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ibuprofen + arginine (Spedifen / Zafen / Espedifen)

✓ Approved

Zambon · PTGS1 · 小分子

什么是 ibuprofen + arginine?

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)。

药物档案

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

作用机制

分子靶点

ibuprofen + arginine 作用于 2 个分子靶点:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
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

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 disordersAbdominal pain✓ Approved
Hepatobiliary disordersHepatitis✓ Approved

相关研究文献

PubMedMarine drugs2026-07-27

Microparticles Based on Chitosan/Xanthan Gum Polyelectrolyte Complex Modulate the Anti-Inflammatory and Antinociceptive Effects of Ibuprofen and Escin.

Ćirić Ana A, Martić Nikola N, Bosanac Milana M, Andrejić Višnjić Bojana B et al.

Polyelectrolyte complex (PEC)-based carriers offer a promising strategy to improve the oral delivery of anti-inflammatory agents with limited bioavailability or variable pharmacodynamic profiles. This study evaluated the anti-inflammatory and antinociceptive effects of previously optimized formulations of chitosan/xanthan gum PEC microparticles loaded with either ibuprofen or escin, using the carrageenan-induced paw edema model, histopathological and cyclooxygenase-2 (COX-2) immunohistochemical analyses, and the hot plate test. Ibuprofen-loaded microparticles significantly reduced paw swelling during the peak inflammatory phase (5-6 h after treatment administration), although no significant differences in overall edema response or antinociceptive activity were observed compared with free ibuprofen. In contrast, escin-loaded microparticles at 10 mg/kg produced the most pronounced anti-inflammatory effect, significantly reducing paw swelling, edema area under the curve (AUC), histopathological lesion scores, and COX-2 expression compared with both the negative control and the corresponding free escin formulation. Escin-loaded microparticles also showed stronger and more sustained antinociceptive activity than free escin. However, the 20 mg/kg formulation did not provide additional anti-inflammatory or antinociceptive benefits. These findings demonstrate that chitosan/xanthan gum PEC microparticles can enhance the pharmacodynamic performance of orally administered anti-inflammatory agents. The magnitude of this effect depended on the incorporated drug and was particularly notable for escin, for which microencapsulation improved both anti-inflammatory and antinociceptive efficacy.

PMID 42505965
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PubMedGels (Basel, Switzerland)2026-07-27

Solubility, Release Behavior and Membrane Permeability of a Ibuprofen Hydrogel Co-Assembled with N-Methyl-D-Glucosamine.

Li Guoxun G, Lu Xinru X, Hu Caijuan C, Ji Jiaxuan J et al.

Small-molecule hydrogels have gradually become a research hotspot compared with polymeric hydrogels, but their practical advantages have not been fully realized in the development of pharmaceutical formulations. This study aimed to explore whether the N-methyl-D-glucosamine (GLU) could be introduced to form a ibuprofen (IBU) hydrogel for overcoming its water solubility defect and optimizing its pharmaceutical properties. Such an IBU-GLU hydrogel was prepared by simply mixing IBU with GLU in small-volume deionized water. The formed IBU-GLU hydrogel was characterized by SEM, rheology, DSC, PXRD and FTIR analyses. In addition, the solubility, in vitro release and permeability were also investigated to evaluate the solubilization and permeability-promoting effects. The resulting IBU-GLU hydrogel exhibited a typical 3D structure with excellent viscoelasticity, which relied on the equilibrium of aggregation and dissolution, as well as a good miscibility between IBU and GLU, and self-assembly driven by intermolecular interactions in an aqueous environment. Compared to pure IBU, the IBU solubility of the IBU-GLU hydrogel was significantly improved by 38.4-fold. Furthermore, IBU-GLU hydrogel demonstrated superior release rates and supersaturation ability, which was attributed to its high-energy state and internal molecular complexation. Additionally, compared with the commercially available IBU hydrogel, the prepared IBU-GLU hydrogel significantly accelerated IBU membrane permeation. Thus, this study highlighted that the designed IBU-GLU hydrogel could serve as a feasible approach to enhance the release and permeability of IBU for its druggability optimization.

PMID 42505261
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PubMedDiseases (Basel, Switzerland)2026-07-27

From Insight to Impact: Spotlight on the Potential Implications of the Neuronal Nitric Oxide Synthase Isoenzyme (nNOS) in Experimental Chronic Toxoplasmosis.

Omar Marwa M

The coccidian protozoan Toxoplasma gondii (T. gondii) is among the most prevalent zoonotic parasites worldwide. Nitric oxide (NO) production by macrophages is considered a critical microbicidal mechanism against various intracellular pathogens, including T. gondii. While the role of the inducible nitric oxide synthase isoenzyme (iNOS) has been widely investigated in both acute and chronic T. gondii infections, the specific functions of the neuronal (nNOS) isotype in the antiparasitic immune response, particularly during chronic toxoplasmosis, remain largely uncovered. Hence, this report seeks to bridge the gap regarding the potential participation of nNOS in experimental chronic T. gondii infection. The study included 56 Swiss albino mice, equally allocated into four experimental groups: (G1) negative control, (G2) infected control, (G3) infected-L-arginine-treated, and (G4) infected-7-Nitroindazole-treated. All groups except (G1) were orally infected with the avirulent (ME49) T. gondii strain. Nine weeks post-infection, all mice were euthanized for parasitological, histopathological, immunohistochemical, and biochemical analyses. The NO donor, L-arginine, induced a significant reduction in the number of T. gondii cysts, together with strong nNOS immunoreactivity in the brain sections of the treated mice. Conversely, the highest parasitic burden was observed following selective nNOS inhibition with 7-Nitroindazole, exacerbating parasite-induced pathology. The neuronal isotype serves as a critical source of NO production during the chronic stage of T. gondii infection, thereby enhancing parasite elimination and contributing to host tissue protection.

