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griseofulvin (Grisol)

✓ Approved

Transdermal · 小分子 · 小分子

什么是 griseofulvin？

griseofulvin 是一种小分子，由Transdermal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Grisol
公司Transdermal
药物类别小分子
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Transdermal

治疗适应症

griseofulvin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
InvestigationsDermatologic examination✓ Approved

相关研究文献

PubMedInternational journal of pharmaceutics2026-10-15

Evaluating the effect of griseofulvin on the disintegration properties of tablets.

Armstrong John A JA, Maclean Natalie N, Markl Daniel D, Johnston Blair F BF

Understanding how active pharmaceutical ingredients (APIs) influence tablet disintegration remains essential for optimising oral drug product performance. In this work, we present an integrated, data-driven framework that combines deep-learning-based image segmentation, automated regime detection and mechanistic modelling to characterise liquid absorption and swelling behaviours from sessile drop experiments. Using this workflow, we investigated the effect of incorporating griseofulvin into directly compressed tablets containing a variety of excipient combinations. Across all formulations, the presence of griseofulvin significantly reduced wettability and maximum swelling size, consistent with replacing hygroscopic excipients with a poorly soluble, hydrophobic drug. Bayesian hierarchical modelling confirmed credible decreases in swelling capacity for all formulations and formulation-dependent changes in initial swelling rate. Notably, MCC/lactose tablets exhibited faster initial swelling and shorter disintegration times despite reduced porosity, suggesting API-induced microstructural changes that enhance access of liquid to the swellable excipients. Overall, the proposed framework provides a rapid (<6 min), mechanistic and minimally subjective method for probing formulation-dependent disintegration behaviour. For griseofulvin, the method was sensitive to changes in absorption and swelling behaviour, highlighting its potential as a high-throughput formulation screening approach. Further studies involving a wider range of APIs are needed to determine whether these observations are generalisable and relevant to disintegration and dissolution performance.

PMID 42880651
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PubMedToxicon : official journal of the International Society on Toxinology2026-10-15

Mycotoxin-induced DNA damage response and its association with carcinogenesis.

Singh Priyanka P, Bilachi Ravindranath S RS, Yegneswaran Prakash Peralam PP, Pandit Depanshi D et al.

Fungal species produce various secondary metabolites with carcinogenic and genotoxic properties, including aflatoxins, ochratoxins, fumonisins, sterigmatocystin, and griseofulvin. Acute or chronic exposure to these mycotoxins through contaminated food and feed can cause DNA damage, chromosomal instability, and epigenetic changes, ultimately leading to cancer. This review focuses on IARC-classified carcinogenic mycotoxins and their contribution to cancer development by disrupting the DNA damage response (DDR), thereby affecting apoptosis, cell cycle regulation, and genomic stability. Current knowledge of co-exposure to mycotoxins, host susceptibility, and validated biomarkers remains limited, particularly regarding the regulation of DDR genes. This necessitates more in-depth mechanistic and epidemiological research. Network analysis of host genes associated with mycotoxins in the CTD, integrated with DDR-related genes curated from CancerSEA, identified candidate DDR-associated genes implicated in pathways related to cell cycle regulation, DNA repair, oxidative stress response, and apoptosis. These findings represent database-derived associations and computational prioritization, rather than evidence of causal mechanistic roles in mycotoxin-induced carcinogenesis. Enrichment analysis using the Enrichr tool further identified the association between mycotoxin-associated DDR genes and cancer. In brief, this review enhances the understanding of the role of mycotoxins in DDR mechanisms and their potential contribution to cancer development, thereby providing a basis for improved molecular and translational approaches to address the associated health risks.

PMID 42880423
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PubMedJournal of computer-aided molecular design2026-10-07

Identification of new ER-targeted anticancer hits active against MCF-7 breast cancer cells in the marine fungal secondary metabolite library using computative and experimental approaches.

Yurchenko Ekaterina A EA, Nesterenko Liliana E LE, Kaluzhskiy Leonid A LA, Yablokov Evgeniy O EO et al.

