| The fundamental problem in the research of traditional Chinese medicine preparation is the research on the material basis of pharmacodynamics.In the course of the development of traditional Chinese medicine preparation,the research on the basis of drug effect material is the only way for the modernization of traditional Chinese medicine.Therefore,innovative research and basic research from the source are the guarantee to make traditional Chinese medicine preparations to be controlled,efficient,convenient,stable and safe,and provide a scientific basis for the all-round development of traditional Chinese medicine preparation.Casearia kurzii,a small tree belonging to the Flacourtiaceae plant family,is a kind of Cacearia genus.The genus in the world is mainly distributed in tropical and subtropical regions,mainly distributed in Yunnan and Hainan provinces of China,Some species of this genus have been used for the treatment of dysentery,enteritis,gastric ulcer,virus infection,inflammation,and snakebite.The chemical constituents of the genus are mainly terpenes.Most of terpenoids contain cytotoxic activity,immunomodulatory activity,trypanosomiasis activity and antibacterial activity.In this study,the methanol extracts of the leaves of Casearia kurzii,were suspended in water,and then portioned by silica gel column chromatography,column chromatography and semi preparative HPLC separation method,combined with HRESIMS,NMR,CD spectral analysis method,and identified the structure 30 compounds,respectively:balanterpene C(1),balanterpene D(2),balanterpene E(3),balanterpene F(4),balanterpene H(5),balanterpene L(6),balanterpene N(7),balanterpene O(8),balanterpene P(9),balanterpene Q(10),balanterpene R(11),balanterpene S(12),corymbulosin M(13),13-Epito-rulousyl acetate[19-acetoxy-labda-8-(17),14-dien-13S-ol](14),2-Oxo-18-acetoxy-10?,17?,19?,20?-(-)-cle-roda-3,13(16),14-triene(15),balanspene G(16),graveopene F(17),balanspene F(18),casearlucin B(19),esculentin A(20),graveopene E(21),rel-18(S),19(R)-diacet-oxy-18,19-epoxy-6(R)-methoxy-2(S)-(2?-methylbutanoyloxy)-5(R),8(S),9(S),1 0(R)-cleroda-3,13(16),14-triene(22),graveopene G(23),balanterpene J(24),balanterpene G(25),24-Meth-ylenecycloartane-3?,22-diol(26),balanterpene A(27),balanterpene B(28),balanterpene K(29),22-hydroxy-cyclolaudenol(30),Compounds 1-12 are new compounds that have not been reported in the literature and compounds 13?14 and 26 were isolated from the genus Casearia for the first time.Combined with previous studies of pharmacological activities of Casearia kurzii related literatures,this paper take A549 cells,study on antitumor activity of new compounds have been isolated from Casearia kurzii.The results showed that compounds 6,8,9,10,11 significantly inhibit the growth of A549 cells in human lung cancer and anti tumor effect of compounds 8,9,11 higher than that of the positive control antineoplastic effect of etoposide(IC50 14.12 ?M),the IC50 values were 10.94,8.74,0.87,0.56 11.19 0.71 ?M,the results for the subsequent preparation of effective parts by Casearia kurzii and provide a theoretical.The final of the Casearia kurzii extract capsule preparation process was studied,through the granulation process of single factor test,The optimum formulation process was as follows:dry extract powder and dextrin were mixed with 1:6,and 80%ethanol as wetting agent to make soft wood.The three batches of capsules prepared according to the above formulation were in conformity with the standard of Chinese Pharmacopoeia in the 2015 edition.This conclusion provides a reference for the preparation of Casearia kurzii capsule.However,further research is still needed for the further and comprehensive quality inspection of the preparation. |
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