Cancer is a leading cause of death globally,with limited treatment options and several limitations.Chemotherapeutic agents often result in toxicity which long-term conventional treatment.Phytochemicals are natural con...Cancer is a leading cause of death globally,with limited treatment options and several limitations.Chemotherapeutic agents often result in toxicity which long-term conventional treatment.Phytochemicals are natural constituents that are more effective in treating various diseases with less toxicity than the chemotherapeutic agents providing alternative therapeutic approaches to minimize the resistance.These phytoconstituents act in several ways and deliver optimum effectiveness against cancer.Nevertheless,the effectiveness of phyto-formulations in the management of cancers may be constrained due to challenges related to inadequate solubility,bioavailability,and stability.Nanotechnology presents a promising avenue for transforming current cancer treatment methods through the incorporation of phytochemicals into nanosystems,which possess a range of advantageous characteristics such as biocompatibility,targeted and sustained release capabilities,and enhanced protective effects.This holds significant potential for future advancements in cancer management.Herein,this review aims to provide intensive literature on diverse nanocarriers,highlighting their applications as cargos for phytocompounds in cancer.Moreover,it offers an overview of the current advancements in the respective field,emphasizing the characteristics that contribute to favourable outcomes in both in vitro and in vivo settings.Lastly,clinical development and regulatory concerns are also discussed to check on the transformation of the concept as a promising strategy for combination therapy of phytochemicals and chemotherapeutics that could lead to cancer management in the future.展开更多
In a brand new era,with chaotic scenario that exists within the world,people are undermined with diverse psychological assaults.There have been numerous sensible approaches on the way to understand and lessen those at...In a brand new era,with chaotic scenario that exists within the world,people are undermined with diverse psychological assaults.There have been numerous sensible approaches on the way to understand and lessen those attacks.Bioscrypt developments have verified to be one of the beneficial approaches for intercepting these troubles.Identifying recognition through human iris organ is said as one of the well-known biometric strategies because of its reliability and higher accurate return in comparison to different developments.Reviewing beyond literatures,terrible imaging condition,low flexibility of version,and small length iris image dataset are the constraints desiring solutions.Among these kinds of developments,the iris popularity structures are suitable gear for the human identification.Iris popularity has been an energetic studies location for the duration of previous couple of decades,due to its extensive packages in the areas,from airports to native land protection border protection.In the past,various functions and methods for iris recognition have been presented.Despite of the very fact that there are many approaches published in this field,there are still liberal amount of problems in this methodology like tedious and computational intricacy.We suggest an all-encompassing deep learning architecture for iris recognition supported by a genetic algorithm and a wavelet transformation,which may jointly learn the feature representation and perform recognition to realize high efficiency.With just a few training photos from each class,we train our model on a well-known iris recognition dataset and demonstrate improvements over prior methods.We think that this architecture can be frequently employed for various biometric recognition jobs,assisting in the development of a more scalable and precise system.The exploratory aftereffects of the proposed technique uncover that the strategy is effective inside the iris acknowledgment.展开更多
Upconversion nanoparticles(UCNPs)doped with lanthanides can convert near-infrared excitation into UV and visible emissions.Because of their relatively high emission efficiency,UCNPs are appealing materials for use in ...Upconversion nanoparticles(UCNPs)doped with lanthanides can convert near-infrared excitation into UV and visible emissions.Because of their relatively high emission efficiency,UCNPs are appealing materials for use in a variety of sectors.UCNPs are known for low auto-fluorescence,excellent chemical and thermal photo-stability,deep tissue penetration,exceptional biocompatibility,low toxicity,color purity,and ease of surface functionalization.In this review,we explain a few recent strategies to boost the efficiency and luminescence of upconversion nanoparticles and minimize quenching by fabricating them as core/shell,nanofibers,or heavily doped lanthanides.Applications of UCNPs in drug delivery,Photodynamic therapy(PDT),biosensors,bioimaging,and optogenetics are also discussed along with their mechanism of action.Our motivation for this review is to understand the working mechanism of UCNPs and their applications in various fields.展开更多
