Phytochemicals are rich source of bioactive constituents and can be used as another alternative t... more Phytochemicals are rich source of bioactive constituents and can be used as another alternative to currently used drugs for diseases like Diabetes mellitus. The potential of Isoliquiritigenin (a constituent of Pterocarpus marsupium) as PPARđŸ agonist was evaluated by in silico technique. Autodock results showed that Tyr327, and Tyr473 of the PPARÎł forms H-bonds with Isoliquiritigenin (binding energy of -7.46 kcal/mol) and Troglitazone (known drug) showed H bond with Tyr327, Ser289, with binding energy of -11.01 kcal/mol. Isoliquiritigenin, binding energy in Extra precision (XP) was -6.74 kcal/mol while Troglitazone docking, gave binding energy in XP mode as -9.59 kcal/mol. The best Induced fit docking (IFD) score of the optimised PPARÎł- Isoliquiritigenin complexes was -9.39 Kcal/mol. The important residues in IFD forming H bond were Cys 285, Arg 288, Tyr 327 and Leu 340. The post docking MM/GBSA free energy for PPARÎł with Isoliquiritigenin and Troglitazone was -49.29 and -71.48 Kcal/...
Hypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were eval... more Hypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were evaluated in the 3T3-L1 cell line, and an interaction study in silico with XO was performed with considerable bioactive components of acetone extract of faba beans. The protonated and fragmented behavior of acetone seed extract revealed the presence of gallic acid (MS/MS, m/z 169) and catechin (MSn, m/z 288.3). Flow cytometry study explained the effect of hydrogen peroxide (H2O2) on cell line as cell death was increased from 9.72 to 41.66% as compared to the control (without H2O2). The atomic force microscopy (AFM), scanning electron microscopy and reactive oxygen species measurement also confirmed the protective effect of polyphenols in the 3T3-L1 cell lines. Oxidative stress through propidium iodide and 4âČ,6-diamidino-2-phenylindole staining demonstrated that the apoptotic ratio was 0.35 ± 2.62 (P < 0.05) and 30 ± 2.54% in H2O2-treated cells, respectively, as compared to control. The ob...
Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood <i>Ptero... more Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood <i>Pterocarpus marsupium</i> were found to be 124.4 ± 4.6, 485.5 ± 2.7, and 71.6 ± 4.2 mg/gm of plant extract respectively. HPLC analyses of extract showed retention time at 6.2 min and FTIR analysis confirmed presence of Liquiritigenin in methanolic extract. In DPPH scavenging activity and ABTSâ+ scavenging activity, IC<sub>50</sub> values were found to be 138.3, 12.4, 13.5 and 47.8, 3.9, 4.2 ÎŒg/mL for aqueous, methanolic extract and standard ascorbic acid respectively. In α-amylase inhibition assay and α-glucosidase inhibition assay, IC<sub>50</sub> values for standard Acarbose, aqueous and methanolic extract of heartwood were 44.09, 166.72, 48.20 and 45.17, 172.32, 48.12 respectively. Molecular docking study showed hydrogen bonding between Liquiritigenin and catalytic triad (Asp197, Glu233, and Asp300) of α-amylase and His407 of α âGlucosidase with â5.60 and â7.1...
Ginkgo biloba extract was evaluated for prophylactic value against renal ischemia-reperfusion ind... more Ginkgo biloba extract was evaluated for prophylactic value against renal ischemia-reperfusion induced oxidant stress in rat subjected to transient unilateral renal artery ligation. Oral Ginkgo biloba treatment (2mg/kg) was administered by different schedule before experimental induction of ischemia-reperfusion injury. Malondialdehyde has been taken as indicator for free radical damage produced by ischemia-reperfusion injury. Three hour pretreatment by the drug has most prominent inhibitory effect on consequent tissue and plasma malondialdehyde level of lipid peroxidation. Further, the relative inhibition of malondialdehyde level in tissue and plasma allow to infer drug effect on generation, but not the clearance of malondialdehyde. No significant difference of outcome from 1, 2 and 3 days treatment indicate no cumulation and thus safety in that respect. Ginkgo biloba treatment appears both effective and safe for prophylaxis of reperfusion injury following ischemia catastrophies.
