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1.
Pak J Pharm Sci ; 37(1): 163-171, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38741413

RESUMO

Medicinal plants contain a wide variety of bioactive phytoconstituents which can serve as new therapeutic agents for several diseases. This study examines the antidiabetic potential of Aitchisonia rosea in alloxan-induced diabetic rats and identifies its bioactive phytoconstituents using GC-MS. In vitro, antidiabetic potential was established using the α-amylase inhibition assay. In vivo, antidiabetic potential was investigated by employing the oral glucose tolerance test (OGTT). GC-MS analysis was used to identify the bioactive phytoconstituents. The in vitro and in vivo tests showed that the aqueous extract of A. rosea possesses better antidiabetic potential. The α-amylase inhibition assay highlighted an IC50 value of 134.87µg/ml. In an oral glucose tolerance test, rats given an aqueous A. rosea extract significantly lowered their blood sugar levels significant reduction in the blood glucose concentration was observed in the oral glucose tolerance test in rats treated with the aqueous A. rosea extract. GC-MS investigation revealed many phytoconstituents, with serverogenin acetate and cycloheptasiloxane tetradecamethyl being important antidiabetic agents. This study found anti-diabetic properties in A. rosea extract. The phytochemical and GC-MS investigation also found serverogenin acetate and cycloheptasiloxane tetradecamethyl, which could be used to develop new antidiabetic drugs.


Assuntos
Glicemia , Diabetes Mellitus Experimental , Cromatografia Gasosa-Espectrometria de Massas , Hipoglicemiantes , Componentes Aéreos da Planta , Extratos Vegetais , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Componentes Aéreos da Planta/química , Masculino , Glicemia/efeitos dos fármacos , Ratos , Teste de Tolerância a Glucose , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Ratos Wistar , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Aloxano
2.
Microb Pathog ; 183: 106280, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37541555

RESUMO

Antibiotic resistant bacteria are immune to most antibiotics and are therefore very difficult to treat and in most cases lead to death. As such there is a pressing need for alternative and more efficient antibacterial drugs which can target these drug-resistant strains as well. The objective of this research work was to investigate the antibacterial properties of Thymus linearis essential oil (EO) against multiple disease-causing bacterial pathogens. Additionally, the study aimed to examine the molecular docking and molecular dynamic (MD) simulations of the primary components of the EO with the essential bacterial proteins and enzymes. Gas chromatography-mass spectrometry was employed to analyse the chemical composition of Thymus linearis EO. The initial screening for antibacterial properties involved the use of disc diffusion and microdilution techniques. Molecular docking studies were conducted utilising Autodock Vina. The outcomes were subsequently visualised through BIOVIA Discovery Studio. MD simulations were conducted using iMODS, an internet-based platform designed for MD simulations. The essential oil (EO) was found to contain 26 components, with thymol, carvacrol, p-cymene, and γ-terpinene being the primary constituents. The study findings revealed that Thymus linearis EO demonstrated antibacterial effects that were dependent on both the dose and time. The results of molecular docking studies revealed that the primary constituents of the EO, namely thymol, carvacrol, and p-cymene, exhibited robust interactions with the active site of the bacterial DNA gyrase enzyme. This finding provides an explanation for the antibacterial mechanism of the EO. The results indicate that Thymus linearis EO possesses potent antibacterial properties against the MDR microorganisms. Molecular docking analyses revealed that the essential oil's primary components interact with the amino acid residues of the DNA-Gyrase B enzyme, resulting in a favourable docking score.


