesized via a click chemistry procedure and screened for in vitro antimicrobial, antifungal and antioxidant studies. Among them, the compounds CRN-F (IC50 = 35.97), CRN-H (IC50 = 28.76) and CRN-J (IC50 = 29.72) have significant free radical scavenging activity in comparison with the ascorbic acid as control standard (IC50 = 23.07). Some of these novel derivatives exhibited moderate antimicrobial and antifungal activity compared to that of the reference standards. Hence, the novel chromone biheterocycle analogs played a protective role against oxidative damage.

scholarly journals Pharmacological Basis for Traditional Use of theLippia thymoides

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Fabrício Souza Silva ◽  
Pedro Modesto Nascimento Menezes ◽  
Pedro Guilherme Souza de Sá ◽  
André Luís de Santana Oliveira ◽  
Eric Alencar Araújo Souza ◽  
...  
Keyword(s):  
Wound Healing ◽  
Crude Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biologically Active ◽  
Control Group ◽  
Oral Toxicity ◽  
Traditional Use ◽  
Crude Extracts

The aim of this study was to evaluate crude extracts and fractions from leaves and stems ofLippia thymoidesand to validate their use in folk medicine.In vitroantioxidant and antimicrobial activities andin vivowound healing in rats, baker yeast-induced fever in young rats, and acute oral toxicity in mice assays were realized. The crude extracts and their dichloromethane and ethyl acetate fractions had potent radical-scavenging activity against the DPPH but were not effective in theβ-carotene bleaching method. The dichloromethane fraction from the leaves extract showed the broadest spectrum of activity againstS. aureus,B. cereus, andC. parapsilosis. The animals treated with crude extracts showed no difference in wound healing when compared with the negative control group. The crude extract from leaves (1200 mg/kg) has equal efficacy in reducing temperature in rats with hyperpyrexia compared to dipyrone (240 mg/kg) and is better than paracetamol (150 mg/kg). In acute toxicity test, crude extract of leaves fromLippia thymoidesexhibited no mortality and behavioral changes and no adverse effects in male and female mice. This work validates the popular use ofLippia thymoidesfor treating the wound and fever, providing a source for biologically active substances.

scholarly journals Antioxidant and Antiplasmodial Activities of Bergenin and 11-O-Galloylbergenin Isolated fromMallotus philippensis

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Hamayun Khan ◽  
Hazrat Amin ◽  
Asad Ullah ◽  
Sumbal Saba ◽  
Jamal Rafique ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Biologically Active ◽  
Protein Receptors ◽  
Total Antioxidant ◽  
Reducing Power Assay

Two important biologically active compounds were isolated fromMallotus philippensis. The isolated compounds were characterized using spectroanalytical techniques and found to be bergenin (1) and 11-O-galloylbergenin (2). Thein vitroantioxidant and antiplasmodial activities of the isolated compounds were determined. For the antioxidant potential, three standard analytical protocols, namely, DPPH radical scavenging activity (RSA), reducing power assay (RPA), and total antioxidant capacity (TAC) assay, were adopted. The results showed that compound2was found to be more potent antioxidant as compared to1. Fascinatingly, compound2displayed better EC50results as compared toα-tocopherol while being comparable with ascorbic acid. The antiplasmodial assay data showed that both the compound exhibited good activity against chloroquine sensitive strain ofPlasmodium falciparum(D10) and IC50values were found to be less than 8 μM. Thein silicomolecular docking analyses were also performed for the determination of binding affinity of the isolated compounds usingP. falciparumproteins PfLDH and Pfg27. The results showed that compound2has high docking score and binding affinity to both protein receptors as compared to compound1. The demonstrated biological potentials declared that compound2could be the better natural antioxidant and antiplasmodial candidate.

Synthesis, Characterization, Antimicrobial and Antioxidant Potential of Diazenyl Chalcones

2018 ◽  
Vol 18 (10) ◽  
pp. 844-856 ◽  
Author(s):  
Harmeet Kaur ◽  
Balasubramanian Narasimhan
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antioxidant Potential ◽  
Dilution Method ◽  
Dpph Assay ◽  
Antimicrobial Potential ◽  
Structural Conformation ◽  
Uv Visible ◽  
Tube Dilution Method

A series of diazenyl chalcones was prepared by base catalyzed Claisen-Schmidt condensation of synthesized hydroxy substituted acetophenone azo dye with various substituted aromatic/ heteroaromatic aldehydes. The structural conformation of synthesized chalcones was done by a number of physicochemical and spectral means like FTIR, UV-visible, mass, NMR spectroscopy and CHNS/O analysis. These diazenyl chalcones were assessed for their in vitro antimicrobial potential against several Gram-negative, Gram-positive bacterial and fungal strains by serial tube dilution method. The fluconazole and cefadroxil were used as standard drugs. The target compounds were also evaluated for their antioxidant potential by DPPH assay. (2E)-3-(2,4-Dichlorophenyl)-1-(4-((2,6- dihydroxyphenyl)diazenyl)phenyl)prop-2-en-1-one (C-7) had shown very good antimicrobial potential with MIC ranges from 3.79 to 15.76 μg/ml against most of the tested microorganisms. Most of the synthesized diazenyl chalcones were found to be active against B. subtilis. The (2E)-1-(5-((2-Chloro- 4-nitrophenyl)diazenyl)-2-hydroxyphenyl)-3-(2-hydroxynaphthalen-1-yl)prop-2-en-1-one (C-10) had shown high free radical-scavenging activity when compared with the ascorbic acid as the reference antioxidant.

