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1.
Pakistan Journal of Pharmaceutical Sciences. 2018; 31 (6): 2497-2501
in English | IMEMR | ID: emr-205093

ABSTRACT

The fruit-vegetable Lagenaria siceraria is well known for its ethnomedicinal applications. While other parts of the plant have been studied for their medicinal properties, its fruit pedicles have not been yet explored. The present study therefore aimed to investigate their phenolics, flavonoids, antioxidant potential and alpha-amylase inhibitory properties. The bioactivities of this neglected part of the fruit were promising. Ethyl acetate fraction had the highest total phenolic content [TPC], 4.4micro g/mL Gallic acid equivalent [GAE]. The TPC of chloroform and n-butanolic fractions were 3.6 and 2.5 GAE, respectively. Chloroform fraction displayed the highest total flavonoid content [TFC, 295micro g/mL Rutin equivalent]. The trend of TFC among the fractions was chloroform > hexane > ethyl acetate > n-butanolic > aqueous. Ethyl acetate fraction was most potent as a DPPH radical scavenger, and showed notable activity even at very low concentration [IC50 2.65mg/mL]. It was more potent than ascorbic acid [IC50 4.9mg/mL], the standard used in the study. The methanolic extract itself was more powerful than ascorbic acid. The residual aqueous fraction was the strongest inhibitor of alpha-amylase with IC50 1.35mg/mL, which was comparable to the antidiabetic drug Acarbose [IC50 1.26 mg/mL]. The IC50 [mg/mL] of ethyl acetate, hexane and n-butanolic fractions were 2.16,2.05 and 2.44, respectively. The findings indicated that the pedicles of L. siceraria fruits have remarkable antioxidant and alpha-amylase inhibitory potential. Subject to verification by in vivo analysis and clinical trial, consumption of the pedicles of this fruit may be advised to diabetic people. As the aqueous fraction was the most potent inhibitor, a water decoction of the fruit part may safely be recommended for the purpose

2.
Asian Pacific Journal of Tropical Medicine ; (12): 305-310, 2017.
Article in Chinese | WPRIM | ID: wpr-972658

ABSTRACT

Objective To explore pancreatic lipase inhibitory activity under different extraction conditions in order to track the most potent extract. Methods The methanolic extract and its fractions in solvents of increasing polarity, ether, chloroform, ethyl acetate, n-butanol and water, were made through cold maceration. Extracts in ethanol, ethyl acetate, acetone and chloroform were similarly prepared. Aqueous extract was prepared through hot decoction method. A reported method was used to determine lipase inhibitory activity of extracts and fractions over wide ranges of concentrations. Results The extracts and fractions exhibited concentration dependent activity. The IC

3.
Asian Pacific Journal of Tropical Medicine ; (12): 305-310, 2017.
Article in English | WPRIM | ID: wpr-820735

ABSTRACT

OBJECTIVE@#To explore pancreatic lipase inhibitory activity under different extraction conditions in order to track the most potent extract.@*METHODS@#The methanolic extract and its fractions in solvents of increasing polarity, ether, chloroform, ethyl acetate, n-butanol and water, were made through cold maceration. Extracts in ethanol, ethyl acetate, acetone and chloroform were similarly prepared. Aqueous extract was prepared through hot decoction method. A reported method was used to determine lipase inhibitory activity of extracts and fractions over wide ranges of concentrations.@*RESULTS@#The extracts and fractions exhibited concentration dependent activity. The IC (μg/mL) values of methanolic, ethanolic, chloroform, ethyl acetate, acetone, ethyl acetate (after washing with water) and aqueous decoction were 293.40, 266.47, 157.59, 182.12, 352.34, 257.00, and 190.00, respectively. The activity of chloroform, ethyl acetate and aqueous extracts were close to that of the drug orlistat (IC 146 μg/mL). Out of the fractions of the methanolic extract, the chloroform fraction was most active (IC 189.6 μg/mL). The order of inhibitory activity of the fractions was as follows: chloroform>ether>n-butanolic>aqueous>ethyl acetate. The GC/MS analysis of the most active chloroform faction showed the presence of hexadecanoic acid, methyl hexadecanoate, isopropyl palmitate, methyl 9,12-octadecadienate, and methyl 9,12,15-octadecatrienoate.@*CONCLUSIONS@#The study suggests that Lagenaria siceraria has potential to inhibit pancreatic lipase activity, suppressing lipid digestion and thereby diminishing entry of lipids into the body. Regular intake of aqueous decoction of the fruit may therefore be recommended for control of obesity. Fatty acids and their esters may play role as inhibitors of lipase.

