scholarly journals Synthesis, characterization, in-vitro anti-inflammatory and antimicrobial screening of metal(II) mixed diclofenac and acetaminophen complexes

2021 ◽  
Vol 35 (1) ◽  
pp. 77-86
Author(s):  
J. A. Obaleye ◽  
A. A. Aliyu ◽  
A. O. Rajee ◽  
K. E. Bello
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Salt ◽  
Electronic Absorption Spectra ◽  
Salmonella Typhi ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Bidentate Coordination ◽  
Antimicrobial Screening ◽  
Anti Inflammatory

Mixed ligand complexes derived from diclofenac potassium salt (Kdc) and acetaminophen (ace) has been synthesized and proposed to have a general formula [MB] where M = Co2+, Ni2+, Cu2+ and Zn2+and B = (ace)(dc)(H2O)2 except for Mn2+ complex which exists as [Mn(ace)(dc)OH2]. The complexes were characterized by solubility, melting point, conductivity, elemental analyses, UV-Vis, FT-IR spectroscopy, X-ray powder diffraction (XRPD) study and magnetic susceptibility measurement. Electronic absorption spectra data are characteristic of octahedral structures for [MB]. The IR spectra revealed a bidentate coordination mode. In acetaminophen, the nitrogen and carbonyl-O atoms of the amide group were involved while the carboxylate oxygen atoms of potassium diclofenac were used; typical of a carboxylic acid derivative. The compounds were screened for in-vitro anti-inflammatory activity by inhibition of albumin denaturation assay and antimicrobial activity against bacteria strains: Bacillus subtilis, Bacillus anthrax, Escherichia coli, Salmonella typhi and a fungus Aspergillus niger. Some of the tested compounds showed moderate anti-inflammatory activity when compared to the standard drug diclofenac potassium salt. The in-vitro antimicrobial screening revealed an increased activity of the complexes against the bacteria isolates compared to the free ligands.                     KEY WORDS: Metal(II) ion, NSAIDs, Anti-inflammatory activity, Diclofenac potassium salt, XRPD, Antimicrobial activity   Bull. Chem. Soc. Ethiop. 2021, 35(1), 77-86. DOI: https://dx.doi.org/10.4314/bcse.v35i1.6

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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

2017 ◽  
Vol 9 (5) ◽  
pp. 29
Author(s):  
Iswariya S. ◽  
Uma T. S.
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Aqueous Extract ◽  
Seed Extract ◽  
Inflammatory Activity ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Anti Inflammatory ◽  
Seed Extracts

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.

scholarly journals SYNTHESIS, ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ETHYL 2-(2-CYANO-3- (SUBSTITUTED PHENYL)ACRYLAMIDO)-4,5-DIMETHYLTHIOPHENE-3-CARBOXYLATES

2017 ◽  
Vol 10 (7) ◽  
pp. 95 ◽  
Author(s):  
Madhavi K ◽  
Sree Ramya G
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Antioxidant Properties ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: Objective of the study was to synthesize and evaluate a series of novel compounds, ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)- 4,5-dimethylthiophene-3-carboxylates, for in vitro antioxidant and in vivo anti-inflammatory activities.Methods: Ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylates were synthesized by knoevenagel condensation of active methylene group of ethyl 2-(2-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate with substituted benzaldehydes. The synthesized compounds were evaluated for their in vitro antioxidant properties in three different models, viz., reduction of 1,1-diphenyl-2-pycrylhydrazyl free radical, scavenging of nitric oxide free radical, and ferric ion-induced lipid peroxidation using rat brain homogenate. Few selected compounds with good antioxidant properties were pharmacologically evaluated for anti-inflammatory activity by carrageenan-induced rat paw edema model.Results: Clean and efficient synthetic procedure was used for the preparation of series of compounds. The structures of synthesized compounds were confirmed by infrared, 1H nuclear magnetic resonance and mass spectra. The antioxidant activity data revealed that the compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant activity. Hence, the active compounds were evaluated for anti-inflammatory activity and found to possess good activity. The percentage inhibition of rat paw edema obtained for the evaluated compounds was in the range of 70.2-83.1, comparable to the standard drug diclofenac (85.0%).Conclusion: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5- dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant and anti-inflammatory activities.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF METHANOL EXTRACT OF NIEBUHRIA APETALA (ROTH) DUNN – IN VITRO MODELS

2019 ◽  
pp. 278-281
Author(s):  
RAJESH A ◽  
DOSS A ◽  
TRESINA PS ◽  
MOHAN VR
Keyword(s):  
Methanol Extract ◽  
Protein Denaturation ◽  
In Vitro Models ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Inflammatory Agent ◽  
Potential Source ◽  
Anti Inflammatory