The identification of novel estrogen receptor (ER)-targeted anticancer compounds from marine fungal secondary metabolites was performed using a combined computational and experimental approach. A library of 461 marine fungal metabolites was analyzed using chemical space visualization, structural similarity assessment using Tanimoto indices, and target-prediction tools to identify potential ER ligands. Scaffold analysis of predicted hits suggested decalin/bicyclic terpenoid (6-6), tricyclic 6-6-6 terpenoid, bicyclic 5-6 system and several polycyclic system chemotypes as novel for ER ligands. The ER-dependence of the proposed hits cytotoxicity was tested in vitro against ER-positive human breast cancer MCF-7 cells using a 4-hydroxytamoxifen (4-OHT)-competitive viability assay. The compounds virescenoside M, cladosporin, zosteropenilline S, and griseofulvin exhibited ER-dependent cytotoxic effects on MCF-7 cells, confirming the in silico predictions. In 48 h experiments, cladosporin, zosteropenilline S, and griseofulvin at 100 µM decreased the MCF-7 cell viability by 73.6%, 33.2%, and 45.8%, respectively, but statistically significant cytotoxic effect of griseofulvin also was observed at its concentration of 1 µM. Surface plasmon resonance (SPR) experiments confirmed the direct binding of griseofulvin to ERα, with a dissociation constant (Kd) of 8.00 µM. These findings highlight marine fungi as a valuable source of novel ER-targeted anticancer agents and suggest a novel ER-dependent mechanism for the antifungal drug griseofulvin, providing a basis for its potential repositioning in ER-positive breast cancer therapy. This integrated computational-experimental strategy provides a framework for discovering new lead compounds for breast cancer treatment.

PMID 42839117
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PubMedSkin health and disease2026-09-30

A single-centre, retrospective cohort study of paediatric tinea capitis in the United Kingdom.

Herd Elliot E, Gardner Louis L, Leech Suzy S, Weiand Daniel D et al.

Contemporary understanding of the epidemiology and clinical spectrum of paediatric tinea capitis in the UK is limited, with implications for both clinical management and public health interventions. To examine recent trends in the incidence, clinical presentation and microbiological profiles of paediatric tinea capitis, and to explore the implications for quality of care and infection prevention. A single-centre retrospective cohort study was conducted of all patients aged < 18 years with microbiologically confirmed tinea capitis during two 3-year intervals: 2016-19 and 2022-25. Clinical records were reviewed for demographic features, clinical presentation, organisms identified and transmission sources, with a focus on practice standards and preventive strategies influencing quality of care. A total of 102 patients were identified: 32 from 2016-19 and 70 from 2022-25, representing a 118.8% increase in cases. Severe inflammatory presentations (kerion) rose from 19% (n = 6/32) in 2016-19 to 36% (n = 25/70) in 2022-25. Trichophyton tonsurans remained the predominant organism in both cohorts (72% vs. 74% of cultured organisms), but Trichophyton mentagrophytes newly emerged as the second most common pathogen (9% in 2022-25), having been absent in 2016-19. Barber-associated transmission was only reported in 2022-25 (n = 22), exclusively among relatively older boys, who also had a higher rate of kerion (41%). A shift in preferred oral antifungal therapy from griseofulvin to terbinafine was observed with the changing microbiological profile. Our findings demonstrate a significant rise in paediatric tinea capitis, with a disproportionate increase in inflammatory cases and a shift in causative organisms. The emergence of barber-associated transmission and T. mentagrophytes highlights evolving risk factors and the need to adapt practice standards and preventive measures to influence quality of care. Enhanced surveillance targeted educational interventions for practitioners and public, and routine practice measures to moni-tor infection sources are warranted to improve the quality of care and patient outcomes.

PMID 42813165
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PubMedMicrobiology spectrum2026-09-25

Dermatophytosis beyond Trichophyton indotineae: genomic characterization of rare keratinophilic fungi Myriodontium keratinophilum and Aphanoascus verrucosus in North India.

Kaur Amtoj A, Mahanto Sandhyarani S, Bashir Gulnaz G, Malik Meenakshi M et al.

Fungal skin infections represent the fourth most prevalent disease globally, predominantly attributed to dermatophyte species such as Trichophyton. Nevertheless, sporadic instances of dermatophytosis may also arise from opportunistic, uncommon fungi. This study documents the association of keratinophilic fungi, Myriodontium keratinophilum and Aphanoascus verrucosus, with cases of dermatophytosis in Kashmir, North India. Internal transcribed spacer region sequencing of 64 isolates obtained from skin, hair, and nail samples of 62 patients identified 61% of isolates (n = 39) as M. keratinophilum, followed by Trichophyton indotineae and A. verrucosus in 20% (n = 13) and 19% (n = 12) cases, respectively. Furthermore, the first hybrid de novo genome assembly of M. keratinophilum is reported in the present study. Genomic analysis of both M. keratinophilum and A. verrucosus species revealed median intra-species single nucleotide polymorphism (SNP) differences of 100 and 27, respectively, suggesting highly related strains in the patient population. De novo functional annotation identified a higher number of coding regions in M. keratinophilum compared to T. indotineae and A. verrucosus, including carbohydrate-active enzymes (CAZymes) exhibiting unique substrate affinities and subtilisin 3 (SUB3) gene, previously implicated as a potential virulence gene in dermatophytes. Notably, in addition to all the multidrug transporters encoded by Trichophyton species, M. keratinophilum genome contains six putative ATP-binding cassette (ABC) transporters showing 40%-70% sequence similarity with the CDR1 gene. M. keratinophilum exhibited reduced susceptibility to multiple antifungals, including high minimum inhibitory concentrations (MICs) (>16 mg/L) against griseofulvin and itraconazole. Importantly, itraconazole is a primary therapeutic agent for terbinafine-resistant T. indotineae infections, underscoring the necessity for early and accurate identification and intervention of dermatophytic infections.IMPORTANCEThe study reports cases of dermatophytosis associated with two rare keratinophilic fungi, i.e., Myriodontium keratinophilum and Aphanoascus verrucosus. The cases mainly presented as tinea corporis and cruris, commonly caused by Trichophyton indotineae in the Indian subcontinent, which may remain undiagnosed due to a lack of molecular identification. Furthermore, the first-ever genome report of M. keratinophilum and its ab initio functional annotation is useful for further studies and management of opportunistic pathogens that exhibit reduced susceptibility towards itraconazole, the first-line drug of treatment for terbinafine-resistant T. indotineae infections. An early correct molecular identification of the etiologic agents of skin infections is warranted to tackle the new agents of dermatophytosis at the earliest stage.

PMID 42788722
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PubMedTropical medicine and health2026-09-21

Antimicrobial activity of Vepris salicifolia leaf essential oil and δ-cadinene: in vitro evaluation and in silico mechanistic insights into δ-cadinene.

Paulos Biniam B, Mazumder Avijit A, Lindemann Peter P, Yeshak Mariamawit Y MY et al.

The emergence of antimicrobial resistance has intensified the search for new bioactive compounds from natural sources. This study investigated the chemical composition and antimicrobial activity of the essential oil (EO) extracted from the leaves of Vepris salicifolia (Engl.) Mziray. In addition, the molecular interactions and drug-like properties of δ-cadinene, the major constituent of the EO, were evaluated. The EO was extracted by hydrodistillation and subsequently characterized chemically using gas chromatography-mass spectrometry (GC-MS). The antibacterial and antifungal activities of the EO and δ-cadinene were assessed using disc diffusion and agar dilution assays, while molecular docking and ADMET analyses were performed to elucidate the potential mechanism of antimicrobial action and evaluate the pharmacokinetic and drug-likeness properties of δ-cadinene. GC-MS analysis identified 26 compounds, representing 84.3% of the EO. The predominant constituents were δ-cadinene (23.5%), intermedeol (18.3%), germacrene D (10.2%), α-muurolol (9.0%), and germacrene D-4-ol (7.5%). The EO and δ-cadinene effectively inhibited the growth of a wide range of Gram-positive and Gram-negative bacteria and fungi. Notably, δ-cadinene showed antibacterial activity against S. aureus ML267, with an inhibition zone of 17.8 mm, comparable to that of ciprofloxacin (18.0 mm). Furthermore, the EO exhibited greater antifungal activity against Penicillium notatum, with an inhibition zone of 14.0 mm compared with 11.0 mm for griseofulvin. Docking results showed favorable binding energies for δ-cadinene with the CrtM enzyme of S. aureus (- 7.757 kcal/mol) and the CYP51 enzyme of P. notatum (- 5.756 kcal/mol). ADMET studies further revealed that δ-cadinene has favorable drug-like characteristics, including high intestinal permeability and oral bioavailability, and did not predict any cardiotoxicity. The findings of this study indicate that V. salicifolia leaf EO, particularly δ-cadinene, represents a promising source of antimicrobial agents for future medicinal applications. Nevertheless, the predicted molecular mechanisms of δ-cadinene should be validated through enzyme inhibition assays.

PMID 42764376
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