钝叶水丝梨化学成分研究

自钝叶水丝梨(Sycopsis tutckerii Hemsl)树皮中得到二十一个化合物。经鉴定为豆甾烷-6α-羟基-3β-月桂酸酯(Ia);豆甾烷-6α-羟基3β-肉豆蔻酸酯(Ib);豆甾烷-6α-羟基-3β-棕榈酸酯(Ic);及其它两个豆甾烷-6α-羟基-3β-脂肪酸酯(Id、Ie,其酸部分结构待定);乙酰白桦脂酸甲酯(Ⅱa);乙酰白桦脂酸(Ⅱb);白桦脂酸甲酯(Ⅱc);白桦酯酸(Ⅱb);乙酰齐墩果酸(Ⅲa);齐墩果酸(Ⅲb);β-谷甾醇(Ⅳa);β-谷甾醇-β-D-葡萄糖甙(Ⅳb);3-O-甲基-鞣花酸-4'-α-L-鼠李糖甙(Ya);3-O-甲基鞣花酸(Vb);3,4-二-O-甲基鞣花酸(Vc);鞣花酸(Vd);(?)-茶儿茶素(Ⅵ);没食子酸(Ⅷa);原儿茶酸(Ⅷd);焦性没食子酚(Ⅶc)。其中Ia-Ie是一组尚未单离的新化合物。上述化令物,除( )-茶儿茶素外,均系首次从水丝梨属植物中发现。     

紫茎泽兰化学成分的研究（Ⅰ）

从云南紫茎泽兰(Eupatorium aclenophorum Spreng)茎、叶中分出10个化合物,经波谱(IR,MS,~1H-NMR,~(13)C-NMR)分别鉴定为9-oxo-ageraphorone(Ⅰ),9β-hydroxy-ager-aphorone(Ⅱ),表木栓醇(epifriedelinol,Ⅲ),豆甾醇(stigmasterol,Ⅳ),正二十八烷酸(octa-cosanoic acid,V),β-胡萝卜甙(β-daucosterol,Ⅵ),邻羟基桂皮酸(O-hydroxy cinnamic acid,Ⅶ),阿魏酸(ferulic acid,Ⅷ),咖啡酸(caffeic acid,Ⅸ),2-异丙烯基-5-乙酰基-6-羟基苯骈呋喃的乙酰化物(2-isopropenyl-5-acetyl-6-hydroxybenzofuran acetate,Ⅹ)。化合物(Ⅲ～Ⅹ)均系首次从该植物中分离到。     

云南普洱茶原料晒青毛茶的化学成分

从云南临沧地区生产普洱茶的原料晒青毛茶中分离到 2 1个化合物 ,通过波谱分析分别鉴定为 :(- )表儿茶素、 (- )表没食子儿茶素、 (- )表没食子儿茶素 - 3-O -没食子酸酯、 (- )表儿茶素 - 3-O -没食子酸酯、 (- )表阿福豆素 - 3-O -没食子酸酯、 ( )儿茶素、 (± )没食子儿茶素、槲皮素、槲皮素 - 3-O - β -D -葡萄吡喃糖甙、芦丁、山奈酚、山奈酚 - 3-O - β -D -葡萄吡喃糖甙、山奈酚 - 3-O -芦丁糖甙、小木麻黄素 (strictinin)、 1,6 -O -二没食子酰基 - β -D -葡萄吡喃糖、茶倍素、绿原酸、 3α ,5α -二羟基 - 4 -α -O -咖啡酰基金鸡纳酸、松柏醇甙、没食子酸和咖啡因     

万年蒿中两个新贝壳杉烷型二萜的分离与结构测定

自菊科蒿属植物万年蒿(Artemisia sacrorum Ledeb.)地上部分首次分得3个单体化合物(两个贝壳杉烷型二萜和一个酸性化合物),经理化常数测定及光谱分析(UV,IR,~1H-NMR,~(13)C-NMR,MS)鉴定其结构分别为3α,16α-二羟基贝壳杉烷-200-O-β-D-葡萄糖甙(Ⅰ)(3α,16α-dihydroxykaurane-20-O-β-D-glucoside(Ⅰ)),3α,6α-二羟基贝壳杉烷-19-O-β-D-葡萄糖甙(Ⅱ)(3α,16α-dihydroxykaurane-19-O-β-D-glucoside(Ⅱ))和1,4-二咖啡酰奎宁酸(Ⅲ)(1,4-dicaffeylquinic acid(Ⅲ))。(Ⅰ)和(Ⅱ)为两个未见报道的新化合物。     

