| Hedyotis caudatifolia Merr.et Metcalf belongs to Hedyotis Linn genera in Rubiaceae family.It is mainly distributed in Guangdong,Guangxi,Jiangxi,south of Zhejiang,Hunan provinces etc.With moderate,sweet,cool,and non-poisonous drug property,H.caudatifolia can relieve cough and eliminate phlegm,invigorate spleen to promote digestion,stop bleeding,relieve fever and moisten lung.Therefore,in clinical,H.caudatifolia is used to treat tuberculosis hemoptysis,bronchitis,pediatric malnutrition disorders,and pediatric fever.At present,there are few works to study the chemical constituents of H.caudatifolia,only a small amount of coumarins,steroids,triterpenoids and anthraquinones have been isolated.So,study on its chemical constituents and the finding of some novel antitumor ingredients could be used to develop the therapeutic products and the development of therapeutic drugs and clinical application has important significance.The systematic and scientific research on the components of this plant were carried out,and 20 compounds were obtained by the modern chromatographic techniques of chromatography on sillca gel,HPLC,Sephadex LH-20 and so on.Their structures were identified by physicochemical properties,MS,and NMR spectra asβ-sitosterol（1）,9-hydroxy-2,3-dimethoxy-1,4-anthraquinone（2）,1,6-dihydroxy-2-methyl-9,10-anthraquinone（3）,1,4-dihydroxy-2-hydroxymethyl-9,10-anthraquinone（4）,10-hydroxy-2-hydroxymethyl-1,4-anthraquinone（5）,5α-stigmstane-3,6-dione（6）,1-hydroxy-2-hydroxymethyl-9,10-anthraquinone（7）,7-hydro-xy-6-methoxycoumain（8）,oleanolic acid（9）,ursane acid（10）,pomolic acid（11）,1,4,7-trihydroxy-2-hydroxymethyl-9,10-anthraquinone（12）,3α,19α-dihydroxyurs-12-en-24,28-dioic acid（13）,2α,3β,24-trihydroxyolean-12-en-28-oic acid（14）,1,6-dihydroxy-2,5-dimethoxy-9,10-anthraquinone（15）,daucosterol（16）,2α,3α-dihydroxyolean-12-en-28-oic acid（17）,3β,24-dihydroxyolean-12-en-28-oic acid（18）,hedycaffeoylglucoside A（19）,3β,19α,24-trihydroxyurs-12-en-28-olic acid（20）.Compounds 12,15,and 19are three new natural products.The antitumor activities against to HL-60（human promyelocytic leukemic cell）of H.caudatifolia extract（petroleum ether extract,ethyl acetate extract,water extract）were examined by MTT assays.As a result,ethyl acetate extract and water extract showed good antitumor activities with IC50 values of 10.67 and 12.58μM respectively,while petroleum ether extract exibited relatively weak antitumor activities with IC50values of 30.65μM.So ethyl acetate extract and water extract were further purified.The antitumor activities against to HL-60（human promyelocytic leukemic cell）,Bcap37（breast cancer cell）,SMMC7721（Human hepatoma cell）,P388（mouse leukemia cells）of compounds 7,12,13,15,19 were also examined by MTT assays.As a result,these five compounds all show moderate inhibitory activity against these four kinds of tumor cells with IC50 values from 13.71 to 50.21μM.This thesis also summarized the chemical constituents and biological activities of Hedyotis Linn.The results of this study will provide the scientific basis to the development and utilization of H.caudatifolia. |