Objective:To evaluate the effect of formononetin on type 2 diabetic cardiomyopathy.Methods:Diabetes was induced by feeding high-fat diet for 2 weeks and administration of 35 mg/kg of streptozotocin in rats.Formononeti...Objective:To evaluate the effect of formononetin on type 2 diabetic cardiomyopathy.Methods:Diabetes was induced by feeding high-fat diet for 2 weeks and administration of 35 mg/kg of streptozotocin in rats.Formononetin was administered at 10,20 and 40 mg/kg for 16 weeks once a day.Plasma glucose,lipid parameters,and cardiac markers in blood samples were measured.Body weight and relative heart weight were recorded.Hemodynamic parameters,oxidative stress parameters and silence information regulator 1(SIRT1)expression in cardiac tissue were estimated.Histopathological changes in cardiac tissue were also observed.Results:Formononetin significantly reduced the levels of glucose,triglycerides,cholesterol,low density lipoprotein,creatine kinaseMB,lactate dehydrogenase and aspartate aminotransferase.In addition,formononetin significantly improved hemodynamic parameters,alleviated oxidative stress and increased SIRT1 expression.Conclusions:The study indicates that formononetin can improve hyperglycemia and hyperlipemia,reduce oxidative stress and increase SIRT1 expression.It can be a potential therapeutic agent for diabetic cardiomyopathy.展开更多
Objective: To study the effects of aqueous extract of Gmelina arborea bark on normoglycemic levels and streptozotocin (STZ) induced diabetes in rats. Methods: After single administration of the aqueous extract, plasma...Objective: To study the effects of aqueous extract of Gmelina arborea bark on normoglycemic levels and streptozotocin (STZ) induced diabetes in rats. Methods: After single administration of the aqueous extract, plasma glucose level was determined up to 6 h. In subacute study, the aqueous extract was administered for 28 d and plasma glucose level was determined weekly. The diabetes was induced in rats by the intraperitoneal injection of STZ at a dose of 55 mg/kg body weight. The diabetic animals were divided into four groups containing six in each: Group 栺 diabetic control, Group 栻 and 栿 treated with the aqueous extract respectively at a dose of 250 and 500 mg/kg body weight once daily and Group 桇 treated with glibenclamide at a dose of 0.6 mg/kg body weight once daily. In acute study, the aqueous extract and glibenclamide were administered orally to rats. Plasma glucose levels were determined at 30, 60, 120, 240 and 360 min after the administration of the test samples. To study subacute effects, test samples (the aqueous extract and glibenclamide) were administered for 28 d consecutively. The effects of each test sample on plasma glucose level, body weight as well as food and water intake were also monitored weekly. The oral glucose tolerance test and biochemical indicators were estimated on day 28. Results: The aqueous extract did not significantly decrease the plasma glucose level in the normoglycemic rats as shown by the acute and subacute assays. However, after oral administration of the aqueous extract, the plasma glucose level was significantly ( P<0.001) decreased in the diabetic rats in the acute study. The long-term administration of the aqueous extract significantly ( P<0.001) reduced plasma glucose levels of the diabetic rats. Additionally, the aqueous extract also reduced loss of body weight and significantly decreased food and water intake in the diabetic animals. Nevertheless, no effects on biochemical indicators were observed at the selected doses. Conclusions: The aqueous extract of Gmelina arborea bark had antihyperglycemic activity against STZ induced diabetes in rats, after single and subacute oral administration. Moreover, it did not show significant glucose lowering effect in normoglycemic rats.展开更多