狭叶香蒲花粉（蒲黄）中的亲脂性成分

从狭叶香蒲(Typha angustifolia L.)的干燥花粉中分离到5个化合物,经理化试验和波谱分析其中4个化合物的结构确定为7-甲基-4-三十烷酮(7-methyl-4-triacontanone,Ⅰ)、6-三十三烷醇(6-tritriacontanol,Ⅱ)、二十五烷(pentacosane,Ⅲ)和β-谷甾醇棕榈酸酯(β-sitosterol patmitate,Ⅳ),另外还分得一个化合物Ⅴ。Ⅳ是降低血清胆固醇的有效成分。Ⅰ、Ⅱ是新化合物。     

云南山楂果化学成分的研究

从云南山楂的果实中分得10个化物,经光谱分析及化学反应分别鉴定为槲皮素(Ⅰ)、芦丁(Ⅱ)、牡荆素(Ⅲ)、金丝挑甙(Ⅳ)、胡萝卜甙(Ⅴ)、熊果酸(Ⅵ)、氯原酸(Ⅶ)、奎宁酸(Ⅷ)、β-谷甾醇(Ⅺ)及二十九烷醇(Ⅹ)。     

药用植物灯笼草的化学成分研究

从药用植物灯笼草(Clinopvdium polycephalum)中分离鉴定了5个化合物。其中主要成分为乌索酸(ursolic acid,Ⅰ),其余4个分别鉴定为:异樱花素(isosakuranetin.Ⅱ),香蜂草甙(didymin,Ⅲ),6'-十六碳酸酯基-α-菠甾醇-3-O-β-D-葡萄糖甙(6’-Palmityl-α-spinasteryl-3-O-β-D-glucoside,Ⅳ a)和十八碳酸酯基-α-波甾醇-3-O-β-D-葡萄糖甙(6’-stearyl-α-spinasteryl-3-O-β-D-glucoside,Ⅳ b)。上述化合物在该植物中均为首次报道。     

■岗通城虎化学成分的研究(Ⅱ)

<正> (山弄)岗通城虎Aristolochia longgangensis C.F.Liang.在前文我们曾报导从其根中分得结晶性单体(Ⅰ—Ⅺ),其中四个(Ⅰ、Ⅱ、Ⅲ、Ⅳ)经鉴定为尿囊素(Allantion)、马兜铃酸(Aristolochic acid)、马兜铃酸C(Aristolochic acid C)和马兜铃内酰胺-β-D-葡萄糖甙(Aristololactam-β-D-glucoside)。本文报导另外三个化合物(Ⅶ、Ⅴ、Ⅸ)的鉴定,它们分别为马兜铃内酰胺AⅡ(Aristololactam AⅡ),朱砂莲内酰胺     

新疆鼠尾草的化学成分研究

从新疆鼠尾草（Salvia deserta Schang0根中分离得到8个单体成分,根据化学和光谱方法鉴定为：正三十三烷（Tritriacontane)[Ⅰ]、6,7－去氢罗列酮（6,7－SDehydroroyleanone)[Ⅱ],7,β-羟基罗列酮（Taxochinon）[Ⅲ]、二十六烷酸（Hexaconsanoic acid）[Ⅳ]、3－乙酰剂墩果酸（3－Acetoxy-oleanolic acid)[Ⅴ]、β－谷甾醇（β-Sitosterol)[Ⅵ]、熊果酸（Ursolic acid)[Ⅶ],D-甘露醇（Mannitolum）[Ⅷ]。     

枸骨的化学成分

从枸骨(Ilex cornuta Lindl,ex paxt.)中分离得到20个化合物,鉴定了16个,分别为：枸骨甙1(Gougusidel,V)即坡摸酸3-β-O-O-L吡喃阿拉伯糖甙;枸骨甙2(Gouguside 2,Ⅵ)即3-β-O-D-吡喃葡萄糖基坡摸酸-β-28-O-D吡喃葡萄糖酯;枸骨甙3(Gouguside 3,Ⅶ)即3-β-O-(β-D-吡喃葡萄糖基)-α-L吡喃葡萄糖基坡摸酸-β-28-O-D-吡喃葡萄糖酯的类似物;枸骨甙4(Gouguside 5,ⅩⅦ)即3-β-O-(β-D-吡喃葡萄糖基)-α-L-吡喃葡萄糖基坡摸酸-β-28-O-D-吡喃葡萄糖酯;枸骨甙5(Gouguside 5,ⅩⅧ)即坡摸酸3-β-O-α-L-2’-乙酰氧基吡喃阿拉伯糖基-28-O-β-D-吡喃葡萄糖酯,枸骨甙6(Gouguside 6,ⅩⅪ)即3-β-O-(β-D-吡喃葡萄糖基)-α-L-4-乙酰氧基吡喃阿拉伯糖基坡摸酸-β-28-O-D-吡喃葡萄糖酯;枸骨甙7(Gouguside 7,ⅩⅩ)即3-β-O-α-L-吡喃阿拉伯糖基-28-O-β-D-吡喃葡萄糖酯;胡萝卜甙(daucostorol Ⅷ);2,4-二羟基苯甲酸(2,4-dihydroxybenzoicacid I);3,4-二羟基桂皮酸(3,4-dihyroxycinnamunic acid Ⅱ,Ⅳ);长链脂肪酸或醇5个(Longchain fatty acid Ⅲ,Ⅵ,Ⅶ,Ⅷ,ⅩⅣ)。在鉴定的16个化合物中,枸骨甙1、枸骨甙2、枸骨甙6和枸骨甙7为首次从枸骨中分离得到,枸骨甙3和枸骨甙4为新化合物。     

