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Int J Biol Macromol. 2022 Jan 05;201:47-58. doi: 10.1016/j.ijbiomac.2021.12.098. Epub 2022 Jan 05.

Preparation and characterization of 2-deacetyl-3-O-sulfo-heparosan and its antitumor effects via the fibroblast growth factor receptor pathway.

International journal of biological macromolecules

Zhengqi Zha, Yaoyao Liu, Yinghua Miao, Shiying Liao, Su-Yan Wang, Huiling Tang, Hongping Yin

Affiliations

  1. School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
  2. Department of Pharmacy, Jiangsu Food and Pharmaceutical Science College, Huaian 223003, People's Republic of China. Electronic address: [email protected].
  3. School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, People's Republic of China. Electronic address: [email protected].

PMID: 34998873 DOI: 10.1016/j.ijbiomac.2021.12.098

Abstract

Heparosan, with a linear chain of disaccharide repeating units of → 4) β-D-glucuronic acid (GlcA) (1 → 4)-α-D-N-acetylglucosamine (GlcNAc) (1→, is a potential starting chemical for heparin synthesis. However, the chemoenzymatic synthesis of single-site sulfated heparosan and its antitumor activity have not been studied. In this study, 2-deacetyl-3-O-sulfo-heparosan (DSH) was prepared successively by the N-deacetylation chemical reaction and enzymatic modification of human 3-O-sulfotransferase-1 (3-OST-1). Structural characterization of DSH was shown the success of the sulfation with the sulfation degree of 0.87. High performance gel permeation chromatography (HPGPC) analysis revealed that DSH had only one symmetrical sharp peak with a molecular weight of 9.6334 × 10

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Keywords: 2-Deacetyl-3-O-sulfo-heparosan; Apoptosis; FGFRs; Human lung cancer A549 cell; MAPK/JNK pathway

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