Trang: 79
Tập 32, số 9 2022
Identification of bioactive compounds Inhibitors of M. tuberculosis Growth Using Whole Cell Based High-Throughput Screening
Tác giả: Pham Thi Kim Lien, Sang Huyn Cho, Tran Thi Van Phuong, Tran Thi Mai Hung, Vu Thi Mai Anh, Dang Duc Anh
Tóm tắt:
Drug discovery and development for Mycobacterium tuberculosis (Mtb) has progressed significantly in more than
20 years, although it is still woefully underfunded. From a drug discovery perspective, tuberculosis is a particularly
challenging disease. Screening for new antimicrobial agents is routinely conducted only against actively replicating
bacteria. However, it is now widely accepted that a physiological state of nonreplicating persistence (NRP) is responsible for antimicrobial tolerance in many bacterial infections. The MICs of 138 established pure bioactive compounds
determined in microplate cultures, of which anaerobic conditions were maintained for ten days and, for comparative
purposes, aerobic conditions for seven days. Cultures exposed to drugs under anaerobic conditions followed by 28h of
“recovery” under ambient oxygen produced a luminescent signal that was, for most compounds, proportional to the
number of hits determined > 90% in MICs MABA was 99 (71.7%), GAS was 118 (85.5%), and MICs LORA was
7 (5.1%). As a result, aerobic and anaerobic bacteria conditions in vitro assays are prone to support a drug discovery
program for tuberculosis. These potential bioactive compounds are in the drug discovery and development of anti-tubercular drugs.
Summary:
Từ khóa:
Mycobacterium tuberculosis; High - Throughput screening; natural products; fluorescence - luminescent signal; drug discovery
DOI: https://doi.org/10.51403/0868-2836/2022/926
File nội dung:
o220979.pdf
Tải file:
