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kojic acid (kojic acid, Vinas)

✓ Approved

Vinas · TYR

什么是 kojic acid？

kojic acid 是一种治疗药物，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kojic acid, Vinas
公司Vinas
分子靶点TYR
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Vinas

作用机制

分子靶点

kojic acid 作用于 1 个分子靶点：

TYRtyrosinase (ATN, OCAIA)
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

kojic acid 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 disordersSkin disorder✓ Approved
Skin and subcutaneous tissue disordersDermatosis✓ Approved

相关研究文献

PubMedJournal of applied biomaterials & functional materials2026-10-26

Arbutin/kojic acid-loaded MHA hydrogel array patches attenuate UVB-induced epidermal hyperplasia and remodeling-associated responses.

Lee Seung-Min SM, Cha Sangryul S, Jeon DooLee D, Choi Wooseok W et al.

Acute ultraviolet B (UVB) exposure induces epidermal hyperplasia, pigmentation-related responses, and early extracellular matrix remodeling. Topical tyrosinase inhibitors, including arbutin and kojic acid, can have limited residence on damaged skin. Here, we evaluated a skin-conformal composite patch comprising aligned polyurethane nanofiber membranes integrated with methacrylated hyaluronic acid (MHA) hydrogel arrays loaded with arbutin or kojic acid. Seven-week-old Hairless Mouse, Strain 2 (HRM2) mice were assigned to six groups: control (CTL), UVB only (UV), UVB plus topical arbutin (UVA), UVB plus topical kojic acid (UVK), UVB plus arbutin-loaded MHA patch (UV-A-MHA), and UVB plus kojic acid-loaded MHA patch (UV-K-MHA). Dorsal skin received a single UVB dose (200 mJ/cm2), was treated immediately, and was analyzed on Day 4. Drug-loaded MHA patch treatment attenuated UVB-induced epidermal thickening and was associated with qualitative differences in dermal matrix organization, while direct comparisons with the corresponding freely applied formulations varied across endpoints. These histological findings were evaluated using hematoxylin and eosin, Masson's trichrome, Picro-Sirius Red, and Fontana-Masson staining. GFP-loaded MHA hydrogels remained detectable in the epidermis and upper dermis through Day 4, supporting local cargo retention under skin-contact conditions. Preliminary HPLC-UV analysis detected arbutin and kojic acid parent peaks in MHA formulations before and after 60 s of UV exposure. Patch treatment was associated with significant reductions in α-smooth muscle actin and vimentin, whereas effects on SMAD phosphorylation differed between the two drug formulations, without detectable changes in body weight or serum TNF-α and IL-6. Because the main experiment lacked drug-free MHA patch and bandage-only controls, scaffold-, occlusion-, and drug-specific effects could not be fully separated. These findings support aligned nanofiber-supported MHA hydrogel arrays as functional biomaterial patches for localized cutaneous delivery and modulation of acute UVB-induced remodeling-associated responses.

PMID 42929246
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PubMedPakistan journal of pharmaceutical sciences2026-10-26

Stability studies and characterization of nanoemulgel containing gallic acid.

Awan Hina H, Khan Hira H, Haq Rizwan Ul RU, Fatima Nighat N et al.

Gallic acid is a natural phenolic compound with excellent antioxidant, antimicrobial and anti-inflammatory activity and good skin penetration. Gallic acid demonstrates both stability and solubility problems in topical formulations. A nanoemulgel combines an emulsion for enhanced solubility with a gel base for improved physical stability. The main objective of this study is to characterize and assess the stability of a gallic acid-containing nanoemulgel. Various gallic acid nanoemulsions (GNE) were prepared using optimized ratios of oil, surfactants, gallic acid and water and evaluated for stability. Finally, stable GNE-19 was characterized for particle size and converted to nanoemulgel (GNEG-19). Nanoemulgel was subjected to short-term and accelerated stability studies and characterized for pH, viscosity, spreadability, occlusion effect, FTIR, in-vitro drug release and in-vitro pharmacological activities. The results showed that formulation GNEG-19 showed optimum thermodynamic stability, having no phase separation and color change. The droplet size of freshly prepared GNE and after 28 days was 175.43nm and 183.23nm, respectively. The pH was slightly acidic but still within the human skin range (3.9-4.5). No interaction was found between the gallic acid and other components of nanoemulgel following FTIR analysis. The viscosity of freshly prepared GNEG-19 was 2127.1 cP and after 90 days, it was 2102.3 cP, which showed its stability. The percent drug release of gallic acid from nanoemulgel after 24 hrs was 93.12%. GNEG-19 also showed effective occlusion properties when compared with gel base and petroleum jelly. In-vitro pharmacological activities showed that GNEG-19 had antioxidant activity of 63.77% and a zone of inhibition (ZOI) of 11.4 mm compared to pure gallic acid (9.5 mm). In conclusion, nanoemulgel containing gallic acid showed good physical and chemical stability and was pharmacologically active.

