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降糖活性物6-苄氧基-9-(-4-氯甲苯酰基)-四氢化咔唑-3-羧酸在人工胃肠液中的稳定性研究及降解产物分析 被引量:1
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作者 张吉泉 郝阳 +2 位作者 陈瑞 王丽丽 汤磊 《中国药房》 CAS 北大核心 2019年第9期1177-1181,共5页
目的:考察降糖活性物6-苄氧基-9-(-4-氯甲苯酰基)-四氢化咔唑-3-羧酸(简称"ZgO2")在人工胃肠液中的稳定性,并分析其降解产物。方法:采用高效液相色谱法,以吲哚美辛为内标,检测ZgO2在空白人工胃液(pH 1.3,不含酶)、空白人工肠... 目的:考察降糖活性物6-苄氧基-9-(-4-氯甲苯酰基)-四氢化咔唑-3-羧酸(简称"ZgO2")在人工胃肠液中的稳定性,并分析其降解产物。方法:采用高效液相色谱法,以吲哚美辛为内标,检测ZgO2在空白人工胃液(pH 1.3,不含酶)、空白人工肠液(pH6.8,不含酶)、人工胃液(pH 1.3,含胃蛋白酶)和人工肠液(pH 6.8,含胰蛋白酶)中孵育6 h的含量变化,计算ZgO2剩余百分比;利用超高效液相色谱-四极杆-飞行时间质谱(UPLC-Q-TOF/MS)技术分析对照样品(ZgO2对照品溶液)、空白样品(未加入ZgO2的孵育溶液)、孵育样品(稳定性试验中ZgO2浓度变化最明显的孵育体系)的总离子流图,比较差异峰,通过MS图推测降解产物。结果:ZgO2在空白人工肠液和人工肠液中孵育不同时间的剩余百分比均在90%~110%范围内;ZgO2在酸性(pH 1.3)条件中不稳定,在孵育3 h时剩余百分比约为50%,继续孵育剩余百分比无明显变化,人工胃液(含酶)中的剩余百分比低于空白人工胃液(不含酶)的剩余百分比,但相差不明显。孵育样品与对照样品、空白样品的差异体现在负模式扫描下保留时间为5.23 min时,该时间点色谱峰的MS显示,低能量扫描通道存在m/z 320.127 2[M-H]-的准分子离子峰,高能量通道可见碎片离子峰230.081 5、276.138 2,推测ZgO2在酸性(pH 1.3)条件下可能发生酰胺键断裂生成6-苄氧基-四氢化咔唑-3-羧酸。结论:ZgO2在人工肠液中稳定性良好;在酸性(pH 1.3)条件下不稳定,基本上不受胃蛋白酶的影响,降解产物可能为6-苄氧基-四氢化咔唑-3-羧酸。 展开更多
关键词 降糖活性物 6-苄氧基-9-(-4-氯甲苯酰基)-四氢化咔唑-3-羧酸 人工胃肠液 稳定性 降解产
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红花降糖活性成分谱效关系研究 被引量:3
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作者 武鹤婷 赛那瓦尔·芒思尔 +2 位作者 高彦华 信学雷 宁慧霞 《天然产物研究与开发》 CAS CSCD 2021年第2期188-197,255,共11页
红花为菊科植物红花(Carthamus tinctorius L.)的干燥花,具有活血通经,散瘀止痛等功能。为研究其降糖活性成分及谱效关系,本文确定了红花降糖活性部位;建立了HPLC指纹图谱,通过对照品指认其中7个主要成分后,用灰色关联度法和正交偏最小... 红花为菊科植物红花(Carthamus tinctorius L.)的干燥花,具有活血通经,散瘀止痛等功能。为研究其降糖活性成分及谱效关系,本文确定了红花降糖活性部位;建立了HPLC指纹图谱,通过对照品指认其中7个主要成分后,用灰色关联度法和正交偏最小二乘法分析,揭示了这7个共有峰协同发挥蛋白酪氨酸磷酸酯酶1B抑制作用,其中羟基红花黄色素A(HSYA,6号峰)和6-羟基山柰酚-3,6-二-O-葡萄糖基-7-O-葡萄糖苷(3号峰)是贡献最大的成分。含量测定显示10批红花中羟基红花黄色素A及山柰素的含量均在1.67%~1.94%和0.09%~0.12%之间,该研究为红花在糖尿病药物开发领域的应用提供了依据。 展开更多
关键词 红花 降糖活性提取 谱效关系 灰色关联度分析法 正交偏最小二乘法分析
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Silkworm Extract Ameliorates Type 2 Diabetes Mellitus and Protects Pancreaticβ-cell Functions in Rats 被引量:2
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作者 WAN Hui-Qi QI Huan-Yang +1 位作者 XU Guang-Hui HUANG Yi-Qi 《Digital Chinese Medicine》 2020年第4期275-282,共8页
Objective The aim of the present study was to investigate the hypoglycemic effects of silkworm extract(SE)on experimental type 2 diabetes mellitus(T2DM)rats.Methods SE was prepared by dissolving freeze-dried silkworm ... Objective The aim of the present study was to investigate the hypoglycemic effects of silkworm extract(SE)on experimental type 2 diabetes mellitus(T2DM)rats.Methods SE was prepared by dissolving freeze-dried silkworm powder in 70%(v/v)aqueous ethanol.T2DM rats were induced by feeding them a high fat diet and an intraperitoneal injection of streptozotocin(STZ).The blood glucose,free fatty