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Synthesis of 12-quinoline substituted andrographolide derivatives and their preliminary evaluation as anti-aggregation drugs 12-喹啉取代穿心莲内酯衍生物的合成及其抗凝集作用的初步评价
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-02-28 DOI: 10.1071/ch22248
Xue Li, Jiafeng Yu, Xian-Ling Wu, Cui Hu, Xiaoqing Wang
Based on the structure of the natural product andrographolide, a series of novel 12-quinoline substituted derivatives 9 were designed and synthesized. In preliminary biological evaluation, these synthesized compounds showed prominent anti-platelet aggregation activities in response to thrombin and adenosine diphosphate (ADP) agonists. Among them, compound 9o (inhibition rate 55.73%, IC50 0.36 µM/L) had the highest anti-platelet aggregation activity induced by ADP. Compound 9q (inhibition rate 54.31%, IC50 0.30 µM/L) showed the highest anti-platelet aggregation activity induced by thrombin. Most of the derivatives had no significant cytotoxicity. Our research results provide a novel candidate drug structure for anti-platelet aggregation and enrich the scope of application of andrographolide derivatives.
基于天然产物穿心莲内酯的结构,设计并合成了一系列新的12-喹啉取代衍生物。在初步的生物学评价中,这些合成的化合物对凝血酶和二磷酸腺苷(ADP)激动剂表现出显著的抗血小板聚集活性。其中化合物90(抑制率55.73%,IC50 0.36µM/L)抗ADP诱导的血小板聚集活性最高。化合物9q抗凝血酶诱导的血小板聚集活性最高,抑制率为54.31%,IC50为0.30µM/L。大多数衍生物没有明显的细胞毒性。我们的研究结果为抗血小板聚集提供了一种新的候选药物结构,丰富了穿心莲内酯衍生物的应用范围。
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引用次数: 0
A simple 3D printed microfluidic device for point-of-care analysis of urinary uric acid 一种简单的3D打印微流体装置,用于尿尿酸的即时分析
4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-02-10 DOI: 10.1071/ch22180
Kolsoum Dalvand, Alireza Ghiasvand, Sepideh Keshan-Balavandy, Feng Li, Michael Breadmore
Point-of-care testing (POCT) technology allows scientists to monitor and diagnose diseases at the patient site, much faster than classical lab-based methods. Herein, a rapid, simple, and sensitive 3D printed microfluidic device integrated with smartphone-based on-chip detection is described for POCT quantification of urinary uric acid. The device includes two circular inputs each connected to a microliter-scale chamber, separated by an integrated porous membrane, located between the sample and reagent chambers. The microfluidic device was fabricated from a transparent photopolymer using a 3D printer, in a single run. The concentration of uric acid was determined based on a chromogenic reaction in which ferrous ion, produced via the reduction of ferric ion by the analyte, complexed with 1,10-phenanthroline, and the color was recorded by a smartphone. Response surface methodology including a central composed design was utilized to evaluate the experimental parameters and subsequent introduction of a multivariate model to describe the experimental conditions. Under the optimum conditions, the calibration curve was linear over the concentration range of 30–600 mg L−1. The limit of detection was determined to be 10.5 mg L−1. The microfluidic device was successfully utilized for the recovery and quantification of uric acid in the urine, with recoveries ranging from 91.7 to 99.7%.
