麦冬中几种二氢高异黄酮的立体结构

目的研究麦冬中几种二氢高异黄酮的立体结构。方法采用光谱方法,并用圆二色谱确定立体结构。结果确定6个二氢高异黄酮的立体结构,鉴定结果为:5,7-d ihydroxy-6-m ethyl-8-m ethoxy-3(R)-(2-′hydroxy-4′-m ethoxy-benzyl)chroman-4-one(Ⅰa);5,7-d ihydroxy-6-methyl-8-methoxy-3(S)-(2′-hydroxy-4′-methoxybenzyl)chroman-4-one(Ⅰb);5,7-d ihydroxy-6,8-d im ethyl-3(R)-(3-′m ethoxy-4-′hydroxybenzyl)chrom an-4-one(Ⅱa);5,7-d ihydroxy-6,8-d im ethyl-3(S)-(3′-m ethoxy-4′-hydroxybenzyl)chrom an-4-one(Ⅱb);R-m ethyloph iopogonanone B(Ⅲ)和R-m ethyloph iopogonanone A(Ⅳ)。结论首次确定了6个二氢高异黄酮(Ⅰ~Ⅳ)的立体构型。     

麦冬中新成分二氢高异黄酮的研究

目的研究麦冬的化学成分。方法运用多种色谱方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构。结果从麦冬80%乙醇提取物的乙酸乙酯萃取部分中分得3个化合物,分别鉴定为:5,7-dihydroxy-6,8-dimethyl-3-(3’,4’-dihydroxybenzyl)chroman-4-one(Ⅰ)、5,7-dihydroxy-3-(4’-hydroxybenzyl)chromone(Ⅱ)和5,7-dihydroxy-6,8-dimethyl-3-(4’-dihydroxy-2’,6’-dimethoxybenzyl)chroman-4-one(Ⅲ)。结论化合物I为一个新的高异黄酮类化合物,化合物Ⅱ为首次从麦冬中分离得到。     

鹰爪种子化学成分的研究

目的研究药用植物鹰爪Artabotrys hexapetalus (L.f.)Bhandari的化学成分。方法利用各种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据进行结构鉴定。结果从鹰爪种子分得4种木脂素:异洋商陆素A(isoamericaninA,1)、异洋商陆醇A(isoamericaninolA,2)、洋商陆素B(americaninB,3)、鹰爪木脂醇(artabotrycinol,4),以及(R)-鹰爪三醇［(R)-artabotriol,5］、棕榈酸(6)、β-谷甾醇(7)和胡萝卜苷(8)等。结论鹰爪木脂醇(4)和鹰爪三醇(5)为新化合物,其余3种木脂素为首次从该植物分得。     

麦冬中高异黄酮的分离与鉴定

从浙江产麦冬(Ophiopogon japonicus(Thunb)Ker-Gawl)的块根中分离出5个高异黄酮。通过理化性质和光谱分析鉴定了结构,其中3个是文献已报道的高异黄烷酮,即6-醛基异麦冬黄烷酮A(晶Ⅰ,6-aldehydo-isoophiopogonanone A),甲基麦冬黄烷酮B(晶Ⅱ,methylophiopogonanone B),甲基麦冬黄烷酮A(晶Ⅲ,methylophiopogonanone A),2个是新的高异黄酮,命名为6-醛基异麦冬黄酮B(晶Ⅳ,6-aldehydo-isoophiopogonone B)和6-醛基异麦冬黄酮A(晶Ⅴ,6-aldehydo-isoophiopogonone A)。     

红花锦鸡儿地上部分抗HIV化学成分的研究

为了研究红花锦鸡儿(Caragana rosea)地上部分的化学成分，寻找具有抗HIV作用的药用成分。在抗HIV生物活性指导下，利用色谱技术进行分离纯化，从红花锦鸡儿地上部分的乙酸乙酯提取部位分得5个化合物，根据理化性质和波谱技术进行结构鉴定，分别鉴定为myricetin(1)，mearnsetin(2)，对羟基桂皮酸(3)，cararosinol A(4)，cararosinol B(5)，并推测了cararosinol B与该植物中发现的另一白藜芦醇四聚体kobophenol A的转化关系。化合物4和5为新的白藜芦醇四聚体，化合物1～3为首次从该植物中分得。上述化合物体外均无明显的抑制HIV作用。     

