SCREENING OF POLYACETYLENIC ALCOHOLS IN CRUDE DRUGS USING THE ELISA FOR PANAXYTRIOL

SCREENING OF POLYACETYLENIC ALCOHOLS IN CRUDE DRUGS USING THE ELISA FOR PANAXYTRIOL
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DOI:
10.1248/bpb.18.933
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发表时间:
1995-07-01
影响因子:
2
通讯作者:
MORI, M
MORI, M
中科院分区:
医学4区
文献类型:
--
作者:
SAITA, T;KATANO, M;MORI, M

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从人参C, A. MEYER的根中分离得到的聚乙基醇如panaxytriol, panaxynol和panaxydol对多种培养的肿瘤细胞具有抗增殖活性。用人参三醇-牛血清白蛋白偶联物免疫家兔获得抗人参三醇抗体。虽然抗体的反应性主要针对panaxytriol,但与其他聚乙基化合物也有轻微的交叉反应,因此,该抗体可用于筛选大量的聚乙基化合物,如panaxytriol,并对31种药材的甲醇提取物进行了检测。已有文献报道的五加科、菊科和伞形科的15种甲醇提取物均有显著的反应性。从15种生药中选取3种进行强交叉反应性化合物的测定。用硅胶柱层析法分离得到4种交叉反应性化合物,酶联免疫吸附法(ELISA)对各组分进行检测,其中从菝葜中分离到panaxynol和heptadeca-1,8-二烯-4,6-二烯-3,10-二醇,从Peucedani芫花中分离到Falcarindiol。此外,还从茴香果中分离到一个新的聚乙炔醇,9,10-环氧-16-羟基-十八烷基-17-烯-12,14-二炔-1-al。所有这些聚乙炔醇都以剂量依赖的方式抑制人胃腺癌细胞系MK-1细胞的生长。这些结果表明,panaxytriol抗体是“筛选”抗增生性聚乙炔化合物的有效工具。
Polyacetylenic alcohols such as panaxytriol, panaxynol and panaxydol isolated from the roots of Panax ginseng C, A. MEYER have antiproliferative activity against various cultured tumor cells. Anti-panaxytriol antibody was obtained by immunizing rabbits,vith panaxytriol-bovine serum albumin conjugates. Although the antibody reactivity was directed mainly toward panaxytriol, there was a slight cross-reactivity with other polyacetylenic compounds, The antibody was, therefore, used for screening a large number of crude drugs for polyacetylenic compounds such as panaxytriol, Methanol-extracts from 31 crude drugs were examined. Significant reactivity was observed in 15 methanol-extracts from Aralieaceae, Compositae and Umbelliferae as reported by other investigators. Three out of the 15 crude drugs were selected for determination of the potent cross-reactive compounds. Four kinds of cross-reactive compounds mere isolated by silica gel column chromatography, monitoring each fraction using the enzyme-linked immunosorbent assay (ELISA), Among them, panaxynol and heptadeca-1,8-diene-4,6-diyne-3,10-diol were identified from Saposhnikoviae Radix, Falcarindiol was newly identified from Peucedani Radix. A new polyacetylenic alcohol, 9,10-epoxy-16-hydroxy-octadeca-17-ene-12,14-diyne-1-al, was also isolated from Foeniculi Fructus. All these polyacetylenic alcohols inhibited the growth of a human gastric adenocarcinoma cell line, MK-1 cells, in a dose-dependent manner. These results indicate that the antibody against panaxytriol is an effective tool for ''screening'' antiproliferative polyacetylenic compounds.