Strong inhibitory effects of curcumin and its demethoxy analog on Escherichia coli ATP synthase F1 sector.
Strong inhibitory effects of curcumin and its demethoxy analog on Escherichia coli ATP synthase F1 sector.
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DOI：
10.1016/j.ijbiomac.2014.06.055
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发表时间：
2014-09
影响因子：
8.2
通讯作者：
Mizuki Sekiya;Eiko Chiba;Momoe Satoh;Hiroyuki Yamakoshi;Y. Iwabuchi;M. Futai;M. Nakanishi‐Matsui
中科院分区：
文献类型：
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作者：
Mizuki Sekiya;Eiko Chiba;Momoe Satoh;Hiroyuki Yamakoshi;Y. Iwabuchi;M. Futai;M. Nakanishi‐Matsui
姜黄素是一种从多年生草本植物（姜黄）中分离出来的膳食植物多酚，是一种众所周知的有效治疗细菌感染和肿瘤的化合物，也是一种抗氧化剂。在这项研究中，我们报告了姜黄素及其类似物对大肠杆菌ATP合成酶F1区的抑制作用。构效关系研究表明，4′-羟基和β-二酮基团对抑制作用具有重要作用。3′-去甲氧基类似物（DMC）对F1的抑制作用强于姜黄素。此外，这些化合物抑制E.通过氧化磷酸化共生长，与它们对ATP酶活性的影响一致。这些结果表明，这两种化合物通过抑制ATP合酶来影响细菌生长。包括双（芳基亚甲基）丙酮（C5姜黄素类化合物）的衍生物对ATP酶和细菌生长仅表现出较弱的活性。
Curcumin, a dietary phytopolyphenol isolated from a perennial herb (Curcumalonga), is a well-known compound effective for bacterial infections and tumors, and also as an antioxidant. In this study, we report the inhibitory effects of curcumin and its analogs on theEscherichia coliATP synthase F1sector. A structure–activity relationship study indicated the importance of 4′-hydroxy groups and a β-diketone moiety for the inhibition. The 3′-demethoxy analog (DMC) inhibited F1more strongly than curcumin did. Furthermore, these compounds inhibitedE. coligrowth through oxidative phosphorylation, consistent with their effects on ATPase activity. These results suggest that the two compounds affected bacterial growth through inhibition of ATP synthase. Derivatives including bis(arylmethylidene)acetones (C5curcuminoids) exhibited only weak activity toward ATPase and bacterial growth.