原黄素(Proflavine) - 药物靶点：DNA_在研适应症：口腔肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

2,8-Diaminoacridine、Proflavine hemisulfate

靶点

DNA

作用机制

DNA嵌入剂

治疗领域

肿瘤口颌疾病

在研适应症

口腔肿瘤

非在研适应症

食管腺癌巴雷特食管恶性上皮肿瘤+ [13]

原研机构-

在研机构

National Cancer Institute

非在研机构

Icahn School of Medicine at Mount Sinai

National Institutes of Health

Baylor College of Medicine

最高研发阶段早期临床1期

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

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结构

分子式C13H13N3O4S

InChIKeyWSFHCKWLECYVBS-UHFFFAOYSA-N

CAS号553-30-0

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关联

11

项与原黄素相关的临床试验

NCT05396781 / Completed临床2期IIT

Acceptability and Performance of a Mobile Optical Biopsy Technology for Gastrointestinal Cancer Screening: A Clinical Study in Brazil

The investigators have a current trial in China and the US which provides significant support for the safety, cost-effectiveness, accuracy and efficiency of a high resolution microendoscope (HRME)-guided approach in the hands of experienced clinicians. To improve functionality, portability and broader use of this device by non-experts, the investigators recently developed a prototype marHRME platform with an automated, augmented reality (AR)-interpretation that provides an overlaid endoscopic + micro-endoscopic view, facilitating diagnosis and biopsy targeting.

开始日期2022-01-13

申办/合作机构

Rice University

[+2]

NCT02714439 / Active, not recruiting早期临床1期IIT

Low-Cost Imaging for Cervical Cancer Prevention in the Texas Lower Rio Grande Valley

The purpose of this study is to evaluate a different type of medical equipment called "High-Resolution Microendoscope" (HRME) for the diagnosis of cervical pre-cancerous lesions and cervical cancer. The investigators want to compare patients' clinical findings using the current equipment used in clinic with the clinical findings using new equipment we are testing on this research project. If the new equipment is proven to give comparable findings with current equipment being used, doctors might be able to offer a diagnosis and treat cervical lesions in one visit. It might not be necessary to wait for cervical biopsies to come back before women would receive the indicated treatment. Study subjects are being asked to participate because they have been diagnosed with an abnormal Papanicolaou (Pap) PAP smear, positive human papillomavirus (HPV) test or history of cervical dysplasia and need to have a colposcopic examination to determine the reason for abnormal results and receive treatment.

开始日期2016-10-25

申办/合作机构

University of Texas Medical Branch

[+3]

NCT02206048 / CompletedN/AIIT

Use of High-Resolution Microendoscopy (HRME) in Patients With Adenocarcinoma In-Situ (AIS) of the Cervix

The goal of this clinical research study is to learn if it is possible to get high-resolution microendoscopy (HRME) images of AIS tissue and/or tissue from microinvasive carcinoma right before a biopsy of the cervix. Researchers also want to learn if HRME images can show the difference between cancerous tissue and normal cervical tissue.

开始日期2015-10-02

申办/合作机构

The University of Texas MD Anderson Cancer Center

100 项与原黄素相关的临床结果

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100 项与原黄素相关的转化医学

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100 项与原黄素相关的专利（医药）

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812

项与原黄素相关的文献（医药）

2024-05-21·Journal of Biomedical Optics

Use of topical methylene blue to image nuclear morphometry with a low-cost scanning darkfield microendoscope

Article

作者: Carns, Jennifer ; Schwarz, Richard A ; Richards-Kortum, Rebecca R ; Anandasabapathy, Sharmila ; Hou, Huayu ; Gillenwater, Ann M

SignificanceFiber-optic microendoscopy is a promising approach to noninvasively visualize epithelial nuclear morphometry for early cancer and precancer detection. However, the broader clinical application of this approach is limited by a lack of topical contrast agents available for in vivo use.AimThe aim of this study was to evaluate the ability to image nuclear morphometry in vivo with a novel fiber-optic microendoscope used together with topical application of methylene blue (MB), a dye with FDA approval for use in chromoendoscopy in the gastrointestinal tract.ApproachThe low-cost, high-resolution microendoscope implements scanning darkfield imaging without complex optomechanical components by leveraging programmable illumination and the rolling shutter of the image sensor. We validate the integration of our system and MB staining for visualizing epithelial cell nuclei by performing ex vivo imaging on fresh animal specimens and in vivo imaging on healthy volunteers.ResultsThe results indicate that scanning darkfield imaging significantly reduces specular reflection and resolves epithelial nuclei with enhanced image contrast and spatial resolution compared to non-scanning widefield imaging. The image quality of darkfield images with MB staining is comparable to that of fluorescence images with proflavine staining.ConclusionsOur approach enables real-time microscopic evaluation of nuclear patterns and has the potential to be a powerful noninvasive tool for early cancer detection.