4.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (3): 705-712
in English | IMEMR | ID: emr-186464

ABSTRACT

The present study aimed to explore antioxidant, antimicrobial and anti-diabetic properties of the fern Adiantum venustum. The TPC [total phenolic content] of methanolic extract of the plant was 247.95+/-0.0007micro g of Gallic acid equivalents per gram of dried extract [mg GAE/g]. The highest TPC was in n-butanolic fraction, which was 981.45+/-0.1562mg GAE/g. Hexane fraction showed lowest TPC [256.95+/-0.0420mg GAE/g]. Ethyl acetate fraction exhibited highest total flavonoid content [TFC], i.e., 62.0+/-0.050mg of Rutin equivalents per gram of sample. DPPH [1,1- diphenyl-2- picryl hydrazyl] radical scavenging activity of the plant was significant. n-Butanolic fraction was most potent with IC[50]being 1.06mg/mL. The IC[50]of methanolic extract was 1.50mg/mL, that of aqueous fraction was 2.51 mg/mL, and that of chloroform fraction was 2.65mg/mL. Antibacterial potential of the fern was tested against two Grampositive bacterial strains, Pseudomonas aeruginosa and Escherichia coli and two Gram-negative bacterial strains, Bacillus subtilis and Staphylococcus aureus. n-Butanolic fraction showed highest zone of inhibition [ZOI, 25.13+/-1.237 mm] against P. aeruginosa. Ethyl acetate fraction was most active [ZOI, 15.75+/-1.060 mm] against S. aureus. Against E. coli, aqueous and n-butanolic fractions were most active [ZOI, 14.75+/-0.353 and 14.50+/-0.707mm, respectively]. Minimum inhibitory concentration [MIC] of methanolic extract against B. subtilis was as low as 1.98mg/mL. The hexane fraction was least toxic against all the fractions. The plant displayed significant alpha-amylase inhibitory activity. Chloroform fraction was most effective with lowest IC[50][1.10mg/mL] followed by ethyl acetate fraction [1.92mg/mL]. A. venustum is rich in phenolics and has substantial antioxidant, antimicrobial and alpha-amylase inhibitory potential

5.
Asian Pacific Journal of Tropical Biomedicine ; (12): 541-545, 2015.
Article in Chinese | WPRIM | ID: wpr-950931

ABSTRACT

Objective: To study the antibacterial and antifungal activities of methanolic extract of roots of Carissa opaca and its fractions in hexane, chloroform, ethyl acetate, n-butanol and water, and the isolated compounds. Methods: The zones of inhibition of the samples against test microorganisms were determined by agar well diffusion method. Minimum inhibitory concentrations of the samples were determined by agar well dilution method. Test microorganisms included four standard bacteria [Bacillus subtilis ATCC 6633 (B. subtilis), Escherichia coli ATCC 8739 (E. coli), Pseudomonas aeruginosa ATCC 9027 (P. aeruginosa), and Staphylococcus aureus ATCC 6538], two standard fungi [Candida albicans ATCC 10231 (C. albicans)] and Aspergillus niger, and six clinical isolates (B. subtilis, E. coli, P. aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterobacter cloacae). The most active fraction was investigated to isolate compounds. The chemical compounds isolated from the ethyl acetate fraction were identified by gas chromatography-mass spectrometer, high performance liquid chromatography and liquid chromatographymass spectrometer. Results: E. coli, P. aeruginosa, and C. albicans were the most susceptible. Less polar fractions exhibited stronger efficacy than polar ones, and ethyl acetate fraction proved to be the most potent. Zones of inhibition of hexane, chloroform and ethyl acetate fractions, and amoxil against C. albicans were 19.96, 22.01, 23.10 and 19.20 mm, respectively. Ethyl acetate faction was the most toxic to all the test microorganisms, with minimum inhibitory concentrations of 8.0, 7.8 and 7.78 μg/mL against P. aeruginosa, C. albicans and B. subtilis, respectively. Isolated compounds, limonene, 2'-hydroxyacetophenone, vanillin, naphthalenone, 2,3,3-trimethyl-2-(3-methylbuta-1,3-dienyl)-6-methylenecyclohexanone, 2-benzenedicarboxylic acid, mono(2-ethylhexyl) ester, β-sitosterol, vitamin E, rutin, quercetin, lupeol, epigallocatechin, showed considerable antimicrobial activities against test microorganisms. Conclusions: The roots of Carissa opaca contain compounds with significant antimicrobial potential.

