INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2022
·Vol. 24
·期 1
·64
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IF 6.208
Lini Huo,Xiaochen Liu,Yogini Jaiswal,Hao Xu,Rui Chen,Rumei Lu,Yaqin Nong,Leonard Williams,Yan Liang,Zhiruo Jia
We report herein the design and synthesis of a series of novel acridine-triazole and acridine-thiadiazole derivatives. The newly synthesized compounds and the key intermediates were all evaluated for their antitumor activities against human foreskin fibroblasts (HFF), human gastric cancer cells-803 (MGC-803), hepatocellular carcinoma bel-7404 (BEL-7404), large cell lung cancer cells (NCI-H460), and bladder cancer cells (T24). Most of the compounds exhibited high levels of antitumor activity against MGC-803 and T24 but low toxicity against human normal liver cells (LO2), and their effect was even better than the commercial anticancer drugs, 5-fluorouracil (5-FU) and cis-platinum. Further, pharmacological mechanisms such as topo I, cell cycle, cell apoptosis, and neovascularization were all evaluated. Only a few compounds exhibited potent topo I inhibitory activity at 100 μM. In addition, the most active compounds with an IC50value of 5.52–8.93 μM were chosen, and they could induce cell apoptosis in the G2 stage of MGC-803 or mainly arrest T24 cells in the S stage. To our delight, most of the compounds exhibited lower zebrafish cytotoxicity but could strongly inhibit the formation of zebrafish sub-intestinal veins, indicating a potential for clinical application.Keywords:acridine-triazole;acridine-thiadiazole;topoisomerase I;anti-angiogenesis;zebrafish
研究领域:
肿瘤学
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药理学
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分子生物学
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化学
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DOI
PubMed
高影响因子
MOLECULES
·
2021
·Vol. 26
·期 8
·2115
·
IF 4.412
Jiayong Huang,Zhenshuo Yan,Peiling Qiu,Yufeng Mo,Qizhen Cao,Qiuhong Li,Lini Huo,Lichun Zhao
A new coumarin-acridone fluorescent probe S was designed and synthesized, and the structure was confirmed with1H/13C NMR spectrometry, single-crystal X-ray diffraction, and high-resolution mass spectrometry. This probe has high sensitivity and selectivity for Fe3+over other testing metal ions at 420 or 436 nm in acetonitrile–MOPS (3-Morpholinopropanesulfonic Acid) buffer solution (20.0 μM, pH = 6.9, 8:2 (v/v)). Under physiological conditions, the probe displayed satisfying time stability with a detection limit of 1.77 µM. In addition, probe S was successfully used to detect intracellular iron changes through a fluorescence-off mode, and the imaging results of cells and zebrafish confirmed their low cytotoxicity and satisfactory cell membrane permeability, as well as their potential biological applications.Keywords:Fe3+detection;bioimaging;coumarin-acridone compound
研究领域:
分析化学
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生物学
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产品关联
DOI
PubMed
高影响因子
ANALYTICA CHIMICA ACTA
·
2021
·
IF 6.558
Tao Zhang,Wenhui He,Xiaodan Song,Dongzhi Wu,Yaokun Xia,Yan Liu,Linzhao Wu,Weiming Sun,Fengfei Lin,Jinghua Chen
Currently, organic artificial enzymes as biocatalysts have been extensively used to construct various colorimetric sensors. However, exploiting a potential organic artificial enzyme with high catalytic efficiency still remains a challenge. To address this issue, herein, we synthesize an acridone derivative 10-benzyl-2-amino-acridone (BAA). The synthesized BAA exhibits an intrinsic visible-light-stimulated oxidase-like activity, which is capable of oxidizing various chromogenic substrates without destructive hydrogen peroxide (H 2 O 2 ) under visible light stimulation , resulting in colored products. The reaction system can be regulated by switching light on and off, which is milder and more reliable means than others H 2 O 2 -dependent. The photocatalytic mechanism of BAA is investigated in detail. However, l -ascorbic acid (AA), an antioxidant generating from the acid phosphatase (ACP)-mediated hydrolysis of 2-phospho- l -ascorbic acid (AAP), is able to inhibit the catalytic activity of BAA. Based on the above properties, a facile, photo-switchable and low-cost colorimetric sensing strategy is developed for ACP detection. The linear range is 0.05–2.5 U/L (r = 0.9994), and the limit of detection (LOD) is 0.0415 U/L. Moreover, the proposed sensing system can be applied for monitoring ACP activity in practical samples, demonstrating promising applications in clinical analysis and biosensor platform.
