The Experts below are selected from a list of 150 Experts worldwide ranked by ideXlab platform
Iyanar Kannan - One of the best experts on this subject based on the ideXlab platform.
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Antifungal Activity, Gas Chromatographic-Mass Spectrometric Analysis And in silico Study of Punica Granatum Peel Extracts Against Fluconazole Resistant Strains of Candida Species
Current Pharmaceutical Biotechnology, 2018Co-Authors: Sony Paul, Kalyani Mohanram, Iyanar KannanAbstract:Candida species is the common cause of opportunistic fungal infections all over the world with increased mortality and morbidity especially in immunosuppressed patients. Fluconazole is the first line therapy for candidiasis. The antifungal resistance pattern in high-risk patients is a major concern. The present study was aimed to assess the anticandidal activity of Punica granatum peel against fluconazole resistant Candida species isolated from HIV patients. Ethanol, chloroform, petroleum ether and aqueous extracts of the peel of P. granatum were evaluated against standard strains of Candida spp. and fluconazole resistant clinical isolates by agar diffusion and broth dilution techniques. The GC-MS analysis of the extracts was performed to identify the phytochemicals present in it. The predominant phytochemical was subjected to molecular docking study to determine its binding efficacy with Lanosterol 14-alpha demethylase. P. granatum peel extracts showed excellent anticandidal activity with ethanol extract exhibiting the most inhibitory activity. C. albicans and C. krusei were the most inhibited and C. parapsilosis was the least inhibited species. The GC-MS analysis of the ethanol extract identified five predominant phytochemicals. On docking studies, the five phytochemicals showed a good binding to the Lanosterol 14-alpha demethylase. The present study is the first report on the antifungal activity of various extracts of P. granatum against fluconazole resistant Candida isolates. Ethanol extract of P. granatum peel showed excellent anticandidal activity against fluconazole resistant Candida spp. Hence, it can be explored further to identify a potential drug candidate. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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Antifungal Activity, Gas Chromatographic-Mass Spectrometric Analysis And in silico Study of Punica Granatum Peel Extracts Against Fluconazole Resistant Strains of Candida Species.
Current Pharmaceutical Biotechnology, 2018Co-Authors: Sony Paul, Kalyani Mohanram, Iyanar KannanAbstract:AIMS: Candida species is the common cause of opportunistic fungal infections all over the world with increased mortality and morbidity especially in immunosuppressed patients. Fluconazole is the first line therapy for candidiasis. The antifungal resistance pattern in high-risk patients is a major concern. The present study was aimed to assess the anticandidal activity of Punica granatum peel against fluconazole resistant Candida species isolated from HIV patients. MATERIALS & METHODS: Ethanol, chloroform, petroleum ether and aqueous extracts of the peel of P. granatum were evaluated against standard strains of Candida spp. and fluconazole resistant clinical isolates by agar diffusion and broth dilution techniques. The GC-MS analysis of the extracts was performed to identify the phytochemicals present in it. The predominant phytochemical was subjected to molecular docking study to determine its binding efficacy with Lanosterol 14-alpha demethylase. RESULTS: P. granatum peel extracts showed excellent anticandidal activity with ethanol extract exhibiting the most inhibitory activity. C. albicans and C. krusei were the most inhibited and C. parapsilosis was the least inhibited species. The GC-MS analysis of the ethanol extract identified five predominant phytochemicals. On docking studies, the five phytochemicals showed a good binding to the Lanosterol 14-alpha demethylase. CONCLUSION: The present study is the first report on the antifungal activity of various extracts of P. granatum against fluconazole resistant Candida isolates. Ethanol extract of P. granatum peel showed excellent anticandidal activity against fluconazole resistant Candida spp. Hence, it can be explored further to identify a potential drug candidate.
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In vitro antifungal activity of cassia fistula extracts against fluconazole resistant strains of Candida species from HIV patients
Journal De Mycologie Medicale, 2017Co-Authors: P. Sony, Iyanar Kannan, M. Kalyani, D. Jeyakumari, R.g. SukumarAbstract:Summary Background Candida species is the fourth common cause of blood stream infections all over the world which is life threatening. Invasive candidiasis leads to increased mortality and morbidity especially in immunosuppressed. The antifungal resistance pattern in high-risk patients is major concern. Purpose The present study was to access the anticandidal activity of leaves, bark and seeds of Cassia fistula against fluconazole resistant Candida species, C. albicans , C. glabrata , C. krusei , C. tropicalis , C . kefyr and C. parapsilosis isolated from HIV patients. The predominant phytochemical component responsible for fungicidal activity was to be accessed. Material and methods Ethanol, chloroform, petroleum ether and aqueous extracts of leaves, bark and seeds of C. fistula linn. was evaluated against Microbial type culture collection (MTCC) Candida strains and 21 fluconazole resistant clinical isolates. Antifungal activity was evaluated by agar diffusion and broth dilution techniques. The active phytochemical component present in the ethanol extract of seeds was accessed by high performance thin layer chromatography. The docking study was done with Lanosterol 14-alpha demethylase, the azole drug target with the predominant phytochemical from the extract having antifungal activity. Results All the extracts of C. fistula showed excellent anticandidal activity. Ethanol extract of C. fistula seed exhibited the most inhibitory activity. C. krusei and C. parapsilosis were the most inhibited and C. kefyr was the least inhibited species. The predominant phytochemical active component of the ethanol extract of seed was gallic acid. Gallic acid showed excellent binding with Lanosterol 14-alpha demethylase. Conclusion The present study reports the antifungal activity of various extracts of Cassia fistula for the first time against fluconazole resistant Candida isolates. We can conclude that the polyphenolic compound gallic acid is a potent natural antifungal agent. Further research is needed to assess the pharmacokinetic property.
