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A facile fluorescence-coupling approach to visualizing leonurine uptake and distribution in living cells and Caenorhabditis elegans.
Shi, Hao; Yang, Jinrong; Lin, Jiajie; Hong, Xiaobing; Zhou, Ziyuan; Zhao, Jiamin; Li, Yiwen; Li, Junjie; Wu, Chaofeng; Yan, Jinwu; Wong, Nai-Kei; Gao, Lei.
Afiliación
  • Shi H; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Yang J; School of Biology and Biological Engineering, South China University of Technology, Guangzhou 510006, China.
  • Lin J; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Hong X; Department of Pharmacy, The Second Affiliated Hospital, Shantou University Medical College, Shantou, China.
  • Zhou Z; National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital & Shenzhen Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Shenzhen 518116, China.
  • Zhao J; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Li Y; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Li J; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Wu C; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China.
  • Yan J; School of Biology and Biological Engineering, South China University of Technology, Guangzhou 510006, China. Electronic address: yjw@scut.edu.cn.
  • Wong NK; Clinical Pharmacology Section, Department of Pharmacology, Shantou University Medical College, Shantou, Guangdong 515041, China. Electronic address: wongnk@stu.edu.cn.
  • Gao L; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong 510515, China; Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Southern Medical University, Guangzhou, Guangdong 510515, China; Guangdong Basic Research Center of Excellence for Integrate
Phytomedicine ; 130: 155737, 2024 Jul 25.
Article en En | MEDLINE | ID: mdl-38772183
ABSTRACT

BACKGROUND:

Caenorhabditis elegans (C. elegans) has been recognized for being a useful model organism in small-molecule drug screens and drug efficacy investigation. However, there remain bottlenecks in evaluating such processes as drug uptake and distribution due to a lack of appropriate chemical tools.

PURPOSE:

This study aims to prepare fluorescence-labeled leonurine as an example to monitor drug uptake and distribution of small molecule in C. elegans and living cells.

METHODS:

FITC-conjugated leonurine (leonurine-P) was synthesized and characterized by LC/MS, NMR, UV absorption and fluorescence intensity. Leonurine-P was used to stain C. elegans and various mammalian cell lines. Different concentrations of leonurine were tested in conjunction with a competing parent molecule to determine whether leonurine-P and leonurine shared the same biological targets. Drug distribution was analyzed by imaging. Fluorometry in microplates and flow cytometry were performed for quantitative measurements of drug uptake.

RESULTS:

The UV absorption peak of leonurine-P was 490∼495 nm and emission peak was 520 nm. Leonurine-P specifically bound to endogenous protein targets in C. elegans and mammalian cells, which was competitively blocked by leonurine. The highest enrichment levels of leonurine-P were observed around 72 h following exposure in C. elegans. Leonurine-P can be used in a variety of cells to observe drug distribution dynamics. Flow cytometry of stained cells can be facilely carried out to quantitatively detect probe signals.

CONCLUSIONS:

The strategy of fluorescein-labeled drugs reported herein allows quantification of drug enrichment and visualization of drug distribution, thus illustrates a convenient approach to study phytodrugs in pharmacological contexts.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Caenorhabditis elegans / Ácido Gálico Límite: Animals / Humans Idioma: En Revista: Phytomedicine Asunto de la revista: TERAPIAS COMPLEMENTARES Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Alemania
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Caenorhabditis elegans / Ácido Gálico Límite: Animals / Humans Idioma: En Revista: Phytomedicine Asunto de la revista: TERAPIAS COMPLEMENTARES Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Alemania