灯台七化学成分及抗癌活性研究

目的研究灯台七化学成分及抗癌活性。方法采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、半制备高效液相色谱等方法分离纯化,理化性质及现代波谱技术鉴定其结构。通过MTT法评价化合物4~8的抗癌活性。结果共分离鉴定了8个化合物,分别为β-蜕皮激素(1)、pinnatasterone(2)、豆甾醇(3)、豆甾醇-3-O-β-D-吡喃葡萄糖苷(4)、偏诺皂苷元3-O-α-L-鼠李吡喃糖(l→2)[α-L-阿拉伯呋喃糖(1→4)]-β-D-葡萄吡喃糖苷(5)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖(l→4)α-L-鼠李吡喃糖(1→4)-[α-L-鼠李吡喃糖(l→2)]-β-D葡萄吡喃糖苷(6)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖(l→4)-[α-L-鼠李吡喃糖基(1→2)]-β-D-葡萄糖苷(7)、偏诺皂苷元-3-O-α-L-鼠李吡喃糖基(l→4)-[α-L-鼠李吡喃糖基(1→4)]-β-D-葡萄糖苷(8)。化合物5~8对结肠癌SW620和HT-29细胞有显著的抑制作用。结论化合物5~8均表现出很强的细胞毒活性。     

薯蓣属植物化学成分的研究——Ⅱ.叉蕊薯蓣中甾体皂甙的分离和鉴定

从叉蕊薯蓣(D.collettii HooK.f.)根茎的乙醇提取物分离到四个甾体皂甙,根据理化性质、光谱数据,推定化学结构为3-O-(β-D-葡萄吡喃糖)-约莫皂甙元(3-O-(β-D-glucopyranosyl)-yamogenin)[Ⅰ];3-O-[α-L-鼠李吡喃糖(1→4)-β-D-葡萄吡喃糖]-约莫皂甙元(3-O-[α-L-rahmnopyranosyl(1→4)-β-D-glucopyranosyl]-yamogenin)[Ⅱ];3-O-{α-L-鼠李吡喃糖(1→4)-[α-L-鼠李吡喃糖(1→2)]-β-D-葡萄吡喃糖}-约莫皂甙元(3-O-{α-L-rhamnopyranosyl(1→4)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopranosyl}-yamogenin)[Ⅲ];3-O-{β-D-葡萄吡喃糖(1→3)-[α-L-鼠李吡喃糖(1→2)3-β-D-葡萄吡喃糖}-约莫皂甙元(3-O-{β-D-glucopyranosyl(1→3)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl}-yamogenin)[Ⅳ]。其中Ⅰ为已知物,Ⅱ、Ⅲ、Ⅳ为首次从植物界得到的新甾体皂甙。     

黄花败酱中三萜皂苷类成分的分离鉴定

目的 研究黄花败酱中的化学成分.方法 将黄花败酱全草的乙醇提取物经大孔树脂、硅胶、ODS柱分离得到6个化合物,通过(1H、13CNMR、ESI-MS等分析和化学方法进行结构鉴定.结果 6个化合物分别被鉴定为3-O-β-D-吡喃木糖-(1→3)-α-L-吡喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖-常春藤皂苷元-28-O-β-D-吡喃葡萄糖(6→1)-β-D-吡喃葡萄糖-(4→1)-α-L-吡喃鼠李糖酯苷(Ⅰ)、3-O-β-D-α-L-吡喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖-常春藤皂苷元-28-O-β-D-吡喃葡萄糖(6→1)-β-D-吡喃葡萄糖-(4→1)-α-L-吡喃鼠李糖酯苷 (Ⅱ)、齐墩果酸-3-α-L-吡喃阿拉伯糖-(2→1)-α-L-吡喃鼠李糖-(3→1)-O-β-D-吡喃木糖苷(Ⅲ)、3-O-β-D-吡喃木糖-(1→3)-α-L-吡喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖-齐墩果酸-28-O-β-D-吡喃葡萄糖酯苷 (Ⅳ)、齐墩果酸-3-O-β-D-吡喃木糖-(2→1)-α-L-吡喃鼠李糖苷(Ⅴ)、常春藤皂苷元-3-O-α-L-吡喃阿拉伯糖-(2→1)-α-L-吡喃鼠李糖苷 (Ⅵ).结论 化合物Ⅳ为一个新的天然产物,化合物Ⅰ和Ⅲ为首次从该植物中分离得到.     

