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Browsing by Subject "Azaphenothiazines"

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    Therapeutic effects of an azaphenothiazine derivative in mouse experimental colitis
    (Universidad de Murcia, Departamento de Biologia Celular e Histiologia, 2020) Artym, Jolanta; Kocięba, Maja; Zaczyńska, Ewa; Zimecki, Michał; Kałas, Wojciech; Strządała, Leon; Pawlak, Alicja; Jeleń, Małgorzata; Morak Młodawska, Beata; Pluta, Krystian; Kaleta Kuratewicz, Katarzyna; Madej, Jan P.; Kuropka, Piotr; Kuryszko, Jan
    Phenothiazines represent a class of compounds of potential therapeutic utility. In this report we evaluated therapeutic value of an azaphenothiazine derivative, 6-acetylaminobutyl-9-chloroquino[3,2- b]benzo[1,4]thiazine (QBT), given intragastrically, in the model of dextran sodium sulfate-induced colitis in C57BL/6 mice using 5-aminosalicylic acid (5-ASA) as a reference drug. Colitis symptoms such as body weight loss, diarrhea and hematochezia (blood in stool) were observed and registered and disease activity index (DAI) was calculated. In addition, weight and cell numbers in the lymphatic organs and histological parameters of the colon wall were analyzed. The effects of QBT on viability of colon epithelial cell lines were also determined. We showed that weight and cell number of draining mesenteric lymph nodes were lower in mice treated with QBT in comparison to their control counterparts. The number of thymocytes, drastically reduced in control mice, was elevated in mice treated with the compounds with a significant effect of 5-ASA. In addition, an abnormal composition of blood cell types was partially corrected in these groups. Histological analysis of the colon revealed that the pathological changes were partially normalized by QBT and even to a higher degree by 5-ASA. In conclusion we demonstrated a therapeutic efficacy of the compound in amelioration of local and systemic pathological changes associated with chemically-induced colitis in mice. A possible mechanism of action of the compound is discussed.
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    Topically applied azaphenothiazines inhibit contact sensitivity to oxazolone in mice
    (Universidad de Murcia. Departamento de Biología Celular e Histología, 2018) Artym, Jolanta; Kocięba, Maja; Zaczyńska, Ewa; Zimecki, Michał; Jeleń, Małgorzata; Morak Młodawska, Beata; Pluta, Krystian; Kaleta Kuratewicz, Katarzyna; Madej, Jan P.; Kuropka, Piotr; Kuryszko, Jan
    In this work we investigated the efficacy of two topically applied azaphenothiazine derivatives, 9- c h l o r o - 6 - a c e t y l ami n o b u t y l q u i n o b e n z o [ 3 , 2 - b][1,4]thiazine (compound 4) and 6-chloroethylureidoethyldiquino[3,2-b;2’;3’-e][1,4]thiazine (compound 5), in the amelioration of inflammatory symptoms of contact sensitivity (CS) to oxazolone in mice, in relation to the commercial ointment Protopic® (tacrolimus), the reference drug. The compounds were administered 24 h following elicitation of CS and, 24 h later, the parameters of inflammation, such as ear edema, blood composition, leukocyte level, numbers of cells in the draining lymph nodes, histological picture of the inflamed tissue, and the morphometric analysis, were analyzed. The study showed that the effectiveness of the studied azaphenothiazines applied as a 0.1% ointment was comparable to the reference drug regarding suppression of the inflammatory process, when all the investigated histological parameters are taken into account.

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