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We examined the clinical safety and efficacy of F105 in 11 subjects with moderate dyslipidemia. F105 is a combination of bergamot fruit extract (Citrus bergamia, BFE) and 9 phytoextracts selected for their ability to improve the antioxidant and anti-inflammatory activity of BFE. In vitro F105 exhibited a synergistic inhibition of oxygen radical absorbing capacity, peroxynitrite formation, and myeloperoxidase activity. Following 12 weeks of F105 daily, no treatment-related adverse events or changes in body mass were seen. Statistically significant changes were noted in total cholesterol (-7.3%), LDL-cholesterol (- 10%), non-HDL cholesterol (-7.1%), cholesterol/HDL (-26%), and apolipoprotein B (-2.8%). A post hoc analysis of 8 subjects with HbA1c > 5.4 and HOMA-IR score > 2 or elevated triglycerides revealed additional statistically significant changes in addition to those previously observed in all subjects including triglycerides (-27%), oxLDL (-19%), LDL/HDL (-25%), triglycerides/HDL (-27%), oxLDL/HDL (-25%), and PAI-1 (-37%). A follow-up case report of a 70-year-old female patient, nonresponsive to statin therapy and placed on F105 daily, demonstrated improved cardiometabolic variables over 12 weeks similar to the subgroup. In summary, F105 was clinically well-tolerated and effective for ameliorating dyslipidemia in subjects with moderate cardiometabolic risk factors, particularly in the individuals with HbA1c > 5.4%. Key words: cardiometabolic disease, bergamot, antioxidant, myeloperoxidase, oxidized LDL, dyslipidemia, HbA1c. Les auteurs ont examine la securite et l'efficacite cliniques du F105 chez 11 sujets presentant une dyslipidemie moderee. Le F105 est une combinaison d'extrait de bergamote (Citrus bergamia, EB) et 9 extraits vegetaux selectionnes pour leur capacite a ameliorer l'activite antioxydante et anti-inflammatoire de l'EB. In vitro, le F105 montrait une inhibition synergique de la capacite d'absorption des radicaux d'oxygene, de formation de peroxynitrite et de l'activite myeloperoxydase. Apres 12 semaines d'administration quotidienne de F105, aucun effet secondaire indesirable relie au traitement ou changements de poids corporels n'etaient observes. Des changements statistiquement significatifs ont ete notes quant au cholesterol total (- 7,3%), LDL-cholesterol (-10%), non-HDL-cholesterol (-7,1%), cholesterol/HDL (-26%) et apolipoproteine B (-2,8%). Une analyse post hoc de 8 sujets presentant une HbA1c > 5.4 et un indice HOMA-IR >2 ou des triglycerides eleves a revele des changements additionnels statistiquement significatifs en plus de ceux precedemment observes chez tous les sujets incluant les triglycerides (- 27%), oxLDL (-19%), LDL/HDL (-25%) triglycerides/HDL (-27%), oxLDL/HDL (-25%), et PAI-1 (-37%). Une etude de cas de suivi d'une patiente de 70 ans, ne repondant pas a la therapie par les statines et traitee au F105 quotidiennement, a demontre amelioration des variables cardiometaboliques pendant les 12 semaines similaire au sous-groupe. En resume, le F105 est bien tolere cliniquement et il est efficace pour ameliorer la dyslipidemie chez des sujets presentant des facteurs de risques cardiometaboliques moderes, particulierement les individus ayant une HbA1c > 5,4%. [Traduit par la Redaction] Mots-cles: maladie cardiometabolique, bergamote, antioxydant, myeloperoxydase, LDL oxydees, dyslipidemie, HbA1c., Updated online 26 October 2016: The license for this article has been changed to the CC BY 4.0 license. The PDF and HTML versions of the article have been modified [...]

Cell cultures isolated from epicardial myocytes of dogs were used in the investigation of the mechanism reducing the transient outward potassium current in diseased myocytes. Results reveal that epinephrine and beta adrenergic agonists restored channel density but not channel kinetics in diseased myocytes. Inhibition studies also revealed a possible role for intracellular calcium in mediating the effects of epinephrine and beta adrenergic agonists.

The maturation of the transient outward current, I(sub to), takes place during the first 20-30 weeks of age in canine epicardium, but the mechanism of regulation of development and the physiological significance of the increase in I(sub to) with age is unknown. A study of beagle fetal tissue and right ventricular free wall indicate I(sub to) activation because of a pronounced phase 1 repolarization decreased by 4-aminopyridine or a conditioning voltage clamp step. I(sub to) showed age-related changes as well as a relationship with action potential configuration.

The study of Trypanosoma cruzi reveals that this psecies inhibits the transient outward current in epicardial myocytes. The Trypanosoma cruzi is the primary cause for Chagas' disease which results in cardia aerhythimas and cardiomyopathy. The inhibition property of Trypanosoma is involved in the regulation and control of cardiac diseases.

The plant-based compounds rho-iso-alpha acids (RIAA) from Humulus lupulus (hops) and proanthocyanidins (PAC) from Acacia nilotica have been shown tomodulate insulin signaling in vitro. We investigated their effects on triglyceride (TG) deposition in 3T3- L1 adipocytes, glucose and insulin in obese mouse models, and metabolic syndrome markers in adults with metabolic syndrome. The combination of RIAA and PAC synergistically increased TG content and adiponectin secretion in 3T3-L1 adipocytes under hyperinsulinemic conditions and reduced glucose or insulin in obese mice. In a clinical trial, tablets containing 100 mg RIAA and 500 mg PAC or placebo were administered to metabolic syndrome subjects (3 tablets/day, n = 35; 6 tablets/day, n = 34; or placebo, n = 35) for 12 weeks. Compared to placebo, subjects taking 3 tablets daily showed greater reductions in TG, TG : HDL, fasting insulin, and HOMA scores. The combination of RIAA : PAC at 1 : 5 (wt : wt) favorably modulates dysregulated lipids in insulin resistance and metabolic syndrome. [ABSTRACT FROM AUTHOR]

Presents a study on transient outward potassium current (Ito) in canine heart muscle. Changes in cardiac ionic current as suggesting development of heart disease; Alterations of action potential configuration.

Introduction: A colony of inbred German shepherd dogs with inherited ventricular arrhythmias has been established. Methods and Results: The inward rectifier (IK1), the slow delayed rectifier (IKs), and the transient outward current (Ito) were recorded from epicardial myocytes, and Ito was recorded from Purkinje myocytes isolated from the left ventricles of dogs mildly or severely affected with arrhythmias, and unaffected relatives. There were no differences between unaffected and severely affected dogs in the densities of either IK1 or IKs. Peak Ito density at +40 mV was reduced by 49% in epicardial myocytes from severely affected dogs. Ito density was also reduced in a subset of Purkinje myocytes. Boltzmann analysis of steady-state inactivation showed no differences between groups in slope factor. V½ the half-inactivation voltage, was shifted by +6.2 mV in epicardial cells from severely affected versus unaffected dogs. In addition, the time constant for Ito decay was reduced in mildly and severely affected dogs compared to unaffected dogs. Conclusion: Altered density and inactivation of Ito are associated with the presence of severe ventricular arrhythmias in inbred dogs at risk for sudden death. [ABSTRACT FROM AUTHOR]