Technological application potential of polyethylene and polystyrene biodegradation by macro-organisms such as mealworms and wax moth larvae.

Multiple recent reports showed accelerated biodegradation of polyethylene by employing macro-organisms such as mealworms (Tenebrio molitor) and larvae of the greater wax moth (Galleria mellonella), which seemingly chew and digest the plastic. Nevertheless, doubts regarding analytical data were published, and results are not universally transferrable. This paper aims at gaining mechanistic insights and exploring the technological prospects of potential future optimized biodegradation.

Synthesis and in vitro and in vivo antifungal activity of the hydroxy metabolites of saperconazole.

Herein we describe the scalable diastereoselective and enantioselective syntheses of eight enantiomers of hydroxy metabolites of saperconazole. The in vitro antifungal activity of the eight stereoisomers (compounds 1-8) was compared against a broad panel of Candida spp. (n=93), Aspergillus spp.

Blood interactions with noble metals: coagulation and immune complement activation.

Noble metals are interesting biomaterials for a number of reasons, e.g., their chemical inertness and relative mechanical softness, silver's long known antimicrobial properties, and the low allergenic response shown by gold.

Pyrrolo[1,2-a][1,4]benzodiazepine: a novel class of non-azole anti-dermatophyte anti-fungal agents.

Broad screening revealed compound 1a to be a novel anti-fungal agent with high specificity towards dermatophytes. The anti-fungal structure-activity relationship of this novel class of 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepines is described together with its mode of action that appeared to be the inhibition of squalene epoxidase. Preliminary in vivo results of the most active compounds are also reported.

Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.

In search for new compounds with potential for clinical use as antifungal agents in dermatology, a series of 12 azole compounds were synthesized stereospecifically and investigated specifically for their activity against dermatophyte fungal infections in animal models. This panel of azoles was studied in vitro and compared with itraconazole and terbinafine for their antifungal activity using a panel of 24 Candida spp. and 182 dermatophyte isolates.

In vitro and in vivo activities of the novel azole antifungal agent r126638.

R126638 is a new triazole agent with potent antifungal activity in vitro against various dermatophytes, Candida spp., and Malassezia spp. Its activity against Malassezia spp.

Identification of R146225 as a novel, orally active inhibitor of interleukin-5 biosynthesis.

Interleukin (IL)-5 regulates the growth, differentiation, and activation of eosinophils. When activated, eosinophils release an array of proinflammatory and cytotoxic products and act as prominent effector cells in the process of allergic inflammation. Depriving eosinophils of IL-5 may therefore represent a viable approach to treat allergic disorders.

Activities of an intravenous formulation of itraconazole in experimental disseminated Aspergillus, Candida, and Cryptococcus infections.

An intravenous (i.v.) formulation of itraconazole was evaluated in disseminated fungal infection models in guinea pigs.

Evaluation of possible correlations between antifungal susceptibilities of filamentous fungi in vitro and antifungal treatment outcomes in animal infection models.

Nine isolates of filamentous fungi previously tested in 11 different laboratories for their susceptibilities to amphotericin B and itraconazole in vitro were injected intravenously into mice and guinea pigs, and responses to treatment with both agents were studied. The experiments were done in a single laboratory. Mean survival times, the percentages of animals surviving 12 days after infection, and culture results for samples of deep organs obtained postmortem were used as markers of antifungal efficacy.

The anti-Malassezia furfur activity in vitro and in experimental dermatitis of six imidazole antifungal agents: bifonazole, clotrimazole, flutrimazole, ketoconazole, miconazole and sertaconazole.

Bifonazole, clotrimazole, flutrimazole, ketoconazole, miconazole and sertaconazole were tested for their activity against 23 isolates of Malassezia furfur by agar dilution in vitro. Topical formulations of the same agents were evaluated for efficacy against M. furfur skin infections in guinea pigs in vivo.

The antiinflammatory effects of ketoconazole. A comparative study with hydrocortisone acetate in a model using living and killed Staphylococcus aureus on the skin of guinea-pigs.

Several reports have demonstrated the efficacy of topical ketoconazole in dermatologic conditions that are not exclusively related to fungi. Some basic pharmacologic studies have indicated effects of ketoconazole on cholesterol production in keratinocytes, on the 5-lipoxygenase enzyme, and on the metabolism of all-trans-retinoic acid in the skin. These observations have led to the hypothesis that topically applied ketoconazole may possess antiinflammatory properties.

The effects of saperconazole on the morphology of Candida albicans, Pityrosporum ovale and Trichophyton rubrum in vitro.

