chemical modification

化学改性
  • 文章类型: Journal Article
    本综述是新颖的,因为它讨论了研究人员对该主题的主要发现及其含义,并强调了这一特定领域的新兴研究及其未来前景。亚麻(Linumusitatissimum)的种子挤出粘液(FSM),具有多样化和广泛的应用,特别是在食品工业和作为药物成分。FSM已与几种食品和乳制品混合,以提高胶凝能力,光学性质,味道,和用户合规性。FSM被认为是泡沫,封装,乳化,暂停,成膜,和胶凝剂用于几种药物制剂和保健材料。由于刺激(pH)响应性溶胀-去溶胀特性,在人体不同生理pH值下的高肿胀指数,和生物相容性,FSM被认为是一种智能材料,有针对性的,和控制药物输送应用通过传统和先进的药物输送系统。FSM已通过羧甲基化修饰,乙酰化,共聚,和静电络合以获得药物所需的特性,食物,和保健产品。因此,本综述致力于隔离技术,结构表征,对食品和制药行业非常有价值的特性,临床前和临床试验,药理学方面,生物医学属性,和FSM的专利。
    The present review is novel as it discusses the main findings of researchers on the topic and their implications, as well as highlights the emerging research in this particular area and its future prospective. The seeds of Flax (Linum usitatissimum) extrude mucilage (FSM) that has a diverse and wide range of applications, especially in the food industry and as a pharmaceutical ingredient. FSM has been blended with several food and dairy products to improve gelling ability, optical properties, taste, and user compliance. The FSM is recognized as a foaming, encapsulating, emulsifying, suspending, film-forming, and gelling agent for several pharmaceutical preparations and healthcare materials. Owing to stimuli (pH) -responsive swelling-deswelling characteristics, high swelling indices at different physiological pHs of the human body, and biocompatibility, FSM is considered a smart material for intelligent, targeted, and controlled drug delivery applications through conventional and advanced drug delivery systems. FSM has been modified through carboxymethylation, acetylation, copolymerization, and electrostatic complexation to get the desired properties for pharma, food, and healthcare products. The present review is therefore devoted to the isolation techniques, structural characterization, highly valuable properties for food and pharmaceutical industries, preclinical and clinical trials, pharmacological aspects, biomedical attributes, and patents of FSM.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    糖胺聚糖透明质酸(HA)是一种普遍存在的透明质酸,非硫酸化多糖通过其与HA结合蛋白(HABP)的相互作用介导不同的生物学作用。大多数HABP属于Link模块超家族,包括主要的HA受体,CD44和分泌蛋白TSG-6,其催化重链(HC)从α-抑制剂(IαI)到HA的共价转移。已经确定了CD44(HABD_CD44)和TSG-6(Link_TSG6)的HA结合结构域(HABD)的结构,并广泛表征了它们与HA的相互作用。结合的机制是不同的,Link_TSG6主要通过离子和CH-π相互作用与HA相互作用,而HABD_CD44仅通过氢键和范德华力结合。在这里,我们利用这些差异来产生HA寡糖,在它们的还原端进行了化学修饰,与这些靶HABP特异性和差异性结合。用2-或3-氨基苯甲酸或2-氨基-4-甲氧基苯甲酸(HA6-2AA,HA6-3AA,HA6-2A4MBA,分别)与未修饰的HA6AN相比,Link_TSG6的亲和力增加。这些修饰不增加对CD44_HABD的亲和力。将HA6-2AA模型(源自HA4-2AA的溶液动态3D结构)对接到Link_TSG6结构中,提供2AA-羧基与精氨酸-81形成盐桥的证据。这些建模结果为HA寡糖的第二系列化学修饰提供了信息,再次显示与两种蛋白质的差异结合。发现对HA4和HA6的几种修饰将寡糖转化为HC转移的底物,而未修饰的HA4和HA6则不是。这项研究产生了有价值的研究工具,以进一步了解HA生物学。
    The glycosaminoglycan hyaluronan (HA) is a ubiquitous, non-sulfated polysaccharide with diverse biological roles mediated through its interactions with HA-binding proteins (HABPs). Most HABPs belong to the Link module superfamily, including the major HA receptor, CD44, and secreted protein TSG-6, which catalyzes the covalent transfer of Heavy Chains (HC) from inter-α-inhibitor (IαI) onto HA. The structures of the HA-binding domains (HABD) of CD44 (HABD_CD44) and TSG-6 (Link_TSG6) have been determined and their interactions with HA extensively characterized. The mechanisms of binding are different, with Link_TSG6 interacting with HA primarily via ionic and CH-π interactions, whereas HABD_CD44 binds solely via hydrogen bonds and van der Waals forces. Here we exploit these differences to generate HA oligosaccharides, chemically modified at their reducing ends, that bind specifically and differentially to these target HABPs. Hexasaccharides (HA6AN) modified