文冠果的化学成分研究进展

文冠果近年来广泛受到学术界关注,全身是宝,化学成分复杂多样,本文就文冠木、文冠果干燥果柄、文冠果果壳、文冠果种仁等部位化学成分做一简要总结.     

HPLC法测定文冠果各部位中文冠果皂苷E的含量

目的建立HPLC法测定文冠果各部位的文冠果皂苷E(bunkanka saponins E)的含量。方法采用重结晶分离纯化,波谱分析鉴定其结构;HPLC法测定其含量。用Hypersil ODS2柱(250 mm×4.6 mm,5μm),流动相为甲醇-水-磷酸(体积比为70.00∶30.00∶0.02),流速为1.0 mL.min-1,柱温为34℃,检测波长为210 nm。结果文冠果皂苷E质量浓度在0.009 8~0.196 0 g.L-1内与峰面积成良好线性关系r=0.999 9(n=6);果壳、果柄、种皮和种仁中文冠果皂苷E的平均回收率及RSD值分别为100.4%、1.64%(n=6);100.2%、2.72%(n=6);100.2%、2.12%(n=6);99.2%2、.28%(n=6)。结论该方法为文冠果不同药用部位(果壳、果柄和种皮)的质量控制提供实验依据。     

文冠果的化学成分和药理作用研究进展

目的:为文冠果的深入研究和应用提供参考。方法:系统查阅国内、外文献并进行整理和归纳,对文冠果的化学成分和药理作用研究进展进行综述。结果与结论:文冠果中含有多种类型化学成分,主要有黄酮类、三萜皂苷类、甾类、香豆素类等,并具有抗炎、抗肿瘤、抑制人类免疫缺陷病毒蛋白酶、改善学习记忆功能、抑菌、抗氧化等多方面的药理作用。进一步深入开展文冠果化学成分和药理作用的研究,对全方位综合利用文冠果这一植物资源具有重要意义。     

HPLC法测定文冠果果仁中文冠果皂苷B的含量

目的:建立文冠果果仁中文冠果皂苷B测定方法,为文冠果果仁及其制剂的工艺研究与质量控制提供评价指标与评价方法。方法:采用反相高效液相色谱法,色谱柱为YMC C18(250×4．6mm,5μm),流动相为甲醇-0．1％磷酸溶液(60:40),流速1．0ml／min,检测波长为215nm。结果:文冠果皂苷B在0．204-1．02μg线性范围内有良好的线性关系,平均回收率为99．05％。结论:本方法准确可靠,重现性好,可作为文冠果果仁质量控制的依据。     

文冠果的食用和药用价值

<正> 文冠果属无患子科文冠果属植物,别名文官果、文光果、木瓜等,是我国特有的一种优良木本食用油料树种。其适应性极强,根深、耐旱、耐寒、耐盐碱、耐脊薄,且综合价值高。分布于我国13个省(市、自治区)。1、文冠果的食用价值文冠果的果实含有高油脂及多种生物活性成分:     

HPLC法测定文冠果果仁中文冠果皂苷B的含量

目的:建立文冠果果仁中文冠果皂苷B测定方法,为文冠果果仁及其制剂的工艺研究与质量控制提供评价指标与评价方法。方法:采用反相高效液相色谱法,色谱柱为YMC C18(250×4．6mm,5μm),流动相为甲醇-0．1％磷酸溶液(60:40),流速1．0ml／min,检测波长为215nm。结果:文冠果皂苷B在0．204-1．02μg线性范围内有良好的线性关系,平均回收率为99．05％。结论:本方法准确可靠,重现性好,可作为文冠果果仁质量控制的依据。     

文冠果化学成分及药理作用研究进展

目的对文冠果 (XanthocerassorbifoliaBunge )化学成分及药理作用研究进展进行综述。 方法按照化学成分和药理作用类型进行分类综述。结果与结论文冠果中主要含有三萜皂苷、黄酮、香豆素等类型成分 ,并且具有抗炎、抑制HIV 1蛋白酶、改善学习记忆功能等药理活性     