6.
Pakistan Journal of Pharmaceutical Sciences. 2015; 28 (2): 449-455
in English | IMEMR | ID: emr-178140

ABSTRACT

As the pathogens soon develop resistance to the existing antibiotics, the demand for new and more effective anti-microbial agents is a continuous phenomenon. In this paper we are reporting synthesis and spectral data of eight Schiff bases of salicylaldehyde with different amines, and evaluation of their anti-microbial activities against different bacterial strains. The bases were synthesized by reflux method, and their structures were determined based FT-IR,[1]HNMR,[13]C-NMR and Mass spectrometric data. The Schiff bases synthesized included 2-[[[Z]-[2-hydroxyphenyl] methylidene] amino]benzoicacid [SB1], 4-[[[Z]-[2-hydroxyphenyl] methylidene] amino] benzoic acid [SB2],2- [[naphthalene-2-ylimino] methyl] phenol [SB3],2-2'-[benzene-1,4- iylbis [nitrilomethylylidene]] diphenol [SB4], 2-2'- [benzene-1,2-diylbis [nitrile-[E]-methylylidene]]diphenol [SB5], 2-[[2- phenylhydrazineylidene] methyl]phenol [SB6], 2- 2'-[ethene-1,2-diylbis[iminomethanediyl]]diphenol [SB7] and 2-[[Z]-[phenylimino] methyl]phenol [SB8]. The antimicrobial activities of synthesized Schiff bases were determined in terms of zones of inhibition and minimum inhibitory concentrations [MICs]. All the bases showed moderate to good activities against all the tested microorganisms. The MICs of most compounds were 100-200microg/mL against different microorganisms. However, it was 50micro g/mL for SB1 against P. aeruginosa [1], SB3 against P. aurantiaca, P. aeruginosa [1], E. coli [2], S. typhi [2] and C. freundii, SB4against E. coli [2], S. typhi [1] and S. maltophilia, SB5 against K. pneumoniae and S. typhi [2], SB6 against P. aeruginosa [3] and C. freundii, SB7 against E. cloacae and A. lipoferum, andSB8against E. coli [2]. Considerably active bases may prove to be potential candidates for future antibiotic drugs


Subject(s)
Schiff Bases , Anti-Infective Agents , Spectrum Analysis
7.
Asian Pacific Journal of Tropical Biomedicine ; (12): 533-537, 2015.
Article in Chinese | WPRIM | ID: wpr-498931