Current rates of increase in population are calling into question the capacity of humanity to con... more Current rates of increase in population are calling into question the capacity of humanity to continue to ensure supply of food for all. At the same time aquaculture within the agriculture is the fastest growing food production sectors in the world as we can say itâs a âfood goldâ of the present as well as future. Aquaculture has become an extremely important and much promising undertaking for scientific research, engineering development, economic growth, food security, alleviation of poverty, improvement of nutrition, supplying new material for pharmaceuticals and even more significant for protection of the endangered species and conservation of water bodies. The fisheries need to rely on scientific advancement and innovations to realize its sustainable development. But main hurdle on the way to sustain fishery business is the heavy metal pollution of water bodies. Among heavy metal pollutants, cadmium merits special attention due to its potential hazards to freshwater aquatic biota as well as to human being. Cadmium is released in considerable amounts through industrial effluents into soil, surface and ground water systems. These excess amounts in addition to naturally occurring levels gradually build up to toxic levels causing damage to the aquatic system in which freshwater fishes are the main victim of it. So, an attempt has been made to assess the cadmium toxicity on freshwater snakehead fish Channa punctatus. The aim of this study was to detect LC50 of cadmium sulphate on freshwater air breathing snakehead fish and its adverse effect on morphology and behavioural changes. For this study, freshwater fish Channa punctatus was selected due to its adaptation in polluted water, hence it can be good biological indicator to detect the pollution status of freshwater aquatic body.
L-asparaginase has proven itself as a potential anti-cancer drug and in the mitigation of acrylam... more L-asparaginase has proven itself as a potential anti-cancer drug and in the mitigation of acrylamide formation in the food industry. In the present investigation, a novel utilization of niger (Guizotia abyssinica) de-oiled cake as the sole source for the cost-effective production of L-asparaginase was evaluated and compared with different agro-substrates in solid-state fermentation. The substrate provided a favorable C/N content for the L-asparaginase production as evident from the chemical composition (CHNS analysis) of the substrate. The influential process parameters viz; autoclaving time, moisture content, temperature and pH were optimized and modeled using machine-learning based artificial neural network (ANN) and statistical-based response surface methodology (RSM). The maximum enzyme activity of 34.65â±â2.18âIU/gds was observed at 30.3âmin of autoclaving time, 62% moisture content, 30â°C temperature and 6.2âpH in 96âh. A 1.36 fold improvement in enzyme activity was observed on utilizing optimized parameters. In comparison with RSM, the ANN model showed superior prediction with a low mean squared error of 0.072, low root mean squared error of 0.268 and 0.99 value of regression coefficient. The present study demonstrates the novel utilization of inexpensive and readily available agro-industrial waste for the development of cost-effective L-asparaginase production process.
Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Im... more Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Imbach (AbPI) on glucose uptake and oxidative stress in 3T3-L1 adipocytes. Methods: Adipocytes were differentiated and stained with Oil-Red-O staining to confirm adipogenesis. The toxic/protective effect of AbPI on the adipocytes was determined by MTT assay, intracellular reactive oxygen species generation through flow cytometry, and morphologically through confocal microscopy using propidium iodide, 4,6-diamino-2-phenylindol dihydrochloride, and 2â,7â-dichlorofluorescein diacetate dyes. The uptake of fluorescent glucose analog, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-d-glucose by adipocytes was also studied through confocal microscopy. Results: MTT assay showed that the cell survival rate was (28.00±3.00)%, (92.33±2.60)%, and (71.34±2.10)% in the presence of 2 mM H2O2, AbPI alone, and AbPI and H2O2 both, respectively, in comparison to the control. Oil-Red-O staining indicated that AbPI enhanced adipogenesis. AbPI stimulated the glucose uptake by adipocytes similar to the drug rosiglitazone, and showed insulin-sensitizing effect in the presence of insulin, but failed to stimulate the uptake in the absence of insulin. Intracellular reactive oxygen species generation was reduced in differentiating adipocytes upon AbPI treatment. Confocal microscopy showed that the damaged cell population rose to 3.50%, 117.84%, and 261.50% in the presence of AbPI alone, AbPI with H2O2, and H2O2 alone, respectively. Conclusions: The protease inhibitor enhances glucose uptake by adipocytes and exhibits a cytoprotective effect on them.
