Marine Biotechnology Division, Central Marine Fisheries Research Institute, Ernakulam North, P.B. No. 1603, Cochin 682018, Kerala, India.
Marine Biotechnology Division, Central Marine Fisheries Research Institute, Ernakulam North, P.B. No. 1603, Cochin 682018, Kerala, India.
Int J Biol Macromol. 2020 Nov 15;163:1223-1232. doi: 10.1016/j.ijbiomac.2020.07.037. Epub 2020 Jul 9.
Angiotensin converting enzyme (ACE) is a multifunctional enzyme involved in translation of angiotensin-I (Ang) to vasoconstrictor angiotensin-II (Ang). A sulfated N-acetylglucosamino-glucuronopyranosyl-arabinopyranan characterized as poly-[(2-methoxy-β-arabinopyranosyl)-(1 → 3)-(β-glucurono)-(1 → 4)-(2-acetamido-2-deoxy-3,6-di-O-sulfonato-β-glucopyranose)] was purified and reported first time from the edible portion of Amphioctopus neglectus and evaluated for various pharmacological properties. The polysaccharide exhibited potential ACE attenuation property (IC 0.11 mg mL), whereas molecular docking simulations displayed its efficient binding at the ACE active site with lesser inhibitory constant (K) of 17.36 nM and binding energy (-10.59 kcal mol). The in-vitro analysis showed that the studied polysacharide attenuated Ang prompted cardiac hypertrophy at 50 μg mL in the cardiomyoblast cells, whereas 48% reduction in cellular surface area with extended viability could be correlated with anti-hypertrophic properties of the studied polysaccharide. The sulfated N-acetylglucosamino-glucuronopyranosyl-arabinopyranan purified from A. neglectus could function as a prospective functional lead against the pathophysiological conditions leading to hypertension.
血管紧张素转换酶(ACE)是一种多功能酶,参与将血管紧张素-I(Ang)转化为血管收缩素-II(Ang)。一种被表征为聚[(2-甲氧基-β-阿拉伯吡喃基)-(1→3)-(β-葡糖醛酸)-(1→4)-(2-乙酰氨基-2-去氧-3,6-二-O-磺基-β-吡喃葡萄糖]的硫酸化 N-乙酰氨基葡萄糖基葡糖醛酸阿拉伯吡喃聚糖首次从食用部分的 Amphioctopus neglectus 中分离出来,并对其进行了各种药理学性质的评估。该多糖表现出潜在的 ACE 抑制特性(IC 0.11mg mL),而分子对接模拟显示其在 ACE 活性部位的结合效率较高,抑制常数(K)为 17.36nM,结合能(-10.59kcal mol)。体外分析表明,在所研究的多糖在 50μg mL 的心肌细胞中可减轻 Ang 诱导的心肌肥大,而细胞表面积减少 48%,同时保持较高的存活率,这与所研究多糖的抗肥大特性有关。从 A. neglectus 中分离出的硫酸化 N-乙酰氨基葡萄糖基葡糖醛酸阿拉伯吡喃聚糖可作为一种有前途的功能先导物,用于治疗导致高血压的病理生理状况。