Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 11, 2019
Previous Article Next Article

A forskolin-conjugated insulin analog targeting endogenous glucose-transporter for glucose-responsive insulin delivery

Author affiliations

Abstract

Insulin administration for the management of diabetes is accompanied by hypoglycemia, which is expected to be mitigated by glucose-responsive smart insulin that has self-regulation ability in response to blood glucose level (BGL) fluctuation. Here, we have prepared a new insulin analog by modifying insulin with forskolin (designated as insulin-F), a glucose-transporter (Glut) inhibitor. In vitro, insulin-F is capable of binding to Glut on erythrocyte ghosts, which can be inhibited by glucose and cytochalasin B. Upon subcutaneous injection in type 1 diabetic mice, insulin-F maintains BGLs below 200 mg mL−1 for up to 10 h, and achieves 20 h with two sequential injections. Moreover, insulin-F also binds to endogenous Gluts. Upon a glucose challenge, the elevated level of glucose competitively replaces and liberates insulin-F that binds to Glut, rapidly restoring BGLs to the normal range.

Graphical abstract: A forskolin-conjugated insulin analog targeting endogenous glucose-transporter for glucose-responsive insulin delivery

Back to tab navigation

Supplementary files

Article information


Submitted
14 Aug 2019
Accepted
18 Sep 2019
First published
14 Oct 2019

Biomater. Sci., 2019,7, 4508-4513
Article type
Communication

A forskolin-conjugated insulin analog targeting endogenous glucose-transporter for glucose-responsive insulin delivery

J. Wang, Z. Wang, J. Yu, Y. Zhang, Y. Zeng and Z. Gu, Biomater. Sci., 2019, 7, 4508
DOI: 10.1039/C9BM01283D

Social activity

Search articles by author

Spotlight

Advertisements