Development of a rapid, reliable and quantitative method — “SPOTi” for testing antifungal efficacy

Rizi, Khalida; Murdan, Sudaxshina; Danquah, Cynthia Amaning; Faull, J. L.; Bhakta, Sanjib

doi:10.1016/j.mimet.2015.07.005

Cited by 13 publications

(16 citation statements)

References 21 publications

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“…This assay is modified based on the SPOTi experimental method [ 55 , 56 , 57 , 58 ] to evaluate formulated compounds more appropriately. The microtiter plate with the drug/nanoformulation and the M. smegmatis cells were prepared as for the REMA.…”

Section: Methodsmentioning

confidence: 99%

Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide

et al. 2017

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Tuberculosis (TB) is a bacterial disease responsible for millions of infections and preventable deaths each year. Its treatment is complicated by patients’ noncompliance due to dosing frequency, lengthy treatment, and adverse side effects associated with current chemotherapy. However, no modifications to the half-a-century old standard chemotherapy have been made based on a nanoformulation strategy to improve pharmacokinetic efficacy. In this study, we have designed a new nanodelivery formulation, using graphene oxide as the nanocarrier, loaded with the anti-TB antibiotic, ethambutol. The designed formulation was characterized using a number of molecular analytical techniques. It was found that sustained release of the drug resulted in better bioavailability. In addition, the designed formulation demonstrated high biocompatibility with mouse fibroblast cells. The anti-TB activity of the nanodelivery formulation was determined using whole-cell resazurin microtiter plate assay, modified-spot culture growth inhibition assay, and biofilm inhibition assay. The nanodelivery formulation showed good anti-mycobacterial activity. The anti-mycobacterial activity of Ethambutol was unaffected by the drug loading and release process. The results of this study demonstrated the potential of this new nanodelivery formulation strategy to be considered for modifying existing chemotherapy to yield more efficacious antibiotic treatment against TB.

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Section: Methodsmentioning

confidence: 99%

Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide

et al. 2017

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Section: Cytotoxicity Vs Antimycobacterial Activitymentioning

confidence: 99%

“…The novel C8-linked PBD-adenosine hybrid (PBD-ADN) 16 and intermediates 5, 11, 15 were evaluated for cytotoxicity and growth inhibition activity against Mycobacterium aurum and Mycobacterium bovis BCG (Table 1), using the high throughput agar-based spot culture growth inhibition assay (HT-SPOTi) [33][34][35] [36,37]. PBD-ADN 16 displayed no cytotoxicity against RAW 264.7 cells and was found to be ineffective against the mycobacterial strains used in this screen.…”

Section: Cytotoxicity Vs Antimycobacterial Activitymentioning

confidence: 99%

Synthesis and Biological Evaluation of a Novel C8-Pyrrolobenzodiazepine (PBD) Adenosine Conjugate. A Study on the Role of the PBD Ring in the Biological Activity of PBD-Conjugates

et al. 2020

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Here we sought to evaluate the contribution of the PBD unit to the biological activity of PBD-conjugates and, to this end, an adenosine nucleoside was attached to the PBD A-ring C8 position. A convergent approach was successfully adopted for the synthesis of a novel C8-linked pyrrolo(2,1-c)(1,4)benzodiazepine(PBD)-adenosine(ADN) hybrid. The PBD and adenosine (ADN) moieties were synthesized separately and then linked through a pentynyl linker. To our knowledge, this is the first report of a PBD connected to a nucleoside. Surprisingly, the compound showed no cytotoxicity against murine cells and was inactive against Mycobacterium aurum and M. bovis strains and did not bind to guanine-containing DNA sequences, as shown by DNase I footprinting experiments. Molecular dynamics simulations revealed that the PBD–ADN conjugate was poorly accommodated in the DNA minor groove of two DNA sequences containing the AGA-PBD binding motif, with the adenosine moiety of the ligand preventing the covalent binding of the PBD unit to the guanine amino group of the DNA duplex. These interesting findings shed further light on the ability of the substituents attached at the C8 position of PBDs to affect and modulate the biological and biophysical properties of PBD hybrids.

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“…SPOTi is a solid-culture based technique wherein an optimised number of bacteria are spotted on to agar containing a series of dilutions of inhibitor molecules. [131][132][133] This method has been adapted to 96-well microplate format thereby increasing the throughput.…”

Section: The Search For Novel Therapeutic Targetsmentioning

confidence: 99%

Early diagnosis and effective treatment regimens are the keys to tackle antimicrobial resistance in tuberculosis (TB): A report from Euroscicon's international TB Summit 2016

et al. 2016

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To say that tuberculosis (TB) has regained a strong foothold in the global human health and wellbeing scenario would be an understatement. Ranking alongside HIV/AIDS as the top reason for mortality due to a single infectious disease, the impact of TB extends far into socio-economic context worldwide. As global efforts led by experts and political bodies converge to mitigate the predicted outcome of growing antimicrobial resistance, the academic community of students, practitioners and researchers have mobilised to develop integrated, inter-disciplinary programmes to bring the plans of the former to fruition. Enabling this crucial requirement for unimpeded dissemination of scientific discovery was the TB Summit 2016, held in London, United Kingdom. This report critically discusses the recent breakthroughs made in diagnostics and treatment while bringing to light the major hurdles in the control of the disease as discussed in the course of the 3-day international event. Conferences and symposia such as these are the breeding grounds for successful local and global collaborations and therefore must be supported to expand the understanding and outreach of basic science research.

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Development of a rapid, reliable and quantitative method — “SPOTi” for testing antifungal efficacy

Cited by 13 publications

References 21 publications

Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide

Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide

Synthesis and Biological Evaluation of a Novel C8-Pyrrolobenzodiazepine (PBD) Adenosine Conjugate. A Study on the Role of the PBD Ring in the Biological Activity of PBD-Conjugates

Early diagnosis and effective treatment regimens are the keys to tackle antimicrobial resistance in tuberculosis (TB): A report from Euroscicon's international TB Summit 2016

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