Objective:To investigate the hepatoprotective activity of methanolic leaf extract of Cyathea gigantea(C.gigantea)against paracetamol induced liver damage in rats.Methods:The hepatoprotective activity for plant extract...Objective:To investigate the hepatoprotective activity of methanolic leaf extract of Cyathea gigantea(C.gigantea)against paracetamol induced liver damage in rats.Methods:The hepatoprotective activity for plant extract was investigated for paracetamol induced hepatoxicity in rats.Wislar albino rats of either sex were divided into five groups of 6 animals each and are given orally the following treatment for seven days.The normal control group was given 1%Na.CMC 1mL/kg bw,p.o.Paracetamol at dose of 1g/kg bw,p.o.was given as toxic dose for inducing hepatoloxicity.Silymarin(50mg/kg.p.o.) was given as reference standard.Two doses of C. gigantea extract i.e.,100 mg/kg.p.o.and 200 mg/kg,p.o.were tested for hepatoprotective activity. The treatment was given for seven days and after 24 h of last treatment blood was collected from retro-orbital plexus and analysed for various serum parameters like serum glutamic-oxaloacetic transaminase(SGOT),serum glutamic pyruvic transaminase(SGPT),alkaline phosphatase(ALP),total bilirubin(TB)and total protein(TP)in different groups.Results:The paracetamol intoxication lead to histological and biochemical deteriorations.The treatment with methanolic leaf extract of C.gigantea reduced the elevated levels of SCOT,SGPT,ALP,TB and also reversed the hepatic damage towards normal which further supports the hepatoprotective activity of leaf extract of C.gigantea.Conclusions:The methanolic extract of leaves of C.gigantea at doses of 100 mg/kg bw and 200 mg/kg bw have significant effect on liver of paracetamol induced hepatotoxicity model in rats.展开更多
In the primitive era, humans benefited partially from plants and metals to treat microbial infections. Later these infections were cured with antibiotics but further suffered from resistance issues. In searching of an...In the primitive era, humans benefited partially from plants and metals to treat microbial infections. Later these infections were cured with antibiotics but further suffered from resistance issues. In searching of an alternative, researchers developed an adjuvant therapy but were hampered by spreading resistance. Subsequently, nanoparticles(NPs) were proposed to cease the multi-drug resistant bacteria but were hindered due to toxicity issues. Recently, a novel adjuvant therapy employed metals and botanicals into innovative nanotechnology as nano-antibiotics. The combination of green synthesized metallic NPs with antibiotics seems to be a viable platform to combat against MDR bacteria by alleviating resistance and toxicity. This review focuses on the primitive to present era dealings with bacterial resistance mechanisms, newer innovations of nanotechnology and their multiple mechanisms to combat resistance. In addition, special focus is paid on greener NPs as antibiotic carriers, and their future prospects of controlled release and toxicity study.展开更多
A high throughput ultra pressure liquid chromatography-mass spectrometry (UPLC-MS/MS) method with good sensitivity and selectivity has been developed and validated for simultaneous quantification of esomeprazole, ra...A high throughput ultra pressure liquid chromatography-mass spectrometry (UPLC-MS/MS) method with good sensitivity and selectivity has been developed and validated for simultaneous quantification of esomeprazole, rabeprazole and levosulpiride in human plasma using lansoprazole as internal standard (IS). The extraction method based on liquid-liquid extraction technique was used to extract the analytes and IS from of 50 μL of human plasma using methyl tert-butyl ether:ethyl acetate (80:20, v/v), which offers a high recovery. Chromatographic separation of analytes and IS was achieved on a Hypersil gold C18 column using gradient mobile phase consisting of 2 mM ammonium formate/acetonitrile. The flow rate was set at 0.5 mL/min to elute all the analytes and IS within 1.00 min runtime. Detection of target compounds was performed on a triple quadruple mass spectrometer by multiple reaction monitoring (MRM) mode via positive electrospray ionization (ESI). Method validation results demonstrated that the developed method has good precision and accuracy over the concentration ranges of 0.1-2000 ng/mL for each analyte. Stability of compounds was established in a battery of stability studies, i.e., bench top, autosampler, dry extract and long-term storage stability as well as freeze-thaw cycles. The validated method has been successfully applied to analyze human plasma samples for application in pharmaco- kinetic studies.展开更多
Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro...Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro antioxidant activity was evaluated for superoxide radical, Hydroxyl radical and DPPH radical scavenging activity.Three doses 200 mg/kg,400 mg/kg and 800 mg/kg of D.paniculala were tested for anti-inflammatory activity in Carrageenan induced rat paw edema model and paw thickness was measured every one hour up to 6 h. Results:The melhanolic leaf extract of D.paniculala produced dose dependent inhibition of Superoxide radical,Hydroxyl radical and OPPH radicals.In Carrageenan induced inflammation model,all three doses produced significant percentage inhibition of rat paw edema and 800 mg/kg dose produced maximum percent inhibition of rat paw edema(47.83%) at 3h compared to control group.Conclusions:In the present study we found that methanolic leaf extract of D.paniculata showed good in vitro antioxidant activity and in vivo anti-inflammatory activity in rats.展开更多
Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphyl...Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.展开更多
Objective:To evaluate bepato protective and antioxidant capacity of Melochia corchorifolia (M.corchorifolia)aerial part extracts.Methods:Antioxidant activitywas evaluated by using three free radicals(Superoxide,Hyd...Objective:To evaluate bepato protective and antioxidant capacity of Melochia corchorifolia (M.corchorifolia)aerial part extracts.Methods:Antioxidant activitywas evaluated by using three free radicals(Superoxide,Hydroxyl and DPPH) and hepatoprotective activity was assessed against CCl4 induced liver intoxication in ruts.Results:The extracts produced concentration dependent percentage protection in decrease of serum enzymes and percentage inhibition on free radicals.Among all extracts methanol extract showed better activity with percentage protection of SGOT(78.98%),SGPT(79.65%),ALP(82.48%) and total bilirubin(80.0%)levels against CCl4 liver intoxication and also methanolic extract showed better activity with IC50 values on superoxide. hydroxyl and DPPH radicals were 127μg.240μg and 179μg.Conclusions:From the results obtained during the study it could be concluded that M.corchorifolia aerial part extracts have antioxidant and hepaloprotective components.Further study is necessary for isolation and characterization of bioactive molecules which are responsible for hepatoprotective and antioxidant activity.展开更多
Objective:To evaluate the anti-proliferative and apoptogenic activity of ethyl acetate extract from the leaves of Memecylon edule(EtAc-LME) in MKN-74,NUGC gastric cancer cells and non cancerous gastric mucous cells(GE...Objective:To evaluate the anti-proliferative and apoptogenic activity of ethyl acetate extract from the leaves of Memecylon edule(EtAc-LME) in MKN-74,NUGC gastric cancer cells and non cancerous gastric mucous cells(GES-1),and to explore the mechanism of EtAc-LME induced apoptosis.Methods:The mechanism of EtAc-LME induced apoptosis was explored by analysing the activation of pro-caspases,PARP cleavage,expression of cytochrome-c (Cyt-c) was determined by western blotting,mRNA expression of Bcl-2,Bax by RT-PCR,loss of mitochondrial potential using DiOC6 dye,annexin binding assay and its influence on cell cycle arrest by flow cytometry.Results:The results indicated that EtAc-LME inhibited the gastric cancer cell growth in dose-dependent manner and cytotoxicity was more towards the gastric cancer cells(NUCC and MKN-74) compared to normal gastric cells(GES-1),suggesting more specific cytotoxicity to the malignant cells.Over expression of Cyt-c and subsequent activation of caspases-3 and down regulation of Bcl-2 and loss in mitochondrial potential in EtAc-LME treated MKN-74 and NUGC cells suggested that EtAc-LME induced apoptosis by mitochondrial dependent pathway.Conclusions:The present findings suggest that ethyl acetate extract of Memecylon edule induces apoptosis selectively in gastric cancer cells emphasizing the importance of this traditional medicine for its potential in the treatment of gastric cancer.展开更多
