A new variant,JN.1,stemming from the omicron subvariant BA.2.86,garnered the attention of the World Health Organization(WHO)as a"variant of interest."Despite its rapid global spread,especially in the US,Cana...A new variant,JN.1,stemming from the omicron subvariant BA.2.86,garnered the attention of the World Health Organization(WHO)as a"variant of interest."Despite its rapid global spread,especially in the US,Canada,France,Singapore,Sweden[1],and the UK,JN.1 is considered to pose minimal danger.Current vaccinations are believed to remain effective against it.The WHO underscores the importance of maintaining immunization records amid co-occurring respiratory illnesses,and epidemiologists recommend monitoring hospitalizations,particularly in areas with low vaccination rates.展开更多
Crystal engineering concept has been utilized to modify the physico-chemical parameters of a naturally occurring alkaloid, quinine sulphate, by exploring its H-bond interactions to generate different forms. Quinine su...Crystal engineering concept has been utilized to modify the physico-chemical parameters of a naturally occurring alkaloid, quinine sulphate, by exploring its H-bond interactions to generate different forms. Quinine sulphate is found to exist in four different crystal forms. The Forms I and II depict endo/exo events suggesting conversion of metastable low melting forms to higher melting and stable form indicated by sharp melting endotherms. The low melting form IL is found to be monotropically related to high melting Form IH while low melting Form IIL is enantiotropically related to high melting Form IIH. The Form III and IV showed broad endotherms accompanied by mass loss in TGA prior to melting indicating the existence of solvatomorphism. The solvent molecules are tightly bound in the crystal lattice of the drug molecules which is shown by high values of the binding energies of the solvents in these two forms. The enthalpy of solution was found to be endothermic for all the forms which followed the order: Form O > Form II > Form III > Form I > Form IV and is further related to the lattice energy suggesting Form II to be least crystalline. The solubility for Form II was found to be highest with maximum release rate in dissolution studies. The effectiveness of new polymorphic forms was confirmed by performing in vivo antimalarial activity against P. berghei infection. The studies have shown an increase in antimalarial activity of Form IV concluding a successful development of new polymorphic form.展开更多
The aim of the present work is to develop rifampicin loaded phospholipid lipospheres containing sulfphobutyl etherβ-cyclodextrin and Vitamin C for inhalation to test their potential for deep lung delivery.The finding...The aim of the present work is to develop rifampicin loaded phospholipid lipospheres containing sulfphobutyl etherβ-cyclodextrin and Vitamin C for inhalation to test their potential for deep lung delivery.The findings of the solid state characterization revealed the amorphous nature of the lipospheres.These exhibited a better flowability,an aerodynamic diameter in the range of 1.76 to 3.99μm.Moreover,the fine particle fraction and emitted dose was found in the range of 68.84–83.73% and 80–93%,respectively.Moreover,lipospheres exhibited enhanced/equivalent efficacy in vitro in H37Rv strain.Hence,the results show the potential of lipospheres for pulmonary delivery of rifampicin.展开更多
The binding pursuits of trans-resveratrol(t-RSV),an amazing health supplement are investigated with an antioxidant enzyme,superoxide dismutase(SOD1).The aim of the study is to dock t-RSV on the adrenaline binding site...The binding pursuits of trans-resveratrol(t-RSV),an amazing health supplement are investigated with an antioxidant enzyme,superoxide dismutase(SOD1).The aim of the study is to dock t-RSV on the adrenaline binding site on SOD1 in order to explore its potential to act as a safety net against amyotrophic lateral sclerosis(ALS),a fatal neurodegenerative disorder that affects motor neurons.In silico GLIDE docking methodology and in vitro microcalorimetry technique is utilized for the investigation of binding parameters of t-RSV with SOD1.The study provides useful and distinct information about the amino acids involved in the interactions at molecular level along with the nature of forces involved in binding of t-RSV with SOD1.The docking analysis using the scoring functions of Schrodinger’s Glide package depicts that GLU100,PRO28,LYS23,TRP32 residues of the peptide backbone on SOD1 interact with phenolic groups of t-RSV.The information on thermodynamic parameters,i.e.binding constant(Kb),free energy(△G)and enthalpy(△H)generated through calorimetric titrations suggests that the reaction between t-RSV and SOD1 is spontaneous and exothermic.Both the studies are found to be in close agreement with each other based as far as the magnitude of binding constant(Kb=9.9×10^4)is concerned.展开更多
