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nicotinic acid (nicotinic acid ER / Niaspanor / Niaspan)

✓ Approved

Merck KGaA · HCAR2 · 小分子

什么是 nicotinic acid？

nicotinic acid 是一种小分子，由Merck KGaA研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名nicotinic acid ER, Niaspanor, Niaspan
公司Merck KGaA
药物类别小分子
分子靶点HCAR2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merck KGaA

作用机制

分子靶点

nicotinic acid 作用于 1 个分子靶点：

HCAR2hydroxycarboxylic acid receptor 2 (NIACR1, GPR109A)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

nicotinic acid 针对 8 个适应症，涉及 4 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersArteriosclerosis✓ Approved
Metabolism and nutrition disordersHypercholesterolaemia✓ Approved
Metabolism and nutrition disordersHypertriglyceridaemia✓ Approved
Cardiac disordersMyocardial infarction✓ Approved
Metabolism and nutrition disordersDyslipidaemia✓ Approved

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相关研究文献

PubMedThe Journal of biological chemistry2026-08-06

Peptides containing SARS-CoV-2 spike-protein residues are antagonists of α7 and α9α10 nAChRs and modulate interleukin-1β release from human monocytes.

Hone Arik J AJ, Richter Katrin K, Riaz Zoha Z, Wakkuri Joseph J et al.

Immune system dysregulation during COVID-19 illness remains an area of intense investigation. Excessive release of proinflammatory cytokines and multi-organ injury suggest aberrant control of the immune system. Given the established role of nicotinic acetylcholine receptors (nAChRs) in modulating inflammatory responses, we explored the possibility that the SARS-CoV-2 spike-protein may directly perturb this regulatory pathway. The spike protein contains a furin cleavage-site with sequence similarities to α-neurotoxins known to antagonize α7, α9, and α10 nAChR subtypes. To test whether this region of the spike protein can influence nAChR function, we synthesized short peptides corresponding to putative nAChR-interacting domains from several SARS-CoV-2 variants. Electrophysiological recordings from Xenopus laevis oocytes expressing human nAChRs revealed potent, virus-variant dependent inhibition of nAChR activity. In human monocytic THP-1 cells, these peptides reversed acetylcholine-mediated suppression of interleukin-1β release. Our findings identify a potential molecular mechanism by which SARS-CoV-2 may directly suppress nAChR signaling on immune cells thereby amplifying inflammatory cytokine release. This work supports the broader concept that structural motifs present in the SARS-CoV-2 spike-protein can disrupt cholinergic anti-inflammatory pathways and elucidates a mechanism that may contribute to the pathophysiology and immune system dysregulation that can occur in severe COVID-19.

PMID 42556725
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PubMedRSC advances2026-08-06

A sustainable pH responsive hydrogel-based phosphorus fertilizer using nano oxalic acid-modified rock phosphate and humic acid.

Perera Tharushi T, Dabare Sanduni S, Munaweera Imalka I, Thambugala Kasun M KM et al.

Phosphorus (P) fixation and precipitation severely limit fertilizer efficiency in alkaline soils, contributing to resource depletion and environmental losses. In this study, a sustainable, pH-responsive phosphorus nano fertilizer was developed by mechanochemically converting Eppawala rock phosphate (ERP) into nano oxalic acid-modified rock phosphate (nano-Ox-ERP) and encapsulating it within a biodegradable sodium alginate-carboxymethyl cellulose (SA-CMC) hydrogel matrix supplemented with humic acid (HA). Nano Ox-ERP particles (60-180 nm) were characterized using PXRD, SEM-EDX, and FTIR. Hydrogel beads with varying nano Ox-ERP (20-80%) and humic acid (1-3%) compositions were evaluated for encapsulation efficiency, swelling behavior, and phosphorus release across pH 3.5-8.5. Formulation B8 (80% nano Ox-ERP + 2% HA) achieved 91.5% phosphate encapsulation and sustained release following Korsmeyer-Peppas kinetics. Pot experiments using Capsicum annuum L. (banana pepper) grown in alkaline soil demonstrated that the optimized formulation significantly enhanced plant growth, yield, and phosphorus uptake compared with conventional phosphorus sources, including triple super phosphate (TSP), untreated rock phosphate, and oxalic acid-treated rock phosphate, while also increasing soil bacterial abundance. The integrated nano-hydrogel-humic acid system effectively improves phosphorus bioavailability, minimizes nutrient losses, and promotes soil microbial activity, offering a scalable and environmentally benign strategy for sustainable phosphorus management in alkaline agroecosystems.

