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P K Murthy - One of the best experts on this subject based on the ideXlab platform.

  • Antifilarial activity of gum from moringa oleifera lam on human lymphatic filaria brugia malayi
    Chronicles of Young Scientists, 2011
    Co-Authors: Vikas Kushwaha, K C Saxena, S K Verma, Vijai Lakshmi, Rolee Sharma, P K Murthy
    Abstract:

    Aim: Currently available Antifilarial drugs diethylcarbamazine, ivermectin and albendazole and their combinations, are not able to control lymphatic filariasis. Therefore, a better Antifilarial Agent is urgently required for proper management of the disease. Materials and Methods: In this study, we evaluated the Antifilarial activity of gum extract of plant Moringa oleifera Lam. against the human lymphatic filarial parasite Brugia malayi using adult worms and microfilariae (mf) in two in vitro assays (motility and inhition in MTT reduction) for viability and two animal models, primary (Meriones unguiculatus implanted with B. malayi adult worms in the peritoneal cavity) and secondary (subcutaneous B. malayi infective larvae induced Mastomys coucha, the model closer to the natural human filarial infection) screens. Results: The gum extract inhibited 100% motility (irreversible loss of motility) of mf and inhibited more than 56% MTT reduction potential of the adult female worms. The extract was safe in cytotoxicity test using Vero cell line, therefore followed in vivo in primary and secondary screens. In primary screen, the extract (5×500 mg/kg) caused 69% macrofilaricidal and 83% sterilization of female worms and 44% macrofilaricidal activity in secondary screen (5 × 1000 mg/kg) by oral route. Conclusion: Thus, it is concluded that the gum of the plant is macrofilaricidal in both in vitro and in vivo and may provide valuable leads for design and development of new Antifilarial Agents. This is the first ever report on the Antifilarial efficacy of M. oleifera.

  • Antifilarial activity in vitro and in vivo of some flavonoids tested against brugia malayi
    Acta Tropica, 2010
    Co-Authors: Vijai Lakshmi, S K Verma, Sujith K Joseph, Shishir Srivastava, Malaya K Sahoo, V Dube, Sunil Kumar Mishra, P K Murthy
    Abstract:

    We evaluated the Antifilarial activity of 6 flavonoids against the human lymphatic filarial parasite Brugia malayi using an in vitro motility assay with adult worms and microfilariae, a biochemical test for viability (3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT)-reduction assay), and two animal models, Meriones unguiculatus (implanted adult worms) and Mastomys coucha (natural infections). In vitro, naringenin and hesperetin killed the adult worms and inhibited (>60%) MTT-reduction at 7.8 and 31.2 μg/ml concentration, respectively. Microfilariae (mf) were killed at 250-500 μg/ml. The half maximal inhibitory concentration (IC(50)) of naringenin for motility of adult females was 2.5 μg/ml. Flavone immobilized female adult worms at 31.2 μg/ml (MTT>80%) and microfilariae at 62.5 μg/ml. Rutin killed microfilariae at 125 μg/ml and inhibited MTT-reduction in female worms for >65% at 500 μg/ml. Naringin had adulticidal effects at 125 μg/ml while chrysin killed microfilariae at 250 μg/ml. In vivo, 50 mg/kg of naringenin elimiated 73% of transplanted adult worms in the Meriones model, but had no effect on the microfilariae in their peritoneal cavity. In Mastomys, the same drug was less effective, killing only 31% of the naturally acquired adult worms, but 51%, when the dose was doubled. Still, effects on the microfilariae in the blood were hardly detectable, even at the highest dose. In summary, all 6 flavonoids showed Antifilarial activity in vitro, which can be classed, in a decreasing order: naringenin>flavone=hesperetin>rutin>naringin>chrysin. In jirds, naringenin and flavone killed or sterilized adult worms at 50mg/kg dose, but in Mastomys, where the parasite produces a patent infection, only naringenin was filaricidal. Thus naringenin and flavone may provide a lead for design and development of new Antifilarial Agent(s). This is the first report on Antifilarial efficacy of flavonoids.

Vikas Kushwaha - One of the best experts on this subject based on the ideXlab platform.

