A new macrocyclic diterpenoid,named kansuinine J（1）,was isolated from the roots of Euphorbia kansui.Its structure was characterized on the basis of spectroscopic analysis.
Kansuinine A is a macrocyclic jatrophane diterpene that was isolated from Euphorbia kansui. Further investigation of the structure was revealed that the benzoyl group located at C-8 and the position of C-3 was the pr...Kansuinine A is a macrocyclic jatrophane diterpene that was isolated from Euphorbia kansui. Further investigation of the structure was revealed that the benzoyl group located at C-8 and the position of C-3 was the present of an acetyl group by means of HMQC, HMBC spectra.展开更多
Although compatibility is highly advocated in traditional Chinese medicine (TCM), inappropriate combination of some herbs may reduce the therapeutic action and even produce toxic effects. Kansui and licorice, one of T...Although compatibility is highly advocated in traditional Chinese medicine (TCM), inappropriate combination of some herbs may reduce the therapeutic action and even produce toxic effects. Kansui and licorice, one of TCM “Eighteen Incompatible Medicaments”, are the most representative cases of improper herbal combination, which may still be applied simultaneously under given conditions. However, the potential mechanism of their compatibility and incompatibility is unclear. In the present study, two different ratios of kansui and licorice, representing their compatibility and incompatibility respectively, were designed to elucidate their interaction by comparative plasma/tissue metabolomics and a heatmap with relative fold change. As a result, glycocholic acid, prostaglandin F2a, dihydroceramide and sphinganine were screened out as the principal alternative biomarkers of compatibility group;sphinganine, dihydroceramide, arachidonic acid, leukotriene B4, acetoacetic acid and linoleic acid were those of incompatibility group. Based on the values of biomarkers in each tissue, the liver was identified as the compatible target organ, while the heart, liver, and kidney were the incompatible target organs. Furthermore, important pathways for compatibility and incompatibility were also constructed. These results help us to better understand and utilize the two herbs, and the study was the first to reveal some innate characters of herbs related to TCM “Eighteen Incompatible Medicaments”.展开更多
Background:The herbs should be processed by different methods before use,and the efficacy and toxicity of Chinese herbal medicines may change,which may enhance efficacy and reduce toxicity after processing.Gansui(Kans...Background:The herbs should be processed by different methods before use,and the efficacy and toxicity of Chinese herbal medicines may change,which may enhance efficacy and reduce toxicity after processing.Gansui(Kansui radix)is a common clinical herbal medicine,and there are considerable changes in its toxicity and efficacy after processing.Gaocao(Glycyrrhizae radix et rhizome)has a detoxifying effect.Methods:Using the contents of euphorbiadienol and the alcohol-soluble extract of Glycyrrhizae radix-processed Kansui radix as evaluation indexes,response surface methodology was used to optimize the processing technology of Kansui radix by exploring the effects of Glycyrrhizae radix et rhizoma-addition amount,frying temperature,and frying time on the processing technology of Kansui radix.Meanwhile,response surface software was used to analyze experimental data to determine the processing parameters of Kansui radix by Glycyrrhizae radix et rhizoma.Integrative Pharmacology-based Research Platform of Traditional Chinese Medicine is used to analysis the potential ingredients of Kansui radix and verify the potential ingredients by western blotting.Results:The technology of Glycyrrhizae radix et rhizoma-processed Kansui radix was optimized for the Glycyrrhizae radix et rhizoma-addition amount of 27%,frying temperature of 180℃,and frying time of 11 min.The network pharmacology analysis revealed that Kansui radix could cause kidney,liver,and heart injury by the PI3K/AKT signaling pathway.Kansui radix at high or low dose could decrease the ratio of p-AKT/AKT while Glycyrrhizae radix et rhizoma-processed Kansui could increase it.Conclusion:The model established by response surface methodology is relatively accurate and can predict the contents of euphorbiadienol and alcohol extract of processed Kansui radix.The toxic effects and its mechanism of action of Kansui radix and processed Kansui radix on kidney,liver,and heart,from the perspective of systems biology,have provided scientific evidence to its clinical application.展开更多
