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抗糖尿病多肽药物的口服递送研究进展 被引量:1
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作者 李静静 蔡祥胜 李红卫 《广东医学》 CAS 2018年第S2期294-296,共3页
糖尿病是一种复杂的疾病,发病率和病死率都很高,有大量新的治疗药物和给药途径被研究和开发。到现在为止,已有多个治疗糖尿病的多肽药物研发成功,其中包括胰岛素、胰高血糖素样肽-1(GLP-1)及其类似物。这些抗糖尿病多肽最常见的注射给... 糖尿病是一种复杂的疾病,发病率和病死率都很高,有大量新的治疗药物和给药途径被研究和开发。到现在为止,已有多个治疗糖尿病的多肽药物研发成功,其中包括胰岛素、胰高血糖素样肽-1(GLP-1)及其类似物。这些抗糖尿病多肽最常见的注射给药途径存在若干个缺点,而通过口服途径递送这些抗糖尿病多肽是该类药物研发数十年来的目标。糖尿病多肽药物口服递送遇到的主要问题是蛋白水解酶降解和胃肠道吸收差(GIT)导致的治疗效果不佳,本综述着重讲述目前改善抗糖尿病多肽的口服生物利用效率的研究进展。 展开更多
关键词 糖尿病药物 胰岛素 胰高血糖素样-1 口服递送
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枯草芽孢杆菌发酵紫菜制备一种α-葡萄糖苷酶抑制剂 被引量:1
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作者 许育衔 程慧敏 +2 位作者 韩贵新 毛相朝 姜宏 《食品与发酵工业》 CAS CSCD 北大核心 2023年第17期1-9,共9页
糖尿病是一种以高血糖为特征的慢性代谢疾病,由于化学降糖药物容易增加患者的肝肾负担与心血管疾病风险,因此针对轻症患者亟需一种能够控制血糖水平且低副作用的方法。许多研究表明紫菜具有降低餐后血糖的潜力,在降糖功能食品开发方面... 糖尿病是一种以高血糖为特征的慢性代谢疾病,由于化学降糖药物容易增加患者的肝肾负担与心血管疾病风险,因此针对轻症患者亟需一种能够控制血糖水平且低副作用的方法。许多研究表明紫菜具有降低餐后血糖的潜力,在降糖功能食品开发方面具有广阔的前景。该研究采用源自威海紫菜养殖基地的枯草芽孢杆菌(Bacillus subtilis)对条斑紫菜(Porphyra yezoensis)进行发酵,探究并优化了具有α-葡萄糖苷酶(α-glucosidase,GTase)抑制活性发酵产物的发酵条件,采用凝胶色谱法、LC-MS/MS分离并鉴定出具有GTase抑制活性的肽段,最后使用分子对接法对活性成分进行了模拟验证。结果表明,紫菜发酵粉对GTase形成竞争型抑制,IC_(50)为0.21 mg/mL,优于阳性对照阿卡波糖(IC_(50)=0.88 mg/mL)。成分分析与分子对接结果表明,抑制活性可能来源于肽段GPGDFL和SPPPPPA。该研究制备了一款具有GTase抑制作用的食品原料,并初步阐明了其中的主要活性成分,证明紫菜可以作为降血糖功能食品的来源之一,为紫菜的高值化开发利用提供了有效的理论支持。 展开更多
关键词 条斑紫菜 枯草芽孢杆菌 抗糖尿病肽 Α-葡萄糖苷酶 分子对接
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EFFECT OF ERYTHROMYCIN ON GASTRIC DYSMOTILITY AND NEUROENDOCRINE PEPTIDES IN RATS WITH DIABETES MELLITUS 被引量:3
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作者 Lin Lin Min Ji Hong-jie Zhang Zheng Lin Zhi-quan Zhao 《Chinese Medical Sciences Journal》 CAS CSCD 2005年第3期176-180,共5页
Objective To investigate the effect of erythromycin on the contractive activity of the isolated gastric antrum smooth muscle and somatostatin (SS), vasoactive intestinal peptide (VIP), motilin (MTL), and substan... Objective To investigate the effect of erythromycin on the contractive activity of the isolated gastric antrum smooth muscle and somatostatin (SS), vasoactive intestinal peptide (VIP), motilin (MTL), and substance P (SP) in plasma and isolated gastric antrum tissue of diabetes mellitus (DM) rat models. Methods Thirty male Sprague-Dawley rats were divided into three groups: control group (n = 10), DM group (n = 10), and erythromycin group (DM models with erythromycin treatment, n = 10). A single dose of streptozotocin (100 mg/kg, dissolved in 0. I mol/L citric acid buffer, pH4.5) was injected intraperitoneally. After 48 to 72 hours, rats with blood glucose above 16.7 mmol/L and urine glucose level to be (+++ ) to (++++) over one week were considered successful DM models. The resting tension, mean contractile amplitude and fi'equency of spontaneous change in isolated longitudinal and circular gastric antrum smooth muscle strips were measured. SS, VIP, MTL, and SP levels in plasma and gastric antrum tissue were measured using radioimmunoassay. Results (1) In the isolated gastric antrum smooth muscle strips, the gastric motility parameters were lower in DM group than those in control group except circular smooth muscle contractile amplitude and longitudinal smooth muscle contractile fi'equency. The gastric motility parameters were significantly strengthened in erythromycin group, compared with DM group except longitudinal smooth muscle resting tension (P 〈 0.01 ). (2) Plasma SS, VIP, and MTL concentrations in DM group were higher than those in control (P 〈 0.05), while the SP level decreased (P 〈 0.05). In the gastric antrum, SS of DM group was significantly higher than that of control group (P 〈 0.01 ), while SP and MTL levels were lower than those of control group (P 〈 0.05 and P 〈 0.01, respectively). However, the level of VIP in gastric antrum tissue did not change among three groups. The plasma level of SS in erythromycin group was higher than that of DM group (P 〈 0.05). (3) The blood glucose was lower in erythromycin group than DM group (P 〈 0.01 ). Conclusions Erythromycin has direct effects on contractive activity of gastric smooth muscle in diabetic rats, but there are few effects on neuroendocrine peptides. Gastric-motility disorders in diabetic rats have a correlation with the changes of neuroendocrine peptide levels in plasma and gastric antrum tissue. 展开更多
关键词 diabetes mellitus gastric dysmotility ERYTHROMYCIN SOMATOSTATIN vasoactive intestinal peptide MOTILIN substance P
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