  • diarylheptanoid compounds from alnus nepalensis express in vitro and in vivo Antifilarial activity
    Acta Tropica, 2013
    Co-Authors: Deepti Yadav, Vikas Kushwaha, Kirti Saxena, Richa Verma, Kalpana P Murthy, Madan M Gupta
    Abstract:

    Abstract A large number of medicinal plants remain to be explored for Antifilarial compounds. In the present study a crude methanolic extract of leaves of Alnus nepalensis, chloroform- and n-butanol-partitioned fractions from the crude extract and 6 bioactivity-guided isolated compounds including two new diarylheptanoid from the fractions were assayed for microfilaricidal, macrofilaricidal and female worm sterilizing activity using the lymphatic filariid Brugia malayi in in vitro and in vivo systems. In vitro, the crude methanolic extract exerted better microfilaricidal (LC100: 15.63 μg/ml, IC50: 6.00 μg/ml) than macrofilaricidal (LC100: >250; IC50: 88 μg/ml) activity whereas chloroform and n-butanol fractions were more macrofilaricidal (LC100: 125 and 31.25 μg/ml; IC50: 13.14 and 11.84, respectively) than microfilaricidal (LC100: 250–500 μg/ml, IC50: 44.16 μg/ml). In addition, n-butanol fraction also caused 74% inhibition in MTT reduction potential of the adult worms. In vivo (doses: crude: 100–200 mg/kg; fractions: 100 mg/kg, i.p. × 5 days) the chloroform fraction exerted >50% macrofilaricidal activity whereas methanolic extract and n-butanol fraction produced 38–40% macrofilaricidal action along with some female sterilizing efficacy. Of the 5 diarylheptanoid compounds isolated, alnus dimer, and (5S)-5-hydroxy-1-(4-hydroxyphenyl)-7-(3,4-dihydroxyphenyl)-3-heptanone were found to show the most potent with both macrofilaricidal (LC100: 15.63 μg/ml, IC50: 6.57–10.31 μg/ml) and microfilaricidal (LC100: 31.25–62.5 μg/ml, IC50: 11.05–22.10 μg/ml) activity in vitro. These findings indicate that the active diarylheptanoid compounds may provide valuable lead for design and development of new Antifilarial Agent(s).

  • glycyrrhetinic acid and its analogs a new class of Antifilarial Agents
    Bioorganic & Medicinal Chemistry Letters, 2013
    Co-Authors: Komal Kalani, Vikas Kushwaha, Richa Verma, Kalpana P Murthy, Suchita Srivastava
    Abstract:

    Although a number of chemicals have been isolated from Glycyrrhiza glabra, only a few have been evaluated for their biological significance. As part of our drug discovery program for Antifilarial Agents from Indian medicinal plants, the roots of G. glabra were chemically investigated, which resulted in the isolation and characterization of an Antifilarial Agent, glycyrrhetinic acid (GA, 1a) effective against microfilariae (mf) in vitro (LC100: 12.5 μM; IC50: 1.20 μM), but was inactive against adult worms. Further, GA (1a) was converted into six analogs (2a-7a) and their Antifilarial potential was evaluated by studying in vitro motility and MTT reduction assays employing mf and adult worms of Brugia malayi. The results showed that out of six GA analogs, the benzyl amide analog (6a) killed adults and mf at 25 and 50 μM concentration, respectively, and inhibited 49% MTT reduction potential of the adult parasites. The IC50 values were found to be 8.8 and 2.2 μM for adults and mf, respectively. The SI of the compound was >60. On the other hand the octylamide analog (7a) required much higher concentration to adversely affect the parasites. Finally, both active amide analogs (6a and 7a) were in vivo evaluated using B. malayi-jird model, which showed that analog 6a possesses promising macrofilaricidal activity at 100mg/kg, s.c. ×5 days and around 40% of the treated animals showed calcified masses of worm fragments in peritoneal cavity of the animals. To the best of our knowledge this is the first ever report on the Antifilarial potential of GA analogs. Further work on optimization of the Antifilarial lead is under progress.

  • Antifilarial activity of gum from moringa oleifera lam on human lymphatic filaria brugia malayi
    Chronicles of Young Scientists, 2011
    Co-Authors: Vikas Kushwaha, K C Saxena, S K Verma, Vijai Lakshmi, Rolee Sharma, P K Murthy
    Abstract:

