Zambon · PTGS1 · 小分子
ibuprofen + arginine 是一种小分子，由Zambon研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。
| 商品名 | Spedifen, Zafen, Espedifen |
| 公司 | Zambon |
| 药物类别 | 小分子 |
| 分子靶点 | PTGS1, PTGS2 |
| 给药途径 | Oral (PO) |
| 状态 | Approved |
ibuprofen + arginine 作用于 2 个分子靶点：
| PTGS1 | prostaglandin-endoperoxide synthase 1 (COX3, PCOX1) |
| PTGS2 | prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2) |
ibuprofen + arginine 针对 2 个适应症，涉及 2 个治疗领域。
| 治疗领域 | 疾病/病症 | 分期 |
|---|---|---|
| Gastrointestinal disorders | Abdominal pain | ✓ Approved |
| Hepatobiliary disorders | Hepatitis | ✓ Approved |
Bargiacchi Giuditta G, De Marco Oriana O, Petruzzelli Luigi Annicchiarico LA, Tucci Celeste C et al.
He Yanan Y, Yu Lu L, Lu Yixun Y, Zhou Zhikang Z et al.
Pyrroloquinoline quinone (PQQ) was reported to be neuroprotective after experimental traumatic brain injury (TBI), but its mechanisms remain undefined. We tested whether PQQ protects against TBI in mice and identified the associated pathways. Male C57BL/6 mice received intraperitoneal PQQ (6.25, 12.5 or 25 mg/kg) immediately after controlled cortical impact. Mortality, modified neurological severity score (mNSS) and beam balance were followed to day 14; histopathology, immunofluorescence, western blot, ELISA and ATP assays were performed on day 3. Transcriptomics, metabolomics, network pharmacology and docking were integrated to identify candidate mechanisms. PQQ reduced mortality (lowest at 12.5 mg/kg) and dose-dependently improved neurological deficits, neuronal apoptosis, brain edema, pro-inflammatory cytokines, and oxidative stress; the mNSS and beam balance benefits persisted to day 14. At 12.5 mg/kg, multi-omics and network pharmacology identified arginine biosynthesis, mediated by argininosuccinate synthetase 1 (ASS1) and carbamoyl phosphate synthetase 1 (CPS1), as the top-ranked pathway suppressed by PQQ; docking predicted binding of PQQ to both enzymes, suggesting putative targets pending validation. PQQ concurrently restored PTEN-induced kinase 1 (PINK1)/Parkin-mediated mitophagy and ATP production. PQQ attenuates secondary injury after TBI in male mice, in association with increased markers of PINK1/Parkin-mediated mitophagy initiation and suppressed ASS1/CPS1-driven arginine biosynthesis, identifying a candidate dual-axis mechanism and nominating the mitophagy-arginine axis as a target for neuroprotection in TBI.
Binidris Mutasim M, Shehata Menatalla M, Mahfouz Ahmed A, Abousaad Omar O et al.
Invasive meningococcal disease is a life-threatening infection that classically presents as meningitis or meningococcemia. Extra-meningeal manifestations, including pericarditis and septic arthritis, are uncommon and may complicate diagnosis, particularly in the absence of meningeal involvement. A previously healthy vaccinated man in his 50s presented with acute bilateral knee pain and swelling following a short history of fever, productive cough, fatigue, and dyspnea. Blood cultures grew Neisseria meningitidis serogroup W, whereas cerebrospinal fluid, synovial fluid, and pericardial fluid cultures remained negative. Cardiac magnetic resonance imaging demonstrated constrictive pericarditis with circumferential pericardial enhancement and pericardial effusion. The patient was successfully treated with intravenous ceftriaxone, colchicine, ibuprofen, pericardiocentesis, and bilateral knee washout, followed by oral ciprofloxacin. This case adds to the limited literature describing concurrent cardiac and musculoskeletal manifestations of invasive meningococcal disease without meningitis and shows the importance of early recognition, comprehensive investigation and multidisciplinary management of these uncommon presentations.
