School of Life Science, Beijing University of Chinese Medicine, No. 11, Bei San Huan Dong Lu, Chaoyang District, Beijing, China.
School of Chinese Materia Medica, Beijing University of Chinese Medicine, No. 11, Bei San Huan Dong Lu, Chaoyang District, Beijing, China.
J Biochem. 2019 Sep 1;166(3):223-230. doi: 10.1093/jb/mvz029.
Vinegar soaked black soybean is a traditional Chinese food widely used for the treatment of hypertension. While its pharmacodynamic substance was not fully unveiled. It contained abundant glutelin, thus the purpose of this study was to obtain potent antihypertensive peptides from vinegar soaked black soybean. Black soybean was soaked with vinegar and then glutelin was first catalyzed by alcalase. Ultrafiltration, ion exchange chromatography and reversed-phase high performance liquid chromatography were sequentially applied to separate and purify the angiotensin-I converting enzyme (ACE) inhibitory peptides from glutelin hydrolysates. As a result, the fraction L1-4 with the highest ACE inhibitory activity (83.41%) at the final concentration of 0.01 mg/ml was obtained and five peptides were then identified. These peptides were further optimized by virtual screening combining with in silico proteolysis. Finally, a novel tetrapeptide Phe-Gly-Ser-Phe (FGSF) was obtained. FGSF exhibited high in vitro ACE inhibitory activity (IC50 = 117.11 μM) and in vivo hypotensive effect which maximally reduced systolic blood pressure of 21.95 mmHg at 20 mg/kg body weight in spontaneously hypertensive rats. Our study demonstrated that FGSF derived from vinegar soaked black soybean might be used as a promising ingredient for pharmaceuticals against hypertension and its related diseases.
醋泡黑豆是一种传统的中国食品,广泛用于治疗高血压。虽然其药效物质尚未完全揭示,但它含有丰富的球蛋白,因此本研究旨在从醋泡黑豆中获得具有强力降压作用的肽。黑豆用醋浸泡,然后用碱性蛋白酶催化球蛋白。通过超滤、离子交换色谱和反相高效液相色谱依次分离和纯化球蛋白水解物中的血管紧张素转化酶(ACE)抑制肽。结果,在终浓度为 0.01mg/ml 时,获得了具有最高 ACE 抑制活性(83.41%)的 L1-4 级分,然后鉴定了 5 个肽。这些肽通过虚拟筛选与计算机蛋白水解相结合进行了进一步优化。最终得到了一个新的四肽 FGSF(苯丙氨酸-甘氨酸-丝氨酸-苯丙氨酸)。FGSF 表现出很高的体外 ACE 抑制活性(IC50=117.11μM)和体内降压作用,在自发性高血压大鼠中,20mg/kg 体重时最大降低收缩压 21.95mmHg。本研究表明,醋泡黑豆衍生的 FGSF 可能可作为治疗高血压及其相关疾病的药物的有前途的成分。