PMID 42505568
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PubMedPhysical chemistry chemical physics : PCCP2026-07-27

Mechanistic insights into Kv1.6 inhibition by conotoxin Pl14A from molecular dynamics simulation.

Vanneikima, Paul Sandip S

Conotoxins are peptide toxins that are found in marine cone snails and inhibit ion channels with high affinity and selectivity. Pl14A is a conotoxin belonging to the J-superfamily, and is one of a few conotoxins that can inhibit two types of receptors, the Kv1.6 subtype of voltage-gated potassium channels as well as nicotinic acetylcholine receptors (nAChRs). In this work, we use classical molecular dynamics simulations to examine the mechanism of inhibition and structural interactions between Pl14A and the Kv1.6 channel. Our study reveals that Pl14A binds stably in the extracellular vestibule of Kv1.6, engaging key residues within the selectivity filter and turret region through a combination of electrostatic and hydrophobic contacts. The peptide's basic residues, mainly the arginine residue and putative dyad motif Lys18 and Tyr19, are implicated in its subtype specificity and pore-blocking activity. Structural analysis and free energy calculations provide a quantitative view of the conformational changes in both the peptide and the channel, consistent with a pore blocking mode of inhibition. These findings help us to understand the modulation of the Kv1.6 channel by conotoxin Pl14A and offer insight for designing selective peptide inhibitors with therapeutic potential against Kv1.6 related pathologies.

PMID 42506986
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PubMedBiomaterials science2026-07-27

Self-assembly of DOPA-containing peptides for enhanced antimicrobial efficacy and promoted wound healing.

Zhou Xiang X, Wang Xinyao X, Wang Haozhan H, Zhang Cong C et al.

Bacterial infection and excessive reactive oxygen species (ROS) accumulation synergistically disrupt the wound microenvironment and severely impair the healing process. Therefore, multifunctional biomaterials with intrinsic antibacterial and antioxidant properties are highly desirable for the effective treatment of infected wounds. Here, we rationally designed and synthesized two DOPA-containing constitutional isomeric peptides with dual antimicrobial and antioxidant activities, each containing one 3,4-dihydroxy-L-phenylalanine (DOPA), four tryptophan residues (W), and three arginine residues (R), and designated as WRWRWRW(DOPA) and WWWWRRR(DOPA), respectively. These peptides can self-assemble in aqueous solutions into different morphologies, with WRWRWRW(DOPA) forming vesicles, whereas WWWWRRR(DOPA) assembles into micelles. Notably, both self-assembled nanostructures exhibited enhanced antibacterial activity compared with their corresponding peptide precursors, and the vesicular assemblies showed superior antimicrobial efficacy relative to their micellar counterparts. Based on these findings, the vesicle-forming peptide system was further investigated for ROS-scavenging capability and wound healing performance. The results demonstrated that the vesicular assemblies possessed efficient ROS elimination capacity and significantly promoted infected wound repair. Overall, this work highlights the critical role played by the morphology of self-assembled nanostructures in regulating antimicrobial and antioxidant performance, providing a promising strategy for the design of multifunctional peptide-based systems for infected wound therapy.

PMID 42504667
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PubMedMetabolites2026-07-27

Maternal Vitamin D Deficiency During Pregnancy Alters Hepatic Metabolism in Adult Female Offspring Without Overt Metabolic Dysfunction.

Isogai Miyu M, Imai Norihiro N, Ogawa Tadashi T, Hayashi Yumi Y

Background/Objectives: Vitamin D deficiency (VDD) is a major global health concern. Although maternal VDD during pregnancy may influence metabolic health in offspring, previous studies have focused predominantly on male offspring, leaving its effects in females insufficiently characterized. This study aimed to comprehensively assess hepatic metabolic profiles in female offspring exposed to maternal VDD during gestation. Methods: Pregnant 129/Sv mice were fed either a control diet or a vitamin D-deficient diet throughout pregnancy. After weaning, female offspring were maintained on a normal diet and analyzed at 12 weeks of age following a 16 h fast. Hepatic metabolomic profiling was conducted using GC-MS/MS, followed by multivariate analysis. To evaluate the potential contribution of fasting, publicly available liver RNA-seq data from ad libitum-fed and 16 h-fasted mice (GSE130127) were also analyzed. Results: No overt metabolic abnormalities were detected between the groups. However, principal component analysis revealed differences in hepatic metabolic profiles between the Control and VDD groups. Levels of 4-aminobutyric acid and proline were significantly elevated in the VDD group. Pathway analysis revealed significant alterations in arginine and proline metabolism and purine metabolism, along with changes in pathways associated with amino acid and energy metabolism. Comparison with fasting-associated liver RNA-seq data revealed minimal overlap, although the potential influence of fasting cannot be completely excluded. Conclusions: Maternal VDD during pregnancy was associated with altered hepatic metabolic profiles in female offspring despite the absence of overt metabolic abnormalities. These findings suggest that maternal VDD may influence hepatic metabolism in female offspring and indicate that the potential long-term effects of maternal VDD on offspring metabolism warrant further investigation.

PMID 42506454
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