Objective: The objective of this study was to determine the anti-inflammatory activity of methanol extract of Niebuhria apetala and its possible mechanism of action. Methods: Methanol extract of Niebuhria apetala leaf (NAL) was assessed for its anti-inflammatory activity by in vitro methods. Using albumin denaturation assay, proteinase inhibitory activity, membrane stabilization, and antilipoxygenase activity at different concentrations, in vitro anti-inflammatory activity was estimated. The standard drug used for this purpose was aspirin. Results: Methanol extract NAL at a concentration range of 100–500 μg/ml significant (p<0.01) protects the heat-induced protein denaturation. At the concentration of 500 mg/ml, NAL showed significant (p<0.01) inhibition of protease inhibitory action. Heat-induced hemolysis of erythrocyte, hypotonicity-induced hemolysis, and lipooxygenase activity were significant (p<0.01) inhibited at the concentration of 500 μg/ml. Conclusion: Finally, the present study indicates that methanol extract of Niebuhria apetala can be a potential source of anti-inflammatory agent.

scholarly journals A scientific validation of In vitro anti-inflammatory activity of Punica granatum L. by human red blood cell membrane stabilization

2018 ◽  
Vol 6 (7) ◽  
pp. 2430
Author(s):  
Karunakar Kota ◽  
Sandhya Sharma ◽  
Jameela Tahashildar
Keyword(s):  
Methanolic Extract ◽  
Punica Granatum ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Fruit Peel ◽  
Standard Drug ◽  
Membrane Lysis ◽  
Anti Inflammatory ◽  
Punica Granatum L

Background: In recent years there has been growing interest in therapeutic use of natural products, especially those derived from plants. P. granatum is very common dietary ingredient in many parts of India and has remarkable biological and medicinal properties.Methods: In the present study, the methanolic extract of fruit peels of Punica granatum Linn. (MEPG) were investigated for anti-inflammatory activity by simple, reliable, less toxic and less time consuming HRBC membrane stabilization method. The presentation of hypo tonicity induced HRBC membrane lysis was taken a measure of anti-inflammatory activity. Their activities were compared with standard drug diclofenac.Results: The results of the study demonstrated that P. granatum contains active constituents, which possess anti-inflammatory activity which is probably related to the inhibition of prostaglandin synthesis.Conclusions: It is concluded that methanolic extract of P. granatum fruit peel possesses significant anti-inflammatory activity and this is a possible rationale for its folkloric use as an anti-inflammatory agent.

scholarly journals Anti-inflammatory and Anti-arthritic Potentials of Maesa Montana Roots

2021 ◽  
Vol 18 (16) ◽  
Author(s):  
Sanjida SHARMIN ◽  
Rabeya Gazi JHUMA ◽  
Sanjida ISLAM ◽  
Riniara KHATUN
Keyword(s):  
Bovine Serum ◽  
Protein Denaturation ◽  
Inflammatory Activity ◽  
Flowering Plant ◽  
Activity Measurement ◽  
Root Extract ◽  
Standard Drug ◽  
Activity Test ◽  
Anti Inflammatory

Maesa Montana is a flowering plant of the Myrsinaceae family, which is locally known as ramjani. The current study aimed to evaluate the in-vitro anti-arthritic and anti-inflammatory activities of the root extract of this plant. The anti-inflammatory performances were measured by the hindrance of egg white denaturation, and anti-arthritic activity was investigated by Bovine serum protein. In the anti-inflammatory activity test, the methanolic root extract of this plant showed 69.29 ± 1.19 % of inhibition at a concentration of 1000 µg/mL and standard drug exhibited 90.11 ± 1.45 % of inhibition at the same concentration. Furthermore, in the anti-arthritic activity test, the extract demonstrated 68.18 ± 1.34 % of inhibition at a concentration of 1000 µg/mL whereas the standard diclofenac drug showed 90.65 ± 1.19 % of inhibition at the same concentration. These results revealed that the root extract of this plant possesses significant anti-arthritic and anti-inflammatory activities based on the inhibition of BSA and protein denaturation. HIGHLIGHTS Methanol soluble compounds extraction from the roots of Maesa Montana Anti-inflammatory activity determination using egg albumin Anti-arthritic activity measurement using bovine serum albumin GRAPHICAL ABSTRACT

scholarly journals POTENTIAL ANTIOXIDANT, ANTI-INFLAMMATORY AND ANTIBACTERIAL EVALUATION OF EXTRACTS OF LEUCAS ASPERA USING IN VITRO MODELS

