Snake Venom Components: Tools and Cures to Target Cardiovascular Diseases

Cardiovascular diseases (CVDs) are considered as a major cause of death worldwide. Therefore, identifying and developing therapeutic strategies to treat and reduce the prevalence of CVDs is a major medical challenge. Several drugs used for the treatment of CVDs, such as captopril, emerged from natural products, namely snake venoms. These venoms are complex mixtures of bioactive molecules, which, among other physiological networks, target the cardiovascular system, leading to them being considered in the development and design of new drugs. In this review, we describe some snake venom molecules targeting the cardiovascular system such as phospholipase A2 (PLA2), natriuretic peptides (NPs), bradykinin-potentiating peptides (BPPs), cysteine-rich secretory proteins (CRISPs), disintegrins, fibrinolytic enzymes, and three-finger toxins (3FTXs). In addition, their molecular targets, and mechanisms of action—vasorelaxation, inhibition of platelet aggregation, cardioprotective activities—are discussed. The dissection of their biological effects at the molecular scale give insights for the development of future snake venom-derived drugs.     

功能化石墨烯的制备及抗癌药物递送载体的研究

以聚苯乙烯磺酸钠(PSS)为保护剂,利用水合肼还原氧化石墨烯制备了一种新型的聚苯乙烯磺酸钠功能化石墨烯(PSS-GNS).结果表明制备的PSS-GNS是水溶分散性的纳米片层材料.考察了PSS-GNS对模型抗癌药物罗丹明6G(R6G)的吸附行为,结果表明PSS-GNS对R6G吸附量较大(2.77 mg/mg).体外释放研究结果表明PSS-GNS/R6G对R6G的释放具有p H响应性和缓释作用.PSS-GNS的细胞毒性较低,能顺利进入癌细胞内并持续缓慢地释放R6G.因此,PSS-GNS有望成为一种新型的抗癌药物递送载体.     

荧光增白剂检测方法研究进展

介绍荧光增白剂的主要应用,对荧光增白剂常用的检测方法紫外灯法、紫外分光光度法、分子荧光光谱法、液相色谱法、高效液相色谱–质谱联用法的应用进行综述,并分析了各检测方法的优缺点,展望了未来的发展方向。     

气相色谱-质谱联用法测定日用品及食品中9种凉味剂的含量

建立了日用品及食品中薄荷脑等9种新型凉味剂含量的测定方法.样品经乙醇超声提取后,用DB-1701 MS毛细管色谱柱(30 m×0.25 mm×0.25 μm)分离,选择离子监测模式(SIM)进行质谱检测.在优化分析条件下,9种凉味剂分离良好,其在0.25～250 μg/mL浓度范围内线性关系良好,相关系数均大于0.996,除薄荷氧基.1,2丙二醇(0.26 μg/g)外,其余凉味剂的检出限均小于0.1μg/g;在3个不同加标浓度下的平均回收率为82.8％～103.5％,相对标准偏差(RSD,n=6)均不高于3.7％.该方法灵敏、准确、可靠,能较好地分离薄荷脑等9种凉味剂,具有分析时间短、抗干扰性好、定量准确等优点,可为含薄荷(清凉)口味食品的质量控制及未知凉味剂含量样品的分析提供科学数据.     

模板法制备无机纳米材料的研究进展

模板法在无机纳米材料的制备过程中能够有效地控制形貌、粒径和结构,已成为合成无机纳米材料的前沿方法。综述了模板法制备无机纳米材料的研究进展,主要介绍了硬模板剂(多孔阳极氧化铝、介孔碳)和软模板剂(高分子聚合物、生物高分子)的制备及其应用,结合模板法的作用机制,重点论述了不同种类的模板剂在无机纳米材料制备过程中对于形貌的影响。并对模板法制备无机纳米材料的前景和现存问题进行了总结。参考文献35篇。     

二甲双胍化学反应性的密度泛函理论研究及实验研究

二甲双胍(MET)是一个非常优良的降血糖药,一直是治疗II型糖尿病(T2DM)的首选药物,但其脂溶性较差,也存在引起胃肠道不适等副作用,对其结构修饰和衍生化,特别是将其研制成前药(Prodrug)具有一定的临床意义。为了探明二甲双胍化学反应的性能特点,本文基于密度泛函理论（DFT）开展了二甲双胍的化学内禀性质研究,包括各种可能互变异构体的单点能和量子化学反应性指数。此外,还对各异构体互变过程的过渡态以及它们的反应路径进行了研究。在此基础上,本文还对二甲双胍与亲电试剂的化学反应机理进行了初探,并用化学合成反应来验证,从而让我们能够从理论上弄清楚二甲双胍化学反应的特殊性质。     

碳酸钙固硫固体进样测汞仪快速测定硫化铅精矿中汞

在使用固体进样测汞仪直接测定硫化铅精矿中汞时,由于试样中硫含量通常较高(高达30%以上),在测定过程中大量的硫被氧化会污染甚至腐蚀固体进样测汞仪的核心部件催化管,导致催化管寿命严重缩短。为解决该问题,建立碳酸钙固硫-固体进样测汞仪直接测定硫化铅精矿中汞的分析方法;并对Ca/S比,分解温度,分解时间,齐化时间等参数进行优化。在最优条件下,Hg的含量在2~20 ng和20~500ng线性范围内回归系数(R²)分别为0.9996和0.9998;方法检出限(LOD)为0.006 μg/g。用该法对3个典型样品进行测定,相对标准偏差RSD≤9%(n=7),加标回收率为96%~106%。该方法简单、快捷,准确度和精密度高,适合硫化铅精矿中汞的快速测定。     