with 2- or 3-aminobenzoic acid or 2-amino-4-methoxybenzoic acid (HA6-2AA, HA6-3AA, HA6-2A4MBA, respectively) had increased affinities for Link_TSG6 compared to unmodified HA6AN. These modifications did not increase the affinity for CD44_HABD. A model of HA6-2AA (derived from the solution dynamic 3D structure of HA4-2AA) was docked into the Link_TSG6 structure, providing evidence that the 2AA-carboxyl forms a salt bridge with Arginine-81. These modeling results informed a 2nd series of chemical modifications for HA oligosaccharides, which again showed differential binding to the two proteins. Several modifications to HA4 and HA6 were found to convert the oligosaccharide into substrates for HC-transfer, whereas unmodified HA4 and HA6 are not. This study has generated valuable research tools to further understand HA biology.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    多年生草本植物乌头草Nakai(毛茸茸科)在中国已被用作传统的东方药物多年。A.sinomontanum的主要药理成分,高乌甲素(LA),表现出镇痛药,抗炎,抗肿瘤,抗心律失常,和抗癫痫活性。由于其强大的功效和非成瘾性质,LA广泛用于治疗癌症疼痛和术后镇痛。这篇综述涵盖了与LA有关的研究进展,包括提取方法,分离技术,药理学性质,化学修饰,和临床应用。此外,它提供了与LA相关的潜在应用和当前挑战的见解,以促进未来的研究工作。
    The perennial herb Aconitum sinomontanum Nakai (Ranunculaceae) has been utilized as a traditional oriental medicine in China for numerous years. The principal pharmacological constituent of A. sinomontanum, lappaconitine (LA), exhibits analgesic, anti-inflammatory, anti-tumor, anti-arrhythmic, and anti-epileptic activities. Due to its potent efficacy and non-addictive nature, LA is widely utilized in the management of cancer pain and postoperative analgesia. This review encompasses the research advancements pertaining to LA including extraction methods, separation techniques, pharmacological properties, chemical modifications, and clinical applications. Additionally, it offers insights into the potential applications and current challenges associated with LA to facilitate future research endeavors.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    海藻酸盐是一种线性多糖,具有可修饰的结构和丰富的官能团,为定制各种基于藻酸盐的材料提供了巨大的潜力,以满足生物医学应用的需求。鉴于改性技术的进步,通过物理方法分析和总结海藻酸盐的改性具有重要意义,化学和生物方法。这些方法提供了大量的准备信息,海藻酸盐基材料的表征和应用。物理改性通常包括共混和物理交联,虽然化学修饰依赖于化学反应,主要包括酰化,硫酸化,磷酸化,碳二亚胺偶联,亲核取代,接枝共聚,终端修改,和退化。化学修饰藻酸盐含有化学交联的藻酸盐,接枝藻酸盐和低聚藻酸盐。与各种酶相关的生物修饰以实现水解或接枝。这些不同的修饰在充分利用藻酸盐在未来蓬勃发展的生物医学应用中的潜力方面具有很大的希望。总之,这篇综述提供了不同的改性方法,用于改善海藻酸盐的性质,同时扩大其生物医学潜力的综合讨论和总结。
    Alginate is a linear polysaccharide with a modifiable structure and abundant functional groups, offers immense potential for tailoring diverse alginate-based materials to meet the demands of biomedical applications. Given the advancements in modification techniques, it is significant to analyze and summarize the modification of alginate by physical, chemical and biological methods. These approaches provide plentiful information on the preparation, characterization and application of alginate-based materials. Physical modification generally involves blending and physical crosslinking, while chemical modification relies on chemical reactions, mainly including acylation, sulfation, phosphorylation, carbodiimide coupling, nucleophilic substitution, graft copolymerization, terminal modification, and degradation. Chemical modified alginate contains chemically crosslinked alginate, grafted alginate and oligo-alginate. Biological modification associated with various enzymes to realize the hydrolysis or grafting. These diverse modifications hold great promise in fully harnessing the potential of alginate for its burgeoning biomedical applications in the future. In summary, this review provides a comprehensive discussion and summary of different modification methods applied to improve the properties of alginate while expanding its biomedical potentials.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    紫山竹多糖具有许多重要的生理功能,但是它的制备方法,结构,和功能需要进一步探索。通过超声波辅助提取并纯化了山竹竹多糖。在此基础上,研究了其结构和理化性质。刚果红实验用于确定其是否具有三螺旋构象。通过红外光谱和核磁分析进一步分析了紫色山竹多糖的结构。经由过程相干实验研讨了上述三种多糖的抗氧化活性。发现紫色山竹多糖的单糖组成主要含有大量的阿拉伯糖,少量的鼠李糖和极少量的半乳糖醛酸,其核心主链由1,4-α-阿拉伯糖组成。它没有这种空间配置。紫色山竹多糖乙酰化后,得到取代度为0.33的乙酰化衍生物。发现它们对羟基自由基和脂质过氧化有一定的清除和抑制作用,其活性与多糖浓度有关。同时,经乙酰化改性处理后,多糖的抗氧化活性明显增强,表明化学修饰能有效提高多糖的某些活性。上述研究为紫山竹多糖的进一步研究和开发提供了一定的参考价值。