刺五加叶中黄酮类成分的分离与鉴定

目的分离、鉴定刺五加叶提取物中的化学成分。方法采用硅胶柱、ODS开放柱和制备液相等色谱方法分离,并通过NMR和MS等谱学技术确定结构。结果从提取物中分离得到9个黄酮类化合物,分别鉴定为异鼠李素-3-O-刺槐二糖苷(isorhamnetin-3-O-robinobioside,1)、山柰酚-3-O-刺槐二糖苷(kaempferol-3-O-robinobioside,2)、金丝桃苷(hyperin,3)、异鼠李素-3-O-β-D-半乳糖苷(isorhamnetin-3-O-β-D-galactopyranoside,4)、异鼠李素-3-O-β-D-鼠李糖基-(1→6)-[α-L-鼠李糖基-(1→2)]-β-D-半乳糖苷(isorhamnetin-3-O-α-L-rhamnopyranosyl-(1→6)-[α-L-rhamnopyranosyl-(1→2)]-β-D-galactopyr-anosid,5)、山柰酚-3-O-α-L-鼠李糖基-(1→2)-β-D-葡萄糖苷(kaempferol-3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside,6)、槲皮素-3-O-α-L-阿拉伯糖基-(1→2)-β-D-半乳糖苷(quercetin-3-O-α-L-arabinopyaranosyl-(1→2)-β-D-ga-lactopyranoside,7)、槲皮素(quercetin,8)山柰酚(kaempferol,9)。其中化合物1、2、4-7为首次从五加属植物中分离得到。结论     

薯蓣属植物化学成分的研究——Ⅱ.叉蕊薯蓣中甾体皂甙的分离和鉴定

从叉蕊薯蓣(D.collettii HooK.f.)根茎的乙醇提取物分离到四个甾体皂甙,根据理化性质、光谱数据,推定化学结构为3-O-(β-D-葡萄吡喃糖)-约莫皂甙元(3-O-(β-D-glucopyranosyl)-yamogenin)[Ⅰ];3-O-[α-L-鼠李吡喃糖(1→4)-β-D-葡萄吡喃糖]-约莫皂甙元(3-O-[α-L-rahmnopyranosyl(1→4)-β-D-glucopyranosyl]-yamogenin)[Ⅱ];3-O-{α-L-鼠李吡喃糖(1→4)-[α-L-鼠李吡喃糖(1→2)]-β-D-葡萄吡喃糖}-约莫皂甙元(3-O-{α-L-rhamnopyranosyl(1→4)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopranosyl}-yamogenin)[Ⅲ];3-O-{β-D-葡萄吡喃糖(1→3)-[α-L-鼠李吡喃糖(1→2)3-β-D-葡萄吡喃糖}-约莫皂甙元(3-O-{β-D-glucopyranosyl(1→3)-[α-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl}-yamogenin)[Ⅳ]。其中Ⅰ为已知物,Ⅱ、Ⅲ、Ⅳ为首次从植物界得到的新甾体皂甙。     

噬琼胶卵链菌β-琼胶酶基因YM01-5的克隆表达及其酶学性质的研究

目的 从青岛近海海水中分离鉴定了1株能够降解琼胶的海洋新菌—嗜琼胶卵链菌（Catenovulumagarivoransgen. nov. sp. nov.）YM01T,并对其进行了全基因组测序。本文对该菌的1个β-琼胶酶基因YM01-5进行了克隆表达,并对重组琼胶酶的酶学性质进行了研究。方法 利用镍柱亲和层析对重组琼胶酶进行了分离纯化,采用DNS法测定重组酶的酶学性质,薄层层析(TLC)和质谱(MS)法对AgaYM01-5的酶解产物进行分析。结果 β-琼胶酶基因YM01-5全长2 412 bp,编码803个氨基酸,预测分子量为91.6 kDa,其催化模块属于糖苷水解酶GH50家族。重组琼胶酶YM01-5酶学性质的研究结果表明,该酶的最适温度为40 ℃,最适pH为9.0。在35 ℃以下具有良好的热稳定性,pH 6～10之间保持较高的稳定性,在该范围的pH缓冲液中放置12 h后,YM01-5仍能保持80%以上的酶活力。此外,该重组琼胶酶降解琼脂糖的Km、Vmax值分别为15.6 mg/mL和188 U/mg, 对降解产物的薄层层析及质谱分析结果表明,β-琼胶酶基因YM01-5以外切酶的形式作用于琼脂糖产生新琼二糖作为终产物。结论 该酶降解产物单一,有利于琼胶寡糖的制备,具有较高的工业应用潜力,它的发现也为研究菌株YM01中琼脂糖的代谢通路提供了参考。     

