The Experts below are selected from a list of 528 Experts worldwide ranked by ideXlab platform
Hiroshi Yasuda - One of the best experts on this subject based on the ideXlab platform.
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Bactericidal effect of plaunotol, a cytoprotective Antiulcer Agent, against
2016Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol> M-6> M-5> M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-material from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane
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bactericidal effect of plaunotol a cytoprotective Antiulcer Agent against helicobacter pylori
Journal of Antimicrobial Chemotherapy, 1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol > M-6 > M-5 > M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-material from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane.
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in vitro and in vivo antibacterial activity of plaunotol a cytoprotective Antiulcer Agent against helicobacter pylori
Journal of Antimicrobial Chemotherapy, 1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:Recently, some Antiulcer Agents have been reported to have antibacterial activity against Helicobacter pylori, which is highly associated with gastritis and peptic ulcers. In-vitro and in-vivo activity of plaunotol, a cytoprotective Antiulcer Agent, against H. pylori was investigated. Antibacterial activity of plaunotol against a standard strain (NCTC 11637) and 14 clinical isolates was compared with those of other cytoprotective Antiulcer Agents : benexate, sofalcone, teprenone, cetraxate, and gefarnate, by an agar dilution method. The MIC 50 and MIC 90 of plaunotol against 15 strains were 6.25 and 12.5 mg/L, respectively, making it the most potent of the cytoprotective Antiulcer Agents. The bactericidal effect of plaunotol was investigated using an in-vitro killing assay. Plaunotol at concentrations of more than 6 mg/L induced a rapid reduction of culture turbidity, with an extensive loss of viability, within 30 min. Observation by scanning electron microscopy revealed that plaunotol caused autolysis and treated cells were deformed. In-vivo activity of plaunotol against H. pylori was examined in a nude mouse gastritis model. Plaunotol significantly decreased the number of H. pylori in the stomach of nude mice. In addition, the Antiulcer Agent enhanced the antibacterial activity of amoxycillin or clarithromycin in the infection model.
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bactericidal effect of plaunotol a cytoprotective Antiulcer Agent against heticobacter pylori
1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol > M-6 > M-5 > M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-mat erial from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane.
Goverdhan Mehta - One of the best experts on this subject based on the ideXlab platform.
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multiple aryne insertions into oxindoles synthesis of bioactive 3 3 diarylated oxindoles and dibenzo b e azepin 6 ones
Organic Letters, 2016Co-Authors: Ramesh Samineni, Chandramohan Reddy C Bandi, P Srihari, Goverdhan MehtaAbstract:An aryne insertion cascade reaction on oxindoles has been observed and constitutes a convenient “one pot” preparation of bioactive di- and triarylated oxindoles in good yields under mild conditions. A temperature controlled “reaction switch” enables ready access to dibenzo[b,e]azepin-6-one derivatives employing the same reaction regime. This tactic has been extended to a short synthesis of potent Antiulcer Agent darenzepine.
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Multiple Aryne Insertions into Oxindoles: Synthesis of Bioactive 3,3-Diarylated Oxindoles and Dibenzo[b,e]azepin-6-ones
2016Co-Authors: Ramesh Samineni, P Srihari, Chandramohan Reddy C. Bandi, Goverdhan MehtaAbstract:An aryne insertion cascade reaction on oxindoles has been observed and constitutes a convenient “one pot” preparation of bioactive di- and triarylated oxindoles in good yields under mild conditions. A temperature controlled “reaction switch” enables ready access to dibenzo[b,e]azepin-6-one derivatives employing the same reaction regime. This tactic has been extended to a short synthesis of potent Antiulcer Agent darenzepine
Tetsufumi Koga - One of the best experts on this subject based on the ideXlab platform.
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Bactericidal effect of plaunotol, a cytoprotective Antiulcer Agent, against
2016Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol> M-6> M-5> M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-material from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane
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bactericidal effect of plaunotol a cytoprotective Antiulcer Agent against helicobacter pylori
Journal of Antimicrobial Chemotherapy, 1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol > M-6 > M-5 > M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-material from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane.
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in vitro and in vivo antibacterial activity of plaunotol a cytoprotective Antiulcer Agent against helicobacter pylori
Journal of Antimicrobial Chemotherapy, 1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:Recently, some Antiulcer Agents have been reported to have antibacterial activity against Helicobacter pylori, which is highly associated with gastritis and peptic ulcers. In-vitro and in-vivo activity of plaunotol, a cytoprotective Antiulcer Agent, against H. pylori was investigated. Antibacterial activity of plaunotol against a standard strain (NCTC 11637) and 14 clinical isolates was compared with those of other cytoprotective Antiulcer Agents : benexate, sofalcone, teprenone, cetraxate, and gefarnate, by an agar dilution method. The MIC 50 and MIC 90 of plaunotol against 15 strains were 6.25 and 12.5 mg/L, respectively, making it the most potent of the cytoprotective Antiulcer Agents. The bactericidal effect of plaunotol was investigated using an in-vitro killing assay. Plaunotol at concentrations of more than 6 mg/L induced a rapid reduction of culture turbidity, with an extensive loss of viability, within 30 min. Observation by scanning electron microscopy revealed that plaunotol caused autolysis and treated cells were deformed. In-vivo activity of plaunotol against H. pylori was examined in a nude mouse gastritis model. Plaunotol significantly decreased the number of H. pylori in the stomach of nude mice. In addition, the Antiulcer Agent enhanced the antibacterial activity of amoxycillin or clarithromycin in the infection model.
