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hydroquinone (pigmentasa / pigmentasa)

✓ Approved

Vinas · 小分子 · 小分子

什么是 hydroquinone？

hydroquinone 是一种小分子，由Vinas研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名pigmentasa, pigmentasa
公司Vinas
药物类别小分子
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Vinas

治疗适应症

hydroquinone 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Skin and subcutaneous tissue disordersChloasma✓ Approved
Skin and subcutaneous tissue disordersSkin hyperpigmentation✓ Approved

相关研究文献

PubMedJournal of molecular histology2026-09-10

4-Phenylbutyric acid alleviates acrylamide-induced sexual behavioral deficits and testicular damage in male Wistar rats: modulation of ER-stress associated signaling.

Singh Jiten J, Rani Ankita A, Yadav Rachna R, Quasmi Mohammed Nazish MN et al.

Acrylamide (ACR) is an industrial chemical utilized to produce polyacrylamide, a primary flocculant for wastewater treatment. ACR is also classified as a food process contaminant that forms as a byproduct during the processing of carbohydrate-rich foods at high temperatures (> 120 °C). Recent studies show that ACR induces reproductive toxicity, neurotoxicity, and skin irritation through mechanisms including oxidative stress and mitochondrial damage. Despite increasing evidence, ACR-induced testicular damage and its mechanisms remain poorly understood, highlighting the requirement for further investigation. In this study, we aimed to find the ameliorative effect of 4-Phenylbutyric acid (4-PBA) on the ACR-induced reproductive toxicity in male rats. Thirty-two adult male rats were randomly grouped, each containing eight rats: vehicle control group (10 ml/kg of saline; p.o.), ACR group (10 mg/kg of ACR: p.o.), ACR + 4-PBA low dose group (ACR + 4-PBA-500 mg/kg; p.o.), and ACR + 4-PBA high dose group (ACR + 4-PBA-1000 mg/kg; p.o.). ACR was administered for 28 days, while 4-PBA treatment was started on day 15 and continued until day 28. Our findings revealed marked alterations in sexual behavior, as evident by intromission latency, frequency, and ejaculation latency & frequency. Further, ACR exposure elicited significant oxidative stress and endoplasmic reticulum (ER) stress in the testicular tissue. Epididymal sperm count and serum testosterone level were also reduced in ACR-exposed rats. Correlation analysis further supported a close relationship between impaired reproductive performance, oxidative stress, ER stress activation, and testicular structural damage. However, 4-PBA treatment during the last 14 days of treatment significantly improved sexual performance, reversed the decreased testosterone level and sperm count, and restored testicular histopathological damage. Furthermore, these ameliorative effects were accompanied by reduced expression of GRP78, CHOP, and caspase-12, suggesting that modulation of ER stress-associated signaling may contribute to the therapeutic effects of 4-PBA.

PMID 42717142
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PubMedJournal of medicinal chemistry2026-09-10

Structure-Based Design of First Ndc80 Loop-Targeting Peptide Disrupting Ndc80-Nuf2 Interaction for Hepatocellular Carcinoma Therapy.

Jin Xing X, Niu Miao-Miao MM, Geng Yifei Y, Han Liqiao L et al.

Ndc80 is essential for kinetochore-microtubule attachment, but its broad protein-protein interaction interface remains difficult to target. Here, we used structure-guided peptide optimization to develop Peptide-4, a loop-directed peptide designed to modulate the Ndc80-Nuf2 interaction. In contrast to reported Ndc80-directed compounds acting through the Hec1-Nek2 axis or the calponin homology domain, Peptide-4 addresses an underexplored loop region. Peptide-4 bound Ndc80 with a Kd of 0.45 ± 0.01 nM and inhibited the Ndc80-Nuf2 interaction with an IC50 of 0.76 ± 0.03 nM. In Huh7 cells, Peptide-4 altered microtubule organization, suppressed proliferation, clonogenic growth, migration, and invasion, and induced G2/M-phase accumulation and apoptosis. Ndc80 depletion attenuated its antiproliferative effect, consistent with a contribution of Ndc80 to its cellular activity. Peptide-4 also reduced tumor growth in Huh7 xenografts without apparent toxicity under the tested conditions. These findings support the Ndc80 loop as an underexplored peptide-addressable site and identify Peptide-4 as a lead for further optimization.

