Department of Food Science & Technology, University of Karachi, 75270, Pakistan.
Department of Food Science & Technology, University of Karachi, 75270, Pakistan.
Int J Biol Macromol. 2024 Sep;276(Pt 1):133735. doi: 10.1016/j.ijbiomac.2024.133735. Epub 2024 Jul 8.
Urinary tract infection caused by Klebsiella, Proteus and Streptococcus is a urease dependent process, hence treatment of these infections by antibacterial compounds lies in inhibition of their virulence factors. The crude methanolic extracts derived from sumac fruit, pomegranate peel and Indian almond leaves were separated into anthocyanin and non-anthocyanin fractions using solid phase cartridges. The inhibitory effect of these fractions was determined on the growth of urease producing species and jack bean urease activity. Known compounds in the fractions were also docked with ureases of different biological origins viz. K. pneumoniae (PDB ID: 8HCN), K. aerogenes (PDB ID: 2KAU), Helicobacter pylori (PDB ID:8HC1)and Canavalia ensiformis (jack bean) (PDB ID: 3LA4) to determine their binding affinities and interaction with the enzyme. All the fractions showed significant inhibition growth for P. mirabilis, S. epidermidis and K.pneumoniae. Among the samples, sumac showed greatest inhibition against all (MIC 6-25 mg.mL) while among the fractions, anthocyanin was found to be most active (MIC 6-12 mg/mL). Likewise, all fractions inhibited urease with lowest ICs shown by sumac fractions (21-116 μg.mL). Out of 39 compounds docked, 27 showed interaction with movable flaps and/or active site of ureases which explains their mode of inhibition.
由克雷伯氏菌、变形杆菌和链球菌引起的尿路感染是一个依赖于脲酶的过程,因此,通过抗菌化合物治疗这些感染在于抑制其毒力因子。从漆树果实、石榴皮和印度苦杏仁叶中提取的粗甲醇提取物使用固相柱分离为花青素和非花青素部分。这些部分对产脲酶物种的生长和豇豆脲酶活性的抑制作用进行了测定。部分中的已知化合物也与不同生物来源的脲酶(即肺炎克雷伯菌(PDB ID:8HCN)、产气克雷伯菌(PDB ID:2KAU)、幽门螺杆菌(PDB ID:8HC1)和刀豆(豇豆)(PDB ID:3LA4)进行了对接,以确定它们的结合亲和力和与酶的相互作用。所有部分均显示对奇异变形杆菌、表皮葡萄球菌和肺炎克雷伯菌的生长有显著抑制作用。在这些样品中,漆树显示出对所有(MIC 6-25mg.mL)的最大抑制作用,而在这些部分中,花青素被发现最活跃(MIC 6-12mg/mL)。同样,所有部分均抑制脲酶,其中漆树部分的 IC50 最低(21-116μg.mL)。对接的 39 种化合物中有 27 种与可移动瓣和/或脲酶的活性部位相互作用,这解释了它们的抑制模式。