Assuntos
Óleos Voláteis , Thymus (Planta) , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Timol , Simulação de Acoplamento Molecular , DNA Girase , Novobiocina , Antibacterianos/farmacologia
3.
Molecules ; 28(8)2023 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-37110767

RESUMO

Many plants of the Berberis genus have been reported pharmacologically to possess anti-diabetic potential, and Berberis calliobotrys has been found to be an inhibitor of α-glucosidase, α-amylase and tyrosinase. Thus, this study investigated the hypoglycemic effects of Berberis calliobotrys methanol extract/fractions using in vitro and In vivo methods. Bovine serum albumin (BSA), BSA-methylglyoxal and BSA-glucose methods were used to assess anti-glycation activity in vitro, while in vivo hypoglycemic effects were determined by oral glucose tolerance test (OGTT). Moreover, the hypolipidemic and nephroprotective effects were studied and phenolics were detected using high performance liquid chromatography (HPLC). In vitro anti-glycation showed a significant reduction in glycated end-products formation at 1, 0.25 and 0.5 mg/mL. In vivo hypoglycemic effects were tested at 200, 400 and 600 mg/kg by measuring blood glucose, insulin, hemoglobin (Hb) and HbA1c. The synergistic effect of extract/fractions (600 mg/kg) with insulin exhibited a pronounced glucose reduction in alloxan diabetic rats. The oral glucose tolerance test (OGTT) demonstrated a decline in glucose concentration. Moreover, extract/fractions (600 mg/kg) exhibited an improved lipid profile, increased Hb, HbA1c levels and body weight for 30 days. Furthermore, diabetic animals significantly exhibited an upsurge in total protein, albumin and globulin levels, along with a significant improvement in urea and creatinine after extract/fractions administration for 42 days. Phytochemistry revealed alkaloids, tannins, glycosides, flavonoids, phenols, terpenoids and saponins. HPLC showed the presence of phenolics in ethyl acetate fraction that could be accountable for pharmacological actions. Therefore, it can be concluded that Berberis calliobotrys possesses strong hypoglycemic, hypolipidemic and nephroprotective effects, and could be a potential therapeutic agent for diabetes treatment.


Assuntos
Berberis , Diabetes Mellitus Experimental , Ratos , Animais , Hipoglicemiantes/química , Aloxano , Berberis/metabolismo , Hemoglobinas Glicadas , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Extratos Vegetais/química , Glicemia , Glucose/efeitos adversos , Insulina , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico
4.
Microb Pathog ; 173(Pt A): 105854, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36374855

RESUMO

The commercially used synthetic pesticides have been proven to be toxic not only to humans and other animals, but also to non-target plant, the surrounding organisms around the plant, and the environment. There are also increased concerns regarding the development of pest resistance towards these synthetic pesticides. As such, biopesticides, which are defined as the certain kinds of pesticides derived from natural sources such as plants, bacteria, fungi, animals and some minerals, are potential alternative pesticides and are gaining increasing attention. Biopesticides are safer and eco-friendly pesticides used for pest management. Among these, plant-based biopesticides constitute a small but important group of biopesticides. Plant based extracts and essential oils have been particularly used in the management of insects exhibiting a variety of anti-insecticidal mechanisms. Their chemical compositions are very complex and as such acquiring resistance by the pest against such biopesticide is very difficult. As far as their mechanism of action is concerned, these can act as insect repellants, insect attractants, or anti-feedants. They can also inhibit respiration or they can obstruct the host plant identification. These insecticides can inhibit oviposition and decrease adult emergence by ovicidal and larvicidal effects. Some of the essential oil based insecticides have even been commercialized for use. However, there are some limitations that restrict the widespread use of such biopesticides. These limitations include cost, difficulties in production, gentle action, and dearth of appropriate biopesticide formulations. As far as their regulations are concerned, it is still a problem in many countries further halting biopesticide use. But one thing is clear that biopesticides do have a promising future due to their eco-friendly nature and unique chemical compositions and unique mode of action.