Design,synthesis and docking studies of new hydrazinyl-thiazole derivatives as anticancer and antimicrobial agents

Increase in the number of infections caused by pathogenic microbes in cancer patients has prompted the searcher to invest in the development of agents having dual anticancer and antimicrobial properties. The present study is concerned with synthesis and screening for anticancer and antimicrobial activity of a series of 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thiazole derivatives. The structure elucidation of the synthesized hydrazinyl thiazole derivatives was illustrated by spectroscopic and elemental analysis. All the newly synthesized compounds 5a-p were evaluated for in-vitro cytotoxic activity against breast carcinoma (MCF-7 cell line), hepatocellular carcinoma (HePG-2) and colorectal cancer (HCT-116) cell lines using MTT assay method. Compounds 5 g, 5h showed broad spectrum activity against three cancer cell lines with IC₅₀ ranged from 3.81 to 11.34 µM in compared to the reference drug Roscovitine (IC₅₀ = 9.32 to 13.82 µM), while compounds 5 l and 5 m were found to be more selective against HePG-2 and HCT-116 cell line (IC₅₀ = 9.29 and 8.93 µM respectively) and compound 5j was more selective against HePG-2 and MCF-7 cell lines (IC₅₀ = 6.73 and 10.87 µM respectively). The inhibitory activity of the most promising compounds was tested against the EGFR and ARO enzymes and were further tested for apoptosis and Annexin V/PI staining. The results of enzyme-based tests revealed that the tested compound 5j has a dual inhibitory effect on the EGFR and ARO enzymes with IC₅₀ = 82.8 and 98.6 nM respectively in compared to the reference drugs Erlotinib and Letrozole (IC₅₀ = 62.4 and 79 nM respectively). Furthermore, the majority of the tested hydrazinyl thiazole derivatives exhibited significant antimicrobial activity against the used pathogenic microbes species. Compounds 4b, 5h, 5j and 5 m exerted a good antibacterial and antifungal activity against all tested pathogenic microbes. Therefore, it was concluded that compounds 5 h, 5j and 5 m proved to possess dual anticancer and antimicrobial agent and may serves as a useful lead compounds in search for further modification or derivatization to give more potent and selective agents.     

锌活化Fe/Co/N掺杂的生物质碳基高效氧还原催化剂

为了推动清洁能源-燃料电池的广泛应用, 迫切需要研发成本低、 原料来源广泛的过渡金属基高效氧还原反应(ORR)催化材料, 来替代目前使用的贵金属铂基催化材料. 本文以铁和钴等非贵金属离子作为催化材料的主要活性位点, 通过金属-羧基/羟基螯合键原位预锚定在具有三维(3D)孔道结构、 富含羧基和羟基以及极易在水溶液中形成凝胶网络的海洋生物质材料海藻酸钠上, 经冷冻干燥得到气凝胶; 然后通过高温碳化, 得到活性位点均匀分布在具有多级孔结构的碳骨架中的高活性、 高稳定的Co/Zn/Fe/N@bio-C-2氧还原催化剂材料, 该催化剂包含2种不同的铁基活性材料(Fe₂O₃和Fe)以及2种不同的钴基活性材料(CoO和Co).利用硝酸锌作为活化剂来改善催化材料的孔道结构, 使制备碳材料的总面积从149.3 m²/g增加到325.3 m²/g. 通过一系列对比实验发现, Fe/Co双活性位点与合适比表面积的协同作用使得Co/Zn/Fe/N@bio-C-2获得了最佳的ORR催化活性.其在0.1 mol/L KOH溶液中起始电位达到0.99 V, 半波电位可达0.87 V.     

A new procedure for determination of nickel in some fake jewelry and cosmetics samples after dispersive liquid–liquid microextraction by FAAS

A new, simple and cheap dispersive liquid–liquid microextraction (DLLME) procedure was optimized for the preconcentration of trace amounts of Ni(II) as a prior step to its determination by flame atomic absorption spectrometry (FAAS). It is based on the microextraction of nickel, where appropriate amounts of the extraction solvent (CHCl₃), disperser solvent (ethanol) and chelating agent, name 5‐[(Z)‐isoxazol‐3‐yl‐diazenyl]‐2‐methyl‐quinolin‐8‐ol (MMD), were firstly synthesized/characterized and used. Various parameters that affect the extraction procedure such as pH, centrifugation rate and time, the chelating agent (MMD) concentration and sampling volume on the recovery of Ni(II) were investigated. The preconcentration of a 20 ml sample solution was thus enhanced by a factor of 80. The resulting calibration graph was linear in the range of 0.24–10 mg L⁻¹ with a correlation coefficient of 0.9998. The limit of detection (3 s/b) obtained under optimal conditions was 1.00 μg L⁻¹. The relative standard deviation for certified reference material determinations was 1.2%. The accuracy of the method was verified by the determination of Ni(II) in the certified reference material of wastewater (Waste water CWW TMD). The proposed procedure was successfully applied to the determination of Ni(II) in some fake jewelry and cosmetics samples.