In vitro evaluation and in vivo performance of lyophilized gliclazide

Enhancement of the dissolution rate of the poorly water-soluble hypoglycemic agent, gliclazide, by the aid of lyophilization was investigated. Mannitol, sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP-k-30) were employed in different weight ratios (43%, 56% and 64% w/w, respectively) as water-soluble excipients in the formulation. Lyophilized systems were found to exhibit extremely higher in vitro dissolution rate compared to the unprocessed drug powder. Solid state characterization of the lyophilized systems using X-ray powder diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry techniques revealed that dissolution enhancement was attributable to transformation of gliclazide from the crystalline to an amorphous state in the solid dispersion formed during the lyophilization process. The gastrointestinal absorption and hypoglycemic effect of the lyophilized gliclazide/SLS system were investigated following oral administration to Albino rabbits. C_max and area under the plasma concentration–time curve of gliclazide (AUC_0–12) after administration of the lyophilized formulations were significantly higher than those obtained after administration of the unprocessed gliclazide.     

Isolation,Purification, and Structural Features of a Polysaccharide from Phellinus linteus and Its Hypoglycemic Effect in Alloxan‐Induced Diabetic Mice

Phellinus linteus is a medicinal mushroom that has been used in Oriental countries for centuries for its antitumor, antioxidant, immunomodulatory, and biological activity on hyperglycemia. A water‐soluble crude polysaccharide was extracted using hot water from P. linteus mycelia grown under submerged culture. An orthogonal experiment was used to optimize the extraction conditions of P. linteus mycelia polysaccharides (PLP). The crude polysaccharide was purified using DEAE Sephadex A‐50 and Sephadex G‐200 chromatography. Fourier transform infrared (FT‐IR) spectroscopy and nuclear magnetic resonance (¹H NMR) spectroscopy were used to investigate the structure of the purified P. linteus polysaccharide (PLP‐I), revealing that it was mainly a branched‐type glycan with both α‐ and β‐linkages and a pyranoid sugar ring conformation. PLP orally administered at 100 mg/kg body weight/d could significantly reduce the blood glucose level by 35.60% in alloxan‐induced diabetic mice. The results of an oral glucose tolerance test (OGTT) revealed that PLP had an effect on glucose disposal after 28 d of treatment. The result revealed that PLP from a submerged culture of P. linteus mycelia possessed potent hypoglycemic properties. The polysaccharide may be useful as a functional food additive and a hypoglycemic agent.     

豌豆超微粉碎膳食纤维对糖尿病小鼠肠道菌群及其代谢产物的影响

目的：研究豌豆超微粉碎膳食纤维（ultrafine ground pea dietary fiber,UGPDF）对糖尿病小鼠肠道菌群及其代谢产物的影响,从而揭示其降血糖的作用机制。方法：通过腹腔注射链脲佐菌素建立糖尿病小鼠模型,用二甲双胍和高剂量（0.9 g/（mL·d））、低剂量（0.45 g/（mL·d））UGPDF分别灌胃干预4 周,测定小鼠血糖浓度、观察肝脏细胞形态变化,Western blot检测小鼠肝脏中磷脂酰肌醇-3-激酶（phosphatidylinositol-3-kinase,PI3K）/蛋白激酶B（protein kinase B,AKT）/类胰岛素生长因子（insulin-like growth factors,IGF）蛋白表达水平,高通量测序分析各组小鼠粪便中的肠道菌群组成。结果：UGPDF能够调节糖尿病小鼠的肠道菌群丰度及多样性,高剂量UGPDF组操作分类单元（operational taxonomic units,OTU）数达300±36,其Shannon、Simpson指数与糖尿病小鼠存在显著差异（P＜0.05）。在肠道菌群组成中,与模型组相比,UGPDF干预后,Lactobacillus、Lachnospiraceae有益菌相对丰度显著上升（P＜0.05）,Helicobacter、Klebsiella、Clostridium致病菌相对丰度显著下降（P＜0.05）。从代谢产物来看,与模型组相比,经过UGPDF干预后,小鼠粪便内的6 种短链脂肪酸含量总体显著升高（P＜0.05）,其中以高剂量组效果最为显著,乙酸、丙酸、丁酸含量分别提高了63.7%、75.9%和96.0%,且接近正常对照组。同时,肝脏组织切片及Western blot检测结果表明UGPDF可调节糖尿病小鼠肝脏PI3K/AKT/IGF信号通路,修复肝细胞损伤,提高胰岛素敏感性。本实验可为豌豆膳食纤维的高值化利用拓宽思路,并补充完善其降血糖理论。     

