Parasites are the accomplished evaders of host immunity. Several life threat-ening disorders have... more Parasites are the accomplished evaders of host immunity. Several life threat-ening disorders have been reported to be caused by them. But, at the same time their immunogenic effect in terms of stimulation of production of cyto-kines like IL-4 and IL-10 which can potentially stop the activation of self ag-gressive T lymphocyte may also not be overlooked. Several in-vivo experi-ments to explore the beneficial effects of parasites like helminthes, protozo-ans and others have been performed at various levels. The encouraging re-sults of them, depicting lasting protection against the chronic autoimmune disorders like diabetes, Multiple Sclerosis (MS), Arthritis and Encephalomye-litis have attracted the scientific brains in last decade. Few of those studies with possible mechanisms of protective role of parasitic infections are criti-cally reviewed in the present article. Also, futures prospective to exploit the parasites for the treatment of such life challenging autoimmune disorders are...
Leishmaniasis is one of the most well-known neglected infectious diseases, which is severe proble... more Leishmaniasis is one of the most well-known neglected infectious diseases, which is severe problem for public health. Heterocyclic derivatives are known to displays wide range of pharmacology activities including isoxazole ring that exhibit antileishmanial activity. In the given paper series of 59, 4-aminomethyl 5-aryl-3-substituted isoxazoles were used to identify the structural insights and to find the binding affinity with protein through quantitative structure activity relationship (QSAR) and docking approaches. The designed model produced statistically significant results with of R2 = 0.72and Q2 = 0.72. Most potent compound formed hydrogen bonds with active amino acidsArg 87, Arg 104, Gly 112, His 117, Gly 118 and Asp 120. Structure activity relationship (SAR) revealed that substitution of hydrophobic and steric groups may enhance the biological activity of compounds as antiprotozoal agents.The given strategies of computational studies could be an encouraging way for designing ...
Breast cancer is one of the important public health problems today and recent treatments have not... more Breast cancer is one of the important public health problems today and recent treatments have not been found to be very effective for advanced-stage metastatic disease of the breast. In the present study ten 3,4,5- trihydroxybenzohy- drazone derivatives (AR 01- AR 10) were synthesized by two different methods viz. reflux and stirring. It was observed that compounds synthesized by stirring method acquire good yield and require less time in comparison to reflux method. Further cytotoxicity activity performed on two breast cancer cell lines viz. MDA-MB-468 and MCF-7 revealed moderate activity in all compounds at 40 μg/mL and 80 μg/mL which has the highest in samples AR 01 and AR 10 for both cell lines. Considerably all compounds have shown potent antioxidant activity at 50 μg/mL and above concentrations. Tumor in mice treated with compound AR 01 was found to be smaller in comparison to control and AR 10. Findings revealed that compound having electron donating group showed more potent ...
Background: Antimicrobial resistance bacteria are the source of a threat to the community and hos... more Background: Antimicrobial resistance bacteria are the source of a threat to the community and hospital settings. There are many drug resistant human pathogenic bacteria are reported from all over world. Extended spectrum of β lactamases producing organism are increasing and causing more severe infection due to mutation leads to Multi Drug Resistances (MDR) which make treatment difficult. Aims: The study focus was undertaken to detect the prevalence and susceptibility of Multi drug resistant (MDR) Pseudomonas aeruginosa strains isolated from clinical specimens in a tertiary care hospital. Materials & Methods: Total 110 samples collected from clinical specimen’s urine, blood, pus, sputum of different hospitals and clinics and isolates MDR strains of Pseudomonas aeruginosa. ESBLs detection by phenotypic double disk synergy method and antimicrobial susceptibility is done by broth dilution method Minimum inhibitory concentration (MICs) breakpoints using AST instrument VITEK 2 machine rec...
Organotin and organosilicon complexes have showed potential antimicrobial activity and bind to th... more Organotin and organosilicon complexes have showed potential antimicrobial activity and bind to the protein's active site. Inorganic-based metallodrugs have emerged as an effective strategy for drugs based on metal selection and characteristics.
