Study On Chemical Constituents And Biological Activities Of Nauclea Officinalis

Nauclea officinalis belongs to the Rubiaceae Juss(Nauclea Linn),which distributed mainly in Guangdong,Guangxi,Hainan and other provinces in southern China.the bark and twigs of N.officinalis is widely used for the treatment of fever,colds,sore throat,acute tonsillitis,conjunctivitis,enteritis,eczema and other ailments.Nauclea officinalis is reported to contain alkaloids and terpenoids as major components.?Objective?To study the chemical constituents from Nauclea officinalis.The obtained compounds were tested in vitro for cytotoxic potential against three tumor cell lines and anti-inflammatory.?Methods?The dried and powdered plant materials were extracted with 75% ethanol,the extract was isolated and purified by silica gel,Sephadex LH-20,ODS,preparative HPLC,re-crystallization etc.Then the structures of the obtained compounds were identified by MS UV,IR and NMR approaches as well as comparison with those reported data.The cytotoxic activities of seven compounds against human tumour cell lines(LOVO,A549 and Hep G2)were evaluated by MTT colorimetric assay,The seven compounds were also tested their anti-inflammatory in vitro.?Results?To study the CH2Cl2 and Et OAc fraction of methanol exact of N.officinalis,Twenty one compounds were characterised mainly by analysing its physical data including 1D,2D NMR,and Physicochemical properties,etc.Their chemical structures were identified as17-oxo-19-(Z)-naucline(1),10-hydroxyvincosamide(2),vincosamide(3),angustoline(4),angustine(5),nauclefine(6),1,2,3,4-tetrahydro-1-oxo-?-carboline(7),2?,3?-dihydroxy-urs-12-en-28-oic acid(8),2?,3?,19?-trihydroxyurs-12-en-28 oic acid(9),23-hydroxyursolic acid(10),2?,3?,19?,23-tetrahydroxyurs-12-en-28-oic acid(11),2?,3?,19?-trihydroxy-urs-12-en-28-oic acid(12),3-O-?-D-glucopyranosyl-23-hydroxyursolic acid(13),Naringin(14),kaempferol(15),3?,19?,23-trihydroxyurs-12-en-28-oic acid(16),ursolic acid(17),gallic acid(18),3,4-dihydroxybenzoic acid(19),daucosterol(20),?-sitosterol(21).Compounds 1-7 were tested in vitro for cytotoxic potential against three tumor cell lines and anti-inflammatory.Compounds 1-7 showed very weak cytotoxicity against human tumour cell lines.Compounds 1,4,5,6 and 7 showed significant anti-inflammatory activity.Compounds 2 and 3 displayed weak anti-inflammatory activity.?Conclusions?Twenty compounds were obtained and identified from Et OH extract of Nauclea officinalis,Among them,compound 1 was a new indole alkaloid,compounds 8-15 were isolated from the Nauclea officinalis for the first time,and compounds 1,4,5,6,7 showed significant anti-inflammatory activity.