Antibacterial activity of griseofulvin analogues as an example of drug repurposing. Griseofulvin is a well-known antifungal drug that was launched in 1962 by Merck & Co. for the treatment of dermatophyte infections. However, according to predictions using the Way2Drug computational drug repurposing platform, it may also have antibacterial activity. As no confirmation of this prediction was found in the published literature, this study estimated in-silico antibacterial activity for 42 griseofulvin derivatives. Antibacterial activity was predicted for 33 of the 42 compounds, which led to the conclusion that this activity might be considered as typical for this chemical series. Therefore, experimental testing of antibacterial activity was performed on a panel of Gram-positive and Gram-negative micro
The science and rationale of arriving at the correct drug & dosimetry of griseofulvin, fluconazole, terbinafine, and itraconazole in superficial dermatophyte infections: an important step before a pragmatic trial.
Limited effectiveness of four oral antifungal drugs (fluconazole, griseofulvin, itraconazole and terbinafine) in the current epidemic of altered dermatophytosis in India: results of a randomized pragmatic trial. Dermatophytic infections have undergone unprecedented changes in India in the recent past. Clinical trials to find out the effectiveness of the four main oral antifungal drugs are lacking. We tested the effectiveness of oral fluconazole, griseofulvin, itraconazole and terbinafine in chronic and chronic relapsing tinea corporis, tinea cruris and tinea faciei in an investigator-initiated, randomized, pragmatic trial. Two hundred patients with microscopy-confirmed tinea were allocated to four groups (50 patients in each group): fluconazole 5 mg kg per day, griseofulvin 10 mg kg per
Clinico-mycological profile of tinea capitis and its comparative response to griseofulvin versus terbinafine. Tinea capitis is the most common superficial mycosis in children. This disease is a contagious infection with worldwide distribution and is occasionally associated with permanent alopecia. The treatment of this infection usually requires the administration of appropriate oral antifungal agents. The current study was conducted to evaluate the clinico-mycological profile of tinea capitis and compare the efficiency of oral griseofulvin and terbinafine in the treatment of this disease. This study was conducted on 69 patients, including 23 females (33.3%) and 46 males (66.7%), clinically suspected of tinea capitis. After the confirmation of tinea capitis diagnosis through direct
Utility of Laboratory Test Result Monitoring in Patients Taking Oral Terbinafine or Griseofulvin for Dermatophyte Infections. Terbinafine hydrochloride and griseofulvin are effective oral treatments for dermatophyte infections but have been associated with hepatic and hematologic abnormalities. The prevalence of alanine aminotransferase elevations, aspartate aminotransferase elevations, anemia , lymphopenia, and neutropenia among adults and children taking terbinafine and griseofulvin is unclear. To measure the rate of laboratory test result abnormalities in healthy adults and children taking terbinafine or griseofulvin for dermatophyte infections. This retrospective study assessed adults and children taking terbinafine or griseofulvin for dermatophyte infections from January 1, 2006, to December
Design, Synthesis, and Cytotoxicity Evaluation of Novel Griseofulvin Analogues with Improved Water Solubility Griseofulvin is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Study of SAR of some griseofulvin analogues has led to the identification of 2'-benzyloxy griseofulvin , a more potent analogue which retards tumor growth through inhibition of centrosomal clustering. However, similar to griseofulvin , compound exhibited poor aqueous solubility. In order to improve the poor water solubility, six new griseofulvin analogues - were synthesized and tested for their antiproliferative activity and water solubility. The semicarbazone and aminoguanidine analogues were the most potent against HCT116 and MCF
Chemoselective fluorination and chemoinformatic analysis of griseofulvin: natural vs fluorinated fungal metabolites Griseofulvin is a fungal metabolite and antifungal drug used for the treatment of dermatophytosis in both humans and animals. Recently, griseofulvin and its analogues have attracted renewed attention due to reports of their potential anticancer effects. In this study griseofulvin (1 , including two fluorinated derivatives, were centered around the chemical space that was occupied by the parent compound, griseofulvin, suggesting that modifications must preserve certain attributes of griseofulvin to conserve its activity.
