Inhibition Of Albumin Denaturation Research Articles

Comparative study of the polyphenol content-related anti-inflammatory and antioxidant activities of two Urera aurantiaca specimens from different geographical areas

BackgroundUrera aurantiaca is an Argentinean species that has been traditionally used to treat symptoms of inflammation. The aim of this study was to determine and compare the anti-inflammatory and antioxidant effects of two specimens of Urera aurantiaca obtained in the provinces of Salta and Misiones, which are two different geographical areas of Argentina.MethodsThe anti-inflammatory activity of the extracts was tested in LPS-stimulated macrophages through the DPPH radical scavenging activity, the SOD-like activity, the reducing power and the inhibition of lipid peroxidation. The anti-inflammatory activity was also evaluated by the inhibition of albumin denaturation and proteinase inhibitory action tests. The total polyphenols, flavonoids and tannins content were quantified.ResultsBoth extracts were able to reduce the augmented NO release in LPS-activated macrophages and showed antioxidant and in vitro anti-inflammatory activities. The polyphenols content was higher in the extract obtained from the specimen from Salta than in that obtained in Misiones. This finding accounts for the higher anti-inflammatory and antioxidant properties obtained with the former.ConclusionThe differences in chemical composition and the biological activities observed between the extracts are probably related to the different environmental conditions found in both provinces.

ASSESSING THE THERAPEUTIC ROLE OF JOSHANDA: PHYTOCHEMICAL, ANTIOXIDANT, ANTI-INFLAMMATORY AND ANTIMICROBIAL ACTIVITIES

Objective: Joshanda, a polyherbal Unani formulation is extensively used as a common home remedy for the treatment of a cough and cold accompanied by pharyngeal inflammation and fever. This study aimed to analyze phytochemicals, antioxidant, anti-inflammatory, and antibacterial activity.Methods: The study investigated the presence of phyto-compounds in joshanda and antioxidant, antibacterial, anti-fungal, and anti-inflammatory activities by various in vitro standard methods using ascorbic acid, ampicillin, and aspirin respectively as standard drugs.Results: Joshanda aqueous extract revealed the presence of tannins, phenols, flavonoids glycosides, terpenoids, and alkaloids and absence of sterols, saponins, xanthoprotiens, and carboxylic acid. Joshanda showed the highest inhibition against B. subtilis (% MGI 99.000±0.577) and least inhibition against P. aeruginosa (%MGI of 84.102±0.491). Joshanda extract, ascorbic acid demonstrated highest % DPPH radical scavenging of 98.379±0.313%, 98.843±0.443% and a minimum of 36.210±1.174%, 83.192±0.422%. Results showed H2O2 scavenging activity of 0.047±0.001 μg/ml per minute degradation of H2O2. FRAP value was observed in joshanda and ascorbic acid with a maximum of 0.945±0.024, 0.687±0.047 mmol and minimum of 0.171±0.036, 0.059±0.005 mmol respectively. Joshanda extract showed the highest albumin denaturation inhibition of 14.069±0.350% and the lowest of 1.880±0.194% at extract volume of 1000 µl and 100 µl respectively. The extract demonstrated the highest proteinase inhibition of 24.003±0.291 % and the lowest of 4.959±0.254% comparable to aspirin. Joshanda had no potent anticandidal activity up to 1 mg/ml.Conclusion: Results clearly suggested that joshanda is a potent phytodrug and can also be used as a strong reactive oxygen species scavenger, might be used as anti-arthritic and strong natural antibiotic agent for effective treatment of various oxidative stressed disorders.

Efficient Access to Imidazo[1,2- a]pyridines/pyrazines/pyrimidines via Catalyst-Free Annulation Reaction under Microwave Irradiation in Green Solvent.

An expeditious catalyst-free heteroannulation reaction for imidazo[1,2- a]pyridines/pyrimidines/pyrazines was developed in green solvent under microwave irradiation. Using H2O-IPA as the reaction medium, various substituted 2-aminopyridines/pyrazines/pyrimidines underwent annulation reaction with α-bromoketones under microwave irradiation to provide the corresponding imidazo[1,2- a]pyridines/pyrimidines/pyrazines in excellent yields. The synthetic methodology appears to be very simple and superior to the already reported procedures with the high abundance of commercial reagents and great ability in expanding the molecular diversity. The present synthetic sequence is visualized as an environmentally benign process which allows the introduction of three points of structural diversity to expand chemical space with excellent purity and yields. The anti-inflammatory and antimicrobial activities of the derivatives were evaluated. Screening results uncovered three derivatives with strong inhibition of albumin denaturation and two derivatives were active on Proteus and Klebsiella bacteria. These positive bioassay results implied that the library of potential anti-inflammatory agents could be rapidly prepared in an ecofriendly manner, and provided new insights into drug discovery for medicinal chemists.