ABSTRACT

Objective:To study the antibacterial and antifungal activities of methanolic extract of roots of Carissa opaca and its fractions in hexane, chloroform, ethyl acetate, n-butanol and water, and the isolated compounds. Methods:The zones of inhibition of the samples against test microorganisms were determined by agar well diffusion method. Minimum inhibitory concentrations of the samples were determined by agar well dilution method. Test microorganisms included four standard bacteria [Bacillus subtilis ATCC 6633 (B. subtilis), Escherichia coli ATCC 8739 (E. coli), Pseudomonas aeruginosa ATCC 9027 (P. aeruginosa), and Staphylococcus aureus ATCC 6538], two standard fungi [Candida albicans ATCC 10231 (C. albicans)] and Aspergillus niger, and six clinical isolates (B. subtilis, E. coli, P. aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterobacter cloacae). The most active fraction was investigated to isolate compounds. The chemical compounds isolated from the ethyl acetate fraction were identified by gas chromatography-mass spectrometer, high performance liquid chromatography and liquid chromatography-mass spectrometer. Results:E. coli, P. aeruginosa, and C. albicans were the most susceptible. Less polar fractions exhibited stronger efficacy than polar ones, and ethyl acetate fraction proved to be the most potent. Zones of inhibition of hexane, chloroform and ethyl acetate fractions, and amoxil against C. albicans were 19.96, 22.01, 23.10 and 19.20 mm, respectively. Ethyl acetate faction was the most toxic to all the test microorganisms, with minimum inhibitory concentrations of 8.0, 7.8 and 7.78 μg/mL against P. aeruginosa, C. albicans and B. subtilis, respectively. Isolated compounds, limonene, 2'-hydroxyacetophenone, vanillin, naphthalenone, 2,3,3-trimethyl-2-(3-methylbuta-1,3-dienyl)-6-methylenecyclohexanone, 2-benzenedicarboxylic acid, mono(2-ethylhexyl) ester,β-sitosterol, vitamin E, rutin, quercetin, lupeol, epigallocatechin, showed considerable antimicrobial activities against test microorganisms. Conclusions:The roots of Carissa opaca contain compounds with significant antimicrobial potential.

8.
Asian Pacific Journal of Tropical Medicine ; (12): S249-S255, 2014.
Article in Chinese | WPRIM | ID: wpr-951781

ABSTRACT

Objective: To conduct a comparative analysis of the phenolic and flavonoid contents and anti-oxidative potential of epicarp and mesocarp of Lagenaria siceraria fruit. Methods: The dried methanolic extracts of mesocarp and epicarp of the fruit and their hexane, chloroform, ethyl acetate, n-butanolic and aqueous fractions were subjected to antioxidant assays including ferric reducing antioxidant potential, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid, reducing power capacity, 2,2-diphenyl-1-picrylhydrazyl, lipid peroxidation inhibitory and phosphomolybdate assays. Total phenolic and flavonoid contents were also determined. Results: Ethyl acetate fractions of epicarp and mesocarp had considerable amounts of phenolics (243.50 and 109.50 μg/mL of gallic acid equivalents, respectively). 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity of ethyl acetate fractions of both the plant parts showed higher activity than vitamin C with IC

9.
Asian Pacific Journal of Tropical Medicine ; (12): S473-S480, 2014.
Article in Chinese | WPRIM | ID: wpr-951738

ABSTRACT

Objective: To evaluate antioxidant and radical scavenging activities of organic extracts from fruit, roots and aerial parts of Fagonia cretica. Methods: Shed dried and powdered plant parts were initially extracted in methanol and subsequently partitioned in n-hexane, chloroform, ethyl acetate and 1-butanol successively. Antioxidant and radical scavenging potential of the methanol extracts and the fractions of each part were evaluated using total phenolic contents (TPC) and total flavonoid contents (TFC), 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation radicals scavenging, reducing power (potassium ferricyanide-trichloroacetic acid system), ferric ion reducing antioxidant potential, lipid peroxidation inhibition activity (linoleic acid system) and total antioxidant activity (phosphomolybdate) assays. Results: TPC and TFC values for methanol extracts and various fractions ranged from 0.23-4.30 mg/L gallic acid equivalents and from 30-545 mg/L rutin equivalents, respectively. Overall, methanol extracts and all the fractions of root and aerial parts showed higher TPC and TFC values. Methanol extracts and aqueous fractions of root and aerial parts and the n-butanol fraction of root showed lower EC

