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Rudolf Gesztelyi,Zita Wachal,Bela Juhasz,Mariann Bombicz,Evelin Csepanyi,Krisztian Pak,Judit Zsuga,Csaba Papp,Zoltan Galajda,Klara Branzaniuc,Robert Porszasz,Andras Jozsef Szentmiklosi,Arpad Tosaki,Zs 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.3
A1 adenosine receptors (A1 receptors) arewidely expressed in mammalian tissues; therefore attainingproper tissue selectivity is a cornerstone of drug development. The fact that partial agonists chiefly act on tissueswith great receptor reserve can be exploited to achieve anappropriate degree of tissue selectivity. To the best of ourknowledge, the A1 receptor reserve has not been yetquantified for the atrial contractility. A1 receptor reservewas determined for the direct negative inotropic effect ofthree A1 receptor full agonists (NECA, CPA and CHA) inisolated, paced guinea pig left atria, with the use of FSCPX, an irreversible A1 receptor antagonist. FSCPXcaused an apparently pure dextral displacement of theconcentration–response curves of A1 receptor agonists. Accordingly, the atrial A1 receptor function converging toinotropy showed a considerably great, approximately80–92 % of receptor reserve for a near maximal (about91–96 %) effect, which is greater than historical atrial A1receptor reserve data for any effects other than inotropy. Consequently, the guinea pig atrial contractility is verysensitive to A1 receptor stimulation. Thus, it is worthwhileconsidering that even partial A1 receptor agonists, given inany indication, might decrease the atrial contractile force,as an undesirable side effect, in humans.
Istvan Bak,Istvan Lekli,Bela Juhasz,Edit Varga,Balazs Varga,Rudolf Gesztelyi,Levente Szendrei,Arpad Tosaki 한국식품영양과학회 2010 Journal of medicinal food Vol.13 No.4
A plant-based diet reduces the risk for the development of several chronic diseases, such as ischemic heart disease or cancer due to natural compounds found in plants. Numerous cereals, berries, fruits, and vegetables, including sour cherry (Prunus cerasus), which is a favored fruit worldwide, contain biological active components. The antioxidant components of the sour cherry seed kernel have not been investigated until now. The aim of our study was to isolate and analyze the bioactive constituents of sour cherry seed kernel. We separated the oil fraction of the kernel; then the remaining solid fraction was dried, and the oil-free kernel extract was further analyzed. Our results show that sour cherry seed kernel oil contains vegetable oils including unsaturated fatty acids, oleic acids, α-tocopherol, tocotrienols, and tocopherol-like components. The components of the solid fraction include various bioactive structures such as polyphenols, flavonoids, vegetable acids, and pro- and anthocyanidins, which could have useful therapeutic effects in the prevention of various vascular diseases.
Sedigh Bayegan1,Laszlo Majoros,Gabor Kardos,Adam Kemény-Beke,Cecilia Miszti,Renato Kovacs,Rudolf Gesztelyi 한국미생물학회 2010 The journal of microbiology Vol.48 No.2
We investigated the activity of caspofungin against a Candida tropicalis clinical isolate showing paradoxical growth in vitro. BALB/c mice immunosuppressed by cyclophosphamide were infected intraperitoneally using 107 CFU/mouse. Caspofungin was administered intraperitoneally once daily for 5 days or as a single dose using the following doses: 0.12, 0.25, 1, 2, 3, 5, and 15 mg/kg. The single dose of caspofungin was effective only at 5 and 15 mg/kg concentrations (100% survival). Five-day caspofungin treatment led to 100% survival at doses of 1 mg/kg or higher. Caspofungin treatment significantly decreased the number of viable yeasts in the peritoneal lavage samples as well as in the infected abscesses at doses 1, 3, 5, and 15 mg/kg caspofungin as compared to the untreated control (P<0.001 in all cases), and even to the group treated with 0.12 mg/kg caspofungin (P<0.05 in all cases). At 2 mg/kg caspofungin dose, sterilization of the internal organs was reproducibly incomplete, suggesting that the role of paradoxical growth in the late clinical failure cannot be excluded.