天名精内酯醇衍生物的合成及其抑菌活性

Synthesis and Fungistatic Activity of Carpesialactone Derivant

为了探明天名精内酯醇衍生物的结构变化对植物抑菌效果的影响,分别对其4位羟基、α-亚甲基-γ-内酯环和11,13位双键进行结构修饰,得到了一系列衍生物,并采用悬滴法测定衍生物对黄瓜炭疽病菌孢子的萌发抑制作用。结果表明:衍生物对黄瓜炭疽病均表现有一定的抑菌活性,其中羟基醚化的衍生物Vd和Ve抑菌活性最强,在5 mg/kg时已分别达91.94%和100%,至80 mg/kg时均达到100%,另外4位羟基酯化得到的衍生物抑菌活性较天名精内酯醇也有所提高,但通过羟基脱水和改变α-亚甲基-γ-内酯环结构得到的衍生物较天名精内酯醇活性均降低。初步说明,在保持α-亚甲基-γ-内酯结构不变的情况下,将4位羟基乙醚化得到的衍生物Ve能够显著提高天名精内酯醇的抑菌活性。

A series of derivants from modifying the structure of carpesialactone extracted from Carpesium macrocepha were tested to determine the inhibition effect on spore germination of Colletotrichum lagenarium.The results showed that the series of derivants all had a certain fungistatic activity to Colletotrichum lagenarium,the highest fungistatic activity of Vd and Ve（the derivants）with hydroxyl etherification was 91.94% and 100% respectively when the concentration was 5mg/kg and both was 100% when the concentration was 80mg/kg,the fungistatic activity of four derivants with hydroxyl esterification was higher than carpesialactone but the fungistatic activity of the derivants from hydroxyl dehydration and structural modification of α-methylene-γ-lactone was lower than carpesialactone,which indicates that Ve from hydroxyl etherification can significantly improve the gungistatic activity of carpesialactone when the structure of α-methylene-γ-lactone is not changed.