    Aim: Currently available Antifilarial drugs diethylcarbamazine, ivermectin and albendazole and their combinations, are not able to control lymphatic filariasis. Therefore, a better Antifilarial Agent is urgently required for proper management of the disease. Materials and Methods: In this study, we evaluated the Antifilarial activity of gum extract of plant Moringa oleifera Lam. against the human lymphatic filarial parasite Brugia malayi using adult worms and microfilariae (mf) in two in vitro assays (motility and inhition in MTT reduction) for viability and two animal models, primary (Meriones unguiculatus implanted with B. malayi adult worms in the peritoneal cavity) and secondary (subcutaneous B. malayi infective larvae induced Mastomys coucha, the model closer to the natural human filarial infection) screens. Results: The gum extract inhibited 100% motility (irreversible loss of motility) of mf and inhibited more than 56% MTT reduction potential of the adult female worms. The extract was safe in cytotoxicity test using Vero cell line, therefore followed in vivo in primary and secondary screens. In primary screen, the extract (5×500 mg/kg) caused 69% macrofilaricidal and 83% sterilization of female worms and 44% macrofilaricidal activity in secondary screen (5 × 1000 mg/kg) by oral route. Conclusion: Thus, it is concluded that the gum of the plant is macrofilaricidal in both in vitro and in vivo and may provide valuable leads for design and development of new Antifilarial Agents. This is the first ever report on the Antifilarial efficacy of M. oleifera.

Richa Verma - One of the best experts on this subject based on the ideXlab platform.

  • diarylheptanoid compounds from alnus nepalensis express in vitro and in vivo Antifilarial activity
    Acta Tropica, 2013
    Co-Authors: Deepti Yadav, Vikas Kushwaha, Kirti Saxena, Richa Verma, Kalpana P Murthy, Madan M Gupta
    Abstract:

    Abstract A large number of medicinal plants remain to be explored for Antifilarial compounds. In the present study a crude methanolic extract of leaves of Alnus nepalensis, chloroform- and n-butanol-partitioned fractions from the crude extract and 6 bioactivity-guided isolated compounds including two new diarylheptanoid from the fractions were assayed for microfilaricidal, macrofilaricidal and female worm sterilizing activity using the lymphatic filariid Brugia malayi in in vitro and in vivo systems. In vitro, the crude methanolic extract exerted better microfilaricidal (LC100: 15.63 μg/ml, IC50: 6.00 μg/ml) than macrofilaricidal (LC100: >250; IC50: 88 μg/ml) activity whereas chloroform and n-butanol fractions were more macrofilaricidal (LC100: 125 and 31.25 μg/ml; IC50: 13.14 and 11.84, respectively) than microfilaricidal (LC100: 250–500 μg/ml, IC50: 44.16 μg/ml). In addition, n-butanol fraction also caused 74% inhibition in MTT reduction potential of the adult worms. In vivo (doses: crude: 100–200 mg/kg; fractions: 100 mg/kg, i.p. × 5 days) the chloroform fraction exerted >50% macrofilaricidal activity whereas methanolic extract and n-butanol fraction produced 38–40% macrofilaricidal action along with some female sterilizing efficacy. Of the 5 diarylheptanoid compounds isolated, alnus dimer, and (5S)-5-hydroxy-1-(4-hydroxyphenyl)-7-(3,4-dihydroxyphenyl)-3-heptanone were found to show the most potent with both macrofilaricidal (LC100: 15.63 μg/ml, IC50: 6.57–10.31 μg/ml) and microfilaricidal (LC100: 31.25–62.5 μg/ml, IC50: 11.05–22.10 μg/ml) activity in vitro. These findings indicate that the active diarylheptanoid compounds may provide valuable lead for design and development of new Antifilarial Agent(s).

  • glycyrrhetinic acid and its analogs a new class of Antifilarial Agents
    Bioorganic & Medicinal Chemistry Letters, 2013
    Co-Authors: Komal Kalani, Vikas Kushwaha, Richa Verma, Kalpana P Murthy, Suchita Srivastava
    Abstract:

    Although a number of chemicals have been isolated from Glycyrrhiza glabra, only a few have been evaluated for their biological significance. As part of our drug discovery program for Antifilarial Agents from Indian medicinal plants, the roots of G. glabra were chemically investigated, which resulted in the isolation and characterization of an Antifilarial Agent, glycyrrhetinic acid (GA, 1a) effective against microfilariae (mf) in vitro (LC100: 12.5 μM; IC50: 1.20 μM), but was inactive against adult worms. Further, GA (1a) was converted into six analogs (2a-7a) and their Antifilarial potential was evaluated by studying in vitro motility and MTT reduction assays employing mf and adult worms of Brugia malayi. The results showed that out of six GA analogs, the benzyl amide analog (6a) killed adults and mf at 25 and 50 μM concentration, respectively, and inhibited 49% MTT reduction potential of the adult parasites. The IC50 values were found to be 8.8 and 2.2 μM for adults and mf, respectively. The SI of the compound was >60. On the other hand the octylamide analog (7a) required much higher concentration to adversely affect the parasites. Finally, both active amide analogs (6a and 7a) were in vivo evaluated using B. malayi-jird model, which showed that analog 6a possesses promising macrofilaricidal activity at 100mg/kg, s.c. ×5 days and around 40% of the treated animals showed calcified masses of worm fragments in peritoneal cavity of the animals. To the best of our knowledge this is the first ever report on the Antifilarial potential of GA analogs. Further work on optimization of the Antifilarial lead is under progress.

