Bioactive compounds as an alternative for drug co-therapy: Overcoming challenges in cardiovascular disease prevention

Abstract

Different pharmacological interventions have been applied with success to reduce the progression of atherosclerosis. However, many patients are not good responders or must interrupt treatment due to adverse effects. Bioactive compounds such as omega-3 fatty acids (n-3 FA), plant sterol esters (PSE) and phenolic compounds (PHC) are natural molecules with great potential to reduce the atherosclerosis burden by reducing inflammation, LDL cholesterol (LDL-C) and oxidative stress, respectively. Although their physiological effects on biomarkers are much lower than those expected by drugs used for the same purpose, bioactive compounds can easily be incorporated into the daily diet and present no adverse effects. However, little is known about the combination of n-3 FA, PSE, PHC, and drugs in atherosclerosis progression. This review article summarizes potential effects of co-therapies involving n-3 FA, PSE, and PHC combined with major hypolipidemic drugs on atherosclerosis biomarkers and clinical outcomes. Evidence of additive and/or complementary effects regarding drugs action reveals possible roles for bioactive compounds in disease management. Pharmaceutical companies, physicians, and food scientists should be prepared to better understand this type of interaction and its consequences in terms of efficacy and life quality.

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

“…[75][76][77] However, most phyto-bioactive compounds taken with the diet or through an oral delivery system have exhibited a lower bioavailability in systemic circulation. [78][79][80] Recently, many phyto-bioactive compounds showed an improved bioavailability through SLN or MSLN delivery systems, which can further improve their cardioprotective activity. Puerarin is among the most cardioprotective compounds, and its successful loading in SLNs resulted in a higher bioavailability in various organs, especially three times higher in the heart and the brain.…”

Ensuring the future of functional foods

“…These products are successfully marketed to older consumers who have either had a diagnosis of high cholesterol or who may be clinically prescribed pharmaceutical cholesterol lowering agents such as statins (Köhler et al ., ; Poli et al ., ; Scolaro et al ., ; Yang et al ., ). Plant stanol products are also attractive to consumers who want to maintain a healthy lifestyle regardless of a clinical diagnosis of potential cardiovascular risk factors.…”

Cardiovascular Disease Prevention: The Earlier the Better? A Review of Plant Sterol Metabolism and Implications of Childhood Supplementation

“…However, the intestinal absorption of plant sterols is very limited in healthy subjects (about 0.5-2%), while absorption efficiency of daily consumption of 250-500 mg of cholesterol is 50-60%. Although plant sterols are taken up from the intestinal lumen into the enterocyte through the same transporter as cholesterol, Niemann-Pick C1-Like 1 (NPC1L1), absorption of these compounds is controlled by ATP-binding cassette co-transporters G5 and G8 (ABCG5/ABCG8), which act as efflux pumps to export free sterols from enterocytes back into the intestinal lumen [40] (Figure 2, [41][42][43]). The few plant sterol molecules that escape from this clearance mechanism are carried by lipoproteins in the circulation in a similar quantitative distribution as cholesterol molecules, therefore circulating primarily in LDL particles (70-80%).…”