1. Academic Validation
  2. Preparation and Anti-Tobacco Mosaic Virus Activities of Crocetin Diesters

Preparation and Anti-Tobacco Mosaic Virus Activities of Crocetin Diesters

  • J Agric Food Chem. 2021 Nov 17;69(45):13637-13643. doi: 10.1021/acs.jafc.1c03884.
Ling Li 1 Jiyong Zou 1 Changjiang Xu 1 Shengyong You 1 Zhaoyang Deng 1 Guihua Chen 1 Yuxiu Liu 2 Qingmin Wang 2
Affiliations

Affiliations

  • 1 Institute of Applied Chemistry, Jiangxi Academy of Sciences, Nanchang, Jiangxi 330096, People's Republic of China.
  • 2 State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin 300071, People's Republic of China.
Abstract

The development of Antiviral agents with an original structure and noticeable effect is always in great need. Natural Products are important lead compounds in the development of new pesticides. Crocin-1 and crocin-2 were effectively isolated from Gardeniae fructus and found to have higher anti-tobacco mosaic virus (TMV) activity levels than ribavirin. A series of the crocetin diester derivatives were synthesized with separated crocetin-1 as material and evaluated for their anti-TMV activities. They could be dissolved in common organic solvents as dichloromethane, ethyl acetate, tetrahydrofuran, and methanol. Compounds 5, 9, 13, 14, and 15 displayed higher activities in vivo than ribavirin. Compound 14 with significantly higher Antiviral activities than lead compounds (crocin-1 and crocin-2) emerged as a new Antiviral candidate.

Keywords

anti-TMV activity; crocetin diesters; extraction; natural product; solubility; synthesis.

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