Both Aconitum hemsleyanum and Aconitum geniculatun have abundant contents of yunaconitine(1).Yunaconitine(1)has similar skeleton to crassicauline A(3);the only difference between them is that 1 contains aα-hydroxyl g...Both Aconitum hemsleyanum and Aconitum geniculatun have abundant contents of yunaconitine(1).Yunaconitine(1)has similar skeleton to crassicauline A(3);the only difference between them is that 1 contains aα-hydroxyl group at C-3.Our team attempts to convert 1 into 3 because 3 owns pharmacological activity.There are two steps to achieve the transformation above:firstly,use dehydration reaction to transform yunaconitine(1)into dehydroyunaconitine(2);secondly,use hydrogen reduction to acquire crassicauline A(3).Compared with other methods,this one below is more suitable for production application and more concise;moreover,the cost is lower with higher yield.展开更多
The synthesis of a new N,19-seco norditerpenoid alkaloid 7 bearing nitro group from yunaconitine 1 as the starting material through a series of steps was described.
[Objectives]To establish an acute yunaconitine poisoning rat model with a single oral administration and to determine the contents of yunaconitine in rat tissues by UPLC-MS/MS method,then investigate the distribution ...[Objectives]To establish an acute yunaconitine poisoning rat model with a single oral administration and to determine the contents of yunaconitine in rat tissues by UPLC-MS/MS method,then investigate the distribution of yunaconitine in rats. [Methods]The rats were randomly divided into three groups and were intragastrically administered a single dose of 2. 2,1. 1,and 0. 7 mg/kg of yunaconitine,respectively.The rats were killed 2 h later,the stomach tissue,intestine tissue,liver tissue,pancreas tissue,kidney tissue,lung tissue,spleen tissue,heart tissue,bladder tissue,testis tissue,brain tissue and heart blood samples were collected. The contents of yunaconitine in the biological materials were determined by UPLC-MS/MS method after the biological samples extracted by liquid-liquid extraction. [Results] A rat model of the yunaconitine poisoning was made with a single dose of 1. 1 mg/kg,the concentrations of yunaconitine shown in the organs with the following order: stomach,small intestine,liver,pancreas,kidney,lung,spleen,heart,bladder,testis,heart blood and brain. [Conclusions]Yunaconitine was widely distributed in rats,especially the levels in the stomach,small intestine and liver were the highest. The conclusion is expected to provide a basis for the selection of test materials for the poisoning of Aconitum vilmorinianum Kom.展开更多
文摘Both Aconitum hemsleyanum and Aconitum geniculatun have abundant contents of yunaconitine(1).Yunaconitine(1)has similar skeleton to crassicauline A(3);the only difference between them is that 1 contains aα-hydroxyl group at C-3.Our team attempts to convert 1 into 3 because 3 owns pharmacological activity.There are two steps to achieve the transformation above:firstly,use dehydration reaction to transform yunaconitine(1)into dehydroyunaconitine(2);secondly,use hydrogen reduction to acquire crassicauline A(3).Compared with other methods,this one below is more suitable for production application and more concise;moreover,the cost is lower with higher yield.
基金Financial support for this research was provided by the National Natural Science Foundation of China (No. 3007088). We are grateful to Professor Xiao-Tian Liang for his advice on this manuscript.
文摘The synthesis of a new N,19-seco norditerpenoid alkaloid 7 bearing nitro group from yunaconitine 1 as the starting material through a series of steps was described.
基金Supported by Scientific and Technological Planning Project of Yunnan Province(2013FB118)Innovation Team Project of Kunming Medical University(CXTD201604)Scientific Research Foundation of Yunnan Provincial Department of Education(2017zDX161)
文摘[Objectives]To establish an acute yunaconitine poisoning rat model with a single oral administration and to determine the contents of yunaconitine in rat tissues by UPLC-MS/MS method,then investigate the distribution of yunaconitine in rats. [Methods]The rats were randomly divided into three groups and were intragastrically administered a single dose of 2. 2,1. 1,and 0. 7 mg/kg of yunaconitine,respectively.The rats were killed 2 h later,the stomach tissue,intestine tissue,liver tissue,pancreas tissue,kidney tissue,lung tissue,spleen tissue,heart tissue,bladder tissue,testis tissue,brain tissue and heart blood samples were collected. The contents of yunaconitine in the biological materials were determined by UPLC-MS/MS method after the biological samples extracted by liquid-liquid extraction. [Results] A rat model of the yunaconitine poisoning was made with a single dose of 1. 1 mg/kg,the concentrations of yunaconitine shown in the organs with the following order: stomach,small intestine,liver,pancreas,kidney,lung,spleen,heart,bladder,testis,heart blood and brain. [Conclusions]Yunaconitine was widely distributed in rats,especially the levels in the stomach,small intestine and liver were the highest. The conclusion is expected to provide a basis for the selection of test materials for the poisoning of Aconitum vilmorinianum Kom.