In vitro anticancer, anti-inflammatory, and antioxidant potentials of Ephedra aphylla.

The goal of our study is to test whether a naturally occurring plant, Ephedra aphylla, will show antiproliferative ability against tested cell lines and to test its anti-inflammatory and antioxidative potentials. In our study, we used four solvents with different polarities - aqueous, chloroform, methanol, and n-hexane - to extract different compounds from the aerial parts of E. aphylla. Antioxidant activity of E. aphylla was determined by measuring nitric oxide (NO) and hydrogen peroxide (H2O2) scavenging activities. The anti-inflammatory activity was studied using the inhibition of albumin denaturation assay. Finally, the antiproliferative activity of breast cancer cell lines (T47D, MCF-7) and Vero cell line (African green monkey kidney) was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Phytochemical screening for various extracts of E. aphylla showed the presence of medicinally important compounds including cardiac glycosides, alkaloids, triterpenes, tannins, and flavonoids. The scavenging activity for H2O2 of various solvent extracts was in the order of methanol > aqueous > chloroform > ethyl acetate > n-hexane. In addition, E. aphylla solvent extracts also exhibited a scavenging activity for NO in the order of methanol > ethyl acetate > aqueous > chloroform > n-hexane. All of the solvent extracts showed IC50 inhibition of albumin denaturation at a concentration between 209.5 ± 8.1 and 225 ± 11 μg/ml. Moreover, all extracts displayed strong antiproliferative potential against MFC7, T47D tested cell lines and very weak cytotoxic activity against Vero normal cell line. E. aphylla has a promising potential to be used as a drug source for breast cancer treatment based on its strong antiproliferative activity.

FORMULATION AND EVALUATION OF NOVEL ANTIBACTERIAL AND ANTI-INFLAMMATORY CREAM CONTAINING MUNTINGIA CALABURA LEAVES EXTRACT

Objective: The main objective of the present study was to formulate antibacterial and anti-inflammatory cream using Muntingia calabura leaves extract.Methods: 500 g of matured leaves of M. calabura were extracted with 70% methanol using maceration method for a week. The antibacterial activity of the extract and formulated cream in different concentration was investigated against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus) and two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) through disc diffusion method. The anti-inflammatory activity of extract and formulated cream was studied using inhibition of albumin denaturation technique.Results: The antibacterial activity of the methanolic extract was studied in different concentrations (5, 10, and 25 mg/ml) and the formulated cream was studied in the concentration of (10, 25, 50, and 100 mg/ml). The extract showed significant antibacterial activity with all the tested pathogens with a zone of inhibition ranges from 3.33 ± 0.88-14.60 ± 0.80 mm. As for the formulated cream, the zone of inhibition for F1 ranged from 0.67 ± 0.67 mm to 14.80 ± 1.17 mm. F2 presented zone of inhibition at 3.40 ± 1.64 mm to 15.00 ± 1.18 mm. The anti-inflammatory activity showed maximum inhibition of 63.93 ± 5.90, 41.83 ± 5.64, and 27.20 ± 2.72 was observed at 1000 μg/ml for the extract, F2 and F1, respectively. The cream was found to be in stable state after 2 months.Conclusion: The results showed that the formulated cream can be used for bacterial infections and to reduce inflammation. We recommend this formulation need to be further developed into commercial standards.