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bactericidal effect of plaunotol a cytoprotective Antiulcer Agent against heticobacter pylori
1996Co-Authors: Tetsufumi Koga, Harumi Kawada, Yukio Utsui, Haruki Domon, Chika Ishii, Hiroshi YasudaAbstract:In order to investigate the bactericidal effect of plaunotol, an oily Antiulcer Agent, against Helicobacter pylori, comparative studies were conducted using its derivatives, M-4, M-5, and M-6, whose hydrophobicity decreased in the order of plaunotol > M-6 > M-5 > M-4 by log P determination. Plaunotol rapidly reduced the viability of H. pylori in vitro, and cell death was associated with cell lysis. In addition, plaunotol showed eightfold stronger bactericidal activity against H. pylori than M-6 and M-5, while the compound with the lowest hydrophobicity, M-4, showed no bactericidal activity. The bactericidal activities of plaunotol and its derivatives were related to the hydrophobicity of these compounds. To investigate a possible interaction between these compounds and the cell membrane of H. pylori, their effects on liposomal membranes prepared from phosphatidylethanolamine and cardiolipin, which are known to be present in the membrane of H. pylori, were determined by detection of glucose release from the liposomes. Plaunotol showed eight-fold higher activity than M-6 and M-5, while M-4 showed no activity. The effects of plaunotol and its derivatives on liposomal membrane were therefore related to their bactericidal activities. In addition, it was confirmed that the bactericidal effect of plaunotol against H. pylori was neutralized by the liposomal membrane, and that plaunotol led to an increase in permeability of the membrane, as evidenced by measurement of the leakage of 260 nm absorbing-mat erial from H. pylori. These results suggest that the bactericidal effect of plaunotol against H. pylori is due to the interaction between this compound and the bacterial cell membrane.
Claudiu T Supuran - One of the best experts on this subject based on the ideXlab platform.
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famotidine an Antiulcer Agent strongly inhibitshelicobacter pyloriand human carbonic anhydrases
ACS Medicinal Chemistry Letters, 2018Co-Authors: Andrea Angeli, Marta Ferraroni, Claudiu T SupuranAbstract:Famotidine, an Antiulcer drug incorporating a sulfamide motif, was investigated as carbonic anhydrase inhibitor (CAI). It acts as a nanomolar inhibitor of several human (hCA II, VI, VII and XII) and Helicobacter pylori CAs. The high resolution X-ray structures of famotidine bound to hCA I and II revealed interesting aspects related to its CA inhibition mechanism, offering the possibility to develop antibacterials with a novel mechanism of action.
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Famotidine, an Antiulcer Agent, Strongly Inhibits Helicobacter pylori and Human Carbonic Anhydrases
2018Co-Authors: Andrea Angeli, Marta Ferraroni, Claudiu T SupuranAbstract:Famotidine, an Antiulcer drug incorporating a sulfamide motif, was investigated as carbonic anhydrase inhibitor (CAI). It acts as a nanomolar inhibitor of several human (hCA II, VI, VII and XII) and Helicobacter pylori CAs. The high resolution X-ray structures of famotidine bound to hCA I and II revealed interesting aspects related to its CA inhibition mechanism, offering the possibility to develop antibacterials with a novel mechanism of action
Ramesh Samineni - One of the best experts on this subject based on the ideXlab platform.
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multiple aryne insertions into oxindoles synthesis of bioactive 3 3 diarylated oxindoles and dibenzo b e azepin 6 ones
Organic Letters, 2016Co-Authors: Ramesh Samineni, Chandramohan Reddy C Bandi, P Srihari, Goverdhan MehtaAbstract:An aryne insertion cascade reaction on oxindoles has been observed and constitutes a convenient “one pot” preparation of bioactive di- and triarylated oxindoles in good yields under mild conditions. A temperature controlled “reaction switch” enables ready access to dibenzo[b,e]azepin-6-one derivatives employing the same reaction regime. This tactic has been extended to a short synthesis of potent Antiulcer Agent darenzepine.
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Multiple Aryne Insertions into Oxindoles: Synthesis of Bioactive 3,3-Diarylated Oxindoles and Dibenzo[b,e]azepin-6-ones
2016Co-Authors: Ramesh Samineni, P Srihari, Chandramohan Reddy C. Bandi, Goverdhan MehtaAbstract:An aryne insertion cascade reaction on oxindoles has been observed and constitutes a convenient “one pot” preparation of bioactive di- and triarylated oxindoles in good yields under mild conditions. A temperature controlled “reaction switch” enables ready access to dibenzo[b,e]azepin-6-one derivatives employing the same reaction regime. This tactic has been extended to a short synthesis of potent Antiulcer Agent darenzepine