10.
Asian Pacific Journal of Tropical Medicine ; (12): S249-55, 2014.
Article in English | WPRIM | ID: wpr-820602

ABSTRACT

OBJECTIVE@#To conduct a comparative analysis of the phenolic and flavonoid contents and anti-oxidative potential of epicarp and mesocarp of Lagenaria siceraria fruit.@*METHODS@#The dried methanolic extracts of mesocarp and epicarp of the fruit and their hexane, chloroform, ethyl acetate, n-butanolic and aqueous fractions were subjected to antioxidant assays including ferric reducing antioxidant potential, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid, reducing power capacity, 2,2-diphenyl-1-picrylhydrazyl, lipid peroxidation inhibitory and phosphomolybdate assays. Total phenolic and flavonoid contents were also determined.@*RESULTS@#Ethyl acetate fractions of epicarp and mesocarp had considerable amounts of phenolics (243.50 and 109.50 μg/mL of gallic acid equivalents, respectively). 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity of ethyl acetate fractions of both the plant parts showed higher activity than vitamin C with IC50 (0.75 and 3.91 mg, respectively). In phosphormolybdate assay, the hexane fractions of both the parts showed highest activity [1.16 and 2.99 μg/mL of ascorbic acid equivalents (AAE) for epicarp and mesocarp, respectively], mesocarp being much potent than epicarp. The n-butanolic fraction of mesocarp also showed much higher activity (1.13 μg/mL AAE) than that of epicarp (0.74 μg/mL AAE), while the chloroform and ethyl acetate fractions of epicarp were also considerably potent. In ferric reducing antioxidant potential assay, the chloroform fractions of both the fruit parts were most active. The hexane fractions of both the parts showed highest activity in reducing power assay, epicarp being more potent than mesocarp. In 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid assay, the antioxidant activities of ethyl acetate and chloroform fractions of both the parts were comparable to gallic acid and vitamin C. In lipid peroxidation inhibitory assay, all the samples were moderate to good activity sustainable over the period of 72 h, indicating the presence of both slow and fast releasing antioxidants.@*CONCLUSIONS@#The findings of the study suggest that epicarp is a better source of antioxidants than the mesocarp, and the ethyl acetate fractions of both the parts contain higher contents of antioxidants.

11.
Asian Pacific Journal of Tropical Medicine ; (12): S473-80, 2014.
Article in English | WPRIM | ID: wpr-820177

ABSTRACT

OBJECTIVE@#To evaluate antioxidant and radical scavenging activities of organic extracts from fruit, roots and aerial parts of Fagonia cretica.@*METHODS@#Shed dried and powdered plant parts were initially extracted in methanol and subsequently partitioned in n-hexane, chloroform, ethyl acetate and 1-butanol successively. Antioxidant and radical scavenging potential of the methanol extracts and the fractions of each part were evaluated using total phenolic contents (TPC) and total flavonoid contents (TFC), 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation radicals scavenging, reducing power (potassium ferricyanide-trichloroacetic acid system), ferric ion reducing antioxidant potential, lipid peroxidation inhibition activity (linoleic acid system) and total antioxidant activity (phosphomolybdate) assays.@*RESULTS@#TPC and TFC values for methanol extracts and various fractions ranged from 0.23-4.30 mg/L gallic acid equivalents and from 30-545 mg/L rutin equivalents, respectively. Overall, methanol extracts and all the fractions of root and aerial parts showed higher TPC and TFC values. Methanol extracts and aqueous fractions of root and aerial parts and the n-butanol fraction of root showed lower EC50 values for 2,2-diphenyl-1-picrylhydrazyl scavenging than the other plant extracts. The 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging, total antioxidant potential and ferric ion reducing antioxidant potential values confirmed the presence of potent antioxidant principles in the methanol extract of roots. In general, all the extracts/fractions and especially those of root showed high antioxidant and radical scavenging activities.@*CONCLUSIONS@#The crude methanol extract of root can be explored further for in vivo studies. This study revealed the potent antioxidant potential of Fagonia cretica and its prospective efficacy against various reactive oxygen species-mediated diseases.