Abstract The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored ... more Abstract The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored as an α-glucosidase inhibitor. The inhibition of α-glucosidase is one of the alternatives approach to control postprandial hyperglycemia by, resulting in the delay of the carbohydrate digestion of absorbable monosaccharides. Ethanolic seed extract showed phenolic compounds, flavonoid such as gallic acid (m/z [MââH]â=â169.0124,C7H6O5) ellagic acid derivatives epigallocatechin (m/z [MââHâ=â305.0644,C15H14O7),catechin (m/z [MââH]â=â289.0656,C15H14O6), epigallocatechin gallate (m/z [MââH]â=â457.0578,C22H18O11) and epicatechin monogallate (m/z [MââH]â=â441.081, C22H18O10). The extract was found to exert inhibitory activity (88.28â±â2.67%) (IC50 value of 2.30â±â0.032âmg/mL) with a mixed mode of inhibition (Km, apparent = 0.54â±â0.020âmM and Vmax, apparent 0.136â±â0.04âmM/min). Molecular docking studies of gallic acid and catechin on α-glucosidase proposed productive binding modes having binding energy (â6.58âkcal/mol and â7.25âkcal/mol) with an effective number of hydrogen bonds and binding energy. Tyr63, Arg197, Asp198, Glu 233, Asn324, Asp 326 of α-glucosidase participated in binding events with gallic acid and catechin. Molecular dynamics simulation studies were performed for both complexes i.e. gal:α-glucosidase and cat:α-glucosidase along with apo state of α-glucosidase, which revealed stable systems during the simulation. These findings of the present study may give an insight into the further development of the novel antidiabetic drug from the seeds of faba beans.
L-asparaginase is a valuable protein therapeutic drug utilized for the treatment of leukemia and ... more L-asparaginase is a valuable protein therapeutic drug utilized for the treatment of leukemia and lymphomas. Administration of asparaginase leads to asparagine starvation causing inhibition of protein synthesis, growth, and proliferation of tumor cells. Besides its clinical significance, the enzyme also finds application in the food sector for mitigation of a cancer-causing agent acrylamide. The numerous applications ensue huge market demands and create a continued interest in the production of costeffective, more specific, less immunogenic and stable formulations which can cater both the clinical and food processing requirements. The current review article approaches the process parameters of submerged and solid-state fermentation strategies for the microbial production of the L-asparaginase from diverse sources, genetic engineering approaches used for the production of L-asparaginase enzyme and major applications in clinical and food sectors. The review also addresses the immunolog...
Abstract Imbalance of free radicals over antioxidants in human body may result in oxidative damag... more Abstract Imbalance of free radicals over antioxidants in human body may result in oxidative damage to biomolecules (lipids, proteins, DNA) that causes severe chronic diseases. The aim of this proposed research was to examine the hypoglycemic and oxidative stress potential of fava bean (Vicia faba L.) seed extract. Acetone extract showed a significant effect on glucose uptake rate (77.28â±â2.42%) in yeast cells at 25âmM glucose concentration. Minimum glucose uptake rate was found to be 52.36â±â2.06% % by chloroform seed extract. Atomic force microscopy revealed that 3% hydrogen peroxide concentration results in roughness was found to be maximum (441â±â6.7ânm) and along with extract treatment showed a significant reduction in roughness (251â±â6.2ânm). Propidium iodide and DAPI staining showed apoptotic ratio as 0.40 (40â±â1.18%,) and 0.42 (42â±â1.16%) in hydrogen peroxide treated cell only as compared to other treatments. MTT assay showed that acetone extract had maximum survival rate (82.067%) and least survival rate was found in chloroform extract (70.48%). Hypoglycaemic potential and oxidative stress might be polyphenols (phenolics, flavonoids) present in seed extract or synergistic effect.