Dai Hanqi H, Wang Qianwen Q, Zhan Yi Y
Kawasaki disease (KD) is one of the most common rheumatic diseases in children and manifests with multisystem clinical features. Using untargeted metabolomics, our study investigated alterations in small-molecule metabolites in plasma of children with acute KD. Our study aimed to identify differential metabolic pathways and potential biomarkers. Plasma samples were collected from 30 children diagnosed with KD and 30 age-matched healthy controls (HC) at Jinhua Maternal and Child Health Hospital between January 2025 and December 2025. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to analyse plasma samples. Enriched pathways were identified using the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis, and differential metabolic pathways were determined using MetaboAnalyst 5.0. Differential metabolites were screened using the nonparametric Mann-Whitney U-test and receiver operating characteristic curve area (AUC). The conservative average AUC from nested cross-validation was reported as the primary performance metric. Pearson correlation analysis was conducted to evaluate correlations between metabolites and clinical parameters. In total, 261 differential metabolites were identified between the KD and HC groups, including 87 lipids and lipid-like molecules, 69 organic heterocyclic compounds, 38 benzenoids, 34 organic acids, 14 phenylpropanoids, and 19 other compounds. Pathway analysis of these differential metabolites revealed 30 putatively enriched metabolic pathways for exploratory analysis. Of these pathways, primary bile acid biosynthesis, arginine biosynthesis, histidine metabolism, and phenylalanine-tyrosine-tryptophan biosynthesis were nominally associated with KD. Six metabolites with exploratory discriminatory performance (AUC > 0.8) were further identified: L-tyrosine, L-tryptophan, glutamine, histidine, histamine, and taurocholic acid. A combined model incorporating these metabolites achieved an apparent AUC of 0.984 in the full dataset; nested cross-validation yielded a more conservative AUC of 0.889 (95% CI 0.798-0.968), indicating promising exploratory discriminatory performance. Untargeted metabolomics enables identification of metabolically perturbed pathways during the acute phase of KD. L-tyrosine, L-tryptophan, glutamine, histidine, histamine, and taurocholic acid may serve as candidate biomarkers for acute phase of KD.
Kobayashi Madoka M, Kato Fumitaka F, Okada Kotaro K
The present study evaluated the applicability of time-domain NMR (TD-NMR) for detecting crystalline ibuprofen components in ibuprofen-loaded mesoporous silica. Ibuprofen-loaded mesoporous silica samples with different drug loadings were prepared, and the physical state of ibuprofen was characterized by nitrogen adsorption, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), 13C solid-state NMR spectroscopy, and TD-NMR relaxation measurements. PXRD, DSC, and 13C solid-state NMR spectroscopy did not clearly detect crystalline ibuprofen in samples with ibuprofen loadings of 10-30%. By contrast, crystalline components were observed in samples with loadings of 40% or higher. These crystalline components were considered to originate predominantly from excess ibuprofen that crystallized outside the mesopores. In the T1 relaxation analysis using TD-NMR, IBU10-30 was mainly described by a monoexponential function, whereas IBU40-70 required a biexponential function, yielding a long T1 component associated with crystalline ibuprofen. In the T2 relaxation analysis, IBU40-70 exhibited an initial rapid decay that was described by a Gaussian function, whereas IBU10-30 showed a gradual exponential decay. The signal proportions of these NMR relaxation components increased with increasing ibuprofen loading and showed trends consistent with the apparent crystallinity estimated by DSC. These results suggest that TD-NMR, particularly T2 relaxation analysis, may serve as a complementary, nondestructive, and rapid method for evaluating the appearance and increase of crystalline ibuprofen components in mesoporous silica formulations and for monitoring changes in crystallinity.
Wei Junjun J, Mao Xinyuan X, Zhang Ting T, Han Yiping Y et al.
The transport process usually causes fish stress and induces physiological perturbations and tissue structural damage. Arginine, an essential amino acid for fish, plays a significant role in immune regulation. In this work, we investigated the effect of arginine on alleviating transport stress of Culter alburnus. The diets with arginine levels of 1.96% (CON group) and 2.52% (ARG group) were fed to C. alburnus for 70 days, followed by a 24-h simulated transport. The groups were defined as follows: non-transported control (CON0h), non-transported arginine (ARG0h), transported control (CON24h), and transported arginine (ARG24h). The results showed that dietary arginine significantly reduced the levels of NH3-N and NO2--N in the transport water, increased the enzyme activities of GSH, AKP, and NOS, and decreased the content of MDA after transport (P < 0.05). The ARG group had significantly thinner primary gill lamellae and longer secondary gill lamellae than the CON group (P < 0.05). Transcriptome sequencing identified a total of 1190 differentially expressed genes (DEGs: 755 up, 435 down) between CON24h and ARG24h. KEGG enrichment indicated that arginine alleviated transport stress mainly by enhancing immune response and inhibiting inflammatory response, such as CD9, CFB were significantly up-regulated, and CCL20 was significantly down-regulated. In summary, dietary arginine enhanced the antioxidant and immune response of C. alburnus, reducing inflammation after transport. The present study demonstrates that arginine has a positive impact on alleviating transport stress in C. alburnus, which may be used as a dietary supplement to alleviate stress in live fish during transport.
注册免费账户还可查看另外 9996 篇文献
免费注册查看全部文献 →