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Miri Park - One of the best experts on this subject based on the ideXlab platform.
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antibacterial activity of 10 gingerol and 12 gingerol isolated from ginger rhizome against periodontal bacteria
Phytotherapy Research, 2008Co-Authors: Miri ParkAbstract:Ginger (Zingiber officinale Roscoe) has been used widely as a food spice and an herbal medicine. In particular, its gingerol-related components have been reported to possess antimicrobial and antifungal properties, as well as several pharmaceutical properties. However, the effective ginger constituents that inhibit the growth of oral bacteria associated with periodontitis in the human oral cavity have not been elucidated. This study revealed that the ethanol and n-hexane extracts of ginger exhibited antibacterial activities against three anaerobic Gram-negative bacteria, Porphyromonas gingivalis ATCC 53978, Porphyromonas endodontalis ATCC 35406 and Prevotella intermedia ATCC 25611, causing periodontal diseases. Thereafter, five ginger constituents were isolated by a preparative high-performance liquid chromatographic method from the active silica-gel column chromatography fractions, elucidated their structures by nuclear magnetic resonance spectroscopy and electrospray ionization mass spectrometry and their antibacterial activity evaluated. In conclusion, two highly alkylated gingerols, [10]-gingerol and [12]-gingerol effectively inhibited the growth of these oral pathogens at a minimum inhibitory concentration (MIC) range of 6–30 µg/mL. These ginger compounds also killed the oral pathogens at a minimum bactericidal concentration (MBC) range of 4–20 µg/mL, but not the other ginger compounds 5-acetoxy-[6]-gingerol, 3,5-diacetoxy-[6]-gingerdiol and Galanolactone. Copyright © 2008 John Wiley & Sons, Ltd.
James Almada Da Silva - One of the best experts on this subject based on the ideXlab platform.
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Search of cathepsin k inhibitors in medicinal plants used in the treatment of diseases osteoarthritis
Universidade Federal de São Carlos, 2011Co-Authors: James Almada Da SilvaAbstract:Dez plantas utilizadas pela medicina tradicional com indicativos na literatura de suas eficácias frente a doenças osteoarticulares foram selecionadas para a realização de uma triagem de atividade inibitória frente à catepsina K, uma importante enzima responsável pela clivagem do colágeno, principal constituinte da matriz extracelular da cartilagem e ossos. Das dez plantas selecionadas (gengibre, açafrão, camélia, unha-de-gato, mentrasto, moringa, babaçu, garra-do-diabo, urtigão e pequi), uma, gengibre (Zingiber officinale), merece destaque pela alta inibição de seu extrato e frações frente à catepsina K e por seu uso milenar como agente terapêutico. Da fração de diclorometano obtida do extrato bruto dos rizomas de Z. officinale isolou-se e identificou-se 18 substâncias (4-gingerol, 6-gingerol, 8-gingerol, 6-shogaol, 8- shogaol, 10-shogaol, 6-paradol, 6-gingerdiol, metil-6-gingerol, metil-6-shogaol, diacetato de 6-gingerdioila, diacetato de metil-6-gingerdioila, zingerona, gingerenona A, galanolactona, 3-acetato de 5-hidroxi-1,7-bis(4-hidroxi-3-metoxifenil)-heptila e hexaidrocurcumina). Da fração de n-hexano e do óleo essencial, foram identificados 2 monoterpenos e 4 sesquiterpenos. As substâncias mais ativas frente à catepsina K foram os gingerois e shogaois de maior cadeia alquílica. Otimização da separação das substâncias majoritárias (6, 8 e 10-gingerol) e um estudo de sobrecarga de uma coluna C18 por CLAE, foram realizados, obtendo-se como resultado o isolamento de dezenas a centenas de miligramas de cada gingerol com considerável grau de pureza. Modificações estruturais do 6-gingerol foram realizadas e, das sete substâncias obtidas, 4 tiveram um aumento considerável do poder inibitório. Das substâncias obtidas, três, SSi6, 