Acetone extract of faba bean (Vicia faba L.) was found to be highest total phenol and flavonoid c... more Acetone extract of faba bean (Vicia faba L.) was found to be highest total phenol and flavonoid content among all extracts. Antioxidant activity for inhibition percentage (free radical scavenging activity) had 86.47% for acetone extract, and 97.36% for ascorbic acid respectively. IC value of ascorbic acid and acetone extact were found to be 9 Όg/mL ± 0.20 and 30 Όg/mL ± 0.21. Faba bean seeds had catechin, epicatechin, gallic acid and ellagic acid which on molecular docking study revealed that it binds effectively with xanthine oxidase by binding energy of -7.78, -6.11, -6.39, -5.78 kcal/mol respectively compared to allopurinol drug having binding energy of -4.94 kcal/mol. Gallic acid, ellagic acid, catechin, epicatechin (polyphenols) and allopurinol bind other than catalytic residues (Glu-1261) of xanthine oxidase. In vitro and in silico analysis recommended that mode of enzyme inhibition was mixed type.
Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood Pterocarpus ma... more Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood Pterocarpus marsupium were found to be 124.4 ± 4.6, 485.5 ± 2.7, and 71.6 ± 4.2 mg/gm of plant extract respectively. HPLC analyses of extract showed retention time at 6.2 min and FTIR analysis confirmed presence of Liquiritigenin in methanolic extract. In DPPH scavenging activity and ABTSâ+ scavenging activity, IC values were found to be 138.3, 12.4, 13.5 and 47.8, 3.9, 4.2 Όg/mL for aqueous, methanolic extract and standard ascorbic acid respectively. In α-amylase inhibition assay and α-glucosidase inhibition assay, IC values for standard Acarbose, aqueous and methanolic extract of heartwood were 44.09, 166.72, 48.20 and 45.17, 172.32, 48.12 respectively. Molecular docking study showed hydrogen bonding between Liquiritigenin and catalytic triad (Asp197, Glu233, and Asp300) of α-amylase and His407 of α -Glucosidase with -5.60 and -7.10 binding energies respectively.
The production of a protease inhibitor from Agaricus bisporus through solid-state fermentation wa... more The production of a protease inhibitor from Agaricus bisporus through solid-state fermentation was studied. The purpose was to produce protease inhibitor from natural, cheap, and readily available carbon and nitrogen sources. Solid-state fermentation enhanced the mycelia growth and also gave a higher yield of the product. Further, fungal growth and other production parameters were statistically optimized. The specificity of the inhibitor was tested and was effective against trypsin. Screening of significant factors (wheat bran, cyanobacterial biomass, initial pH, temperature, incubation period, and moisture content and inoculum size) was performed using Plackett-Burman design. Central composite design was used to determine the optimized values of the significant variables which were found to be temperature (27.5°C), incubation time (156âhr), cyanobacterial biomass (1âg), and moisture content (50%) and gave a statistical yield of 980 PIU/g which was 25.6% higher than experimental yield (780 PIU/g). The inhibitor was purified by ammonium sulfate precipitation and diethylaminoethyl (DEAE) cellulose chromatography (yield 43.89% and 0.21%, respectively) and subjected to reversed-phase HPLC to validate its identity. Since protease inhibitors act against proteases, finding ample therapeutic roles; the isolated protease inhibitor from A. bisporus can also be a probable medicinal agent after its further characterization.