Received on 15-01-2014 Accepted on 08-02-2014 Madhucalongifolia member of the family Sapotaceae w... more Received on 15-01-2014 Accepted on 08-02-2014 Madhucalongifolia member of the family Sapotaceae was studied for its immunomodulatory activity on albino mice in the present study. The ethanolic extract of the plant (EEML) was administered at the dose of 100 and 200mg/kg body weight in the treated groups III and IV. The antibody titre value, DTH response and effect on myelosuppression were checked against the control group I and cyclophosphomide induced myelosuppressed group II. The significant (p<0.01) increase in antibody titre value and DTH response in group III & IV was reported as a sign of its stimulating effect on humoral and cell mediated immunity respectively. Moreover, the restoration of Total Leukocyte Count (TLC) and Differential Leukocyte Count (DLC) to normal level in EEML treated group III & IV as compared to cyclophosphomide treated group II has shown it ameliorating effect on myeloid regeneration too. Hence, the M. longifolia with the significant immunostimulatory ...
An improved and green method has been developed for the synthesis of substituted 2-benzylidene-1-... more An improved and green method has been developed for the synthesis of substituted 2-benzylidene-1-benzofuran-3-ones by treating 2-hydroxychalcones with CuBr 2 in DMF-water mixture (7:3; v/v) using grinding methodology. Molecular docking study was also carried out and it revealed that compound 4h binds with the active amino Glu-277, Try-406 and Arg-152 of neuraminindase against influenza virus.
The novel corona virus, also known as severe acute respiratory syndrome coronavirus 2, has rapidl... more The novel corona virus, also known as severe acute respiratory syndrome coronavirus 2, has rapidly spread all over the world. Various reports suggested number of drugs could be potential target for the treatment of COVID-19 although the effectiveness of all these drugs have not yet fully evaluated. Copper shows viricidal activities which involved various fundamental mechanisms viz. Oxygen transcription, hematopoiesis, energy generation, cellular metabolism and signal transduction. Copper and its complexes could be potential drug target as an antiviral agent against corona virus.
Synthesis of new drugs and evolution of new biologically active molecules constitutes major assig... more Synthesis of new drugs and evolution of new biologically active molecules constitutes major assignment for chemists in organic synthesis. Therapeutic drugs have played a major role in increasing average life. For a long time, natural sources have been used to prepare medicines for treatment of human ailments. Variety of medicinal agents have symbolic qualities and better results with numerous reactions for providing new chemical entities. Among well-known reactions, Mannich reaction has been of great importance due to its diversified applications especially in medicinal chemistry. Mannich reaction has been used as an important tool for several years to acquire compounds with several pharmacological properties [1-4]. Rapid expansion of investigations in this field is largely due to increasing utility on these compounds.
The regulation of gene expression in brain vicissitudes during aging is still not much known and ... more The regulation of gene expression in brain vicissitudes during aging is still not much known and explored. Differential gene expression and regulation is a key factor involved to identify the important landmarks within the brain transcriptome to study neuronal aging. Recently, transcriptomic studies are highly explored to understand and depict diseased versus normal as next generation sequencing enables to capture the complete biological context to the entire genome. Study of gene expression during aging compared to young flies provides a signature and scenario of gene expression and regulation during aging. In this study, we took advantage of NGS raw data of young and old flies head from SRA database of NCBI and decrypted the gene expression regulation during normal aging in drosophila model. We identified 350 genes with significant differential expression between young and old flies having 0.01% FDR. Various pathways in context to identified genes which are involved in aging inclu...
In this investigation the antioxidant as well as antiproliferative activities of different isolat... more In this investigation the antioxidant as well as antiproliferative activities of different isolated compounds from ethyl acetate fraction of Prunus domestica (peel + flesh) were studied in two human breast cancer cell lines, MCF-7 and MDA-MB-468. Free radical scavengering as done with 2, 2-diphenyl-1-picrylhydrazyl (DPPH) study indicated different degrees of antioxidative activity of the isolated compounds such as chlorogenic acid, protocatechuic acid, vanillic acid, ferulic acid, p-coumaric acid and rutin. However maximum antioxidative activity was observed in chlorogenic acid with IC50 of 0.115 mg/ml . With respect to antiproliferative potential, chlorogenic acid also exhibited the maximum antiproliferative activity on MCF-7 and protocatechuic acid on MDA-MB-468 human breast cancer cell lines . This appears to be the first report that provides a comparative account on the antioxidant and antiproliferative property of some isolated active compounds of the Indian variety of fruit, P...