Assuntos
Produtos Biológicos , Inseticidas , Óleos Voláteis , Praguicidas , Animais , Humanos , Agentes de Controle Biológico/farmacologia , Praguicidas/farmacologia , Inseticidas/farmacologia , Produtos Biológicos/farmacologia , Produtos Biológicos/química , Controle Biológico de Vetores , Óleos Voláteis/farmacologia
5.
Microb Pathog ; 166: 105540, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35430270

RESUMO

The essential oil composition of the shoot parts of Prangos pabularia, growing in Drass area of Ladakh, India, along with its antioxidant, antibacterial and anticancer activity, is reported for the first time. Gas chromatography coupled with mass spectrometry (GC-MS) revealed the presence of 31 constituents, representing 97.342% of the total essential oil. The major constituents of essential oil were Durylaldehyde (62.161%), Bicyclo [3.1.1] hept-2-en-4-ol (8.846%), Chrysanthenyl acetate (5.120%) followed by unknown (3.420%), (-)-Spathulenol (3.028%), Mesityl aldehyde (2.402%) and Hexahydro farnesyl acetone (1.683%. Cytotoxic activity of the essential oil by MTT assay against human breast adenocarcinoma (MCF7), human breast (HBL-100), human cervical cancer (HELA) and human lung adenocarcinoma epithelial (A549) cells, at four different concentrations (20, 30, 50 & 100 µg/mL) revealed that the activity of 56.12% against A549 (human lung) cell line at 20 µg/mL concentration was the highest. The Essential oil displayed a significant free radical scavenging activity with DPPH. Antibacterial activity was carried out against 3 g positive and 2-g negative bacteria at four different concentrations using Agar Well Diffusion Method taking streptomycin sulphate as reference. The essential oil displayed significant and broad-spectrum antibacterial activity against different bacteria used. The MIC of the oil ranged from 2.06 to 5.00 µg/mL. The zones of inhibition were lesser for Micrococcus and Escherichia coli compared to other strains of bacteria.


Assuntos
Óleos Voláteis , Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Bactérias , Escherichia coli , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Voláteis/farmacologia
6.
Pak J Pharm Sci ; 35(2): 465-471, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35642401

RESUMO

We investigated the protective effect of fractions and essential oil from Berberis calliobotrys on H2O2 induced oxidative damage on pBR322 DNA. The crude plant material was extracted using 90% methanolic and liquid-liquid fractionation was accomplished. The essential oil analysis was performed using GC/MS. The FRAP and DPPH assays were performed to determine antioxidant activity. The DNA protection assay was performed using plasmid pBR 322 DNA. The essential oil analysis indicated presence of germacrene D (9.26%), stearic acid (7.50%), methyl tetradecanoate (6.36%) α-thujene (5.71%) and α-muurolol (5.30%) methyl eugenol (5.17%). In vitro analysis showed significant antioxidant activity of all tested extracts and essential oil. The extract showed significant effects at (1000 µg/mL) on pBR322 DNA. Finally it was concluded that Berberis calliobotrys possesses signifgant protective on effects pBR322 DNA and RBC cellular membrane.


Assuntos
Berberis , Óleos Voláteis , Antioxidantes/química , DNA , Peróxido de Hidrogênio/toxicidade , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Estresse Oxidativo , Extratos Vegetais/química , Extratos Vegetais/farmacologia
7.
Pak J Pharm Sci ; 34(1(Special)): 441-446, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34275792

RESUMO

A series of new derivatives of 4-(2-chloroethyl)morpholine hydrochloride (5) were efficiently synthesized. Briefly, different aromatic organic acids (1a-f) were refluxed to acquire respective esters (2a-f) using conc. H2SO4 as catalyst. The esters were subjected to nucleophillic substitution by monohydrated hydrazine to acquire hydrazides (3a-f). The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Finally, the derivatives, 6a-f, were prepared by reacting oxadiazoles (4a-f) with 5 using NaH as activator. Structures of all the derivatives were elucidated through 1D-NMR EI-MS and IR spectral data. All these molecules were subjected to antibacterial and hemolytic activities and showed good antibacterial and hemolytic potential relative to the reference standards.


