黄褐毛忍冬和灰毡毛忍冬几种成分对大、小鼠化学性肝损伤的保护作用

目的：研究黄褐毛忍冬和灰毡毛忍冬几种成分对四氯化碳（ＣＣｌ_４）,Ｄ-氨基半乳糖（Ｄ-Ｇａｌ）等肝毒物造成大、小鼠肝损伤的保护作用。方法：大、小鼠分别ｓｃ黄褐毛忍冬和灰毡毛忍冬几种成分后,ｉｐＣＣｌ_４或Ｄ-Ｇａｌ,检测血清谷丙转氨酶（ｓＧＰＴ）、肝脏甘油三酯（ＴＧ）和丙二醛（ＭＤＡ）含量。结果：黄褐毛忍冬和灰毡毛忍冬几种成分均不同程度的降低由ＣＣｌ_４和Ｄ-Ｇａｌ引起的ｓＧＰＴ和ＴＧ的升高,降低ＣＣｌ_４引起的ＭＤＡ升高。结论：黄褐毛忍冬和灰毡毛忍冬几种成分具有降低几种肝毒物引起的肝脏毒性的作用。     

反复心理应激大鼠血浆和下丘脑单胺神经递质的变化及加味四逆散的影响

目的 :观察反复心理应激大鼠血浆和下丘脑内DA、5 HT、E、NE的变化以及加味四逆散的影响。方法 :采用限制大鼠活动空间的方法造成反复心理应激的动物模型 ;血浆和下丘脑内DA、5 HT、E、NE含量测定采用电化学高效液相色谱分析方法。结果 :反复心理应激大鼠血浆DA、5 HT含量明显降低 ,NE、E含量则明显升高 ,下丘脑DA和 5 HT含量明显降低。加味四逆散可以升高应激大鼠下丘脑和血浆中DA、5 HT含量 ,并能降低血浆中NE、E含量 ,升高下丘脑和血浆 5 HT/NE以及血浆 5 HT/E ,作用优于人参总皂甙。结论 :加味四逆散可显著增强反复心理应激状态大鼠的抗应激能力 ,其机制与其升高中枢和血浆中 5 HT及DA含量 ,降低血浆中NE和E含量有关。     

Effects of essential oil from Croton tiglium L. on intestinal transit in mice

AIM OF THE STUDY: Croton tiglium (Croton tiglium L., Euphorbiaceae) is widely used as a herb for treatment of gastrointestinal disturbances. Previous studies established its purgative and inflammational properties. The present study aimed to investigate the effects of Croton tiglium oil (CO) on intestinal transit in mice. MATERIALS AND METHODS: Gastrointestinal transit in mice and contractile characteristics of isolated intestinal strips from mice were evaluated. Intestinal inflammation was confirmed by histological examination. RESULTS: Low dose of CO increased the gastrointestinal transit of charcoal and barium meal as well as the production of fecal pellets in mice. In contrast, high dose exerted inhibitory effects. For normal colonic circular strips, both high and low dose of CO inhibited the contractile frequency. Low doses (0-20 microg/ml) of CO enhanced the phasic contractions, while high doses (>40 microg/ml) reduced them. Colonic longitudinal strips in CO-treated mice were less sensitive to electrical field stimulation than those in control mice. The contraction of colonic longitudinal, colonic and jejunal circular strips in CO-treated mice was more sensitive to atropine than that in control mice. CONCLUSIONS: CO might modulate gastrointestinal motility and induce intestinal inflammation related to immunological milieu and motor activity. Our findings may highlight the ethno-medical uses of Croton tiglium on intestinal disorders.     

