Investigation of Medicinal Lead Compounds from Natural Resource

自然资源药用先导化合物的研究

• 批准号: 06672084
• 负责人: OHTA Tomihisa
• 金额: $ 1.34万
• 依托单位: TOHOKU UNIVERSITY
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for General Scientific Research (C)
• 财政年份: 1994
• 资助国家: 日本
• 起止时间: 1994 至 1995
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-06672084/
• 关键词: Anti tumor; Brazilian plant; Mushroom; Enzyme inhibition; Monoamine oxidase; Phosphodiesterase; Amino Acid; Alkaloid; 細胞毒性; 中枢毒性; グルタミンデカルボキシラーゼ; 天然資源; 生物活性; NMR; 植物; 微生物; 天然物

Under the research project on the investigation of a medicinal lead compound from natural resource, we have isolated and elucidated the structures of several natural substances from medicinal plants and mushrooms. Three new isoprenoids, faveloxide, favelol and isofavelol were isolated from Brazilian plant Cnidoscolus phyllacanthus. Since those compounds are congeners of faveline that has anti tumor activity, the mode of action should be studied. As a cytotoxic component of mushroom Russula subnigricans, russuphelol was isolated and the chemical structure was determined. It may be of interest to isolate the biosynthetic enzyme of russuphelol having optical activity. Confluentic acid and 2'-O-methylperlatolic acid were isolated from the Brazilian plant Himatamthus sucuuba. Because of its potent and specific activity against monoamine oxidase-B and the increase of the activity of the synthetic analogs, confluentic acid may act as a lead compound in the development of a new type of medicine. Ibotenic acid was isolated from the mushroom Tricholoma muscarium. As a new chlorinated amino acid in the mushroom Amanita vergineoides, (S)-cis-2-amino-5-chloro-4-pentenoic acid was isolated and structure was elucidated. From the mushroom Laccaria vinaceoavellanea, a new alkaloid laccarin was isolated as a inhibitor of cAMP phosphodiesterase and the chemical structure was elucidated.

在天然药物先导化合物的研究项目下，我们从药用植物和蘑菇中分离并鉴定了几种天然物质的结构。从巴西植物叶棘蛇床蕨（Cnidocalusphylacanthus）中分离得到三个新的类异戊二烯化合物：faveloxide、favelol和isofavelol。由于这些化合物是具有抗肿瘤活性的faveline的同系物，因此应研究其作用方式。从亚黑红菇中分离得到一种具有细胞毒性的活性成分--红菇醇，并对其化学结构进行了测定。分离具有光学活性的罗素醇生物合成酶可能是有意义的。从巴西植物Himatamthus sucuuba中分离出汇流酸和2 '-O-甲基perlatolic酸。由于其对单胺氧化酶-B的有效和特异性活性以及合成类似物的活性增加，汇流酸可能在开发新型药物中充当先导化合物。鹅膏蕈氨酸是从蕈类口蘑（Tricholoma muscarium）中分离得到的。（S）-cis-2-amino-5-chloro-4-pentenoic acid是一种新的含氯氨基酸，从蘑菇Amanita vergesterides中分离得到，并鉴定了其结构。从蘑菇Laccariavinaceoavellanea中分离得到一种新的生物碱--漆苷，并鉴定了其化学结构。

项目成果

Masao Maruyama: "Ineupatorolides from Carpesium glossophyllm" Planta Med.61. 388-389 (1995)

Masao Maruyama：“来自 Carpesium glsophophyllm 的 Ineupatorolides” Planta Med.61。

M.Maruyama, K.Watanabe, T.Kawakami, M.Maeda, M.Kato, S.Nozoe, and T.Ohta: "Ineupatorolides from Carpesium glossophyllum" Planta Med. 61. 388-389 (1995)

M.Maruyama、K.Watanabe、T.Kawakami、M.Maeda、M.Kato、S.Nozoe 和 T.Ohta：“来自 Carpesium glhophyllum 的 Ineupatorolides” Planta Med。

Mamoru Matsuda: "Laccarin, a New Alkaloid from the Mushroom Laccaria vinaceoavelanea" Heterocycles. 43(in press). (1996)

Mamoru Matsuda：“Laccarin，一种来自蘑菇 Laccaria vinaceoavelanea 的新生物碱”杂环化合物。

T.Ohta, Y.Endo, R.Kikuchi, and S.Nozoe: "Faveloxide, a New Isoprenoid Derivative from the Brazilian Plant, Cnidoscolus phyllacanthus" Heterocycles. 38. 55-56 (1994)

T.Ohta、Y.Endo、R.Kikuchi 和 S.Nozoe：“Faveloxy，一种来自巴西植物 Cnidoscolus phyllacanthus 的新类异戊二烯衍生物”杂环化合物。

T.Ohta, M.Matsuda, S.Kamo, A.Takahashi, T.Agatsuma, T.Endo, and S.Nozoe: "Russufelol, a Novel Optically Active Chlorohydroquinone Tetramer from the Mushroom Russula subnigricans" Tetrahedron Lett. 36. 5223-5226 (1995)

T.Ohta、M.Matsuda、S.Kamo、A.Takahashi、T.Agatsuma、T.Endo 和 S.Nozoe：“Russufelol，一种来自蘑菇 Russula subnigricans 的新型光学活性氯氢醌四聚体”Tetrahedron Lett。