Parasites are the accomplished evaders of host immunity. Several life threat-ening disorders have... more Parasites are the accomplished evaders of host immunity. Several life threat-ening disorders have been reported to be caused by them. But, at the same time their immunogenic effect in terms of stimulation of production of cyto-kines like IL-4 and IL-10 which can potentially stop the activation of self ag-gressive T lymphocyte may also not be overlooked. Several in-vivo experi-ments to explore the beneficial effects of parasites like helminthes, protozo-ans and others have been performed at various levels. The encouraging re-sults of them, depicting lasting protection against the chronic autoimmune disorders like diabetes, Multiple Sclerosis (MS), Arthritis and Encephalomye-litis have attracted the scientific brains in last decade. Few of those studies with possible mechanisms of protective role of parasitic infections are criti-cally reviewed in the present article. Also, futures prospective to exploit the parasites for the treatment of such life challenging autoimmune disorders are...
Leishmaniasis is one of the most well-known neglected infectious diseases, which is severe proble... more Leishmaniasis is one of the most well-known neglected infectious diseases, which is severe problem for public health. Heterocyclic derivatives are known to displays wide range of pharmacology activities including isoxazole ring that exhibit antileishmanial activity. In the given paper series of 59, 4-aminomethyl 5-aryl-3-substituted isoxazoles were used to identify the structural insights and to find the binding affinity with protein through quantitative structure activity relationship (QSAR) and docking approaches. The designed model produced statistically significant results with of R2 = 0.72and Q2 = 0.72. Most potent compound formed hydrogen bonds with active amino acidsArg 87, Arg 104, Gly 112, His 117, Gly 118 and Asp 120. Structure activity relationship (SAR) revealed that substitution of hydrophobic and steric groups may enhance the biological activity of compounds as antiprotozoal agents.The given strategies of computational studies could be an encouraging way for designing ...
Breast cancer is one of the important public health problems today and recent treatments have not... more Breast cancer is one of the important public health problems today and recent treatments have not been found to be very effective for advanced-stage metastatic disease of the breast. In the present study ten 3,4,5- trihydroxybenzohy- drazone derivatives (AR 01- AR 10) were synthesized by two different methods viz. reflux and stirring. It was observed that compounds synthesized by stirring method acquire good yield and require less time in comparison to reflux method. Further cytotoxicity activity performed on two breast cancer cell lines viz. MDA-MB-468 and MCF-7 revealed moderate activity in all compounds at 40 μg/mL and 80 μg/mL which has the highest in samples AR 01 and AR 10 for both cell lines. Considerably all compounds have shown potent antioxidant activity at 50 μg/mL and above concentrations. Tumor in mice treated with compound AR 01 was found to be smaller in comparison to control and AR 10. Findings revealed that compound having electron donating group showed more potent ...
Background: Antimicrobial resistance bacteria are the source of a threat to the community and hos... more Background: Antimicrobial resistance bacteria are the source of a threat to the community and hospital settings. There are many drug resistant human pathogenic bacteria are reported from all over world. Extended spectrum of β lactamases producing organism are increasing and causing more severe infection due to mutation leads to Multi Drug Resistances (MDR) which make treatment difficult. Aims: The study focus was undertaken to detect the prevalence and susceptibility of Multi drug resistant (MDR) Pseudomonas aeruginosa strains isolated from clinical specimens in a tertiary care hospital. Materials & Methods: Total 110 samples collected from clinical specimen’s urine, blood, pus, sputum of different hospitals and clinics and isolates MDR strains of Pseudomonas aeruginosa. ESBLs detection by phenotypic double disk synergy method and antimicrobial susceptibility is done by broth dilution method Minimum inhibitory concentration (MICs) breakpoints using AST instrument VITEK 2 machine rec...
Organotin and organosilicon complexes have showed potential antimicrobial activity and bind to th... more Organotin and organosilicon complexes have showed potential antimicrobial activity and bind to the protein's active site. Inorganic-based metallodrugs have emerged as an effective strategy for drugs based on metal selection and characteristics.
