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1

Role of chicoric acid and 13-cis retinoic acid in Mycobacterium tuberculosis infection control by human U937 macrophage

100%
Abd-Nikfarjam B., Nassiri-Asl M., Hajiaghayi M., Farivar T. N.
Archivum Immunologiae et Therapiae Experimentalis
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2018
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tom 66
|
nr 5
2

5'-Esters of 2'-deoxyadenosine and 2-chloro-2'-deoxyadenosine with cell differentiation-provoking agents

100%
Grieb P., Kryczka T., Wojtowicz R., Kawiak J., Kazimierczuk Z.
Acta Biochimica Polonica
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2002
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tom 49
|
nr 1
Phenylacetic and retinoic acids are carboxyacidic cell differentiating agents display­ing anticancer activities. We report on a new class of compounds including the 5'-es- ters of 2'-deoxyadenosine (dA) or 2-chloro-2'-deoxyadenosine (cladribine, 2CdA) and the aforementioned acids. The rationale behind the synthesis of these esters was that if they are hydrolyzed inside the lymphoid cells, either dA will be removed from the intracellular environment by deamination, or 2CdA will be phosphorylated and accu­mulated. In either case targetted delivery of the differentiating agent to the lymphoid cells may be envisaged. The said compounds were synthesized by the Mitsunobu pro­cedure employing triphenylphosphine and azadicarboxylic acid esters, and their sta­bility was tested against various esterases. Esters of dA and 2CdA with phenylacetic acids were found to be resistant to enzymatic hydrolysis, whereas those with retinoic acids were efficiently hydrolyzed by commercially available hepatic esterase as well as by esterases present in the blood plasma and in diluted human lymphocyte lysate. Susceptibility to enzymatic hydrolysis was found to be a prerequisite of cytotoxic and/or differentiating activity of these esters in leukemic cell lines.
3
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Short term 13-cis-retinoic acid treatment at therapeutic doses elevates expression of leptin, GLUT4, PPARgamma and aP2 in rat adipose tissue

80%
Krskova-Tybitanclova K., Macejova D., Brtko J., Baculikova M., Krizanova O., Zorad S.
Journal of Physiology and Pharmacology
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2008
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tom 59
|
nr 4
731-743
Temporary defects in the plasma lipid and glucose homeostasis are frequent complication accompanying chronic treatment with 13-cis-retinoic acid (13cRA). White adipose tissue acts as an endocrine organ producing a variety of hormones (adipocytokines) including leptin, adiponectin, tumor-necrosis factor alpha (TNF) and angiotensin II (Ang II), which influence lipid metabolism, systemic insulin sensitivity and inflammation. To study the effect of a short-term 13cRA administration on metabolism of epididymal fat tissue, we treated Wistar rats with five identical therapeutic doses of 13cRA (0.8 mg/kg b.w.) by gavage during a period of 10 days. Expression of adiponectin, leptin, TNF and selected proteins such as adipocyte fatty acid binding protein (aP2), insulin-dependent glucose transporter GLUT4, peroxisome proliferator-activated receptor gamma (PPAR) and retinoid X receptors (RXRs) was investigated using RT-PCR. Short-term treatment with therapeutic doses of 13cRA caused significant increase of the aP2, PPAR and moderately RXR gene expression. Similarly, the relative amount of mRNA for leptin and GLUT4 was increased, while the TNF transcript was decreased after treatment with 13cRA. The gene expression and plasma concentration of adiponectin were without any significant changes. Since local adipose renin-angiotensin system (RAS) has been presumed to be involved in the regulation of fat tissue metabolism, we also investigated the gene expression of RAS components in epididymal fat depot. Our data has shown that 13cRA elevated Ang II receptor type 1 (AT1 receptor) - at both, mRNA and protein level. Thus, our results demonstrate that short-term 13cRA treatment is inducing alterations in fat tissue metabolism in relation to stimulated adipogenesis.
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