Fungal cultures were incubated for various periods of time with saperconazole at concentrations ranging from 10(-10) to 10(-5) M: Candida albicans (4 and 24 h), Pityrosporum ovale (2 and 7 days), and Trichophyton rubrum (1, 2, 3, 7 and 14 days). At the end of the incubation period, fungal morphology was compared with that of control cultures by transmission and scanning electron microscopy. In all three species, major ultrastructural changes were seen from concentrations of 10(-8) to 10(-7) M saperconazole onwards, depending on the species and time of incubation.

The in vitro antifungal activity of ketoconazole, zinc pyrithione, and selenium sulfide against Pityrosporum and their efficacy as a shampoo in the treatment of experimental pityrosporosis in guinea pigs.

The fungistatic and fungicidal activity of ketoconazole, zinc pyrithione, and selenium sulfide against Pityrosporum, a yeast thought to play a pathogenic role in seborrheic dermatitis and dandruff, was assessed in Dixon broth for Pityrosporum ovale and Sabouraud broth for Pityrosporum pachydermatis. Ketoconazole inhibited growth at concentrations ranging from 0.001 to 1 micrograms/ml.

Detection of circulating galactomannan by Pastorex Aspergillus in experimental invasive aspergillosis.

The performance of Pastorex Aspergillus, a new latex agglutination test for the detection of circulating galactomannan in the serum of patients with invasive aspergillosis, was evaluated in a blind trial in standardized guinea-pig models of invasive aspergillosis and other invasive mycoses. In these animal models, the invasive nature of the fungal infection was confirmed by re-isolation of the etiologic agent from the organs of every animal. Ninety-two plasma samples from 42 animals with invasive aspergillosis were submitted to the test.

Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals.

Saperconazole (R 66905) is a broad-spectrum antifungal triazole with potent in vitro activity against Aspergillus spp. A total of 279 strains were tested in brain heart infusion broth. Development of the Aspergillus spp.

Treatment of experimental zygomycosis in guinea pigs with azoles and with amphotericin B.

Nonpredisposed Albino guinea pigs were infected intravenously with Rhizopus microsporus var. rhizopodiformis or with Rhizopus oryzae. Both strains were highly pathogenic.

Activity of orally, topically, and parenterally administered itraconazole in the treatment of superficial and deep mycoses: animal models.

The activity of itraconazole in vitro was evaluated for 2,094 strains of 132 fungal species, one achloric alga, nine actinomycetes, and six bacterial species. Itraconazole was active against dermatophytes (271 strains), Candida species (1,303), Cryptococcus neoformans (27), Torulopsis species (170), Pityrosporum species (40), Aspergillus species (87), Sporothrix schenckii (12), dimorphic fungi, Dematiaceae, and various other organisms. This activity depended largely on the test conditions and the medium used.

[Anti-Candida activity of azoles].

The in vitro activity of the broad-spectrum antifungals miconazole, ketoconazole and itraconazole was evaluated by the decimal dilution method in liquid media, for respectively 2511, 1536 and 1859 strains of yeasts belonging to 31 species. Sabouraud broth was used for miconazole and brain heart infusion broth for ketoconazole and itraconazole. These three azoles proved to be potent anti-yeast compounds.

Effects of ketoconazole and itraconazole on growth and sterol synthesis in Pityrosporum ovale.

The effects of ketoconazole and itraconazole on growth and sterolsynthesis in Pityrosporum ovale was studied. Itraconazole was at least 10 times more active than ketoconazole. Sterol synthesis was inhibited more rapidly than growth, suggesting that the antifungal activity of both azoles originates from an effect on the 14 alpha demethylase system, as seen in other species.

Oral treatment with ketoconazole in systemic candidosis of guinea-pigs: microbiology, hematology and histopathology.

Non-pretreated Albino guinea-pigs were infected intravenously with Candida albicans and treated orally either with placebo or ketoconazole. The 17-day follow-up of the fungal dissemination was based upon hematology, on gross and microscopic lesions and on the demonstration of the fungus by culture techniques. The efficacy of ketoconazole, both with regard to the quantity and the morphology of fungi in various organs and the tissue-healing process are discussed.

Itraconazole, a new triazole that is orally active in aspergillosis.

Itraconazole is a new orally active triazole derivative with broad-spectrum antifungal activity. This drug is effective in experimental aspergillosis and possesses in vitro activity against various species and strains of Aspergillus. Morphological destruction of inoculated hyphae and complete inhibition of hyphal outgrowth in culture is obtained from 0.