Palacios Javier, Villarroel Carlos, Asunción-Alvarez Daniel, Cifuentes Fredi, Paredes Adrián, Nwokocha Chukwuemeka R, Castro-Álvarez Alejandro, Parra Claudio
Laboratorio de Bioquímica Aplicada, Facultad de Ciencias de la Salud, Universidad Arturo Prat, Iquique 1110939, Chile.
Laboratorio de Fisiología Experimental, Instituto Antofagasta, Universidad de Antofagasta, Antofagasta 1271155, Chile.
Int J Mol Sci. 2025 Apr 17;26(8):3786. doi: 10.3390/ijms26083786.
Angiotensin-Converting Enzyme (ACE) plays a pivotal role in the renin-angiotensin system, modulating blood pressure and electrolyte homeostasis by deactivating bradykinin and activating angiotensin II. Metabolites from ( and ), a plant indigenous to the Andean region of the Atacama Desert, and their respective oximes, and , were subjected to molecular docking analysis, employing six ACE crystal structures. ACE activity assays revealed that oximes exhibited superior inhibitory effects compared to metabolites. Among the compounds investigated, emerged as the most potent ACE inhibitor ( = 11.5 μM and = 13.4 μM). The vascular contractile response to Angiotensin I showed significant ( < 0.05) reductions in Ang I contraction with , , and (97 ± 6%, 81 ± 6%, 81 ± 3% compared to control), while exhibited no such effect. These results reinforce the potential of as a promising ACE inhibitor and highlight its impact on vascular contractility. As such, it is a promising candidate for ACE inhibition and hypertension treatment.
血管紧张素转换酶（ACE）在肾素-血管紧张素系统中起关键作用，通过使缓激肽失活和激活血管紧张素II来调节血压和电解质平衡。对来自阿塔卡马沙漠安第斯地区的一种本土植物（ 和 ）的代谢产物及其各自的肟（ 和 ），采用六种ACE晶体结构进行了分子对接分析。ACE活性测定表明，肟类化合物比代谢产物表现出更强的抑制作用。在所研究的化合物中， 是最有效的ACE抑制剂（ = 11.5 μM， = 13.4 μM）。对血管紧张素I的血管收缩反应显示， 、 和 可使血管紧张素I收缩显著降低（ < 0.05）（与对照组相比分别为97 ± 6%、81 ± 6%、81 ± 3%），而 则无此作用。这些结果强化了 作为一种有前景的ACE抑制剂的潜力，并突出了其对血管收缩性的影响。因此，它是ACE抑制和高血压治疗的一个有前景的候选药物。
