Lead Compounds

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Palavesam Suganthi - One of the best experts on this subject based on the ideXlab platform.

  • seaweeds as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi
    Abstract:

    The problems of resistant lines of Plasmodium falciparum are escalating. Twelve seaweeds species belong to five different families (Sargassaceae, Gracilariaceae, Hypneaceae, Corallinaceae and Halimedaceae) were collected from Mandapam coastal area, and the seaweeds extracts were tested for in vitro antiplasmodial activity against P. falciparum. Among the tested seaweeds, Gracilaria verrucosa (IC50 5.55 μg.ml−1) and Hypnea espera (IC50 8.94 μg.ml−1) showed good antiplasmodial activity, and these results are comparable with positive controls such as artemether (IC50 4.09 μg.ml−1) and chloroquine (IC50 19.59 μg.ml−1), respectively. Turbinaria conoides, Sargassum myriocystem, Hypnea valentiae and Jania rubens extracts showed IC50 values between 5 to 50 μg.ml−1. Sargassum sp., Turbinaria decurrens and Halimeda gracilis extracts showed IC50 values between 50 to 100 μg.ml−1. Gracilaria corticata, Jania adherens and Halimeda opuntia extracts showed IC50 value of more than 100 μg.ml−1. Statistical analysis reveals that significant in vitro antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that no morphological changes in erythrocytes by the ethanolic extract of seaweeds extracts after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of sugars, proteins, phenols and carboxylic acid in the ethanolic extracts of seaweeds. It is concluded from the present study that the ethanolic extracts of seaweeds of G. verrucosa and Hypnea espera possess Lead Compounds for development of antiplasmodial drugs.

  • mangrove plants as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi, Malaiyandi Venkatesan, Andy Ramu
    Abstract:

    Malaria is the world’s Leading killer among the infectious diseases. The treatment of malaria is mystified by the challenges of widespread resistance of the malaria parasites to cheap and affordable antimalarial drugs. The present study was made in an attempt to identify the in vitro antiplasmodial activity against mangrove plant parts. (Avicennia marina, Acanthus ilicifolius, Bruguiera cylindrica, Excoecaria agallocha, Rhizophora apiculata, and Rhizophora mucronata mangrove plant extracts exhibited in vitro antiplasmodial activity against Plasmodium falciparum). Of the selected mangrove plant parts, the bark extract of A. marina exhibited minimum concentration of inhibitory activities IC50 49.63 μg.ml−1. The leaf extract of A. marina, the hypocotyl extract of B. cylindrica, the leaf extract of E. agallocha, the flower extract of R. mucronata, and the hypocotyl extract of R. apiculata showed IC50 values between 50 and 100 μg.ml−1. Statistical analysis reveals that significant antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that there were no morphological changes in erythrocytes by the ethanolic extract of mangrove plants after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of alkaloids, carboxylic acids, coumarins, saponins, flavonoids, xanthoproteins, tannins, phenols, sugars, resins, steroids, and proteins in the ethanolic extracts of mangrove plants. It is concluded from the present study that the ethanolic extracts of mangrove plant parts of A. marina possess Lead Compounds for the development of antiplasmodial drugs.

S Ravikumar - One of the best experts on this subject based on the ideXlab platform.

  • seaweeds as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi
    Abstract:

    The problems of resistant lines of Plasmodium falciparum are escalating. Twelve seaweeds species belong to five different families (Sargassaceae, Gracilariaceae, Hypneaceae, Corallinaceae and Halimedaceae) were collected from Mandapam coastal area, and the seaweeds extracts were tested for in vitro antiplasmodial activity against P. falciparum. Among the tested seaweeds, Gracilaria verrucosa (IC50 5.55 μg.ml−1) and Hypnea espera (IC50 8.94 μg.ml−1) showed good antiplasmodial activity, and these results are comparable with positive controls such as artemether (IC50 4.09 μg.ml−1) and chloroquine (IC50 19.59 μg.ml−1), respectively. Turbinaria conoides, Sargassum myriocystem, Hypnea valentiae and Jania rubens extracts showed IC50 values between 5 to 50 μg.ml−1. Sargassum sp., Turbinaria decurrens and Halimeda gracilis extracts showed IC50 values between 50 to 100 μg.ml−1. Gracilaria corticata, Jania adherens and Halimeda opuntia extracts showed IC50 value of more than 100 μg.ml−1. Statistical analysis reveals that significant in vitro antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that no morphological changes in erythrocytes by the ethanolic extract of seaweeds extracts after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of sugars, proteins, phenols and carboxylic acid in the ethanolic extracts of seaweeds. It is concluded from the present study that the ethanolic extracts of seaweeds of G. verrucosa and Hypnea espera possess Lead Compounds for development of antiplasmodial drugs.