To counter the poor aqueous solubility of itraconazole(ITC),its sulfate salt(ITCSUL)was synthesized and characterized by 1 H NMR,MS,FTIR,DSC,XRPD,DLS and SEM.Antifungal properties of ITCSUL were confirmed against diff...To counter the poor aqueous solubility of itraconazole(ITC),its sulfate salt(ITCSUL)was synthesized and characterized by 1 H NMR,MS,FTIR,DSC,XRPD,DLS and SEM.Antifungal properties of ITCSUL were confirmed against different fungal pathogens by broth microdilution method.Enhanced solubility of the salt in various pharmaceutical solvents was observed.Approximately 5.5 fold increase in percentage drug release from ITCSUL than that of ITC in 3 h was observed.Further,the physical mixtures of ITCSUL with two cyclodextrins;b-cyclodextrin(b-CD)and HP-b-cyclodextrin(HP-b-CD)were prepared in 3 M ratios.The in vitro release studies of CD mixtures of ITC and ITCSUL exhibited markedly enhanced dissolution in comparison to ITC and ITCSUL respectively.The promising in vitro performance of ITCSUL and ITCSUL CD mixtures along with advantage of expedient preparation suggest their potential applications in designing a better oral drug delivery system.展开更多
Anxiety is the most common disorder nowadays.Anxiety can be acute or can be chronic.There are several scientific evidences that prove nutrition’s importance and role of different therapies in the treatment of anxiety...Anxiety is the most common disorder nowadays.Anxiety can be acute or can be chronic.There are several scientific evidences that prove nutrition’s importance and role of different therapies in the treatment of anxiety.But very few people are familiar with the role of taking proper nutrition or a balanced diet in anxiety treatment.This article helps many people to know deeply about the therapies they can do at their home and the nutrition and food for healthy lives and controlling the mental disorder.This scoping review also helps to under the anxiety,symptoms,causes,prevalence in patient and how it should be treated with or without the use of medication.Long-term analysis of previous studies show more than 60,000 results with the use of Artificial intelligence which are totally different.So brief literature was studied and found that nutrition plays definitely a major role in treatment.Literature survey revealed the relation between a large intake of fruits,vegetables,omega 3,fatty acids,a ketogenic diet,calorie,magnesium,zinc,selenium,probiotics with low level of anxiety.Paper also revealed the association between higher anxiety levels with high intake of fat diet,sugar intake,carbohydrate,oily food.This paper helps you to understand the value of each therapy and nutrition for successive decreasing anxiety.This paper has main aim to describe the prevalence,causes,symptoms of anxiety so that it can help people to understand that what kind of anxiety is there which they are suffering from and what ways can be done to treat it naturally with the help of huge beneficial therapies,nutritional food,exercises and marketed medicines with advantages and disadvantages and by adding some herbal plants in their diet.展开更多
OBJECTIVE: Different parts of Murraya paniculata have been used traditionally for treating several ailments including mental disorders. The present study was designed to evaluate the antianxiety and antidepressant po...OBJECTIVE: Different parts of Murraya paniculata have been used traditionally for treating several ailments including mental disorders. The present study was designed to evaluate the antianxiety and antidepressant potential of M. paniculata leaves using elevated plus maze model and forced swim test, respectively. METHODS: Extracts of M. panicu/ata made with petroleum ether (60-80 ℃), chloroform, ethanol and water were evaluated for antianxiety and antidepressant activity. The anxiolytic chloroform extract was subjected to column chromatography, yielding five fractions (F1-F5). Fraction F5 (100 mg/kg), which showed notable anxiolytic activity, was further chromatographed to get four subfractions (F5.1-F5.4). Simultaneously, the ethano extract was partitioned with ethyl acetate to obtain ethyl acetate soluble fraction (EASF) and ethyl acetate insoluble fraction. Phytochemical screening of bioactive extracts/fractions and detection of mahanimbine in M paniculata leaf extract by thin-layer chromatography was also carried out. RESULTS: Fraction F5.3 (25 mg/kg) and EASF (20 mg/kg) showed significant anxiolytic and antidepressant activity, respectively. Thin-layer chromatography and phytochemical screening demonstrated the absence of mahanimbine in M. paniculata leaves. Coumarins were observed to be responsible for the anxiolytic activity. CONCLUSION: The results validate the traditional use of M. paniculata leaves in the treatment of menta disorders.展开更多
