Interactions between cyclodextrins and cellular components: Towards greener medical applications?

Leclercq, Loïc

However, the process, which leads to an aberrant accumulation of cholesterol in artery walls forming atherosclerotic plaques, is complex. Thus the alteration of RCT as well as the expression and the functionality of transporters (ABCA1, ABCG1, and SR-BI) involved in this process could be very useful in the fight against atherosclerosis pathogenesis. As pointed out by Coisne and co-workers, "RCT alterations have been poorly studied at the arterial endothelial cell and smooth muscle cells levels" [132] . Consequently, the authors investigated the effect of different methylated β-CDs on the RCT of arterial endothelial and smooth muscle cells. It should be noted that these two cell types express basal levels of ABCA1 and SR-BI whereas ABCG1 was solely found in arterial endothelial cells. The authors highlighted the correlation between the percentages of cholesterol extraction and the methylation degree of the CDs. This effect was clearly independent of the membrane composition. The expression levels of ABCA1 and ABCG1, as well as the cholesterol efflux to ApoA-I and HDL, were reduced due to cholesterol-methylated β-CD interaction. Consequently, the cellular cholesterol involved in atherosclerotic lesions is lowered and the expression of ABCA1 and ABCG1 transporters involved in RCT is clearly modulated.