Objective:To explore the anti-tumor effects of asiatic moonseed rhizome extraction-dauricine on bladder cancer EJ cell strain,prostate cancer PC-3Mcell strain and primary cell culture system.Methods:The main effective...Objective:To explore the anti-tumor effects of asiatic moonseed rhizome extraction-dauricine on bladder cancer EJ cell strain,prostate cancer PC-3Mcell strain and primary cell culture system.Methods:The main effective component-phenolic alkaloids of Menispermum dauricum was extracted and separated from asiatic moonseed rhizome by chemical method.MTT method was used to detect dauricine anti-tumor effect.Results:Dauricine had an obvious proliferation inhibition effect on the main tumor cells in urinary system.The minimum drug sensitivity concentration was between 3.81-S.ISμg/mL,and the inhibition ratio increased with the increase of concentration.Condusioiis:Dauricine,the main effective component extracted from asiatic moonseed rhizome,had a good inhibition effect on tumor cells in urinary system.At the same time,Dauricine has certain inhibition effects on the primary cultured tumor cell.展开更多
Summary: To establish the determination method of dauricine (Dan) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be ...Summary: To establish the determination method of dauricine (Dan) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dan and its internal standard, daurisoline were 9. 2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70 %, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0. 030 to 3. 000 rug/L in blood samples and 0. 050 to 5. 000 mg/L in other tissue samples. The intraday and interday coefficients of varia- tion were below 10 %. The results showed that the method can be used for detecting Dan in all kinds of biological samples.展开更多
To study the metabolism of dauricine in vivo and in vitro and identify the structure of its main metabolites, urine of rats after drug administration as the samples of dauricine metabolism in vivo was studied. Rat liv...To study the metabolism of dauricine in vivo and in vitro and identify the structure of its main metabolites, urine of rats after drug administration as the samples of dauricine metabolism in vivo was studied. Rat liver S9 fraction was prepared and the oxygenation metabolism system reconstituted to perform phase I reaction of dauricine in vitro. TLC, HPLC DAD and MS were used to analyze and identify dauricine and its main phase I metabolites in the samples. The results showed that besides the untransformed dauricine, in the urine samples there was little product of X' which had the same features of TLC, HPLC DAD and MS as those of N desmethyl dauricine (N ddau). Part of dauricine could be transformed to a main metabolite X after incubating with S9 fraction in appropriate conditions. The molecular ion peak of X was m/z 611. The full scan MS2 spectrum of m/z 611 peak from S9 sample were m/z 580, m/z 566, m/z 552, m/z 206, which were same as those of N ddau. Liver is the major organ for dauricine metabolism and part of dauricine is biotransformed by liver. The major metabolite is considered to be N ddau.展开更多
Intravenous injection of platelet agonists ADP and thrombin induced the accumulation of 111 In labelled platelets within the pulmonary vasculature. Pretreatment with i.v. administration of Dauricine significan...Intravenous injection of platelet agonists ADP and thrombin induced the accumulation of 111 In labelled platelets within the pulmonary vasculature. Pretreatment with i.v. administration of Dauricine significantly inhibited the platelet accumulation induced by ADP and thrombin in a dose related fashion and this effect lasted less than 40 min. Inhibitor of NO synthase, L NAME, did not change the inhibition of platelet accumulation by Dauricine, but inhibitor of cyclooxygenase, indomethacin, abolished the inhibitory action of Dauricine. These results suggest that Dauricine pretreatment inhibits ADP and thrombin induced platelet aggregation in vivo and its mechanism is related to inhibition of arachidonic acid metabolism.展开更多
Objective: To investigate the effect of dauricine on the irreversible platelet aggregability of patients with mitral stenosis (MS).Methods: Glycoprotein Ⅳ (GPⅣ ) and thrombospondin (TSP) levels on the membrane surfa...Objective: To investigate the effect of dauricine on the irreversible platelet aggregability of patients with mitral stenosis (MS).Methods: Glycoprotein Ⅳ (GPⅣ ) and thrombospondin (TSP) levels on the membrane surface of the stationary platelet or platelet activated by thrombin (0. 05 U/ml, 0. 1 U/ml,0. 5 U/ml, 1. 0 U/ml) in 16 patients with MS were measured with flow cytometric method and compared with those of the healthy (14 subjects). Results: The GPⅣ level of stationary platelet, the GPⅣ and TSP level of activated platelet in MS patients were higher than those in the healthy significantly (P < 0. 01,< 0. 05, < 0. 005 ), while the TSP level of stationary platelet in the patients was not different to the healthy (P > 0. 05). The GPⅣ redistribution on the activated platelet surface was apparently inhibited by dauricine (50 μmol/L, P < 0. 05 - 0. 005) and the release of TSP from intracellular α-granules was inhibited by dauricine only in the activated platelets induced by thrombin of low concentration (0. 05 U/ml and 0. 1 U/ml, P < 0. 05 - 0. 01 ), inhibiting effect was not found in those activated with high concentration of thrombin. Conclusion: The activity and reactivity to thrombin of platelets increased in MS patients, and dauricine was able to reduce the occurrence of the irreversible platelet aggregation in MS patients.Original article on CJIM(Chin) 1998; 18(8): 461展开更多
文摘Objective:To explore the anti-tumor effects of asiatic moonseed rhizome extraction-dauricine on bladder cancer EJ cell strain,prostate cancer PC-3Mcell strain and primary cell culture system.Methods:The main effective component-phenolic alkaloids of Menispermum dauricum was extracted and separated from asiatic moonseed rhizome by chemical method.MTT method was used to detect dauricine anti-tumor effect.Results:Dauricine had an obvious proliferation inhibition effect on the main tumor cells in urinary system.The minimum drug sensitivity concentration was between 3.81-S.ISμg/mL,and the inhibition ratio increased with the increase of concentration.Condusioiis:Dauricine,the main effective component extracted from asiatic moonseed rhizome,had a good inhibition effect on tumor cells in urinary system.At the same time,Dauricine has certain inhibition effects on the primary cultured tumor cell.