AIM: Stress is recognized to precipitate anxiety and related psychological problems characterized by a wide range of biochemical and behavioral changes. The present study was carried out to investigate the protective ...AIM: Stress is recognized to precipitate anxiety and related psychological problems characterized by a wide range of biochemical and behavioral changes. The present study was carried out to investigate the protective effects of melatonin and buspirone, and their combination, against six hours immobilization stress-induced, anxiety-like behavioral and oxidative damage in mice. METHOD: Male Laca mice were pre-treated with melatonin(2.5, 5 mg·kg–1), buspirone(5, 10 mg·kg–1), and their combination for consecutive five days. On the 6th day, animals were immobilized for six hours, and thereafter various behavioral tests were performed followed by biochemical tests. RESULTS: Immobilization stress significantly impaired body weight, locomotor activity, and caused anxiety-like behavior, along with increased oxidative damage. Pretreatment with melatonin and buspirone significantly improved the loss in body weight and locomotor activity, attenuated anxiety-like behavior(in both the mirror chamber and plus maze performance tasks), further restored the levels of brain total proteins, and caused antioxidant-like effects, as evidenced by reduced lipid peroxidation, nitrite concentration, and restoration of reduced glutathione and catalase activity, as compared to control animals. In addition, combination of melatonin(2.5, 5 mg·kg–1) with buspirone(5 mg·kg–1) significantly potentiated their protective effects, as compared to their effects individually. CONCLUSION: The present study suggests that melatonin potentiates the beneficial effect of buspirone against immobilization stress-induced, anxiety-like behavioral and oxidative damage in mice possibly by involving a serotonergic mechanism.展开更多
Non-steroidal anti-inflammatory drugs(NSAIDs) have been successfully used for the alleviation of pain and inflammation in the past and continue to be used daily by millions of patients worldwide. However, gastrointest...Non-steroidal anti-inflammatory drugs(NSAIDs) have been successfully used for the alleviation of pain and inflammation in the past and continue to be used daily by millions of patients worldwide. However, gastrointestinal(GI) toxicity associated with NSAIDs is an important medical and socioeconomic problem. Local generation of various reactive oxygen species plays a significant role in the formation of gastric ulceration associated with NSAIDs therapy. Co-medication of antioxidants along with NSAIDs has been found to be beneficial in the prevention of GI injury. This paper describes the synthesis and biological evaluation of N-1-(phenylsulfonyl)-2-methylamino-substituted-1H-benzimidazole derivatives as anti-inflammatory analgesic agents with lower GI toxicity. Studies in vitro and in vivo demonstrated that the antioxidant activity of the test compounds decreased GI toxicity.展开更多
文摘A new variant,JN.1,stemming from the omicron subvariant BA.2.86,garnered the attention of the World Health Organization(WHO)as a"variant of interest."Despite its rapid global spread,especially in the US,Canada,France,Singapore,Sweden[1],and the UK,JN.1 is considered to pose minimal danger.Current vaccinations are believed to remain effective against it.The WHO underscores the importance of maintaining immunization records amid co-occurring respiratory illnesses,and epidemiologists recommend monitoring hospitalizations,particularly in areas with low vaccination rates.
文摘Crystal engineering concept has been utilized to modify the physico-chemical parameters of a naturally occurring alkaloid, quinine sulphate, by exploring its H-bond interactions to generate different forms. Quinine sulphate is found to exist in four different crystal forms. The Forms I and II depict endo/exo events suggesting conversion of metastable low melting forms to higher melting and stable form indicated by sharp melting endotherms. The low melting form IL is found to be monotropically related to high melting Form IH while low melting Form IIL is enantiotropically related to high melting Form IIH. The Form III and IV showed broad endotherms accompanied by mass loss in TGA prior to melting indicating the existence of solvatomorphism. The solvent molecules are tightly bound in the crystal lattice of the drug molecules which is shown by high values of the binding energies of the solvents in these two forms. The enthalpy of solution was found to be endothermic for all the forms which followed the order: Form O > Form II > Form III > Form I > Form IV and is further related to the lattice energy suggesting Form II to be least crystalline. The solubility for Form II was found to be highest with maximum release rate in dissolution studies. The effectiveness of new polymorphic forms was confirmed by performing in vivo antimalarial activity against P. berghei infection. The studies have shown an increase in antimalarial activity of Form IV concluding a successful development of new polymorphic form.