PMID 42929401
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PubMedGels (Basel, Switzerland)2026-10-26

Cyclodextrin-Containing Tannic Acid-Lipoic Acid Hydrogels for the Loading and Reduction-Responsive Release of Nile Red.

Zhu Yuzheng Y, Kobayashi Kazuya U KU, Hatano Akihiko A, Suzuki Manabu M et al.

Hydrophobic molecules are generally difficult to incorporate into aqueous hydrogels because of their poor water solubility. In this study, a cyclodextrin (CD)-containing tannic acid-lipoic acid (TA-LA) hydrogel was developed using lipoic acid-modified β-cyclodextrin (LACD). LACD retained the host-guest recognition ability of the cyclodextrin cavity after lipoic acid modification and was successfully incorporated into the TA-LA hydrogel without interfering with gel formation. Using Nile Red (NR) as a model hydrophobic molecule, the LACD-containing hydrogel showed higher NR encapsulation efficiency and greater cyclodextrin retention than the hydrogel containing unmodified β-cyclodextrin. The LACD-containing hydrogel also exhibited reduction-responsive NR release in the presence of dithiothreitol (DTT). These results show that LACD can be incorporated into the TA-LA hydrogel while retaining the host-guest recognition ability of the cyclodextrin cavity and can be used for reduction-responsive release of NR.

PMID 42929903
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PubMedPakistan journal of pharmaceutical sciences2026-10-26

Chicoric acid regulates IL-1β to improve the inflammatory response in mice undergoing myomectomy under propofol anesthesia.

Zhai Zixuan Z, Zhao Zheng Z, Yu Jianfeng J

Surgical excision of uterine fibroids triggers acute inflammation, impacting postoperative recovery. Propofol anesthesia may modulate this response. Chicoric acid possesses anti-inflammatory properties, but its perioperative utility remains unexplored. To investigate whether preoperative chicoric acid enhances the anti-inflammatory effect of propofol in a mouse model of myomectomy and to explore the involvement of the p38 MAPK/NF-κB/IL-1β axis. A human uterine fibroid xenograft mouse model was established using CB-17 SCID mice. Mice underwent simulated myomectomy under propofol or ketamine anesthesia, with or without preoperative chicoric acid (50 mg/kg, 7 days). Controls included sham and model groups. The p38 MAPK/NF-κB agonist LPS and the IL-1β blocker Rilonacept were used to probe mechanisms. Inflammatory cytokines (MSD), pathway protein expression (Western blot), and uterine histopathology (H&E) were assessed 12h post-surgery. Propofol anesthesia significantly inhibited surgery-induced p38 MAPK/NF-κB activation and reduced levels of inflammatory cytokines compared with the model group. Preoperative cholic acid further suppressed this pathway and enhanced the anti-inflammatory effect beyond that of propofol alone. LPS reversed chicoric acid's effects, confirming the involvement of the pathway. Unexpectedly, Rilonacept did not enhance but rather reversed the anti-inflammatory effect of chicoric acid, suggesting complex, compensatory interactions within a cytokine network. Preoperative chicoric acid augments propofol's anti-inflammatory effect during myomectomy by inhibiting the p38 MAPK/NF-κB pathway. However, the paradoxical effect of IL-1β blockade reveals unforeseen complexity in the perioperative cytokine network, warranting further investigation into the multitarget effects of chicoric acid and potential network-compensation mechanisms.

PMID 42929413
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PubMedEuropean journal of immunology2026-10-26

Cholic Acid Reprograms RORγt+ Th17 Cells into IL-10-Producing T Cells to Limit Experimental Colitis.

