New paper for the New Year

The Year 2022 started effectively, we already have our first paper for this year out! 😀 This paper is a continuation of our collaborative metformin project, in which we have designed and synthesized different kind of metformin analogues, and then studied their cellular uptake, the uptake mechanisms (what transporters are carrying them) and if they would have better cytotoxic effects in cancer cells than metformin itself and by which mechanism. We found that the sulfonamide derivative of metformin with long fatty acid tail attached to the benzyl ring had increased cellular accumulation in human breast cancer cells (MCF-7 and MDA-MB-231 lines) resulting in induced early and late apoptosis due to the cell cycle arrest in the G0/G1 and G2/M phases. This compound also induced intracellular reactive oxygen species (ROS) production and reduced mitochondrial membrane potential, which can ultimately lead to mitochondrial dysfunction and activation of the mitochondrial-associated apoptosis-signaling pathway. So in overall, this compound seems to be one of the best metformin analogues we have had so far, which guides us in the structural design of new analogues and encourages to continue to study this compound even further. However, you can read more about the present results here (not open access, unfortunately):

Sulfonamide metformin derivatives induce mitochondrial-associated apoptosis and cell cycle arrest in breast cancer cells (link for the publication)

And greatest thanks of this publication goes to the first and corresponding author Magdalena! Job well done! And now since this paper is out, she has already submitted another manuscript related to the anti-coagulation properties of these compounds. Let's hope I can have something more to write about this topic during the upcoming spring! 😀