文冠果药理作用的研究

本文针对于文冠果成分复杂的特点,对其药理作用的研究现状做了细致的总结,希望科研工作者能挖掘出文冠果最大的经济价值和药用价值,使它能够为人们的生活和患者的健康提供更加有利的服务。     

GC-MS法对超临界提取文冠果油中总甾醇和脂肪酸的测定

目的：测定文冠果油的理化参数、采用气质联用色谱法建立测定文冠果油总甾醇含量和脂肪酸组成的方法。方法：采用GC—MS对文冠果油中总甾醇和脂肪酸成分进行鉴定;总甾醇测定条件为：进样口温度280℃,柱温为程序升温100％（15℃／min）→280℃（28min）;脂肪酸组分测定条件为：进样口温度250℃,柱温程序升温70℃（10％／min）→220℃（17min）,分流比60：1。结果：文冠果油总甾醇含量为1．09g/kg;饱和脂肪酸占10．6％,不饱和脂肪酸占89．0％。结论：GC—MS法准确可行,可作为文冠果油质量评价方法之一。     

文冠果化学成分及药理作用研究进展

文冠果(Xanthoceras sorbi folia Bunge．)为无患子科文冠果属植物。又名木瓜、僧灯毛道、温旦革子，原产于我国北方，秦岭、淮河以北，内蒙古以南，东起辽宁，西至青海，南至河南及江苏北部。生于海拔52-2260米处的荒山坡、沟谷间和丘陵地带。文冠果有较强的适应性，具抗旱、耐寒、病虫害少、易繁殖、结实早、产量大等特点。文冠果还是我国特有的珍惜木本油料植物，     

SAR maps: a new SAR visualization technique for medicinal chemists

We present structure-activity relationship (SAR) maps, a new, intuitive method for visualizing SARs targeted specifically at medicinal chemists. The method renders an R-group decomposition of a chemical series as a rectangular matrix of cells, each representing a unique combination of R-groups and thus a unique compound. Color-coding the cells by chemical property or biological activity allows patterns to be easily identified and exploited. SAR maps allow the medicinal chemist to interactively analyze complicated datasets with multiple R-group dimensions, rapidly correlate substituent structure and biological activity, assess additivity of substituent effects, identify missing analogs and screening data, and create compelling graphical representations for presentation and publication. We believe that this method fills a long-standing gap in the medicinal chemist's toolset for understanding and rationalizing SAR.     

苯并噻唑衍生物抗肿瘤活性研究进展

杂环化合物的生物活性研究一直受到药物化学家的重视。苯并噻唑属于苯环并五元杂环,其衍生物易于合成,已被广泛应用于抗肿瘤尤其是具有分子靶向性抗肿瘤药物的研发。苯并噻唑衍生物可以通过多种途径发挥抗肿瘤作用,如激酶抑制、诱导凋亡、作用于DNA等。本文简要综述了近几年(2010²014年)苯并噻唑衍生物在抗肿瘤药物研究方面的一些新发现。     

天山堇菜化学成分及生物活性研究

通过近年来相关文献查阅,综述天山堇菜的化学成分及生物活性的研究进展。天山堇菜含有多种对人体有益的化学成分。天山堇菜作为新疆特种植物,具有很好的药用价值,值得深入研究。     

Characterization and quantification of the triterpenoids in different parts of Xanthoceras sorbifolia by HPLC-ESI-MS

Two new triterpenoid glycosides, sorbifoside A (2) and B (3), were isolated from the husks of Xanthoceras sorbifolia along with two known saponins (1, 5). Their structures were established on the basis of 1D and 2D NMR data. A simple and sensitive assay was developed for the simultaneous determination of 6 triterpenoids (1-6, including two triterpenoid aglycones) in X. sorbifolia based on high performance liquid chromatography-mass spectrometry (HPLC-MS) coupled to an electrospray ionization (ESI) interface. The analytes were detected by positive ESI ionization mode and quantified by selected ion monitoring (SIM). All the linear regressions were acquired with r2>0.998. The precisions were evaluated by intra- and inter-day tests, and the relative standard deviation (RSD) values were within the range of 2.0-2.8% and 1.7-2.9%, respectively. The recoveries for the quantified compounds were observed over the range of 95.3-104.7% with RSD values less than 4.6%. The method developed was successfully applied for simultaneous quantification of the six triterpenoids in X. sorbifolia, and our results showed that the contents of triterpenoids in different parts of X. sorbifolia varied significantly.     

