4.7 Article

Synthesis and biological evaluation of salicylic acid conjugated isoxazoline analogues on immune cell proliferation and angiogenesis

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 114, Issue -, Pages 153-161

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.02.052

Keywords

Salicylic acid; Isoxazaoline; Mitogenecity; Lymphocytes; IL-2

Funding

  1. UGC [MRP(S)-0551-13-14/KAMY013/UGC-SWRO]
  2. Vision Group on Science and Technology, Government of Karnataka [VGST/CISEE/2012-13/282]
  3. Department of Information technology, Biotechnology and science & technology, Bangalore, India
  4. VGST [VGST/P-2/CISEE/GRD-231/2013-14]

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Mitogenicity is the ability of the natural or synthetic compounds to induce cell division or proliferation. A series of salicylic acid derivatives containing isoxazoline moiety (8a-j) were synthesized and their immunopharmacological activities targeting lymphocyte proliferation and angiogenesis were evaluated. The compounds 8a-j mitogenicity were investigated on immunological cells that include human peripheral blood lymphocytes and murine splenocytes in-vitro. The results implicate that among the series of 8a-j, compound 8e showed a potent proliferative response on both human and murine lymphocytes. The proliferative index of the compound 8e was comparable to the reference mitogen Con A and mitogenecity is due to increased secretion IL-2. In-vivo CAM and rat corneal angiogenesis assays were performed to assess the compound's effect on endothelial cell migration and proliferation which inferred that 8e also induces the proliferation of endothelial cells. The study reports the synthetic immunostimulatory and pro-angiogenic activity of novel mitogen 8e which could be translated into new drug in future. (C) 2016 Elsevier Masson SAS. All rights reserved.

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