Study On Chemical Constituents And Their Bioactivities From Buddleja Daviddi

Buddleja daviddi Franch.(Loganiaceae)is widely distributed in the southwest ofChina.As a Chinese folk medicine,rhizomes of B.daviddi have the properties ofreducing tussis,expelling wind and removing cold,promoting blood circulation toarrest pain.B.davidii are used to treat pertussis,beriberoid disease,thresh damage,bone fracture,itching,empyrosis,and so on.Many constituents have been reported,such as flavonoids,phenylethanoids,triterpenes,lignins.Bioactivities have included neuroprotective effects,antioxidativeeffects,liver-protective activities,antiviral properties,and so on.In order to searchthe bioactive constituents from natural source,we began to study the chemicalconsitituents from B.daviddi.By repeated column chromatography,including Silicagel,Sephadex LH-20,Toyopearl HW-40 and macroporous adsorption resin,andpreparative HPLC,six new compounds(1-6)and 19 known compounds were isolatedfrom 95% EtOH extract of B.daviddi.The structures of compounds were elucidatedby means of IR,MS,¹H-NMR,2D-NMR spectra and X-ray.Compounds 7,12～25were isolated from B.daviddi for the first time.In a screen for immunosuppressive agents from the extract of B.daviddi,weexamined the inhibitory effect of the isolated compounds on lymphocytetransformation.Compounds 8～11,16 and 17 revealed a significantimmunosuppressive activity(IC₅₀values＜30.00μg/mL).In the anti-tumor screening experiment,the different extracts and isolatedcompounds from B.daviddi were detected by cytotoxity effect with BEL-7402/5-FU,L929 and HeLa cell lines.The P.E.and EtOAc extracts revealed significant antitumoractivities,we could presume that they were the efficient location of anti-tumoractivities.Compounds 8～11 and 14 revealed positive cytotoxic effects onBEL-7402/5-FU,L929 and HeLa cells.(IC₅₀values of compound 8＜20.00μg/mL)Furthermoe,in a screen for reversal agents of cancer multidrug resistance from B.daviddi,we investigated the reversal effect of sesquiterpene compound 8 and 10 onBEL-7402/5-FU and MCF-7/ADR cells by MTT assay.Compound 8 revealedpartially reverse effect on the multidrug resistance of MCF-7/ADR cells,theresistance index to VCR and DOX were 1.36 and 1.67 respectively in MCF-7/ADRcells.