Nanomole-scaled high-throughput chemistry plus direct bioautography on the same chromatography plate for drug discovery

Yüce, Imanuel; Morlock, Gertrud E.

doi:10.1016/j.aca.2021.338950

Cited by 5 publications

(2 citation statements)

References 28 publications

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“…After validating that the number of bacterial cells in a 1 mm hydrophilic droplet was comparable to that from a 96-well plate, Lei et al screened antibiotics in nanoliter scale against nanoliter bacterial suspension containing 1.8 × 10 9 ± 0.9 × 10 9 CFU mL −1 using I-DOT and CellScreenChip (CSC). Yüce and Morlock developed a high-performance thin layer chromatography-based high-throughput antibacterial assay that enabled the synthesis, identification, and screening of products from 60 organic reactions at the nano-mole level in parallel with the successful identification of antibacterial agents against B. subtilis and Aliivibrio fischeri [ 149 ]. These miniaturized approaches are extremely smart ways to screen antibacterial activities and hold potential in the antibacterial drug discovery field using a very small material (nano to picoliter) with a single bacterial cell that can screen one million compounds in a day [ 150 ].…”

Section: Natural Product Library (Npl) Screening For Antibacterial Dr...mentioning

confidence: 99%

High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery

Ayon

2023

Metabolites

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Due to the continued emergence of resistance and a lack of new and promising antibiotics, bacterial infection has become a major public threat. High-throughput screening (HTS) allows rapid screening of a large collection of molecules for bioactivity testing and holds promise in antibacterial drug discovery. More than 50% of the antibiotics that are currently available on the market are derived from natural products. However, with the easily discoverable antibiotics being found, finding new antibiotics from natural sources has seen limited success. Finding new natural sources for antibacterial activity testing has also proven to be challenging. In addition to exploring new sources of natural products and synthetic biology, omics technology helped to study the biosynthetic machinery of existing natural sources enabling the construction of unnatural synthesizers of bioactive molecules and the identification of molecular targets of antibacterial agents. On the other hand, newer and smarter strategies have been continuously pursued to screen synthetic molecule libraries for new antibiotics and new druggable targets. Biomimetic conditions are explored to mimic the real infection model to better study the ligand–target interaction to enable the designing of more effective antibacterial drugs. This narrative review describes various traditional and contemporaneous approaches of high-throughput screening of natural products and synthetic molecule libraries for antibacterial drug discovery. It further discusses critical factors for HTS assay design, makes a general recommendation, and discusses possible alternatives to traditional HTS of natural products and synthetic molecule libraries for antibacterial drug discovery.

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Section: Natural Product Library (Npl) Screening For Antibacterial Dr...mentioning

confidence: 99%

High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery

Ayon

2023

Metabolites

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“…the effect detection and analysis are performed in a miniaturized way on the same surface and the straightforward prioritization on important active compounds requires less data evaluation and data storage [9,13], hyphenated HPTLC contributes substantially to rethinking separation science and analytical methods to be more environmentally friendly and sustainable [14,15].…”

Section: Introductionmentioning

confidence: 99%

Simple performance of the planar SOS-Umu-C–FLD genotoxicity bioassay shown for perfume and packaging material analysis

Windisch,

Kittinger,

Heil

et al. 2023

JPC-J Planar Chromat

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Planar bioassays are powerful, sustainable tools for nontargeted detection of hazardous compounds in complex samples. They provide more information on a sample than corresponding in vitro assays and are more sustainable in terms of plastic material and solvent consumption. However, instrument investment costs for high-performance thin-layer chromatography are high. Hence, the question arose of whether the sophisticated sensitive planar genotoxicity bioassay could be performed manually without instrumentation under simple conditions. Cheaper plate types were studied as well as manual application of the samples, cell suspension, and substrate solution. As a result, genotoxic compound zones were detected as rose-colored or orange fluorescent resorufin end-product formed upon contact of the genotoxins in tested perfume and packaging materials with a genetically modified Salmonella Typhimurium strain. The simple performance was found to be possible for low sample application volumes. Knowledge on neutral pH value and thickness of the adsorbent layer were further key aspects. Manual spraying was found to be superior to manual immersion if excess liquid was avoided. For high sample volumes and a higher level of standardization, the open-source 2LabsToGo system was proposed as excellent option for low investment costs. Its very low instrumental footprint and the straightforward prioritization strategy help analytical chemistry to balance between technology and nature/ecology to reduce the instrumental footprint and planetary overshoot.

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Data analysis tools in thin-layer chromatography

Trifković

Andrić

Milojković‐Opsenica

et al. 2023

Instrumental Thin-Layer Chromatography

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Nanomole-scaled high-throughput chemistry plus direct bioautography on the same chromatography plate for drug discovery

Cited by 5 publications

References 28 publications

High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery

High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery

Simple performance of the planar SOS-Umu-C–FLD genotoxicity bioassay shown for perfume and packaging material analysis

Data analysis tools in thin-layer chromatography

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