NPC1L1:固醇脂质吸收的关键蛋白质

NPC1L1是最近发现的一种与NPC1同源的蛋白质。在体内的分布有物种差异性,其亚细胞定位存在很大争议。近些年发现NPC1L1在固醇类脂质代谢途径中起着重要作用,是肠道吸收固醇类脂质尤其是胆固醇的关键蛋白质,这项新发现使得人们对固醇类脂质的吸收机制有了了解。高胆固醇血症是心血管系统疾病的一个高危因子,因此,对NPC1L1的研究具有重大的实际意义,正逐渐成为研究的热点。     

Stoichiometry studies reveal functional properties of KDC1 in plant shaker potassium channels

Functional heteromeric plant Shaker potassium channels can be formed by the assembly of subunits from different tissues, as well as from diverse plant species. KDC1 (K(+) Daucus carota 1) produces inward-rectifying currents in Xenopus oocytes when coexpressed with KAT1 and other subunits appertaining to different plant Shaker subfamilies. Owing to the presence of KDC1, resulting heteromeric channels display slower activation kinetics, a shift of the activation threshold toward more negative membrane potentials and current potentiation upon the addition of external zinc. Despite available information on heteromerization of plant Shaker channels, very little is known to date on the properties of the various stoichiometric configurations formed by different subunits. To investigate the functional properties of heteromeric nKDC1/mKAT1 configurations, we realized a series of dimeric constructs combining KDC1 and KAT1 alpha-subunits. We found that homomeric channels, formed by monomeric or dimeric alpha-subunit constructs, show identical biophysical characteristics. Coinjections of diverse tandem constructs, instead, displayed significantly different currents proving that KDC1 has high affinity for KAT1 and participates in the formation of functional channels with at most two KDC1 subunits, whereas three KDC1 subunits prevented the formation of functional channels. This article brings a contribution to the understanding of the molecular mechanisms regulating plant Shaker channel functionality by association of modulatory subunits.     

Variation in salinity tolerance and shoot sodium accumulation in Arabidopsis ecotypes linked to differences in the natural expression levels of transporters involved in sodium transport

Salinity tolerance can be attributed to three different mechanisms: Na⁺ exclusion from the shoot, Na⁺ tissue tolerance and osmotic tolerance. Although several key ion channels and transporters involved in these processes are known, the variation in expression profiles and the effects of these proteins on Na⁺ transport in different accessions of the same species are unknown. Here, expression profiles of the genes AtHKT1;1, AtSOS1, AtNHX1 and AtAVP1 are determined in four ecotypes of Arabidopsis thaliana. Not only are these genes differentially regulated between ecotypes, the expression levels of the genes can be linked to the concentration of Na⁺ in the plant. An inverse relationship was found between AtSOS1 expression in the root and total plant Na⁺ accumulation, supporting a role for AtSOS1 in Na⁺ efflux from the plant. Similarly, ecotypes with high expression levels of AtHKT1;1 in the root had lower shoot Na⁺ concentrations, due to the hypothesized role of AtHKT1;1 in retrieval of Na⁺ from the transpiration stream. The inverse relationship between shoot Na⁺ concentration and salinity tolerance typical of most cereal crop plants was not demonstrated, but a positive relationship was found between salt tolerance and levels of AtAVP1 expression, which may be related to tissue tolerance.     