  • mangrove plants as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi, Malaiyandi Venkatesan, Andy Ramu
    Abstract:

    Malaria is the world’s Leading killer among the infectious diseases. The treatment of malaria is mystified by the challenges of widespread resistance of the malaria parasites to cheap and affordable antimalarial drugs. The present study was made in an attempt to identify the in vitro antiplasmodial activity against mangrove plant parts. (Avicennia marina, Acanthus ilicifolius, Bruguiera cylindrica, Excoecaria agallocha, Rhizophora apiculata, and Rhizophora mucronata mangrove plant extracts exhibited in vitro antiplasmodial activity against Plasmodium falciparum). Of the selected mangrove plant parts, the bark extract of A. marina exhibited minimum concentration of inhibitory activities IC50 49.63 μg.ml−1. The leaf extract of A. marina, the hypocotyl extract of B. cylindrica, the leaf extract of E. agallocha, the flower extract of R. mucronata, and the hypocotyl extract of R. apiculata showed IC50 values between 50 and 100 μg.ml−1. Statistical analysis reveals that significant antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that there were no morphological changes in erythrocytes by the ethanolic extract of mangrove plants after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of alkaloids, carboxylic acids, coumarins, saponins, flavonoids, xanthoproteins, tannins, phenols, sugars, resins, steroids, and proteins in the ethanolic extracts of mangrove plants. It is concluded from the present study that the ethanolic extracts of mangrove plant parts of A. marina possess Lead Compounds for the development of antiplasmodial drugs.

Andy Ramu - One of the best experts on this subject based on the ideXlab platform.

  • mangrove plants as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi, Malaiyandi Venkatesan, Andy Ramu
    Abstract:

    Malaria is the world’s Leading killer among the infectious diseases. The treatment of malaria is mystified by the challenges of widespread resistance of the malaria parasites to cheap and affordable antimalarial drugs. The present study was made in an attempt to identify the in vitro antiplasmodial activity against mangrove plant parts. (Avicennia marina, Acanthus ilicifolius, Bruguiera cylindrica, Excoecaria agallocha, Rhizophora apiculata, and Rhizophora mucronata mangrove plant extracts exhibited in vitro antiplasmodial activity against Plasmodium falciparum). Of the selected mangrove plant parts, the bark extract of A. marina exhibited minimum concentration of inhibitory activities IC50 49.63 μg.ml−1. The leaf extract of A. marina, the hypocotyl extract of B. cylindrica, the leaf extract of E. agallocha, the flower extract of R. mucronata, and the hypocotyl extract of R. apiculata showed IC50 values between 50 and 100 μg.ml−1. Statistical analysis reveals that significant antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that there were no morphological changes in erythrocytes by the ethanolic extract of mangrove plants after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of alkaloids, carboxylic acids, coumarins, saponins, flavonoids, xanthoproteins, tannins, phenols, sugars, resins, steroids, and proteins in the ethanolic extracts of mangrove plants. It is concluded from the present study that the ethanolic extracts of mangrove plant parts of A. marina possess Lead Compounds for the development of antiplasmodial drugs.

Samuel Jacob Inbaneson - One of the best experts on this subject based on the ideXlab platform.

  • seaweeds as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi
    Abstract:

    The problems of resistant lines of Plasmodium falciparum are escalating. Twelve seaweeds species belong to five different families (Sargassaceae, Gracilariaceae, Hypneaceae, Corallinaceae and Halimedaceae) were collected from Mandapam coastal area, and the seaweeds extracts were tested for in vitro antiplasmodial activity against P. falciparum. Among the tested seaweeds, Gracilaria verrucosa (IC50 5.55 μg.ml−1) and Hypnea espera (IC50 8.94 μg.ml−1) showed good antiplasmodial activity, and these results are comparable with positive controls such as artemether (IC50 4.09 μg.ml−1) and chloroquine (IC50 19.59 μg.ml−1), respectively. Turbinaria conoides, Sargassum myriocystem, Hypnea valentiae and Jania rubens extracts showed IC50 values between 5 to 50 μg.ml−1. Sargassum sp., Turbinaria decurrens and Halimeda gracilis extracts showed IC50 values between 50 to 100 μg.ml−1. Gracilaria corticata, Jania adherens and Halimeda opuntia extracts showed IC50 value of more than 100 μg.ml−1. Statistical analysis reveals that significant in vitro antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that no morphological changes in erythrocytes by the ethanolic extract of seaweeds extracts after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of sugars, proteins, phenols and carboxylic acid in the ethanolic extracts of seaweeds. It is concluded from the present study that the ethanolic extracts of seaweeds of G. verrucosa and Hypnea espera possess Lead Compounds for development of antiplasmodial drugs.

