叶瓜参多糖活性成分的研究

目的对叶瓜参中的多糖进行分析。方法应用现代提取分离方法和化学及光谱鉴定技术对多糖成分进行分离鉴定。结果从叶瓜参中分离鉴定了CFG-1、CFG-2和CFG-3等3种多糖成分。结论 CFG-1由木糖、3-甲氧基葡萄糖和葡萄糖组成,其摩尔数比=2︰1︰1;CFG-2由木糖、喹纳糖、3-甲氧基葡萄糖和葡萄糖组成,其摩尔数比=2︰1︰1︰1;CFG-3由喹纳糖和葡萄糖组成,其摩尔数比=1︰1。叶瓜参多糖CFG-2的PTP1B酶活性抑制试验显示,对PTP1B酶具有显著的抑制活性。     

Contribution of momilactones A and B to diabetes inhibitory potential of rice bran: Evidence from in vitro assays

This study was the first to detect the presence of the two compounds momilactone A (MA) and momilactone B (MB) in rice bran using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). By in vitro assays, both MA and MB exhibited potent inhibitory activities on pancreatic α-amylase and α-glucosidase which were significantly higher than γ-oryzanol, a well-known diabetes inhibitor. Remarkably, MA and MB indicated an effective inhibition on trypsin with the IC₅₀ values of 921.55 and 884.03 µg/mL, respectively. By high-performance liquid chromatography (HPLC), quantities of MA (6.65 µg/g dry weight) and MB (6.24 µg/g dry weight) in rice bran were determined. Findings of this study revealed the α-amylase, α-glucosidase and trypsin inhibitors MA and MB contributed an active role to the diabetes inhibitory potential of rice bran.     

2010-2012年我院抗糖尿病药物应用分析

目的:分析我院2010-2012年抗糖尿病药物的应用情况,为其合理用药提供依据。方法:对我院2010-2012年抗糖尿病药物的使用数据用Excel2003软件进行销售金额、用药频度(DDDs)、构成比、日均费用(DDC)等统计分析。结果:我院抗糖尿病药物的用药金额逐年稳定上升,DDDs排在前3位的为甘精胰岛素、瑞格列奈、精蛋白生物合成人胰岛素(预混30R);DDC排名前3位的为依帕司他、甘精胰岛素、精蛋白锌重组赖脯胰岛素混合注射液(25R)。结论:我院2010-2012年抗糖尿病药物的使用状况较为合理,非磺脲类促胰岛素分泌剂的选用倾向较大,口服新贵药和胰岛素制剂将会占据更大份额,临床应引起足够重视。     

Clinical potentials of ginseng polysaccharide for treating gestational diabetes mellitus

Gestational diabetes mellitus (GDM) is the most common glucose metabolism complication or cause of potential impaired glucose tolerance that can occur either before or during pregnancy and lactation. The prevalence of GDM and its related complications in young women is increasing, and this condition may cause serious outcomes and health hazards to the foetus. However, traditional oral hypoglycaemic drugs have potential safety hazards; therefore, it is urgent to develop new, safe, effective, and easily administered agents and remedies. Ginseng polysaccharide (GPS), which is isolated from Panax (P.) ginseng C. A. Meyer, exhibits notably promising biological activities and effects; specifically, it has been shown to lower blood glucose with mild, safe, and nontoxic characteristics, and it can also improve human bodily functions. Hence, we hypothesise that GPS might be used as an additional therapy and candidate agent for treating GDM. This review innovatively summarizes the available reports and evidence from basic studies to analyze the potential for and feasibility of using GPS as a new therapeutic agent for treating GDM. Additionally, for the first time, this review provides a rationale for the use of GPS. Our summarized results show that GPS may be developed as a novel antidiabetic drug and a remedy for use in preventing and treating GDM, with great application prospects.     

Anti-diabetic effects including diabetic nephropathy of anti-osteoporotic trace minerals on diabetic mice

Objective

In our previous study to evaluate the effects of soluble silicon (Si) on bone metabolism, Si and coral sand (CS) as a natural Si-containing material suppressed peroxisome proliferator-activated receptor γ (PPARγ), which regulates both glucose and bone metabolism and increases adipogenesis at the expense of osteogenesis, leading to bone loss. In this study, we investigated the anti-diabetic effects of bone-seeking elements, Si and stable strontium (Sr), and CS as a natural material containing these elements using obese diabetic KKAy mice.

