Publications by authors named "Satoru Tamaoki"
Metabolic dysfunction-associated steatohepatitis (MASH) is a progressive liver disease linked to fibrosis and hepatocellular carcinoma (HCC). Gut-derived lipopolysaccharide (LPS) promotes hepatic inflammation, fibrosis, and angiogenesis through toll-like receptor 4 (TLR4) signaling. This study examined the effects of rifaximin, a non-absorbable, gut-targeted antibiotic, on MASH-related liver fibrosis and early hepatocarcinogenesis, with a focus on the LPS-epiregulin-IL-8-angiogenesis axis.
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- Rifaximin, a broad-spectrum antibiotic used for treating hepatic encephalopathy, doesn't significantly change the overall stool microbiota but may impact microbial composition in the duodenum and jejunum due to increased bile acid levels.
- In an experiment with BALB/c mice, those treated with carbon tetrachloride (CCl) showed an increase in Lactobacillaceae in their intestines, but rifaximin treatment led to a notable decrease of this bacterial family in the duodenum and jejunum.
- Additionally, rifaximin appeared to boost Bacteroidetes levels in those same areas, suggesting a complex interaction between these bacterial populations influenced by the antibiotic treatment.
[Pharmacological properties and clinical findings of rifaximin (RIFXIMA TABLETS 200 mg)].
Nihon Yakurigaku Zasshi
October 2017
Hepatic encephalopathy (HE) is a neuropsychiatric syndrome associated with hepatic dysfunction. However, the precise mechanism of HE is unclear. To elucidate the mechanism, we developed a new rat model of HE with coma using a combination of subcutaneous splenic transposition, partial hepatectomy and portal vein stenosis.
View Article and Find Full Text PDFWe have prepared a series of quinazolinone derivatives linked with piperazinylquinoline for the treatment of irritable bowel syndrome (IBS). Using pharmacophore analysis, we designed and synthesized compounds which bind to both serotonin receptor subtype 1A (5-HT(1A)) and subtype 3 (5-HT(3)). Quinazolinone derivatives with a sulfur atom in the linker showed high affinity in in vitro assays, but low in vivo activity.
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- Researchers developed piperazinylpyridine derivatives aimed at treating irritable bowel syndrome (IBS), focusing on specific receptor interactions.
- The compounds were designed using pharmacophore analysis, highlighting crucial elements like the nitrogen atom of isoquinoline, a methoxy group, and piperazine for effective receptor binding.
- One promising compound, TZB-20810, showed strong affinity for serotonin receptors and exhibited both agonistic and antagonistic properties, indicating its potential as a therapeutic option for IBS.
3-Amino-5,6,7,8-tetrahydro-2-[4-[4-(quinolin-2-yl)piperazin-1-yl]butyl]quinazolin-4(3H)-one (TZB-30878) is a novel compound with both 5-hydroxytryptamine (5-HT)(1A) agonism and 5-HT(3) antagonism effects. We hypothesized that TZB-30878 might have benefits from these dual effects as a medication for diarrhea-predominant irritable bowel syndrome (d-IBS), and these studies were designed to confirm the pharmacological properties of TZB-30878 and its efficacy in an IBS-like animal model. The binding assays demonstrated that [(3)H]TZB-30878 selectively binds to human 5-HT(1A) and 5-HT(3) receptors, with K(d) values of 0.
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