10-gingerol, 6-shogaol, foram selecionadas para ensaios posteriores: determinação do tipo de inibição frente à catepsina K, inibição da catepsina K e inibição da produção de óxido nítrico (NO), em meio celular. As inibições determinadas foram não-competitiva parcial, acompetitiva parcial e acompetitiva completa, para o SSi6, 10-gingerol e 6-shogaol, respectivamente. Excelentes atividades de inibição frente à catepsina K, em meio celular, puderam ser observadas para o SSi6 e 6-shogaol. No ensaio de inibição da produção de NO, o 6- shogaol foi a única substância que se apresentou como efetivo.Ten herbs used in traditional medicine supported by literature for its effectiveness to osteoarticular diseases were selected to conduct a screening of inhibition activity against the cathepsin K, an important enzyme responsible for cleavage of collagen, the main constituent of extracellular matrix of cartilage and bone. Out of the ten herbs selected (ginger, saffron, camellia, cats claw, mentrasto, moringa, babaçu, devils claw, urtica e pequi), one, gengibre (Z. officinale), should be highlighted by a high inhibitory activity of its extracts and fractions against cathepsin K and due to its ancient use as a therapeutic agent. From the dichloromethane fraction obtained of the crude extract of the rhizome of Z. officinale were isolated and identified 18 compounds (4-gingerol, 6-gingerol, 8-gingerol, 6-shogaol, 8-shogaol, 10-shogaol, 6- paradol, 6-gingerdiol, methyl 6-gingerol, methyl 6-shogaol, diacetoxy-6-gingerdiol, methyl diacetoxy-6-gingerdiol, zingerone, gingerenone A, Galanolactone, 3-acetoxy- 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)-heptane and hexahydrocurcumin). From the hexane fraction and essential oil were identified two monoterpenes and four sesquiterpenes. The most active compounds against cathepsin K were gingerols and shogaols with longer alkyl chain. Optimization of the separation of major compounds (6, 8 and 10-gingerol) and an overload study of C18 column was performed using HPLC, obtained as result dozens to hundreds of milligrams of each gingerol with high purity. Structural modifications of 6-gingerol were carried out and of the seven derivatives obtained 4 presented significant increase in inhibition of cathepsin K. Of all the compounds, three, SSi6, 10-gingerol, 6-shogaol, were selected for later tests: determinating of the mode the inhibition against cathepsin K, inhibition against cathepsin K and inhibition of nitric oxide (NO) production, in cellular culture. The inhibitions determined were: partially noncompetitive, partially uncompetitive and complete uncompetitive for the SSi6, 10-gingerol and 6-shogaol, respectively. Excellent inhibition activity against the cathepsin K, in cellular culture, can be observed for SSi6 and 6-shogaol. In the inhibition assay of NO production, the 6- shogaol was the only compound that appeared as effective
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Search of cathepsin k inhibitors in medicinal plants used in the treatment of diseases osteoarthritis
Programa de Pós-graduação em Química, 2011Co-Authors: James Almada Da SilvaAbstract:Ten herbs used in traditional medicine supported by literature for its effectiveness to osteoarticular diseases were selected to conduct a screening of inhibition activity against the cathepsin K, an important enzyme responsible for cleavage of collagen, the main constituent of extracellular matrix of cartilage and bone. Out of the ten herbs selected (ginger, saffron, camellia, cat s claw, mentrasto , moringa , babaçu , devil s claw, urtica e pequi ), one, gengibre (Z. officinale), should be highlighted by a high inhibitory activity of its extracts and fractions against cathepsin K and due to its ancient use as a therapeutic agent. From the dichloromethane fraction obtained of the crude extract of the rhizome of Z. officinale were isolated and identified 18 compounds (4-gingerol, 6-gingerol, 8-gingerol, 6-shogaol, 