Iris recognition enjoys universality, high degree of uniqueness and moderate user co-operation. This makes iris recognition systems unavoidable in emerging security ＆ authentication mechanisms. An iris recognition sy...Iris recognition enjoys universality, high degree of uniqueness and moderate user co-operation. This makes iris recognition systems unavoidable in emerging security ＆ authentication mechanisms. An iris recognition system based on vector quantization （VQ） techniques is proposed and its performance is compared with the discrete cosine transform （DCT）. The proposed system does not need any pre-processing and segmentation of the iris. We have tested Linde-Buzo- Gray （LBG）, Kekre＇s proportionate error （KPE） algorithm and Kekre＇s fast codebook generation （KFCG） algorithm for the clustering purpose. Proposed vector quantization based method using KFCG requires 99.99% less computations as that of full 2-dimensional DCT. Further, the KFCG method gives better performance with the accuracy of 89.10% outperforming DCT that gives accuracy around 66.10%.展开更多
The aim of the present investigation was to demonstrate an approach involving use of liquid chromatography(LC) and liquid chromatography-mass spectrometry(LC–MS) to separate, identify and characterize very small quan...The aim of the present investigation was to demonstrate an approach involving use of liquid chromatography(LC) and liquid chromatography-mass spectrometry(LC–MS) to separate, identify and characterize very small quantities of degradation products(DPs) of acebutolol without their isolation from the reaction mixtures. The drug was subjected to oxidative, hydrolytic, thermal and photolytic stress conditions as per International Conference on Harmonization(ICH) guideline Q1 A(R2). Among all the stress conditions the drug was found to be labile in hydrolytic(acidic & basic) and photolytic stress conditions, while it was stable in water-induced hydrolysis, oxidative and thermal stress conditions. A total of four degradation products were formed. A C18 column was employed for the separation of all the DPs on a gradient mode by using high-performance liquid chromatography(HPLC). All the DPs were characterized with the help of their fragmentation pattern and the masses obtained upon LC–MS/MS and MSnanalysis. All the hitherto unknown degradation products were identified as 1-(2-(2-hydroxy-3-(isopropylamino)propoxy)-5-(amino)phenyl)ethanone(DP-I), N-(4-(2-hydroxy-3-(isopropylamino)propoxy)-3-acetylphenyl)acrylamide(DP-II), 1-(2-(2-hydroxy-3-(isopropylamino)propoxy)-5-(hydroxymethylamino)phenyl)ethanone(DP-III) and 1-(6-(2-hydroxy-3-(isopropylamino)propoxy)-2,3-dihydro-2-propylbenzo[d]oxazol-5-yl)ethanone(DP-IV). Finally the in-silico carcinogenicity and hepatotoxicity predictions of the drug and all the DPs were performed by using toxicity prediction softwares viz., TOPKAT, LAZAR and Discovery Studio ADMET. The results of in-silico toxicity studies revealed that acebutolol(0.967) and DP-I(0.986) were found to be carcinogenic, while acebutolol(0.490) and DP-IV(0.437) were found to be hepatotoxic.展开更多
Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antima...Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antimalarial activities, but has some limitations. Therefore, new strategies are to be implemented for optimal utilization of artemisinin to improve its therapeutic effectiveness and to overcome its limitations. The present review focuses on present scenario of malaria and pharmacological as well as analytical aspects of artemisinin. Data from 2000 to 2018 were collected from NCBI for understanding the various analytical techniques used for estimation of artemisinin. This review will reveal the facts about artemisinin which can be utilized to develop novel drug delivery system either in a combination or as alone for the wellbeing of the patients suffering from malaria.展开更多
Metformin hydrochloride and sitagliptin phosphate is the common combination among diabetic drugs.Available dosage forms cannot avoid the dose dumping which leads to the complication such as lactic acidosis,gastrointes...Metformin hydrochloride and sitagliptin phosphate is the common combination among diabetic drugs.Available dosage forms cannot avoid the dose dumping which leads to the complication such as lactic acidosis,gastrointestinal complication,and severe hypoglycemia.Metformin hydrochloride has a very short half-life,i.e.4 hrs,and thus fails to give action for the long period.This leads to the increase number of dosings per day.Single-unit formulations contain the active ingredient within the single tablet or capsule,whereasmultiple-unit dosage forms comprise a number of discrete particles that are combined into one dosage unit.展开更多
