Dihydroxy-7,4′-dimethoxy-dihydroflavonol and （±）-3,5,7-trihydroxy-4′-methoxy-dihydroflavonol were found in many medicinal plants, here we describe a concise synthesis route by selective protection, aldol-cond...Dihydroxy-7,4′-dimethoxy-dihydroflavonol and （±）-3,5,7-trihydroxy-4′-methoxy-dihydroflavonol were found in many medicinal plants, here we describe a concise synthesis route by selective protection, aldol-condensation, 30% H2O2 epoxidation, cyclization and deprotection from 2,4,6-trihydroxyacetophone and anisaldehyde.展开更多
A sensitive,specific and rapid high-performance liquid chromatography-electronic spray ionization-tandem mass spectrometric method was developed and validated for the determination of 7,4'-dihydroxylflavone(7,4...A sensitive,specific and rapid high-performance liquid chromatography-electronic spray ionization-tandem mass spectrometric method was developed and validated for the determination of 7,4'-dihydroxylflavone(7,4'-DHF)in rat plasma.Genistein(internal standard,IS)was added in the collected plasma samples and subsided together by a simple one-step protein precipitation using acetonitrile-methanol(1:1,v/v).Chromatographic separation was performed on an Agilent Zorbax XDB C18 chromatography column and gradient elution with the mobile phase consisting of methanol and 0.1%formic acid was used.The mass spectrometric detection was performed by negative ion electro-spray ionization in multiple selected reactions monitoring(MRM)mode,with the transitions of m/z 253.1→113.0 for 7,4'-DHF and m/z 268.9→158.8 for IS.The calibration curve has liner relationship over the concentration range of 0.1-50.ng/mL(r=0.995.4).The intra-and inter-day precision(RSD%)was less than 10%,and the accuracy(RE%,relative error)ranged from-5.2%to 8.0%.The fully validated method was applied to the pharmacokinetics(PK)of 7,4'-dihydroxylflavone(7,4'-DHF)in rat plasma after oral administration(two doses:15 and 30.mg/kg)and intravenous injection(5.mg/kg).The result showed that Tmax and Cmax was 1.33±0.29.h and 0.12±0.02.ng/mL(15.mg/kg),and 1.17±0.29.h and 0.17±0.04.ng/mL(30.mg/kg),respectively.The bioavailability was 0.078%(15.mg/kg)and 0.070%(30.mg/kg),respectively.展开更多
文摘Dihydroxy-7,4′-dimethoxy-dihydroflavonol and （±）-3,5,7-trihydroxy-4′-methoxy-dihydroflavonol were found in many medicinal plants, here we describe a concise synthesis route by selective protection, aldol-condensation, 30% H2O2 epoxidation, cyclization and deprotection from 2,4,6-trihydroxyacetophone and anisaldehyde.
基金National Natural Science Foundation of China(81573693)。
文摘A sensitive,specific and rapid high-performance liquid chromatography-electronic spray ionization-tandem mass spectrometric method was developed and validated for the determination of 7,4'-dihydroxylflavone(7,4'-DHF)in rat plasma.Genistein(internal standard,IS)was added in the collected plasma samples and subsided together by a simple one-step protein precipitation using acetonitrile-methanol(1:1,v/v).Chromatographic separation was performed on an Agilent Zorbax XDB C18 chromatography column and gradient elution with the mobile phase consisting of methanol and 0.1%formic acid was used.The mass spectrometric detection was performed by negative ion electro-spray ionization in multiple selected reactions monitoring(MRM)mode,with the transitions of m/z 253.1→113.0 for 7,4'-DHF and m/z 268.9→158.8 for IS.The calibration curve has liner relationship over the concentration range of 0.1-50.ng/mL(r=0.995.4).The intra-and inter-day precision(RSD%)was less than 10%,and the accuracy(RE%,relative error)ranged from-5.2%to 8.0%.The fully validated method was applied to the pharmacokinetics(PK)of 7,4'-dihydroxylflavone(7,4'-DHF)in rat plasma after oral administration(two doses:15 and 30.mg/kg)and intravenous injection(5.mg/kg).The result showed that Tmax and Cmax was 1.33±0.29.h and 0.12±0.02.ng/mL(15.mg/kg),and 1.17±0.29.h and 0.17±0.04.ng/mL(30.mg/kg),respectively.The bioavailability was 0.078%(15.mg/kg)and 0.070%(30.mg/kg),respectively.
