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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

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

PubMedBioorganic chemistry2026-06-13

A homologous cell membrane-coated peptide-based USP7 degrader enhances degradation efficiency and anti-tumor activity in gastric Cancer.

Ma Cong-Cong CC, Jin Cheng-Yun CY, Guo Nin-Jie NJ, Liu Hong-Min HM et al.

Ubiquitin-specific protease 7 (USP7) is an oncogenic deubiquitinase that promotes tumor cell proliferation and immune evasion, making it a promising therapeutic target. Here, we designed peptide-based proteolysis-targeting chimeras (p-PROTACs) by leveraging Epstein-Barr nuclear antigen 1 (EBNA1), a natural ligand of USP7, as the targeting moiety. By screening multiple E3 ligands, we identified a potent USP7 degrader, DP-4, capable of inducing USP7 degradation in gastric cancer (GC) cells. To overcome the intrinsic permeability limitation of peptide degraders, DP-4 was further packaged into homologous MKN-45 cell membranes (MM) to generate MM@DP-4 nanoparticles, which markedly improved intracellular delivery. MM@DP-4 achieved substantially enhanced cellular uptake compared with free DP-4 (60.9% vs 2.50% at 4 h) and promoted robust, post-transcriptional USP7 degradation with a DC50 of 1.24 μM in MKN-45 cells. Functionally, MM@DP-4 enhanced T-cell-mediated killing and suppressed gastric cancer cell proliferation. Collectively, our findings establishes DP-4 as a potent peptide-based USP7 degrader and demonstrates that homologous cancer cell membrane coating is an effective strategy to boost intracellular delivery and degradation efficacy, supporting USP7 degradation as a promising therapeutic approach for GC.

PMID 42284879
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PubMedCarbohydrate research2026-06-13

Structural elucidation of a novel arabinogalactoglucan from Polygonum multiflorum and its binding to the m6A reader YTHDF2.

Zhang Yupeng Y, Pei Haihan H, Zhou Jing J, Ding Kan K et al.

Polygonum multiflorum Thunb. (P. multiflorum) is a traditional Chinese medicinal herb with a long history of use, and its polysaccharide constituents have been reported to possess a range of biological activities. Nevertheless, most existing studies have focused on crude polysaccharide fractions or preliminary bioactivity evaluations, leaving the fine structural features and molecular targets of these polysaccharides insufficiently defined. Here, a homogeneous polysaccharide, FM02 (Mw 12.1 kDa), was isolated from P. multiflorum. Structural characterisation indicated that FM02 is a novel arabinogalactoglucan with a backbone of alternating →4)-α-Glcp-(1→ and →4, 6)-α-Glcp-(1→ residues. Branches at the O-6 position of 1, 4, 6-linked glucosyl residues comprise three distinct types: a terminal T-α-Glcp cap, a trisaccharide branch →1)-α-Glcp-(4 → 1)-β-Galp-(3 → 1)-α-Araf, and a longer chain →1)-α-Glcp-(4→[1)-Galp-(4]3→[1)-α-Glcp-(4]4 → 1)-α-Glcp. Affinity pull-down of LX-2 hepatic stellate cell lysates combined with mass spectrometry identified YTHDF2 as a candidate binding protein. Surface plasmon resonance (SPR) detected a concentration-dependent interaction between FM02 and YTHDF2 (KD 5.47 × 10-7 M). Neither the acid-hydrolysis-resistant fraction FM02I nor the released degradation fragment FM02E showed detectable binding to YTHDF2, suggesting that the intact primary structure of the polysaccharide may be required to sustain this interaction. In summary, this study reports for the first time a novel arabinogalactoglucan, FM02, isolated from P. multiflorum, and reveals its potential direct interaction with the m6A reader protein YTHDF2, thereby providing foundational data for further activity screening, mechanistic studies, and related drug development of this polysaccharide.