Separation of copper and nickel by liquid-liquid extraction from aqueous solutions was studied using LIX 664N in kerosene as solvent. Both metals were taken in their sulfate form and ratio of copper to nickel in feed ...Separation of copper and nickel by liquid-liquid extraction from aqueous solutions was studied using LIX 664N in kerosene as solvent. Both metals were taken in their sulfate form and ratio of copper to nickel in feed solutions was maintained as 10:1. LIX 664N concentration in kerosene was varied from 10% to 40% (v/v) and its effect was studied on percent extraction of copper and nickel for organic to aqueous (O:A) phase ratio of 2:1 at pH 2. Experimental results showed that at pH 2, copper was selectively extracted from its mixture with nickel. Selectivity for copper extraction was as high as 6000 with 40% LIX 664N. Calculations using extraction isotherm indicate almost complete recovery of copper in two stages with O:A ratio of 1:1 and in one stage with O:A ratio of 2:1. After extraction of copper, the pH of raffinate containing nickel was adjusted to a value of 9 by addition of ammonia solution. The effect of LIX 664N concentration on extraction of nickel was studied. Up to 80% nickel could be extracted with 30% LIX 664N at O:A phase ratio of 2:1. Stripping of copper from the organic phase with 180 g/l sulfuric acid at O:A phase ratio of 1:1 gave 98.5% copper recovery in a two-stage operation.展开更多
Process intensification using liquid emulsion membranes (LEMs) for extraction of copper has been studied in this work. In LEM process the extraction and stripping processes are combined in one stage. The solubility of...Process intensification using liquid emulsion membranes (LEMs) for extraction of copper has been studied in this work. In LEM process the extraction and stripping processes are combined in one stage. The solubility of the solute or the chemical affinity between the solute and carrier reagent in the membrane results in the separation of the solute from the feed mixture. In this work the membrane phase comprised of LIX 664N as the extractant dissolved in kerosene and Span 80 as surfactant. The stripping phase was sulfuric acid with 180 g/l concentration and feed phase had copper concentration of 3.5 g/l. Effect of various process parameters such as batch contact time, speed of agitation, W:O ratio and treat ratio has been experimentally investigated to get better insight of the process. The maximum enrichment of copper in the internal phase obtained was 11.6 times with batch contact time of 10 minutes, agitation speed of 300 rpm and treat ratio of 6:1.展开更多
In the present study,comprehensive stress testing of amlodipine（AM） was carried out according to International Conference on Harmonization（ICH） Q1A（R2） guideline.AM was subjected to acidic,neutral and alkaline h...In the present study,comprehensive stress testing of amlodipine（AM） was carried out according to International Conference on Harmonization（ICH） Q1A（R2） guideline.AM was subjected to acidic,neutral and alkaline hydrolysis,oxidation,photolysis and thermal stress conditions.The drug showed instability in acidic and alkaline conditions,while it remained stable to neutral,oxidative,light and thermal stress.A total of nine degradation products（DPs） were formed from AM.which could be separated by the developed gradient LC method on a C18 column.The products formed under various stress conditions were investigated by LC-MS/MS analysis.The previously developed LC method was suitably modified for LC-MS/MS studies by replacing phosphate buffer with ammonium acetate buffer of the same concentration（pH 5.0）.A complete fragmentation pathway of the drug was first established to characterize all the degradation products using LC-MS/MS and multi-stage mass（MS^n） fragmentation studies.The obtained mass values were used to study elemental compositions,and the total information helped with the identification of DPs.along with its degradation pathway.展开更多
Objective:To investigate the effect of aloin against chronic constriction injury(CCI)-induced neuropathic pain in rats.Methods:Rats were randomly divided into 7 groups:GroupⅠ(normal control),GroupⅡ(sham-operated),Gr...Objective:To investigate the effect of aloin against chronic constriction injury(CCI)-induced neuropathic pain in rats.Methods:Rats were randomly divided into 7 groups:GroupⅠ(normal control),GroupⅡ(sham-operated),GroupⅢ(CCI control)and GroupⅣ,Ⅴ,Ⅵ,andⅦ,which underwent CCI surgery and then were administered with aloin(5 mg/kg,p.o.;25 mg/kg,p.o.;125 mg/kg,p.o.)and gabapentin(50 mg/kg,p.o.),respectively for 14 days.Peripheral neuropathy was induced by silk ligatures(4-0)loosely placed around the sciatic nerve.Nociceptive thresholds against mechanical stimuli(Von-Frey