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proflavine
JOURNAL OF CHEMICAL PHYSICS · 2024 ·Vol. 160 ·期 12 · IF 3.1

Ultrafast spectroscopy study of DNA photophysics after proflavine intercalation

Zhou Jie,Wang Xueli,Jia Menghui,He Xiaoxiao,Pan Haifeng,Chen Jinquan

Proflavine (PF), an acridine DNA intercalating agent, has been widespread applied as an anti-microbial and topical antiseptic agent due to its ability to suppress DNA replication. On the other hand, various studies show that PF intercalation to DNA can increase photogenotoxicity and has potential chances to induce carcinomas of skin appendages. However, the effects of PF intercalation on the photophysical and photochemical properties of DNA have not been sufficiently explored. In this study, the excited state dynamics of the PF intercalated d(GC) 9  • d(GC) 9 and d(AT) 9  • d(AT) 9 DNA duplex are investigated in an aqueous buffer solution. Under 267 nm excitation, we observed ultrafast charge transfer (CT) between PF and d(GC) 9  • d(GC) 9 duplex, generating a CT state with an order of magnitude longer lifetime compared to that of the intrinsic excited state reported for the d(GC) 9  • d(GC) 9 duplex. In contrast, no excited state interaction was detected between PF and d(AT) 9  • d(AT) 9 . Nevertheless, a localized triplet state with a lifetime over 5 µ s was identified in the PF–d(AT) 9  • d(AT) 9 duplex.

CAS / MDL: 121-69-7
研究领域: 生物物理学 · 分子生物学 · 药理学
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SENSORS AND ACTUATORS B-CHEMICAL · 2017 · IF 5.401

Graphene oxide-enhanced and proflavine-probed fluorescence polarization biosensor for ligand-RNA interaction assay

Liang Qi,Yao-Yao Fan,He Wei,Dan Zhang,Zhi-Qi Zhang

Proflavine could recognise HIV RRE (Rev response element) RNA, thus inhibiting its interaction with Rev peptide. Owing to the non-significant difference in fluorescence polarization (FP) signal between the proflavine and proflavine-RRE complex, it is not practicable for the identification of antagonists of HIV Rev peptide using proflavine as a FP probe. In the present study, graphene oxide (GO) was introduced to amplify the FP signal to enhance the sensitivity for the identification of Rev antagonists, thereby enabling the development of a primary GO-enhanced FP biosensor for the discovery of Rev antagonists. The effect of the amount of GO on the FP changes was investigated via displacement assay using a known Rev antagonist, neomycin B. The mechanism underlying the changes in FP caused by the addition of neomycin B was explored in the presence of GO. Finally, the performance of this biosensor was further evaluated using other 4 test drugs. The introduction of GO to this interaction system increased the practicability for the discovery of Rev antagonists using proflavine as a probe, and this label-free method does not suffer from limitations caused by fluorescent covalent labeling, thus providing a novel strategy for the characterization of ligand-RNA binding interactions.

CAS / MDL: 7782-42-5
研究领域: 生物物理 · 分子生物学 · 药物发现 · 纳米技术
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SUPRAMOLECULAR CHEMISTRY · 2017 · IF 1.264

A novel fluorescent indicator displacement assay for sensing the anticancer drug gefitinib

Yun-Yun Xi,Qing Tang,Ying Huang,Zhu Tao,Sai-Feng Xue,Qingdi Zhou,Gang Wei

Fluorescent indicator displacement assays have become popular for converting synthetic receptors into optical sensors. We have now shown that a 1:2 host–guest complex between cucurbit[8]uril (Q[8]) and proflavine (PF) can be used as a fluorescent indicator for sensing the anticancer drug gefitinib. The 2PF@Q[8] complex can be used to detect gefitinib with high selectivity using fluorescence spectrometry with a detection limit of 6.63 × 10−8 mol−L. The proposed sensing mechanism was investigated using 1H nuclear magnetic resonance spectroscopy (1H NMR), isothermal titration calorimetry and electrospray ionisation mass spectrometry. The 2PF@Q[8] complex was shown to be suitable for imaging gefitinib in prostate cancer (PC3) cells, which may help to elucidate relevant biological processes at the molecular level. We have developed a novel F-IDA to detect the anticancer drug GEF with high selectivity. The new indicator has excellent selectivity and a low detection limit for GEF. We have also demonstrated that the F-IDA can be used for the practical determination of drugs in living cells.

CAS / MDL: 184475-35-2
研究领域: 生物化学 · 药物分析 · 分子生物学
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2017 ·Vol. 409 ·期 11 ·2813-2819 · IF 3.431

Determination of proflavine in rat whole blood without sample pretreatment by laser desorption postionization mass spectrometry

Chen Jiaxin,Hu Yongjun,Lu Qiao,Wang Pengchao,Zhan Huaqi

A novel pretreatment-free method involving laser desorption postionization (LDPI) coupled with time-of-flight mass spectrometry (MS) was developed for the monitoring of proflavine level in rat whole blood. It comprises a protocol for dosing via intravenous administration and collection of whole blood, followed by direct LDPI-MS analysis without any sample pretreatment. An intense ion signal at m / z 209 was observed from whole blood without any interference signals, except some background signals below m / z 100. The calibration curve was established with use of 9-phenylacridine as the internal standard for proflavine determination from the plotting of the peak ratios of proflavine to the internal standard, with a correlation coefficient ( R 2 ) greater than 0.99. The limit of detection was estimated to be 0.48 pmol/mm 2 and the quantification range was 0.5-16.5 μg/mL for proflavine. In addition, only a minimal matrix effect was observed, as expected from considerations of the desorption and ionization mechanism. Interday and intraday accuracy and precision were calculated to be within 13% and 82–114%, respectively. Estimated concentrations of proflavine residue in whole blood were also successfully obtained at selected time points after dosing. The proposed method is simple, low cost, and sensitive, and should be seen as a complementary method for monitoring drug levels in blood. Monitoring proflavine levels in rat whole blood at different time points using laser desorption postionization mass spectrometry (LDPI-MS)

CAS / MDL: 92-62-6
研究领域: 分析化学 · 药理学 · 生物医学
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