PMID 42720478
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PubMedChemistry (Weinheim an der Bergstrasse, Germany)2026-09-10

Enabling the Synthesis of the 4'-Thioremdesivir Core.

Wei Liuqing L, Kasthuri Mahesh M, Na Christina C, Bagley Scott S et al.

Nucleosides and nucleoside analogs represent a long established and highly important class of pharmaceutical agents, with numerous U.S. Food and Drug Administration (FDA)-approved examples spanning antiviral, anticancer, and immunological indications. Among these, 4'-thionucleosides-wherein the endocyclic ribose oxygen is replaced by sulfur-have emerged as particularly attractive bioisosteric analogs, frequently exhibiting enhanced pharmacokinetic and pharmacodynamic properties. Despite decades of investigation into 4'-thionucleosides, the literature overwhelmingly focuses on anomeric N-linked derivatives, while reports describing C-linked 4'-thionucleosides remain remarkably scarce. In this study, we report the first successful synthesis of the parent 4'-thionucleoside core of remdesivir. In contrast to the well-established β-selective deoxycyanation observed in the ribose series, substitution of oxygen with sulfur results in a pronounced reversal of anomeric selectivity, favoring the undesired α-isomer. This intrinsic bias was overcome through the discovery and exploitation of an unprecedented bridged oxythioketal intermediate, enabling access to the β-configured product. The relative and absolute stereochemistry was confirmed by single-crystal x-ray diffraction, correcting a recent misassignment in the literature. Computational and NMR reaction monitoring studies provide mechanistic insight into thioribose reactivity and establish a framework for controlling anomeric stereochemistry in C-linked 4'-thionucleoside synthesis. These results establish a foundation for future C-linked 4'-thionucleoside antiviral development.

PMID 42720396
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PubMedExperimental biology and medicine (Maywood, N.J.)2026-09-10

Altered serum interleukin-4 and monocyte chemoattractant protein-3 levels are associated with generalized anxiety disorder: a case-control study.

Binta Rashid Most Humayra MH, Islam Mehedi M, Ashraful Islam Sardar Mohammad SM, Islam Md Rabiul MR

Generalized Anxiety Disorder (GAD) is a long-term mental health condition often associated with immune system dysregulation. While pro-inflammatory and anti-inflammatory cytokines are known to influence neuroinflammation, their specific roles in GAD remain less understood. This study investigates the relationship between serum levels of IL-4 and MCP-3 and GAD in a Bangladeshi population. This case-control study included 44 patients with GAD and 44 healthy controls (HCs). Participants were examined using the GAD-7 scale. Serum IL-4 and MCP-3 levels were measured using ELISA. Data were analyzed using t-tests, Spearman's correlation, and Receiver Operating Characteristic (ROC) curve analysis to assess diagnostic performance. GAD patients had significantly lower serum IL-4 levels (11.82 ± 10.91 pg/mL) and higher MCP-3 levels (57.80 ± 19.85 pg/mL) compared to HCs (IL-4: 24.51 ± 15.36 pg/mL; MCP-3: 34.01 ± 15.75 pg/mL; p < 0.001). IL-4 levels showed a significant negative correlation with GAD-7 scores (r = -0.496, p < 0.001), while MCP-3 showed a positive correlation (r = 0.544, p < 0.001). ROC analysis indicated that MCP-3 had higher diagnostic accuracy (AUC = 0.848, sensitivity = 87.6%, specificity = 84.3%) compared to IL-4 (AUC = 0.782, sensitivity = 80.2%, specificity = 78.5%). Moreover, decreased IL-4 and elevated MCP-3 levels were found to be significantly associated with GAD severity, suggesting an immune imbalance. These cytokines may serve as promising diagnostic biomarkers and therapeutic targets for GAD. Further longitudinal studies are recommended to investigate this causal relationship and its underlying mechanisms.

PMID 42719764
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PubMedCytotechnology2026-09-10

ADH1 dysfunction exacerbates neurovascular injury in diabetic stroke by impairing 4-HNE clearance and promoting neutrophil infiltration.