研究领域:
生物化学
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分析化学
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生物技术
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传感器
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHEMICAL RESEARCH
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2015
·
IF 0.633
Fang-Ming Wang,Dan Bao,Bing-Xiang Hu,Ze-Yu Zhou,Deng-Deng Huang,Li-Zhuang Chen,Yuan-Yuan Dan
A series of novel 10-substituted 3,6-diphenyl-9-aryl-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-dione derivatives synthesised by condensation of different amines with xanthenes, was prepared from 5-phenylcyclohexane-1,3-dione and aromatic aldehydes by a Knoevenagel and Michael reaction and cyclisation catalysed by a trace of l-proline at room temperature. In addition, the molecular structure of a xanthene was determined by single-crystal X-ray diffraction analysis.
研究领域:
有机化学
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药物化学
✓ 已验证
DOI
高影响因子
DALTON TRANSACTIONS
·
2020
·Vol. 49
·期 46
·17033-17038
·
IF 4.174
Weichi Liang,Jiali Wen,Yukai Zhao,Meng Zhang,Jiuxing Jiang
A layered aluminophosphate |C14H11NO|2[Al4(HPO4)4F4(H2O)2] (denoted as SYSU-2) with a new topology has been hydrothermally synthesized with N-methyl-9-acridone (NMA) as the organic structure-directing agent. Single-crystal X-ray diffraction analysis reveals that SYSU-2 crystallizes in a triclinic space group P, with the inorganic sheets stacked in an AA sequence. Hydrogen bonds are responsible for the neutral inorganic–organic layer connection. The layer structure of SYSU-2 is constructed by alternating AlO4F2 octahedra and PO4 tetrahedra. The topological analysis of SYSU-2 indicates an independent topology. The NMA layers are self-assembled with π–π interaction. SYSU-2 crystals show interesting dual-band emission fluorescence properties compared with NMA crystals. Under 406 nm UV irradiation, SYSU-2 crystals emit yellow light with two emission bands at 477 and 566 nm, while NMA crystals emit blue light with only one band at 473 nm. The differences may be derived from the difference of stacking orders and distance of NMA molecule layers between the two crystals.
研究领域:
材料科学
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化学
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DOI
高影响因子
RAPID COMMUNICATIONS IN MASS SPECTROMETRY
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2015
·Vol. 29
·期 14
·1328-1334
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IF 2.253
Ping Liu,Yongjun Hu,Jiaxin Chen,Qing Yang
Rationale Traditionally, drug analysis in biological tissue by mass spectrometry has required complicated sample pre-treatment, which not only wasted time, but also had adverse effects on the results. In order to assist assessment of potential drugs rapidly and accurately, a direct analytical method for drug detection in tissues is needed. The development of such a method is described in this study. Methods An anti-cancer drug, 9-phenylacridine (ACPH), injected into the kidney of mice, was directly analysed from tissues placed on the surface of a graphite rod by near-infrared (1064 nm) laser desorption single photon ionization mass spectrometry (LD/SPI-MS). Results The LD/SPI-MS method was successfully validated by direct analysis of ACPH in kidney sections of mice, without any complicated and time-consuming sample pre-treatment. The sensitivity of detection was down to about 100 fmol per spot and the wide linear dynamic range allowed quantitative detection of ACPH in complex biological samples. A drug-time curve was acquired of ACPH in the kidney of mice after the drug had been injected into the caudal vein. Conclusions It was demonstrated that the anti-tumor drug ACPH could be directly and rapidly detected by LD/SPI-MS in biological tissues without any time-consuming pre-treatment procedure. This method could potentially be applied to the selective localization and analysis of small molecule drugs in tissues and to the study of the pharmacokinetics of new drugs. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
分析化学
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药理学
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
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2019
·Vol. 9
·期 12
·6717-6723
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IF 3.049
Xiuli Dong,Jiayuan Tang,Yan Ren,Xiangming Chen