Assuntos
Antibacterianos/química , Hemolíticos/química , Morfolinas/química , Oxidiazóis/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Hemolíticos/síntese química , Hemolíticos/farmacologia , Klebsiella pneumoniae/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Morfolinas/síntese química , Morfolinas/farmacologia , Oxidiazóis/síntese química , Oxidiazóis/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Salmonella typhi/efeitos dos fármacos , Espectrofotometria Infravermelho , Staphylococcus aureus/efeitos dos fármacos
8.
Pak J Pharm Sci ; 33(4): 1697-1705, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33583804

RESUMO

A series of propanamide compounds 6a-l was derived by N-substitution reactions, encompassing tosyl, piperidine and 1,3,4-oxadiazole moieties. The intended array of compounds 6a-l was afforded by a series of five steps reaction scheme. 1-Tosylpiperidin-4-carboxylate (1) was synthesized by the reaction of tosyl chloride (a) with ethyl isonipecotate (b) under mild basic conditions. Compound 1 was subjected to nucleophillic substitution by hydrazine to synthesize 1-tosylpiperidin-4-carbohydrazide (2). The compound, 5-(1-tosylpiperidin-4-yl)-1,3,4-oxadiazole-2-thiol (3) was synthesized by intermolecular cyclization of compound 2 by CS2 under strong basic conditions. The target compounds, 6a-l, were finally synthesized from 3 by reacting with different electrophiles, 5a-l, in an aprotic polar solvent with sodium hydride as an activator. The different propanamoyl electrophiles, 5a-l, were synthesized by the reaction of different aromatic and aliphatic amines, 4a-l, with 3-bromopropionyl chloride under mild basic conditions. The structural elucidation was carried out using modern spectroscopic techniques including IR, 1H-NMR and EI-MS. The antibacterial potential of synthesized compounds was assessed against five bacterial strains. Compounds 6a, 6c, 6d, 6e and 6f were found to be potent antibacterial agents.


Assuntos
Antibacterianos/síntese química , Oxidiazóis/química , Piperidinas/química , Compostos de Tosil/química , Hidrazinas/química , Testes de Sensibilidade Microbiana
9.
Pak J Pharm Sci ; 33(2(Supplementary)): 871-876, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32863264

RESUMO

A novel series of 5-(3-Chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives was efficiently synthesized and screened for antibacterial, hemolytic and thrombolytic activities. The molecule 7c remained the best inhibitor of all selected bacterial strains and furthermore possessed very low toxicity, 8.52±0.31. Compound 7a 7b and 7f showed very good thrombolytic activity relative to Streptokinase employed as reference drug. In addition to low toxicity and moderately good thrombolytic activity, the synthesized compounds possessed excellent to moderate antibacterial activity, relative to ciprofloxacin. All compounds especially 7b and 7f can be consider for further clinical studies and might be helpful in synthesis of new drugs for treatment of cardiovascular diseases.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Fibrinolíticos/química , Fibrinolíticos/farmacologia , Hemólise/efeitos dos fármacos , Oxidiazóis/química , Oxidiazóis/farmacologia , Bactérias/efeitos dos fármacos , Ciprofloxacina/farmacologia , Testes de Sensibilidade Microbiana/métodos
10.
Pak J Pharm Sci ; 33(1): 149-160, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32122843

RESUMO

A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10 % potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. 1H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization.


Assuntos
Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Inibidores da Colinesterase/farmacologia , Simulação de Acoplamento Molecular , Albumina Sérica/metabolismo , Triazóis/farmacologia , Antibacterianos/síntese química , Anti-Inflamatórios/síntese química , Inibidores da Colinesterase/síntese química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Piperidinas/química , Relação Estrutura-Atividade , Triazóis/síntese química , Triazóis/química
11.
Pak J Pharm Sci ; 32(3): 987-996, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31278711

