Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560 012, India.
Org Biomol Chem. 2011 Mar 7;9(5):1356-65. doi: 10.1039/c0ob00823k. Epub 2010 Dec 24.
Angiotensin converting enzyme (ACE) catalyzes the conversion of angiotensin I (Ang I) to angiotensin II (Ang II). ACE also cleaves the terminal dipeptide of vasodilating hormone bradykinin (a nonapeptide) to inactivate this hormone. Therefore, inhibition of ACE is generally used as one of the methods for the treatment of hypertension. 'Oxidative stress' is another disease state caused by an imbalance in the production of oxidants and antioxidants. A number of studies suggest that hypertension and oxidative stress are interdependent. Therefore, ACE inhibitors having antioxidant property are considered beneficial for the treatment of hypertension. As selenium compounds are known to exhibit better antioxidant behavior than their sulfur analogues, we have synthesized a number of selenium analogues of captopril, an ACE inhibitor used as an antihypertensive drug. The selenium analogues of captopril not only inhibit ACE activity but also effectively scavenge peroxynitrite, a strong oxidant found in vivo.
血管紧张素转化酶（ACE）可催化血管紧张素 I（Ang I）转化为血管紧张素 II（Ang II）。ACE 还能裂解扩血管激素缓激肽（九肽）的末端二肽，使该激素失活。因此，抑制 ACE 通常被用作治疗高血压的方法之一。“氧化应激”是由氧化剂和抗氧化剂产生失衡引起的另一种疾病状态。许多研究表明，高血压和氧化应激是相互依存的。因此，具有抗氧化特性的 ACE 抑制剂被认为对治疗高血压有益。由于硒化合物的抗氧化行为优于其硫类似物，我们已经合成了一些 ACE 抑制剂卡托普利的硒类似物，卡托普利被用作抗高血压药物。卡托普利的硒类似物不仅抑制 ACE 活性，而且还能有效地清除过氧亚硝酸盐，过氧亚硝酸盐是体内发现的一种强氧化剂。