A novel fluorescence labeling reagent N-acetylhydrazine acridone (AHAD) was designed and synthesized. A highly sensitive high performance liquid chromatography (HPLC) method coupled with fluorescence detection to determine benzaldehyde after derivatization with AHAD was developed. Optimum derivatization was obtained at 40 °C for 30 min with trichloroacetic acid as catalyst. Benzaldehyde derivative was separated on a reversed-phase SB-C18 column in conjunction with a gradient elution and detected by fluorescence detection at excitation and emission wavelengths of 371 nm and 421 nm. The established method exhibited excellent linearity over the injected amount of benzaldehyde of 0.003 to 5 nmol mL−1. The method was successfully applied to the determination of serum semicarbazide-sensitive amine oxidase (SSAO) activity in humans. SSAO is a significant biomarker because serum SSAO activity is elevated in patients with Alzheimer's disease, vascular disorders, heart disease and diabetes mellitus. It was demonstrated that the SSAO activity of the hyperglycemic group (60 ± 4 nmol mL−1 h−1) was significantly higher than that of normal blood sugar group (44 ± 4 nmol mL−1 h−1) with P < 0.05.
研究领域:
分析化学
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医学
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生物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
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2024
·
IF 3.9
Xian Xiao,Qiang Gao,Lan-Ying Wang,Yun-Fei Zhang,Yan-Ping Luo
An aromatic ring-containing compound with a wide range of biological activities, 9-methylacridine (AD-9-Me) is a precursor for the synthesis of various drugs. However, its photoactivation properties and mechanism of damage as a photo activator against Aedes aegypti are unknown. The toxic effects of AD-9-Me on Aedes aegypti mosquitoes were determined under light and non-light conditions. The results showed that the toxicity of AD-9-Me to mosquito larvae was significantly higher than that of the dark treatment after 24 h of light exposure; AD-9-Me was mainly distributed in the midgut of larvae, after 24 h of treatment, it can cause an increase in calcium ion concentration, reactive oxygen species (ROS) eruption and ROS accumulation by blocking the ROS elimination pathway in midgut cells. This in turn caused an increase in protein carbonyl and malondialdehyde (MDA) content, a decrease in mitochondrial membrane potential (MMP), a disruption of the barrier function of midgut tissues, a significant decrease in midgut weight and chitin content, which induced the up-regulation of AeDronc , AeCaspase8 and AeCaspase7 genes, leading to apoptotic cell death. In this study, we confirmed that AD-9-Me has photoactivation activity and mainly acts on the midgut of mosquito larvae, which can generate a large amount of ROS in the cells of the midgut and induce apoptosis to occur, resulting in the disruption of the function of the tissues of mosquito larvae, accelerating the death and delaying the development of the mosquito larvae.
研究领域:
昆虫学
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毒理学
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生物化学
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
DESALINATION
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2020
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IF 7.098
Weiwei Zhang,Hui-Jing Li,Liwei Chen,Jiani Sun,Xingyi Ma,Yunfei Li,Chao Liu,Xu Han,Boyi Pang,Yan-Chao Wu
An environment-friendly scaling–corrosion inhibitor composed of 10-methylacridinium iodide (MAI) and sodium citrate (SC) was developed, whose scale inhibition performance were studied through weight loss, electrochemical techniques , static tests and surface analysis techniques (SEM, SECM , XPS , XRD). The optimum mass ratio of MAI and SC corrosion inhibition was found to be 1:2, and the optimum mass ratio of scale inhibition was 1:3. The experimental results showed that MAI–SC mixture as mixed-type scaling–corrosion inhibitor with excellent corrosion ( η w = 92.7%) and scale inhibition performance ( η Ca = 98.3%). The electrochemical stability of the inhibitor film was investigated by chronoamperometry (CA). SEM and XRD simulations indicated that the MAI–SC mixture inhibitor can distort and disperse the crystal lattice of calcium carbonate without forming scale, and it plays a dominant role in the inhibition of calcite (110) surface growth. The structure-activity relationship between the molecule structure of the MAI–SC mixture and its scale–corrosion inhibition performance was discussed based on the quantum chemistry calculation.