acid(FFA),malondialdehyde(MDA),tumor necrosis factor alpha(TNF-α)and superoxide dismutase(SOD)levels were detected by enzyme-linked immunosorbent assay(ELISA).The quality of SE was controlled by high performance liquid chromatography(HPLC;Agilent 1260,Agilent,USA).Hematoxylin-eosin(HE)staining was performed for histological evaluation.Antibody expression was assessed via immunohistochemistry(IHC)staining.Results SE could improve insulin resistance and islet cell function by reducing FFA,MDA and TNF-αlevels and increasing SOD level.In addition,pancreatic HE staining analysis revealed that SE has a protective effect on isletβ-cells.Conclusions The present study indicates that SE has hypoglycemic as well as pancreatic protective effects in T2DM model rats. 展开更多
关键词 Silkworm extract Hypoglycemic activity Type 2 diabetes mellitus(T2DM) Insulin resistance Pancreatic protection
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Antioxidant Activity and Anti-Hyperglycemic Effect of Lagenaria Siceraria Fruit Extract
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作者 Nguyen Kinh Luan Nguyen Ngoc Hong 《Journal of Food Science and Engineering》 2016年第1期26-31,共6页
Lagenaria siceraria (Molina) Standl., known as bottle gourd is widely available throughout Vietnam as an edible vegetable. Bottle gourd is a commonly fruit but there are little reports about its biological activitie... Lagenaria siceraria (Molina) Standl., known as bottle gourd is widely available throughout Vietnam as an edible vegetable. Bottle gourd is a commonly fruit but there are little reports about its biological activities. The aim of the present study was to evaluate antioxidant activity and anti-hyperglycemic potential of ethanolic extract of bottle gourd. The ethanolic extract was tested for its antioxidant activity on chelating power, the ferric reducing/antioxidant power assay (FRAP) and the 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging assay. The results showed that chelating activity was 80.02%, FRAP value was 92.84 μmol Fe^2+/g and active radical scavenging which showed an IC50 was 49.50 μg/ml. The five different doses of ethanolic extract were treated by oral tolerance to mice body before oral glucose tolerance and blood glucose level was measured using glucose oxidase method. The result indicated that inhibition percentage of ethanolic extract of bottle gourd at the dose of 400 mg/kg in glucose-induced hyperglycemic mice was effectively similar to standard drug glibenclamide. The results obtained indicate that ethanolic extract from bottle gourd is the potential antioxidant and anti-hyperglycemic agent. 展开更多
关键词 Lagenaria siceraria fruit ethanolic extract chelating power FRAP DPPH anti-hyperglycemic
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