Hypoglycemic effects of the wood of Taxus yunnanensis on streptozotocin-induced diabetic rats and its active components

Hypoglycemic effects of the H(2)O and MeOH extracts of the wood of Taxus yunnanensis were examined in streptozotocin (STZ)-induced diabetic rats. The H(2)O extract significantly lowered the fasting blood glucose level by 33.7% at a 100mg/kg dose on intraperitoneal administration. From the active H(2)O extract of the wood, three lignans, i.e., isotaxiresinol (1), secoisolariciresinol (2) and taxiresinol (3), were isolated as major components. These lignans were further tested for their hypoglycemic effects on the same experimental model. At a dose of 100mg/kg (i.p.), isotaxiresinol (1) reduced the fasting blood glucose level of diabetic rats by 34.5%, while secoisolariciresinol (2) and taxiresinol (3) reduced by 33.4% and 20.9%, respectively. The blood glucose lowering effects of 1 and 2 were stronger than the mixture of tolbutamide (200mg/kg) and buformin (1mg/kg) used as a positive control, which lowered fasting blood glucose level by 24.0%.     

Constituents of Chrysothamnus viscidiflorus

A phytochemical investigation of the aerial parts of Chrysothamnus viscidiflorus var. viscidiflorus afforded three new [chrysothol (1), 2 and 4] and seven known compounds, including five sesquiterpenes, two cinnamic acid derivatives, two ketoalcohol derivatives and one coumarin glucoside. The structures of two previously reported compounds, 1b and 1c, were revised on the basis of chemical reaction. Structures of the compounds were determined by extensive NMR studies, including DEPT, COSY, NOE, HMQC, HMBC and X-ray analysis. The unpublished X-ray data of the known compounds 6 and 7 are reported. Compounds chrysothol (1), and 8-10 showed anti-cancer activity against human breast cancer cells.     

Lignan, phenolic and iridoid glycosides from Stereospermum cylindricum

A lignan glycoside [(+)-cycloolivil 4'-O-beta-d-glucopyranoside], a phenolic glycoside [3,4-dimethoxyphenyl 1-O-beta-d-xylopyranosyl-(1-->6)-beta-d-glucopyranoside] and a iridoid glycoside (stereospermoside) were isolated from the leaves and branches of Stereospermum cylindricum, together with (+)-cycloolivil, (+)-cycloolivil 6-O-beta-d-glucopyranoside, (-)-olivil, (-)-olivil 4-O-beta-d-glucopyranoside, (-)-olivil 4'-O-beta-d-glucopyranoside, vanilloloside, decaffeoyl-verbascoside, isoverbascoside, 3,4,5-trimethoxyphenyl 1-O-beta-d-xylopyranosyl-(1-->6)-beta-d-glucopyranoside, ajugol, verminoside, and specioside. The structure elucidations were based on spectroscopic evidence.     

Bridelionosides A-F: Megastigmane glucosides from Bridelia glauca f. balansae

The chemical investigation of leaves of Bridelia glauca f. balansae afforded six megastigmane glucosides, named bridelionosides A-F, along with seven known megastigmane glucosides. Their structures were determined by a combination of spectroscopic analyses and by application of the modified Mosher's method.     

Concentration measurements of sucrose and sugar surfactants solutions by using the 1H NMR ERETIC method

The ERETIC method has been used to determine precise concentrations of aqueous solutions of sucrose and sugar surfactants, namely octyl glucoside and fatty acid sucrose esters by (1)H NMR spectroscopy. The effects of NMR tuning, acquisition parameters, and spectrum processing on the measurement have been assessed in these particular cases. The linearity upholds over the whole concentration range, with both sucrose and octyl glucoside, whatever the physicochemical phenomena occurring, either an increasing viscosity or the micellization of the surfactant. For sucrose solutions, an accuracy of 2% is measured for concentrations between 0.1 and 200 mmol/L, which is consistent with literature data.     

Synergistic activity and mode of action of flavonoids isolated from smaller galangal and amoxicillin combinations against amoxicillin-resistant Escherichia coli