filaments)and thermal stimuli(12℃and 40℃)were measured at midplantar paw region ipsilateral to the compressed nerve on day-3,7,11,and 14.The concentration of cytokines including tumor necrosis factor-α(TNF-α),interleukin-6,and interleukin-1βwas estimated at day-7.At day 14,motor nerve conduction velocity was determined under urethane anesthesia(1.25 g/kg).Oxidative stress parameters(malondiadehyde,glutathione,catalase,and superoxide dismutase)were estimated in sciatic nerve homogenates at day 14.Representative nerve samples were processed for histological investigations.Results:Aloin significantly reduced CCI-induced mechanical and thermal allodynia.It also improved motor nerve conduction velocity and decreased oxidative stress in nerve tissues.In addition,it decreased pro-inflammatory cytokine levels and restored the histoarchitecture of compressed sciatic nerve.Conclusions:Aloin mitigates CCI-induced neuropathic pain in rats by inhibiting oxidative stress and pro-inflammatory cytokines in the afflicted sciatic nerve.展开更多
文摘Cancer is a leading cause of death globally,with limited treatment options and several limitations.Chemotherapeutic agents often result in toxicity which long-term conventional treatment.Phytochemicals are natural constituents that are more effective in treating various diseases with less toxicity than the chemotherapeutic agents providing alternative therapeutic approaches to minimize the resistance.These phytoconstituents act in several ways and deliver optimum effectiveness against cancer.Nevertheless,the effectiveness of phyto-formulations in the management of cancers may be constrained due to challenges related to inadequate solubility,bioavailability,and stability.Nanotechnology presents a promising avenue for transforming current cancer treatment methods through the incorporation of phytochemicals into nanosystems,which possess a range of advantageous characteristics such as biocompatibility,targeted and sustained release capabilities,and enhanced protective effects.This holds significant potential for future advancements in cancer management.Herein,this review aims to provide intensive literature on diverse nanocarriers,highlighting their applications as cargos for phytocompounds in cancer.Moreover,it offers an overview of the current advancements in the respective field,emphasizing the characteristics that contribute to favourable outcomes in both in vitro and in vivo settings.Lastly,clinical development and regulatory concerns are also discussed to check on the transformation of the concept as a promising strategy for combination therapy of phytochemicals and chemotherapeutics that could lead to cancer management in the future.
文摘In a brand new era,with chaotic scenario that exists within the world,people are undermined with diverse psychological assaults.There have been numerous sensible approaches on the way to understand and lessen those attacks.Bioscrypt developments have verified to be one of the beneficial approaches for intercepting these troubles.Identifying recognition through human iris organ is said as one of the well-known biometric strategies because of its reliability and higher accurate return in comparison to different developments.Reviewing beyond literatures,terrible imaging condition,low flexibility of version,and small length iris image dataset are the constraints desiring solutions.Among these kinds of developments,the iris popularity structures are suitable gear for the human identification.Iris popularity has been an energetic studies location for the duration of previous couple of decades,due to its extensive packages in the areas,from airports to native land protection border protection.In the past,various functions and methods for iris recognition have been presented.Despite of the very fact that there are many approaches published in this field,there are still liberal amount of problems in this methodology like tedious and computational intricacy.We suggest an all-encompassing deep learning architecture for iris recognition supported by a genetic algorithm and a wavelet transformation,which may jointly learn the feature representation and perform recognition to realize high efficiency.With just a few training photos from each class,we train our model on a well-known iris recognition dataset and demonstrate improvements over prior methods.We think that this architecture can be frequently employed for various biometric recognition jobs,assisting in the development of a more scalable and precise system.The exploratory aftereffects of the proposed technique uncover that the strategy is effective inside the iris acknowledgment.