PMID 42284954
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PubMedInorganic chemistry2026-06-13

Six Lanthanide Complexes: Crystal Structures, Spectroscopic Properties, and Pyrolysis Characteristics Analysis by Thermogravimetry-Differential Scanning Calorimetry/Fourier Transform Infrared/Mass Spectrometry.

Qu Zi-Yi ZY, Zhao Jin-Jin JJ, Ren Ning N, Zhang Jian-Jun JJ

Six dinuclear lanthanide complexes were synthesized: [Ln(4-MOBA)3(4,4'-DM-2,2'-bipy)]2·(H2O)·(C2H5OH) (Ln = Eu (1)) and [Ln(4-MOBA)3(4,4'-DM-2,2'-bipy)]2·2(H2O) (Ln = Sm (2)) (where 4-MOBA = 4-methoxybenzoate, 4,4'-DM-2,2'-bipy = 4,4'-dimethyl-2,2'-bipyridine); [Ln(3-MBA)3(5,5'-DM-2,2'-bipy)]2 (Ln = Tb (3)), [Ln(3-MBA)3(5,5'-DM-2,2'-bipy)]2·(5,5'-DM-2,2'-bipy) (Ln = Dy (4), Eu (5)) and [Ln(3-MBA)4(5,5'-DM-2,2'-bipy)]2 (Ln = Ce (6)) (where 3-MBA = 3-methylbenzoate, 5,5'-DM-2,2'-bipy = 5,5'-dimethyl-2,2'-bipyridine). Single-crystal X-ray diffraction analysis determined that the structure of complex 6 contains eight 3-MBA ligands, which adopt monodentate, bridging bidentate, and bridging tridentate coordination modes, respectively, a feature that is relatively rare in the study of such complex structures. In addition, the pyrolysis characteristics of the six complexes were studied using coupled TG-DSC/FTIR/MS techniques. The decomposition initially involves the loss of free substances at relatively low temperatures, followed by the elimination of neutral ligand molecules. Subsequently, the organic carboxylate ligands are progressively removed at higher temperatures. Based on the fluorescence spectra of complexes 1-5, we further investigated the fluorescence decay behavior and quantum yields of complexes 1, 3, and 4, observing significantly long fluorescence lifetimes. DFT calculations unveiled an optimal energetic match wherein the triplet state of the neutral ligands aligns favorably with the excited states of the Ln3+.

PMID 42285779
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PubMedBiochemical pharmacology2026-06-13

Targeting neuropilin-1 attenuates 4-hydroxytamoxifen-induced stemness and sensitizes ERα-re-expressing TNBC to tamoxifen.

Yu Qinglong Q, Tang Wei W, Xiao Yani Y, Kong Ying Y et al.

Reactivating functional estrogen receptor alpha (ERα) expression represents a promising strategy for tamoxifen (TAM)-based endocrine therapy in triple-negative breast cancer (TNBC). However, TAM and its metabolites may exert potential oncogenic effects, which could compromise TAM efficacy in TNBC. Here, we report that low-dose 4-hydroxytamoxifen (4-OHT), an active metabolite of TAM, enhances stemness in TNBC cells via the Neuropilin-1 (NRP-1)/Calpain-2 (CAPN2)/β-catenin axis. Mechanistically, 4-OHT stimulates CAPN2 activation by promoting its membrane localization, increasing substrate cleavage, and inducing degradation of its endogenous inhibitor calpastatin. Activated CAPN2 suppresses ubiquitin-mediated degradation of β-catenin, leading to elevated β-catenin stability and intracellular accumulation. This enhances β-catenin transcriptional activity and ultimately promotes stemness in TNBC cells. Kaplan-Meier survival analysis showed that high NRP1 expression correlates with poorer overall survival in breast cancer patients undergoing endocrine therapy. Moreover, 4-OHT triggers Ca2+ release and ERK phosphorylation in TNBC cells through the NRP-1/PLC-γ1 pathway, thereby activating CAPN2. Finally, we demonstrate that the NRP-1 inhibitor EG00229 sensitizes ERα-re-expressing TNBC cells to TAM treatment. Our study uncovers a molecular mechanism by which 4-OHT promotes TNBC stemness via the NRP-1/CAPN2/β-catenin signaling cascade. Targeting NRP-1 may serve as a valuable strategy to improve TAM efficacy in ERα-re-expressing TNBC.