Objective To investigate the mechanism of Radix Kansui(RK)stir-fried with vinegar(VRK)decreased hepatotoxicity in mice.Methods According to a random number table,40 mice were randomly divided into negative control gro...Objective To investigate the mechanism of Radix Kansui(RK)stir-fried with vinegar(VRK)decreased hepatotoxicity in mice.Methods According to a random number table,40 mice were randomly divided into negative control group(0.5%carboxymethylcellulose sodium,20 mL/kg),positive control group(0.1%mixture of carbon tetrachloride in soybean oil,20 mL/kg),RK group(the ethyl acetate extracts of RK,250 g crude drug/kg)and VRK group(the ethyl acetate extracts of VRK,250 g crude drug/kg)with 10 mice per group.All mice were administered orally by gavage daily for 7 continuous days.The morphology of liver tissues was examined to assess the liver injury by a transmission electron microscope.Hepatocyte apoptosis in vivo was determined by terminal deoxynucleotidyltransferase-mediated dUTP-biotin nickend labeling(TUNEL)assay.Immunohistochemical technique was adopted to detect the expression of particular antiapoptotic and proapoptotic proteins in the mitochondrial pathways,including B-cell lymphoma(Bcl-2)and caspase-3,as well as the expression of inflammatory mediators,including nuclear factor kappa B(NF-κB)and intercellular adhesion molecule-1(ICAM-1).Results Liver injury and hepatocyte apoptosis were observed in RK mice,and the liver injury were significantly reduced in VRK-treated mice.In immunohistochemistry study,compared with the negative control group,RK inhibited dramatically the Bcl-2 protein expression and significantly increased the expression of caspase-3,NF-κB and ICAM-1(all P<0.01).Compared with the RK group,VRK group induced significant increase on Bcl-2 protein expression,and decreased the caspase-3,NF-κB and ICAM-1 protein expression(P<0.05 or <0.01).Conclusion The mechanism of reduced hepatotoxicity of VRK may be associated with the reduced inflammation,regulation of antiapoptotic and proapoptotic mediators in the mitochondrial pathway.展开更多
基金supported by grants from the Ministry of Science and Technology(Nos.2009CB940900 and 2009CB522300)
文摘A new macrocyclic diterpenoid,named kansuinine J（1）,was isolated from the roots of Euphorbia kansui.Its structure was characterized on the basis of spectroscopic analysis.
文摘Kansuinine A is a macrocyclic jatrophane diterpene that was isolated from Euphorbia kansui. Further investigation of the structure was revealed that the benzoyl group located at C-8 and the position of C-3 was the present of an acetyl group by means of HMQC, HMBC spectra.
基金financially supported by the National Basic Research Program of China (2011CB505300,2011CB505303)the National Natural Science Foundation of China (81603258, 81673599,81773882)+4 种基金Key Research Project in Basic Science of Jiangsu College and University (14KJA360001)Youth Talent Project Funded by Shaanxi Higher Education Association for Science and Technology (20180307)333 High Level Talents Training Project Funded by Jiangsu Province (BRA2016387)financially supported by a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)the Discipline Innovation Team Program of Shaanxi University of Chinese Medicine (2019-YL10)
文摘Although compatibility is highly advocated in traditional Chinese medicine (TCM), inappropriate combination of some herbs may reduce the therapeutic action and even produce toxic effects. Kansui and licorice, one of TCM “Eighteen Incompatible Medicaments”, are the most representative cases of improper herbal combination, which may still be applied simultaneously under given conditions. However, the potential mechanism of their compatibility and incompatibility is unclear. In the present study, two different ratios of kansui and licorice, representing their compatibility and incompatibility respectively, were designed to elucidate their interaction by comparative plasma/tissue metabolomics and a heatmap with relative fold change. As a result, glycocholic acid, prostaglandin F2a, dihydroceramide and sphinganine were screened out as the principal alternative biomarkers of compatibility group;sphinganine, dihydroceramide, arachidonic acid, leukotriene B4, acetoacetic acid and linoleic acid were those of incompatibility group. Based on the values of biomarkers in each tissue, the liver was identified as the compatible target organ, while the heart, liver, and kidney were the incompatible target organs. Furthermore, important pathways for compatibility and incompatibility were also constructed. These results help us to better understand and utilize the two herbs, and the study was the first to reveal some innate characters of herbs related to TCM “Eighteen Incompatible Medicaments”.
