b Institute of Chemistry, Academia Sinica, Taipei, Taiwan 11529, China One pot hydroiodination and deconjugation of 5 aryloxy(or thiophenyl) 3 pentyn 2 one with a reagent system of sodium iodide/trimethylsily...b Institute of Chemistry, Academia Sinica, Taipei, Taiwan 11529, China One pot hydroiodination and deconjugation of 5 aryloxy(or thiophenyl) 3 pentyn 2 one with a reagent system of sodium iodide/trimethylsilyl chloride/water in acetonitrile at 25 ℃ have been described. The plausible mechanism was discussed. The reaction provided a simple and useful method for the preparation of ( Z ) β substituted β,γ enones and ( Z ) β substituted α,β unsaturated ketones.展开更多
In the present study, 20 selected Lactobacillus strains already characterized in a previous research for their capability to grow in conditions simulating the intestinal environment, their resistance to antibiotics, t...In the present study, 20 selected Lactobacillus strains already characterized in a previous research for their capability to grow in conditions simulating the intestinal environment, their resistance to antibiotics, their antibacterial activity and their adhesion capability to intestinal human Caco-2 TC7 and HT-29 MTX cell lines, were further investigated to explore more their probiotic properties. Growth behaviour in the presence of prebiotic (fructooligosac-charides (FOS) and lactulose) at a concentration of 2%, cholesterol removal by measuring the residual cholesterol in medium supplemented with cholesterol, ability to deconjugate bile salts using BSH enzyme and antioxidant activity of culture supernatant of Lactobacillus strains by ABTS·+ and DPPH methods were analyzed. All probiotic strains demonstrated important prebiotic assimilation (P > 0.05) even with OD600 > 3 after 30 h of contact, cholesterol removal ability with maximum percentage of 57% after 24 h of contact and they were found to liberate significantly (P < 0.05) more cholic acid with maximum of 0.40 mM of sodium glycocholate, 0.33 mM of sodium taurocholate and 0.41 mM of their mixte and scavenge both radicals with 52% and 2.19% of ABTS·+ and DPPH respectively. This study confirmed the suitability of these probiotic strains for application in functional food formulations especially where cholesterol reduction and antioxidant activity in food are needed to assess possible in vivo human health benefits.展开更多
Equol is a metabolite of soybean isoflavone, daidzein, and many health benefits are expected. Endogenous equol in urine is S-equol and mostly exists as glucuronate or sulfate conjugate. In this study we preliminary es...Equol is a metabolite of soybean isoflavone, daidzein, and many health benefits are expected. Endogenous equol in urine is S-equol and mostly exists as glucuronate or sulfate conjugate. In this study we preliminary established the simple enzyme-linked immunosorbent assay (ELISA) without deconjugation, then developed the S-equol specific ELISA involves deconjugation showing high stereospecificity to S-equol without using stereospecific antibody. For the simple ELISA, we used a polyclonal antibody that targets the regions not influenced by inhibition by conjugation of glucuronate and sulfate and achieved the correlation coefficient;r = 0.975, but the value was 30 % lower than high performance liquid chromatography (HPLC). Developing upon this we invented the specific ELISA established from S-equol homogeneous combination for the standard and enzyme-labeled antigen to enhance stereospecificity. The correlation with HPLC was favorable: r = 0.986, y = 0.996x – 6. Compared to the previous method using (R,S)-equol combination, cross-reactivity with R-equol was reduced from 65 to 13 %, and that with daidzein from 0.31% to 0.08%, markedly increased in the specificity. This study is expected to be applied for both simple clinical researches, and stereospecific immunoassays in which specific antibody preparation is difficult.展开更多
The syntheses of 2-[(4-Fluorophenoxy)methylene]-4-(3,4,5-trimethoxyphenyl)-4-butanolide 8and 2-[(4-Fluorophenoxy)methyl]-4-(3,4,5-trimethoxyphenyl)-2-buten-γ-lactone 9 from 3-(4-Fluoro-phenoxy)propyne 1 tbrough 5 ste...The syntheses of 2-[(4-Fluorophenoxy)methylene]-4-(3,4,5-trimethoxyphenyl)-4-butanolide 8and 2-[(4-Fluorophenoxy)methyl]-4-(3,4,5-trimethoxyphenyl)-2-buten-γ-lactone 9 from 3-(4-Fluoro-phenoxy)propyne 1 tbrough 5 steps have been described.The one pot deconjugation and hydroiodination of 3with a reagent system of TMSCL/NaI/H 2O in CH 3CN was key step.展开更多
Deconjugation of cyclopent-2-enone aldols were attempted under various conditions, and the desired deconjugated product was achieved via dianion approach. Various results obtained in this study are explained by struc... Deconjugation of cyclopent-2-enone aldols were attempted under various conditions, and the desired deconjugated product was achieved via dianion approach. Various results obtained in this study are explained by structure and transition state analysis.展开更多
基金theScienceCouncilandAcademiaSinicaofTaiwan China
文摘b Institute of Chemistry, Academia Sinica, Taipei, Taiwan 11529, China One pot hydroiodination and deconjugation of 5 aryloxy(or thiophenyl) 3 pentyn 2 one with a reagent system of sodium iodide/trimethylsilyl chloride/water in acetonitrile at 25 ℃ have been described. The plausible mechanism was discussed. The reaction provided a simple and useful method for the preparation of ( Z ) β substituted β,γ enones and ( Z ) β substituted α,β unsaturated ketones.
