Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis

Hydrophobic interaction mediating self-assembled nanoparticles of succinobucol suppress lung metastasis of breast cancer by inhibition of VCAM-1 expression

“…Succinobucol (purity 99.2%) was synthesized from probucol as previously described methods [20,23]. Poloxamer P188 (P188) was purchased from BASF Co. Ltd (Germany).…”

“…Importantly, SCB exhibits surprisingly potent and selective inhibitory activity on VCAM-1 expression [23]. Accordingly, we supposed that SCB could be a promising candidate for suppressing lung metastasis of breast cancer, which still remained unexplored yet.…”

Assessment of lipoprotein profiles study (ALPS) and antioxidant activity in healthy subjects treated with AGI-1067

“…16 -20 Results from CART-1 also found that AGI-1067 had favorable effects on luminal dimensions of proximal references segments away from the stent, which indicates that vascular protection appears to be a new endpoint for this class of drugs that combine antioxidant properties with unique antiatherosclerotic activities. 3,21 The relationships between AGI-1067-mediated inhibition of the vascular oxidative-inflammatory cascade and cardiovascular event outcomes are being evaluated from the recently completed ARISE (Aggressive Reduction of Inflammation Stops Events) trial. 22 The HDL-C reductions with AGI-1067 may involve enhanced CETP activity and/or an upregulated SR-BI; each of these play a role in reverse cholesterol transport (RCT) and both have been implicated in the antiatherosclerotic effects of probucol, although many aspects regarding the impact of CETP on the RCT pathway are unclear.…”

“…1,2 Clinical trials are evaluating the anti-atherosclerotic effect of AGI-1067 as well as assessing its potential improvement over one of probucol's perceived major disadvantages, ie, high-density lipoprotein cholesterol (HDL-C)-lowering. [3][4][5][6][7] In the Canadian Antioxidant Restenosis Trial-1 (CART-1), a 6-week exposure to AGI-l067 (2 weeks before and 4 weeks after percutaneous coronary intervention [PCI]) resulted in significant dose-related increases in luminal area of the intervened segment of the coronary artery (P ϭ 0.02); with the greatest increase of 3.36 Ϯ 2.12 mm 2 observed for the 280 mg qd group that was comparable to the 3.69 Ϯ 2.69 mm 2 increase observed with 500 mg bid probucol. 5 In CART-1, there were dose-dependent decreases in HDL-C (Ϫ4.4%, Ϫ9.0% and Ϫ18.7%, respectively, in the 70, 140 and 280 mg AGI-1067 groups), but the reductions were not as great as those seen with probucol (Ϫ35.2%).…”

Antioxidants and atherosclerosis: Emerging drug therapies

“…AGI-1067, the monosuccinic acid ester of probucol, is a phenolic antioxidant member of a novel class of agents termed vascular protectants (Table 1) [40]. It has strong antioxidant properties equipotent to those of probucol and antiinflammatory properties [4,41].…”