8-shogaol, 10-shogaol, 6- paradol, 6-gingerdiol, methyl 6-gingerol, methyl 6-shogaol, diacetoxy-6-gingerdiol, methyl diacetoxy-6-gingerdiol, zingerone, gingerenone A, Galanolactone, 3-acetoxy- 5-hydroxy-1,7-bis(4 -hydroxy-3 -methoxyphenyl)-heptane and hexahydrocurcumin). From the hexane fraction and essential oil were identified two monoterpenes and four sesquiterpenes. The most active compounds against cathepsin K were gingerols and shogaols with longer alkyl chain. Optimization of the separation of major compounds (6, 8 and 10-gingerol) and an overload study of C18 column was performed using HPLC, obtained as result dozens to hundreds of milligrams of each gingerol with high purity. Structural modifications of 6-gingerol were carried out and of the seven derivatives obtained 4 presented significant increase in inhibition of cathepsin K. Of all the compounds, three, SSi6, 10-gingerol, 6-shogaol, were selected for later tests: determinating of the mode the inhibition against cathepsin K, inhibition against cathepsin K and inhibition of nitric oxide (NO) production, in cellular culture. The inhibitions determined were: partially noncompetitive, partially uncompetitive and complete uncompetitive for the SSi6, 10-gingerol and 6-shogaol, respectively. Excellent inhibition activity against the cathepsin K, in cellular culture, can be observed for SSi6 and 6-shogaol. In the inhibition assay of NO production, the 6- shogaol was the only compound that appeared as effective.Financiadora de Estudos e ProjetosDez plantas utilizadas pela medicina tradicional com indicativos na literatura de suas eficácias frente a doenças osteoarticulares foram selecionadas para a realização de uma triagem de atividade inibitória frente à catepsina K, uma importante enzima responsável pela clivagem do colágeno, principal constituinte da matriz extracelular da cartilagem e ossos. Das dez plantas selecionadas (gengibre, açafrão, camélia, unha-de-gato, mentrasto, moringa, babaçu, garra-do-diabo, urtigão e pequi), uma, gengibre (Zingiber officinale), merece destaque pela alta inibição de seu extrato e frações frente à catepsina K e por seu uso milenar como agente terapêutico. Da fração de diclorometano obtida do extrato bruto dos rizomas de Z. officinale isolou-se e identificou-se 18 substâncias (4-gingerol, 6-gingerol, 8-gingerol, 6-shogaol, 8- shogaol, 10-shogaol, 6-paradol, 6-gingerdiol, metil-6-gingerol, metil-6-shogaol, diacetato de 6-gingerdioila, diacetato de metil-6-gingerdioila, zingerona, gingerenona A, galanolactona, 3-acetato de 5-hidroxi-1,7-bis(4 -hidroxi-3 -metoxifenil)-heptila e hexaidrocurcumina). Da fração de n-hexano e do óleo essencial, foram identificados 2 monoterpenos e 4 sesquiterpenos. As substâncias mais ativas frente à catepsina K foram os gingerois e shogaois de maior cadeia alquílica. Otimização da separação das substâncias majoritárias (6, 8 e 10-gingerol) e um estudo de sobrecarga de uma coluna C18 por CLAE, foram realizados, obtendo-se como resultado o isolamento de dezenas a centenas de miligramas de cada gingerol com considerável grau de pureza. Modificações estruturais do 6-gingerol foram realizadas e, das sete substâncias obtidas, 4 tiveram um aumento considerável do poder inibitório. Das substâncias obtidas, três, SSi6, 10-gingerol, 6-shogaol, foram selecionadas para ensaios posteriores: determinação do tipo de inibição frente à catepsina K, inibição da catepsina K e inibição da produção de óxido nítrico (NO), em meio celular. As inibições determinadas foram não-competitiva parcial, acompetitiva parcial e acompetitiva completa, para o SSi6, 10-gingerol e 6-shogaol, respectivamente. Excelentes atividades de inibição frente à catepsina K, em meio celular, puderam ser observadas para o SSi6 e 6-shogaol. No ensaio de inibição da produção de NO, o 6- shogaol foi a única substância que se apresentou como efetivo
Patoomratana Tuchinda - One of the best experts on this subject based on the ideXlab platform.