辣木叶总黄酮的提取及其降血糖作用

采用乙醇回流法从辣木叶中提取黄酮类化合物,经AB-8型大孔吸附树脂柱纯化获得辣木叶总黄酮（TFM）;以四氧嘧啶糖尿病小鼠为动物模型,以中成药消渴丸为对照,进行TFM的降血糖动物试验研究。结果表明TFM能明显降低糖尿病模型小鼠的血糖,同时能提高血清SOD活力,降低血清MDA含量,但TFM对正常小鼠的血糖水平无影响。     

癞葡萄降糖活性成分的提取及其降糖活性的研究

对癞葡萄中水溶性降糖活性成分的提取进行了研究.以水作为溶剂提取癞葡萄的降糖活性成分,通过10kdal的超滤膜将水提物分为二个组分,并对这两个组分分别进行了降糖活性动物实验.结果表明,大、小分子组分均有一定降糖效果,但相对分子量大于10kdal的组分降糖效果不显著;相对分子量小于10kdal的组分降糖活性显著,起着主要的降糖作用.     

天然降糖食品——南瓜的最新研究进展

南瓜是一种极具开发潜力和开发价值的天然降血糖保健食品,从南瓜的历史起源、植物学性状、营养价值、医疗保健作用等方面对南瓜的效用及研究进展做以简要介绍。     

大叶紫薇叶中降血糖活性成分的筛选

为筛选大叶紫薇叶中具有降血糖活性的成分,采用3T3-L1细胞葡萄糖消耗模型作为检测手段,对大叶紫薇叶提取物采用HP-20树脂吸附、溶剂萃取、制备薄层分离和制备高效液相分离,导向筛选具有降血糖作用的各分离组分.结果发现,大叶紫薇叶中corosolic acid、熊果酸和总三萜具有降血糖活性.     

肉桂降糖活性成分提取方法的研究

用乙醇回流提取法、超声波提取法、新装置提取法提取肉桂降糖活性成分。结果表明,新装置提取法比回流提取法、超声波提取法提取效率高,且快速简便。新装置提取法提取肉桂降糖活性成分的最佳条件为:多功能提取器装置,提取溶剂为95%乙醇,提取时间2 h,产品粗提率达21.0%。     

红参浓缩液对小鼠的抗氧化、免疫调节及降血糖作用

该研究通过建立衰老小鼠模型和II型糖尿病小鼠模型,对比不同剂量的红参浓缩液对小鼠体内抗氧化、免疫及降血糖活性影响。实验发现：与模型组相比,红参浓缩液给药组显著降低丙二醛含量（MDA）、空腹血糖（FBG）和口服葡萄糖耐量（OGTT）血糖曲线下面积（AUC）并且显著提高羟自由基清除率（•OH）、总超氧化物歧化酶（T-SOD）、谷胱甘肽过氧化氢酶（GSH-Px）和过氧化氢酶（CAT）活力和免疫球蛋白G（Ig G）、免疫球蛋白M（Ig M）、白细胞介素4（IL-4）和γ干扰素（IFN-γ）含量（P<0.05）,明显改善脾脏损害。以上结果表明一定浓度的红参浓缩液可以延缓衰老、提高衰老模型小鼠的免疫力,增强II型糖尿病模型小鼠的葡萄糖耐受力,具有降血糖的效果。