| Budget Amount *help |
¥1,600,000 (Direct Cost: ¥1,600,000)
Fiscal Year 1987: ¥300,000 (Direct Cost: ¥300,000)
Fiscal Year 1986: ¥300,000 (Direct Cost: ¥300,000)
Fiscal Year 1985: ¥1,000,000 (Direct Cost: ¥1,000,000)
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| Research Abstract |
The extraction and isolation methods of nine homoisoflavanones and homoisoflavones from "Bakumonod" (Ophiopogonis Tuber; tuber of Ophiopogon japonicus Ker-Gawler), which is described in the present Japanese Pharmaco[poeia, have been reinvestigated and the samples testing for the biological activity have been prepared. As the results, the effective method for the isolation and purification of homoisoflavonoids were established as follows. The methanol extract of each crude drug was partitioned between ether and water, and the ether extract chromatographed on Sephadex LH-20 column with water to separate crude phenolic fraction, which was rechromatographed on Silisic acid column with chrologorm-methanol solvent system. Each fraction was further chromatographed on the column of Silicic acid-benzene system, Sephadex LH-20-ethanol system or Silicic acid-(benzene acetone) system. Based on the results, six homoisoflavonoidal compounds from O. ohwii Okuyama, four from O. jaburan (Kunth) Lodd. and seven from O. chekiangensis Kimura et H. Migo have been isolated and the structures have been elucidated. Furthermore, the presence of homoisoflavonoidal compounds in O. planiscapus Nakai and O. japonicus Ker-Gawl. f. nanus hort. has been confirmed. The synthesis of homoisoflavonoidal compounds to test the biological and pharmacological activity has been carried out by Dr. Hirai. For the selection of the objective compound, six natural homoisoflavonoid were examined the differentiation activity of three different human leukemia cell line (U-937,HL-60, ML-1). The known methods for the synthesis of methylophiopogonanone A, B, isoophiopogonone A, B, desmethylophiopogonanone B, were difficult to obtain the starting materials, namely monomethyl- or dimethylphloroacteophenone. The improvement of synthetic method of homoisoflavonoid was studied.
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