The purpose of this research was to apply statistical design for the preparation of a gastric floating tablet(GFT)of propranolol HCl and to investigate the effect of formulation variables on drug release and the buoya...The purpose of this research was to apply statistical design for the preparation of a gastric floating tablet(GFT)of propranolol HCl and to investigate the effect of formulation variables on drug release and the buoyancy properties of the delivery system.The contents of polyethylene oxide(PEO)WSR coagulant and sodium bicarbonate were used as independent variables in central composite design of the best formulation.Main effects and interaction terms of the formulation variables were evaluated quantitatively using a mathematical model approach showing that both independent variables have significant effects on floating lag time,%drug release at 1 h(D_(1h))and time required to release 90%of the drug(t_(90)).The desired function was used to optimize the response variables,each with a different target,and the observed responses were in good agreement with the experimental values.FTIR and DSC studies of the statistically optimized formulation revealed there was no chemical interaction between drug and polymer.The statistically optimized formulation released drug according to first order kinetics with a non-Fickian diffusion mechanism.Evaluation of the optimized formulation in vivo in human volunteers showed that the GFT was buoyant in gastric fluid and that its gastric residence time was enhanced in the fed but not the fasted state.展开更多
Paracetamol(PCM) hepatotoxicity is related to reactive oxygen species(ROS) formation and excessive oxidative stress; natural antioxidant compounds have been tested as an alternative therapy. This study evaluated the h...Paracetamol(PCM) hepatotoxicity is related to reactive oxygen species(ROS) formation and excessive oxidative stress; natural antioxidant compounds have been tested as an alternative therapy. This study evaluated the hepatoprotective activity of an alcoholic extract of Boswellia ovalifoliolata(BO) bark against PCM-induced hepatotoxicity. BO extract also demonstrated antioxidant activity in vitro, as well as scavenger activity against 2, 2-diphenyl-1-picrylhydrazyl. Administration of PCM caused a significant increase in the release of transaminases, alkaline phosphatase, and lactate dehydrogenase in serum. Significant enhancement in hepatic lipid peroxidation and marked depletion in reduced glutathione were observed after parac intoxication with severe alterations in liver histology. BO treatment was able to mitigate hepatic damage induced by acute intoxication of PCM and showed a pronounced protective effect against lipid peroxidation, deviated serum enzymatic variables, and maintained glutathione status toward control. The results clearly demonstrate the hepatoprotective effect of BO against the toxicity induced by PCM.展开更多
基金Supported by University Grants Commission.(No.Fdb/Pharmacy/C6102/2008-2010/5162)
文摘Objective:To investigate the hepatoprotective activity of methanolic leaf extract of Cyathea gigantea(C.gigantea)against paracetamol induced liver damage in rats.Methods:The hepatoprotective activity for plant extract was investigated for paracetamol induced hepatoxicity in rats.Wislar albino rats of either sex were divided into five groups of 6 animals each and are given orally the following treatment for seven days.The normal control group was given 1%Na.CMC 1mL/kg bw,p.o.Paracetamol at dose of 1g/kg bw,p.o.was given as toxic dose for inducing hepatoloxicity.Silymarin(50mg/kg.p.o.) was given as reference standard.Two doses of C. gigantea extract i.e.,100 mg/kg.p.o.and 200 mg/kg,p.o.were tested for hepatoprotective activity. The treatment was given for seven days and after 24 h of last treatment blood was collected from retro-orbital plexus and analysed for various serum parameters like serum glutamic-oxaloacetic transaminase(SGOT),serum glutamic pyruvic transaminase(SGPT),alkaline phosphatase(ALP),total bilirubin(TB)and total protein(TP)in different groups.Results:The paracetamol intoxication lead to histological and biochemical deteriorations.The treatment with methanolic leaf extract of C.gigantea reduced the elevated levels of SCOT,SGPT,ALP,TB and also reversed the hepatic damage towards normal which further supports the hepatoprotective activity of leaf extract of C.gigantea.Conclusions:The methanolic extract of leaves of C.gigantea at doses of 100 mg/kg bw and 200 mg/kg bw have significant effect on liver of paracetamol induced hepatotoxicity model in rats.