文摘In the present study, 20 selected Lactobacillus strains already characterized in a previous research for their capability to grow in conditions simulating the intestinal environment, their resistance to antibiotics, their antibacterial activity and their adhesion capability to intestinal human Caco-2 TC7 and HT-29 MTX cell lines, were further investigated to explore more their probiotic properties. Growth behaviour in the presence of prebiotic (fructooligosac-charides (FOS) and lactulose) at a concentration of 2%, cholesterol removal by measuring the residual cholesterol in medium supplemented with cholesterol, ability to deconjugate bile salts using BSH enzyme and antioxidant activity of culture supernatant of Lactobacillus strains by ABTS·+ and DPPH methods were analyzed. All probiotic strains demonstrated important prebiotic assimilation (P > 0.05) even with OD600 > 3 after 30 h of contact, cholesterol removal ability with maximum percentage of 57% after 24 h of contact and they were found to liberate significantly (P < 0.05) more cholic acid with maximum of 0.40 mM of sodium glycocholate, 0.33 mM of sodium taurocholate and 0.41 mM of their mixte and scavenge both radicals with 52% and 2.19% of ABTS·+ and DPPH respectively. This study confirmed the suitability of these probiotic strains for application in functional food formulations especially where cholesterol reduction and antioxidant activity in food are needed to assess possible in vivo human health benefits.
文摘Equol is a metabolite of soybean isoflavone, daidzein, and many health benefits are expected. Endogenous equol in urine is S-equol and mostly exists as glucuronate or sulfate conjugate. In this study we preliminary established the simple enzyme-linked immunosorbent assay (ELISA) without deconjugation, then developed the S-equol specific ELISA involves deconjugation showing high stereospecificity to S-equol without using stereospecific antibody. For the simple ELISA, we used a polyclonal antibody that targets the regions not influenced by inhibition by conjugation of glucuronate and sulfate and achieved the correlation coefficient;r = 0.975, but the value was 30 % lower than high performance liquid chromatography (HPLC). Developing upon this we invented the specific ELISA established from S-equol homogeneous combination for the standard and enzyme-labeled antigen to enhance stereospecificity. The correlation with HPLC was favorable: r = 0.986, y = 0.996x – 6. Compared to the previous method using (R,S)-equol combination, cross-reactivity with R-equol was reduced from 65 to 13 %, and that with daidzein from 0.31% to 0.08%, markedly increased in the specificity. This study is expected to be applied for both simple clinical researches, and stereospecific immunoassays in which specific antibody preparation is difficult.
文摘The syntheses of 2-[(4-Fluorophenoxy)methylene]-4-(3,4,5-trimethoxyphenyl)-4-butanolide 8and 2-[(4-Fluorophenoxy)methyl]-4-(3,4,5-trimethoxyphenyl)-2-buten-γ-lactone 9 from 3-(4-Fluoro-phenoxy)propyne 1 tbrough 5 steps have been described.The one pot deconjugation and hydroiodination of 3with a reagent system of TMSCL/NaI/H 2O in CH 3CN was key step.
文摘 Deconjugation of cyclopent-2-enone aldols were attempted under various conditions, and the desired deconjugated product was achieved via dianion approach. Various results obtained in this study are explained by structure and transition state analysis.
