Month: May 2024

Metabolomic analysis of diet-induced obese mice supplemented with eicosapentaenoic acid was written by Nishitani, Shigeki;Fukuhara, Atsunori;Jinno, Yasutaka;Kawano, Hiroyuki;Yano, Takashi;Otsuki, Michio;Shimomura, Iichiro. And the article was included in Experimental and Clinical Endocrinology & Diabetes in 2020.Electric Literature of C4H7NO2S This article mentions the following:

Eicosapentaenoic acid (EPA) is an omega-3 fatty acid with anti-inflammatory effects. To determine the effects of EPA on metabolic pathways in obese adipose tissues and liver, mice were fed normal chow diet (NCD), high-fat diet (HFD), or 3% EPA-containing high fat diet (HFD+EPA) for 8 wk. Metabolomic anal. was performed using epididymal adipose tissues (epi WAT) and liver. Metabolites that were specifically elevated in HFD+EPA, were assessed for their anti-inflammatory properties using RAW264.7 macrophage cells. Body and adipose tissue weights were significantly higher in HFD than NCD, and lower in HFD+EPA than HFD. Plasma insulin levels were significantly higher in HFD than NCD, and lower in HFD+EPA compared with HFD. Plasma monocyte chemotactic protein-1 (MCP-1) levels were higher in HFD than NCD, and tended to be lower in HFD+EPA than HFD. The levels of intermediate metabolites in the glycolytic pathways were lower in HFD compared with NCD and HFD+EPA in both epi WAT and liver, while intermediate metabolites of the TCA cycles were elevated in HFD and HFD+EPA compared with NCD in epi WAT. Among the metabolites in epi WAT, the levels of thiaproline, phenaceturic acid, and pipecolic acid were specifically elevated in HFD+EPA, but not in HFD or NCD. Treatment of RAW264.7 cells with thiaproline significantly ameliorated LPS-induced iNOS expression, while pipecolic acid inhibited LPS-induced IL-1β expression. These results suggest that EPA normalizes glycolytic pathway intermediates in both epi WAT and liver, and induces metabolites with anti-inflammatory properties. In the experiment, the researchers used many compounds, for example, Thiazolidine-4-carboxylic acid (cas: 444-27-9Electric Literature of C4H7NO2S).

Thiazolidine-4-carboxylic acid (cas: 444-27-9) belongs to thiazolidine derivatives. The thiazolidine ring is a cyclic N,S acetal, and most syntheses of perhydrothiazolo [3,2-a]pyridines construct the five-membered ring by condensation of aldehydes or ketones either as such or masked. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Electric Literature of C4H7NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Unique anti-myeloma activity by thiazolidine-2,4-dione compounds with Pim inhibiting activity was written by Fujii, Shiro;Nakamura, Shingen;Oda, Asuka;Miki, Hirokazu;Tenshin, Hirofumi;Teramachi, Jumpei;Hiasa, Masahiro;Bat-Erdene, Ariunzaya;Maeda, Yusaku;Oura, Masahiro;Takahashi, Mamiko;Iwasa, Masami;Endo, Itsuro;Yoshida, Sumiko;Aihara, Ken-ichi;Kurahashi, Kiyoe;Harada, Takeshi;Kagawa, Kumiko;Nakao, Michiyasu;Sano, Shigeki;Abe, Masahiro. And the article was included in British Journal of Haematology in 2018.Formula: C13H13NO3S This article mentions the following:

Proviral integrations of Moloney virus 2 (PIM2) is overexpressed in multiple myeloma (MM) cells, and regarded as an important therapeutic target. Here, we aimed to validate the therapeutic efficacy of different types of PIM inhibitors against MM cells for their possible clin. application. Intriguingly, the thiazolidine-2,4-dione-family compounds SMI-16a and SMI-4a reduced PIM2 protein levels and impaired MM cell survival preferentially in acidic conditions, in contrast to other types of PIM inhibitors, including AZD1208, CX-6258, and PIM447. SMI-16a also suppressed the drug efflux function of breast cancer resistance protein, minimized the sizes of side populations and reduced in vitro colony-forming capacity and in vivo tumorigenic activity in MM cells, suggesting impairment of their clonogenic capacity. PIM2 is known to be subject to ubiquitination-independent proteasomal degradation Consistent with this, the proteasome inhibitors bortezomib and carfilzomib increased PIM2 protein levels in MM cells without affecting its mRNA levels. However, SMI-16a mitigated the PIM2 protein increase and cooperatively enhanced anti-MM effects in combination with carfilzomib. Collectively, the thiazolidine-2,4-dione-family compounds SMI-16a and SMI-4a uniquely reduce PIM2 protein in MM cells, which may contribute to their profound efficacy in addition to their immediate kinase inhibition. Their combination with proteasome inhibitors is envisioned. In the experiment, the researchers used many compounds, for example, 5-(4-propoxybenzylidene)thiazolidine-2,4-dione (cas: 587852-28-6Formula: C13H13NO3S).

5-(4-propoxybenzylidene)thiazolidine-2,4-dione (cas: 587852-28-6) belongs to thiazolidine derivatives. Thiazolidine is an important scaffold and has a wide range of promising biological activities. Thiazolidine derivatives have reported anti-inflammatory and anti-nociceptive activity. Thiazolidines unsubstituted on the nitrogen atom are readily hydrolyzed by boiling aqueous solutions of acids or bases and the dissociation is complete in the presence of a compound reacting with one of the cleavage products.Formula: C13H13NO3S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com