Supramolecular assembly of Cp1-11 peptide and insulin for rapid-acting formulation

In order to improve the life quality of diabetic patients,it is very important to develop rapid-acting insulin formulations that can mimic the physiological meal-time secretion profile of insulin in healthy people.Although several insulin analogues have been designed to provide postprandial glycemic control,still there are some serious disadvantages.A supramolecular strategy is presented here to inhibit insulin aggregation and improve its bioactivity by using Cp1-11 peptide.As a fragment of C-peptide in proinsulin,Cp1-11 peptide was found to influence insulin oligomerization by supramolecular interactions.This work demonstrates that the Cp1-11 peptide can interact with oligomeric insulin and facilitate its disaggregation into the physiologically active monomeric form.Computer simulation indicates that Cp1-11 can insert into the space between the C-terminal tail and the N-terminal helix of the B-chain of insulin,causing dissociation of the insulin dimer.The supramolecular assembly of Cp1-11 and insulin can improve the bioavailability and therapeutic effect of insulin on the control of in vivo blood glucose levels.These results suggest that Cp1-11 peptide can modulate the intermolecular interaction of aggregated insulin and prevent the transition from monomeric to multimeric states,and shows great potential for the development of an effective rapid-acting strategy to treat diabetes.

Modification of polyfluorene nanoparticles via inclusion complexa- tion based on cyclodextrin for lectin sensing and cell imaging

Currently, conjugated polymer nanoparticles are widely used with many biological applications, especially bio-imaging and labeling. Thus their modification with different biomacromolecules becomes a crucial step before various applications. In literature,this modification was normally performed via covalent bonds. To our best knowledge, modification based on inclusion complexation has not been reported. Herein, via host-guest interaction between cyclodextrin and adamantane, supramolecular modification to conjugated polyfluorene nanoparticles has been successfully achieved. The glycopolymer-modified conjugated polymer nanoparticles showed excellent binding ability to lectins, such as Galectin-3 and selective imaging behavior to Hep G2 cells.

The glyco-regioisomerism effect on dynamic interactions between glycopolymers with galactose pendants and benzoxaborole-containing polymer

This work investigated the effect of glyco-regioisomerism of glycopolymers on their dynamic interaction with benzoxaborole-containing polymers. Two kinds of glycopolymers, P-1-Gal and P-6-Gal, i.e. galactoside pendant group linked to the identical main chain through its anomeric(C1) and C6-hydroxyl group position, respectively, were studied. We found that P-6-Gal showed stronger binding strength to the PNIPAM-co-PBOB polymer than P-1-Gal did, which controlled the macroscopic property of the resultant hydrogels at a molecular level.