从绵毛白花苋中分得铁屎米酮和β-咔啉类生物碱

苋科绵毛白毛苋Aerva lanata是印度的一种常见的观赏植物,其水提取物有利尿作用。早期,有人曾从其乙醚提取物中分得3个甾体化合物。作者以前也曾报道过4个黄酮β-番豆基葡萄糖甙、2个阿魏酰胺和其它酚类化合物的分离。文本报道从其全草中分得6种生物碱(Ⅰ～Ⅵ)和化合物Ⅱ、Ⅲ、Ⅳ、Ⅵ的结构鉴定。铁屎酮类生物碱Ⅱ、Ⅲ、和Ⅳ从该植物的根中分得,但β-咔啉类生物碱V和Ⅵ在根中没有分到。其中,铁屎米酮(1)和β     

石虎化学成分研究

目的　研究药用植物石虎(Evodiarutaecarpa (Juss.)Benth .var.officinalis (Dode)Huang)的化学成分。方法利用各种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据进行结构鉴定。结果　从石虎中分得多个化合物,本文主要报道石虎柠檬素A(R and S ,1)、大黄酚(chrysophanol,2 )、大黄素(emodin ,3)、大黄素甲醚(physcion ,4)和已知柠檬素(limonin ,5 )等化合物。结论　石虎柠檬素A(R and S)为新化合物,结构鉴定为21(R and S)-羟基-23-羰基-20-烯-柠檬素[21(R and S)-OH-23-oxo-20-en-limonin],化合物2 - 4等蒽醌类化合物为从吴茱萸属中首次获得     

仙茅补肾壮阳有效成分的初步研究及仙茅素A的含量测定

目的 初步研究仙茅补肾壮阳的有效成分,并测定其有效成分仙茅素A的含量.方法 采用大孔吸附树脂及反复常压硅胶柱层析分离纯化仙茅乙醇提取物,根据化合物的理化性质和光谱数据进行结构鉴定;采用HPLC法测定药材中仙茅素A的含量,色谱柱为Agilent C18(150 mm×4.6 mm,5 μm),流动相为乙腈-1%磷酸(21:79),流速1.0 ml·min-1,检测波长285 nm.结果 从仙茅中分得4个已知化合物,分别为仙茅苷、仙茅苷乙、仙茅素A及2,6-二甲氧基苯甲酸;仙茅索A的含量为0.0084%.结论 所用方法简便、可靠,可用于仙茅药材的质量控制.     

马兜铃酸的倍半萜的酯类化合物VI.绵毛马兜铃中马兜铃酸萜酯I的结构鉴定

从绵毛马兜铃(Aristolocha mannisima Hance)中分得一个马兜铃酸倍半萜的酯类化合物,经红外、紫外、高分辩质谱和多种一维和二维核磁共振谱鉴定,确定了其骨架结构及顺反构型,命名为马兜铃酸萜酯I。     

麦冬研究进展

本文综述了近年来对麦冬类植物研究的进展。从该类植物中分得45种皂甙和21种高异黄酮。麦冬为常用滋阴中药,对心血管系统疾病有一定的疗效。该类植物在我国分布广泛,资源丰富,但开发利用尚有限。     

HPLC法测定麦冬中沿阶草酮甲的含量

目的:建立测定麦冬中沿阶草酮甲的高效液相色谱法。方法:色谱柱:Hypersil C18柱(150mm×4.6mm,5μm);流动相:甲醇-水(75∶25);流速1.0mL/min;检测波长298nm。结果:沿阶草酮甲进样量在0.918～5.508μg范围内与峰面积线性关系良好,回归方程Y=3645282X-420010(r=0.99976),平均回收率为99.80%,RSD=1.74%(n=6)。结论:所建立的高效液相色谱法简便、快速、重复性好,可用于麦冬中沿阶草酮甲的质量控制。     

Adenosine and its receptors as therapeutic targets: An overview

The main goal of the authors is to present an overview of adenosine and its receptors, which are G-protein coupled receptors. The four known adenosine receptor subtypes are discussed along with the therapeutic potential indicating that these receptors can serve as targets for various dreadful diseases.     