文摘In the primitive era, humans benefited partially from plants and metals to treat microbial infections. Later these infections were cured with antibiotics but further suffered from resistance issues. In searching of an alternative, researchers developed an adjuvant therapy but were hampered by spreading resistance. Subsequently, nanoparticles(NPs) were proposed to cease the multi-drug resistant bacteria but were hindered due to toxicity issues. Recently, a novel adjuvant therapy employed metals and botanicals into innovative nanotechnology as nano-antibiotics. The combination of green synthesized metallic NPs with antibiotics seems to be a viable platform to combat against MDR bacteria by alleviating resistance and toxicity. This review focuses on the primitive to present era dealings with bacterial resistance mechanisms, newer innovations of nanotechnology and their multiple mechanisms to combat resistance. In addition, special focus is paid on greener NPs as antibiotic carriers, and their future prospects of controlled release and toxicity study.
文摘A high throughput ultra pressure liquid chromatography-mass spectrometry (UPLC-MS/MS) method with good sensitivity and selectivity has been developed and validated for simultaneous quantification of esomeprazole, rabeprazole and levosulpiride in human plasma using lansoprazole as internal standard (IS). The extraction method based on liquid-liquid extraction technique was used to extract the analytes and IS from of 50 μL of human plasma using methyl tert-butyl ether:ethyl acetate (80:20, v/v), which offers a high recovery. Chromatographic separation of analytes and IS was achieved on a Hypersil gold C18 column using gradient mobile phase consisting of 2 mM ammonium formate/acetonitrile. The flow rate was set at 0.5 mL/min to elute all the analytes and IS within 1.00 min runtime. Detection of target compounds was performed on a triple quadruple mass spectrometer by multiple reaction monitoring (MRM) mode via positive electrospray ionization (ESI). Method validation results demonstrated that the developed method has good precision and accuracy over the concentration ranges of 0.1-2000 ng/mL for each analyte. Stability of compounds was established in a battery of stability studies, i.e., bench top, autosampler, dry extract and long-term storage stability as well as freeze-thaw cycles. The validated method has been successfully applied to analyze human plasma samples for application in pharmaco- kinetic studies.
文摘Objective:To investigate the antioxidant and anti-inflammatory activity of orally administered methanolic leaf extract of Dalbergia paniculala(D.paniculata) in Carrageenan induced inflammation in rats.Methods:In vitro antioxidant activity was evaluated for superoxide radical, Hydroxyl radical and DPPH radical scavenging activity.Three doses 200 mg/kg,400 mg/kg and 800 mg/kg of D.paniculala were tested for anti-inflammatory activity in Carrageenan induced rat paw edema model and paw thickness was measured every one hour up to 6 h. Results:The melhanolic leaf extract of D.paniculala produced dose dependent inhibition of Superoxide radical,Hydroxyl radical and OPPH radicals.In Carrageenan induced inflammation model,all three doses produced significant percentage inhibition of rat paw edema and 800 mg/kg dose produced maximum percent inhibition of rat paw edema(47.83%) at 3h compared to control group.Conclusions:In the present study we found that methanolic leaf extract of D.paniculata showed good in vitro antioxidant activity and in vivo anti-inflammatory activity in rats.
文摘Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.
基金The authors are grateful to the Principal,A.U.College of Pharmaceutical Sciences,Andhra University,Visakhapatnam,India for providing necessary facilities to carry out the work.
文摘Objective:To evaluate bepato protective and antioxidant capacity of Melochia corchorifolia (M.corchorifolia)aerial part extracts.Methods:Antioxidant activitywas evaluated by using three free radicals(Superoxide,Hydroxyl and DPPH) and hepatoprotective activity was assessed against CCl4 induced liver intoxication in ruts.Results:The extracts produced concentration dependent percentage protection in decrease of serum enzymes and percentage inhibition on free radicals.Among all extracts methanol extract showed better activity with percentage protection of SGOT(78.98%),SGPT(79.65%),ALP(82.48%) and total bilirubin(80.0%)levels against CCl4 liver intoxication and also methanolic extract showed better activity with IC50 values on superoxide. hydroxyl and DPPH radicals were 127μg.240μg and 179μg.Conclusions:From the results obtained during the study it could be concluded that M.corchorifolia aerial part extracts have antioxidant and hepaloprotective components.Further study is necessary for isolation and characterization of bioactive molecules which are responsible for hepatoprotective and antioxidant activity.
