Objective:To explore the effects of arteannuin B,arteannuic acid and scopoletin on the pharmacokinetics of artemisinin in mice.Methods:Artemisinin and a combination of artemisinin,arteannuin B,arteannuic acid and scop...Objective:To explore the effects of arteannuin B,arteannuic acid and scopoletin on the pharmacokinetics of artemisinin in mice.Methods:Artemisinin and a combination of artemisinin,arteannuin B,arteannuic acid and scopoletin were administered together to mice via oral administration.Blood samples were collected at different time intervals and pretreated by liquid-liquid extraction.The contents of four compounds in mouse plasma were determined by a validated HPLC-MS/MS method.Results:Compared to single artemisinin group,the C_(max) values from the combination group rose from 947 ng/mL to 1 254 ng/mL.AUC_((0-t))(2 371 h·ng/mL) was significantly higher than that from single artemisinin group(747 h·ng/mL).The peak time lag and the CL values reduced at a proportion of 66%.Conclusions:Arteannuin B,arteannuic acid and scopoletin can markedly affect the pharmacokinetics of artemisinin.展开更多
Arteannuic acid and(-)11R,13-d(?)ydroarteannuic acid are the key intermediates in the biosynthesis of arteannuin by the leaf homogenate of Artemisia annua L.,and arteannuic acid and epoxyarteannuic acid are the interm...Arteannuic acid and(-)11R,13-d(?)ydroarteannuic acid are the key intermediates in the biosynthesis of arteannuin by the leaf homogenate of Artemisia annua L.,and arteannuic acid and epoxyarteannuic acid are the intermediates of arteannuin B.and epoxyarteannuic acid can not be transformed into arteannuin by the homogenate.展开更多
基金supported by the National Natural Science Foundation of China (No.81573682 and No.81102752)the Beijing Natural Science Foundation (No.2112010)
文摘Objective:To explore the effects of arteannuin B,arteannuic acid and scopoletin on the pharmacokinetics of artemisinin in mice.Methods:Artemisinin and a combination of artemisinin,arteannuin B,arteannuic acid and scopoletin were administered together to mice via oral administration.Blood samples were collected at different time intervals and pretreated by liquid-liquid extraction.The contents of four compounds in mouse plasma were determined by a validated HPLC-MS/MS method.Results:Compared to single artemisinin group,the C_(max) values from the combination group rose from 947 ng/mL to 1 254 ng/mL.AUC_((0-t))(2 371 h·ng/mL) was significantly higher than that from single artemisinin group(747 h·ng/mL).The peak time lag and the CL values reduced at a proportion of 66%.Conclusions:Arteannuin B,arteannuic acid and scopoletin can markedly affect the pharmacokinetics of artemisinin.
基金This project was supported by National Natural Science Foundation of China.
文摘Arteannuic acid and(-)11R,13-d(?)ydroarteannuic acid are the key intermediates in the biosynthesis of arteannuin by the leaf homogenate of Artemisia annua L.,and arteannuic acid and epoxyarteannuic acid are the intermediates of arteannuin B.and epoxyarteannuic acid can not be transformed into arteannuin by the homogenate.