Xu Pei-Pei PP, Shi Ying-Na YN

Diabetes significantly exacerbates ischemic stroke injury, yet the underlying metabolic-inflammatory mechanisms remain elusive. This study investigates the role of Alcohol Dehydrogenase 1 (ADH1) in the pathophysiology of neurovascular injury following diabetic stroke. Diabetic mice were established via intraperitoneal injection of streptozotocin. Distal middle cerebral artery occlusion (dMCAO) was performed to induce ischemic stroke. In vitro, primary microglia and endothelial cells were exposed to high glucose (HG) and oxygen-glucose deprivation/reoxygenation (OGD/R) conditions. Transcriptomic analysis of a public dataset (GSE196266) identified key differentially expressed genes, including ADH1. In vivo, ADH1 function was assessed via intracerebroventricular injection of adeno-associated virus (AAV)-ADH1 vector. Infarct volume was quantified via 2,3,5-triphenyltetrazolium chloride (TTC) staining; neurological deficits were assessed using the modified Neurological Severity Score (mNSS); 4-HNE levels were measured by enzyme-linked immunosorbent assay (ELISA) and Western blot; neutrophil infiltration was quantified via flow cytometry and microglial polarization were evaluated by real-time quantitative polymerase chain reaction (RT-qPCR). ADH1 was significantly downregulated in diabetic stroke brains. Overexpression of ADH1 markedly reduced infarct volume and cerebral edema while improving long-term neurological recovery. Mechanistically, ADH1 attenuated oxidative stress by facilitating the clearance of 4-hydroxy-2-nonenal (4-HNE), which subsequently inhibited microglial M1 polarization and apoptosis. Furthermore, ADH1 preserved BBB integrity by preventing 4-HNE-mediated impairment of tight junction protein integrity (ZO-1, OCLN, CLDN5) and suppressed neutrophil recruitment by downregulating chemotactic signals (CXCL1/2). Exogenous 4-HNE treatment directly exacerbated these pathological processes, whereas ADH1 restoration effectively rescued the neurovascular unit. ADH1 dysfunction exacerbates neurovascular injury in diabetic stroke by impairing 4-HNE clearance and promoting neutrophil infiltration. Targeting the ADH1/4-HNE axis represents a promising therapeutic strategy for ameliorating diabetic stroke outcomes.

PMID 42718815
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PubMedChemistry & biodiversity2026-09-10

Clean Synthesis of N-4-Alkylamino-7-chloroquinoline Cyclic Imides: Influence of Lipophilicity on Antibacterial and Ecotoxicological Properties.

Luz-Filho Agenor P AP, Silva Thais C TC, Silva Matheus B MB, Sousa Abraão P AP et al.

Motivated by the promising antimicrobial and ecotoxicological effects of 4-alkylamino-7-chloroquinoline and N-alkylphthalimide derivatives, these privileged nuclei were linked to investigate how lipophilicity influences antibacterial activity and ecotoxicity. For this purpose, seven 4-alkylamino-7-chloroquinolines (2a-g) were prepared, of which four were used as precursors (2a-d) and reacted with different anhydrides. Using a clean synthetic approach, 4-alkylamino-7-chloroquinoline-succinimides (3a-d) and -phthalimides (5a-d) were obtained in yields of 60%-99% after only filtration with distilled water. In vitro assays were performed to determine the minimum inhibitory/bactericidal concentration (MIC/MBC) against Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus mutans. Lipophilicity (log P) and toxicity were predicted using the pkCSM program. In vitro toxicity tests on Artemia salina larvae were used as an indicator of ecotoxicity. 4-Alkylamino-7-chloroquinolines (2b, 2f, 2g) revealed a moderate MIC of 156.25 µg·mL-1 against Gram-(-) and Gram-(+) bacteria, whose predicted toxicity does not pose a potential risk to human health. Results indicate a correlation between increased lipophilicity and higher ecotoxicity, where less lipophilic compounds were less toxic to A. salina (LC50 133.01-777.50 µg·mL-1) than 4-alkylamino-7-chloroquinoline-phthalimides, suggesting further investigation of their cytotoxicity.

PMID 42720095
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