即时检测(POCT)技术使科学家能够在患者现场监测和诊断疾病,比传统的基于实验室的方法快得多。本文描述了一种快速、简单、灵敏的3D打印微流控装置,该装置与基于智能手机的芯片检测相结合,用于尿尿酸POCT定量。该装置包括两个圆形输入,每个输入连接到一个微升规模的腔室,由位于样品和试剂腔之间的集成多孔膜分开。微流控装置由透明光聚合物制成,使用3D打印机,一次运行。尿酸的浓度是根据分析物还原铁离子产生的亚铁离子与1,10-菲罗啉络合的显色反应来确定的,并通过智能手机记录颜色。包括中心组合设计在内的响应面方法被用于评估实验参数,随后引入了一个多变量模型来描述实验条件。在最佳条件下,在30 ~ 600 mg L−1的浓度范围内,校准曲线呈线性关系。检测限为10.5 mg L−1。该微流控装置成功地用于尿液中尿酸的回收和定量,回收率为91.7% ~ 99.7%。
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引用次数: 3
Reactive intermediates and unusual molecules at Heron Island Heron岛的活性中间体和异常分子
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-20 DOI: 10.1071/chv76n1_fo
C. Wentrup
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引用次数: 0
Synthesis of R- and S-MDMA via nucleophilic ring-opening of homochiral N-tosylaziridines 亲核开环合成R-和S-MDMA的同手性n - tosyziridine
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch23064
Katie D. Lewis, Glenn A Pullella, H. Loh, B. Skelton, G. Flematti, M. Piggott
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引用次数: 1
Identification of NQO1 as a target of herbal drug agrimol B in hepatocellular carcinoma NQO1作为中草药agrimol B在肝癌中的靶点的鉴定
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch22255
Dingyue Zhang, Lixia Dong, Wenyong Yang, Kui Wang
{"title":"Identification of NQO1 as a target of herbal drug agrimol B in hepatocellular carcinoma","authors":"Dingyue Zhang, Lixia Dong, Wenyong Yang, Kui Wang","doi":"10.1071/ch22255","DOIUrl":"https://doi.org/10.1071/ch22255","url":null,"abstract":"","PeriodicalId":8575,"journal":{"name":"Australian Journal of Chemistry","volume":"14 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84868780","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Directed chemical dimerisation enhances the antibacterial activity of the antimicrobial peptide MSI-78(4–20) 定向化学二聚化增强抗菌肽MSI-78(4-20)的抗菌活性
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch23022
Rong Li, Thomas N. G. Handley, Wenyi Li, N. O’Brien-Simpson, M. Hossain, J. Wade
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引用次数: 1
Chemical constituents of lawang root oil 罗旺根油的化学成分
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch23013
Neanne Alnafta, Marlowe S Graham, N. Proschogo, C. McErlean
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引用次数: 0
Controlling emission energy in metal–organic frameworks featuring cyclometalated iridium(III) linkers 环金属化铱(III)金属有机骨架的发射能量控制
4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch23127
Carol Hua, Timothy U. Connell
Efficient solid-state luminescent materials are critical components in varied optoelectronic devices. Here, we report three metal–organic frameworks combining calcium(II) with heteroleptic iridium(III) metalloligands containing the same 1,2-diimine ancillary ligand but different cyclometalating ligands. The synthesised frameworks exhibit similar supramolecular structure but different emission properties depending on the cyclometalating ligand. Binding calcium(II) to the metalloligands further affects framework emission depending on the relative contribution of triplet charge transfer (3MLLCT) or ligand-centred (3LC) transitions to the emissive excited state.
高效的固态发光材料是各种光电器件的关键部件。在这里,我们报道了三种金属有机框架,结合钙(II)和异电性铱(III)金属配体,它们含有相同的1,2-二亚胺辅助配体,但不同的环金属化配体。合成的框架具有相似的超分子结构,但根据环金属化配体的不同具有不同的发射特性。将钙(II)结合到金属配体上进一步影响骨架发射,这取决于三重态电荷转移(3MLLCT)或配体中心(3LC)跃迁到发射激发态的相对贡献。
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引用次数: 0
The C-terminal pentapeptide acein analogue (JMV3315) stimulates dopamine release in the brain c端五肽acein类似物(JMV3315)刺激大脑释放多巴胺
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch22232
Charlène Lucas-Valmalle, G. Subra, P. Verdié, M. Kemel, V. Daugé, Karine Puget, Jean Martinez
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引用次数: 1
Fast protodeboronation of arylboronic acids and esters with AlCl3 at room temperature 芳基硼酸和酯与AlCl3在室温下的快速原波化反应
IF 1.1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-01-01 DOI: 10.1071/ch23028
Z. Yuan, Yun-Xia Liang, Yi He, Hui-Qing Deng, Haiting Wu, Bohong Lin, Jing Zhang
{"title":"Fast protodeboronation of arylboronic acids and esters with AlCl3 at room temperature","authors":"Z. Yuan, Yun-Xia Liang, Yi He, Hui-Qing Deng, Haiting Wu, Bohong Lin, Jing Zhang","doi":"10.1071/ch23028","DOIUrl":"https://doi.org/10.1071/ch23028","url":null,"abstract":"","PeriodicalId":8575,"journal":{"name":"Australian Journal of Chemistry","volume":"141 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77234816","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Australian Journal of Chemistry
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