人骨髓间充质干细胞向神经细胞分化过程中Notch通路信号分子表达的变化

本研究探讨Noah信号通路在人骨髓间充质干细胞（human mesenchymal stem cells,hMSCs）体外增殖及向神经细胞分化过程中的作用。采集健康自愿者骨髓,体外培养获得hMSCs,取第3代hMSCs,在诱导剂（β-ME,DMSO,BHA）作用下向神经细胞分化。诱导后用免疫细胞化学鉴定神经元特异性烯醇化酶（neuron-specific enolase,NSE）和尼氏体的表达以确定诱导效果：用流式细胞术检测细胞生长周期时相的变化。在诱导前后,用免疫荧光和RT-PCR方法检测Notch通路中Notch1受体蛋白、配体Jagged1（JAG1）、调节蛋白活化相关物早老素1（presenilin 1,PS1）、靶基因hairy and enhancer of split1（HES1）信号分子表达的变化。结果显示：诱导前,处于G0/G1期的hMSCs占58．5％,S＋G2/M期的细胞占41．5％;诱导后,G0/G1期细胞比例升高,而S＋G2/M期细胞比例下降,NSE阳性细胞率达（77±0．35）％,细胞质中可见深蓝色的块状或颗粒状尼氏体。免疫荧光显示,诱导前后hMSCs内Notch1和JAG1均呈阳性表达,但RT-PCR检测发现诱导后Notch1、JAG1、PSl和HES1 mRNA表达量较诱导前明显降低（均P〈0．05）。结果表明,诱导hMSCs向神经细胞分化能抑制Notch信号分子表达,低水平的Notch信号激活可能有利于神经细胞的分化。     

Carboxamide SIRT1 inhibitors block DBC1 binding via an acetylation-independent mechanism

SIRT1 is an NAD⁺-dependent deacetylase that counteracts multiple disease states associated with aging and may underlie some of the health benefits of calorie restriction. Understanding how SIRT1 is regulated in vivo could therefore lead to new strategies to treat age-related diseases. SIRT1 forms a stable complex with DBC1, an endogenous inhibitor. Little is known regarding the biochemical nature of SIRT1-DBC1 complex formation, how it is regulated and whether or not it is possible to block this interaction pharmacologically. In this study, we show that critical residues within the catalytic core of SIRT1 mediate binding to DBC1 via its N-terminal region, and that several carboxamide SIRT1 inhibitors, including EX-527, can completely block this interaction. We identify two acetylation sites on DBC1 that regulate its ability to bind SIRT1 and suppress its activity. Furthermore, we show that DBC1 itself is a substrate for SIRT1. Surprisingly, the effect of EX-527 on SIRT1-DBC1 binding is independent of DBC1 acetylation. Together, these data show that protein acetylation serves as an endogenous regulatory mechanism for SIRT1-DBC1 binding and illuminate a new path to developing small-molecule modulators of SIRT1.     

Enhancement of hepatic microsomal drug oxidation and glucuronidation in rat by 1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane (DDT)

A single dose of 1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane (DDT) (160 mg/kg i.p.) enhanced the monooxygenase step of drug biotransformation in rat liver. The O-demethylation of p-nitroanisole was especially increased, a peak in activity approximately 5-fold compared with controls being attained in 7 days. On the other hand, there was only a 2-fold increase in aryl hydrocarbon hydroxylase activity.DDT increased the cytochrome P-450 content of the liver, this increase coincided well with that in p-nitroanisole O-demethylation activity.The UDPglucuronosyltransferase activity of liver microsomes was not enhanced by DDT administration, unless the microsomes were pretreated to reveal latent activity prior to assay. After trypsin digestion of microsomes a maximum increase in activity of approximately 3-fold was observed as a result of DDT dosage. The canonic surfactant cetylpyridinium chloride was less active in revealing the latent UDP-glucuronosyltransferase activity, and two other membrane perturbants, the detergent digitonin and phospholipase A, were unable to show enhancement in UDPglucuronosyltransferase as a result of DDT dosage.     

达菲药物对H1N1病毒作用研究

甲型H1N1病毒在全世界范围内爆发,引起人们广泛关注,而目前疫苗和新的药物正处于研发阶段,与此同时该病毒神经氨酸酶蛋白序列不断被报道。达菲作为治疗H1N1病毒的药物被患者广泛使用。通过同源性建模的方法比较神经氨酸酶的变异情况,从而预测达菲药物对变异前后的作用效果评价。通过AUTODOCK计算结合能,发现达菲药物与神经氨酸酶的结合能维持在2.4～4.2 kJ/mol范围内,动力学常数最高值达到18.2 mM。证明达菲药物对抑制病毒进入寄主细胞有明显效果。     

细胞色素P450 1A1基因多态性与我国某些肿瘤遗传易感性

近年来有关细胞色素P450基因多态性与肿瘤遗传易感性的研究正日益吸引越来越多的关注,本文对我国近年来有关细胞色素P450 1A1(CYP1Al)基因多态性与几种肿瘤遗传易感性的研究进行探讨,推测我国几种高发病率肿瘤的发生与我国CYP1A1基因多态分布状况有关,以此为进一步研究CYP1A1与肿瘤的关系作参考。