The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers,and the compatibility mechanism of Jiao-Tai-Wan（JTW） composed of Rhizoma Coptidis granules an...The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers,and the compatibility mechanism of Jiao-Tai-Wan（JTW） composed of Rhizoma Coptidis granules and Cinnamon granules were investigated.The concentration of berberine in plasma of healthy male volunteers was determined directly by high performance liquid chromatogra-phy（HPLC） after an oral administration of Rhizoma Coptidis granules alone or combined with Cinnamon granules（JTW）.The plasma concentration-time curves of berberine were plotted.The data were analyzed with Drug and Statistics（DAS） 2.0 pharmacokinetic program（Chinese Pharmacology Society） to obtain the main pharmacokinetic parameters.The results showed that the plasma concentration-time curve of berberine was described by a two-compartment model.The Cmax,Tmax,t1/2 and CLz/F of berberine in Rhizoma Coptidis granules were 360.883 μg/L,2.0 h,3.882 h,119.320 L.h-1.kg-1 respectively,and those of berberine in JTW were 396.124 μg/L,1.5 h,4.727 h,57.709 L.h-1.kg-1 respectively.It was suggested that Rhizoma Coptidis granules combined with Cinnamon granules could increase the plasma concentration of berberine,promote berberine absorption and lengthen the detention time of berberine in healthy male volunteers.展开更多
Coptidis Rhizoma(Chinese:Huanglian)and Phellodendri Chinensis Cortex(Chinese:Huangbo)are widely used Traditional Chinese Medicine,and often used in combination because of their similar pharmacological effects in clini...Coptidis Rhizoma(Chinese:Huanglian)and Phellodendri Chinensis Cortex(Chinese:Huangbo)are widely used Traditional Chinese Medicine,and often used in combination because of their similar pharmacological effects in clinical practice.However,the quality control methods of the two drugs are different and complicated,which is time consuming and laborious in practical application.In this paper,rapid and simultaneous determination of moisture and berberine in Coptidis Rhizoma(CR)and Phellodendri Chinensis Cortex(PC)was realized by near-infrared spectroscopy(NIRs)combined with global models.Competitive adaptive reweighted sampling(CARS)and successive projection algorithm(SPA)method were applied for variable selection.Principal component analysis(PCA)and partial least squares regression method(PLSR)were applied for qualitative and quantitative analysis,respectively.The characteristic variables of berberine showed similarity and consistency in distribution,providing basis for the global models.For moisture content,the global model had relative standard error of prediction set(RSEP)value of 3.04%and 2.53%for CR and PC,respectively.For berberine content,the global model had RSEP value of 5.41%and 3.97%for CR and PC,respectively.These results indicated the global models based on CARS-PLS method achieved satisfactory prediction for moisture and berberine content,improving the determination e±ciency.Furthermore,the greater range and larger number of samples enhanced the reliance of the global model.The NIRs combined with global models could be a powerful tool for quality control of CR and PC.展开更多
Objective: Sepsis, a systemic response to infection, often leads to end-organ dysfunction. Despite its high rates of mortality and morbidity, its pathophysiology is still poorly understood. Coptidis Rhizoma and its ma...Objective: Sepsis, a systemic response to infection, often leads to end-organ dysfunction. Despite its high rates of mortality and morbidity, its pathophysiology is still poorly understood. Coptidis Rhizoma and its main active alkaloid compound, berberine, have been as anti-bacterial and anti-inflammatory drugs used in clinic. The objective of this study was to gain more insights towards understanding the sepsis associated with drug absorption and disposition and treatments of berberine and Coptidis Rhizoma dynamically.Methods: Pharmacokinetic and metabolomic studies of Coptidis Rhizoma and its main active component berberine have been performed.Results: Cecal ligation and puncture(CLP) induced sepsis showed marked changes of metabolites concerning energy metabolism and amino acids metabolisms, which could be reversed towards the normal state by Coptidis Rhizoma and berberine.Conclusion: Berberine exhibited an equivalent and even better therapeutic effect than Coptidis Rhizoma.展开更多
AIM:Coptidis Rhizoma(CR),the dried rhizomes of Asian herbs(including Coptis chinensis Franch),has been used to treat diabetes mellitus for thousands of years.We explored the possibility that CR acts directly on skelet...AIM:Coptidis Rhizoma(CR),the dried rhizomes of Asian herbs(including Coptis chinensis Franch),has been used to treat diabetes mellitus for thousands of years.We explored the possibility that CR acts directly on skeletal muscle,the major organ responsible for glucose homeostasis,and activates 5'-AMP-activated protein kinase(AMPK),a signaling intermediary leading to metabolic enhancement of skeletal muscle.METHODS:Isolated rat epitrochlearis and soleus muscles were incubated in a buffer containing a CR water extract(CE),and activation of AMPK and related events were examined.RESULTS:In response to CE treat-ment,phosphorylation of Thr172 at the catalyticαsubunit of AMPK,an essential step for full kinase activation,increased in both mus-cles.Phosphorylation of Ser79 of acetyl CoA carboxylase(ACC),an endogenous substrate of AMPK,increased concomitantly.Analysis of isoform-specific AMPK activity revealed that CE activated both the α1 and α2 isoforms of the catalytic subunit.Importantly,the maximal effect of CE on AMPK phosphorylation was significantly greater than that of berberine(BBR),indicating that the action of CE is not totally ascribed to BBR.CONCLUSION:We propose that CE is an acute activator of AMPK in both fast-and slow-twitch skeletal muscles.展开更多
基金supported by a grant from the National Natu-ral Sciences Foundation for Distinguished Young Scholars of China(No.30801492)
文摘The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers,and the compatibility mechanism of Jiao-Tai-Wan（JTW） composed of Rhizoma Coptidis granules and Cinnamon granules were investigated.The concentration of berberine in plasma of healthy male volunteers was determined directly by high performance liquid chromatogra-phy（HPLC） after an oral administration of Rhizoma Coptidis granules alone or combined with Cinnamon granules（JTW）.The plasma concentration-time curves of berberine were plotted.The data were analyzed with Drug and Statistics（DAS） 2.0 pharmacokinetic program（Chinese Pharmacology Society） to obtain the main pharmacokinetic parameters.The results showed that the plasma concentration-time curve of berberine was described by a two-compartment model.The Cmax,Tmax,t1/2 and CLz/F of berberine in Rhizoma Coptidis granules were 360.883 μg/L,2.0 h,3.882 h,119.320 L.h-1.kg-1 respectively,and those of berberine in JTW were 396.124 μg/L,1.5 h,4.727 h,57.709 L.h-1.kg-1 respectively.It was suggested that Rhizoma Coptidis granules combined with Cinnamon granules could increase the plasma concentration of berberine,promote berberine absorption and lengthen the detention time of berberine in healthy male volunteers.