基金SVKM's NMIMS University(PhD/20.08.2020)for providing fellowship to carry out research。
文摘Upconversion nanoparticles(UCNPs)doped with lanthanides can convert near-infrared excitation into UV and visible emissions.Because of their relatively high emission efficiency,UCNPs are appealing materials for use in a variety of sectors.UCNPs are known for low auto-fluorescence,excellent chemical and thermal photo-stability,deep tissue penetration,exceptional biocompatibility,low toxicity,color purity,and ease of surface functionalization.In this review,we explain a few recent strategies to boost the efficiency and luminescence of upconversion nanoparticles and minimize quenching by fabricating them as core/shell,nanofibers,or heavily doped lanthanides.Applications of UCNPs in drug delivery,Photodynamic therapy(PDT),biosensors,bioimaging,and optogenetics are also discussed along with their mechanism of action.Our motivation for this review is to understand the working mechanism of UCNPs and their applications in various fields.
文摘Objective:To evaluate the effect of formononetin on type 2 diabetic cardiomyopathy.Methods:Diabetes was induced by feeding high-fat diet for 2 weeks and administration of 35 mg/kg of streptozotocin in rats.Formononetin was administered at 10,20 and 40 mg/kg for 16 weeks once a day.Plasma glucose,lipid parameters,and cardiac markers in blood samples were measured.Body weight and relative heart weight were recorded.Hemodynamic parameters,oxidative stress parameters and silence information regulator 1(SIRT1)expression in cardiac tissue were estimated.Histopathological changes in cardiac tissue were also observed.Results:Formononetin significantly reduced the levels of glucose,triglycerides,cholesterol,low density lipoprotein,creatine kinaseMB,lactate dehydrogenase and aspartate aminotransferase.In addition,formononetin significantly improved hemodynamic parameters,alleviated oxidative stress and increased SIRT1 expression.Conclusions:The study indicates that formononetin can improve hyperglycemia and hyperlipemia,reduce oxidative stress and increase SIRT1 expression.It can be a potential therapeutic agent for diabetic cardiomyopathy.
文摘Objective: To study the effects of aqueous extract of Gmelina arborea bark on normoglycemic levels and streptozotocin (STZ) induced diabetes in rats. Methods: After single administration of the aqueous extract, plasma glucose level was determined up to 6 h. In subacute study, the aqueous extract was administered for 28 d and plasma glucose level was determined weekly. The diabetes was induced in rats by the intraperitoneal injection of STZ at a dose of 55 mg/kg body weight. The diabetic animals were divided into four groups containing six in each: Group 栺 diabetic control, Group 栻 and 栿 treated with the aqueous extract respectively at a dose of 250 and 500 mg/kg body weight once daily and Group 桇 treated with glibenclamide at a dose of 0.6 mg/kg body weight once daily. In acute study, the aqueous extract and glibenclamide were administered orally to rats. Plasma glucose levels were determined at 30, 60, 120, 240 and 360 min after the administration of the test samples. To study subacute effects, test samples (the aqueous extract and glibenclamide) were administered for 28 d consecutively. The effects of each test sample on plasma glucose level, body weight as well as food and water intake were also monitored weekly. The oral glucose tolerance test and biochemical indicators were estimated on day 28. Results: The aqueous extract did not significantly decrease the plasma glucose level in the normoglycemic rats as shown by the acute and subacute assays. However, after oral administration of the aqueous extract, the plasma glucose level was significantly ( P<0.001) decreased in the diabetic rats in the acute study. The long-term administration of the aqueous extract significantly ( P<0.001) reduced plasma glucose levels of the diabetic rats. Additionally, the aqueous extract also reduced loss of body weight and significantly decreased food and water intake in the diabetic animals. Nevertheless, no effects on biochemical indicators were observed at the selected doses. Conclusions: The aqueous extract of Gmelina arborea bark had antihyperglycemic activity against STZ induced diabetes in rats, after single and subacute oral administration. Moreover, it did not show significant glucose lowering effect in normoglycemic rats.
