Department of Chemistry, Faculty of Engineering and Natural Sciences, Istanbul Medeniyet University, Istanbul, Turkey.
Drug Chem Toxicol. 2021 Jul;44(4):359-364. doi: 10.1080/01480545.2019.1600532. Epub 2019 Apr 22.
Lactoperoxidase (LPO, E.C.1.11.1.7) is a natural antibacterial agent which is secreted from salivary, mammary, and other mucosal glands. It is one of the crucial enzymes in biological systems, so protection of LPO activity is extremely important for the immune system. Within the scope of this study; effects of some thiophene-2-sulfonamide derivatives () on bovine milk LPO enzymatic activity were investigated. LPO was purified from the Sepharose-4B-L-tyrosine-5-amino-2-methylbenzenesulfonamide column prepared using affinity chromatography technique with a yield of 169.66 EU/mg specific activity in 452.44 times. As a result, 5-(2-thienylthio) thiophene-2-sulfonamide demonstrated the strongest inhibition impact among these compounds. This molecule has shown a competitive inhibition and it was determined that the IC value was 3.4 nM and the Ki value was 2 ± 0.6 nM.
乳过氧化物酶（LPO，E.C.1.11.1.7）是一种天然的抗菌剂，由唾液腺、乳腺和其他黏膜腺分泌。它是生物系统中至关重要的酶之一，因此保护 LPO 活性对免疫系统极为重要。在本研究范围内；研究了一些噻吩-2-磺酰胺衍生物（）对牛乳 LPO 酶活性的影响。LPO 是通过亲和层析技术从 Sepharose-4B-L-酪氨酸-5-氨基-2-甲基苯磺酰胺柱中纯化得到的，产率为 169.66 EU/mg，比活度为 452.44 倍。结果表明，在这些化合物中，5-(2-噻吩基硫代)噻吩-2-磺酰胺的抑制作用最强。该分子表现出竞争性抑制作用，IC 值为 3.4 nM，Ki 值为 2±0.6 nM。