2024-05-14·The Journal of Chemical Physics

Absorption and fluorescence spectroscopy of cold proflavine ions isolated in the gas phase

Article

作者: Langeland, Jeppe ; Kjaergaard, Henrik G ; Kjær, Christina ; Lindkvist, Thomas Toft ; Vogt, Emil ; Nielsen, Steen Brøndsted

Proflavine, a fluorescent cationic dye with strong absorption in the visible, has been proposed as a potential contributor to diffuse interstellar bands (DIBs). To investigate this hypothesis, it is essential to examine the spectra of cold and isolated ions for comparison. Here, we report absorption spectra of proflavine ions, trapped in a liquid-nitrogen-cooled ion trap filled with helium-buffer gas, as well as fluorescence spectra to provide further information on the intrinsic photophysics. We find absorption- and fluorescence-band maxima at 434.2 ± 0.1 and 434.7 ± 0.3 nm, corresponding to a Stokes shift of maximum 48 cm−1, which indicates minor differences between ground-state and excited-state geometries. Based on time-dependent density functional theory, we assign the emitting state to S2 as its geometry closely resembles that of S0, whereas the S1 geometry differs from that of S0. As a result, simulated spectra involving S1 exhibit long Franck-Condon progressions, absent in the experimental spectra. The latter displays well-resolved vibrational features, assigned to transitions involving in-plane vibrational modes where the vibrational quantum number changes by one. Dominant transitions are associated with vibrations localized on the NH2 moieties. Experiments repeated at room temperature yield broader spectra with maxima at 435.5 ± 1 nm (absorption) and 438.0 ± 1 nm (fluorescence). We again conclude that prevalent fluorescence arises from S2, i.e., anti-Kasha behavior, in agreement with previous work. Excited-state lifetimes are 5 ± 1 ns, independent of temperature. Importantly, we exclude the possibility that a narrow DIB at 436.4 nm originates from cold proflavine cations as the band is redshifted compared to our absorption spectra.

2024-05-02·The Journal of Physical Chemistry Letters

Environmentally Driven Symmetry Breaking Quenches Dual Fluorescence in Proflavine

Article

作者: Mao, Yuezhi ; Hunter, Kye E ; Chin, Alex W ; Zuehlsdorff, Tim J

Nonadiabatic couplings between several electronic excited states are ubiquitous in many organic chromophores and can significantly influence optical properties. A recent experimental study demonstrated that the proflavine molecule exhibits surprising dual fluorescence in the gas phase, which is suppressed in polar solvent environments. Here, we uncover the origin of this phenomenon by parametrizing a linear-vibronic coupling Hamiltonian from spectral densities of system-bath coupling constructed along molecular dynamics trajectories, fully accounting for interactions with the condensed-phase environment. The finite-temperature absorption, steady-state emission, and time-resolved emission spectra are then computed using powerful, numerically exact tensor network approaches. We find that the dual fluorescence in vacuum is driven by a single well-defined coupling mode but is quenched in solution due to dynamic solvent-driven symmetry breaking that mixes the two low-lying electronic states. We expect the computational framework developed here to be widely applicable to the study of non-Condon effects in complex condensed-phase environments.

100 项与原黄素相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	原黄素	-	DB01123

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
幽门螺杆菌感染	临床2期	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
肠道疾病	临床2期	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
鳞状上皮内病变	临床2期	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
胃癌	临床2期	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
鳞状上皮内病变	药物发现	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
食管鳞状细胞癌	药物发现	中国	Baylor College of Medicine	2014-01-31
食管鳞状细胞癌	药物发现	美国	Baylor College of Medicine	2014-01-31
食管腺癌	药物发现	美国	Baylor College of Medicine	2012-09-30
巴雷特食管	药物发现	美国	Baylor College of Medicine	2012-09-30
细菌性心内膜炎	药物发现	美国	Baylor College of Medicine	2012-09-30

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02206048 (CTgov)	N/A	宫颈原位腺癌	9	High-Resolution Microendoscopy (HRME) Imaging+Proflavine	齋鏇衊壓鹹衊鏇齋淵鬱(艱鹹鑰鏇鹽醖鬱糧範網) = 鏇鹹窪鏇積範積齋窪齋壓網襯選選壓糧鏇積鑰 (夢夢構醖窪餘願築積衊, 憲製醖獵艱構積鏇齋繭 ~ 鹽齋鹽廠構淵憲顧淵鬱) 更多	-	2022-07-25