基金supported by National Major Scientic and Technological Special Project for"Signicant New Drugs Development"(2018ZX09201010).
文摘Coptidis Rhizoma(Chinese:Huanglian)and Phellodendri Chinensis Cortex(Chinese:Huangbo)are widely used Traditional Chinese Medicine,and often used in combination because of their similar pharmacological effects in clinical practice.However,the quality control methods of the two drugs are different and complicated,which is time consuming and laborious in practical application.In this paper,rapid and simultaneous determination of moisture and berberine in Coptidis Rhizoma(CR)and Phellodendri Chinensis Cortex(PC)was realized by near-infrared spectroscopy(NIRs)combined with global models.Competitive adaptive reweighted sampling(CARS)and successive projection algorithm(SPA)method were applied for variable selection.Principal component analysis(PCA)and partial least squares regression method(PLSR)were applied for qualitative and quantitative analysis,respectively.The characteristic variables of berberine showed similarity and consistency in distribution,providing basis for the global models.For moisture content,the global model had relative standard error of prediction set(RSEP)value of 3.04%and 2.53%for CR and PC,respectively.For berberine content,the global model had RSEP value of 5.41%and 3.97%for CR and PC,respectively.These results indicated the global models based on CARS-PLS method achieved satisfactory prediction for moisture and berberine content,improving the determination e±ciency.Furthermore,the greater range and larger number of samples enhanced the reliance of the global model.The NIRs combined with global models could be a powerful tool for quality control of CR and PC.
基金funded by the Key Project of the National Natural Science Foundation of China(No.81430092,81773857)the Program for Changjiang Scholars and Innovative Research Team in University(IRT_15R63)the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘Objective: Sepsis, a systemic response to infection, often leads to end-organ dysfunction. Despite its high rates of mortality and morbidity, its pathophysiology is still poorly understood. Coptidis Rhizoma and its main active alkaloid compound, berberine, have been as anti-bacterial and anti-inflammatory drugs used in clinic. The objective of this study was to gain more insights towards understanding the sepsis associated with drug absorption and disposition and treatments of berberine and Coptidis Rhizoma dynamically.Methods: Pharmacokinetic and metabolomic studies of Coptidis Rhizoma and its main active component berberine have been performed.Results: Cecal ligation and puncture(CLP) induced sepsis showed marked changes of metabolites concerning energy metabolism and amino acids metabolisms, which could be reversed towards the normal state by Coptidis Rhizoma and berberine.Conclusion: Berberine exhibited an equivalent and even better therapeutic effect than Coptidis Rhizoma.
基金supported by the research grants from the Japan Society for the Promotion of Science (No.20500576)Japan Vascular Disease Research Foundation
文摘AIM:Coptidis Rhizoma(CR),the dried rhizomes of Asian herbs(including Coptis chinensis Franch),has been used to treat diabetes mellitus for thousands of years.We explored the possibility that CR acts directly on skeletal muscle,the major organ responsible for glucose homeostasis,and activates 5'-AMP-activated protein kinase(AMPK),a signaling intermediary leading to metabolic enhancement of skeletal muscle.METHODS:Isolated rat epitrochlearis and soleus muscles were incubated in a buffer containing a CR water extract(CE),and activation of AMPK and related events were examined.RESULTS:In response to CE treat-ment,phosphorylation of Thr172 at the catalyticαsubunit of AMPK,an essential step for full kinase activation,increased in both mus-cles.Phosphorylation of Ser79 of acetyl CoA carboxylase(ACC),an endogenous substrate of AMPK,increased concomitantly.Analysis of isoform-specific AMPK activity revealed that CE activated both the α1 and α2 isoforms of the catalytic subunit.Importantly,the maximal effect of CE on AMPK phosphorylation was significantly greater than that of berberine(BBR),indicating that the action of CE is not totally ascribed to BBR.CONCLUSION:We propose that CE is an acute activator of AMPK in both fast-and slow-twitch skeletal muscles.