基金funded by the grants from Applied Basic Research Program of Shanxi Province(201901D111342).
文摘Background:The herbs should be processed by different methods before use,and the efficacy and toxicity of Chinese herbal medicines may change,which may enhance efficacy and reduce toxicity after processing.Gansui(Kansui radix)is a common clinical herbal medicine,and there are considerable changes in its toxicity and efficacy after processing.Gaocao(Glycyrrhizae radix et rhizome)has a detoxifying effect.Methods:Using the contents of euphorbiadienol and the alcohol-soluble extract of Glycyrrhizae radix-processed Kansui radix as evaluation indexes,response surface methodology was used to optimize the processing technology of Kansui radix by exploring the effects of Glycyrrhizae radix et rhizoma-addition amount,frying temperature,and frying time on the processing technology of Kansui radix.Meanwhile,response surface software was used to analyze experimental data to determine the processing parameters of Kansui radix by Glycyrrhizae radix et rhizoma.Integrative Pharmacology-based Research Platform of Traditional Chinese Medicine is used to analysis the potential ingredients of Kansui radix and verify the potential ingredients by western blotting.Results:The technology of Glycyrrhizae radix et rhizoma-processed Kansui radix was optimized for the Glycyrrhizae radix et rhizoma-addition amount of 27%,frying temperature of 180℃,and frying time of 11 min.The network pharmacology analysis revealed that Kansui radix could cause kidney,liver,and heart injury by the PI3K/AKT signaling pathway.Kansui radix at high or low dose could decrease the ratio of p-AKT/AKT while Glycyrrhizae radix et rhizoma-processed Kansui could increase it.Conclusion:The model established by response surface methodology is relatively accurate and can predict the contents of euphorbiadienol and alcohol extract of processed Kansui radix.The toxic effects and its mechanism of action of Kansui radix and processed Kansui radix on kidney,liver,and heart,from the perspective of systems biology,have provided scientific evidence to its clinical application.
基金the National Natural Science Foundation of China(No.81673599,81503250,and 21705081)the Natural Science Research Program of Jiangsu Higher Education Institutions(No.15KJB360009)+2 种基金the Natural Science Foundation of Jiangsu Province(No.BK20161037)the Project Foundation of the Priority Academic Program Development of Jiangsu Higher Education Institutions(No.PAPD-2014)Six Talent Peaks Program of Jiangsu Province(No.2016-YY-026)。
文摘Objective To investigate the mechanism of Radix Kansui(RK)stir-fried with vinegar(VRK)decreased hepatotoxicity in mice.Methods According to a random number table,40 mice were randomly divided into negative control group(0.5%carboxymethylcellulose sodium,20 mL/kg),positive control group(0.1%mixture of carbon tetrachloride in soybean oil,20 mL/kg),RK group(the ethyl acetate extracts of RK,250 g crude drug/kg)and VRK group(the ethyl acetate extracts of VRK,250 g crude drug/kg)with 10 mice per group.All mice were administered orally by gavage daily for 7 continuous days.The morphology of liver tissues was examined to assess the liver injury by a transmission electron microscope.Hepatocyte apoptosis in vivo was determined by terminal deoxynucleotidyltransferase-mediated dUTP-biotin nickend labeling(TUNEL)assay.Immunohistochemical technique was adopted to detect the expression of particular antiapoptotic and proapoptotic proteins in the mitochondrial pathways,including B-cell lymphoma(Bcl-2)and caspase-3,as well as the expression of inflammatory mediators,including nuclear factor kappa B(NF-κB)and intercellular adhesion molecule-1(ICAM-1).Results Liver injury and hepatocyte apoptosis were observed in RK mice,and the liver injury were significantly reduced in VRK-treated mice.In immunohistochemistry study,compared with the negative control group,RK inhibited dramatically the Bcl-2 protein expression and significantly increased the expression of caspase-3,NF-κB and ICAM-1(all P<0.01).Compared with the RK group,VRK group induced significant increase on Bcl-2 protein expression,and decreased the caspase-3,NF-κB and ICAM-1 protein expression(P<0.05 or <0.01).Conclusion The mechanism of reduced hepatotoxicity of VRK may be associated with the reduced inflammation,regulation of antiapoptotic and proapoptotic mediators in the mitochondrial pathway.