Louki Zupa decoction attenuates the airway inflammation in acute asthma mice induced by ovalbumin through IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway

ContextAsthma is a common respiratory system disease. Louki Zupa decoction (LKZP), a traditional Chinese medicine, presents a promising efficacy against lung diseases.ObjectiveTo investigate the pathogenic mechanism of asthma and reveal the intervention mechanism of LKZP.Materials and methodsForty-eight female Balb/c mice were randomly divided into 6 groups: normal control group (NC), ovalbumin (OVA)/saline asthma model group, OVA/LL group, OVA/LM group, OVA/LH group and OVA/DEX group (n = 8 per group). The asthmatic mice were modelled through intraperitoneal injecting and neutralizing OVA. LKZP decoction was administrated by gavage at the challenge stage for seven consecutive days (2.1, 4.2 and 8.4 g/kg/day). We investigated the change in lung function, airway inflammation, mucus secretion and TH-1/TH-2-related cytokines. We further verify the activated status of the IL-33/ST2/NF-κB/GSK3β/mTOR signalling pathway.ResultsLKZP was proved to improve asthmatic symptoms, as evidenced by the down-regulated airway resistance by 36%, 58% and 53% (p < 0.01, p < 0.001 vs. OVA/saline group), up-regulated lung compliance by 102%, 114% and 111%, decreased airway inflammation and mucus secretion by 33%, 40% and 33% (p < 0.001 vs. OVA/saline group). Moreover, the content of cytokines in BALF related to airway allergy (such as IgE) and T helper 1/T helper 2 cells (like IL-2, IL-4, IL-5, IL-13, TNF-α and IFN-γ), were also markedly reduced by 13–65% on LKZP intervention groups compared with model group. Mechanistic research revealed that the IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway was activated in the OVA/saline group and LKZP significantly down-regulated this pathway.Discussion and conclusionLKZP improves lung function, airway inflammation, mucus secretion and correct immune imbalance by intervening with the IL-33/ST2-NF-κB/GSK3β/mTOR signalling pathway, presenting a promising therapeutic choice for asthma.     

Computational exploration for possible reaction pathways,regioselectivity, and influence of substrate in gold-catalyzed cycloaddition of cyanamides with enynamides

The current work focuses on the DFT calculation of the rational mechanism and catalytic activity of the gold(i)-catalyzed isotetradehydro-Diels–Alder cycloaddition of cyanamides and enamides to substituted 2,6-diaminopyridines. IPrAuCl is used as a model catalyst to catalyze cyanamide and enynamide reactants with different substituents in DCM as a research system. DFT data indicates that the catalytic cycle starts from the triple bond coordination between the catalyst''s gold cation and the enamide to obtain the gold π-complex, and the cyanamide attacks the alkynyl carbon atom from different directions to generate two reaction channels of five-membered and six-membered heterocycles, respectively. The calculation results show that the 2,6-diaminopyridine compounds produced by this catalytic reaction have lower activation energy and higher reactivity, that is, the pyridine skeleton structure can be easily obtained under mild reaction conditions. At the same time, electron-withdrawing substituents in the reactants are more helpful for the reaction. In addition to being in good agreement with the experimental data, the calculated results also provide an important contribution to the further understanding of the mechanism of such reactions.

The current work focuses on the DFT calculation of the rational mechanism and catalytic activity of the gold(i)-catalyzed isotetradehydro-Diels–Alder cycloaddition of cyanamides and enamides to substituted 2,6-diaminopyridines.     

国家中医药临床研究基地生物样本库建设初探

标准化生物样本库是众多重要科研成果快速产业化、应用到临床的重要保证,也是生命科学与生物医药技术自主创新体系中至关重要的环节与保证,是最宝贵资源。从生物样本库的概念和作用、建设进展着手分析生物样本库建设的现状、趋势和问题,并从样本的采集、方法及溯源、伦理问题、设施及环境和系统管理等方面详细论述了生物样本库建设的要素,并列举了目前我国生物样本库相关管理规范,旨在为国家中医药临床研究基地生物样本库建设与发展提供参考。     