RESUMO

Heterocyclic chemistry is an important field of organic chemistry due to therapeutic potential. The minor modification in the structure of poly-functional compounds has great effect on therapeutic ability. In the presented research work, substituted 1,3,4-oxadiazole derivatives, 8a-p, have been synthesized by the reaction of 1-(4-bromomethylbenzenesulfonyl)-3-methylpiperidine (7) and 5-substituted-1,3,4-oxadiazole-2-thiol (4a-p). The 5-substituted-1,3,4-oxadiazole-2-thiol were synthesized by converting carboxylic acids correspondingly into esters, hydrazides and oxadiazoles. Secondly the electrophile, 1-(4-Bromomethylbenzenesulfonyl)-3-methylpiperidine (7), was prepared by the reaction of 3-methylpiperidine with 4-bromomethylbenzenesulfonyl chloride in the presence of water and Na2CO3 under pH of 9-10. The compounds were structurally corroborated through spectroscopic data analysis of IR, EI-MS and 1H-NMR. The screening for antibacterial activity revealed the compounds to be moderate to excellent inhibitors against bacteria under study. Anti-enzymatic activity was assessed against urease enzyme and 1-{[4-({[5-(3-nitrophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}methyl)phenyl]sulfonyl}-3-methylpiperidine (8d) was the most active one.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Urease/antagonistas & inibidores , Antibacterianos/síntese química , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/síntese química , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oxidiazóis/química , Piperidinas/química , Espectrofotometria Infravermelho , Sulfonamidas/química
12.
Pak J Pharm Sci ; 32(2 (Supplementary)): 759-764, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31103968

RESUMO

Present work was conducted to improve the bioavailability of Tizanidine HCl (TZN) by formulating mucoadhesive buccal films (MBFs) using novel thiolated arabinoxylan (TAX) as film former. MBF's were prepared by solvent casting technique followed by their evaluation for surface morphology and folding endurance. Moreover, pharmacokinetic parameters including Cmax, tmax, t1/2 and AUC were determined after administering standard oral solution (SOS) and MBFs of TZN at a dose of 1mg/kg. Successful thiolation was confirmed by the presence of 4.98 to 7.04 mmol of thiol content per gram of the polymer. Results of in-vivo pharmacokinetics have signified (p=0.0089) the suitability of MBFs as a carrier of drug through buccal route. Results have explored that, t1/2 was increased from 2.51hrs (SOS) to 10 hrs, Cmax from 42.3 ng/ml (SOS) to 105ng/ml and tmax from 2hrs (SOS) to 6h. Conclusively, TAX has exhibited the potential to form MBFs thereby offering sustained release of TZN with improved pharmacokinetic profile.


Assuntos
Clonidina/análogos & derivados , Portadores de Fármacos/química , Administração Bucal , Animais , Disponibilidade Biológica , Clonidina/administração & dosagem , Clonidina/sangue , Clonidina/farmacocinética , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Polímeros/síntese química , Coelhos , Compostos de Sulfidrila/química , Xilanos/química
13.
Pak J Pharm Sci ; 32(6): 2651-2658, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31969298

RESUMO

A series of 1, 2, 4-triazole derivatives bearing piperidine moiety has been introduced as new anti-diabetic drug candidates with least cytotoxicity. p-Chlorophenylsulfonyl chloride (1) and ethyl nipecotate (2) were the starting reagents that resulted into corresponding 3,4,5-trisubstituted-1,2,4-triazole (6) through a series of steps. A series of electrophiles, 9a-e, were synthesized by reacting 4-bromobutyryl chloride (7) with differently substituted aromatic amines (8a-e) under basic aqueous medium. Target derivatives, 10a-e, were synthesized by the reaction of compound 6 with N-aryl-4-bromobutanamides (9a-e) in an aprotic solvent. Structures of all the derivatives were verified by spectroscopic analysis using IR, 1H-NMR, 13C-NMR and EIMS. Most of the derivatives revealed moderate to good α-glucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity.


Assuntos
Inibidores de Glicosídeo Hidrolases/síntese química , Triazóis/síntese química , Animais , Bovinos , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Hemolíticos/síntese química , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Triazóis/química , Triazóis/farmacologia , alfa-Glucosidases/efeitos dos fármacos
14.
Pak J Pharm Sci ; 31(5): 1783-1790, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150171

RESUMO

A number of novel 5-substituted-2-((6-bromo-3,4-methylenedioxybenzyl)thio)-1,3,4-Oxadiazole derivatives (6a-l) have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids (1a-l) as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-l) were yielded in good amounts. The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride (5) in DMF to synthesize the required compounds. All the synthesized molecules were well characterized by IR, 1H-NMR, 13C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential.