Orientation of oxazolidinones in the active site of monoamine oxidase

Oxazolidinone inhibitors of monoamine oxidase (MAO) and oxazolidinone antibacterials are two distinct classes of drug, often with linear structures and overlapping activities for some derivatives. By synthesizing novel dimerised derivatives with identical substitution of the two C-5 side chains, we have obtained experimental evidence for the orientation of oxazolidinones in the active site of MAO A. Two types of spectral changes, either increasing the absorbance at 510 nm or decreasing it at 495 nm depending on the group nearest to the flavin cofactor, were seen on ligand binding to MAO A. Side chain derivatives with amine substituents are very poor substrates so that it was possible to examine the spectral change due to binding of a substrate before reduction of the flavin occurred. Binding of these amino derivative substrates to MAO A induced a spectral change characterized by a strong decrease in absorbance at 495 nm. These substrates reduced the enzyme fully without any trace of a semiquinone intermediate. Only oxazolidinone inhibitors with a bromo-imidazole substituent increased the yield of semiquinone intermediate obtained during chemical reduction. In accord with the experimental data, results of docking experiments showed that binding of the oxazolidinone ring in the aromatic cage close to the flavin was favored and that the nitrogen of the derivatives that were substrates was within van der Waals distance of N-5 of the flavin.     

国产乌头类生药草乌类的形态组织学研究(续)

根部的性状与显微特征12.工布乌头Aconitum kongboense 材料来源西藏。性状特征呈圆锥形或长圆柱形;长4～9 cm,直径0.5～3.0 cm;表面深棕色至棕褐色,全体皱缩有深皱摺及少数须根痕如顶角。质坚硬难折断,断面乳白色或淡棕色,稍有粉性,可见散列的棕色小圈状中柱(图3;12)。显微特征根横切面观察,后生皮层为3～4列棕色细胞;皮层细胞6～7列呈不规则长条形,切向排列;内有石细胞多数,呈长条形、卵圆形、或菱形,长38～160μm,直径25～     

北极蒿与中药常用蒿属植物的化学成分比较

目的比较北极蒿与三种中药常用蒿属植物的化学成分并对北极蒿的化学成分进行初步研究。方法采用薄层色谱及GC-MS比较小极性成分及挥发油的区别;采用HPLC指纹图谱对极性较大成分进行比较。结论从北极蒿挥发油中分离出52个色谱峰,共鉴定了48个成分,占挥发油总成分的92%以上,其主要成分为香木兰烷-4-醇（24.73%）。经HPLC指纹图谱分析,北极蒿与其他三种植物主要成分相似,但北极蒿的化学成分集中且含量高。青蒿、北极蒿、艾叶、茵陈中绿原酸含量分别是0.065%,0.617%,0.178%,0.192%,北极蒿中绿原酸含量是其它三种植物的六倍之多,提示有较高研究价值。     

Regional differences in the adenosine A(2) receptor-mediated modulation of contractions in rat vas deferens

