Pharmacological profile of BR-931, a new hypolipidemic agent that increases high-density lipoproteins

Sirtori, Cesare R.; Gomarasca, P; D'Atri, G; Cerutti, Silvano; Tronconi, Gianni; Scolastico, Carlo

doi:10.1016/0021-9150(78)90151-x

Cited by 24 publications

(3 citation statements)

References 29 publications

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“…In the present study, the activity of MGO and camphene on plasma cholesterol and triglyceride levels was investigated in a rat model in which the circulating levels of total cholesterol, LDL-cholesterol and triglycerides were substantially increased by administration of the detergent, Triton WR-1339. This compound inhibits lipoprotein lipase resulting in increased cholesterol and triglycerides levels in plasma and thus it has been widely used for induction of acute hyperlipidemia [65] and for assay of putative hypocholesterolemic drugs [52], [66]–[68]. Initially, the effect of MGO was examined in naïve rats.…”

Section: Discussionmentioning

confidence: 99%

Camphene, a Plant-Derived Monoterpene, Reduces Plasma Cholesterol and Triglycerides in Hyperlipidemic Rats Independently of HMG-CoA Reductase Activity

Vallianou

Peroulis

Pantazis³

et al. 2011

PLoS ONE

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BackgroundCentral to the pathology of coronary heart disease is the accumulation of lipids, cholesterol and triglycerides, within the intima of arterial blood vessels. The search for drugs to treat dislipidemia, remains a major pharmaceutical focus. In this study, we evaluated the hypolipidemic properties of the essential oil from Chios mastic gum (MGO).Methodology/Principal FindingsThe hypolipidemic effect of MGO was investigated in naïve as well as in rats susceptible to detergent-induced hyperlipidemia. Serum cholesterol and triglycerides were determined using commercial kits. HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase activity was measured in HepG2 cell extracts using a radioactive assay; cellular cholesterol and cholesterol esters were assessed using gas chromatography. MGO administration into naïve rats resulted in a dose-dependent reduction in the constitutive synthesis of serum cholesterol and triglycerides. In hyperlipidemic rats, MGO treatment had also a strong hypolipidemic effect. By testing various components of MGO, we show for the first time that the hypolipidemic action is associated with camphene. Administration of camphene at a dose of 30 µg/gr of body weight in hyperlipidemic rats resulted in a 54.5% reduction of total cholesterol (p<0.001), 54% of Low Density Lipoprotein (LDL)-cholesterol (p<0.001) and 34.5% of triglycerides (p<0.001). Treatment of HepG2 cells with camphene led to a decrease in cellular cholesterol content to the same extend as mevinolin, a known HMG-CoA reductase inhibitor. The hypolipidemic action of camphene is independent of HMG-CoA reductase activity, suggesting that its hypocholesterolemic and hypotriglyceridemic effects are associated with a mechanism of action different than that of statins.ConclusionsGiven the critical role that the control of hyperlipidemia plays in cardiovascular disease, the results of our study provide insights into the use of camphene as an alternative lipid lowering agent and merits further evaluation.

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Section: Discussionmentioning

confidence: 99%

Camphene, a Plant-Derived Monoterpene, Reduces Plasma Cholesterol and Triglycerides in Hyperlipidemic Rats Independently of HMG-CoA Reductase Activity

Vallianou

Peroulis

Pantazis³

et al. 2011

PLoS ONE

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“…In the present study, the activity of MGO and camphene on plasma cholesterol and triglyceride levels was investigated in a rat model in which the circulating levels of total cholesterol, LDL-cholesterol and triglycerides were substantially increased by administration of the detergent, Triton WR-1339. This compound inhibits lipoprotein lipase resulting in increased cholesterol and triglycerides levels in plasma and thus it has been widely used for induction of acute hyperlipidemia [65] and for assay of putative hypocholesterolemic drugs [52,[66][67][68]. Initially, the effect of MGO was examined in naïve rats.…”

Section: Discussionmentioning

confidence: 99%

“…η θεραπεία με τις υπολιπιδαιμικές φαρμακευτικές ουσίες συνοδεύεται σε πολλές περιπτώσεις από παρενέργειες(Harper et al, 2007, Kornbrust et al, 1989, Masters et al, 1995, γεγονός που εντείνει την ανάγκη ανακάλυψης και ανάπτυξης νέων θεραπευτικών στόχων, ώστε να αντιμετωπιστούν πιο αποτελεσματικά η υπερχοληστερολαιμία και η υπερτριγλυκεριδαιμία(Bays et al, 2003, Costet, 2010. και χημικών υπολιπιδαιμικών φαρμάκων, καθώς και στη μελέτη του μεταβολισμού της χοληστερόλης και των τριγλυκεριδίων(Kourounakis et al, 2002, Sirtori et al, 1978. στον άνθρωπο(Williams et al, 2002).…”

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Μελέτη Του Μοριακού Μηχανισμού Δράσης Του Αιθέριου Ελαίου Της Μαστίχας Που Προκαλεί Υπολιπιδαιμία

Vallianou¹

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Η χοληστερόλη είναι το περισσότερο τιμημένο μικρό μόριο στη Βιολογία. Δεκατρία βραβεία Νομπέλ έχουν απονεμηθεί σε επιστήμονες οι οποίοι αφιέρωσαν το κυριότερο μέρος της έρευνάς τους στη χοληστερόλη. Από τότε που απομονώθηκε από χολόλιθους στα 1734, η χοληστερόλη έχει ασκήσει μια σχεδόν υπνωτική γοητεία στους επιστήμονες από τις περισσότερες περιοχές των θετικών επιστημών και της ιατρικής… Η χοληστερόλη είναι ένα μόριο σαν τον διπρόσωπο Ιανό. Η κύρια ιδιότητα που την κάνει χρήσιμη στις κυτταρικές μεμβράνες, δηλαδή η απόλυτη δυσδιαλυτότητά της στο νερό, την κάνει επίσης και θανατηφόρα.

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Mechanisms of Action of Absorbable Hypolipidemic Drugs

Sirtori

1985

Drugs Affecting Lipid Metabolism VIII

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Pharmacological profile of BR-931, a new hypolipidemic agent that increases high-density lipoproteins

Cited by 24 publications

References 29 publications

Camphene, a Plant-Derived Monoterpene, Reduces Plasma Cholesterol and Triglycerides in Hyperlipidemic Rats Independently of HMG-CoA Reductase Activity

Camphene, a Plant-Derived Monoterpene, Reduces Plasma Cholesterol and Triglycerides in Hyperlipidemic Rats Independently of HMG-CoA Reductase Activity

Μελέτη Του Μοριακού Μηχανισμού Δράσης Του Αιθέριου Ελαίου Της Μαστίχας Που Προκαλεί Υπολιπιδαιμία

Mechanisms of Action of Absorbable Hypolipidemic Drugs

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