为发现具有新结构和显著药理作用的化合物,以异色瓢虫内生真菌木贼镰刀菌Fusarium equiseti为研究对象,采用现代分离手段,从其次级代谢产物中分离鉴定出3种化合物1、2和3. 其中化合物1(equisetin)和2(epi-equisetin)是一对差向异构体,3(6-methoxy-droperylene)属于甾体类. 体外蛋白质酪氨酸磷酸酶1B(PTP1B)抑制活性测试结果表明,化合物1和2对PTP1B具有一定的抑制活性,IC50值分别为(8.73 ± 0.03)、(12.88 ± 0.16)μg/mL. 为新型PTP1B抑制剂的研发提供了潜在的药物先导化合物.
In order to find compounds with new structures and significant pharmacological effects, three compounds 1, 2 and 3 were isolated and identified from the secondary metabolites of the endophytic fungus Fusarium equiseti from Harmonia axyridis by modern isolation methods. Among them, compounds 1(equisetin)and 2(epi-equisetin)are a pair of epiisomers, and 3(6-methoxy-droperylene)belongs to steroids. In vitro protein tyrosine phosphatase 1B(PTP1B)inhibitory activity test showed that compounds 1 and 2 had certain inhibitory activity on PTP1B, and IC50 values were(8.73 ± 0.03),(12.88 ± 0.16)μg/mL. It provides potential drug lead compounds for the development of new PTP1B inhibitors.
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