Study On The Chemical Constituents Of "Fuzi" And "Yimucao Injection"

The lateral roots of Aconitum carmichaeli Debx.(Ranunculaceae) have been used as cardiac drugs in traditional Chinese medicine for a long history, while the material basis of the cardiac has not been determined. In order to study the material basis, the dissertation investigated chemical constituents of the lateral roots of Aconitum carmichaeli Debx., which has been used as traditional application parts for thousands of years. By using a variety of chromatographic techniques and spectroscopic methods, twenty-nine compounds (1*-29), including six new compounds (1*-6*) and one natural product (7#), have been isolated and structurally determined. The pyrazine alkaloids (compound4*and5*) have been obtained from the genus Aconitum for the first time. The pyrrole type alkaloids (compound6*and21) have been isolated from this plant for the first time.In the in vitro assays, compounds2*,3*,4*,5*,8and9showed activity against pentobarbital sodium-induced cardiomyocytes damage by recovering beating rhythm and increasing the cell viability. Compounds6*and22showed moderate antibacterial activity, compound22displayed antibacterial activity against Staphylococcus aureus, Macrococcus caseolyticus, Klebsiella pneumoniae and Streptococcus pneumoniae (MIC50,200,200and200μg/mL, respectively).Yimucao Injection has been used as gynecology drugs in clinical for a long time. To search the bioactive substances, the Yimucao Injection was phytochemically investigated to afford fourteen compounds, including one natural product. Names and structures of the purified compounds are listed in Table1and Figure1&2, respectively. Amino acids and theirs derivatives (30#-33) have been isolated from the injection for the first time. Compounds30#-33,35-36and38-43have been obtained from the genus Leonurus for the first time.In the in vitro assays, compounds35and36showed inhibited abnormal increase of platelet aggregation induced by ADP. Compounds33,34and35inhibited activity of the normal rat uterus, via inhibited the contraction frequency and contractile tension.In addition, the dissertation has summarized the structures and resources of the non-diterpene alkaloids in genus Aconitum and it helps others study this genus more easily and further.