Phytochemicals are rich source of bioactive constituents and can be used as another alternative t... more Phytochemicals are rich source of bioactive constituents and can be used as another alternative to currently used drugs for diseases like Diabetes mellitus. The potential of Isoliquiritigenin (a constituent of Pterocarpus marsupium) as PPARđŸ agonist was evaluated by in silico technique. Autodock results showed that Tyr327, and Tyr473 of the PPARÎł forms H-bonds with Isoliquiritigenin (binding energy of -7.46 kcal/mol) and Troglitazone (known drug) showed H bond with Tyr327, Ser289, with binding energy of -11.01 kcal/mol. Isoliquiritigenin, binding energy in Extra precision (XP) was -6.74 kcal/mol while Troglitazone docking, gave binding energy in XP mode as -9.59 kcal/mol. The best Induced fit docking (IFD) score of the optimised PPARÎł- Isoliquiritigenin complexes was -9.39 Kcal/mol. The important residues in IFD forming H bond were Cys 285, Arg 288, Tyr 327 and Leu 340. The post docking MM/GBSA free energy for PPARÎł with Isoliquiritigenin and Troglitazone was -49.29 and -71.48 Kcal/...
Hypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were eval... more Hypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were evaluated in the 3T3-L1 cell line, and an interaction study in silico with XO was performed with considerable bioactive components of acetone extract of faba beans. The protonated and fragmented behavior of acetone seed extract revealed the presence of gallic acid (MS/MS, m/z 169) and catechin (MSn, m/z 288.3). Flow cytometry study explained the effect of hydrogen peroxide (H2O2) on cell line as cell death was increased from 9.72 to 41.66% as compared to the control (without H2O2). The atomic force microscopy (AFM), scanning electron microscopy and reactive oxygen species measurement also confirmed the protective effect of polyphenols in the 3T3-L1 cell lines. Oxidative stress through propidium iodide and 4âČ,6-diamidino-2-phenylindole staining demonstrated that the apoptotic ratio was 0.35 ± 2.62 (P < 0.05) and 30 ± 2.54% in H2O2-treated cells, respectively, as compared to control. The ob...
Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood <i>Ptero... more Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood <i>Pterocarpus marsupium</i> were found to be 124.4 ± 4.6, 485.5 ± 2.7, and 71.6 ± 4.2 mg/gm of plant extract respectively. HPLC analyses of extract showed retention time at 6.2 min and FTIR analysis confirmed presence of Liquiritigenin in methanolic extract. In DPPH scavenging activity and ABTSâ+ scavenging activity, IC<sub>50</sub> values were found to be 138.3, 12.4, 13.5 and 47.8, 3.9, 4.2 ÎŒg/mL for aqueous, methanolic extract and standard ascorbic acid respectively. In α-amylase inhibition assay and α-glucosidase inhibition assay, IC<sub>50</sub> values for standard Acarbose, aqueous and methanolic extract of heartwood were 44.09, 166.72, 48.20 and 45.17, 172.32, 48.12 respectively. Molecular docking study showed hydrogen bonding between Liquiritigenin and catalytic triad (Asp197, Glu233, and Asp300) of α-amylase and His407 of α âGlucosidase with â5.60 and â7.1...
Ginkgo biloba extract was evaluated for prophylactic value against renal ischemia-reperfusion ind... more Ginkgo biloba extract was evaluated for prophylactic value against renal ischemia-reperfusion induced oxidant stress in rat subjected to transient unilateral renal artery ligation. Oral Ginkgo biloba treatment (2mg/kg) was administered by different schedule before experimental induction of ischemia-reperfusion injury. Malondialdehyde has been taken as indicator for free radical damage produced by ischemia-reperfusion injury. Three hour pretreatment by the drug has most prominent inhibitory effect on consequent tissue and plasma malondialdehyde level of lipid peroxidation. Further, the relative inhibition of malondialdehyde level in tissue and plasma allow to infer drug effect on generation, but not the clearance of malondialdehyde. No significant difference of outcome from 1, 2 and 3 days treatment indicate no cumulation and thus safety in that respect. Ginkgo biloba treatment appears both effective and safe for prophylaxis of reperfusion injury following ischemia catastrophies.
