Synthesis and Biological Evaluation of Peripheral 5HT Antagonists for Liver Fibrosis.

Liver fibrosis is characterized by an excessive accumulation of extracellular matrix components, leading to the distortion of liver architecture and function. Recent studies have shown that antagonizing 5-hydroxytryptamine receptor 2B (5HT) stimulates the apoptosis of activated hepatic stellate cells and inhibits their proliferation while concurrently regressing hepatocyte proliferation. In this study, we present compound , which demonstrates promising efficacy both and .

Structure-activity relationship analysis of mono-methylated quercetins by comprehensive MS/MS analysis and anti-proliferative efficacy in human colorectal cancer cells.

Flavonoids and their derivatives are known for their diverse biological activities. This study aims to elucidate the structure-activity relationships (SARs) of flavonoids, including fisetin, luteolin, quercetin, and mono-methylated quercetins (MQs), with a focus on their potential as therapeutic agents for colorectal cancer (CRC). Using electrospray ionization tandem mass spectrometry (ESI-QTOF MS/MS) and retro Diels-Alder (rDA) analysis, we developed a novel analytical method to differentiate between MQs, despite their identical molecular weights, by analyzing their unique fragmentation patterns.

Serotonin Regulates Lipogenesis and Endoplasmic Reticulum Stress in Alcoholic Liver Disease.

Background: Serotonin (5-hydroxytryptamine [5-HT]) is a monoamine neurotransmitter that has various functions in central and peripheral tissues. While 5-HT is known to regulate various biological processes in liver, direct role of 5-HT and its receptors, especially 5-HT receptor 2A (HTR2A) and HTR2B, in development and progression of alcoholic liver disease (ALD) in vivo is not well understood.

Methods: Blood 5-HT level was measured from both human ALD patients and ethanol (EtOH) diet-fed mouse models.

Synergistic effects of L-arginine and argininosuccinate synthetase 1 in inducing apoptosis in hepatocellular carcinoma.

Background/aims: Hepatocellular carcinoma (HCC) is a malignant cancer with an increasing incidence worldwide. Although numerous efforts have been made to identify effective therapies for HCC, current strategies have limitations. We present a new approach for targeting L-arginine and argininosuccinate synthetase 1 (ASS1).

Synthesis and Biological Evaluation of Peripheral HTR2A Antagonists for Colorectal Cancer.

Colorectal cancer is a prevalent and prominent contributor to global cancer-related fatalities with challenges in drug resistance and metastasis. Recent research highlights the potential relationship between serotonin and cancer. 5-Hydroxytryptamine receptor 2A (HTR2A) mRNA expression in colorectal cancer cells was found to be notably elevated compared to that in normal colon cells.

Pyramidal cell types and 5-HT receptors are essential for psilocybin's lasting drug action.

Psilocybin is a serotonergic psychedelic with therapeutic potential for treating mental illnesses. At the cellular level, psychedelics induce structural neural plasticity, exemplified by the drug-evoked growth and remodeling of dendritic spines in cortical pyramidal cells. A key question is how these cellular modifications map onto cell type-specific circuits to produce psychedelics' behavioral actions.

Mast cell-derived BH4 and serotonin are critical mediators of postoperative pain.

Postoperative pain affects most patients after major surgery and can transition to chronic pain. The considerable side effects and limited efficacy of current treatments underline the need for new therapeutic options. We observed increased amounts of the metabolites BH4 and serotonin after skin injury.

PRMT1 promotes pancreatic cancer development and resistance to chemotherapy.

Pancreatic ductal adenocarcinoma (PDAC) remains one of the most lethal types of cancer, and novel treatment regimens are direly needed. Epigenetic regulation contributes to the development of various cancer types, but its role in the development of and potential as a therapeutic target for PDAC remains underexplored. Here, we show that PRMT1 is highly expressed in murine and human pancreatic cancer and is essential for cancer cell proliferation and tumorigenesis.

Ethyl acetate fraction of Osmanthus fragrans var. aurantiacus and its triterpenoids suppress proliferation and survival of colorectal cancer cells by inhibiting NF-κB and COX2.

Ethnopharmacological Relevance: Colorectal cancer (CRC) remains a significant global health concern, and targeting inflammation has emerged as a promising approach for its prevention and treatment. Medicinal plants and phytochemicals have garnered attention for their potential efficacy against inflammation with minimal toxicity. Osmanthus fragrans var.

Multiparity increases the risk of diabetes by impairing the proliferative capacity of pancreatic β cells.