    Purple mangosteen scarfskin polysaccharide has many important physiological functions, but its preparation method, structure, and function need further exploration. A polysaccharide was obtained from mangosteen scarfskin by ultrasonic-assisted extraction and purified. On this basis, its structure and physicochemical properties were investigated. The Congo red experiment was used to determine whether it has a triple helix conformation. The structure of purple mangosteen scarfskin polysaccharide was further analyzed by infrared spectroscopy and nuclear magnetic analysis. The antioxidant activities of the above three polysaccharides were studied by related experiments. It was found that the monosaccharide composition of purple mangosteen scarfskin polysaccharide mainly contained a large amount of arabinose, a small amount of rhamnoose and a very small amount of galacturonic acid, and its core main chain was composed of 1,4-α-arabinose. It did not have this spatial configuration. After the acetylation of purple mangosteen scarfskin polysaccharide, the acetylated derivative with a degree of substitution of 0.33 was obtained. It was found that they had certain scavenging and inhibiting effects on hydroxyl radicals and lipid peroxidation, and their activities were related to the concentration of polysaccharides. Meanwhile, the antioxidant activity of the polysaccharide was significantly enhanced after the modified treatment of acetylation, which indicated that chemical modification could effectively improve some activities of polysaccharide. The above studies provided some reference value for the further research and development of purple mangosteen scarfskin polysaccharide.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    背景:山竹果皮多糖具有多种生物学活性,值得进一步研究。
    方法:UAEE-GMRP的抗氧化性能,UAEE-GMRP-1A,通过两种不同的抗氧化活性实验系统评估了CM-30和Ac-30。
    结果:四种多糖对羟自由基有较好的清除作用,而对脂质过氧化的抑制作用相对较弱。然而,总的来说,四种多糖在上述两个抗氧化实验中显示出一定程度的潜在应用,特别是来自藤黄果皮的化学改性多糖,从而有效地提高了它们的抗氧化活性。这也表明化学修饰是提高多糖活性的较好方法。此外,在这两个抗氧化剂探索实验中,与其他三种多糖相比,羧甲基化多糖显示出更强的活性。
    结论:羧甲基化修饰可能具有很大的应用潜力。
    BACKGROUND: Polysaccharide from Garcinia mangostana rind has many biological activities and deserves further research.
    METHODS: The antioxidant properties of UAEE-GMRP, UAEE-GMRP-1 A, CM-30, and Ac-30 were evaluated through two different antioxidant activity experimental systems.
    RESULTS: The four polysaccharides had a better scavenging effect on hydroxyl radicals, while their inhibitory effect on lipid peroxidation was relatively weak. However, overall, the four polysaccharides showed a certain degree of potential application in the two antioxidant experiments mentioned above, especially the chemically modified polysaccharides from Garcinia mangostana rind, which effectively improved their antioxidant activity. This also indicates that chemical modification is a better method to improve polysaccharide activity. In addition, in these two antioxidant exploration experiments, carboxymethylated polysaccharide showed stronger activity compared to the other three polysaccharides.
