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1.
PLoS One ; 18(11): e0295129, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38032959

RESUMO

Pomegranate (Punica granatum) peels have shown numerous health benefits such as antioxidant, anti-inflammatory, and antimicrobial activities. These health activities are owed to the unique phytochemical components present in pomegranate peels. Variations in the pomegranate cultivar, geographical region, and extraction methods significantly affect the phytochemical composition and concentrations of pomegranate fruits and their peels, hence their health outcomes. Therefore, this study aimed to examine the phytochemical contents of pomegranate peels of Jordanian origin and their antioxidant and antimicrobial activities. Among the 6 extracts of pomegranate peels tested, the ethanol extract exhibited the highest total phenolic content (TPC = 297.70 ± 1.73 mg GAE/g DW), highest total flavonoids content (TFC = 116.08 ± 3.46 mg RE/g DW), highest hydrolyzable tannins (HT) contents (688.50 ± 3.54 mg TE/g DW). Whereas the highest condensed tannins (CT) content was found in both the ethanol (13.87 ± 0.58 mg CE/g DW) and methanol (13.84 ± 0.55 mg CE/g DW) extracts. For the antioxidant activities, the water extract of pomegranate peels displayed the highest inhibitory effect on DPPH radicals (9.43 ± 0.06 µmole TE/g DW), while for the ABTS+ assay the methanol and ethanol extracts exhibited the highest activities of 11.09 ± 0.02 and 11.09 ± 0.06 µmole TE/g DW, respectively. For the FRAP assay, the aqueous methanol extract exhibited the highest reducing activity (1.60 ± 0.09 mmole Fe (II)/g DW). As for the antimicrobial activities of various extracts of pomegranate peels, the highest antimicrobial activity against Micrococcus luteus was achieved by the ethanol extract (MIC = 6.25 mg/mL), whereas the lowest antimicrobial activity was observed against Candida krusei using the methanol extract (MIC = 100 mg/mL). These results indicate that pomegranate peels of Jordanian origin are rich in phytochemical content and exhibited strong antioxidant and antimicrobial activities making these agroindustrial by-products potential candidates for various medical applications and possible safe sources for important bioactive components.


Assuntos
Anti-Infecciosos , Punica granatum , Antioxidantes/química , Frutas/química , Extratos Vegetais/química , Jordânia , Metanol/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Etanol/análise , Anti-Infecciosos/farmacologia , Anti-Infecciosos/análise
2.
Antimicrob Agents Chemother ; 55(10): 4789-801, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21746957

RESUMO

Fungal infections are a serious health problem in clinics, especially in the immune-compromised patient. Disease ranges from widespread superficial infections like vulvovaginal infections to life-threatening systemic candidiasis. Especially for systemic mycoses, only a limited arsenal of antifungals is available. The most commonly used classes of antifungal compounds used include azoles, polyenes, and echinocandins. Due to emerging resistance to standard therapy, significant side effects, and high costs for several antifungals, there is a medical need for new antifungals in the clinic and general practice. In order to expand the arsenal of compounds with antifungal activities, we screened a compound library including more than 35,000 individual compounds derived from organic synthesis as well as combinatorial compound collections representing mixtures of compounds for antimycotic activity. In total, more than 100,000 compounds were screened using a new type of activity-selectivity assay, analyzing both the antifungal activity and the compatibility with human cells at the same time. One promising hit, an (S)-2-aminoalkyl benzimidazole derivative, was developed among a series of lead compounds showing potent antifungal activity. (S)-2-(1-Aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole showed the highest antifungal activity and the best compatibility with human cells in several cell culture models and against a number of clinical isolates of several species of pathogenic Candida yeasts. Transcriptional profiling indicates that the newly discovered compound is a potential inhibitor of the ergosterol pathway, in contrast to other benzimidazole derivatives, which target microtubules.


Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Interações Hospedeiro-Patógeno/efeitos dos fármacos , Animais , Antifúngicos/química , Antifúngicos/toxicidade , Benzimidazóis/química , Benzimidazóis/farmacologia , Benzimidazóis/toxicidade , Células CHO , Candida/genética , Candida/isolamento & purificação , Candidíase/tratamento farmacológico , Candidíase/microbiologia , Linhagem Celular , Cricetinae , Farmacorresistência Fúngica , Ergosterol/antagonistas & inibidores , Genoma Fúngico , Células HeLa , Ensaios de Triagem em Larga Escala , Humanos , Testes de Sensibilidade Microbiana , Análise de Sequência com Séries de Oligonucleotídeos , Relação Estrutura-Atividade , Transcrição Gênica
3.
Adv Appl Bioinform Chem ; 14: 1-11, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33488102

RESUMO

INTRODUCTION: Malaysian stingless bee honey (Trigona) has been aroused as a potential antimicrobial compound with antibiofilm activity. The capability of the gram-negative bacillus P. aeruginosa to sustain a fatal infection is encoded in the bacterium genome. METHODS: In the current study, a transcriptome investigation was performed to explore the mechanism underlying the biofilm dispersal of P. aeruginosa after the exposure to Trigona honey. RESULTS: Microarray analysis of the Pseudomonas biofilm treated by 20% Trigona honey has revealed a down-regulation of 3478 genes among the 6085 screened genes. Specifically, around 13.5% of the down-regulated genes were biofilm-associated genes. The mapping of the biofilm-associated pathways has shown an ultimate decrease in the expression levels of the D-GMP signaling pathway and diguanylate cyclases (DGCs) genes responsible for c-di-GMP formation. CONCLUSION: We predominantly report the lowering of c-di-GMP through the down-regulation of DGC genes as the main mechanism of biofilm inhibition by Trigona honey.

4.
Acta Diabetol ; 57(11): 1351-1358, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32601730

RESUMO

AIM: The study evaluated the effect of different concentrations of sildenafil-containing ointment on wound healing in healthy and streptozotocin (STZ)-induced diabetic rats. METHODS: A total of 108 Sprague Dawley male rats aged 5 months were randomly divided into two groups: healthy and diabetes-inducing rats. Following induction of diabetes by intraperitoneal STZ injection (55 mg/kg), diabetic and healthy rats were subdivided into six groups (9 rats each). Linear incisions of the dorsal backs of rats were made. Then, rats were treated twice daily with either 2%, 2% + Fucidin, 5% sildenafil-containing ointments, oral sildenafil (13.0 mg/kg), moist exposed burn ointment or vehicle. During treatment, the percent reduction of the wound area and tensile strength were measured on days 3, 7 and 10. Furthermore, histopathology was performed on the wounded skin on similar days for the assessment of collagen synthesis and proliferation of new capillary vessels. RESULTS: In healthy and STZ-induced diabetic rats, the percent reduction in wound area on day 3 was significantly higher in sildenafil-containing ointment-treated groups than all other groups, whereas on day 7 only the 5% sildenafil-containing ointment-treated group showed better response in healthy rats. Although the sildenafil-containing ointment significantly showed better tensile strength than all other groups, the 5% sildenafil-treated group significantly enhanced the tensile better than the 2% and 2% + Fucidin dose. Furthermore, the histological evaluation revealed that sildenafil-containing ointment promoted collagen synthesis and proliferation of new capillary vessels. CONCLUSION: Our results suggest that sildenafil-containing ointment can provide an advantage in wound healing by promoting wound contractions and resistance to wound breakage in healthy and diabetic conditions. Therefore, 5% sildenafil-containing ointment can be used as a support factor for wound healing in healthy and diabetic conditions; however, clinical trials are required to confirm the benefits of sildenafil in wound healing.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Citrato de Sildenafila/administração & dosagem , Cicatrização/efeitos dos fármacos , Animais , Diabetes Mellitus Experimental/fisiopatologia , Humanos , Masculino , Pomadas/administração & dosagem , Ratos , Ratos Sprague-Dawley , Pele/efeitos dos fármacos , Pele/fisiopatologia
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