研究领域:
材料科学
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化学工程
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环境科学
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产品关联
DOI
高影响因子
ChemistrySelect
·
2023
·Vol. 8
·期 2
·e202203646
·
IF 2.1
Siying Ren,Wen-Chao Geng,Xuexian Cui,Bian Wu,Zhe Zheng
Graphical We present a robust supramolecular tandem assay to monitor L-DOPA decarboxylase activity and screen enzyme inhibitors using cucurbit[7]uril and acridine orange reporter pair. L–DOPA decarboxylase (DDC) deficiency causes serious progressive neurodegenerative disorders. Developing a sensitive enzyme activity monitoring and inhibitors or activators screening approach is highly on demand for DDC deficiency diagnosis. Here, we report a simple and sensitive fluorescence supramolecular tandem assay based on reporter pair of cucurbit[7]uril and acridine orange for DDC activity monitoring continuously. Furthermore, this strategy demonstrates the potential of STA to screen inhibitors of DDC.
研究领域:
生物化学
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医学诊断
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药物开发
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF FLUORESCENCE
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2025
·
IF 3.1
Fang Fang,Cao Hongyu,Lu Jialu,Chen Nannan,Zhang Lu,Chen Yang
Carbon dots (CDs)-based ratiometric fluorescence strategies have attracted considerable attention. In this study, we developed a facile ratiometric fluorescent biosensor for DNA detection by utilizing the blue-emitting carbon dots (BCDs) as the fluorophore and acriflavine (AF), a fluorescent biological stain reagent, as both the response and recognition molecules. When AF was added, the fluorescence of BCDs decreased effectively and accompanied by a hypsochromic shift from 448 to 425 nm, whereas the fluorescence of AF at about 500 nm appeared due to the synergistic effect of Förster resonance energy transfer (FRET) and the inner filter effect (IFE) between the BCDs and AF. In the presence of DNA, the intercalative binding of AF into the DNA helix resulted in the fluorescence quenching of AF and the fluorescence restoration of BCDs at the same time. Therefore, the quantitative detection of DNA can be carried out vis evaluating the fluorescence intensity ratio of F 425 /F 500 . Under optimized conditions, the developed fluorescence method had an excellent linear range from 0 to 90 µM and a low detection limit of 0.52 µM. In addition, satisfactory results were obtained for the analysis of DNA in synthetic and real samples, with spiked recoveries ranging from 90.1 to 101.3%, demonstrating the enormous potential of the developed sensing platform for bioanalysis and biodetection. Graphical
研究领域:
生物传感器
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分析化学
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纳米技术
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生物分析
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荧光光谱
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYTICAL CHEMISTRY
·
2023
·
IF 7.4
Hongzhan Liu,Fangshuo Liu,Kaixiang Ji,Yuriy T. Zholudov,Islam M. Mostafa,Baohua Lou,Wei Zhang,Guobao Xu
9-Mesityl-10-methylacridinium ion (Acr+-Mes) is a donor–acceptor molecule with a much longer lifetime and a higher energy electron transfer excited state than natural photosynthetic reaction centers. Unlike lucigenin with a coplanar geometry, Acr+-Mes has an orthogonal geometry. There is no π conjugation between Acr+ and Mes. Due to its special electron donor–acceptor structure, it does not rely on strong alkalinity to generate an electron transfer state like lucigenin, which makes it possible to achieve chemiluminescence (CL) under weakly alkaline or neutral conditions. In this study, we report Acr+-Mes CL for the first time. Acr+-Mes generates about 400 times stronger CL intensity than lucigenin under neutral conditions (pH = 7) using KHSO5 as the coreactant. Moreover, Co2+ can enhance Acr+-Mes/KHSO5 CL remarkably. Acr+-Mes/KHSO5 CL enables Co2+ detection with a linear range of 0.5–500 nM and a limit of detection of 28 pM (S/N = 3). This method was tested for the detection of Co2+ in lake water, and the standard recovery rate of 96.8–107% was achieved. This study provides a new way to develop efficient CL systems in neutral solutions.
研究领域:
分析化学
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环境科学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）