Anti-arthritic activity of aqueous-methanolic extract and various fractions of Berberis orthobotrys Bien ex Aitch

BackgroundThe roots and stem bark of Berberis orthobotrys (Berberidaceae) have long been used traditionally to treat joint pain. Though, it has not been pharmacologically assessed for rheumatoid arthritis. The current study explores anti-arthritic activity and phytochemical analysis of aqueous-methanolic extract (30:70) and fractions (ethyl acetate, n-butanol, and aqueous) of Berberis orthobotrys roots.MethodsAnti-arthritic potential was evaluated in vitro using protein denaturation (bovine serum albumin and egg albumin) and membrane stabilization methods at 12.5–800 μg/ml concentration and in vivo via turpentine oil, formaldehyde and Complete Freund Adjuvant (CFA) models at 50, 100 and 150 mg/kg doses. Also, in vitro antioxidant ability was appraised by reducing power assay. Moreover, total flavonoid content, Fourier transform infrared spectroscopy and High performance liquid chromatography of n-butanol fraction were performed.ResultsThe results revealed concentration dependent inhibition of albumin denaturation and notable RBC membrane stabilization, with maximum results obtained at 800 μg/ml. Similarly, plant exhibited dose dependent anti-arthritic effect in turpentine oil and formaldehyde models, with maximum activity observed at 150 mg/kg. The results of CFA model depicted better protection against arthritic lesions and body weight alterations. Also, B.orthobotrys remarkably ameliorated altered hematological parameters, rheumatoid factor and positively modified radiographic and histopathological changes. Additionally, plant exhibited remarkable anti-oxidant activity. Moreover, phytochemical analysis revealed polyphenols and flavonoids.ConclusionTaken together, these results support traditional use of B.orthobotrys as potent anti-arthritic agent that may be proposed for rheumatoid arthritis treatment.

Antioxidant and anti-inflammatory activities of phenolic compounds isolated from Melipona beecheii honey

ABSTRACTMethanolic extract was obtained from Melipona beecheii honey and quantitative analysis of components like total amount of phenolic compounds, flavonoids and flavonols were estimated. Phenolic acids and flavonoids were fractionated by reverse phase HPLC and assessed for antioxidant and anti-inflammatory activities by in vitro methods. Total phenol content was estimated as 63.22 mg of Gallic acid equivalents/100 g of honey. Total flavonoids and flavonols were found to be 3.61 and 3.16 mg of Catechin or Naringenin equivalents/100 g of honey, respectively. The flavonoids fraction exhibited the highest antioxidant activity, with IC50 values of 0.33, 0.92 and 0.36 mg/mL for radical scavenging activity, chelating effects and reducing power, respectively. Inhibition of albumin denaturation, membrane stabilization and proteinase inhibition assays indicated that flavonoids extract showed anti-inflammatory activity. Phenolic compounds like phenolic acids and flavonoids present in the M. beecheii honey could be partially responsible for their antioxidant and anti-inflammatory activities.

EVALUATION OF IN VITRO ANTI-INFLAMMATORY AND ANTIMICROBIAL ACTIVITY OF AQUEOUS AND METHANOLIC SEED EXTRACTS OF CITRULLUS LANATUS

Objective: The present study was designed to identify the bioactive phytochemicals and its antibacterial and in vitro anti-inflammatory potential of aqueous and methanolic seed extract of Citrullus lanatus.Methods: The phytochemical screening of both the aqueous and methanolic seed extract was carried out qualitatively to identify the major Phyto-constituents present in the extracts. The antimicrobial activity of the extracts was evaluated against six pathogenic bacterial strains by agar well diffusion method and the Minimum inhibitory concentration (MIC) was determined by broth dilution method. In vitro anti-inflammatory activity of C. lanatus seed extracts was evaluated by using human red blood cell (HRBC) membrane stabilization and inhibition of albumin denaturation method.Results: The results of the study indicated that both the extracts of the seed having antimicrobial activity, while the methanolic extract showed more significant activity against the tested organism than aqueous extract. Methanol extract had the lowest MIC of 1.562 mg/ml against Escherichia coli, Staphylococcus aureus, Klebsiella pneumonia, Pseudomonas aeruginosa and Bacillus subtilis, whereas in aqueous extract was highly sensitive to Bacillus subtilis, E. coli and Klebsiella pneumonia with MIC of 3.125 and 6.25 mg/ml, respectively. Methanolic extracts exerted comparative higher anti-inflammatory activity than aqueous extract.Conclusion: Present study provides a firm evidence to support that the synergistic effect of C. lanatus seed extracts having potent anti-inflammatory and antimicrobial property, which might serve as an effective drug for various microbial infections and inflammatory disorders.