Current rates of increase in population are calling into question the capacity of humanity to con... more Current rates of increase in population are calling into question the capacity of humanity to continue to ensure supply of food for all. At the same time aquaculture within the agriculture is the fastest growing food production sectors in the world as we can say itâs a âfood goldâ of the present as well as future. Aquaculture has become an extremely important and much promising undertaking for scientific research, engineering development, economic growth, food security, alleviation of poverty, improvement of nutrition, supplying new material for pharmaceuticals and even more significant for protection of the endangered species and conservation of water bodies. The fisheries need to rely on scientific advancement and innovations to realize its sustainable development. But main hurdle on the way to sustain fishery business is the heavy metal pollution of water bodies. Among heavy metal pollutants, cadmium merits special attention due to its potential hazards to freshwater aquatic biota as well as to human being. Cadmium is released in considerable amounts through industrial effluents into soil, surface and ground water systems. These excess amounts in addition to naturally occurring levels gradually build up to toxic levels causing damage to the aquatic system in which freshwater fishes are the main victim of it. So, an attempt has been made to assess the cadmium toxicity on freshwater snakehead fish Channa punctatus. The aim of this study was to detect LC50 of cadmium sulphate on freshwater air breathing snakehead fish and its adverse effect on morphology and behavioural changes. For this study, freshwater fish Channa punctatus was selected due to its adaptation in polluted water, hence it can be good biological indicator to detect the pollution status of freshwater aquatic body.
L-asparaginase has proven itself as a potential anti-cancer drug and in the mitigation of acrylam... more L-asparaginase has proven itself as a potential anti-cancer drug and in the mitigation of acrylamide formation in the food industry. In the present investigation, a novel utilization of niger (Guizotia abyssinica) de-oiled cake as the sole source for the cost-effective production of L-asparaginase was evaluated and compared with different agro-substrates in solid-state fermentation. The substrate provided a favorable C/N content for the L-asparaginase production as evident from the chemical composition (CHNS analysis) of the substrate. The influential process parameters viz; autoclaving time, moisture content, temperature and pH were optimized and modeled using machine-learning based artificial neural network (ANN) and statistical-based response surface methodology (RSM). The maximum enzyme activity of 34.65â±â2.18âIU/gds was observed at 30.3âmin of autoclaving time, 62% moisture content, 30â°C temperature and 6.2âpH in 96âh. A 1.36 fold improvement in enzyme activity was observed on utilizing optimized parameters. In comparison with RSM, the ANN model showed superior prediction with a low mean squared error of 0.072, low root mean squared error of 0.268 and 0.99 value of regression coefficient. The present study demonstrates the novel utilization of inexpensive and readily available agro-industrial waste for the development of cost-effective L-asparaginase production process.
Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Im... more Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Imbach (AbPI) on glucose uptake and oxidative stress in 3T3-L1 adipocytes. Methods: Adipocytes were differentiated and stained with Oil-Red-O staining to confirm adipogenesis. The toxic/protective effect of AbPI on the adipocytes was determined by MTT assay, intracellular reactive oxygen species generation through flow cytometry, and morphologically through confocal microscopy using propidium iodide, 4,6-diamino-2-phenylindol dihydrochloride, and 2â,7â-dichlorofluorescein diacetate dyes. The uptake of fluorescent glucose analog, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-d-glucose by adipocytes was also studied through confocal microscopy. Results: MTT assay showed that the cell survival rate was (28.00±3.00)%, (92.33±2.60)%, and (71.34±2.10)% in the presence of 2 mM H2O2, AbPI alone, and AbPI and H2O2 both, respectively, in comparison to the control. Oil-Red-O staining indicated that AbPI enhanced adipogenesis. AbPI stimulated the glucose uptake by adipocytes similar to the drug rosiglitazone, and showed insulin-sensitizing effect in the presence of insulin, but failed to stimulate the uptake in the absence of insulin. Intracellular reactive oxygen species generation was reduced in differentiating adipocytes upon AbPI treatment. Confocal microscopy showed that the damaged cell population rose to 3.50%, 117.84%, and 261.50% in the presence of AbPI alone, AbPI with H2O2, and H2O2 alone, respectively. Conclusions: The protease inhibitor enhances glucose uptake by adipocytes and exhibits a cytoprotective effect on them.