PMID 42559034
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PubMedFood chemistry2026-08-06

Steam-based solid-phase extraction method for benzoic and sorbic acids in food by HPLC.

Sugiura Jun J, Tsuchiyama Tomoyuki T, Taniguchi Masaru M, Noguchi Shoichiro S

A steam-based solid-phase extraction (SPE) method was developed for the determination of benzoic acid and sorbic acid in food matrices. Samples were heated, and the generated steam was passed through an SPE cartridge in two successive cycles. Analytes were eluted with 0.1% (v/v) acetic acid in methanol and quantified by high-performance liquid chromatography (HPLC). Method validation demonstrated linearity over 1-100 μg mL-1 for benzoic acid and 1-300 μg mL-1 for sorbic acid (R2 ≥ 0.999), and recoveries of 91.9-102.6% with repeatability of 0.7-3.8% RSD and intermediate precision of 1.9-5.0% RSD. Applicability was confirmed in 12 food products with recoveries of 85.2-103.1% and 0.1-4.9% RSD, indicating practical usage in food safety monitoring. By combining two techniques (steam-based extraction and SPE), the method provides a simplified and efficient purification strategy for the analysis of benzoic and sorbic acids in complex food matrices.

PMID 42556240
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PubMedFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association2026-08-06

Perfluorononanoic acid enhances non-small cell lung cancer progression through CD36-driven fatty acid metabolic reprogramming.

Qin Ce C, Yuan Jun J, Zhang Rui R, Liu Li L et al.

Lung cancer ranks among the most prevalent and deadly malignant tumors globally, posing a significant threat to human health. Perfluorononanoic acid (PFNA), as an emerging persistent organic pollutant, has attracted widespread attention due to its extensive presence in the environment. However, the effect of PFNA on lung cancer development and its molecular mechanism have not been reported. This study utilized A549 and H1299 non-small cell lung cancer cell lines to examine the toxicological impact of environmentally relevant PFNA concentrations. The results showed that PFNA exposure significantly enhanced the proliferative capacity of A549 and H1299 cells. Further studies revealed that PFNA promoted fatty acid uptake in lung cancer cells, and detection of fatty acid transporter expression showed that CD36 expression was significantly upregulated. PFNA facilitated the epithelial-mesenchymal transition (EMT) in lung cancer cells. Mechanistic studies revealed that PFNA promotes fatty acid uptake by upregulating CD36 expression, thereby activating the mTOR signaling pathway. PFNA notably enhanced lung cancer cells' resistance to cisplatin-induced ferroptosis. In-depth mechanistic studies found that PFNA inhibits cisplatin-induced ferroptosis by promoting GPX4 expression. In vivo animal models confirmed that PFNA exposure promotes lung cancer progression. This study identifies a novel mechanism where environmentally relevant PFNA concentrations affect lung cancer cell proliferation by modulating fatty acid metabolism, offering insights for assessing PFNA-related lung cancer risk and potential targets for prevention and treatment. This study investigates the role of PFNA in lung cancer, focusing on its interaction with CD36 and the mTOR signaling pathway.

PMID 42556774
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PubMedComprehensive reviews in food science and food safety2026-08-06

Unveiling the Acidic Backbone of Baijiu: A Comprehensive Review on Composition, Metabolic Pathways, and Quality Implications.

