Metabolites characterisation of endophytic Phyllosticta fallopiae L67 isolated from Aloe vera with antimicrobial activity on diabetic wound microorganisms.

This study aimed to assess the antimicrobial activity of endophytic Phyllosticta fallopiae L67 isolated from Aloe vera against diabetic wound microorganisms and characterise their active fraction for biologically important metabolites. The dichloromethane (DCM) extract exhibited the most significant activity with inhibition zones ranging from 11.33 to 38.33 mm. The minimal inhibitory and lethality concentrations of DCM extract ranged from 78.13 to 2500.00 µg/ml and 625.00 to 5000.00 µg/ml, respectively. The extract showed teratogenicity and lethality in the zebrafish model, where peritoneal and hepatic oedema occurred at 62.50 µg/ml, and no abnormality appeared at 31.25 µg/ml. The extract also inhibited more than 82% biofilm formation. Bioassay-guided fractionation on DCM extract yielded 18 fractions and the most active fraction was subjected to UPLC-QTOF-MS/MS analysis. Flavones, stilbenes, flavanonols, isoflavonoids, phenolic glycosides and phenol derivatives were detected. In conclusion, endophytic P. fallopiae possessed bioactive metabolites with significant antimicrobial activity against diabetic wound microorganisms.

Cynometra cauliflora essential oils loaded-chitosan nanoparticles: Evaluations of their antioxidant, antimicrobial and cytotoxic activities.

Nanoencapsulation has appeared as an alternative approach to protect the bioactive constituents of essential oils (EOs) and to improve their properties. In this study, Cynometra cauliflora essential oils (CCEOs) were nanoencapsulated in chitosan nanoparticles (CSNPs) using an emulsion-ionic gelation technique. Transmission electron microscopy (TEM) images illustrated a well dispersion and spherical shape of C. cauliflora EOs-loaded chitosan nanoparticles (CCEOs-CSNPs) with an average size of less than 100 nm. In addition to that, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS) and X-ray diffraction (XRD) analyses revealed the success of CCEOs nanoencapsulation. The encapsulation efficiency (EE) was in the range of 38.83% to 44.16% while the loading capacity (LC) reached 32.55% to 33.73%. The antioxidant activity (IC50) of CCEOs-CSNPs was ranged from 21.65 to 259.13 µg/mL when assessed using DPPH radical scavenging assay. CCEOs-CSNPs showed an appreciable antimicrobial effects on diabetic wound microorganisms. Notably, cytotoxic effects against human breast cancer MCF-7 and MDA-MB-231 cells recorded IC50 of 3.72-17.81 µg/mL and 16.24-17.65 µg/mL, respectively, after 72 h treatment. Interestingly, no cytotoxicity against human breast normal MCF-10A cells was observed. Thus, nanoencapsulation using CSNPs could improve the properties of CCEOs in biomedical related applications.

Cholic acid: a novel steroidal uncompetitive inhibitor against ß-lactamase produced by multidrug-resistant isolates.

ß-lactam antibiotics are the most frequently prescribed class of drugs worldwide, due to its efficacy and good safety profile. However, the emergence of ß-lactamase producing bacterial strains eliminated the use of ß-lactam antibiotics as a chemotherapeutic choice. To restore their usability, a non-antibiotic adjuvant in conjunction with ß-lactam antibiotics is now being utilised. Cholic acid potentially acts as an adjuvant since it can blunt the pro-inflammatory activity in human. Our main objective is to scrutinise the inhibition of ß-lactamase-producing bacteria by adjuvant cholic acid, synergism of the test drugs and the primary mechanism of enzymatic reaction. Antibacterial effect of the cholic acid-ampicillin (CA-AMP) on 7 ß-lactamase positive isolates were evaluated accordingly to disc diffusion assay, antibiotic susceptibility test, as well as checkerboard analysis. Then, all activities were compared with ampicillin alone, penicillin alone, cholic acid alone and cholic acid-penicillin combination. The CA-AMP displayed notable antibiotic activity on all test bacteria and depicted synergistic influence by representing low fractional inhibitory concentration index (FIC ≤ 0.5). According to kinetic analyses, CA-AMP behaved as an uncompetitive inhibitor against beta lactamase, with reducing values of Michaelis constant (Km) and maximal velocity (Vmax) recorded. The inhibitor constant (Ki) of CA-AMP was equal to 4.98 ± 0.3 µM, which slightly lower than ampicillin (5.00 ± 0.1 µM).

Phomopsidione-Loaded Chitosan Polyethylene Glycol (PEG) Nanocomposite Dressing for Pressure Ulcers.

Pressure ulcers are commonly associated with microbial infections on the wounds which require an effective wound dressing for treatment. Thus far, the available silver dressing has shown tremendous result, however, it may cause argyria and complicate the internal organ function. Hence, our study aims to develop and characterize phomopsidione-loaded chitosan-polyethylene glycol nanocomposite hydrogel (C/PEG/Ph) as an antimicrobial dressing. Physically, the C/PEG/Ph hydrogel demonstrated a uniform light blue color, soft, flexible, and elastic, with no aggregation form. The evaluation via Fourier Transform Infrared (FTIR) exposed the C/PEG/Ph hydrogel has a notable shift towards lower frequency at 1600 and 1554 cm-1. For drug release test, the phomopsidione attained plateau at 24 h, with a total release of 67.9 ± 6.4% from the C/PEG/Ph hydrogel. There was a null burst release effect discovered throughout the experimental period. The C/PEG/Ph hydrogel showed significant results against all 4 Gram-negative bacteria and 1 yeast, with 99.99-100% reduction of microbial growth. The findings revealed that the C/PEG/Ph hydrogel can potentially act as an antimicrobial dressing for pressure ulcers.