Abstract The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored ... more Abstract The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored as an α-glucosidase inhibitor. The inhibition of α-glucosidase is one of the alternatives approach to control postprandial hyperglycemia by, resulting in the delay of the carbohydrate digestion of absorbable monosaccharides. Ethanolic seed extract showed phenolic compounds, flavonoid such as gallic acid (m/z [MââH]â=â169.0124,C7H6O5) ellagic acid derivatives epigallocatechin (m/z [MââHâ=â305.0644,C15H14O7),catechin (m/z [MââH]â=â289.0656,C15H14O6), epigallocatechin gallate (m/z [MââH]â=â457.0578,C22H18O11) and epicatechin monogallate (m/z [MââH]â=â441.081, C22H18O10). The extract was found to exert inhibitory activity (88.28â±â2.67%) (IC50 value of 2.30â±â0.032âmg/mL) with a mixed mode of inhibition (Km, apparent = 0.54â±â0.020âmM and Vmax, apparent 0.136â±â0.04âmM/min). Molecular docking studies of gallic acid and catechin on α-glucosidase proposed productive binding modes having binding energy (â6.58âkcal/mol and â7.25âkcal/mol) with an effective number of hydrogen bonds and binding energy. Tyr63, Arg197, Asp198, Glu 233, Asn324, Asp 326 of α-glucosidase participated in binding events with gallic acid and catechin. Molecular dynamics simulation studies were performed for both complexes i.e. gal:α-glucosidase and cat:α-glucosidase along with apo state of α-glucosidase, which revealed stable systems during the simulation. These findings of the present study may give an insight into the further development of the novel antidiabetic drug from the seeds of faba beans.
L-asparaginase is a valuable protein therapeutic drug utilized for the treatment of leukemia and ... more L-asparaginase is a valuable protein therapeutic drug utilized for the treatment of leukemia and lymphomas. Administration of asparaginase leads to asparagine starvation causing inhibition of protein synthesis, growth, and proliferation of tumor cells. Besides its clinical significance, the enzyme also finds application in the food sector for mitigation of a cancer-causing agent acrylamide. The numerous applications ensue huge market demands and create a continued interest in the production of costeffective, more specific, less immunogenic and stable formulations which can cater both the clinical and food processing requirements. The current review article approaches the process parameters of submerged and solid-state fermentation strategies for the microbial production of the L-asparaginase from diverse sources, genetic engineering approaches used for the production of L-asparaginase enzyme and major applications in clinical and food sectors. The review also addresses the immunolog...
Abstract Imbalance of free radicals over antioxidants in human body may result in oxidative damag... more Abstract Imbalance of free radicals over antioxidants in human body may result in oxidative damage to biomolecules (lipids, proteins, DNA) that causes severe chronic diseases. The aim of this proposed research was to examine the hypoglycemic and oxidative stress potential of fava bean (Vicia faba L.) seed extract. Acetone extract showed a significant effect on glucose uptake rate (77.28â±â2.42%) in yeast cells at 25âmM glucose concentration. Minimum glucose uptake rate was found to be 52.36â±â2.06% % by chloroform seed extract. Atomic force microscopy revealed that 3% hydrogen peroxide concentration results in roughness was found to be maximum (441â±â6.7ânm) and along with extract treatment showed a significant reduction in roughness (251â±â6.2ânm). Propidium iodide and DAPI staining showed apoptotic ratio as 0.40 (40â±â1.18%,) and 0.42 (42â±â1.16%) in hydrogen peroxide treated cell only as compared to other treatments. MTT assay showed that acetone extract had maximum survival rate (82.067%) and least survival rate was found in chloroform extract (70.48%). Hypoglycaemic potential and oxidative stress might be polyphenols (phenolics, flavonoids) present in seed extract or synergistic effect.
