The present study aimed at studying the characteristics of tissue distribution and excretion of scopoletin,a coumarin compound,in Sprague-Dawley rats.Scopoletin was orally administered at a dose of 50 mg/kg,and the co...The present study aimed at studying the characteristics of tissue distribution and excretion of scopoletin,a coumarin compound,in Sprague-Dawley rats.Scopoletin was orally administered at a dose of 50 mg/kg,and the concentrations in heart,liver,spleen,lung,kidney,muscle,fat,brain,testis,uterus,stomach and small intestine were determined at 5,15,30,60,120,240 min post-dose,respectively.It was shown that scopoletin was widely distributed into various tissues and reached the maximal concentrations in most tissues at 15 min post-dose,and the levels in liver,kidney,stomach and small intestine were relatively higher.Furthermore,the excretions of scopoletin in bile,urine and feces were only 0.032%,3.752% and 0.784%,respectively,suggesting that scopoletin was mainly eliminated by metabolism rather than excretion as parent drug.展开更多
[Objectives] This study was conducted to investigate the effect of scopoletin on the growth of breast cancer cell lines.[Methods] Cell culture,light microscopy and MTT assay for measuring cell viability were used to c...[Objectives] This study was conducted to investigate the effect of scopoletin on the growth of breast cancer cell lines.[Methods] Cell culture,light microscopy and MTT assay for measuring cell viability were used to compare the inhibition of different concentrations of scopoletin to breast cancer cells,so as to provide an experimental basis for finding new therapeutic drugs for breast cancer cells.[Results] It was shown that a high concentration of scopoletin can inhibit the growth of breast cancer cells and promote apoptosis.[Conclusions] Scopoletin can be used as a potential drug for the treatment of breast cancer.展开更多
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
Cancer is considered a leading cause of death worldwide due to its high morbidity and mortality rate.Conventional treatments for cancer therapy,such as chemotherapy,and radiotherapy,have been hampered by their side ef...Cancer is considered a leading cause of death worldwide due to its high morbidity and mortality rate.Conventional treatments for cancer therapy,such as chemotherapy,and radiotherapy,have been hampered by their side effects.Natural product-derived plants have been used for decades to treat diseases.Compared to conventional therapy,natural product has the potential to be effective against cancer with fewer side effects.This current review discussed the potential of scopoletin,a coumarin present in many edible plants,which elicits anticancer properties through multiple mechanisms,including modulating cell cycle arrest,inducing apoptosis,and regulating multiple signaling pathways.Understanding these mechanisms highlights the potential of scopoletin as a candidate for chemoprevention and chemotherapy.展开更多
[Objectives]This study was conducted to investigate the effect of scopoletin on the proliferation of breast cancer cell lines.[Methods]Cell viability,gene expression and cell cycle were measured by cell culture,RT-PCR...[Objectives]This study was conducted to investigate the effect of scopoletin on the proliferation of breast cancer cell lines.[Methods]Cell viability,gene expression and cell cycle were measured by cell culture,RT-PCR and flow cytometry.The effects of different concentrations of scopoletin on proliferation and cell cycle of breast cancer cells were compared.[Results]After a certain period of time,the breast cancer cells showed different degrees of apoptosis,and the growth cycle was arrested in the G1 phase,which promoted the down-regulation of three genes in breast cancer metastasis.[Conclusions]The study proves that scopoletin inhibits the proliferation and metastasis of breast cancer cells in a concentration-and time-dependent manner.展开更多
[Objective] This study aimed to investigate the acaricidal lffect of scopo- letin, and provide the biochemical evidences of scopoletin influencus Ca2＋-ATPase activity and gene expressions in the Carmine Spider Mite, ...[Objective] This study aimed to investigate the acaricidal lffect of scopo- letin, and provide the biochemical evidences of scopoletin influencus Ca2＋-ATPase activity and gene expressions in the Carmine Spider Mite, Tetranych＇us cinnabarinus. in increased protein contents; kinetic analysis showed that the catalytic capability of Ca2＋-ATPase was significantly reduced by scopoletin. [Conclusion] Scopoletin exhibits a significant inhibitory effect on Ca2＋-ATPase, and its acaricidal effect against T. cinnabarinus might be due to the direct inhibition of Ca2＋-ATPase.展开更多
Artemisia annua （Asteraceae） is well known for its antimalarial activities due to presence of the compound artemisinin. We isolated a methoxy coumarin from the stem part of A. annua and confirmed its identity as sco...Artemisia annua （Asteraceae） is well known for its antimalarial activities due to presence of the compound artemisinin. We isolated a methoxy coumarin from the stem part of A. annua and confirmed its identity as scopoletin through mass spectral data. The structure was established from 1H-nuclear magnetic resonance （NMR）, 13C-NMR. The compound scopoletin was evaluated for its feeding deterrence and growth inhibitory potential against a noxious lepidopteran insect, Spilartctia obliqua Walker. Scopoletin gave FD50（feeding deterrence of 50%） value of 96.7 μg/g diet when mixed into artificial diet. S. obliqua larvae （12-day-old） exposed to the highest concentration （250μg/g diet） of scopoletin showed 77.1% feeding-deterrence. In a growth inhibitory assay, scopoletin provided 116.9% growth inhibition at the highest dose of 250μg/g diet with a GI50 （growth inhibition of 50%） value of 20.9μg/g diet. Statistical analysis showed a concentrationdependent dose response relationship toward both feeding deterrent and growth inhibitory activities. Artemisinin is found mainly in the leaves of A. annua and not in the stems, which are typically discarded as waste. Therefore identification of scopoletin in stems of A. annua may be important as a source of this material for pest control.展开更多
基金The Fundamental Research Funds for the Central Universities(Grant No.JKZ2011016)the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘The present study aimed at studying the characteristics of tissue distribution and excretion of scopoletin,a coumarin compound,in Sprague-Dawley rats.Scopoletin was orally administered at a dose of 50 mg/kg,and the concentrations in heart,liver,spleen,lung,kidney,muscle,fat,brain,testis,uterus,stomach and small intestine were determined at 5,15,30,60,120,240 min post-dose,respectively.It was shown that scopoletin was widely distributed into various tissues and reached the maximal concentrations in most tissues at 15 min post-dose,and the levels in liver,kidney,stomach and small intestine were relatively higher.Furthermore,the excretions of scopoletin in bile,urine and feces were only 0.032%,3.752% and 0.784%,respectively,suggesting that scopoletin was mainly eliminated by metabolism rather than excretion as parent drug.
