ABSTRACT
The aims of the present investigation were to assess the antibacterial, antifungal, enzyme inhibition and hemolytic activities of various fractions of Rhynchosia pseudo-cajan Cambess. The methanolic extract of the plant was dissolved in the water (distilled) and then partitioned with the n-hexane, chloroform, EtOAc and n-BuOH sequentially. Antibacterial activity was checked against Escherichia coli, Pasturella multocida, Bacillus subtilis and Staphylococcus aureus by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform and ethyl acetate soluble fractions showed good activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. These fractions also showed good MIC values. The n-butanol soluble and remaining aqueous fraction also showed good activity against some strains. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Chloroform, n-butanol and ethyl acetate soluble fraction showed good activity only against G. lucidum. Enzyme inhibition studies were done against four enzymes i.e. α-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Aqueous fraction possessed very good activity against α-glucosidase, even greater than acarbose, a reference standard drug. Its IC50 value was found as 29.81±0.12 µg/ml as compared to acarbose having IC50 38.62±0.04 µg/ml. Chlroform and ethyl acetate soluble fractions also showed good activity against α-glucosidase. Ethyl acetate soluble and remaining aqueous fractions showed good activity against lipoxygenase. All the studied fractions showed very less toxicity i.e. <2.5%.
Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Fabaceae/chemistry , Hemolysis/drug effects , Hemolytic Agents/pharmacology , Plant Extracts/pharmacology , 1-Butanol/chemistry , Bacteria/drug effects , Chloroform/chemistry , Disk Diffusion Antimicrobial Tests/methods , Fungi/drug effects , Hexanes/chemistry , Microbial Sensitivity Tests/methods , Phytotherapy/methodsABSTRACT
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.
Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Urease/antagonists & inhibitors , Anti-Bacterial Agents/chemical synthesis , Drug Evaluation, Preclinical , Enzyme Inhibitors/chemical synthesis , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Structure , Oxadiazoles/chemistry , Piperidines/chemistry , Spectrophotometry, Infrared , Sulfonamides/chemistryABSTRACT
The purpose of the research work was to examine the in vitro antioxidant activity of the different aqueous and organic fractions of Lonicera quinquelocularis Hardwicke. The methanol extract was dissolved in distilled water and fractioned with n-hexane, chloroform, ethyl acetate and n-butanol, successively. The antioxidant potential of the remaining aqueous and organic fractions was determined by using 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity, total antioxidant activity, ferric reducing antioxidant power (FRAP) assay, ferric thiocyanate assay and total phenolics method. Among these fractions ethyl acetate fraction displayed the maximum antioxidant activity with IC50 of (11.13±0.12µg/ml). It also exhibited the highest total antioxidant activity (0.595±0.00), FRAP value (128.2±4.54µg/mL) and total phenolic contents (66.89±7.73µg/g) as compared to other organic fractions. Phytochemical investigation of the above mentioned fractions showed the presence of flavanoids, phenolics, terpenoids, sugars, alkaloids, tannins, saponins and cardiac glycosides in appreciable amounts, which have major contribution towards antioxidant activity.
Subject(s)
Antioxidants/pharmacology , Lonicera/chemistry , Phytochemicals/analysis , Plant Extracts/pharmacology , 1-Butanol/chemistry , Acetates/chemistry , Chloroform/chemistry , Hexanes/chemistryABSTRACT
The purpose of the present investigation was to assess the enzyme inhibition, antifungal, antibacterial and hemolytic activities of various fractions of Colebrookia oppositifolia Smith. The MeOH extract of plant was dissolved in dist. water and partitioned with n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Enzyme inhibition studies were done against four enzymes i.e. α-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Ethyl acetate fraction possessed very good activity against α-glucosidase (IC50 57.38±1.23µg/mL). CHCl3 fraction displayed good activity against α-glucosidase and lipoxygenase while moderate activity against butyryl cholinesterase. EtOAc fraction displayed good activity against lipoxygenase. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Aqueous fraction displayed good activity against G. lucidum and A. flavus. Antibacterial activity was checked against Staphylococcus aureus, Bacillus subtilis, Pasturella multocida and Escherichia coli by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform, ethyl acetate and aqueous fraction showed good activity against E. coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%.
Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Enzyme Inhibitors/pharmacology , Hemolysis/drug effects , Lamiaceae/chemistry , Solvents/chemistry , Acetylcholinesterase/metabolism , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/toxicity , Antifungal Agents/isolation & purification , Antifungal Agents/toxicity , Bacteria/drug effects , Bacteria/growth & development , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/isolation & purification , Cholinesterase Inhibitors/pharmacology , Disk Diffusion Antimicrobial Tests , Enzyme Inhibitors/isolation & purification , Enzyme Inhibitors/toxicity , Fungi/drug effects , Fungi/growth & development , Glycoside Hydrolase Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/pharmacology , Humans , Lamiaceae/toxicity , Lipoxygenase Inhibitors/isolation & purification , Lipoxygenase Inhibitors/pharmacology , Phytotherapy , Plants, MedicinalABSTRACT
Pyrus pashia Buch. & Ham. was subjected to extraction with methanol. Methanolic extracts of fruit, bark and leaf were partitioned separately with four organic solvents in order of increasing polarity, asn-hexane, chloroform, ethyl acetate and n-butanol after dissolving in distilled water. Phytochemical screening revealed the presence of phenolics, flavonoides, alkaloids and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol soluble fractions. The antioxidant activity of crude methanolic extracts, all the obtained fourorganic fractions and remaining aqueous fractions was evaluated by different methods such as: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, ferric reducing antioxidant power (FRAP) assay and total antioxidant activity by phosphomolybdenum complex method as well as determination of total phenolics. The results of antioxidant activity exhibited that chloroform soluble fraction of fruit showed the highest value of percent inhibition of DPPH (48.16 ± 0.21 µg/ml) at the concentration of 10 µg/ml. Ethyl acetate soluble fraction displayed the lowest antioxidant activity having IC50 value of bark as (8.64 ± 0.32 µg/ml) relative to butylated hydroxytoluene (BHT), having IC50 of 12.1 ± 0.92 µg/ml. The ethyl acetate soluble fraction of bark revealed the highest FRAPs value (174.618 ± 0.11TE µM/ml) among all the three parts. This fraction also showed the highest value of total antioxidant activity as (1.499 ± 0.90), determined by phosphomolybdenum complex method. Moreover, this fraction also conferred the highest phenolic content (393.19 ± 0.72) as compared to other studied fractions of fruit and leaf.