Methods

Weanling male mice were fed diets containing 1% Ca supplemented with CaCO₃ as the control and CS, and diets supplemented with 50 ppm Si or 750 ppm Sr to control diet for 56 d. The mRNA expressions related to energy expenditure in the pancreas and kidney were quantified by real-time polymerase chain reaction.

Results

At the end of feeding, plasma glucose, insulin, leptin, and adiponectin levels decreased significantly in three test groups, while pancreatic PPARγ and adiponectin mRNA expression levels increased significantly toward the normal level, improving the glucose sensitivity of β-cells and inducing a significant decrease in insulin expression. The renal PPARγ, PPARα, and adiponectin expression levels, histologic indices of diabetic glomerulopathy, and plasma indices of renal function were also improved significantly in the test groups.

Conclusion

Taken together, anti-osteoporotic trace minerals, Si and Sr, and CS containing them showed novel anti-diabetic effects of lowering blood glucose level, improving the tolerance to insulin, leptin, and adiponectin, and reducing the risk of glomerulopathy through modulation of related gene expression in the pancreas and kidney.     

Bioactive polyphenols in kinkéliba tea (Combretum micranthum) and their glucose-lowering activities

Herbal tea kinkéliba prepared from the leaves of Combretum micranthum has been widely consumed in West African countries for its flavor, nutritional and medicinal properties. Under bio-guided screening, the kinkéliba leaves were chemically investigated using various chromatographic and spectrometric methods that led to the identification of thirteen different flavonoid compounds. Further biological tests illustrated that the identified compounds may have synergistic effects to decrease the expression of phosphoenolpyruvate carboxykinase (PEPCK) mRNA and glucose production in an H4IIE hepatoma cell line, indicating its potential use for insulin-resistant diabetes treatment. Further in vivo study on C57BL/6J mice indicates that kinkéliba can lower plasma glucose levels in a dose-dependent manner without significant weight loss and toxicity. The ethyl acetate extract in rich of flavonoids could also increase the glucose tolerance (GT) after seven weeks' administrations. Both in vitro and in vivo experiments support a potential new application of kinkéliba leaves as an anti-diabetes agent.     

Antidiabetic effects of Swertia macrosperma extracts in diabetic rats

Ethnopharmacological relevance

Swertia macrosperma is a traditional folk medicine used for its anti-hepatitis, antipyretic and antidotal effects as “Dida” or “Zangyinchen” in Tibet, Yunnan and Guizhou province for a long time, and it has been reported for its anti-diabetic effects in a Chinese patent. Swertia macrosperma was reported rich in xanthones, iridoids, seco-iridoids and their glycosides, several of which had been documented as potential antidiabetic agents. The objective of this study was to investigate the antidiabetic effect of Swertia macrosperma in diabetic rats.

Materials and methods

This study was designed firstly to evaluate the effect of Swertia macrosperma on glucose consumption in HepG2 cells. Based on the result in HepG2 cells, the antidiabetic effect of ethanol extract (EE) and n-butanol extract (BE) were investigated in diabetic rats induced by high fat fed and streptozotocin. The effects of EE and BE on fasting blood glucose, oral glucose tolerance test, serum insulin, glycosylated hemoglobin, serum lipid level, serum antioxidant parameters, glucokinase, glucose-6-phosphatase activities and glycogen content in liver tissue were measured, histology examination of pancreatic tissue was also carried out.

Results

After 4 weeks treatment with EE and BE, apparently decreased fasting blood glucose concentrations were observed in these treated groups, compared with the diabetic control groups. Additionally, improvement in serum antioxidant parameters and lipid profile were evidenced clearly. Moreover, EE and BE had effects of protecting the pancreatic β-cells and stimulating insulin secretion from the remaining pancreatic β-cells, evidenced by pancreatic histology examination. Increased glucokinase activity and decreased glucose-6-phosphatase activity were observed in liver.

Conclusion

The results of in vivo and in vitro experiment suggested that EE and BE of Swertia macrosperma had excellent effects on controlling the hyperglycemia and hyperlipidemia in diabetic rats.     

