源自咖啡酸苯乙酯的芳基螺硼酸酯盐的合成及生物活性

Hébert Martin J G, Flewelling Andrew J, Clark Trevor N, Levesque Natalie A, Jean-François Jacques, Surette Marc E, Gray Christopher A, Vogels Christopher M, Touaibia Mohamed, Westcott Stephen A

Department of Chemistry and Biochemistry, Université de Moncton, Moncton, NB, Canada E1A 3E9.

Department of Biology, University of New Brunswick, Saint John, NB, Canada E2L 4L5.

Int J Med Chem. 2015;2015:418362. doi: 10.1155/2015/418362. Epub 2015 Mar 5.

Two novel boron compounds containing caffeic acid phenethyl ester (CAPE) derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes. These results clearly show the effectiveness of the synthesized salts as transporter of CAPE.

已经制备并全面表征了两种含有咖啡酸苯乙酯（CAPE）衍生物的新型硼化合物。对这些新化合物和CAPE的潜在抗氧化和抗菌特性、抑制5-脂氧合酶的能力以及硼螯合是否能改善其生物活性进行了研究。在生物学测定中，钠盐4通常比铵盐5更具活性，并且超过了CAPE的自由基清除能力。化合物4和5在人多形核白细胞中比CAPE和齐留通更具活性。这些结果清楚地表明了合成盐作为CAPE转运体的有效性。