Each side chain of cyclosporin A is not essential for high passive permeability across lipid bilayers

Takahiro Ono; Kazuhito V Tabata; Hiroyuki Noji; Jumpei Morimoto; Shinsuke Sando

doi:10.1039/d3ra01358h

Each side chain of cyclosporin A is not essential for high passive permeability across lipid bilayers

RSC Adv. 2023 Mar 13;13(12):8394-8397. doi: 10.1039/d3ra01358h. eCollection 2023 Mar 8.

Authors

Takahiro Ono¹, Kazuhito V Tabata², Hiroyuki Noji^{2

3}, Jumpei Morimoto¹, Shinsuke Sando^{1

3}

Affiliations

¹ Department of Chemistry & Biotechnology, Graduate School of Engineering, The University of Tokyo 7-3-1 Hongo, Bunkyo-ku Tokyo 113-8656 Japan jmorimoto@chembio.t.u-tokyo.ac.jp ssando@chembio.t.u-tokyo.ac.jp.
² Department of Applied Chemistry, Graduate School of Engineering, The University of Tokyo 7-3-1 Hongo, Bunkyo-ku Tokyo 113-8656 Japan.
³ Department of Bioengineering, Graduate School of Engineering, The University of Tokyo 7-3-1 Hongo, Bunkyo-ku Tokyo 113-8656 Japan.

Abstract

We compared the passive permeability of cyclosporin A (CsA) derivatives with side chain deletions across lipid bilayers. CsA maintained passive permeability after losing any one of the side chains, which suggests that the propensity of the backbone of CsA is an important component for high passive permeability.