Preparation and Microstructural Characterization of Griseofulvin Microemulsions Using Different Experimental Methods: SAXS and DSC The objective of the present study is to formulate and evaluate a new microemulsion (ME) for topical delivery of griseofulvin. The solubilities of griseofulvin in different combinations of surfactant to co-surfactant (S/Co ratio) were determined. Accordingly, based
Comparative Hepatotoxicity of Fluconazole, Ketoconazole, Itraconazole, Terbinafine, and Griseofulvin in Rats Oral ketoconazole was recently the subject of regulatory safety warnings because of its association with increased risk of inducing hepatic injury. However, the relative hepatotoxicity of antifungal agents has not been clearly established. The aim of this study was to compare the hepatotoxicity induced by five commonly prescribed oral antifungal agents. Rats were treated with therapeutic oral doses of griseofulvin, fluconazole, itraconazole, ketoconazole, and terbinafine. After 14 days, only ketoconazole had significantly higher ALT levels ( = 0.0017) and AST levels ( = 0.0008) than the control group. After 28 days, ALT levels were highest in the rats treated with ketoconazole followed
Griseofulvin impairs intraerythrocytic growth of Plasmodium falciparum through ferrochelatase inhibition but lacks activity in an experimental human infection study Griseofulvin, an orally active antifungal drug used to treat dermatophyte infections, has a secondary effect of inducing cytochrome P450-mediated production of N-methyl protoporphyrin IX (N-MPP). N-MPP is a potent competitive inhibitor of the heme biosynthetic-enzyme ferrochelatase, and inhibits the growth of cultured erythrocyte stage Plasmodium falciparum. Novel drugs against Plasmodium are needed to achieve malaria elimination. Thus, we investigated whether griseofulvin shows anti-plasmodial activity. We observed that the intraerythrocytic growth of P. falciparum is inhibited in red blood cells pretreated with griseofulvin
High MIC Values for Griseofulvin and Fluconazole May Indicate Resistance: A Family Outbreak Report of Trichophyton Violaceum and Systematic Review PROSPEROInternational prospective register of systematic reviews Print | PDFHigh MIC Values for Griseofulvin and Fluconazole May Indicate Resistance: A Family Outbreak Report of Trichophyton Violaceum and Systematic ReviewNoor Goandal, Ditte Saunte registration. Further detail is provided here.CitationNoor Goandal, Ditte Saunte, Julia Shen, Maiken Arendrup, Karen Astvad. High MIC Values for Griseofulvin and Fluconazole May Indicate Resistance: A Family Outbreak Report of Trichophyton Violaceum and Systematic Review. PROSPERO 2024 CRD42024506275 Available from: https://www.crd.york.ac.uk/prospero/display_record.php?ID=CRD42024506275Review questionWhat
Influence of the Encapsulation Efficiency and Size of Liposome on the Oral Bioavailability of Griseofulvin-Loaded Liposomes The objective of the present study was to investigate the influence of the encapsulation efficiency and size of liposome on the oral bioavailability of griseofulvin-loaded liposomes. Griseofulvin-loaded liposomes with desired characteristics were prepared from pro-liposome using various techniques. To study the effect of encapsulation efficiency, three preparations of griseofulvin, namely, griseofulvin aqueous suspension and two griseofulvin-loaded liposomes with different amounts of griseofulvin encapsulated [i.e., F1 (32%) and F2(98%)], were administered to rats. On the other hand, to study the effect of liposome size, the rats were given three different griseofulvin
Mechanism of the P450-Catalyzed Oxidative Cyclization in the Biosynthesis of GriseofulvinGriseofulvin is an anti-fungal agent which has recently been determined to have potential anti-viral and anti-cancer applications. The role of specific enzymes involved in the biosynthesis of this natural product has previously been determined, but the mechanism by which a p450, GsfF, catalyzes the key oxidative cyclization of griseophenone B remains unknown. Using density functional theory (DFT), we have determined the mechanism of this oxidation that forms the oxa-spiro core of griseofulvin. Computations show GsfF preferentially performs two sequential phenolic O-H abstractions rather than epoxidation to form an arene oxide intermediate. This conclusion is supported by experimental kinetic isotope
Spatial and Temporal Profiling of Griseofulvin Production in Xylaria cubensis Using Mass Spectrometry Mapping A large portion of natural products research revolves around the discovery of new, bioactive chemical entities; however, studies to probe the biological purpose of such secondary metabolites for the host organism are often limited. Mass spectrometry mapping of secondary metabolite biosynthesis in situ can be used to probe a series of ecological questions about fungi that may be lost through traditional natural products chemistry extraction protocols. A griseofulvin-producing fungal culture of the Xylariaceae family, isolated as an endophyte of the tree Asimina triloba, was analyzed through a series of spatial and temporal mapping experiments. This fungus produced unique fungal
Protective Action of Antioxidants on Hepatic Damage Induced by Griseofulvin Erythropoietic protoporphyria (EPP) is a disease associated with ferrochelatase deficiency and characterized by the accumulation of protoporphyrin IX (PROTO IX) in erythrocytes, liver, and skin. In some cases, a severe hepatic failure and cholestasis were observed. Griseofulvin (Gris) develops an experimental EPP
Bioequivalence (BE) Study of Test Griseofulvin 500 Milligram (mg) Tablets Versus Reference and Dose Proportionality Study of Test Griseofulvin 250 mg and 500 mg Tablets Under Fed Conditions Griseofulvin is an antifungal agent used in treatment of Dermatophytosis caused by Microsporum spp. (species), Trichophyton spp., Epidermophyton spp., where topical therapy is considered inappropriate or has failed. Approved dose of Griseofulvin in Adults (greater than or equal to 50 kg) in India is 500 to 1,000 mg daily, but not less than 10 mg/kg bodyweight daily. As per the World health organization (WHO) guidance, Griseofulvin belongs to Biopharmaceutical Classification System (BCS) Class 2 ("low" solubility-"high" permeability). A Bioequivalence (BE) study will be conducted in India to estimate
Treatment of tinea capitis - griseofulvin versus fluconazole - a comparative study. To compare the efficacy and safety of fluconazole and griseofulvin in the treatment of tinea capitis. Patients with tinea capitis (n = 113) with positive fungal cultures entered the study. The patients were divided into four groups with different treatment regimes. Two groups received griseofulvin 15 or 25 mg/kg /day and two groups received fluconazole 4 or 6 mg/kg/day, all for up to 12 weeks. Griseofulvin was found to be slightly better than fluconazole. The lower doses for both griseofulvin and fluconazole required significantly longer treatment duration until mycological cure than the higher doses, independent of the fungus type. Since no significant difference was found between the drugs, it is suggested