EVALUATION OF ANTIOXIDANT AND ANTI-INFLAMMATORY PROPERTIES OF AQUEOUS EXTRACT OF WILD MUSHROOMS COLLECTED FROM HIMACHAL PRADESH

ABSTRACTObjective: The objective of this study is to elucidate phytochemical contents, antioxidant, and anti-inflammatory activity of wild mushrooms collectedfrom Himachal Pradesh.Methods: Quantitative analysis of phytochemical constituents was carried out using standard methods while 1,1 diphenylpicrylhydrazyl nitric oxide,hydrogen peroxide-free radical scavenging assay were used to evaluate the antioxidant properties of selected wild mushrooms. Anti-inflammatorycapacity of samples was evaluated by human red blood cell membrane stabilization and albumin denaturation inhibition method.Results: The results obtained revealed that Pleurotus floridanus showed higher total phenol, flavonoid carotenoid, and ascorbic acid contentsof 61.13±2.3 mg/g, 15.2±1.13 mg/g, 12.42±0.42 μg/g, 17.36±0.40 μg/g, and 14.55±0.58 mg/g. All the species showed antioxidant potential, butP. floridanus proved to be more active while Macrocybe sp. proved to be least one.Conclusion: The mushroom species analyzed have been showed to be good source of phytoconstituents, antioxidants, and also possess antiinflammatoryproperties, thus can be used in the management of oxidative stress-induced disease.Keywords: Wild mushrooms, Scavenging effect, Total phenol, Antioxidant, Anti-inflammatory.

Design, synthesis and pharmacological analysis of 5-[4'-(substituted-methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles.

In the present paper 5-[4'-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles (5a-g) and [2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h-q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

PHYTOCHEMICAL ANALYSIS AND IN VITRO BIOLOGICAL CHARACTERIZATION OF AQUEOUS AND METHANOLIC EXTRACT OF BACOPA MONNIERI

<p><strong>Objective</strong>:<strong> </strong>The present study was designed to identify the phytocompounds, to compare the antibacterial, antioxidant, and anti-inflammatory effects of aqueous and methanolic extract of <em>Bacopa monnieri</em>.</p><p><strong>Methods</strong>:<strong> </strong>Antioxidant activity was determined by 1, 1-diphenyl-2-picrylhydrazyl (DPPH), Ferric Reducing Antioxidant Power (FRAP), Super oxide dismutase (SOD), Reduced glutathione (GSH), Catalase assays. Anti-inflammatory activity was measured with inhibition of albumin denaturation and trypsin inhibitory assay. Finally, extracts were tested against various pathogenic bacterial and fungal strains by broth dilution assay and disc diffusion assay respectively.</p><p><strong>Results: </strong>Results showed the presence of alkaloids, flavonoids, phenols, quinines and glycosides etc while steroids and carboxylic acid were absent. The extracts demonstrated free radical-scavenging activity quite comparable with standard ascorbic acid. Methanolic extract exerted comparative higher antioxidant and anti-inflammatory activity than aqueous extract. Both extracts were most effective against <em>Bacillus subtilis</em><em> </em>and lowest inhibition against<em> Staphylococcus aureus</em>.</p><p><strong>Conclusion: </strong>The results obtained clearly indicated a promising potential of <em>B. monnieri</em> for serving as a strong ROS scavenger, might be used as anti-arthritic and strong natural antibiotic agent for effective treatment of various oxidative stressed disorders (cancer, cardiovascular diseases), inflammatory disorders (rheumatoid arthritis) and various bacterial infections.</p>

Evaluation of in Vitro Anti-inflammatory and Antioxidant Activity of Selected Zimbabwean Plant Extracts

ABSTRACTThe in vitro anti-inflammatory and antioxidant activities of Zimbabwean medicinal plant extracts were investigated by COX-1 and COX-2 enzyme inhibitory activity, the erythrocyte membrane stabilization, and albumin denaturation inhibition assays; free-radical scavenging activity of the plant extracts was determined using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and tetramethoxy azobismethylene quinone (TMAMQ) radical scavenging assays. Combretum zeyheri, C. molle, and Parinari curatellifolia inhibited COX-2, inhibiting COX-1 the least with inhibitions of 42, 68, and 77%, respectively, for COX-2. C. platypetalum selectively inhibited COX-2 by 85% and COX-1 inhibition by 42%. IC50 of C. platypetalum and indomethacin for COX-2 were 571 and 414 µg.mL–1, respectively. C. platypetalum, C. molle, and Brachystegia boehmii stabilized the erythrocyte membrane and inhibited the precipitation of proteins in vitro. Plant extracts that inhibited the COX enzymes were tested for antioxidant activity using the DPPH and the TMAMQ free-radical scavenging assays. P. curatellifolia extract showed potent antioxidant activity in both assays with 100% of the radicals quenched at 16 and 18 µg.mL–1, respectively.

