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作 者:梁劲杰 赵艺 褚辉程 郭嵩然 陈海英 张文静 陈祖君 王灵芝 LIANG Jin-jie;ZHAO Yi;CHU Hui-cheng;GUO Song-ran;CHEN Hai-ying;ZHANG Wen-jing;CHEN Zu-jun;WANG Ling-zhi(School of Life Sciences,Beijing University of Chinese Medicine,Beijing 102488;Department of Surgical Intensive Care Unit,Fuwai Hospital,Chinese Academy of Medical Sciences,Beijing 100030)
机构地区:[1]北京中医药大学生命科学学院,北京102488 [2]中国医学科学院阜外医院成人外科恢复室,北京100030
出 处:《中南药学》2024年第9期2307-2313,共7页Central South Pharmacy
基 金:北京中医药大学纵向发展基金(No.2023-ZXFZJJ-064);国家自然科学基金(No.81872972);中国医学科学院阜外医院高水平医院临床科研业务费(No.2023-GSP-GG-30)。
摘 要:目的探究模拟胃肠消化对薏苡仁谷蛋白血管紧张素转换酶(ACE)抑制肽活性的影响,并对其水解工艺进行优化。方法模拟胃肠环境水解薏苡仁谷蛋白,超滤法(截留分子量3 kDa)进行组分分离,反相高效液相色谱法测定其ACE抑制率;高活性组分进行体内降压药效-1评价。进一步以水解度为指标,通过正交实验优化水解工艺。结果在终浓度0.04 mg·mL^(-1)时,肠道水解物≤3 kDa组分的ACE抑制活性最高(99.94±0.01)%;单次灌胃给药可显著降低自发性高血压大鼠的血压。胰蛋白酶水解薏苡仁谷蛋白的最佳参数为:水解时间6 h、底物浓度1.5%、酶底比1∶5,谷蛋白的水解度为(16.37±1.68)%。结论薏苡仁谷蛋白经胃肠模拟消化后可产生具有显著降压作用的小分子生物肽,有望开发为降压药物或功能食品。Objective To determine the effect of simulated gastrointestinal digestion in vitro on the activity of angiotensin-converting enzyme(ACE)inhibitory peptides from Coix seed glutelin,and to optimize the hydrolysis conditions.Methods Coix seed glutelin was hydrolyzed under simulated gastrointestinal contiditions.The components were separated by ultrafiltration with 3 kDa molecular weight cut off,and the ACE inhibition rate was determined by RP-HPLC method.Antihypertensive efficacy of the potently active components were further evaluated in spontaneously hypertensive rats.The hydrolysis conditions were finally optimized by-orthogonal experiment with hydrolysis degree as the index.Results At the concentration of 0.04 mg·mL^(-1),the ACE inhibition activity of≤3 kDa component from the simulated intestinal digestion by trypsin ranked first at(99.94±0.01)%.Single administration of this hydrolysate significantly reduced the blood pressure in spontaneously hypertensive rats.The optimum conditions for trypsin hydrolysis of Coix seed glutelin were as follows:hydrolysis time of 6 h,substrate concentration 1.5%,enzyme-substrate ratio at 1∶5,and the corresponding degree of hydrolysis was(16.37±1.68)%.Conclusion Coix seed glutelin can be used to generate small molecular peptides with obvious antihypertension effect after simulated gastrointestinal digestion,which can further help develop antihypertension drugs or functional foods.
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