具有网状内皮系统活性的几种中药多糖的研究

从几种中药的热水提取物中分离到11种多糖,它们能显著增强网状内皮系统(RES)的活力。这些多糖对RES的作用是用改良的ICR-SPF雄性小鼠体内碳廓清试验证明的。用化学和光谱方法阐明了这些免疫活性多糖的结构特征。从防风(Saposknikovia divaricata)根和根茎中分到防风多糖A、B、C(saposknikovans A、B、C)。多糖A的主链为α-1→4-D-聚半乳糖醛酸,侧链为α-1→5-L-阿拉伯糖-β-3,6-分支D-半乳聚糖,多糖C则具有果胶样聚鼠李糖半乳糖醛酸主链和α-3,5-分支-L-阿拉伯聚糖和β-3.4-分支-D-半乳聚糖。从冬葵(Malva verticillata)中分得一中性     

瘤果黑种草子的化学成分

目的研究中药瘤果黑种草子的化学成分。方法运用多种色谱方法分离化学成分;依据这些化学成分的理化性质和波谱(NMR、EI-MS)数据分析鉴定化合物的结构。结果从瘤果黑种草子中初步分离得到5个化合物,分别鉴定为胡萝卜苷(1)、常春藤皂苷元-3-O-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖苷(2)、常春藤皂苷元-3-O-β-D-吡喃木糖基-(1→3)-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖苷(3)、3-O-β-D-吡喃木糖基-(1→3)-α-L-吡喃鼠李糖基-(1→2)-α-L-吡喃阿拉伯糖常春藤皂苷元-28-O-β-D-吡喃葡萄糖酯苷(4)、山奈酚-3-O-β-D-吡喃葡萄糖基-(1→2)-β-D-吡喃半乳糖基-(1→2)-β-D-吡喃葡萄糖苷(5)。结论化合物4为首次从黑种草属植物中分离得到,化合物5为首次从该种植物中分离得到。     

川续断中皂甙Ⅺ,Ⅻ和ⅩⅢ的结构研究

从川续断(Dipsacus asper Wall.)根的醇提物中得到三个微量新三萜皂甙(Ⅺ～ⅫⅠ),根据光谱分析和化学反应,其结构分别鉴定为3-O-[β-D-吡喃葡萄糖(1→4)][α-L-吡喃鼠李糖(1→3)]-β-D-吡喃葡萄糖(1→3)-α-L-吡喃鼠李糖(1→2)-α-L-吡喃阿拉伯糖-常春藤皂甙元(Ⅺ)、Ⅺ的28-O-β-D-吡喃葡萄糖(1→6)-β-D-吡喃葡萄糖酯甙( Ⅻ)和3-O-[β-D-吡喃木糖(1→4)-B-O-吡喃葡萄糖(1→4)][α-L-吡喃鼠李糖(1→3)]-B-D-吡喃葡萄糖(1→3)-α-L-吡喃鼠李糖(1→2)-α-L-吡喃阿拉伯糖-齐墩果酸-28-O-β-吡喃葡萄糖(1→6)-β-D-吡喃葡萄糖酯甙(ⅫⅠ)。     

人参化学成分的研究 第Ⅱ报人参皂甙B的结构鉴定

从辽宁产的人参(Panax ginseng C A Mey:)根中分离得到的人参皂甙 B,经化学及光谱分析,其结构鉴定为20 S—原人参三醇-6-[0-α-L-鼠李吡喃糖基(1→2)-β-D-葡萄吡喃糖甙]-20-0-β-D-葡萄吡喃糖甙(Ⅰ)。即与 Syuichi Sanada 等人提出的人参皂甙 Re 的结构一致。     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

Emerging drugs for epilepsy

Epilepsy affects ≤ 1% of the world's population. Antiepileptic drugs (AEDs) are the mainstay of treatment, although more than a third of patients are not rendered seizure free with existing medications. Uncontrolled epilepsy is associated with increased mortality and physical injuries, and a range of psychosocial morbidities, posing a substantial economic burden on individuals and society. Limitations of the present AEDs include suboptimal efficacy and their association with a host of adverse reactions. Continued efforts are being made in drug development to overcome these shortcomings employing a range of strategies, including modification of the structure of existing drugs, targeting novel molecular substrates and non-mechanism-based drug screening of compounds in traditional and newer animal models. This article reviews the need for new treatments and discusses some of the emerging compounds that have entered clinical development. The ultimate goal is to develop novel agents that can prevent the occurrence of seizures and the progression of epilepsy in at risk individuals.     