文摘The aim of the present work is to develop rifampicin loaded phospholipid lipospheres containing sulfphobutyl etherβ-cyclodextrin and Vitamin C for inhalation to test their potential for deep lung delivery.The findings of the solid state characterization revealed the amorphous nature of the lipospheres.These exhibited a better flowability,an aerodynamic diameter in the range of 1.76 to 3.99μm.Moreover,the fine particle fraction and emitted dose was found in the range of 68.84–83.73% and 80–93%,respectively.Moreover,lipospheres exhibited enhanced/equivalent efficacy in vitro in H37Rv strain.Hence,the results show the potential of lipospheres for pulmonary delivery of rifampicin.
文摘The binding pursuits of trans-resveratrol(t-RSV),an amazing health supplement are investigated with an antioxidant enzyme,superoxide dismutase(SOD1).The aim of the study is to dock t-RSV on the adrenaline binding site on SOD1 in order to explore its potential to act as a safety net against amyotrophic lateral sclerosis(ALS),a fatal neurodegenerative disorder that affects motor neurons.In silico GLIDE docking methodology and in vitro microcalorimetry technique is utilized for the investigation of binding parameters of t-RSV with SOD1.The study provides useful and distinct information about the amino acids involved in the interactions at molecular level along with the nature of forces involved in binding of t-RSV with SOD1.The docking analysis using the scoring functions of Schrodinger’s Glide package depicts that GLU100,PRO28,LYS23,TRP32 residues of the peptide backbone on SOD1 interact with phenolic groups of t-RSV.The information on thermodynamic parameters,i.e.binding constant(Kb),free energy(△G)and enthalpy(△H)generated through calorimetric titrations suggests that the reaction between t-RSV and SOD1 is spontaneous and exothermic.Both the studies are found to be in close agreement with each other based as far as the magnitude of binding constant(Kb=9.9×10^4)is concerned.
基金grant provided by University Grants Commission(UGC),New Delhi.The authors acknowl-edge the valuable help of Dr.Asim K.Jana and Mr.Sandeep Kumar in carrying out the antifungal assay.
文摘To counter the poor aqueous solubility of itraconazole(ITC),its sulfate salt(ITCSUL)was synthesized and characterized by 1 H NMR,MS,FTIR,DSC,XRPD,DLS and SEM.Antifungal properties of ITCSUL were confirmed against different fungal pathogens by broth microdilution method.Enhanced solubility of the salt in various pharmaceutical solvents was observed.Approximately 5.5 fold increase in percentage drug release from ITCSUL than that of ITC in 3 h was observed.Further,the physical mixtures of ITCSUL with two cyclodextrins;b-cyclodextrin(b-CD)and HP-b-cyclodextrin(HP-b-CD)were prepared in 3 M ratios.The in vitro release studies of CD mixtures of ITC and ITCSUL exhibited markedly enhanced dissolution in comparison to ITC and ITCSUL respectively.The promising in vitro performance of ITCSUL and ITCSUL CD mixtures along with advantage of expedient preparation suggest their potential applications in designing a better oral drug delivery system.
文摘Anxiety is the most common disorder nowadays.Anxiety can be acute or can be chronic.There are several scientific evidences that prove nutrition’s importance and role of different therapies in the treatment of anxiety.But very few people are familiar with the role of taking proper nutrition or a balanced diet in anxiety treatment.This article helps many people to know deeply about the therapies they can do at their home and the nutrition and food for healthy lives and controlling the mental disorder.This scoping review also helps to under the anxiety,symptoms,causes,prevalence in patient and how it should be treated with or without the use of medication.Long-term analysis of previous studies show more than 60,000 results with the use of Artificial intelligence which are totally different.So brief literature was studied and found that nutrition plays definitely a major role in treatment.Literature survey revealed the relation between a large intake of fruits,vegetables,omega 3,fatty acids,a ketogenic diet,calorie,magnesium,zinc,selenium,probiotics with low level of anxiety.Paper also revealed the association between higher anxiety levels with high intake of fat diet,sugar intake,carbohydrate,oily food.This paper helps you to understand the value of each therapy and nutrition for successive decreasing anxiety.This paper has main aim to describe the prevalence,causes,symptoms of anxiety so that it can help people to understand that what kind of anxiety is there which they are suffering from and what ways can be done to treat it naturally with the help of huge beneficial therapies,nutritional food,exercises and marketed medicines with advantages and disadvantages and by adding some herbal plants in their diet.