Adenosine receptors involved in modulation of contractions were characterized in the bisected rat vas deferens by combining pharmacological and immunohistochemical approaches. In both portions, noradrenaline-elicited contractions were enhanced by the adenosine A₁ receptor agonist N⁶-cyclopentyladenosine (CPA), and inhibited by the non-selective adenosine receptor agonist 5′-N-ethylcarboxamidoadenosine (NECA) in the presence of the adenosine A₁ receptor antagonist 1,3-dipropyl-8-cyclopentyl-l,3-dipropylxanthine (DPCPX). The adenosine A_2A receptor agonist 2-p-(2-carboxyethyl)phenethyl-amino-5′-N-ethylcarboxamidoadenosine (CGS 21680) also inhibited noradrenaline-elicited contractions but only in the prostatic portion. Contractions elicited by the stable ATP analogue ,β-methyleneATP (,β-MeATP) were inhibited only by NECA in the presence of DPCPX and only in the prostatic portion. This study provides functional evidence for the presence, in both portions of the rat vas deferens, of an adenosine A₁ receptor-mediated enhancement and of an adenosine A₂ receptor-mediated inhibition of contractions. The latter effect is mediated by both A_2A and A_2B subtypes in the prostatic portion but only by the A_2B subtype in the epididymal portion. This regional variation is supported by the immunohistochemical results that revealed an adenosine A_2A receptor immunoreactivity not co-localized with nerve fibres more abundant in the prostatic than in the epididymal portion.     

儿童全血环孢素A浓度监测结果分析

目的为环孢素A用于儿童疾病的个体化治疗提供依据。方法运用回顾性调查方法,对广州市儿童医院自2006年～2008年共134例次儿童患者应用免疫抑制药全血环孢素A的浓度监测结果进行分析。结果浓度在〈75ng·mL-1的有50例次,75～200ng·mL-1的有52例次,200～400ng·mL-1的有24例次,〉400ng·mL-1的有8例次。结论大部分患儿全血环孢素A的浓度监测的结果都在经验参考范围以内,实行浓度监测对调整用药剂量具有指导意义;实施个体化给药是确保临床治疗效果和用药安全的重要措施之一。     

高效液相色谱法测定丹参舒心胶囊中丹参酮Ⅱ_A的含量

目的:建立以高效液相色谱法测定丹参舒心胶囊中丹参酮ⅡA含量的方法。方法:色谱柱为Shim-PackCLC-ODS,流动相为甲醇-水(15∶5),检测波长为270nm,柱温为40℃,流速为1.5ml/min。结果:丹参酮ⅡA检测浓度在0.05125～0.25625μg/ml范围内线性关系良好(r=0.9996,n=5),平均加样回收率为99.05%(RSD=0.92%)。结论:本方法操作简便、精密度好、结果可靠,可用于丹参舒心胶囊的质量控制。     

Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present)

Introduction: The cyclic nucleotides cAMP and cGMP are ubiquitous intracellular second messengers regulating a large variety of biological processes. The intracellular concentration of these biologically relevant molecules is modulated by the activity of phosphodiesterases (PDEs), a class of enzymes that is grouped in 11 families. The expression of PDEs is tissue- and cell-specific allowing spatiotemporal integration of multiple signaling cascades. PDE2A is a dual substrate enzyme and is expressed in both the periphery and in the central nervous system, however its expression is highest in the brain, where it is mainly localized in the cortex, hippocampus, and striatum. This suggests that this enzyme may regulate intraneuronal cGMP and cAMP levels in brain areas involved in emotion, perception, concentration, learning and memory.

Areas covered: This review covers the patent applications published between January 2010 and February 2016 on phosphodiesterase 2A inhibitors.

Expert opinion: Recent publications in the literature and in filed patent applications demonstrate the interest of pharmaceutical companies for PDE2A. This has increased the insights of its possible therapeutic role but the few clinical trials were terminated. Based on the ongoing interest in the field it is likely that new clinical trials can be expected and will unravel the therapeutic potential of PDE2A inhibition.     

甲型肝炎疫苗的使用现状及研究进展

甲型肝炎(甲肝)是由甲肝病毒引起的以肝脏损害为主的急性、自限性肠道传染病,主要通过污染的水源和食物或人与人接触传播.甲肝疫苗是对抗甲型肝炎最有效的方法.甲肝疫苗的开发和应用对甲肝的预防和控制起到了重要的作用.此文就甲肝的流行病学、疫苗的使用现状及新型疫苗的研发等方面进行综述.