90(P28) Tripterygium属植物に含まれる免疫抑制活性、抗HIV活性物質の探索(ポスター発表の部)

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The genus of Tripterygium has been used as traditional Chinese drugs for the treatment of cancer and as an insecticide for hundreds of years. Recently, the extracts (the so-called total multi-glycoside or T_<11>), derived from an water/chloroform extract of the roots of T. wilfordii Hook f. have been used in clinical treatment of rheumatoid arthritis, skin disorders, in male-fertility control and other inflammatory and autoimmune diseases. The precise mechanism of the therapeutic effect of T_<11>, however, has not been completely delineated. In order to search bioactive constituents of this genus, we started work on the isolation of the immunosuppressive and anti-HIV active principles of T. hypoglaucum and the extracts (T_<11>) of T wilfordii. Repeated column chromatography of the ethyl acetate soluble fraction from the methanol extract of the root barks of Tripterygium hypoglaucum (Levi.) Hutch and the extracts of T. wilfordii Hook f. yielded five novel sesquiterpene derivatives (1-5) from T. hypoglaucum and eleven new sesquiterpene alkaloids (16-26), three new diterpenoids (38-40) from the extracts (T_<11>) of T. wilfordii. Compound 1 was a sesquiterpene pyridine alkaloid derived from dihydroagarofuran polyol esters, contained evoninic acid and a monoterpene moiety by the analysis of 2D NMR spectral data, and finally determined by X-ray analysis. Compound 1 had a monoterpene structure bonded to the sesquiterpene molecule by ester linkage, are unique sesquiterpenoids first found in a natural source. In our bioactive screening experiment for above compounds, we examined inhibitory effect on cytokine production and anti-HIV activity. As a result in this study, compounds 53 and 54 showed significant inhibitory effect on cytokine production from lipopolysaccharide-stimulated human peripheral mononuclear cells compared with the reference compound (prednisolone), and compound 2 inhibited HIV replication in H9 lymphocytes with an EC_<50> value of <0.10mg/ml and it inhibited uninfected H9 cell growth with an IC_<50> value of>100mg/ml, calculated therapeutic index value of>1000. In general, TI>5.0 is considered to be significant activity; compounds 2, 7, 12 and 34 showed extremely potent anti-HIV activity with a TI value of>1000, that is uncommon in bioactive compounds from a natural source.
天然有機化合物討論会の論文
1999-09-01

90(P28) Tripterygium属植物に含まれる免疫抑制活性、抗HIV活性物質の探索(ポスター発表の部)

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