Studies On The Anticancer Constituents Of Ardisia Bicolor Walker

Ardisia bicolor Walker.,a variety of Ardisia crenata Sims.,has been used as the traditional drug 'A.crenata' to treat sore throat,tonsillitis,peratodynia,injury and rheumatism in Traditional Chinese Medicine.The main chemical constituents,such as triterpenoid saponins and isocoumarins,were isolated from A.crenata and the pharmacology activities of anticancer and anti-HIV were clarified.However,few studies in A.bicolor had been reported.To investigate the anticancer and anti-HIV constituents in this plant,several methods have been used in the processes of separation and purification including polyamide chromatography column(CC),silca-gel CC,sephadex LH-20 CC,macroporous resin CC, pre-HPLC and so on.As a result,fifteen compounds have been obtained.On the basis of physical-chemical properties and spectral evidences,their structures were elucidated as:3-O-{α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl}-3β-hydroxy-13β, 28-epoxy-16-oxo-oleanan-30-al(1),3-O- {β-D- xylopyranosyl -(1→2)-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl)-3β-hydroxy-13β,28-epoxy-16a-hydr-oxy -30-al(2),3-O-{α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl} -3β-hydroxy-13β,28-epoxy-16α-hydroxy-30-al(3),3-O- {α-L-rha-mnopyranosyl -(1→2)-β-D-glucopyranosyl-(1→4)-[β- D-glucopyranosyl-(1←2)]-α-L-arabinopyranosyl} -3β-hydroxy- 13β,28-epoxy-16α-hydroxy-30-al(4),3β-O- {α-L-rhamnopyranosyl -(1→2)-β-D-glucopyranosyl-(14→4)-[β- D-glucopyranosyl-(1→2)]-α-L-arabinopyranosyl} - 16α,28-dihydroxyolean- 12-en-30-oic acid(5),bergenin(6), norbergenin(7),11-O-(3′,5′-dihydroxy-4′-methoxygalloyl)-bergenin(8), 11-O-galloylbergenin(9),β-sitosterol(10),a-spinasteml(11),stigmasterol(12),lupeol (13),caffeic acid(14),4-methoxy-3,5-dihydroxy-benzoic acid(15).Among them, compound 2,13,14,15 were isolated from A.bicolor for the first time,the others were firstly isolated from this genus.The experiments were guided by results of cytotoxic activities of three extractions from the plant,and compound 4,8and 9 were investigated in vitro suppressing the proliferation of SMMC-7721 cells by MTT assay for the first time.Data revealed that the EtOAC extraction and water-soluble part had showed moderate activity against SMMC-7721 cells in vitro. What's more,the effect of hydrosoluble part showed dosage relativity.However,compounds 4,8and 9 exhibited weakly activity against the proliferation of SMMC-7721 cells in vitro.So whether hydrosoluble chemicals play an important role in suppressing the cell proliferation and the action is a synergism need further confirmed.It has been reported that bergenin and norbergenin had strong anti-HIV activities. Substituting groups on C₃,C_J1 and C₅ of norbergenin augmented the effects.In A.bicolor, bergenin and norbergenin are major components.Structure-function relationship suggests us bergeninal derivates have anti-HIV activities,which still need more proofs.