Assuntos
Antibacterianos/análise , Antibacterianos/síntese química , Oxidiazóis/análise , Oxidiazóis/síntese química , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/crescimento & desenvolvimento , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Humanos , Testes de Sensibilidade Microbiana/métodos , Oxidiazóis/farmacologia
15.
Acta Pol Pharm ; 74(1): 173-178, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29474773

RESUMO

Pistacia khinjuk is one of the fifteen known species of Pistacia belonging to Anacardiaceae family. Keeping in view the possible therapeutic utility of this genus and the lack of literature on this plant, this study involves phytochemical investigation of P. khinjuk and its antioxidant activity. The phytochemical investigation was conducted on crude methanolic extract and its fractions namely, n-hexane, chloroform, n-butanol, ethyl acetate and aqueous. Total phenolic contents and flavonoids were also determined by phosphomolybdenum and ferric thiocyanate method in crude extract and its fractions. The results of phytochemical investigation indicated the presence of alkaloids, tannins, flavonoids, saponins, triterpenoids, cardiac glycosides, carbohydrates, proteins and sterols in the crude extract of P. khinjuk. Crude extract and its fractions exhibited remarkable antioxidant activity. This study showed that the crude extract and its fractions have potent antioxidant activity, among all ethyl acetate showed 1.109 ± 0.029 the highest activity. This research concluded that crude extract of P. khinjuk and its fractions contained phenolic and flavonoid compounds that show significant antioxidant activity.


Assuntos
Antioxidantes/farmacologia , Pistacia/química , Extratos Vegetais/farmacologia , Flavonoides/análise , Fenóis/análise , Compostos Fitoquímicos/análise , Extratos Vegetais/análise
16.
Pak J Pharm Sci ; 29(4): 1307-15, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27393454

RESUMO

The biological potential of N'-substituted-2-(5-(3-chlorophenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide (8a-p) has been evaluated against bacterial strains of Gram-negative and Gram-positive bacteria. The multistep synthesis involved the conversion of 3-chlorobenzoic acid (1) to ethyl 3-chlorobenzoate (2), 3-chlorobenzohydrazide (3), 5-(3-chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4), ethyl 2-(5-(3-chlorophenyl)-1,3,4-Oxadiazol-2-ylthio) acetate (5) and 2-(5-(3-chlorophenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide (6). The last step involved the reaction of 6 and aryl aldehydes, 7a-p, in methanol to synthesize the Schiff bases, 8a-p, with better yields. The structures of all the molecules were corroborated by spectral analysis. The Schiff bases were further evaluated for the antibacterial activity and found to be moderately good inhibitors of bacterial strains of Gram-bacteria.


Assuntos
Antibacterianos/síntese química , Hidrazinas/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Hidrazinas/química , Hidrazinas/farmacologia
17.
Pak J Pharm Sci ; 29(6): 2109-2117, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28375133

RESUMO

The various p-substituted benzenesulfonyl chlorides (2a-e) were treated with (3,4-methylenedioxy) benzylamine (1) in the presence of aqueous Na2CO3 solution to synthesize N-(3,4-methylenedioxybenzyl)-4-substitutedbenzenesulfonamides (3a-e). The synthesized molecules were further converted into corresponding N-ethyl/benzyl/4-flourobenzyl-N-(3,4-methylenedioxybenzyl)-4-substitutedbenzenesulfonamides (7a-e, 8a-e, 9a-e) on reaction with ethyl iodide (4), benzyl chloride (5) and 4-flourobenzyl chloride (6) in the presence of sodium hydride using N,N-dimethylformamide as solvent. The structure elucidation was processed through different spectral techniques including IR, 1H-NMR and EIMS. The screening of the synthesized molecules against Gram-bacterial strains, to evaluate antibacterial activity, showed them moderately good inhibitors as shown by their low MIC values.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Sulfonamidas/síntese química , Sulfonamidas/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , Benzenossulfonamidas
18.
Pak J Pharm Sci ; 29(1): 27-34, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26826837