  • mangrove plants as a source of Lead Compounds for the development of new antiplasmodial drugs from south east coast of india
    Parasitology Research, 2011
    Co-Authors: S Ravikumar, Samuel Jacob Inbaneson, Palavesam Suganthi, Malaiyandi Venkatesan, Andy Ramu
    Abstract:

    Malaria is the world’s Leading killer among the infectious diseases. The treatment of malaria is mystified by the challenges of widespread resistance of the malaria parasites to cheap and affordable antimalarial drugs. The present study was made in an attempt to identify the in vitro antiplasmodial activity against mangrove plant parts. (Avicennia marina, Acanthus ilicifolius, Bruguiera cylindrica, Excoecaria agallocha, Rhizophora apiculata, and Rhizophora mucronata mangrove plant extracts exhibited in vitro antiplasmodial activity against Plasmodium falciparum). Of the selected mangrove plant parts, the bark extract of A. marina exhibited minimum concentration of inhibitory activities IC50 49.63 μg.ml−1. The leaf extract of A. marina, the hypocotyl extract of B. cylindrica, the leaf extract of E. agallocha, the flower extract of R. mucronata, and the hypocotyl extract of R. apiculata showed IC50 values between 50 and 100 μg.ml−1. Statistical analysis reveals that significant antiplasmodial activity (P < 0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that there were no morphological changes in erythrocytes by the ethanolic extract of mangrove plants after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of alkaloids, carboxylic acids, coumarins, saponins, flavonoids, xanthoproteins, tannins, phenols, sugars, resins, steroids, and proteins in the ethanolic extracts of mangrove plants. It is concluded from the present study that the ethanolic extracts of mangrove plant parts of A. marina possess Lead Compounds for the development of antiplasmodial drugs.

Abhijit Datta - One of the best experts on this subject based on the ideXlab platform.

  • In silico screening of herbal and nanoparticle Lead Compounds for effectivity against H5N1, H1N1 neuraminidase and telomerase
    BMC Bioinformatics, 2020
    Co-Authors: Sayak Ganguli, Manjita Mazumder, Protip Basu, Sayani Mitra, Abhijit Datta
    Abstract:

    Abstract Background Traditionally, drugs were discovered by testing Compounds synthesized in time consuming multi-step processes against a battery of in vivo biological screens. Promising Compounds were then further studied in development, where their pharmacokinetic properties, metabolism and potential toxicity were investigated. Methods Here we present a study on the most talked about herbal Lead Compounds and their potential binding affinity to the effector molecules of major disease causing agents, H5N1 and H1N1(Neuraminidase). The work also encompasses the screening of the nanoparticle compound - fullerene which have been reported to have anti HIV activity. Further studies were also performed with telomerase which has been the target of numerous anti cancer experiments. Results The results revealed that most herbal Lead Compounds were effective targets against H5N1 neuraminidase, namely baicalein was found to be an effective target for inhibiting the neuraminidase of H1N1 virus. Telomerase was found to be effectively bound by curcumin at the RNA binding interface. The study with nanoparticle fullerene also showed that it has the potential of serving as an effective ligand for inhibiting H1N1 neuraminidase and telomerase. Conclusion Our data demonstrate that the new in silico screening method is highly efficient for identifying potential Lead Compounds against major infectious disease.

  • In silico screening of herbal and nanoparticle Lead Compounds for effectivity against H5N1, H1N1 neuraminidase and telomerase.
    BMC bioinformatics, 2010
    Co-Authors: Sayak Ganguli, Manjita Mazumder, Protip Basu, Sayani Mitra, Abhijit Datta
    Abstract:

    Traditionally, drugs were discovered by testing Compounds synthesized in time consuming multi-step processes against a battery of in vivo biological screens. Promising Compounds were then further studied in development, where their pharmacokinetic properties, metabolism and potential toxicity were investigated. Here we present a study on the most talked about herbal Lead Compounds and their potential binding affinity to the effector molecules of major disease causing agents, H5N1 and H1N1(Neuraminidase). The work also encompasses the screening of the nanoparticle compound - fullerene which have been reported to have anti HIV activity. Further studies were also performed with telomerase which has been the target of numerous anti cancer experiments. The results revealed that most herbal Lead Compounds were effective targets against H5N1 neuraminidase, namely baicalein was found to be an effective target for inhibiting the neuraminidase of H1N1 virus. Telomerase was found to be effectively bound by curcumin at the RNA binding interface. The study with nanoparticle fullerene also showed that it has the potential of serving as an effective ligand for inhibiting H1N1 neuraminidase and telomerase. Our data demonstrate that the new in silico screening method is highly efficient for identifying potential Lead Compounds against major infectious disease.