吖啶衍生物合成及其在医药领域的应用进展

吖啶衍生物是一类结构特殊的含氮芳香族化合物,具有明显的抗肿瘤、消炎、抗菌、抗艾滋病毒及治疗老年痴呆症等药用活性.近年来,关于吖啶衍生物的合成及在医药领域中的应用得到了快速的发展.概述了吖啶衍生物的合成方法及其在医药领域中的应用进展.     

熊果酸的抗肿瘤活性及作用机理研究进展

熊果酸属五环三萜类化合物,来源丰富,具有广泛的生物活性。概述了熊果酸在医药领域的研究进展,着重论述了熊果酸的抗肿瘤活性及其抗肿瘤作用机理,并对熊果酸的研究开发前景进行了探讨。     

氮芥类抗肿瘤药物的研究进展

氮芥类药物是应用于临床的一类重要的抗肿瘤药物,是目前研究开发的热点领域之一;近几年,国内外有大量的文献报道新型氮芥衍生物的合成及其生理活性研究,本文就近年氮芥类化合物在抗肿瘤方面的研究进展进行综述。     

线粒体靶向抗肿瘤药物及其分类

线粒体是真核细胞重要的细胞器,在细胞代谢中发挥主要作用。线粒体与疾病的发生、发展、治疗密切相关,线粒体靶向抗肿瘤药物分子的设计和研究已成为药学、化学和生命科学等领域的关注热点。分别简述了8类线粒体靶向抗肿瘤药物的作用机制和特征,介绍了2类新型多功能线粒体靶向抗肿瘤药物,并展望了抗肿瘤药物未来的发展方向。     

姜黄素类化合物抗肿瘤活性研究进展

综合大量国内外相关文献资料,综述了姜黄素类化合物在合成及抗肿瘤活性等方面的研究现状及发展方向,分析现有姜黄素类化合物在合成及抗肿瘤活性等方面的研究成果,探讨姜黄素类化合物结构与其抗肿瘤活性关系,探讨相关研究的发展方向。姜黄素类化合物大多具有显著的抗肿瘤活性,其结构与抗肿瘤活性密切相关,是有研究前景的抗肿瘤化合物,有望通过构-效分析进行设计合成,合成具有高抗肿瘤活性的化合物。     

异喹啉及其衍生物合成方法研究进展

异喹啉及衍生物具有良好的抑菌、抗肿瘤、止痛、抗疟疾、抗心律失齐以及抗艾滋等生物活性,在医药、化工、染料等领域都有广泛的应用。本文主要综述了异喹啉以及衍生物的合成方法及最新进展。     

卤代喹啉的合成方法研究进展

卤代喹啉及衍生物具有良好的抗菌、抗肿瘤、抗结核等生物活性,在医药和农药等领域都有广泛的应用。本文综述了卤代喹啉的环合、直接卤代和间接取代等合成方法进展。     

抗肿瘤靶向药物最新研究进展

近年来,靶向抗肿瘤药物凭借其药物选择性强和毒性低的优点成为抗肿瘤药物研发的热点。根据抗肿瘤靶向药物的来源与制备技术,可分为小分子靶向和抗体靶向抗肿瘤药物2个种类。在小分子药物方面主要介绍了近年国内外研究的最新主流产品的作用位点和治疗领域;在抗体药物方面主要介绍了全人源抗体的临床研究现状。通过以上综述资料剖析,人类仍需展开深入和细致的肿瘤基础理论研究,阐明肿瘤发生发展根源,破解肿瘤之谜从而制备更加有效的治疗药物。     

喹啉-N-氧化物的制备方法进展

喹啉-N-氧化物及衍生物有抑菌、抗病毒、抗肿瘤等作用,在医药、农药、染料和催化等领域都有广泛应用。本文综述了通过氧化、环合和扩环等方法制备喹啉-N-氧化物及其衍生物的进展。     

腐植酸在医药保健品领域大有作为

【报告提要】1腐植酸在医药领域的研究进展近五十年来我国在腐植酸医药保健品的开发应用上,取得了一系列科研成果,包括在消炎止痛、抗肿瘤、抗病毒、调节免疫系统、抗溃疡及调节心血管功能等方面的应用。     

缺氧胁迫影响硝化污泥活性的机理

硝化过程是废水生物脱氮的关键环节。为了研究缺氧胁迫对硝化活性的影响及其机理,采用分批培养法分别测定了经0、12、24 h缺氧滞留处理的污泥硝化活性、过氧化氢酶活性和过氧化物酶活性,以及这些硝化污泥抗氧毒（过氧化氢）性能。经过12、24 h缺氧处理后,污泥平均比氨氧化活性分别从0.894 mg N·(g MLSS)^-1·h^-1降为0.453、0.387 mg N·(g MLSS)^-1·h^-1,下降了46.8％、49.8％,平均比亚硝酸氧化活性也从0.761 mg N·(g MLSS)^-1·h^-1降至0.485、0.459 mg N·(g MLSS)^-1·h^-1,下降了36.3％、39.7％。试验结果证明,缺氧胁迫可降低污泥硝化活性,缺氧胁迫时间越长,硝化活性降幅越大,缺氧胁迫对氨氧化的影响大于亚硝酸氧化。缺氧胁迫可抑制硝化污泥的抗氧化酶活性,POD、CAT活性分别下降了10％、17％（12 h）和24％、21％（24 h）,缺氧胁迫时间越长,抗氧化酶活性越低。缺氧胁迫可削弱硝化细菌的抗氧毒能力,引起硝化活性降低。     

含腙类结构化合物生物活性研究进展

含腙类结构的化合物具有杀虫、杀菌、除草等广泛生物活性,在新农药创制中占有重要地位.根据农药用途进行分类,对其生物活性进行了介绍,并对其发展前景作进一步展望.     

Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives

The worldwide development of antimicrobial resistance forces scientists to search for new compounds to which microbes would be sensitive. Many new structures contain the 1,3,4-oxadiazole ring, which have shown various antimicrobial activity, e.g., antibacterial, antitubercular, antifungal, antiprotozoal and antiviral. In many publications, the activity of new compounds exceeds the activity of already known antibiotics and other antimicrobial agents, so their potential as new drugs is very promising. The review of active antimicrobial 1,3,4-oxadiazole derivatives is based on the literature from 2015 to 2021.     

宝钢Corex渣和常用矿渣性能的比较

研究了宝钢Corex矿渣和常用矿渣的物理性能、易磨性、活性和自身水硬性。结果表明,宝钢Corex渣和常用矿渣的化学成分比较接近。两种矿渣碱度均大于1,说明两者有较高的潜在水化活性。由于Corex渣具有较高的致密性、含铁率和容重,使得Corex渣的易磨性较常用矿渣差。此外,在细度接近时,宝钢Corex渣的自身水硬强度略高于常用矿渣,但Corex渣的早期活性指数明显高于常用矿渣,在比表面积为400~450 m2/kg时,Corex渣的早期(3 d、7 d)活性指数分别高于常用矿渣15%和20%以上,两者后期(28 d)活性相差不大。     

新型具备抑菌活性阴离子型表面活性剂的抑菌性与表面活性的关系研究

本论文利用一种新型具备抑菌活性的阴离子型表面活性剂为实验材料,选取大肠杆菌及金黄色葡萄球菌作为目标菌种,通过纸片扩散法对其抑菌活性进行了研究,利用吊片法对其水溶液的表面张力进行了测定,并研究了其抑菌活性与表面活性的关系,讨论了其抑菌机理。     

Antioxidant and Antibacterial Activity of Nutraceutical Compounds from Chlorella vulgaris Extracted in Hydrothermal Condition

Abstract

Water in hydrothermal condition has been used for extraction of nutraceutical compounds from Chlorella vulgaris. Hydrothermal extraction was carried out in a semi-batch and a batch extractor at various temperatures (120–200°C), pressures (2–10 MPa), and extraction times (30–300 min) to extract antioxidant and antibacterial compounds. The effect of extraction condition on the yield of extract was investigated. The antioxidant and antibacterial activity of extracts obtained by hydrothermal extraction were examined. The increasing extraction temperature resulted in higher antioxidant activity, but lower antimicrobial activity. As comparison with hot water extraction, the antioxidant activity of extract obtained by hydrothermal extraction was higher than that obtained by hot water extraction, but the antibacterial activity of the extract obtained by hydrothermal extraction was lower.     

具有生物活性的肟醚类化合物的研究进展

肟醚化合物具有优良的杀虫、杀菌及除草活性,不少品种还具有低毒、低残留等优点。目前该类化合物的分子设计和合成及生物活性研究是农药创制的热点之一。按照不同的结构和生物活性进行分类,概述了近年来肟醚类化合物的研究进展,并对它的发展趋势、应用前景作了进一步展望。     

Synthesis and Properties of Dicephalic Cationic Surfactants Containing a Quaternary Ammonium and a Guanidine Group

Novel dicephalic surfactants containing a quaternary ammonium and a guanidine group were synthesized, and the effect of the alkyl chain length on micellization and antimicrobial activity were investigated. Surface tension and conductivity were applied to study the self-aggregation of the amphiphilic molecule in aqueous solution. The results indicated that these compounds reduce the surface tension to a level of 30–36 mN/m at the air/water interface and that there is a characteristic chain length dependence of the micellization process of surfactants. The antimicrobial activity was evaluated against Gram-negative, Gram-positive bacteria and fungi, indicating strong antibacterial activity against tested strains.     

表面活性物质强化活性污泥系统作用的研究

复合酶、十二烷基苯磺酸钠和蔗糖酯SE13等表面活性物质分别投加到悬浮生长好氧污泥系统中,采用容积氧传质系数、污泥氧利用速率以及污泥脱氢酶活性作为表征参数,通过对比研究各表面活性物质对混合液氧传质过程的作用以及对活性污泥微生物活性的作用。试验发现,在活性污泥混合液中投加十二烷基苯磺酸钠可以提高了容积氧传质系数（KLa）,改善氧传质．但投加十二烷基苯磺酸钠．会降低微生物的脱氢酶活性,而投加蔗糖酯和复合酶则可以提高微生物的脱氢酶活性。     

Novel Hydrophilic Riminophenazines as Potent Antiprotozoal Agents

SAR studies on a set of novel hydrophilic C-2 aminopyridinyl riminophenazines bearing variously functionalized basic side chains at C-3 were conducted. The novel compounds were evaluated for in vitro activity against two different species of Leishmania promastigotes, intramacrophage Leishmania amastigotes, chloroquine-sensitive and chloroquine-resistant strains of P. falciparum, and also against mature-stage P. falciparum gametocytes. Their cytotoxicity was evaluated as well on BMDM cell lines. Most of the new compounds potently inhibited the growth of both genera of protozoa with IC₅₀ values in the high nanomolar range and good selectivities versus mammalian cells. Besides their potent activity against asexual intraerythrocytic stages of P. falciparum, three compounds showed potential as transmission-blocking agents. The key role of the hydrophilic C-2 aminopyridinyl substituent to improve the leishmanicidal activity and the influence of the length and the nature of the basic side chain on the antiprotozoal activity and cytotoxicity were underlined.