2016 ◽  
Vol 8 (12) ◽  
pp. 292 ◽  
Author(s):  
Tahareen S. ◽  
Shwetha R. ◽  
Myrene R. D.
Keyword(s):  
Inflammatory Activity ◽  
Total Phenolic ◽  
Scavenging Activity ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Leucas Aspera ◽  
Ic50 Value ◽  
Anti Inflammatory ◽  
Stabilization Assay

<p><strong>Objective: </strong>To evaluate the potential antioxidant, anti-inflammatory and antibacterial activities of aqueous and methanolic extracts of leaves of <em>Leucas aspera</em> (Thumbae).</p><p><strong>Methods: </strong>Phytochemical screening of the leaves of <em>L. aspera</em> was followed by analysis of antioxidant activity by means of DPPH (2, 2-diphenyl-1-picrylhydrazyl) radical scavenging activity. <em>In vitro</em> anti‐inflammatory activity was evaluated using lipoxygenase inhibition, albumin denaturation assay, membrane stabilization assay and proteinase inhibitory activity at different concentrations. Aspirin was used as a standard drug for the study of anti‐inflammatory activity. Linear regression analysis was used to calculate half maximal inhibitory concentration, IC50 value. The zone of inhibition was performed against common pathogens to determine the antimicrobial activity at different concentrations of plant extracts (60%, 70%, 80%).</p><p><strong>Results: </strong>The phytochemical analysis revealed the presence of carbohydrates, amino acid, alkaloids, tannins, flavonoids, glycosides, xanthoproteins, and phenols. The total phenolic and flavonoid content was found to be 2.25±0.04 mg GAE/g (gallic acid equivalents) and 1.2±0.05 mg QE/g (Quercetin equivalents) of fresh weight tissue respectively. The IC50 values for hydrogen peroxide scavenging activity were found to be 244.6 µg/ml. The extract inhibited the lipoxygenase enzyme activity with an IC50 value of 356.3 µg/ml. Maximum inhibition of heat-induced protein denaturation of 69% was observed at 400 μg/ml, IC50 249.6 μg/ml. Proteinase activity was also significantly inhibited (IC50 = 421.6 μg/ml). Membrane stabilization assay attributed minor protection by the leaf extract with an IC50 of 206.7. It was observed that <em>E. coli</em> were inhibited at all concentrations, followed by <em>Klebsiella</em> and <em>Pseudomonas</em>.</p><p><strong>Conclusion: </strong>Results indicate that L. aspera possess anti-inflammatory properties due to the strong occurrence of polyphenolic compounds such as alkaloids, flavonoids, tannins and steroids that serve as free radical inhibitors or scavenger. Compounds of the plant L. aspera may hence be used as lead compounds for designing potent anti-inflammatory drug which can be used for treatment of various diseases.</p><p> </p>

scholarly journals Synthesis, characterization and biological evaluation of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole.

2019 ◽  
Vol 9 (4-A) ◽  
pp. 220-228
Author(s):  
Piush Sharma ◽  
Charanjeet Singh
Keyword(s):  
Mannich Reaction ◽  
Mannich Bases ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Plate Method ◽  
Standard Drug ◽  
Excellent Activity ◽  
Anti Inflammatory

A series of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole were synthesized through the condensation reaction of 1,3,4-thiadiazole containing a aromatic secondary amine, aromatic aldehydes and cyclic compounds employing Mannich reaction and using conventional synthesis. All the synthesized compounds were obtained in the range of 57.41-83.3 % yield. The structures of synthesized compounds were confirmed by UV, IR, 1H NMR spectroscopy. the essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. The in vitro antibacterial activity of the synthesized compounds was determined, against two Gram-positive bacteria, viz. S. aureus & B. subtilis and Gram-negative, viz. E. coli and K. pneumoniae, by cup-plate method using the standard drug ciprofloxacin. Minimum inhibitory concentrations (MIC) changed in the range of 1.56_ _ 200 mg mL_1. Compound 3b exhibited excellent activity against both bacteria. The in vitro antifungal activity of the synthesized compound was also evaluated by cup-plate method against the fungi A. niger and C. albicans compared with the standard drug Fluconazole. Compound 4a, 8a exhibited excellent activity against both fungi. The result has shown that the compounds are quite active against pathogens under study and were nontoxic. The anti-inflammatory activity of the compound was evaluated, on albino rats, by carageenan induced rat paw oedema method using the standard drug diclofenac sodium. Compound 7b and 8c exhibited excellent anti-inflammatory and analgesic pharmacological activities. Structurally the compound 7b has a greater number of unsaturated hydrocarbons in schiff base, which shows good lipophilic properties within electron rich morpholine ring in Mannich base. Statistical significance of differences between group was determined by one-way analysis of variance (ANOVA). Among the synthesized compounds 3a, 4b, 5c, 7b, 8a and 8c were found be the most active. All the synthesized compounds were found to be low lethal as ascertained by LD50 test. Keywords: N- Mannich bases of heterocyclic 1,3,4-thiadiazole derivatives; Mannich reaction; antimicrobial agents; anti-inflammatory activity;