基金Supported by Education Department of Sichuan Province(14ZA0152)Health Department of Sichuan Province(130279)
文摘[Objectives] This study was conducted to investigate the effect of scopoletin on the growth of breast cancer cell lines.[Methods] Cell culture,light microscopy and MTT assay for measuring cell viability were used to compare the inhibition of different concentrations of scopoletin to breast cancer cells,so as to provide an experimental basis for finding new therapeutic drugs for breast cancer cells.[Results] It was shown that a high concentration of scopoletin can inhibit the growth of breast cancer cells and promote apoptosis.[Conclusions] Scopoletin can be used as a potential drug for the treatment of breast cancer.
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.
文摘Cancer is considered a leading cause of death worldwide due to its high morbidity and mortality rate.Conventional treatments for cancer therapy,such as chemotherapy,and radiotherapy,have been hampered by their side effects.Natural product-derived plants have been used for decades to treat diseases.Compared to conventional therapy,natural product has the potential to be effective against cancer with fewer side effects.This current review discussed the potential of scopoletin,a coumarin present in many edible plants,which elicits anticancer properties through multiple mechanisms,including modulating cell cycle arrest,inducing apoptosis,and regulating multiple signaling pathways.Understanding these mechanisms highlights the potential of scopoletin as a candidate for chemoprevention and chemotherapy.
基金Supported by Education Department of Sichuan Province(14ZA0152)Health Department of Sichuan Province(130279)
文摘[Objectives]This study was conducted to investigate the effect of scopoletin on the proliferation of breast cancer cell lines.[Methods]Cell viability,gene expression and cell cycle were measured by cell culture,RT-PCR and flow cytometry.The effects of different concentrations of scopoletin on proliferation and cell cycle of breast cancer cells were compared.[Results]After a certain period of time,the breast cancer cells showed different degrees of apoptosis,and the growth cycle was arrested in the G1 phase,which promoted the down-regulation of three genes in breast cancer metastasis.[Conclusions]The study proves that scopoletin inhibits the proliferation and metastasis of breast cancer cells in a concentration-and time-dependent manner.
基金Supported by National Natural Science Foundation of China(31272058)Specialized Research Fund for the Doctoral Program of Higher Education(20100182120021)
文摘[Objective] This study aimed to investigate the acaricidal lffect of scopo- letin, and provide the biochemical evidences of scopoletin influencus Ca2＋-ATPase activity and gene expressions in the Carmine Spider Mite, Tetranych＇us cinnabarinus. in increased protein contents; kinetic analysis showed that the catalytic capability of Ca2＋-ATPase was significantly reduced by scopoletin. [Conclusion] Scopoletin exhibits a significant inhibitory effect on Ca2＋-ATPase, and its acaricidal effect against T. cinnabarinus might be due to the direct inhibition of Ca2＋-ATPase.
文摘Artemisia annua （Asteraceae） is well known for its antimalarial activities due to presence of the compound artemisinin. We isolated a methoxy coumarin from the stem part of A. annua and confirmed its identity as scopoletin through mass spectral data. The structure was established from 1H-nuclear magnetic resonance （NMR）, 13C-NMR. The compound scopoletin was evaluated for its feeding deterrence and growth inhibitory potential against a noxious lepidopteran insect, Spilartctia obliqua Walker. Scopoletin gave FD50（feeding deterrence of 50%） value of 96.7 μg/g diet when mixed into artificial diet. S. obliqua larvae （12-day-old） exposed to the highest concentration （250μg/g diet） of scopoletin showed 77.1% feeding-deterrence. In a growth inhibitory assay, scopoletin provided 116.9% growth inhibition at the highest dose of 250μg/g diet with a GI50 （growth inhibition of 50%） value of 20.9μg/g diet. Statistical analysis showed a concentrationdependent dose response relationship toward both feeding deterrent and growth inhibitory activities. Artemisinin is found mainly in the leaves of A. annua and not in the stems, which are typically discarded as waste. Therefore identification of scopoletin in stems of A. annua may be important as a source of this material for pest control.
