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The recent developments of fast reliable docking, virtual screening and other algorithms gave rise to discovery of many novel ligands of histamine receptors that could be used for treatment of allergic inflammatory disorders, central nervous system pathologies, pain, cancer and obesity. Furthermore, the pharmacological profiles of ligands clearly indicate that these receptors may be considered as targets not only for selective but also for multi-target drugs that could be used for treatment of complex disorders such as Alzheimer’s disease. Therefore, analysis of protein-ligand recognition in the binding site of histamine receptors and also other molecular targets has become a valuable tool in drug design toolkit. This review covers the period 2014–2020 in the field of theoretical investigations of histamine receptors mostly based on molecular modeling as well as the experimental characterization of novel ligands of these receptors. 相似文献
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Yixuan Fan Runze Yu Yongfeng Chen Yufeng Sun Geoffrey I. N. Waterhouse Zhixiang Xu 《Molecules (Basel, Switzerland)》2022,27(20)
In this study, a sensitive capillary electrophoresis (CE) method based on molecularly imprinted solid-phase extraction (MISPE) was proposed to determine histamine in foods. A molecularly imprinted polymer (MIP) synthesized by bulk polymerization was used as the MISPE adsorbent for the selective extraction of histamine. Under the optimal conditions, the MISPE-CE method possessed good linearity for histamine detection in the concentration range of 0.1–100.0 μg/L. The limit of detection and limit of quantification of the method were calculated to be 0.087 μg/L and 0.29 μg/L, respectively. The histamine in spiked rice vinegar and liquor samples were detected by the developed method with recoveries of 92.63–111.00%. The histamine contents in fish, prawn, pork, chicken breast and soy sauce samples were determined using the developed method and a high-performance liquid chromatography method, with no significant difference found between the two methods. 相似文献
43.
Justyna Gody Paula Zarba Dorota Stary Maria Kaleta Kamil J. Kuder Gniewomir Latacz Szczepan Mogilski David Reiner-Link Annika Frank Agata Doroz-Ponka Agnieszka Olejarz-Maciej Sylwia Sudo-Taaj Tobias Nolte Jadwiga Handzlik Holger Stark Anna Wickowska Barbara Malawska Katarzyna Kie-Kononowicz Dorota aewska Marek Bajda 《Molecules (Basel, Switzerland)》2023,28(1)
The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising strategy for research into the effective treatment of Alzheimer’s disease. In this study, a novel series of benzophenone derivatives was designed and synthesized. Among these derivatives, we identified compound 6 with a high affinity for H3R (Ki = 8 nM) and significant inhibitory activity toward BuChE (IC50 = 172 nM and 1.16 µM for eqBuChE and hBuChE, respectively). Further in vitro studies revealed that compound 6 (4-fluorophenyl) (4-((5-(piperidin-1-yl)pentyl)oxy)phenyl)methanone) displays moderate metabolic stability in mouse liver microsomes, good permeability with a permeability coefficient value (Pe) of 6.3 × 10−6 cm/s, and its safety was confirmed in terms of hepatotoxicity in the HepG2 cell line. Therefore, we investigated the in vivo activity of compound 6 in the Passive Avoidance Test and the Formalin Test. While compound 6 did not show a statistically significant influence on memory and learning, it showed analgesic properties in both acute (ED50 = 20.9 mg/kg) and inflammatory (ED50 = 17.5 mg/kg) pain. 相似文献
44.
Similarity searching in large combinatorial chemistry spaces 总被引:2,自引:0,他引:2
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鲭鱼亚目的海洋鱼类在捕获后易产生组胺,导致鲭鱼中毒.为研究组胺消长与微生物的关系,通过平板分离和摇瓶发酵,以荧光光度法测定酶活力,从鲭鱼(Pneumatophorus japonicus)皮肉、内脏和腮中分离筛选组胺降解菌,并对所产组胺降解酶的酶学性质进行研究和分析.结果表明:自内脏中分离筛选到一株组胺降解酶活力较高的革兰氏阴性杆菌,从生长产酶曲线推测该酶为初级代谢产物.该酶反应的最适温度为35℃,最适pH为7.2.在pH6.0~8.0和温度20~35℃范围内有较好的稳定性.Mn^2+、Ca^2+、Na^-、Mg^2+、K^+等金属离子存在时酶活力增加。Zn^2+、Al^3+、Fe^3+、Fe^2+、Cu^2+等金属离子存在时,酶活力下降,在EDTA存在条件下酶活力完全丧失.对其动力学研究表明,在甘氨酸-NaOH缓冲反应体系中,最大反应速度Vmax=156.25U·mL^-1,米氏常数Km=0.22mg·mL^-1.组胺降解菌国内还朱见报道,研究结果对进一步研究水产品组胺生物控制技术具有重要意义. 相似文献
46.
Detection of histamine in beer by nano extractive electrospray ionization mass spectrometry 下载免费PDF全文
Jiuxiao Cai Ming Li Xingchuang Xiong Xiang Fang Ruifeng Xu 《Journal of mass spectrometry : JMS》2014,49(1):9-12
In this study, rapid quantitative detection of histamine in beer was achieved by using nano extractive electrospray ionization mass spectrometry (nano EESI‐MS) coupling with standard addition method. Based on the MS2 experiment, histamine concentrations in three beer samples were determined to be 1.10 ± 0.12 µg/ml, 0.81 ± 0.09 µg/ml and 0.79 ± 0.09 µg/ml. The limit of detection for this method was calculated to be 0.02 µg/ml. These results show that this novel method can be used for direct, rapid and sensitive detection of histamine in beer without any tedious sample pretreatment. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献