文摘Iris recognition enjoys universality, high degree of uniqueness and moderate user co-operation. This makes iris recognition systems unavoidable in emerging security ＆ authentication mechanisms. An iris recognition system based on vector quantization （VQ） techniques is proposed and its performance is compared with the discrete cosine transform （DCT）. The proposed system does not need any pre-processing and segmentation of the iris. We have tested Linde-Buzo- Gray （LBG）, Kekre＇s proportionate error （KPE） algorithm and Kekre＇s fast codebook generation （KFCG） algorithm for the clustering purpose. Proposed vector quantization based method using KFCG requires 99.99% less computations as that of full 2-dimensional DCT. Further, the KFCG method gives better performance with the accuracy of 89.10% outperforming DCT that gives accuracy around 66.10%.
文摘The aim of the present investigation was to demonstrate an approach involving use of liquid chromatography(LC) and liquid chromatography-mass spectrometry(LC–MS) to separate, identify and characterize very small quantities of degradation products(DPs) of acebutolol without their isolation from the reaction mixtures. The drug was subjected to oxidative, hydrolytic, thermal and photolytic stress conditions as per International Conference on Harmonization(ICH) guideline Q1 A(R2). Among all the stress conditions the drug was found to be labile in hydrolytic(acidic & basic) and photolytic stress conditions, while it was stable in water-induced hydrolysis, oxidative and thermal stress conditions. A total of four degradation products were formed. A C18 column was employed for the separation of all the DPs on a gradient mode by using high-performance liquid chromatography(HPLC). All the DPs were characterized with the help of their fragmentation pattern and the masses obtained upon LC–MS/MS and MSnanalysis. All the hitherto unknown degradation products were identified as 1-(2-(2-hydroxy-3-(isopropylamino)propoxy)-5-(amino)phenyl)ethanone(DP-I), N-(4-(2-hydroxy-3-(isopropylamino)propoxy)-3-acetylphenyl)acrylamide(DP-II), 1-(2-(2-hydroxy-3-(isopropylamino)propoxy)-5-(hydroxymethylamino)phenyl)ethanone(DP-III) and 1-(6-(2-hydroxy-3-(isopropylamino)propoxy)-2,3-dihydro-2-propylbenzo[d]oxazol-5-yl)ethanone(DP-IV). Finally the in-silico carcinogenicity and hepatotoxicity predictions of the drug and all the DPs were performed by using toxicity prediction softwares viz., TOPKAT, LAZAR and Discovery Studio ADMET. The results of in-silico toxicity studies revealed that acebutolol(0.967) and DP-I(0.986) were found to be carcinogenic, while acebutolol(0.490) and DP-IV(0.437) were found to be hepatotoxic.
文摘Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antimalarial activities, but has some limitations. Therefore, new strategies are to be implemented for optimal utilization of artemisinin to improve its therapeutic effectiveness and to overcome its limitations. The present review focuses on present scenario of malaria and pharmacological as well as analytical aspects of artemisinin. Data from 2000 to 2018 were collected from NCBI for understanding the various analytical techniques used for estimation of artemisinin. This review will reveal the facts about artemisinin which can be utilized to develop novel drug delivery system either in a combination or as alone for the wellbeing of the patients suffering from malaria.
文摘Metformin hydrochloride and sitagliptin phosphate is the common combination among diabetic drugs.Available dosage forms cannot avoid the dose dumping which leads to the complication such as lactic acidosis,gastrointestinal complication,and severe hypoglycemia.Metformin hydrochloride has a very short half-life,i.e.4 hrs,and thus fails to give action for the long period.This leads to the increase number of dosings per day.Single-unit formulations contain the active ingredient within the single tablet or capsule,whereasmultiple-unit dosage forms comprise a number of discrete particles that are combined into one dosage unit.
文摘Separation of copper and nickel by liquid-liquid extraction from aqueous solutions was studied using LIX 664N in kerosene as solvent. Both metals were taken in their sulfate form and ratio of copper to nickel in feed solutions was maintained as 10:1. LIX 664N concentration in kerosene was varied from 10% to 40% (v/v) and its effect was studied on percent extraction of copper and nickel for organic to aqueous (O:A) phase ratio of 2:1 at pH 2. Experimental results showed that at pH 2, copper was selectively extracted from its mixture with nickel. Selectivity for copper extraction was as high as 6000 with 40% LIX 664N. Calculations using extraction isotherm indicate almost complete recovery of copper in two stages with O:A ratio of 1:1 and in one stage with O:A ratio of 2:1. After extraction of copper, the pH of raffinate containing nickel was adjusted to a value of 9 by addition of ammonia solution. The effect of LIX 664N concentration on extraction of nickel was studied. Up to 80% nickel could be extracted with 30% LIX 664N at O:A phase ratio of 2:1. Stripping of copper from the organic phase with 180 g/l sulfuric acid at O:A phase ratio of 1:1 gave 98.5% copper recovery in a two-stage operation.