Dalal Rajdeep R, Sadhu Srikanth S, Singla Poonam P, Madan Upasna U et al.

Inflammatory bowel disease (IBD) is a relapsing-remitting inflammatory disorder of the gastrointestinal tract driven by dysregulated T helper (Th)-cell responses, gut microbiota imbalance, and altered bile acid metabolism. While cholic acid (CA), a primary bile acid, is immunotoxic at high concentrations, its immunomodulatory role at physiological levels remains unclear. Here, we evaluate the therapeutic potential of CA in an experimental colitis model. Administration of biologically tolerable CA significantly reduced disease activity, preserved colon length, and alleviated histological inflammation. Mechanistically, CA downregulated RORγt levels and promoted Th cell plasticity toward IL-10-producing phenotypes, resulting in diminished production of IFN-γ and IL-17. Dietary depletion of primary bile acid precursors and IL-10 neutralization confirmed IL-10-dependent immunoregulation as a key mechanism. Additionally, synthetic derivatives of CA, similar to CA, attenuated DSS-induced colitis by selectively expanding IL-10-producing Th cells. Collectively, these findings highlight CA and its synthetic derivatives as immunomodulatory candidates for the therapy of ulcerative colitis.

PMID 42929495
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PubMedMicrobiology spectrum2026-10-26

Integrated microbiome and metabolomic profiling reveals alterations across the adenoma-colorectal cancer sequence.

Chang Tien-En T-E, Lin Hung-Hsin H-H, Luo Jiing-Chyuan J-C, Chen Ying-Fan Y-F et al.

The incidence of colorectal cancer (CRC) has been increasing in Taiwan and is associated with multiple risk factors. Increasing evidence suggests that gut microbiota dysbiosis contributes to CRC development. This study aimed to characterize microbial and metabolic alterations across premalignant and malignant colorectal lesions and to identify potential microbiome-associated biomarkers. Individuals undergoing colonoscopy for screening or surveillance at Taipei Veterans General Hospital were enrolled. Gut microbial composition was analyzed using full-length 16S rRNA gene sequencing to achieve high-resolution taxonomic profiling. Predicted functional pathways were inferred from microbial communities, and targeted metabolomic profiling was performed to evaluate microbial metabolic outputs. A total of 122 individuals were included, comprising 62 healthy controls, 15 adenoma cases, and 45 CRC cases. Change in microbial composition and predicted functional pathways were observed across the control, adenoma, and CRC groups. Control-associated taxa were linked to carbohydrate fermentation and amino acid metabolism pathways, whereas CRC-associated taxa, particularly Fusobacterium, showed broad negative correlations with multiple biosynthetic pathways. Metabolomic analysis showed increased tauro-ursocholanic acid and reduced short-chain fatty acids (SCFAs) in CRC. CRC-associated bacteria were negatively correlated with SCFAs and positively correlated with several bile acid metabolites, including lithocholic acid, murocholic acid, tauro-ursocholanic acid, and taurohyocholic acid. Integrative analysis of full-length 16S rRNA sequencing, predicted functional pathways, and metabolomic profiling identified microbial and metabolic differences across the control, adenoma, and CRC groups. These findings are consistent with an association between gut microbial alterations and colorectal neoplasia and may inform future studies of microbial and metabolic biomarkers for CRC.IMPORTANCEColorectal cancer (CRC) develops through an adenoma-carcinoma sequence, yet the microbial and metabolic alterations accompanying this progression remain incompletely understood. In this study, we integrated full-length 16S rRNA gene sequencing with metabolomic profiling to characterize taxonomic, functional, and metabolic changes across healthy controls, adenoma, and CRC. Our results showed coordinated changes in microbial taxa, predicted metabolic pathways, and fecal metabolites across the control, adenoma, and CRC groups. Control-associated taxa were linked to pathways related to carbohydrate fermentation and amino acid metabolism, whereas CRC-associated taxa, particularly Fusobacterium, showed negative correlations with several biosynthetic pathways. In addition, CRC-associated taxa were associated with reduced short-chain fatty acids (SCFAs) and increased levels of certain bile acid-related metabolites. These findings suggest an association between microbiome-associated metabolic alterations and colorectal neoplasia and support further investigation of microbial and metabolic biomarkers.

PMID 42929529
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