Antitermite Activities of Coumarin Derivatives and Scopoletin from Protium javanicum Burm. f.
Antitermite Activities of Coumarin Derivatives and Scopoletin from Protium javanicum Burm. f.
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DOI：
10.1007/s10886-010-9807-1
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发表时间：
2010-07-01
影响因子：
2.3
通讯作者：
Koketsu, Mamoru
中科院分区：
文献类型：
--
作者：
Adfa, Morina;Yoshimura, Tsuyoshi;Koketsu, Mamoru
爪哇青霉的抗白蚁(杀白蚁和拒食)活性。对金针菇提取物进行了考察。乙酸乙酯部分具有较高的活性。通过生物测定引导的分离方法，分离得到了东五味子内酯(1)、槲皮素和豆甾醇。在三种化合物中，东五味子内酯的活性最高。为了研究香豆素骨架C-6和C-7位上的甲氧基和羟基的构效关系(SAR)，我们合成了几个化学结构相似的香豆素衍生物。在所测试的10个化合物中，海参内酯的杀白蚁活性最强，其次是6-甲氧基香豆素(3)、6-羟基香豆素(7)和伞形酮(8)。除香豆素(9)外，其余化合物均有拒食活性。
The antitermite (termiticidal and antifeedant) activity of Protium javanicum Burm. f. extract was investigated. The ethyl acetate fraction was active. Scopoletin (1), quercetin, and stigmasterol were isolated by bioassay-guided fractionation. Scopoletin had the highest activity among the three compounds. In order to investigate the structure-activity relationship (SAR) of the methoxy and hydroxy groups at the C-6 and C-7 positions of the coumarin skeleton, we synthesized several coumarin derivatives whose chemical structures are similar to scopoletin. Scopoletin exhibited the strongest termiticidal activity among the 10 compounds tested, followed by 6-methoxycoumarin (3), 6-hydroxycoumarin (7), and umbelliferone (8). All compounds except coumarin (9) showed antifeedant activity.