Department of Clinical Laboratory Science, Semyung University, Jecheon 27136, Korea.
Division of Crop Foundation, National Institute of Crop Science (NICS), Rural Development Administration (RDA), Wanju 55365, Korea.
Molecules. 2021 May 1;26(9):2663. doi: 10.3390/molecules26092663.
() produces urease in order to improve its settlement and growth in the human gastric epithelium. Urease inhibitors likely represent potentially powerful therapeutics for treating ; however, their instability and toxicity have proven problematic in human clinical trials. In this study, we investigate the ability of a natural compound extracted from Smith, zerumbone, to inhibit the urease activity of by formation of urease dimers, trimers, or tetramers. As an oxygen atom possesses stronger electronegativity than the first carbon atom bonded to it, in the zerumbone structure, the neighboring second carbon atom shows a relatively negative charge (δ) and the next carbon atom shows a positive charge (δ), sequentially. Due to this electrical gradient, it is possible that urease with its negative charges (such as thiol radicals) might bind to the β-position carbon of zerumbone. Our results show that zerumbone dimerized, trimerized, or tetramerized with both urease A and urease B molecules, and that this formation of complex inhibited urease activity. Although zerumbone did not affect either gene transcription or the protein expression of urease A and urease B, our study demonstrated that zerumbone could effectively dimerize with both urease molecules and caused significant functional inhibition of urease activity. In short, our findings suggest that zerumbone may be an effective urease inhibitor that may be suitable for therapeutic use in humans.
()产生脲酶，以提高其在人类胃上皮中的定植和生长。脲酶抑制剂可能是治疗的潜在有效疗法；然而，它们在人体临床试验中的不稳定性和毒性已被证明是个问题。在这项研究中，我们研究了从 Smith 中提取的天然化合物——姜烯，通过形成脲酶二聚体、三聚体或四聚体来抑制 脲酶活性的能力。由于氧原子的电负性比与之键合的第一个碳原子强，在姜烯结构中，相邻的第二个碳原子表现出相对负电荷 (δ)，下一个碳原子表现出正电荷 (δ)，依次排列。由于这种电梯度， 脲酶上的负电荷（如硫自由基）可能与姜烯的β-位碳原子结合。我们的结果表明，姜烯与 脲酶 A 和脲酶 B 分子二聚化、三聚化或四聚化，这种复合物的形成抑制了 脲酶活性。尽管姜烯既不影响脲酶 A 和脲酶 B 的基因转录，也不影响其蛋白表达，但我们的研究表明，姜烯可以有效地与两种脲酶分子二聚化，并导致脲酶活性的显著功能抑制。简而言之，我们的研究结果表明，姜烯可能是一种有效的 脲酶抑制剂，可能适合在人类中进行治疗应用。