Kalpana P Murthy - One of the best experts on this subject based on the ideXlab platform.

  • diarylheptanoid compounds from alnus nepalensis express in vitro and in vivo Antifilarial activity
    Acta Tropica, 2013
    Co-Authors: Deepti Yadav, Vikas Kushwaha, Kirti Saxena, Richa Verma, Kalpana P Murthy, Madan M Gupta
    Abstract:

    Abstract A large number of medicinal plants remain to be explored for Antifilarial compounds. In the present study a crude methanolic extract of leaves of Alnus nepalensis, chloroform- and n-butanol-partitioned fractions from the crude extract and 6 bioactivity-guided isolated compounds including two new diarylheptanoid from the fractions were assayed for microfilaricidal, macrofilaricidal and female worm sterilizing activity using the lymphatic filariid Brugia malayi in in vitro and in vivo systems. In vitro, the crude methanolic extract exerted better microfilaricidal (LC100: 15.63 μg/ml, IC50: 6.00 μg/ml) than macrofilaricidal (LC100: >250; IC50: 88 μg/ml) activity whereas chloroform and n-butanol fractions were more macrofilaricidal (LC100: 125 and 31.25 μg/ml; IC50: 13.14 and 11.84, respectively) than microfilaricidal (LC100: 250–500 μg/ml, IC50: 44.16 μg/ml). In addition, n-butanol fraction also caused 74% inhibition in MTT reduction potential of the adult worms. In vivo (doses: crude: 100–200 mg/kg; fractions: 100 mg/kg, i.p. × 5 days) the chloroform fraction exerted >50% macrofilaricidal activity whereas methanolic extract and n-butanol fraction produced 38–40% macrofilaricidal action along with some female sterilizing efficacy. Of the 5 diarylheptanoid compounds isolated, alnus dimer, and (5S)-5-hydroxy-1-(4-hydroxyphenyl)-7-(3,4-dihydroxyphenyl)-3-heptanone were found to show the most potent with both macrofilaricidal (LC100: 15.63 μg/ml, IC50: 6.57–10.31 μg/ml) and microfilaricidal (LC100: 31.25–62.5 μg/ml, IC50: 11.05–22.10 μg/ml) activity in vitro. These findings indicate that the active diarylheptanoid compounds may provide valuable lead for design and development of new Antifilarial Agent(s).

  • glycyrrhetinic acid and its analogs a new class of Antifilarial Agents
    Bioorganic & Medicinal Chemistry Letters, 2013
    Co-Authors: Komal Kalani, Vikas Kushwaha, Richa Verma, Kalpana P Murthy, Suchita Srivastava
    Abstract:

    Although a number of chemicals have been isolated from Glycyrrhiza glabra, only a few have been evaluated for their biological significance. As part of our drug discovery program for Antifilarial Agents from Indian medicinal plants, the roots of G. glabra were chemically investigated, which resulted in the isolation and characterization of an Antifilarial Agent, glycyrrhetinic acid (GA, 1a) effective against microfilariae (mf) in vitro (LC100: 12.5 μM; IC50: 1.20 μM), but was inactive against adult worms. Further, GA (1a) was converted into six analogs (2a-7a) and their Antifilarial potential was evaluated by studying in vitro motility and MTT reduction assays employing mf and adult worms of Brugia malayi. The results showed that out of six GA analogs, the benzyl amide analog (6a) killed adults and mf at 25 and 50 μM concentration, respectively, and inhibited 49% MTT reduction potential of the adult parasites. The IC50 values were found to be 8.8 and 2.2 μM for adults and mf, respectively. The SI of the compound was >60. On the other hand the octylamide analog (7a) required much higher concentration to adversely affect the parasites. Finally, both active amide analogs (6a and 7a) were in vivo evaluated using B. malayi-jird model, which showed that analog 6a possesses promising macrofilaricidal activity at 100mg/kg, s.c. ×5 days and around 40% of the treated animals showed calcified masses of worm fragments in peritoneal cavity of the animals. To the best of our knowledge this is the first ever report on the Antifilarial potential of GA analogs. Further work on optimization of the Antifilarial lead is under progress.