RESUMO

The most emerging class among the heterocyclic compounds is 1,3,4-oxadiazoles for their diverse biological activities. In the present research work, piperonylic acid (1) was converted consecutively into corresponding ester (2), hydrazide (3) and 1,3,4-oxadiazole (4) through intermolecular cyclization. The synthesized compound 4 was subjected further to S-alkylation/aralkylation, using alkyl/aralkyl halides (5a-m) and S-substituted-1,3,4-oxadiazole derivatives were synthesized (6a-m). The structure elucidation of the synthesized molecules was processed through (1)H-NMR, IR and mass spectral data. The antibacterial activity showed these molecules moderately good inhibitors of gram-negative and gram-positive bacteria.


Assuntos
Antibacterianos/síntese química , Oxidiazóis/síntese química , Antibacterianos/farmacologia , Oxidiazóis/farmacologia , Relação Estrutura-Atividade
19.
Acta Pol Pharm ; 71(3): 415-21, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25265821

RESUMO

Current study was conducted to investigate antimicrobial activity of fruit extracts of two Solanaceous plants (Solanum nigrum and Solanum xanthocarpum) found in Pakistan. Petroleum ether, chloroform, dichloromethane, ethyl acetate, acetone, methanol and water were utilized for extraction. The highest percentages of polar components of both the species were extracted by water; little amount of non-polar components by petroleum ether while very low quantities by other solvents. Antimicrobial activities were estimated by measuring zones of inhibition through hole-plate diffusion method, against three species of Gram positive bacteria, five species of Gram negative bacteria and three species of fungi selected for this study. Doses of 5, 10 and 15 mg/mL prepared through methanolic extracts of each plant's powdered fruit material displayed significant zones of inhibition against all three Gram positive bacteria, three of the Gram negative bacteria out of five and against all three fungi. Although these doses exhibited significant zones of inhibition but they are not as potent as standards: ampicillin or amphotericin B. The present study assures the possible potential of antimicrobial as well as antifungal activity of fruit extracts of these plants.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Extratos Vegetais/farmacologia , Solanum nigrum , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Relação Dose-Resposta a Droga , Frutas , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Metanol/química , Fitoterapia , Plantas Medicinais , Solventes/química
20.
Acta Pol Pharm ; 71(4): 667-75, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25272893

RESUMO

Berberis orhob, otrvs Bien. ex Aitch. (B.o.) has been reported to have antihypertensive effect in different experimental models. The aim of present study was to evaluate the possible antihypertensive mechanism. Aqueous methanolic extract of B.o. roots and its various fractions namely (ethyl acetate, n-butanol or aqueous) in different concentrations (10 ng/mL, 100 ng/mL, I pg/mL, 10 pg/mL, 100 pg/mL ) were evaluated in isolated perfused rabbit heart to assess their effect on force of contraction, HR and perfusion pressure. The crude extract of B.o. and its fractions exhibited a significant decrease in heart rate, contractility and perfusion pressure of isolated rabbit heart, however, butanolic fraction produced more prominent effect and was selected for further study. The effects of butanol fraction were not blocked by atropine (10' M) in isolated perfused heart. However, butanol fraction significantly blocked the effects of adrenaline (10' M). It is therefore conceivable that cardiac depressant activity of B.o. butanol fraction might be due to the presence of certain 3-blocking agents which might be responsible for antihypertensive effect However, further experiments are required to isolate the active compound(s) and elucidate exact mechanism of action.


Assuntos
Berberis , Coração/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Depressão Química , Epinefrina/farmacologia , Feminino , Frequência Cardíaca/efeitos dos fármacos , Técnicas In Vitro , Masculino , Contração Miocárdica/efeitos dos fármacos , Coelhos
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