Synthesis and biological evaluation of molecular probes based on the 9-methylstreptimidone derivative DTCM-glutarimide

Ota, Eisuke; Takeiri, Masatoshi; Tachibana, Miyuki; Ishikawa, Yuichi; Umezawa, Kazuo; Nishiyama, Shigeru

doi:10.1016/j.bmcl.2011.11.045

Cited by 8 publications

(12 citation statements)

References 17 publications

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“…Treatments were administered intraperitoneally twice daily for 5 days in all groups. DTCM-G and DHMEQ were synthesized as described previously (52–55). The rats were monitored frequently, and those that showed any signs of pain were injected subcutaneously with 1 ml Temgesic solution (containing 0.3 g/ml Temgesic; Merck & Co., Inc., Kenilworth, NJ, USA) as an analgesic.…”

Section: Methodsmentioning

confidence: 99%

Abnormal differentiation of stem cells into enteroendocrine cells in rats with DSS-induced colitis

Umezawa

Hatlebakk

Gilja

2017

Molecular Medicine Reports

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The present study aimed to determine whether there is an association between abnormalities in enteroendocrine cells in dextran sulfate sodium (DSS)-induced colitis and the clonogenic and/or proliferative activities of stem cells. A total of 48 male Wistar rats were divided into four groups. Animals in the control group were provided with normal drinking water, whereas DSS colitis was induced in the remaining three groups. The rats with DSS-induced colitis were randomized into the following three groups: i) DSS group, which received 0.5 ml 0.5% carboxymethyl cellulose (CMC; vehicle); ii) DSS-G group, which was treated with 3-[(dodecylthiocarbonyl)-methyl]-glutarimide at 20 mg/kg body weight in 0.5% CMC; and iii) DSS-Q group, which was treated with dehydroxymethylepoxyquinomicin at 15 mg/kg body weight in 0.5% CMC. Treatments were administered intraperitoneally twice daily for 5 days in all groups. Subsequently, tissue samples from the colon were stained with hematoxylin-eosin, or immunostained for chromogranin A (CgA), Musashi 1 (Msi1), Math-1, neurogenin 3 (Neurog3) and neurogenic differentiation D1 (NeuroD1). The densities of CgA, Msi1-, Math-1-, Neurog3- and NeuroD1-immunoreactive cells were determined. DTCM-G, and DHMEQ ameliorated the inflammation in DSS-induced colitis. The density of CgA-, Neurog3- and NeuroD1-immunoreactive cells was significantly higher in the DSS group compared with in the control group, and the density of CgA cells was correlated with the densities of Neurog3- and NeuroD1-immunoreactive cells. There were no significant differences in the densities of Msi1- and Math-1-immunoreactive cells among the four experimental groups. The elevated densities of enteroendocrine cells detected in DSS-induced colitis may be due to the increased differentiation of early enteroendocrine progenitors during secretory lineage. It is probable that the DSS-induced inflammatory processes trigger certain signaling pathways, which control differentiation of the stem-cell secretory lineage into mature enteroendocrine cells.

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Section: Methodsmentioning

confidence: 99%

Abnormal differentiation of stem cells into enteroendocrine cells in rats with DSS-induced colitis

Umezawa

Hatlebakk

Gilja

2017

Molecular Medicine Reports

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“…The infrared (IR), 1H-NMR, and MS data of all the products are in good agreement with their structures. In addition, the melting points correspond to those of the literature 32 as well as the authentic samples prepared from the previously conventional reported methods.…”

Section: Resultsmentioning

confidence: 99%

“…Several substituted pyrrolidine display important biological properties like anticancer 16 , inhibitors of alpha-glucosidase 17 , antimicrobial 18 and other applications [19][20][21][22][23][24][25] . The structural diversity and industrial and biological importance of cyclic imides have made them an attractive target for synthesis over many and justify continuing efforts in the development of new synthetic strategy [26][27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44] .…”

Section: Introductionmentioning

confidence: 99%

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Green synthesis and antimicrobial evaluation of N-aryl cyclic imides using silica bound benzyl chloride mediated solid phase synthesis

2018

IJGHC

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“…All injections were administered intraperitoneally twice daily for 5 days. The synthesis of DTCM-G and DHMEQ is described in detail elsewhere (29–34). Animals exhibiting signs of pain were administered a subcutaneous injection of 1 ml of a 0.3-g/ml Temgesic solution (Merck Pharmaceuticals, Kenilworth, NJ, USA).…”

Section: Methodsmentioning

confidence: 99%

Enteroendocrine cells, stem cells and differentiation progenitors in rats with TNBS-induced colitis

Mazzawi

Umezawa

Gilja

2016

International Journal of Molecular Medicine

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Patients with inflammatory bowel disease (IBD), as well as animal models of human IBD have abnormal enteroendocrine cells. The present study aimed to identify the possible mechanisms underlying these abnormalities. For this purpose, 40 male Wistar rats were divided into 4 groups as follows: the control group, the group with trinitrobenzene sulfonic acid (TNBS)-induced colitis with no treatment (TNBS group), the group with TNBS-induced colitis treated with 3-[(dodecylthiocarbonyl)-methyl]-glutarimide (DTCM-G; an activator protein-1 inhibitor) (DTCM-G group), and the group with TNBS-induced colitis treated with dehydroxymethylepoxyquinomicin (DHMEQ; a nuclear factor-κB inhibitor) treatment (DHMEQ group). Three days following the administration of TNBS, the rats were treated as follows: those in the control and TNBS groups received 0.5 ml of the vehicle [0.5% carboxymethyl cellulose (CMC)], those in the DTCM-G group received DTCM-G at 20 mg/kg body weight in 0.5% CMC, and those in the DHMEQ group received DHMEQ at 15 mg/kg body weight in 0.5% CMC. All injections were administered intraperitoneally twice daily for 5 days. The rats were then sacrificed, and tissue samples were taken from the colon. The tissue sections were stained with hemotoxylin-eosin and immunostained for chromogranin A (CgA), serotonin, peptide YY (PYY), oxyntomodulin, pancreatic polypeptide (PP), somatostatin, Musashi1 (Msi1), Math1, Neurogenin3 (Neurog3) and NeuroD1. The staining was quantified using image analysis software. The densities of CgA-, PYY-, PP-, Msi1-, Neurog3- and NeuroD1-positive cells were significantly lower in the TNBS group than those in the control group, while those of serotonin-, oxyntomodulin- and somatostatin-positive cells were significantly higher in the TNBS group than those in the control group. Treatment with either DTCM-G or DHMEQ restored the densities of enteroendocrine cells, stem cells and their progenitors to normal levels. It was thus concluded that the abnormalities in enteroendocrine cells and stem cells and their differentiation progenitors may be caused by certain signaling substances produced under inflammatory processes, resulting in changes in hormone expression in enteroendocrine cells. These substances may also interfere with the colonogenic activity and the differentiation of the stem-cell secretory lineage into mature enteroendocrine cells.

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Synthesis and biological evaluation of molecular probes based on the 9-methylstreptimidone derivative DTCM-glutarimide

Cited by 8 publications

References 17 publications

Abnormal differentiation of stem cells into enteroendocrine cells in rats with DSS-induced colitis

Abnormal differentiation of stem cells into enteroendocrine cells in rats with DSS-induced colitis

Green synthesis and antimicrobial evaluation of N-aryl cyclic imides using silica bound benzyl chloride mediated solid phase synthesis

Enteroendocrine cells, stem cells and differentiation progenitors in rats with TNBS-induced colitis

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