Vijai Lakshmi - One of the best experts on this subject based on the ideXlab platform.

  • Antifilarial activity of gum from moringa oleifera lam on human lymphatic filaria brugia malayi
    Chronicles of Young Scientists, 2011
    Co-Authors: Vikas Kushwaha, K C Saxena, S K Verma, Vijai Lakshmi, Rolee Sharma, P K Murthy
    Abstract:

    Aim: Currently available Antifilarial drugs diethylcarbamazine, ivermectin and albendazole and their combinations, are not able to control lymphatic filariasis. Therefore, a better Antifilarial Agent is urgently required for proper management of the disease. Materials and Methods: In this study, we evaluated the Antifilarial activity of gum extract of plant Moringa oleifera Lam. against the human lymphatic filarial parasite Brugia malayi using adult worms and microfilariae (mf) in two in vitro assays (motility and inhition in MTT reduction) for viability and two animal models, primary (Meriones unguiculatus implanted with B. malayi adult worms in the peritoneal cavity) and secondary (subcutaneous B. malayi infective larvae induced Mastomys coucha, the model closer to the natural human filarial infection) screens. Results: The gum extract inhibited 100% motility (irreversible loss of motility) of mf and inhibited more than 56% MTT reduction potential of the adult female worms. The extract was safe in cytotoxicity test using Vero cell line, therefore followed in vivo in primary and secondary screens. In primary screen, the extract (5×500 mg/kg) caused 69% macrofilaricidal and 83% sterilization of female worms and 44% macrofilaricidal activity in secondary screen (5 × 1000 mg/kg) by oral route. Conclusion: Thus, it is concluded that the gum of the plant is macrofilaricidal in both in vitro and in vivo and may provide valuable leads for design and development of new Antifilarial Agents. This is the first ever report on the Antifilarial efficacy of M. oleifera.

  • Antifilarial activity in vitro and in vivo of some flavonoids tested against brugia malayi
    Acta Tropica, 2010
    Co-Authors: Vijai Lakshmi, S K Verma, Sujith K Joseph, Shishir Srivastava, Malaya K Sahoo, V Dube, Sunil Kumar Mishra, P K Murthy
    Abstract:

    We evaluated the Antifilarial activity of 6 flavonoids against the human lymphatic filarial parasite Brugia malayi using an in vitro motility assay with adult worms and microfilariae, a biochemical test for viability (3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT)-reduction assay), and two animal models, Meriones unguiculatus (implanted adult worms) and Mastomys coucha (natural infections). In vitro, naringenin and hesperetin killed the adult worms and inhibited (>60%) MTT-reduction at 7.8 and 31.2 μg/ml concentration, respectively. Microfilariae (mf) were killed at 250-500 μg/ml. The half maximal inhibitory concentration (IC(50)) of naringenin for motility of adult females was 2.5 μg/ml. Flavone immobilized female adult worms at 31.2 μg/ml (MTT>80%) and microfilariae at 62.5 μg/ml. Rutin killed microfilariae at 125 μg/ml and inhibited MTT-reduction in female worms for >65% at 500 μg/ml. Naringin had adulticidal effects at 125 μg/ml while chrysin killed microfilariae at 250 μg/ml. In vivo, 50 mg/kg of naringenin elimiated 73% of transplanted adult worms in the Meriones model, but had no effect on the microfilariae in their peritoneal cavity. In Mastomys, the same drug was less effective, killing only 31% of the naturally acquired adult worms, but 51%, when the dose was doubled. Still, effects on the microfilariae in the blood were hardly detectable, even at the highest dose. In summary, all 6 flavonoids showed Antifilarial activity in vitro, which can be classed, in a decreasing order: naringenin>flavone=hesperetin>rutin>naringin>chrysin. In jirds, naringenin and flavone killed or sterilized adult worms at 50mg/kg dose, but in Mastomys, where the parasite produces a patent infection, only naringenin was filaricidal. Thus naringenin and flavone may provide a lead for design and development of new Antifilarial Agent(s). This is the first report on Antifilarial efficacy of flavonoids.