scholarly journals Atherogenic characteristics of oral sugar-reducing sulfonylurea derivatives

1994 ◽  
Vol 40 (3) ◽  
pp. 8-10
Author(s):  
M. A. Maxumova ◽  
I. A. Sobenin ◽  
M. I. Balabolkin ◽  
A. N. Orekhov
Keyword(s):  
Peritoneal Macrophages ◽  
Cholesterol Levels ◽  
Murine Peritoneal Macrophages ◽  
Sulfonylurea Drugs

The authors have examined the effects of sulfonylurea drugs glybenclamide and glypizide and of their analogs manilil and minidiab on cholesterol levels in murine peritoneal macrophages. Both glybenclamide and glypizide had a direct atherogenic effect on cultured murine peritoneal macrophages. A similar effect was observed in vivo: blood sera of diabetics after a single intake of 5 mg of manilil or minidiab increased the atherogenic potential of cultured murine peritoneal macrophages.

Immunocytochemical Analysis of Murine Peritoneal Macrophages Treated with “Poly-Plat”, an in Vitro and in Vivo Study

1998 ◽  
Vol 4 (S2) ◽  
pp. 1122-1123
Author(s):  
H. J. Muenchen ◽  
S.K. Aggarwal
Keyword(s):  
Immune System ◽  
Mechanism Of Action ◽  
Second Generation ◽  
Peritoneal Macrophages ◽  
In Vivo Study ◽  
Immunocytochemical Analysis ◽  
Murine Peritoneal Macrophages

Poly-[(trans-1,2-diaminocyclohexane) platinumj-carboxyamylose (“poly-plat“) is a second generation analog of cisplatin which enhances the immune system with greater efficacy in vitro and in vivo “Poly-plat” contains 1/5 the platinum of CDDP and demonstrates less toxicity. In order to understand the mechanism of action of this compound an in vitro and in vivo study was performed. Swiss Webster mice and isolated murine peritoneal macrophages were treated with “poly-plat” (10 mg/kg). The Swiss Webster mice were given bolus injections and sacrificed at 2 and 12 days. Peritoneal macrophages were then isolated and allowed to incubate in culture for 24 h. Peritoneal macrophages were also isolated from normal mice and treated with the drugs for 2 h. After treatments the macrophages were placed in fresh media and allowed to incubate 24 h. Supematants were isolated at various times during culture for immunocytochemical analysis.Both in vitro and in vivo studies showed enhanced immunostimulation after their respective treatments.

scholarly journals Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity

PLoS ONE ◽  
2021 ◽  
Vol 16 (11) ◽  
pp. e0259008
Author(s):  
Leandro da Costa Clementino ◽  
Guilherme Felipe Santos Fernandes ◽  
Igor Muccilo Prokopczyk ◽  
Wilquer Castro Laurindo ◽  
Danyelle Toyama ◽  
...  
Keyword(s):  
Parasite Burden ◽  
Peritoneal Macrophages ◽  
Biological Evaluation ◽  
Antileishmanial Activity ◽  
Dual Effect ◽  
Design Synthesis ◽  
Murine Peritoneal Macrophages ◽  
Synthesis And Biological Evaluation

Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 μM against L. infantum amastigote forms and CC50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.

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