    CONCLUSIONS: The carboxymethylation modification may have great potential for application.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    合成了支链淀粉(PU)的羧甲基化衍生物,并评估了其作为蓝莓采后保存的涂层。通过醚化反应获得羧甲基普鲁兰,CMP1,CMP2和CMP3的取代度分别为0.52,0.34和0.26。红外光谱和核磁共振结果显示属于羧甲基的羰基的特征信号。热分析表明,CMP1、CMP2和CMP3衍生物的热稳定性值为209.91℃,214.73C,225.52°C,分别,并且相对于Td为238.84°C的PU较低。此外,确定了由于羧甲基化导致的玻璃化转变温度的增加。化学改性降低了相对于PU(71.34°)的接触角,CMP1,CMP2和CMP3的值为39.89°,53.72°和60.61°,分别。羧甲基化还增加了膜的水蒸气渗透性和机械性能。此外,发现CMP分子影响光学性质。与天然支链淀粉相比,基于CMP的涂料的应用降低了蓝莓的质量损失和成熟速率,因此,CMP分子的包装可以用作能够延迟成熟和延长水果保质期的涂层。
    Carboxymethylated derivatives of pullulan (PU) were synthesized and evaluated as coating for the postharvest preservation of blueberries. Carboxymethylpullulan was obtained by etherification reaction with the substitution degrees of 0.52, 0.34, and 0.26 for CMP1, CMP2, and CMP3 respectively. Infrared spectroscopy and nuclear magnetic resonance results showed characteristic signals of the carbonyl group belonging to the carboxymethyl group. Thermal analysis showed that CMP1, CMP2, and CMP3 derivatives presented thermal stability values of 209.91 C, 214.73 C, and 225.52 °C, respectively, and were lower with respect to PU with Td of 238.84 °C. Furthermore, an increase in the glass transition temperature due to carboxymethylation was determined. The chemical modification decreased the contact angle with respect to PU (71.34°) with values for CMP1, CMP2, and CMP3 of 39.89°, 53.72° and 60.61°, respectively. The carboxymethylation also increased the water vapor permeability and mechanical properties of the films. In addition, it was found that the CMP molecules affected the optical properties. The application of CMP-based coatings reduced the mass loss and ripening rate of blueberries compared to native pullulan, therefore, packaging from CMP molecules could be used as a coating capable of delaying ripening and extending the shelf life of fruits.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    铜离子和活性红120偶氮染料(RR-120)作为水污染物在未改性埃洛石(H-NM)上的吸附模型,以及用硫酸(H-SA)和(3-氨基丙基)三乙氧基硅烷(H-APTES)改性的埃洛石,被调查。结果表明,两种吸附物的吸附均具有pH依赖性,并且随着埃洛石用量的增加而增加。评估了吸附动力学,结果表明吸附遵循伪二级模型。通过Langmuir模型令人满意地描述了Cu(II)离子和RR-120染料在埃洛石上的吸附等温线。对Cu(II)离子的最大吸附容量为0.169、0.236和0.507mmol/g,分别,对于H-NM,H-SA,和H-APTES表明NH2官能化而不是吸附剂的表面积是增强的吸附的原因。结果发现,H-NM对RR-120染料的吸附容量为9.64μmol/g,H-SA为75.76μmol/g,和29.33μmol/g的H-APTES。结果表明,APTES官能化和硫酸活化是有希望的改性,两种改性埃洛石对重金属和偶氮染料的去除都有很好的应用潜力。
    The adsorption of copper ions and Reactive Red 120 azo dye (RR-120) as models of water pollutants on unmodified halloysite (H-NM), as well as halloysites modified with sulfuric acid (H-SA) and (3-aminopropyl)triethoxysilane (H-APTES), was investigated. The results showed that adsorption of both the adsorbates was pH-dependent and increased with the increase in halloysite dosage. The adsorption kinetics were evaluated and the results demonstrated that the adsorption followed the pseudo-second-order model. The adsorption isotherms of Cu(II) ions and RR-120 dye on the halloysites were described satisfactorily by the Langmuir model. The maximum adsorption capacities for the Cu(II) ions were 0.169, 0.236, and 0.507 mmol/g, respectively, for H-NM, H-SA, and H-APTES indicating that the NH2-functionalization rather than the surface area of the adsorbents was responsible for the enhanced adsorption. The adsorption capacities for RR-120 dye were found to be 9.64 μmol/g for H-NM, 75.76 μmol/g for H-SA, and 29.33 μmol/g for H-APTES. The results demonstrated that APTES-functionalization and sulfuric acid activation are promising modifications, and both modified halloysites have good application potential for heavy metals as well as for azo dye removal.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    核酸化学是一个巨大的研究领域,由于最近寡核苷酸治疗的爆炸性成功而获得了新的动力。为了使寡核苷酸变得临床有效,其单体部分进行修饰。尽管近年来已经提出了大量重新设计的天然核酸,其中绝大多数是过去50年提出的简单修改的组合。这篇综述致力于迄今为止已知的天然核酸的糖磷酸主链的主要修饰。这里,我们提出了关于核酸单体修饰的现有知识的系统化,并从化学逻辑的角度提出了可接受的分类。视觉表示旨在激励研究人员创建新型修饰或已知修饰的原始组合,这些修饰将产生具有有价值特征的独特寡核苷酸。