Imidazole and benzimidazole derivatives as chemotherapeutic agents

Imidazole and benzimidazole systems are presented in a large number of common therapeutics agents. They were widely used in organic and medicinal chemistry, but recently the development of N-oxide derivatives got an improvement from the point of view of its chemical and biological activity. Though we will review recent developments in chemical and biological profiles (as antitumoral, antiparasitic, antiviral and antimicrobial agents) of these heterocycle systems and the corresponding N-oxides.     

文冠木中杨梅素的含量测定简

目的建立测定文冠木中杨梅素含量的高效液相色谱法。方法采用KromasilODSC·s色谱柱（250mm×4．6mm,5μm）,流动相为甲醇-水-冰醋酸（65：35：0．1）,流速为1．0mL／min,检测波长为295nm,柱温为30℃。结果杨梅素加样回收率为99．56％,RSD为2．04％,符合定量分析要求。结论该方法简便、准确,可作为文冠木药材的质量控制方法。     

Molecular insights into trypanothione reductase‐inhibitor interaction: A structure‐based review

Information on how small molecules bind to the target enzyme has the potential to impact immensely on how medicinal chemists go about antiparasitic drug discovery. In this review, for the first time, we intend to make an assessment of the structural aspects of trypanothione reductase as drug target, and its complexes with several reversible drugs from the Protein Data Bank (PDB). We attempt to reveal the mechanism of these interactions by careful accounting of the X‐ray structures and their possible roles in biological activity to treat Trypanosomatidae diseases. We focus on some of the outstanding findings from structures that are relevant to anti‐trypanocidal drug discovery. We also review new interesting compounds that have appeared in the literature based on these X‐ray structures.

     

文冠果果壳中一个新生物碱

目的研究文冠果果壳的化学成分。方法通过硅胶柱色谱、制备型薄层色谱进行化合物的分离，利用多种波谱技术鉴定化合物结构。结果分离得到10个化合物，鉴定为：2-甲基-6-(2′，3′，4′-三羟基丁基)吡嗪(I)、cleomiscosin D(II)、柚皮素(III)、圣草素(IV)、山柰酚(V)、槲皮素(VI)、芦丁(VII)、5，7-二羟基色原酮(VIII)、酪醇(IX)、1-O-甲基-肌-肌醇(X)。结论化合物I为一新化合物；化合物II，IV，V和VII～X均为首次从该属植物中分离得到。     

Silicon switch: Carbon–silicon Bioisosteric replacement as a strategy to modulate the selectivity,physicochemical, and drug-like properties in anticancer pharmacophores

Bioisosterism is one of the leading strategies in medicinal chemistry for the design and modification of drugs, consisting in replacing an atom or a substituent with a different atom or a group with similar chemical properties and an inherent biocompatibility. The objective of such an exercise is to produce a diversity of molecules with similar behavior while enhancing the desire biological and pharmacological properties, without inducing significant changes to the chemical framework. In drug discovery and development, the optimization of the absorption, distribution, metabolism, elimination, and toxicity (ADMETox) profile is of paramount importance. Silicon appears to be the right choice as a carbon isostere because they possess very similar intrinsic properties. However, the replacement of a carbon by a silicon atom in pharmaceuticals has proven to result in improved efficacy and selectivity, while enhancing physicochemical properties and bioavailability. The current review discusses how silicon has been strategically introduced to modulate drug-like properties of anticancer agents, from a molecular design strategy, biological activity, computational modeling, and structure–activity relationships perspectives.