Dai Mengqi M, Niu Zehua Z, Lu Yanping Y, Wei Anlan A et al.

Acids constitute fundamental molecular determinants that shape the sensory profile, typicity, and overall quality of Baijiu, a traditional Chinese distilled spirit. In this review, the latest advances in the studies of acidic compounds in Baijiu are systematically summarized within the framework of the "composition-function-microbe interaction" chain, with particular emphasis placed on the relationships among acid metabolism, flavor formation, microbial ecology, and product quality stability. We first catalog the diverse acid profiles in Baijiu, highlighting the four major acids (acetic, lactic, butyric, and caproic acids), and their dynamic evolution during product aging. In addition, the roles of acids in sensory perception, aroma regulation, and quality evaluation are comprehensively discussed, while their potential health-related implications are briefly and critically appraised. Crucially, we elucidate the microbial origins of these acids, detailing key metabolic pathways including glycolysis, amino acid catabolism, and reverse β-oxidation. Current studies have demonstrated that microbial community interactions play critical roles in shaping acid metabolism and acid-ester balance, although the underlying mechanisms remain insufficiently resolved. This review concludes by identifying critical knowledge gaps regarding in situ metabolic flux quantification and predictive modeling of microbial interaction networks governing acid-flavor compound dynamics. Future studies integrating multiomics approaches, ecological modeling, and targeted metabolic regulation are expected to facilitate the transition of Baijiu fermentation from descriptive characterization toward predictive and controllable bioprocesses.

PMID 42557861
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PubMedJournal of inflammation research2026-08-06

Vagus Nerve Stimulation Mitigates Sepsis-Induced Lung Injury via Pulmonary proBDNF Suppression.

Gao Ye Y, Wang Ni N, Xiao Zhaoyang Z

Sepsis-associated acute respiratory distress syndrome (ARDS) remains a major contributor to mortality among critically ill patients. Vagus nerve stimulation (VNS) may attenuate inflammatory injury, but the downstream molecular mechanisms underlying its protective effects in septic lung injury remain incompletely understood. The role of proBDNF in VNS-mediated immunoregulation remains unclear. This study aimed to explore whether pulmonary proBDNF contributes to VNS-induced protection against sepsis-associated lung injury. Sepsis-associated lung injury was induced by cecal ligation and puncture (CLP) in rats. The effects of VNS on lung injury, inflammation, and pulmonary proBDNF expression were evaluated. Vagotomy was conducted to assess the dependence of VNS effects on intact vagal signaling. Peripheral cholinergic signaling was probed using methyllycaconitine, an α7 nicotinic acetylcholine receptor (α7nAChR) antagonist. Pulmonary overexpression of proBDNF was achieved via adeno-associated virus (AAV) delivery to determine its functional significance. Histological, molecular, and functional analyses assessed lung injury, inflammation, pulmonary proBDNF, pulmonary edema, and BALF total protein levels. VNS significantly alleviated CLP-induced lung injury, reduced pulmonary inflammatory cytokine expression, decreased pulmonary edema and BALF total protein levels, and partially restored barrier-associated gene expression. Pulmonary proBDNF levels were markedly increased after CLP but suppressed by VNS, whereas vagotomy further elevated proBDNF. Brain proBDNF levels remained largely unchanged across groups. α7nAChR blockade attenuated the inhibitory effect of VNS on pulmonary proBDNF. Immunofluorescence identified macrophages as a major source of proBDNF in injured lungs. Notably, AAV-mediated pulmonary overexpression of proBDNF weakened the beneficial effects of VNS on inflammation, pulmonary edema, alveolar-capillary barrier leakage, and lung damage. VNS protects against sepsis-associated lung injury through suppression of elevated pulmonary proBDNF, a process dependent on intact vagal signaling and, at least in part, mediated by α7nAChR-dependent peripheral cholinergic pathways. These findings identify proBDNF as a possible downstream effector of VNS-mediated lung protection.

PMID 42559398
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