α-Glucosidase Inhibition, Antioxidant and Docking Studies of Hydroxycoumarins and their Mono and Bis O-alkylated/acetylated Analogs

2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Catalytic Site ◽  
Docking Simulations ◽  
In Silico Docking ◽  
Anti Oxidant

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.

Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Enzyme Inhibitor ◽  
Radical Scavenging Activity ◽  
Curcuma Longa ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Inhibitory Effect ◽  
Curcumin Derivatives ◽  
Reducing Power Assay

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

scholarly journals Inhibitory Effect of Antidesma bunius Fruit Extract on Carbohydrate Digestive Enzymes Activity and Protein Glycation In Vitro

Antioxidants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Pattamaporn Aksornchu ◽  
Netima Chamnansilpa ◽  
Sirichai Adisakwattana ◽  
Thavaree Thilavech ◽  
Charoonsri Choosak ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging Activity ◽  
Digestive Enzyme ◽  
Radical Scavenging ◽  
Protein Glycation ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Fruit Extract ◽  
Antioxidant Power ◽  
Ic50 Values

Antidesma bunius (L.) spreng (Mamao) is widely distributed in Northeastern Thailand. Antidesma bunius has been reported to contain anthocyanins, which possess antioxidant and antihypertensive actions. However, the antidiabetic and antiglycation activity of Antidesma bunius fruit extract has not yet been reported. In this study, we investigated the inhibitory activity of anthocyanin-enriched fraction of Antidesma bunius fruit extract (ABE) against pancreatic α-amylase, intestinal α-glucosidase (maltase and sucrase), protein glycation, as well as antioxidant activity. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) chromatogram revealed that ABE contained phytochemical compounds such as cyanidin-3-glucoside, delphinidin-3-glucoside, ellagic acid, and myricetin-3-galactoside. ABE inhibited intestinal maltase and sucrase activity with the IC50 values of 0.76 ± 0.02 mg/mL and 1.33 ± 0.03 mg/mL, respectively. Furthermore, ABE (0.25 mg/mL) reduced the formation of fluorescent AGEs and the level of Nε-carboxymethyllysine (Nε-CML) in fructose and glucose-induced protein glycation during four weeks of incubation. During the glycation process, the protein carbonyl and β-amyloid cross structure were decreased by ABE (0.25 mg/mL). In addition, ABE exhibited antioxidant activity through DPPH radical scavenging activity and Trolox equivalent antioxidant capacity (TEAC) with the IC50 values 15.84 ± 0.06 µg/mL and 166.1 ± 2.40 µg/mL, respectively. Meanwhile, ferric reducing antioxidant power (FRAP) showed an EC50 value of 182.22 ± 0.64 µg/mL. The findings suggest that ABE may be a promising agent for inhibiting carbohydrate digestive enzyme activity, reducing monosaccharide-induced protein glycation, and antioxidant activity.

scholarly journals Antioxidant potential and optimization of production of extracellular polysaccharide by Acinetobacter indicus M6

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Ch. Ravi Teja ◽  
Abraham P. Karlapudi ◽  
Neeraja Vallur ◽  
K. Mamatha ◽  
D. John Babu ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Basal Medium ◽  
Extracellular Polysaccharide ◽  
Extracellular Polysaccharides ◽  
Scavenging Activity ◽  
Promising Alternative ◽  
Food Engineering ◽  
The Face

Abstract Background Extracellular polysaccharides (ECPs) produced by biofilm-producing marine bacterium have great applications in biotechnology, pharmaceutical, food engineering, bioremediation, and bio-hydrometallurgy industries. The ECP-producing strain was identified as Acinetobacter indicus M6 species by 16S rDNA analysis. The polymer produced by the isolate was quantified and purified and chemically analyzed, and antioxidant activities have been studied. The face-centered central composite design (FCCCD) was used to design the model. Results The results have clearly shown that the ECP was found to be endowed with significant antioxidative activities. The ECP showed 59% of hydroxyl radical scavenging activity at a concentration of 500 μg/mL, superoxide radical scavenging activity (72.4%) at a concentration of 300 μg/mL, and DPPH˙ radical scavenging activity (72.2%) at a concentration of 500 μg/mL, respectively. Further, HPLC and GC-MS results showed that the isolated ECP was a heteropolymer composed of glucose as a major monomer, and mannose and glucosamine were minor monomers. Furthermore, the production of ECP by Acinetobacter indicus M6 was increased through optimization of nutritional variables, namely, glucose, yeast extract, and MgSO4 by “Response Surface Methodology”. Moreover the production of ECP reached to 2.21 g/L after the optimization of nutritional variables. The designed model is statistically significant and is indicated by the R2 value of 0.99. The optimized medium improved the production of ECP and is two folds higher in comparison with the basal medium. Conclusions Acinetobacter indicus M6 bacterium produces a novel and unique extracellular heteropolysaccharide with highly efficient antioxidant activity. GC-MS analyses elucidated the presence of quite uncommon (1→4)-linked glucose, (1→4)-linked mannose, and (→4)-GlcN-(1→) glycosidic linkages in the backbone. The optimized medium improved the production of ECP and is two folds higher in comparison with the basal medium. The newly optimized medium could be used as a promising alternative for the overproduction of ECP.

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