盐酸达泊西汀中甲磺酸甲酯、甲磺酸乙酯及甲磺酸异丙酯的顶空毛细管GC-ECD法测定

建立了衍生化顶空毛细管气相色谱-电子捕获检测器(ECD)法测定盐酸达泊西汀中的甲磺酸甲酯(MMS)、甲磺酸乙酯(EMS)和甲磺酸异丙酯(IMS).应用碘化钠衍生技术,使用PW-5毛细管柱,载气为氮气,ECD检测,程序升温.MMS、EMS和IMS分别在0.03～0.30、0.05～0.50和0.05～0.50 μg/ml浓度范围内线性关系良好,平均回收率分别为63.5％、100.3％和96.2％,最低检测限分别为0.30、0.50和0.50 ng/ml.     

血管内皮生长因子的异常与子(癎)前期发病的关系

目的:研究血浆可溶性细胞间黏附分子-1(sICAM-1)浓度和胎盘组织血管内皮生长因子(VEGF)、胎盘生长因子(PLGF)及其血管内皮生长因子受体1(VEGFR1,Flt-1)、可溶性血管内皮生长因子受体1(sVEGFR1,sFlt-1)mRNA的表达与子前期的关系.方法:采用酶联免疫吸附测定法(ELISA)检测45例子前期患者和45例健康产妇血清sICAM-1的浓度,逆转录-聚合酶链反应(RT-PCR)方法检测胎盘组织中VEGF、PLGF、Flt-1、sFlt-1 mRNA的表达.结果:(1)子前期组sICAM-1水平为(218.45±29.93) μg/L,显著高于对照组的(168.84±19.39) μg/L(P < 0.01).(2)子前期患者胎盘组织VEGF、PLGF、Flt-1、sFlt-1 mRNA的相对表达量显著高于对照组(均P < 0.01).(3)血清sICAM-1浓度与胎盘组织中sFlt-1mRNA的相对表达量呈正相关(r = 0.90,P < 0.01).结论:子前期患者血清sICAM-1浓度升高,其胎盘组织VEGF、PLGF、Flt-1、sFlt-1 mRNA的相对表达量也升高.胎盘组织sFlt-1mRNA的高表达与子前期内皮损伤等有密切关系.     

Antiparasitic protozoan vaccines

Parasitic infections caused by pathogenic protozoa affect over 1 billion people worldwide and impose a substantial health and economic burden, particularly on inter-tropical less-developed countries where they are more prevalent. Despite encouraging progress in vaccine development, chemotherapy remains the single most effective, efficient and inexpensive means to control most parasitic infections [1]. However, day to day parasites are becoming increasingly resistant to drugs currently in use, such as Plasmodium towards chloroquine, lending to the start of a promising future for vaccines. Patent applications regarding vaccines for the prevention, control and diagnosis of parasitic protozoan infections are reviewed for the period December 1996 - October 2000. However, vaccines for some of the protozoan infections do not appear in the literature in the period reviewed; only, vaccines against malaria, leishmaniasis, trypanosomiasis, cryptosporidiosis, pneumocystosis, eimeriosis, toxoplasmosis and neosporosis, as well as Babesia microti infections have been found.     

Binding affinity in drug design: experimental and computational techniques

ABSTRACT

Introduction: In pharmaceutical design where future drugs are developed by targeting a specific chosen protein, the evaluation of ligand affinity is crucial. For this very purpose are a multitude of diverse methods which are continuously being improved, which, in turn, makes it difficult to choose which techniques to use in practice.

Areas covered: In this review, the authors discuss both experimental and computational approaches for affinity evaluation. Basic principles, general limitations and advantages, as well as main areas of application in drug discovery, are overviewed for some of the most popular ligand binding assays. The authors further provide a guide to affinity predictions, collectively covering several techniques that are used in the first stages of rational drug design.

Expert opinion: All affinity estimation methods have limitations and advantages that partially overlap and complement one another. Some of the suggested best practices include cross-verification of data using at least two different techniques and careful data interpretation.