山苦瓜化学成分及药理作用的研究进展

山苦瓜Momordica charantia var. abbreviata是苦瓜的野生变种,属于药食同源物质,具有重要的食用与保健功能,常被用作保健食品和民间医药。现代药理学表明,山苦瓜的活性成分和药理作用比苦瓜显著,主要化学成分包括皂苷类、酚类、脂肪酸和丰富的微量元素与矿物质,具有抗糖尿病、抗炎、抗菌、抗癌和抗氧化等多种药理作用。全面概述山苦瓜的化学成分和药理作用,为山苦瓜的开发利用提供理论基础,以期获得更好的实用价值。     

地特胰岛素联合口服降糖药对2型糖尿病患者血糖的影响

目的观察地特胰岛素联合口服降糖药（OAD）对OAD控制不佳的T2DM患者血糖控制的影响。方法入选30例1：3服降糖药效果欠佳的T2DM患者，给予地特胰岛素治疗。分别于治疗前、治疗后12周、治疗后24周测定HbA1c、FBG、体重、BMI。结果应用地特胰岛素治疗24周后HbA1c、FBG较治疗前均明显降低（P〈0．05）。治疗前后血脂、体重、BMI、腰围、臀围无明显变化。应用地特胰岛素治疗低血糖事件发生率较低，且无夜间低血糖事件。结论地特胰岛素联合OAD治疗可以改善OAD疗效差的T2DM病情，体重增加不明显，低血糖发生率低。     

抗糖尿病先导化合物Fla—CN的合成工艺研究

目的：对抗糖尿病先导化合物Fla—CN（3-O-[（E）-4-（4-氰基苯基）-3-烯-2-酮丁基]山萘酚）的合成工艺进行研究。方法：以对氰基苯甲醛和山萘酚为合成起始原料,先后经过Claisen—Schimidt反应,a,β-不饱和酮的a位溴代反应和醚化反应得到目标化合物Fla—CN．并从反应温度、底物浓度、反应物当量比以及催化剂等方面进行单因素考察试验,摸索最佳反应条件,建立合成工艺,提高反应总收率。结果：通过单因素考察等方法,建立了Fla—CN的合成工艺,目标产物的总收率显著提高,达到50％。结论：该工艺采用价廉易得的原料．简便的合成工艺与纯化手段,提高了反应收率,降低了生产成本。     

Oleanolic acid derivatives for pharmaceutical use: a patent review

Introduction: Oleanolic acid belongs to the pentacyclic triterpene family. In China, oleanolic acid has been used as an over the counter (OTC) hepatoprotective drug for decades. Oleanolic acid and its derivatives present a wide variety of biological activities, supporting their pharmaceutical uses for multiple diseases.

Areas covered: Representative patent publications (1971-2015) covering the preparation, pharmaceutical compositions, and medical uses of oleanolic acid and its derivatives are analyzed, with focus on their anticancer, anti-osteoporosis, anti-obesity, anti-diabetic, lipid-lowering, anti-inflammatory, antioxidant, immune-regulatory, and hepatoprotective effects. A large number of Chinese patents have been given particular attention in this review.

Expert opinion: Detailed efficacy studies are highly worth doing to undoubtedly confirm the clinical potential of oleanolic acid and its derivatives. Based on that, it would be critical to identify the key protein targets of the drugs so as to promote drug development and search for new lead compounds. Together, there is a huge potential for drug-repositioning of oleanolic acid, particularly in the areas of metabolic disease and immunological disorders.     

新型PEG化GLP-1受体激动剂的合成及其降血糖活性

为了得到持续稳定控制血糖的胰高血糖素样肽-1(glucagon-like peptide-1,GLP-1)类似物,将平均相对分子质量为350、550和750的单甲氧基聚乙二醇(mPEG)分别缀合到GLP-1肽链上,设计并合成了12个衍生物。初步药理活性表明,所得化合物均保留GLP-1受体激动活性,其中化合物I-12降糖活性维持时间与艾塞那肽(Ex-4)和利拉鲁肽(Liraglutide)相当,具备成为新型长效化GLP-1受体激动剂的潜力。     

Anti-Cancer,Anti-Diabetic and Other Pharmacologic and Biological Activities of Penta-Galloyl-Glucose

1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucose (PGG) is a polyphenolic compound highly enriched in a number of medicinal herbals. Several in vitro and a handful of in vivo studies have shown that PGG exhibits multiple biological activities which implicate a great potential for PGG in the therapy and prevention of several major diseases including cancer and diabetes. Chemically and functionally, PGG appears to be distinct from its constituent gallic acid or tea polyphenols. For anti-cancer activity, three published in vivo preclinical cancer model studies with PGG support promising efficacy to selectively inhibit malignancy without host toxicity. Potential mechanisms include anti-angiogenesis; anti-proliferative actions through inhibition of DNA replicative synthesis, S-phase arrest, and G₁ arrest; induction of apoptosis; anti-inflammation; and anti-oxidation. Putative molecular targets include p53, Stat3, Cox-2, VEGFR1, AP-1, SP-1, Nrf-2, and MMP-9. For anti-diabetic activity, PGG and analogues appear to improve glucose uptake. However, very little is known about the absorption, pharmacokinetics, and metabolism of PGG, or its toxicity profile. The lack of a large quantity of highly pure PGG has been a bottleneck limiting in vivo validation of cancer preventive and therapeutic efficacies in clinically relevant models.     

糖泰胶囊的药效学研究

目的探讨糖泰胶囊的临床疗效机制。方法对糖泰胶囊进行药效学实验研究。结果糖泰胶囊有显著的降血糖和增加肝糖元作用,对血清胰岛素含量水平有一定的升高作用。结论本品是一良好的降糖中药制剂。     

委陵菜抗糖尿病有效部位及有效成分的研究

目的:以四氧嘧啶模型小鼠结合提取分离方法鉴定委陵菜降血糖的有效部位及有效成分。方法:将委陵菜的95%乙醇提取物用不同极性的溶剂萃取得到各提取部位,以四氧嘧啶糖尿病小鼠模型考察各部位的抗糖尿病作用,并对其中抗糖尿病最强的部位进一步分离纯化,进一步检测化合物的抗糖尿病作用。结果:委陵菜F部位与委陵菜黄酮给药后与模型组均有显著性差异(P<0.01),说明委陵菜F部位与委陵菜黄酮具有明显的降低四氧嘧啶糖尿病小鼠血糖的作用,委陵菜黄酮降血糖作用强于阳性对照药盐酸苯乙双胍。结论:F部位是委陵菜降血糖的有效部位,委陵菜黄酮是委陵菜降血糖的有效成分。     

由降糖中成药和保健食品检验情况探索非法添加化学成分的系统快筛思路

本文分析了中成药及保健食品中非法添加降糖成分常是复合添加的特点,探索系统快筛思路,可指导建立一种对常见添加降糖成分的中成药及保健食品进行检测的快筛方法,具有提高检验的覆盖率和节省检验资源的优点。     

Anti-diabetic effects of linarin from Chrysanthemi Indici Flos via AMPK activationOA

Objective:The purpose of this study is to investigate the anti-diabetic effects of linarin,a flavonoid extracted from Chrysanthemi Indici Flos(CIF),and its potential mechanisms.Methods:The effects of linarin on cell viability and glucose consumption in Hep G2 cells were measured.Meanwhile,monosodium glutamate(MSG) mouse model was constructed to monitor the changes of insulin tolerance,glucose tolerance,triglyceride and cholesterol.The protein expression levels of pAMPK,p-ACC,PEPCK and p-GS were ...