文摘Objective:To evaluate the anti-proliferative and apoptogenic activity of ethyl acetate extract from the leaves of Memecylon edule(EtAc-LME) in MKN-74,NUGC gastric cancer cells and non cancerous gastric mucous cells(GES-1),and to explore the mechanism of EtAc-LME induced apoptosis.Methods:The mechanism of EtAc-LME induced apoptosis was explored by analysing the activation of pro-caspases,PARP cleavage,expression of cytochrome-c (Cyt-c) was determined by western blotting,mRNA expression of Bcl-2,Bax by RT-PCR,loss of mitochondrial potential using DiOC6 dye,annexin binding assay and its influence on cell cycle arrest by flow cytometry.Results:The results indicated that EtAc-LME inhibited the gastric cancer cell growth in dose-dependent manner and cytotoxicity was more towards the gastric cancer cells(NUCC and MKN-74) compared to normal gastric cells(GES-1),suggesting more specific cytotoxicity to the malignant cells.Over expression of Cyt-c and subsequent activation of caspases-3 and down regulation of Bcl-2 and loss in mitochondrial potential in EtAc-LME treated MKN-74 and NUGC cells suggested that EtAc-LME induced apoptosis by mitochondrial dependent pathway.Conclusions:The present findings suggest that ethyl acetate extract of Memecylon edule induces apoptosis selectively in gastric cancer cells emphasizing the importance of this traditional medicine for its potential in the treatment of gastric cancer.
基金The author M.V.Srikanth is thankful to the University Grants Commission,India for awarding a Senior Research Fellowship to carry out this project.
文摘The purpose of this research was to apply statistical design for the preparation of a gastric floating tablet(GFT)of propranolol HCl and to investigate the effect of formulation variables on drug release and the buoyancy properties of the delivery system.The contents of polyethylene oxide(PEO)WSR coagulant and sodium bicarbonate were used as independent variables in central composite design of the best formulation.Main effects and interaction terms of the formulation variables were evaluated quantitatively using a mathematical model approach showing that both independent variables have significant effects on floating lag time,%drug release at 1 h(D_(1h))and time required to release 90%of the drug(t_(90)).The desired function was used to optimize the response variables,each with a different target,and the observed responses were in good agreement with the experimental values.FTIR and DSC studies of the statistically optimized formulation revealed there was no chemical interaction between drug and polymer.The statistically optimized formulation released drug according to first order kinetics with a non-Fickian diffusion mechanism.Evaluation of the optimized formulation in vivo in human volunteers showed that the GFT was buoyant in gastric fluid and that its gastric residence time was enhanced in the fed but not the fasted state.
文摘Paracetamol(PCM) hepatotoxicity is related to reactive oxygen species(ROS) formation and excessive oxidative stress; natural antioxidant compounds have been tested as an alternative therapy. This study evaluated the hepatoprotective activity of an alcoholic extract of Boswellia ovalifoliolata(BO) bark against PCM-induced hepatotoxicity. BO extract also demonstrated antioxidant activity in vitro, as well as scavenger activity against 2, 2-diphenyl-1-picrylhydrazyl. Administration of PCM caused a significant increase in the release of transaminases, alkaline phosphatase, and lactate dehydrogenase in serum. Significant enhancement in hepatic lipid peroxidation and marked depletion in reduced glutathione were observed after parac intoxication with severe alterations in liver histology. BO treatment was able to mitigate hepatic damage induced by acute intoxication of PCM and showed a pronounced protective effect against lipid peroxidation, deviated serum enzymatic variables, and maintained glutathione status toward control. The results clearly demonstrate the hepatoprotective effect of BO against the toxicity induced by PCM.