PMID 42285368
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PubMedJournal of chromatography. B, Analytical technologies in the biomedical and life sciences2026-06-13

Single-step purification of soybean peroxidase using Aminobenzohydrazide-based affinity chromatography matrices.

Rasulzade Zahra Z, Abul Nurgül N, Köksal Zeynep Z, Öztekin Aykut A et al.

Soybean peroxidase (SBP, EC 1.11.1.7) is an industrially important enzyme due to its high catalytic activity, remarkable thermostability, and broad application potential in biotechnology, food processing, polymer synthesis, and biosensor development. In this study, novel benzohydrazide derivatives, namely 4-amino-3-bromo-5-fluorobenzohydrazide, 4-amino-3-bromo-5-chlorobenzohydrazide, 4-amino-3-bromo-2-methylbenzohydrazide, and 5-aminoisophytalohydrazide, were synthesized, and their usability as affinity chromatography ligands was investigated. For this purpose, the inhibition kinetics of the synthesized molecules were studied, and enzyme-ligand interactions were evaluated using in silico methods. The estimated free binding energies of the molecules were determined to range from -5.21 to -5.83 kcal/mol. Soybean peroxidase enzyme was purified in a single step from soybean sprout leaves using affinity chromatography columns prepared with synthesized ligands, and the optimization of purification conditions was investigated in detail. According to the results obtained, soybean peroxidase was obtained from the affinity gel containing the 4-amino-3-bromo-5-fluorobenzohydrazide ligand with a purification factor of 130.2-fold and a yield of 8.71%. In addition, a purification factor of 133.8-fold and a yield of 4.3% were obtained with the affinity column designed using the determined 4-amino-3-bromo-2-methylbenzohydrazide ligand, which has the smallest Kİ value of 80.55 ± 12.6 μM. The results show that benzohydrazide-based affinity matrices offer an effective and economical strategy for the purification of SBP.

PMID 42285004
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PubMedBioorganic chemistry2026-06-13

Design, synthesis, and biological evaluation of C-28 carboxyl derivatives of Hederacoside C as anti-inflammatory agents for acute lung injury.

Meng Fancheng F, He Jia J, Li Huilan H, Li Xiang X et al.

Hederacoside C, a bioactive triterpenoid saponin isolated from the dried roots of the Ranunculaceae plant Pulsatilla chinensis, has demonstrated therapeutic efficacy in murine models of nephritis, acute lung injury, and inflammatory bowel disease. However, its further development as a drug candidate has been hampered by hemolytic toxicity and poor oral bioavailability. Based on published evidence that the free carboxyl group at the C-28 position is closely associated with hemolytic activity, a series of C-28 carboxyl derivatives was rationally designed and synthesized with the aim of attenuating hemolytic liability while preserving or enhancing anti-inflammatory potency. Following in vitro anti-inflammatory evaluation and cytotoxicity assessment, compound HSC-4 was identified as the most promising candidate for further in vivo pharmacological studies. Notably, HSC-4 exhibited significant anti-inflammatory efficacy in both a murine systemic sepsis model and an acute lung injury model. An acute toxicity study further demonstrated that HSC-4 did not cause significant hepatotoxicity or nephrotoxicity in KM mice at doses up to 400 mg/kg over five consecutive days. These findings suggest that HSC-4 represents a promising lead compound for the development of novel anti-inflammatory therapeutics, pending further hemolytic activity assessment and pharmacokinetic characterization.

PMID 42284878
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