Mapping of biguanide transporters in human fat cells and their impact on lipolysis.

ABSTRACT:

Aim

To examine the cell membrane transporters involved in mediating the antilipolytic effect of biguanides in human fat cells.

Materials and methods

Gene expression of biguanide transporters was mapped in human subcutaneous adipose tissue and in adipocytes before and after differentiation. Those expressed in mature fat cells were knocked down by RNA interference (RNAi) and the antilipolytic effects of metformin and two novel, highly potent biguanides, NT1014 and NT1044, were examined.

Results

Analysis of the transporter affinity of biguanides in HEK293 cells overexpressing individual transporters showed that NT1014 and NT1044 had >10 times higher affinity than metformin. Animal studies showed that NT1014 was >5 times more potent than metformin in lowering plasma gluco

SUBMITTER: Arner P 

PROVIDER: S-EPMC6133731 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature