RESUMO
BACKGROUND: Treatment of mycoses is often ineffective, usually prolonged, and has some side effects. These facts highlight the importance of discovering new molecules to treat fungal infections. OBJECTIVES: To search the Medicines for Malaria Venture COVID Box for drugs with antifungal activity. METHODS: Fourteen human pathogenic fungi were tested against the 160 drugs of this collection at 1.0 µM concentration. We evaluated the ability of the drugs to impair fungal growth, their fungicidal nature, and morphological changes caused to cells. FINDINGS: Thirty-four molecules (21.25%) presented antifungal activity. Seven are antifungal drugs and one is the agricultural fungicide cycloheximide. The other drugs with antifungal activity included antibiotics (n = 3), antimalarials (n = 4), antivirals (n = 2), antiparasitcs (n = 3), antitumor agents (n = 5), nervous system agents (n = 3), immunosuppressants (n = 3), antivomiting (n = 1), antiasthmatic (n = 1), and a genetic disorder agent (n = 1). Several of these drugs inhibited Histoplasma capsulatum and Paracoccidioides brasiliensis growth (15 and 20, respectively), while Fusarium solani was not affected by the drugs tested. Most drugs were fungistatic, but niclosamide presented fungicidal activity against the three dimorphic fungi tested. Cyclosporine affected morphology of Cryptococcus neoformans. MAIN CONCLUSIONS: These drugs represent new alternatives to the development of more accessible and effective therapies to treat human fungal infections.
Assuntos
COVID-19 , Cryptococcus neoformans , Malária , Preparações Farmacêuticas , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Reposicionamento de Medicamentos , Humanos , Malária/tratamento farmacológico , Testes de Sensibilidade Microbiana , SARS-CoV-2RESUMO
BACKGROUND Treatment of mycoses is often ineffective, usually prolonged, and has some side effects. These facts highlight the importance of discovering new molecules to treat fungal infections. OBJECTIVES To search the Medicines for Malaria Venture COVID Box for drugs with antifungal activity. METHODS Fourteen human pathogenic fungi were tested against the 160 drugs of this collection at 1.0 µM concentration. We evaluated the ability of the drugs to impair fungal growth, their fungicidal nature, and morphological changes caused to cells. FINDINGS Thirty-four molecules (21.25%) presented antifungal activity. Seven are antifungal drugs and one is the agricultural fungicide cycloheximide. The other drugs with antifungal activity included antibiotics (n = 3), antimalarials (n = 4), antivirals (n = 2), antiparasitcs (n = 3), antitumor agents (n = 5), nervous system agents (n = 3), immunosuppressants (n = 3), antivomiting (n = 1), antiasthmatic (n = 1), and a genetic disorder agent (n = 1). Several of these drugs inhibited Histoplasma capsulatum and Paracoccidioides brasiliensis growth (15 and 20, respectively), while Fusarium solani was not affected by the drugs tested. Most drugs were fungistatic, but niclosamide presented fungicidal activity against the three dimorphic fungi tested. Cyclosporine affected morphology of Cryptococcus neoformans. MAIN CONCLUSIONS These drugs represent new alternatives to the development of more accessible and effective therapies to treat human fungal infections.
Assuntos
Humanos , Preparações Farmacêuticas , Cryptococcus neoformans , COVID-19 , Malária/tratamento farmacológico , Testes de Sensibilidade Microbiana , Reposicionamento de Medicamentos , SARS-CoV-2 , Antifúngicos/uso terapêutico , Antifúngicos/farmacologiaRESUMO
The aim of our study was to produce and characterize poly-ε-caprolactone (PCL) nanospheres containing essential oils from Zanthoxylum riedelianum fruit and to evaluate their stability gains as well as their insecticidal and deterrent activities against whitefly (Bemisia tabaci). The PCL nanospheres exhibited a homogeneous spherical morphology, with particle diameters between 106.7 nm and 129.2 nm, pH of approximately 6, zeta potential (ZP) lower than -19.0 mV and encapsulation efficiency higher than 98%. Only 43% of the nanoencapsulated essential oil (NSEO) was degraded in response to ultraviolet light, whereas the essential oil (EO) degraded by 76% over the same period. In a free-choice test, the NSEO and EO reduced the number of whitefly eggs by approximately 70%. NSEO and EO at 1.5% killed 82.87% and 91.23% of 2nd-instar nymphs of whitefly, respectively. Although NSEO displayed lower insecticidal activity, it offers a greater advantage over the free EO, due to protection conferred by polymer against photodegradation. Therefore, its usage may optimize the maintenance of essential oils in the field through photoprotection and controlled release. Our results suggest that the EO of Z. riedelianum fruit can be used for B. tabaci management strategy; nevertheless, the benefits of NSEO require further evaluation at the field level.