文摘Process intensification using liquid emulsion membranes (LEMs) for extraction of copper has been studied in this work. In LEM process the extraction and stripping processes are combined in one stage. The solubility of the solute or the chemical affinity between the solute and carrier reagent in the membrane results in the separation of the solute from the feed mixture. In this work the membrane phase comprised of LIX 664N as the extractant dissolved in kerosene and Span 80 as surfactant. The stripping phase was sulfuric acid with 180 g/l concentration and feed phase had copper concentration of 3.5 g/l. Effect of various process parameters such as batch contact time, speed of agitation, W:O ratio and treat ratio has been experimentally investigated to get better insight of the process. The maximum enrichment of copper in the internal phase obtained was 11.6 times with batch contact time of 10 minutes, agitation speed of 300 rpm and treat ratio of 6:1.
文摘In the present study,comprehensive stress testing of amlodipine（AM） was carried out according to International Conference on Harmonization（ICH） Q1A（R2） guideline.AM was subjected to acidic,neutral and alkaline hydrolysis,oxidation,photolysis and thermal stress conditions.The drug showed instability in acidic and alkaline conditions,while it remained stable to neutral,oxidative,light and thermal stress.A total of nine degradation products（DPs） were formed from AM.which could be separated by the developed gradient LC method on a C18 column.The products formed under various stress conditions were investigated by LC-MS/MS analysis.The previously developed LC method was suitably modified for LC-MS/MS studies by replacing phosphate buffer with ammonium acetate buffer of the same concentration（pH 5.0）.A complete fragmentation pathway of the drug was first established to characterize all the degradation products using LC-MS/MS and multi-stage mass（MS^n） fragmentation studies.The obtained mass values were used to study elemental compositions,and the total information helped with the identification of DPs.along with its degradation pathway.
文摘Objective:To investigate the effect of aloin against chronic constriction injury(CCI)-induced neuropathic pain in rats.Methods:Rats were randomly divided into 7 groups:GroupⅠ(normal control),GroupⅡ(sham-operated),GroupⅢ(CCI control)and GroupⅣ,Ⅴ,Ⅵ,andⅦ,which underwent CCI surgery and then were administered with aloin(5 mg/kg,p.o.;25 mg/kg,p.o.;125 mg/kg,p.o.)and gabapentin(50 mg/kg,p.o.),respectively for 14 days.Peripheral neuropathy was induced by silk ligatures(4-0)loosely placed around the sciatic nerve.Nociceptive thresholds against mechanical stimuli(Von-Frey filaments)and thermal stimuli(12℃and 40℃)were measured at midplantar paw region ipsilateral to the compressed nerve on day-3,7,11,and 14.The concentration of cytokines including tumor necrosis factor-α(TNF-α),interleukin-6,and interleukin-1βwas estimated at day-7.At day 14,motor nerve conduction velocity was determined under urethane anesthesia(1.25 g/kg).Oxidative stress parameters(malondiadehyde,glutathione,catalase,and superoxide dismutase)were estimated in sciatic nerve homogenates at day 14.Representative nerve samples were processed for histological investigations.Results:Aloin significantly reduced CCI-induced mechanical and thermal allodynia.It also improved motor nerve conduction velocity and decreased oxidative stress in nerve tissues.In addition,it decreased pro-inflammatory cytokine levels and restored the histoarchitecture of compressed sciatic nerve.Conclusions:Aloin mitigates CCI-induced neuropathic pain in rats by inhibiting oxidative stress and pro-inflammatory cytokines in the afflicted sciatic nerve.