文摘Summary: To establish the determination method of dauricine (Dan) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dan and its internal standard, daurisoline were 9. 2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70 %, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0. 030 to 3. 000 rug/L in blood samples and 0. 050 to 5. 000 mg/L in other tissue samples. The intraday and interday coefficients of varia- tion were below 10 %. The results showed that the method can be used for detecting Dan in all kinds of biological samples.
基金This project was suported by a grant from the foundation of Youth Sciences and Technology Chenguang Planning ofWuhan (No.2 0
文摘To study the metabolism of dauricine in vivo and in vitro and identify the structure of its main metabolites, urine of rats after drug administration as the samples of dauricine metabolism in vivo was studied. Rat liver S9 fraction was prepared and the oxygenation metabolism system reconstituted to perform phase I reaction of dauricine in vitro. TLC, HPLC DAD and MS were used to analyze and identify dauricine and its main phase I metabolites in the samples. The results showed that besides the untransformed dauricine, in the urine samples there was little product of X' which had the same features of TLC, HPLC DAD and MS as those of N desmethyl dauricine (N ddau). Part of dauricine could be transformed to a main metabolite X after incubating with S9 fraction in appropriate conditions. The molecular ion peak of X was m/z 611. The full scan MS2 spectrum of m/z 611 peak from S9 sample were m/z 580, m/z 566, m/z 552, m/z 206, which were same as those of N ddau. Liver is the major organ for dauricine metabolism and part of dauricine is biotransformed by liver. The major metabolite is considered to be N ddau.
文摘Intravenous injection of platelet agonists ADP and thrombin induced the accumulation of 111 In labelled platelets within the pulmonary vasculature. Pretreatment with i.v. administration of Dauricine significantly inhibited the platelet accumulation induced by ADP and thrombin in a dose related fashion and this effect lasted less than 40 min. Inhibitor of NO synthase, L NAME, did not change the inhibition of platelet accumulation by Dauricine, but inhibitor of cyclooxygenase, indomethacin, abolished the inhibitory action of Dauricine. These results suggest that Dauricine pretreatment inhibits ADP and thrombin induced platelet aggregation in vivo and its mechanism is related to inhibition of arachidonic acid metabolism.
文摘Objective: To investigate the effect of dauricine on the irreversible platelet aggregability of patients with mitral stenosis (MS).Methods: Glycoprotein Ⅳ (GPⅣ ) and thrombospondin (TSP) levels on the membrane surface of the stationary platelet or platelet activated by thrombin (0. 05 U/ml, 0. 1 U/ml,0. 5 U/ml, 1. 0 U/ml) in 16 patients with MS were measured with flow cytometric method and compared with those of the healthy (14 subjects). Results: The GPⅣ level of stationary platelet, the GPⅣ and TSP level of activated platelet in MS patients were higher than those in the healthy significantly (P < 0. 01,< 0. 05, < 0. 005 ), while the TSP level of stationary platelet in the patients was not different to the healthy (P > 0. 05). The GPⅣ redistribution on the activated platelet surface was apparently inhibited by dauricine (50 μmol/L, P < 0. 05 - 0. 005) and the release of TSP from intracellular α-granules was inhibited by dauricine only in the activated platelets induced by thrombin of low concentration (0. 05 U/ml and 0. 1 U/ml, P < 0. 05 - 0. 01 ), inhibiting effect was not found in those activated with high concentration of thrombin. Conclusion: The activity and reactivity to thrombin of platelets increased in MS patients, and dauricine was able to reduce the occurrence of the irreversible platelet aggregation in MS patients.Original article on CJIM(Chin) 1998; 18(8): 461