In vitro xanthine oxidase and albumin denaturation inhibition assay of Barringtonia racemosa L. and total phenolic content analysis for potential anti-inflammatory use in gouty arthritis.

Aim:This study was conducted to evaluate the in vitro anti-inflammatory activities and total phenolic content (TPC) of methanolic extracts of infloresence axes, endosperms, leaves, and pericarps of Barringtonia racemosa L.Methods:The anti-inflammatory study was conducted by assessing the potential through xanthine oxidase (XO) and albumin denaturation inhibition assays. Meanwhile, the TPC in the extracts were assessed by Folin-Ciocalteu assay.Results:In the XO inhibition assay, the infloresence axes extract was found to exert the highest inhibition capacity at 0.1% (w/v) with 59.54 ± 0.001% inhibition followed by leaves (58.82 ± 0.001%), pericarps (57.99 ± 0.003%), and endosperms (57.20 ± 0.003%) extracts. Similarly in the albumin denaturation inhibition assay, the infloresence axes extract had shown the greatest inhibition capacity with 70.58 ± 0.004% inhibition followed by endosperms (66.80 ± 0.024%), leaves (65.29 ± 0.006%), and pericarps extracts (43.33 ± 0.002%). Meanwhile, for TPC analysis, leaves extract was found to have the highest phenolic content (53.94 ± 0.000 mg gallic acid equivalent [GAE]/g DW) followed by infloresence axes (31.54 ± 0.001 mg GAE/g DW), endosperms (22.63 ± 0.001 mg GAE/g DW), and the least was found in pericarps (15.54 ± 0.001 mg GAE/g DW).Conclusion:The results indeed verified the in vitro anti-inflammatory activities of B. racemosa and supported its potential to be used in alleviating gouty arthritis and XO-related diseases.

Ulcerogenicity devoid novel non-steroidal anti-inflammatory agents (NSAIDS): syntheses, computational studies, and activity of 5-aryliden-2-imino-4-thiazolidinones

A series of new 5-aryliden-2-imino-4-thiazolidinones (5a–e and 6a–e) were synthesized via a three-step reaction and characterized by physicochemical and spectral data. The uniqueness of the derivatives lies in the fact that none of them had an acidic group, like conventional NSAIDS, but exhibited significant in vivo activity in acute inflammation models. In particular, 5-(3-chlorobenzyliden)-2-(pyridin-2-yl-imino)-4-thiazolidinone(5a) and 5-(3-chlorobenzyliden)-2-(5-methylisoxazol-3-yl-imino)-4-thiazolidinone (6a) showed remarkable paw oedema inhibition (67.76 and 74.47 % oedema inhibition, respectively, after 3 h) comparable to that of Ibuprofen (74.56 % oedema inhibition, after 3 h) at half of the dose of the standard drug. Also, compounds 5a (72.86 %) and 6a (80.20 %) were found to possess significant inhibition of albumin denaturation when screened for in vitro anti-inflammatory activity. In addition, these compounds were docked into the known active site of COX-2 protein using Glide XP and QPLD algorithms, and the binding-free energy was calculated using Prime MM/GBSA simulation methods. The combined use of molecular docking and MM/GBSA methods gave a good correlation between the predicted binding-free energy and experimentally determined biological activities. It was also evident from the docking results that 2-methylisoxazolylimino or 2-(pyridin-2-yl-imino substitution and 3-chloro moiety on 5-benzylidin nucleus of these 4-thiazolidinone derivatives can easily occupy the COX-2 binding pocket, considered as the critical interaction for COX-2 inhibition. Moreover, pharmacokinetic properties of all the synthesized compounds were predicted, with good results. Further, the synthesized derivatives showed neither acute toxicity nor symptoms of gastric ulceration, at extended doses, owing to the absence of an acidic group.