Pregnancy imposes a substantial metabolic burden on women, but little is known about whether or how multiple pregnancies increase the risk of maternal postpartum diabetes. In this study, we assessed the metabolic impact of multiple pregnancies in humans and in a rodent model. Mice that underwent multiple pregnancies had increased adiposity, but their glucose tolerance was initially improved compared to those of age-matched virgin mice.

Antioxidant and Anti-Inflammatory Activities of High-Glucosinolate-Synthesis Lines of .

Excessive oxidative stress and inflammatory responses are associated with the development of various diseases, including cancer. Glucosinolates (GSLs) are phytochemicals known for their antioxidant properties, and doubled haploid lines (DHLs) of with high GSL contents (HGSL) were intentionally developed from two edible subspecies of : subsp. and subsp.

Synthesis and biological evaluation of xanthine derivatives with phenacyl group as tryptophan hydroxylase 1 (TPH1) inhibitors for obesity and fatty liver disease.

Tryptophan hydroxylase 1 (TPH1) has emerged as a target for the treatment of metabolic diseases including obesity and fatty liver disease. A series of xanthine derivatives were synthesized and evaluated for their TPH1 inhibition. Among the synthesized compounds, compound 40 showed good in vitro activity and liver microsomal stability.

Adipose Tissue-Derived Mesenchymal Stem Cell-Derived Exosomes Promote Wound Healing and Tissue Regeneration.

Wound healing is a complex process involving cell proliferation, migration, and extracellular matrix (ECM) remodeling. Extracellular vesicles (EVs) or exosomes derived from adipose tissue-derived stem cells (ASCs) are emerging as promising alternatives to cell therapy for advanced wound healing. Hyaluronic acid (HA), a major component of the skin ECM, is widely utilized in wound dressings and dermal fillers.

Expression patterns of AEG-1 in the normal brain.

Astrocyte elevated gene-1 (AEG-1) is a well-known oncogene implicated in various types of human cancers, including brain tumors. Recently, AEG-1 has also been reported to play pivotal roles in glioma-associated neurodegeneration and neurodegenerative diseases like Parkinson's disease and amyotrophic lateral sclerosis. However, the normal physiological functions and expression patterns of AEG-1 in the brain are not well understood.

Arginine 65 methylation of Neurogenin 3 by PRMT1 is required for pancreatic endocrine development of hESCs.

Neurogenin 3 (NGN3) is a key transcription factor in the cell fate determination of endocrine progenitors (EPs) in the developing pancreas. Previous studies have shown that the stability and activity of NGN3 are regulated by phosphorylation. However, the role of NGN3 methylation is poorly understood.

Anticancer Effects of High Glucosinolate Synthesis Lines of on Colorectal Cancer Cells.

Chemoprevention is a method of health control in modern industrialized societies. Traditional breeding (hybridization) has been widely used to produce new (sub)species with beneficial phenotypes. Previously, we produced a number of doubled haploid (DH) lines of with a high glucosinolate (GSL) content.

Anti-Cancer Effects of a New Herbal Medicine PSY by Inhibiting the STAT3 Signaling Pathway in Colorectal Cancer Cells and Its Phytochemical Analysis.

Colorectal cancer (CRC) is an inflammation-associated common cancer worldwide. Paejang-san and Mori Cortex Radicis have been traditionally used for treating intestinal inflammatory diseases in Korea and China. In the present study, we developed a new herbal formula as an alternative to CRC treatments, which is composed of two main components of Paejangsan (Patriniae Radix (Paejang in Korean) and Coix Seed (Yiyiin in Korean)), and Mori Cortex Radicis (Sangbekpi in Korean) based on the addition and subtraction theory in traditional medicine, hence the name PSY, and explored the potential therapeutic effects of the new formula PSY in human CRC cells by analyzing viability, cell cycle and apoptosis.

Serotonin in the regulation of systemic energy metabolism.

Serotonin is a well-known neurotransmitter that is synthesized from the amino acid, tryptophan. To date, more than 14 different serotonin receptors have been discovered; they exist universally in our body and enable diverse biological functions in different organs. Central serotonin regulates mood and behavior, and impacts the systemic energy balance by decreasing appetite.

Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT receptor antagonists for nonalcoholic fatty liver disease.

Non-alcoholic fatty liver disease (NAFLD), attributed to excessive fat accumulation in the liver, is reportedly prevalent worldwide. NAFLD is one of the leading causes of chronic liver disease, including non-alcoholic steatohepatitis (NASH), cirrhosis, and hepatic cellular carcinoma (HCC). The peripheral roles of serotonin (5-hydroxytryptamine, 5HT) were found to regulate hepatic lipid metabolism.