The pharmacological profile of Leucoselect® Phytosome® has been defined by extensive in vitro and in vivo experimental studies. For the in vitro studies it has been used in the unformulated form.
- antioxidant activityLeucoselect® demonstrated its effective antioxidant capacity through different mechanisms: free radical scavenging activity, chelation of transition metals, inhibition of enzymes, quenching of singlet oxygen, sparing and regenerating effect on α-tocopherols.
- cardiovascular protective activityLeucoselect® reduced ischemia/reperfusion injury concurrently stimulating prostacyclin release in the isolated rabbit heart, protected endothelial cells from peroxynitrite induced damage and modulated the endothelium-dependent NO release in human artery. Furthermore, Leucoselect® was proven effective on several enzymes involved in the degradation of the extravascular matrix.
- antioxidant activity(22)Leucoselect® Phytosome®, administered for 3 weeks at 2.4% concentration in a standard diet, increased TRAP in young and aged rats (Δ% = +40 and +30) and physiological antioxidant defences of plasma.
- antiatherosclerosis activity(2,23,24)Leucoselect® Phytosome®, administered at 2% concentration in a standard diet, was proven effective against mild and severe atherosclerosis.
Atherosclerotic aortic lesions developed in rabbits fed on a balanced 0.25% cholesterol-rich diet, while in the group supplemented with Leucoselect® Phytosome® a marked reduction of aortic lesions was observed and many animals showed lesion frequencies similar to the standard chow-fed group.
A significant thickening of the carotid, evaluated with the intima/media ratio, developed in rabbits fed on a balanced 1% cholesterol-rich diet. The administration of Leucoselect® Phytosome® (2%, 6 weeks) with the diet significantly reduced the thickness of the arterial wall in comparison with the hypercholesterolemic controls.
Cardiovascular protective activity(22)
Leucoselect® Phytosome®, administered for 3 weeks at 2.4% concentration in a standard diet, reduced ischemia/reperfusion induced damages in the heart of young and aged rats. The recovery of myocardial function, expressed by left ventricular developed pressure (LVDP), at the end of reperfusion was 93% and 74% of the preischemic values, respectively. The protective effect on heart contractility was also strictly associated with a preserved coronary blood flow, expressed by the reduction of coronary perfusion pressure (CPP) close to the preischemic value both in young and aged rats.