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a new diarylheptanoid from the rhizomes of zingiber mekongense
Fitoterapia, 2011Co-Authors: Arthittaya Chareonkla, Manat Pohmakotr, Vichai Reutrakul, Chalobon Yoosook, Jitra Kasisit, Chanita Napaswad, Patoomratana TuchindaAbstract:Abstract A new diarylheptanoid, (3S,5S)-3,5-diacetoxy-1,7-bis(3,4,5-trimethoxyphenyl)heptane (1), together with the known docosyl trans-ferulate (2), (1S,2S,4S)-p-menthan-1,2,4-triol (3), 5αH-eudesmane-4α,11-diol (4), 5αH-eudesmane-4β,11-diol (5), 4α,10β-dihydroxy-1βH,5αH-guaia-6-ene (guaianediol) (6), (+)-Galanolactone (7), (E)-labda-8(17),12(13)-dien-15,16-olide (8), labda-8(17),13(14)-dien-15,16-olide (9), 3,5-dihydroxy-7,4′-dimethoxyflavone (10) and 3,5,3′-trihydroxy-7,4′-dimethoxyflavone (11) were isolated from the rhizomes of Zingiber mekongense. Their structures were determined by spectroscopic methods. The stereochemistry of 1 was proved through chemical conversion. Compounds 1, 4–7 and 9–11 exhibited anti-HIV-1 activities in the anti-syncytium assay using ∆Tat/revMC99 virus and 1A2 cell line system, while only compounds 7 and 11 were found active in the HIV-1 reverse transcriptase assay.
Arthittaya Chareonkla - One of the best experts on this subject based on the ideXlab platform.
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a new diarylheptanoid from the rhizomes of zingiber mekongense
Fitoterapia, 2011Co-Authors: Arthittaya Chareonkla, Manat Pohmakotr, Vichai Reutrakul, Chalobon Yoosook, Jitra Kasisit, Chanita Napaswad, Patoomratana TuchindaAbstract:Abstract A new diarylheptanoid, (3S,5S)-3,5-diacetoxy-1,7-bis(3,4,5-trimethoxyphenyl)heptane (1), together with the known docosyl trans-ferulate (2), (1S,2S,4S)-p-menthan-1,2,4-triol (3), 5αH-eudesmane-4α,11-diol (4), 5αH-eudesmane-4β,11-diol (5), 4α,10β-dihydroxy-1βH,5αH-guaia-6-ene (guaianediol) (6), (+)-Galanolactone (7), (E)-labda-8(17),12(13)-dien-15,16-olide (8), labda-8(17),13(14)-dien-15,16-olide (9), 3,5-dihydroxy-7,4′-dimethoxyflavone (10) and 3,5,3′-trihydroxy-7,4′-dimethoxyflavone (11) were isolated from the rhizomes of Zingiber mekongense. Their structures were determined by spectroscopic methods. The stereochemistry of 1 was proved through chemical conversion. Compounds 1, 4–7 and 9–11 exhibited anti-HIV-1 activities in the anti-syncytium assay using ∆Tat/revMC99 virus and 1A2 cell line system, while only compounds 7 and 11 were found active in the HIV-1 reverse transcriptase assay.
Manat Pohmakotr - One of the best experts on this subject based on the ideXlab platform.
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a new diarylheptanoid from the rhizomes of zingiber mekongense
Fitoterapia, 2011Co-Authors: Arthittaya Chareonkla, Manat Pohmakotr, Vichai Reutrakul, Chalobon Yoosook, Jitra Kasisit, Chanita Napaswad, Patoomratana TuchindaAbstract:Abstract A new diarylheptanoid, (3S,5S)-3,5-diacetoxy-1,7-bis(3,4,5-trimethoxyphenyl)heptane (1), together with the known docosyl trans-ferulate (2), (1S,2S,4S)-p-menthan-1,2,4-triol (3), 5αH-eudesmane-4α,11-diol (4), 5αH-eudesmane-4β,11-diol (5), 4α,10β-dihydroxy-1βH,5αH-guaia-6-ene (guaianediol) (6), (+)-Galanolactone (7), (E)-labda-8(17),12(13)-dien-15,16-olide (8), labda-8(17),13(14)-dien-15,16-olide (9), 3,5-dihydroxy-7,4′-dimethoxyflavone (10) and 3,5,3′-trihydroxy-7,4′-dimethoxyflavone (11) were isolated from the rhizomes of Zingiber mekongense. Their structures were determined by spectroscopic methods. The stereochemistry of 1 was proved through chemical conversion. Compounds 1, 4–7 and 9–11 exhibited anti-HIV-1 activities in the anti-syncytium assay using ∆Tat/revMC99 virus and 1A2 cell line system, while only compounds 7 and 11 were found active in the HIV-1 reverse transcriptase assay.
