Search for Novel Anti-tumor Constituents from Plant Sources and Their Drug Development

从植物中寻找新型抗肿瘤成分及其药物开发

• 批准号: 09672173
• 负责人: FUKUKAWA Hiroshi
• 金额: $ 1.86万
• 依托单位: Meijo University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1997
• 资助国家: 日本
• 起止时间: 1997 至 1999
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-09672173/
• 关键词: Rutaceae; Leguminosae; Guttiferae; Avicenniaceae; coumarins; alkaloids; xanthones; biological activity; フラボノイド; Citrus; Clausena; Glycosmis; Garcinia; カルバゾール; アクリドン; キナゾロン; Calophyllum

In the search of novel anti-tumor constituents from plant sources, many kinds of novel acridone-, carbazole-, quinolone-, and quinazoline-alkaloids, and xanthones, coumarins, fulalvonoids, and phenylpropanoids were isolated and their structures were established by spectrometric and synthetic methods. Further, several types of biological activities were also tested for the compounds isolated in this project.1. Families and genus of plant sources used in this project :(1) Plants of Rutaceae : plants of genus Murraya, Clausena, Glycosmiss, Boronia, Micromelum(2) Plants of Leguminosae : plants of genus Dalbergia, Milletia, Derris(3) Plant of Guttiferae : plants of genus Calophyllum, Garcinia(4) Plant of Avicenniaceae : plants of genus Avicennia2. Assays of Biological Activities(1) Assay of Anti-tumor Promoting Effects : 7-methoxycoumarins, xanthones, Phenylpropanoids(2) Assay of the Activity of Induction of HL-60 Cell Differentiation : acridone alkaloids(3) Assay of Anti-proliferative Effects on Several Cancer Cell Lines : acridone alkaloids(4) Assay of Inhibitory Effects of Nitric Oxide Generation : coumarins

在从植物中寻找新的抗肿瘤活性成分的过程中，从植物中分离得到了许多新的吖啶酮类、咔唑类、喹诺酮类和喹唑啉类生物碱，以及口山酮、香豆素、富拉冯和苯丙烷类化合物，并通过波谱和合成方法确定了它们的结构。此外，本项目中分离的化合物还测试了几种类型的生物活性。本项目所用植物资源的科和属：(1)十字花科植物：九里香属、黄皮属、糖蜜属、博罗尼亚属、小蜜瓜属；(2)豆科植物：黄檀属、千金藤属、Derris属；(3)Guttiferae植物：Calophyllum、Garcinia属植物；(4)Avicenniaceae植物：Avicennia2属植物。生物活性测定(1)抗肿瘤活性测定：7-甲氧基香豆素、黄原酮、苯丙烷类化合物(2)诱导HL-60细胞分化活性测定：吖啶酮生物碱(3)对几种癌细胞株的抗增殖作用(4)抑制一氧化氮生成作用的测定：香豆素

项目成果

Akira Murakami: "Identification of Coumarins from the Fruit of Citrus Hystrix DC. as Inhibitors of Nitric Oxide Generation in Mouse Macrophage RAW264.7 Cills"J. Agr. & Food Chem.. 47. 333-339 (1999)

Akira Murakami：“鉴定柑橘 Hystrix DC 果实中的香豆素作为小鼠巨噬细胞 RAW264.7 Cills 中一氧化氮生成的抑制剂”J。

Satoru Kawaii: "The Antiproliferative Effect of Acridone Alkaloids on Several Cancer Cell Lines"J. Nat. Prod.. 62. 587-589 (1999)

Satoru Kawaii：“吖啶酮生物碱对几种癌细胞系的抗增殖作用”J。

Chihiro Ito: "Anti-tumor-promoting effects of 8-substituted 7-methoxyxoumarins on Epstein-Barr virus activation assay"Cancer Letts. 138. 87-92 (1999)

Chihiro Ito：“8-取代的 7-甲氧基香豆素对 Epstein-Barr 病毒激活测定的抗肿瘤促进作用”Cancer Letts。

Akira Murakami: "1,1-Dimethylallylcoumarins Potently Supress both Lipopoly- saccharide- and Interferon- -induced Nitric Oxide Generation in Mouse Macrophage RAW 264.7 Cells."Booing. & Med. Chem. Lets.. 10. 59-62 (2000)

Akira Murakami：“1,1-二甲基烯丙基香豆素可有效抑制脂多糖和干扰素诱导的小鼠巨噬细胞 RAW 264.7 细胞中一氧化氮的产生。”嘘声。

Chihiro Ito: "Chemical Constituents of Glycosmis pentaphylla.Isolation of A Novel Naphthoquinone and A New Acridone Alkaloid."Chem.Pharm.Bull.. 47. 1579-1581 (1999)

Chihiro Ito：“Glycosmis pentaphylla 的化学成分。新型萘醌和新吖啶酮生物碱的分离。”Chem.Pharm.Bull.. 47. 1579-1581 (1999)