Marcelo S. Castilho - One of the best experts on this subject based on the ideXlab platform.
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Cloning, expression, purification and spectrophotometric analysis of Lanosterol 14-alpha demethylase from Leishmania braziliensis (LbCYP51)
Molecular Biology Reports, 2018Co-Authors: Humberto F. Freitas, Acássia Benjamim Leal Pires, Marcelo S. CastilhoAbstract:Leishmaniasis, a neglected tropical disease, is a major cause of morbidity and mortality worldwide. Of the three main clinical forms, cutaneous leishmaniasis (CL) is the most common and 40 million people are at risk in the endemic areas. Currently, the available drugs to fight leishmaniasis have high toxicity and poor efficiency. Then, it is very important to search for effective and safe drugs that would target essential enzymes from the parasite, such as Lanosterol 14-alpha demethylase (CYP51, EC 1.14.13.70) from Leishmania braziliensis . Because most drug design efforts have been directed for Leishmania non- braziliensis species, there is no structural or kinetic data regarding L. braziliensis CYP51. Herein, we present for the first time molecular biology efforts and purification protocol to obtain the enzyme Lb CYP51. These results lay the ground for future investigation of drugs against this target.
J C Loper - One of the best experts on this subject based on the ideXlab platform.
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multiple regulatory elements control expression of the gene encoding the saccharomyces cerevisiae cytochrome p450 Lanosterol 14 alpha demethylase erg11
Journal of Biological Chemistry, 1992Co-Authors: T G Turi, J C LoperAbstract:Abstract The major cytochrome P450 in the yeast Saccharomyces cerevisiae, Lanosterol 14 Alpha-Demethylase (ERG11), catalyzes an essential reaction in the biosynthesis of ergosterol, the predominant sterol of yeast. Protein levels of this cytochrome P450 are known to be affected by carbon source, oxygen, and heme, as well as the growth state of the culture. We have determined that ERG11 message levels increase during growth on glucose, in the presence of heme, and during oxygen limiting growth conditions and, unexpectedly, during anaerobic growth. To determine the cis-acting regions responsible for regulation of expression of the ERG11 promoter under optimal conditions of fermentative growth, deletion analysis was performed using the Escherichia coli lacZ as a reporter gene. Two upstream activating sequences, UAS1 and UAS2, and an upstream repressor element, URS1, plus a second possible or cryptic repressor element, URS2, were identified in the ERG11 promoter. The HAP1 protein product apparently participates in activation from UAS1 but not from UAS2. Sequences resembling ERG11 UAS2 were identified in seven additional oxygen-regulated genes. Repression of ERG11 expression was dependent upon the ROX1 repressor and additional repressor(s) designated as Old (overexpression of Lanosterol demethylase). These data indicate that ERG11 is a member of the hypoxic gene family which includes ANB1, COX5b, CYC7, and HEM13. Furthermore, NADPH-cytochrome P450 reductase (CPR1), another component in this P450 system, appears to be coordinately regulated with ERG11.
Humberto F. Freitas - One of the best experts on this subject based on the ideXlab platform.
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Cloning, expression, purification and spectrophotometric analysis of Lanosterol 14-alpha demethylase from Leishmania braziliensis (LbCYP51)
Molecular Biology Reports, 2018Co-Authors: Humberto F. Freitas, Acássia Benjamim Leal Pires, Marcelo S. CastilhoAbstract:Leishmaniasis, a neglected tropical disease, is a major cause of morbidity and mortality worldwide. Of the three main clinical forms, cutaneous leishmaniasis (CL) is the most common and 40 million people are at risk in the endemic areas. Currently, the available drugs to fight leishmaniasis have high toxicity and poor efficiency. Then, it is very important to search for effective and safe drugs that would target essential enzymes from the parasite, such as Lanosterol 14-alpha demethylase (CYP51, EC 1.14.13.70) from Leishmania braziliensis . Because most drug design efforts have been directed for Leishmania non- braziliensis species, there is no structural or kinetic data regarding L. braziliensis CYP51. Herein, we present for the first time molecular biology efforts and purification protocol to obtain the enzyme Lb CYP51. These results lay the ground for future investigation of drugs against this target.
Juan L Rodrigueztudela - One of the best experts on this subject based on the ideXlab platform.
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g484s amino acid substitution in Lanosterol 14 alpha demethylase erg11 is related to fluconazole resistance in a recurrent cryptococcus neoformans clinical isolate
Antimicrobial Agents and Chemotherapy, 2003Co-Authors: L Rodero, Emilia Mellado, Carolina A Rodriguez, Angela Salve, Liliana Guelfand, Pedro Cahn, Manuel Cuencaestrella, Graciela Davel, Juan L RodrigueztudelaAbstract:Five sequential Cryptococcus neoformans isolates recovered from an AIDS patient with recurrent meningitis were analyzed. Four isolates were fluconazole susceptible, while the fifth isolate developed fluconazole resistance. Analysis of the 14-α Lanosterol demethylase gene (ERG11) showed a point mutation in the resistant strain responsible for the amino acid substitution G484S.