12.
Pakistan Journal of Pharmaceutical Sciences. 2014; 27 (1): 57-61
in English | IMEMR | ID: emr-142980

ABSTRACT

Melilotus indicus [Linn.] All. is a small herb distributed throughout Pakistan and has a number of ethnomedicinal uses. It is also consumed as a vegetable. In the present work, we are reporting the alpha-amylase and urease inhibitory activities of methanolic extract of M. indicus and its sub-fractions in different solvents. Both the methanolic extract and its fractions in chloroform, ethyl acetate, n-butanol and water showed remarkable inhibitory activities against alpha-amylase with the IC[50] values being 1.29, 1.45, 1.07, 1.45 and 2.10 mg/mL respectively. The efficacy of the methanolic extract was comparable with that of acarbose [1.20 mg/mL], while the ethyl acetate fraction was more potent. The urease inhibitory activities of methanolic extract and chloroform, ethyl acetate, n-butanol and water fractions were more prominent with IC[50] values being 0.95, 0.89, 1.53, 0.98 and 4.90 microg/mL respectively. The activity of methanolic extract was slightly higher than that of thiourea [0.97 microg/mL] which in turn was slightly higher than that of n-butanolic fraction. The chloroform fraction showed the highest anti-urease activity. All the plant samples showed enzyme inhibitory activity in a dose-dependent manner. Moreover, they were manifold more effective against urease than alpha-amylase. The combination of the plant extract with acarbose considerably increased the potency of the latter. The findings suggest that enzyme inhibitory activities of the vegetable M. indicus may have pharmacological significance against diabetes mellitus and gastrointestinal ulcers.


Subject(s)
Urease/antagonists & inhibitors , alpha-Amylases/antagonists & inhibitors , Plant Extracts/pharmacology
13.
Pakistan Journal of Pharmaceutical Sciences. 2013; 26 (3): 553-559
in English | IMEMR | ID: emr-142616

ABSTRACT

The present study aimed to establish relationship between urease and alpha-amylase inhibitory activities on the one hand and on the other between anti-enzymatic activities and total phenolic contents of the methanolic extract of roots of Rumex acetosella and its fractions in various solvents. The methanolic extract and its fractions in chloroform, ethyl acetate, n-butanol and water showed remarkable inhibitory activities against both urease and alpha-amylase, there was a close correspondence between urease and alpha-amylase inhibitory activities of the plant samples. The n-butanol fraction which had the highest total phenolic content [252.19 +/- 2.32 micro g of Gallic Acid Equivalents/mg of dry mass of the sample] showed prominent activity against both urease and alpha-amylase indicating a possible role of phenolics in inhibiting the activities of these enzymes. The samples displayed enzyme inhibitory activities in a dose dependent manner and their effectiveness was comparable with that of the standards, thiourea [for urease] and acarbose [for alphaamylase]. The samples were manifold more effective against urease than alpha-amylase; 2.8 mg/mL of MeOH extract produced about 81% inhibition in alpha-amylase activity, while only 10 micro g/mL of the extract was required to create the same inhibition in urease activity. The IC[50] values of methanolic, chloroform, ethyl acetate, n-butanolic, aqueous and standard solutions were 1.29, 1.31, 1.90, 1.38, 0.85 and 1.20 [mg/mL] respectively against alpha-amylase and 0.99, 3.89, 1.76, 0.91, 0.85 and 0.97 [micro g/mL] respectively against urease. The total phenolic content in MeOH, hexane, chloroform, ethyl acetate, n-butanol and water fractions was 108.88 +/- 2.65, 43.70 +/- 1.90, 34.44 +/- 2.30, 230.71 +/- 1.78, 252.19 +/- 2.32 and 94.07 +/- 2.25 respectively


Subject(s)
Urease/antagonists & inhibitors , alpha-Amylases/antagonists & inhibitors , Phenols/chemistry , Plant Extracts/chemistry , Enzyme Inhibitors/pharmacology , Methanol/chemistry , Phenols/analysis , 1-Butanol/chemistry
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