基金funded by the University Grant Commission,New Delhi,India-110002(Grant number F.4-1/2006(BSR)/5-94/2007)
文摘OBJECTIVE: Different parts of Murraya paniculata have been used traditionally for treating several ailments including mental disorders. The present study was designed to evaluate the antianxiety and antidepressant potential of M. paniculata leaves using elevated plus maze model and forced swim test, respectively. METHODS: Extracts of M. panicu/ata made with petroleum ether (60-80 ℃), chloroform, ethanol and water were evaluated for antianxiety and antidepressant activity. The anxiolytic chloroform extract was subjected to column chromatography, yielding five fractions (F1-F5). Fraction F5 (100 mg/kg), which showed notable anxiolytic activity, was further chromatographed to get four subfractions (F5.1-F5.4). Simultaneously, the ethano extract was partitioned with ethyl acetate to obtain ethyl acetate soluble fraction (EASF) and ethyl acetate insoluble fraction. Phytochemical screening of bioactive extracts/fractions and detection of mahanimbine in M paniculata leaf extract by thin-layer chromatography was also carried out. RESULTS: Fraction F5.3 (25 mg/kg) and EASF (20 mg/kg) showed significant anxiolytic and antidepressant activity, respectively. Thin-layer chromatography and phytochemical screening demonstrated the absence of mahanimbine in M. paniculata leaves. Coumarins were observed to be responsible for the anxiolytic activity. CONCLUSION: The results validate the traditional use of M. paniculata leaves in the treatment of menta disorders.
基金supported by CSIR,New Delhi,provided to Dr.Anil Kumar for carrying out this work
文摘AIM: Stress is recognized to precipitate anxiety and related psychological problems characterized by a wide range of biochemical and behavioral changes. The present study was carried out to investigate the protective effects of melatonin and buspirone, and their combination, against six hours immobilization stress-induced, anxiety-like behavioral and oxidative damage in mice. METHOD: Male Laca mice were pre-treated with melatonin(2.5, 5 mg·kg–1), buspirone(5, 10 mg·kg–1), and their combination for consecutive five days. On the 6th day, animals were immobilized for six hours, and thereafter various behavioral tests were performed followed by biochemical tests. RESULTS: Immobilization stress significantly impaired body weight, locomotor activity, and caused anxiety-like behavior, along with increased oxidative damage. Pretreatment with melatonin and buspirone significantly improved the loss in body weight and locomotor activity, attenuated anxiety-like behavior(in both the mirror chamber and plus maze performance tasks), further restored the levels of brain total proteins, and caused antioxidant-like effects, as evidenced by reduced lipid peroxidation, nitrite concentration, and restoration of reduced glutathione and catalase activity, as compared to control animals. In addition, combination of melatonin(2.5, 5 mg·kg–1) with buspirone(5 mg·kg–1) significantly potentiated their protective effects, as compared to their effects individually. CONCLUSION: The present study suggests that melatonin potentiates the beneficial effect of buspirone against immobilization stress-induced, anxiety-like behavioral and oxidative damage in mice possibly by involving a serotonergic mechanism.
文摘Non-steroidal anti-inflammatory drugs(NSAIDs) have been successfully used for the alleviation of pain and inflammation in the past and continue to be used daily by millions of patients worldwide. However, gastrointestinal(GI) toxicity associated with NSAIDs is an important medical and socioeconomic problem. Local generation of various reactive oxygen species plays a significant role in the formation of gastric ulceration associated with NSAIDs therapy. Co-medication of antioxidants along with NSAIDs has been found to be beneficial in the prevention of GI injury. This paper describes the synthesis and biological evaluation of N-1-(phenylsulfonyl)-2-methylamino-substituted-1H-benzimidazole derivatives as anti-inflammatory analgesic agents with lower GI toxicity. Studies in vitro and in vivo demonstrated that the antioxidant activity of the test compounds decreased GI toxicity.