Received on 15-01-2014 Accepted on 08-02-2014 Madhucalongifolia member of the family Sapotaceae w... more Received on 15-01-2014 Accepted on 08-02-2014 Madhucalongifolia member of the family Sapotaceae was studied for its immunomodulatory activity on albino mice in the present study. The ethanolic extract of the plant (EEML) was administered at the dose of 100 and 200mg/kg body weight in the treated groups III and IV. The antibody titre value, DTH response and effect on myelosuppression were checked against the control group I and cyclophosphomide induced myelosuppressed group II. The significant (p<0.01) increase in antibody titre value and DTH response in group III & IV was reported as a sign of its stimulating effect on humoral and cell mediated immunity respectively. Moreover, the restoration of Total Leukocyte Count (TLC) and Differential Leukocyte Count (DLC) to normal level in EEML treated group III & IV as compared to cyclophosphomide treated group II has shown it ameliorating effect on myeloid regeneration too. Hence, the M. longifolia with the significant immunostimulatory ...
An improved and green method has been developed for the synthesis of substituted 2-benzylidene-1-... more An improved and green method has been developed for the synthesis of substituted 2-benzylidene-1-benzofuran-3-ones by treating 2-hydroxychalcones with CuBr 2 in DMF-water mixture (7:3; v/v) using grinding methodology. Molecular docking study was also carried out and it revealed that compound 4h binds with the active amino Glu-277, Try-406 and Arg-152 of neuraminindase against influenza virus.
The novel corona virus, also known as severe acute respiratory syndrome coronavirus 2, has rapidl... more The novel corona virus, also known as severe acute respiratory syndrome coronavirus 2, has rapidly spread all over the world. Various reports suggested number of drugs could be potential target for the treatment of COVID-19 although the effectiveness of all these drugs have not yet fully evaluated. Copper shows viricidal activities which involved various fundamental mechanisms viz. Oxygen transcription, hematopoiesis, energy generation, cellular metabolism and signal transduction. Copper and its complexes could be potential drug target as an antiviral agent against corona virus.
Synthesis of new drugs and evolution of new biologically active molecules constitutes major assig... more Synthesis of new drugs and evolution of new biologically active molecules constitutes major assignment for chemists in organic synthesis. Therapeutic drugs have played a major role in increasing average life. For a long time, natural sources have been used to prepare medicines for treatment of human ailments. Variety of medicinal agents have symbolic qualities and better results with numerous reactions for providing new chemical entities. Among well-known reactions, Mannich reaction has been of great importance due to its diversified applications especially in medicinal chemistry. Mannich reaction has been used as an important tool for several years to acquire compounds with several pharmacological properties [1-4]. Rapid expansion of investigations in this field is largely due to increasing utility on these compounds.
The regulation of gene expression in brain vicissitudes during aging is still not much known and ... more The regulation of gene expression in brain vicissitudes during aging is still not much known and explored. Differential gene expression and regulation is a key factor involved to identify the important landmarks within the brain transcriptome to study neuronal aging. Recently, transcriptomic studies are highly explored to understand and depict diseased versus normal as next generation sequencing enables to capture the complete biological context to the entire genome. Study of gene expression during aging compared to young flies provides a signature and scenario of gene expression and regulation during aging. In this study, we took advantage of NGS raw data of young and old flies head from SRA database of NCBI and decrypted the gene expression regulation during normal aging in drosophila model. We identified 350 genes with significant differential expression between young and old flies having 0.01% FDR. Various pathways in context to identified genes which are involved in aging inclu...
In this investigation the antioxidant as well as antiproliferative activities of different isolat... more In this investigation the antioxidant as well as antiproliferative activities of different isolated compounds from ethyl acetate fraction of Prunus domestica (peel + flesh) were studied in two human breast cancer cell lines, MCF-7 and MDA-MB-468. Free radical scavengering as done with 2, 2-diphenyl-1-picrylhydrazyl (DPPH) study indicated different degrees of antioxidative activity of the isolated compounds such as chlorogenic acid, protocatechuic acid, vanillic acid, ferulic acid, p-coumaric acid and rutin. However maximum antioxidative activity was observed in chlorogenic acid with IC50 of 0.115 mg/ml . With respect to antiproliferative potential, chlorogenic acid also exhibited the maximum antiproliferative activity on MCF-7 and protocatechuic acid on MDA-MB-468 human breast cancer cell lines . This appears to be the first report that provides a comparative account on the antioxidant and antiproliferative property of some isolated active compounds of the Indian variety of fruit, P...
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