白条党参化学成分研究

目的:研究甘肃省渭源县大宗种植药材白条党参的化学成分。方法:采用硅胶柱色谱等方法分离纯化,利用各种波谱技术(NMR)及理化性质确定化学结构。结果:从渭源产白条党参中分离得到11个化合物,分别为:橙皮苷(Ⅰ)、β-槐糖正己醇苷(Ⅱ)、苍术内酯Ⅲ(Ⅲ)、党参炔苷(Ⅳ)、lobetyolin in(Ⅴ)、蒲公英萜醇(Ⅵ)、蒲公英萜醇乙酸酯(Ⅶ)、α-菠甾醇(Ⅷ)、9,10,13-三羟基-反-11-十八烯酸(Ⅸ)、β-谷甾醇(Ⅹ)、β-胡萝卜苷(Ⅺ)和蔗糖(Ⅻ)。结论:化合物Ⅰ、Ⅱ和Ⅸ为首次从党参中分离得到。     

Glycosides from the stem bark of Fraxinus sieboldiana

A norditerpene glucopyranoside with a novel carbon skeleton (1), eight new aromatic glycosides (2-9), and 25 known glycosides have been isolated from a H2O-soluble portion of an ethanolic extract of the stem bark of Fraxinus sieboldiana. Their structures were determined by spectroscopic and chemical methods. Based on analysis of the NMR data of threo- and erythro-arylglycerols in different solvents, an application of Delta delta C8-C7 values to distinguish threo-arylglycerol and erythro-arylglycerol isomers was proposed. In the in vitro assays, compound 5 displayed TNF-alpha secretion inhibitory activity with an IC50 value of 1.6 microM, compound 6 showed antioxidative activity inhibiting Fe+2-cystine-induced rat liver microsomal lipid peroxidation with an IC50 value of 0.9 microM, and plantasioside (10) showed selective activity against the human colon cancer cell line (HCT-8) with an IC50 value of 3.4 microM.     

款冬花的化学成分

从款冬花（Tussilago farfara L.0中分离得到四个倍半萜类化合物和两个苯二甲酸酯类化合物，经光谱分析确定其中两个倍半萜类化合物为新结构，命名为款冬花酮（tussilagonone,1)和新款冬花内酯（neotussilagolactone,2）。由血小板活化因子（PAF）引起的血小板聚集实验结果表明，两个新化合物均有较强的抑制PAF活性。     

培美曲塞-磷脂偶联物修饰的靶向性舒尼替尼与长春瑞滨脂质体的研制及其在体外对耐药性乳腺癌的抑制效应

乳腺癌是女性最易罹患的疾病,而肿瘤多药耐药性通常是化疗失败的主要原因。本研究以培美曲塞（PMT）和DSPE-PEG2000-NH2为原料合成了新的靶向性偶联物DSPE—PEG2000．PMT,并将其修饰到脂质体表面,制备了同时包封有舒尼替尼与长春瑞滨的靶向性脂质体,以增强化疗药物对多药耐药性乳腺癌的治疗效果。经过质谱分析证实,合成的靶向性载体材料DSPE．PEG2000-PMT与目标产物相符。建立了可同时检测舒尼替尼和长春瑞滨含量的高效液相色谱分析方法,检测波长为215nm,柱温30℃,流动相为乙腈-0．05MKH2P04（pH3．5）-三乙胺（35：65：0．3,v／v／v）。舒尼替尼和长春瑞滨的最低检测浓度分别为25ng／mL和5ng／mL,最低定量浓度均为0．25μg／mL。两药在0．5-25．0μg／mL范围内线性良好。各脂质体包封率均大于90％,粒径均-（～90nm）,Zeta电位略显负电性。在体外耐药乳腺癌MCF-7／Adr细胞中评价了靶向性舒尼替尼与长春瑞滨脂质体的抗增殖效应。结果显示,同对照组相比,靶向性舒尼替尼与长春瑞滨脂质体对MCF-7／Adr细胞具有最强的抑制增殖效应。以靶向性香豆素脂质体为荧光探针,考察了靶向性脂质体在耐药乳腺癌MCF-7／Adr细胞中的靶向性,同非靶向性制剂相比,靶向脂质体在耐药性癌细胞中摄取最多。因此,制备的靶向性舒尼替尼与长春瑞滨脂质体是-种新的靶向制剂,能够被耐药乳腺癌细胞靶向性摄取,可在体外显著抑制耐药性乳腺癌生长,从而为耐药乳腺癌的化学治疗提供了-种新的策略。