Evaluation of extraction protocols for anti-diabetic phytochemical substances from medicinal plants

AIM To examine the efficacy of three extraction techniques: Soxhlet-extraction(SE), cold-maceration(CM) and microwave-assisted-extraction(MAE) using 80% methanol as solvent. METHODS The study was performed on each of 50 g of Vernonia amygdalina(VA) and Occimum gratissimum(OG) leaves respectively. The percentage yield, duration of extraction, volume of solvent used, qualitative and quantitative phytoconstituents present was compared. The biological activities(hypoglycemic effect) were investigated using albino wistar rat model of diabetes mellitus(n = 36) with a combined dose(1:1) of the two plants leaf extracts(250 mg/kg b.w.) from the three methods. Theextracts were administered orally, once daily for 21 d.RESULTS In this report, the percentage VA extract yield from MAE was highest(20.9% ± 1.05%) within 39 min using 250 m L of solvent, when compared to the CM(14.35% ± 0.28%) within 4320 min using 900 m L of solvent and SE(15.75% ± 0.71%) within 265 min using 500 m L of solvent. The percentage differences in OG extract yield between: MAE vs SE was 41.05%; MAE vs CM was 46.81% and SE vs CM was 9.77%. The qualitative chemical analysis of the two plants showed no difference in the various phytoconstituents tested, but differs quantitatively in the amount of the individual phytoconstituents, as MAE had significantly high yield(P 0.05) on phenolics, saponins and tannins. SE technique gave significantly high yield(P 0.05) on alkaloid, while CM gave significant high yield on flavonoids. The extracts from CM exhibited a significantly(P 0.05) better hypoglycemic activity within the first 14-d of treatment(43.3% ± 3.62%) when compared to MAE(36.5% ± 0.08%) and SE methods(33.3% ± 1.60%). However, the percentage hypoglycemic activity, 21 d post-treatment with 250 mg/kg b.w. extract from MAE was 72.6% ± 1.03% and it was more comparable to 10 mg/kg b.w. glibenclamide treated group(75.0% ± 0.73%), unlike the SE(69.5% ± 0.71%) and CM(69.1% ± 1.03%). CONCLUSION CM technique produces extract with better hypoglycemic activity, whereas; MAE is a better option for high yield of phytoconstituents using less solvent within a short time.     

两色金鸡菊化学成分及抗糖尿病功能研究进展

两色金鸡菊是菊科金鸡菊属两色金鸡菊的头状花序,主要分布于新疆南疆地区海拔3000m左右的昆仑山区,是新疆地区临床应用广泛的维吾尔族民族药,其头状花序具有清热解毒、活血化瘀、和胃健脾、降血脂、软化血管等作用。本文针对两色金鸡菊的化学成分及抗糖尿病等药理研究进行综述,为研究发现新型具抗糖尿病功能活性成分的新药开发利用提供重要依据。     

Anti-diabetic and anti-obesitic effects of aqueous extracts of Yangkyuksanhwa-tang and its two major compositions on db/db mice

Type 2 diabetes mellitus (T2DM) is a metabolic syndrome that results from target-tissue resistance to insulin. Obesity is the condition of excess body fat accumulation. T2DM and obesity are both associated with hypertension, hyperlipidemia, and abdominal obesity. In Korean medicine, Yangkyuksanhwa-tang (YKSHT) has been prescribed for patients with T2DM. Oral glucose tolerance tests (OGTT), multiplex assays and hemoglobin A_1C (HbA1C) assessments were performed to determine the anti-diabetic effects of YKSHT and two major compositions of YKSHT, Lonicera japonica Thunb. (LJT) and Rehmannia glutinosa (RG) on db/db mice, a rodent model for T2DM. To study the anti-obesitic effects of LJT, RG or YKSHT, blood profiling including the triglycerides (TGs) and the total, LDL and HDL cholesterol levels were measured. In addition, body index measures such as the liver, retroperitoneal and epididymal fat tissues were collected and weighed. Mice treated with RG or YKSHT showed reduced blood glucose levels after stimulating the plasma GLP-1 levels. The multiplex assay results support the weight-controlling effects of the LJT, RG and YKSHT treatments, showing reducing levels of ghrelin and the induction of peptide YY (PYY) secretion. The YKSHT treatment reduced plasma TG levels and increased HDL cholesterol levels. The weights of the liver, retroperitoneal and epididymal fat tissues were reduced after the YKSHT treatment. Hence, we suggest that YKSHT can be utilized for the prevention and treatment of T2DM and obesity simultaneously.