7−羟基香豆素的抑菌活性及其稳定性研究

以5种植物病原菌为研究对象,用生长速率法测定7−羟基香豆素对各病菌的抑菌活性;以尖孢镰刀菌为指示菌,测定了7−羟基香豆素抑菌活性在不同条件下的稳定性。结果表明:7−羟基香豆素对5种病原菌均显示出不同程度的抑制作用,尤其是对尖孢镰刀菌作用最为显著,当浓度为1.6 mg/mL时,对尖孢镰刀菌的抑制率可达93.66%。7−羟基香豆素在经过光照、氧化剂和还原剂的处理后,抑菌活性稳定;在酸性条件下,抑菌效果显著增强,而在碱性条件下,抑菌活性下降;在经过Ca^(2+)处理后,7−羟基香豆素的抑菌活性稳定;经过Co^(2+)、Ni^(2+)处理后,抑制效果达到100%,经过Mn^(2+)处理后,抑菌效果显著加强;经过K^(+)处理后,抑菌活性受到抑制。

Synthesis of 3-(4-hydroxyphenyl)-4-methyl-6-methoxy-7-hydroxycoumarin and its analogues as angiogenesis inhibitors

3-（4-Hydroxyphenyl）-4-methyl-6-methoxy-7-hydroxycoumarin （2a） and its analogues with different substituents at the p-position of 3-phenyl group were designed and synthesized as the non-steroidal analogues of 2-methoxyestradiol （2-ME 1）. The desired compounds were synthesized via a novel and simple route and the effects of specific substituents on their antiangiogenesis activities were investigated with Human umbilical vein endothelial cells （HUVECs） proliferation assays. Preliminary biological screening showed that compounds 2a and 2d （IC50 = 61.0 and 76.7 ktM, respectively） have potential anti-angiogenesis activities. The bulk of the group at the p-position of 3-phenyl group likely play an important role in their activities.