Aim: The smaller galangal is extracted, purified and identified the bioactive compounds. The purpose of this research was to investigate whether these isolated compounds have antibacterial and synergistic activity against amoxicillin‐resistant Escherichia coli (AREC) when used singly and in combination with amoxicillin. The primarily mode of action is also studied. Method and Results: The galangin, kaempferide and kaempferide‐3‐O‐β‐d ‐glucoside were isolated. The minimum inhibitory concentrations(MIC) of amoxicillin and these flavonoids against AREC were between 500 and >1000 μg ml^?1. Synergistic activity was observed on combining amoxicillin with these flavonoids. The combinations of amoxicillin and these flavonoids exhibited a synergistic effect, reducing AREC cell numbers. Electron microscopy showed that these combinations damaged the ultrastructure of AREC cells. The results indicated that these combinations altered outer membrane permeability but not affecting cytoplasmic membrane. Enzyme assays showed that these flavonoids had an inhibitory activity against penicillinase. Conclusion: These results indicated that these flavonoids have the potential to reverse bacterial resistance to amoxicillin in AREC and may operate via three mechanisms: inhibition of peptidoglycan and ribosome synthesis, alteration of outer membrane permeability, and interaction with β‐lactamases. Significance and Impact of the Study: These findings offer the potential to develop a new generation of phytopharmaceuticals to treat AREC.     

综述:中药治疗阿尔茨海默病的作用特点

阿尔茨海默病(AD)是一种多因素相关的复杂性疾病,目前临床治疗效果不佳．仅针对单靶点或单致病途径的药物不易取得好的疗效．另一个重要原因是干预时机太晚,当诊断出痴呆时患者脑内已有大量神经元死亡．因此,应当针对多靶点、多途径治疗,同时将治疗时机提前到痴呆发生前,才有可能在AD的药物干预领域实现新的突破．本文综述了作者近十多年来在中药治疗AD方面的研究工作,包括中药新复方参乌胶囊、中药提取物何首乌二苯乙烯苷、山茱萸环烯醚萜苷、淫羊藿黄酮和淫羊藿苷对多种拟AD动物模型和细胞模型的影响及其作用机制．这些中药的特点是作用在AD复杂发病机制的多靶点和多途径,尤其是具有神经保护和神经营养/再生作用,且对线粒体和突触具有明显的保护作用,可望用于AD的早期干预或轻度认知障碍期(MCI)的治疗,从而阻止或延缓痴呆的发生与进程．     

芪合酶基因Fm-STS在何首乌毛状根中的过量表达及dsRNA干扰

目的:建立一套探究植物基因功能的方法体系,验证由芪合酶基因保守序列通过RACE扩增技术在何首乌中得到的基因Fm -STS的功能.方法:由含CaMV 35S启动子驱动的gfp基因的植物转基因表达基础质粒pBIN-35S-GFP构建过表达质粒pBIN-35S-STS-GFP(阳性)和双链RNA干扰重组质粒pBIN-35S-正向-反向-GFP(阴性),并同空白表达质粒pBIN-35S-GFP(空白)均导入野生型发根农杆菌ATCC15834中,转化何首乌外植体,诱导生成毛状根并培养,对毛状根进行高效液相色谱分析以及实时荧光定量检测.结果:在过表达组、空白组和干扰组中毛状根中发根农杆菌Ri质粒中的rolB基因和外源基因gfp均有表达,高效液相色谱法分析芪合物二苯乙烯苷含量依次为4.67mg/g、2.18mg/g和0.65 mg/g,在mRNA水平上测试荧光定量检测基因Fm-STS表达量:RNAi组是空白组的1/433.53,过表达组是空白组的2.41倍.结论:结果表明过量表达与双链RNA干扰相结合在植物基因功能研究中有良好的应用,何首乌中芪合酶Fm-STS是二苯乙烯苷主要的合成酶.     

荔枝核的五个苷类成分

通过溶剂分部和多种色谱分离,从荔枝(Litchi chinensis Sonn.)核中得到5个苷类成分。经光谱分析及与文献数据对照,分别鉴定为(-)-松脂素4-O-β- D-吡喃葡萄糖苷 (1)、苯乙基β- D-吡喃葡萄糖苷 (2)、乙基β- D-吡喃葡萄糖苷 (3)、乙基α- D-吡喃葡萄糖苷 (4)和胞苷 (5)。它们均为首次从荔枝核中分离得到。     

Temperature regulates tuber-inducing lipoxygenase-derived metabolites in potato (Solanum tuberosum)

Temperature is one of the major environmental factors affecting potato tuberization. It has been suggested that lipoxygenase (LOX) mediates between temperature and tuber induction. In this study, the contents of the LOX-derived metabolites hydroperoxylinolenic acid (HPOT), jasmonic acid (JA), tuberonic acid (TA) and tuberonic acid glucoside (TAG) were analyzed in leaves of potatoes growing at different temperatures. At low, tuber-inducing temperature, endogenous levels of JA, TA and TAG rise, indicating their crucial role in tuber induction. The concentration of 13(S)-HPOT seems not to be directly affected by temperature. Instead, the molecule has only a short half-life in leaves and is readily metabolized.