    Nucleic acid chemistry is a huge research area that has received new impetus due to the recent explosive success of oligonucleotide therapy. In order for an oligonucleotide to become clinically effective, its monomeric parts are subjected to modifications. Although a large number of redesigned natural nucleic acids have been proposed in recent years, the vast majority of them are combinations of simple modifications proposed over the past 50 years. This review is devoted to the main modifications of the sugar phosphate backbone of natural nucleic acids known to date. Here, we propose a systematization of existing knowledge about modifications of nucleic acid monomers and an acceptable classification from the point of view of chemical logic. The visual representation is intended to inspire researchers to create a new type of modification or an original combination of known modifications that will produce unique oligonucleotides with valuable characteristics.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    目的:单克隆抗体中的化学修饰可以改变疏水性,电荷异质性以及构象,最终会影响它们的物理稳定性。在这项研究中,研究了在下游纯化过程中使用的两种不同的缓冲条件下各个电荷变体对物理稳定性和聚集倾向的影响。
    方法:使用半制备型阳离子交换色谱法分离电荷变体,并在具有pH6.0和3.8的两种缓冲液中进行缓冲液交换。随后使用尺寸排阻色谱和动态光散射分析每个变体的尺寸异质性。构象稳定性,胶体稳定性,和加速稳定条件下的聚集行为。
    结果:当在没有延长储存的情况下分析时,每个电荷变体中的大小变体在两种pH条件下相似。然而,构象稳定性在pH3.8低于pH6.0。所有电荷变体在pH6.0显示相似的表观解链温度。相比之下,在pH3.8时,变体A3,A5,B2,B3和B4显示较低的Tm,表明构象稳定性降低。Further,A2、A3和A5在pH3.8时表现出降低的胶体稳定性。总的来说,酸性变体比碱性变体更容易聚集。
    结论:当今典型的工业实践是检查过程中的中间体稳定性,酸性物种和碱性物种分别作为一个类别。我们建议,由于不同的酸性或碱性物种具有不同的稳定性,因此可能需要在物种水平上进行稳定性评估,并且这些知识可用于下游过程的巧妙设计以实现稳定的产品。
    OBJECTIVE: Chemical modifications in monoclonal antibodies can change hydrophobicity, charge heterogeneity as well as conformation, which eventually can impact their physical stability. In this study, the effect of the individual charge variants on physical stability and aggregation propensity in two different buffer conditions used during downstream purification was investigated.
    METHODS: The charge variants were separated using semi-preparative cation exchange chromatography and buffer exchanged in the two buffers with pH 6.0 and 3.8. Subsequently each variant was analysed for size heterogeneity using size exclusion chromatography and dynamic light scattering, conformational stability, colloidal stability, and aggregation behaviour under accelerated stability conditions.
    RESULTS: Size variants in each charge variant were similar in both pH conditions when analyzed without extended storage. However, conformational stability was lower at pH 3.8 than pH 6.0. All charge variants showed similar apparent melting temperature at pH 6.0. In contrast, at pH 3.8 variants A3, A5, B2, B3 and B4 display lower Tm, suggesting reduced conformational stability. Further, A2, A3 and A5 exhibit reduced colloidal stability at pH 3.8. In general, acidic variants are more prone to aggregation than basic variants.
    CONCLUSIONS: Typical industry practice today is to examine in-process intermediate stability with acidic species and basic species taken as a single category each. We suggest that perhaps stability evaluation needs to be performed at specie level as different acidic or basic species have different stability and this knowledge can be used for clever designing of the downstream process to achieve a stable product.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

公众号