scholarly journals PHYTOCHEMICAL ANALYSIS AND SUPPRESSION OF INFLAMMATORY TARGETS BY ADATHODA VASICA

2018 ◽  
Vol 11 (5) ◽  
pp. 162
Author(s):  
Amala Reddy ◽  
Sujatha Sundaresan
Keyword(s):  
Methanolic Extract ◽  
Maximum Yield ◽  
Foot Ulcer ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Anti Inflammatory

 Objectives: A persistent and chronic inflammation may act as an underlying definition for many of the long-term illness such as diabetic foot ulcer, Alzheimer’s disease and rheumatoid arthritis. Folklore medicinal plants provide immense health benefits with new remedies. Active compounds from plants containing alkaloids and phenolic compounds (flavonoids and tannins) possess antioxidant and anti-inflammatory activity. The leaves of Adhatoda vasica are most known for its effectiveness in treating respiratory diseases such as asthma, chronic bronchitis, and other respiratory conditions. In this report, we investigated the possible action of A. vasica against inflammation.Methods: Solvents with varying polarity (Hexane, dichloromethane, ethyl acetate, and methanol) were used for the sequential extraction of leaves of A. vasica Linn (Family: Acanthaceae). The anti‐inflammatory activity was assessed using simple in vitro methods. Phenols, flavonoids, phytosterols, saponins, alkaloids, and tannins were analyzed qualitatively using standard protocols. Anti‐inflammatory activity was evaluated using albumin denaturation assay, membrane stabilization assay and proteinase inhibitory activity. Aspirin (diclofenac) was used as a standard drug for the study of anti-inflammatory activity.Results: Our results substantiated that methanolic extract of A. vasica gave a maximum yield of 12.5% and apparently all bioactive phytochemical constituents were at a higher concentration in the methanolic extract. Methanolic extract of A. vasica showed a significant inhibition of the heat-induced albumin denaturation, red blood cells membrane stabilization, and proteinase inhibitory effects with 86±1.46, 88±1.24, and 96±0.93% for 1000 μg/ml, respectively.Conclusion: The above results delineate that the bioactive components were extracted using high polar solvent are mostly flavonoids and related polyphenols. These compounds may be the active constituents to render the anti-inflammatory activity to A. vasica.

scholarly journals Evaluation of ex vivo Thrombolytic Activity and in vitro Anti-inflammatory Activity of Thespesia populnea Leaf Extract

2017 ◽  
Vol 9 (05) ◽  
Author(s):  
Vineela Satuluri ◽  
Vidyadhara Suryadevara ◽  
Vijetha Pendyala ◽  
Narasimhareddy M.
Keyword(s):  
Leaf Extract ◽  
Inflammatory Activity ◽  
Clot Lysis ◽  
Dependent Manner ◽  
Thrombolytic Activity ◽  
Standard Drug ◽  
Alcohol Extract ◽  
Thespesia Populnea ◽  
Anti Inflammatory

Thrombotic disorders like myocardial and cerebral infarction are fatal blood clotting related diseases. Synthetic therapeutics used in such disorders has serious adverse effects, so there is a need to investigate some more safe natural thrombolytic agents. Present study is a preliminary work towards such endeavors. During this study analysis of thrombolytic activity and anti-inflammatory activity of Thespesia populnea leaf extract using a simple and quick in vitro clot lysis assay was performed. Various concentrations of leaf extract i.e. 200μg/ml; 400μg/ml and 600μg/ml were tested at various time intervals including; 24, 48 and 72 hours duration of incubation at 37°C for observing maximum clot lysis. The result findings indicated that concentrations of leaf extract enhanced the percentage of clot lysis in dose dependent manner along with the incubation time factor. However; streptokinase SK a reference standard and water were used as a positive and negative control showed clot lysis maximum 96.35% and 35.22% in 72 hours of incubation respectively. Alcohol extract of whole plant of Thespesia populnea (Family: Malvaceae) was assessed for its anti-inflammatory activity by in vitro methods. In vitro anti-inflammatory activity was evaluated using albumin denaturation assay at different concentrations. Diclofenac sodium was used as standard drug. The results showed that Thespesia populnea alcohol extract at a concentration range of 400-1600μl significantly protects from protein denaturation.

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