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センダン樹リモノイド成分の機能性評価と高度利用に関する研究

苦楝树柠檬苦素类成分的功能评价及深度利用研究

基本信息

批准号：
23590017
负责人：
秋久俊博
金额：
$ 3.41万
依托单位：
Nihon University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2011
资助国家：
日本
起止时间：
2011 至 2012
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-23590017/
关键词：
センダンリモノイド抗腫瘍活性発がん予防効果抗炎症活性

项目摘要

センダン果実抽出物から36種のリモノイド化合物を単離し,それらのうち22種は新規構造化合物であり,種々のスペクトル法を駆使して構造解析を行った.発がん予防剤及び抗腫瘍剤リード化合物の開発の観点から,これらの化合物についてHL60(白血病),A549(肺がん),AZ521(胃がん)及びSK-BR-3(乳がん)細胞株を用いてMTT法により細胞傷害活性の評価を行い,12-O-Acetylazedarachin B, 12-O-Acetylazedarachin D, 3-O-Deacetyl-4'-demethyl-28-oxosalannin及び4'-Demethylohchinolalの4種が上記何れかの細胞で強い細胞傷害活性を示すことを見出した.これらの内12-O-AcetylazedarachinB及び 3-O-Deacetyl-4'-demethyl-28-oxosalanninはHL60細胞に対してアポトーシス誘導により細胞傷害活性を示すことを明らかにし,アポトーシス誘導機構の解析も行った.発がん予防剤開発の一次スクリーニング試験であるEpstein-Barr virus早期抗原(EBV-EA)発現抑制試験では,幾つかの化台物にβ-Carotene程度の中程度の抑制活性を認めている.また,上記リモノイド類についてLPS刺激によるRAW264.7細胞を用いたNO産生抑制活性を評価し, 1 O-Decinnamoyl-1-O-cis-cinnamoyl ohchinin ,3-Deacetyl-3-tigloylsalannin及び 4'-Demethylohchinolalの3種に細胞毒性を示すことなく顕著な抑制活性を示すこと見出し,これらが消炎剤開発の有望なリード化台物となり得ることを明らかにした.

The results showed that there were 36 kinds of compounds isolated from the extract, and 22 kinds of compounds with new structure were isolated from the extract, and the structure analysis was carried out by using the method of extraction. The development of anti-inflammatory and anti-inflammatory compounds was investigated by MTT assay for the evaluation of cytotoxic activity of HL60(leukemia),A549(lung cancer),AZ521(stomach cancer) and SK-BR-3(breast cancer) cell lines, 12-O-Acetylazedarachin B, 12-O-Acetylazedarachin D, 4 species of 3-O-Deacetyl-4'-demethyl-28-oxosalannin and 4'-Demethylohchinolal have been shown to exhibit potent cytotoxic activity. The 12-O-Acetylazedarachin B and 3-O-Deacetyl-4'-demethyl-28-oxosalannin in HL60 cells were shown to induce cellular injury. The first step in the development of anti-virus inhibitors was to detect the presence of Epstein-Barr virus early antigen (EBV-EA), and to identify the intermediate level of β-Carotene inhibitory activity of anti-virus inhibitors. In addition, the inhibitory activity of NO production in RAW264.7 cells stimulated by LPS was evaluated. Three kinds of cytotoxicity, 1 O-Decinnamoyl-1-O-cis-cinnamoyl ohchinin, 3-Deacetyl-3-tigloylsalannin and 4'-Demethylohchinolal, were shown.