Acetone extract of faba bean (Vicia faba L.) was found to be highest total phenol and flavonoid c... more Acetone extract of faba bean (Vicia faba L.) was found to be highest total phenol and flavonoid content among all extracts. Antioxidant activity for inhibition percentage (free radical scavenging activity) had 86.47% for acetone extract, and 97.36% for ascorbic acid respectively. IC value of ascorbic acid and acetone extact were found to be 9 Όg/mL ± 0.20 and 30 Όg/mL ± 0.21. Faba bean seeds had catechin, epicatechin, gallic acid and ellagic acid which on molecular docking study revealed that it binds effectively with xanthine oxidase by binding energy of -7.78, -6.11, -6.39, -5.78 kcal/mol respectively compared to allopurinol drug having binding energy of -4.94 kcal/mol. Gallic acid, ellagic acid, catechin, epicatechin (polyphenols) and allopurinol bind other than catalytic residues (Glu-1261) of xanthine oxidase. In vitro and in silico analysis recommended that mode of enzyme inhibition was mixed type.
Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood Pterocarpus ma... more Total amount of phenols, flavonoids and tannins in methanolic extract of heartwood Pterocarpus marsupium were found to be 124.4 ± 4.6, 485.5 ± 2.7, and 71.6 ± 4.2 mg/gm of plant extract respectively. HPLC analyses of extract showed retention time at 6.2 min and FTIR analysis confirmed presence of Liquiritigenin in methanolic extract. In DPPH scavenging activity and ABTSâ+ scavenging activity, IC values were found to be 138.3, 12.4, 13.5 and 47.8, 3.9, 4.2 Όg/mL for aqueous, methanolic extract and standard ascorbic acid respectively. In α-amylase inhibition assay and α-glucosidase inhibition assay, IC values for standard Acarbose, aqueous and methanolic extract of heartwood were 44.09, 166.72, 48.20 and 45.17, 172.32, 48.12 respectively. Molecular docking study showed hydrogen bonding between Liquiritigenin and catalytic triad (Asp197, Glu233, and Asp300) of α-amylase and His407 of α -Glucosidase with -5.60 and -7.10 binding energies respectively.
The production of a protease inhibitor from Agaricus bisporus through solid-state fermentation wa... more The production of a protease inhibitor from Agaricus bisporus through solid-state fermentation was studied. The purpose was to produce protease inhibitor from natural, cheap, and readily available carbon and nitrogen sources. Solid-state fermentation enhanced the mycelia growth and also gave a higher yield of the product. Further, fungal growth and other production parameters were statistically optimized. The specificity of the inhibitor was tested and was effective against trypsin. Screening of significant factors (wheat bran, cyanobacterial biomass, initial pH, temperature, incubation period, and moisture content and inoculum size) was performed using Plackett-Burman design. Central composite design was used to determine the optimized values of the significant variables which were found to be temperature (27.5°C), incubation time (156âhr), cyanobacterial biomass (1âg), and moisture content (50%) and gave a statistical yield of 980 PIU/g which was 25.6% higher than experimental yield (780 PIU/g). The inhibitor was purified by ammonium sulfate precipitation and diethylaminoethyl (DEAE) cellulose chromatography (yield 43.89% and 0.21%, respectively) and subjected to reversed-phase HPLC to validate its identity. Since protease inhibitors act against proteases, finding ample therapeutic roles; the isolated protease inhibitor from A. bisporus can also be a probable medicinal agent after its further characterization.
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Papers by Dr. Abha Mishra