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3,6-Dihydroxyflavone Has Antituberculosis Activity and Suppresses Lung Inflammation
곽철희,이영준,전다솜,DURAIPRASANNAVENKATESH,류성원,김양미 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.8
The antimycobacterial and anti-inflammatory effects of 3,6-dihydroxyflavone (3,6-DHF), a flavonoid with anticancer and antibacterial activities, were investigated in lipopolysaccharide (LPS)-stimulated human lung fibroblast MRC-5 cells. 3,6-DHF had antimycobacterial effects on Mycobacterium tuberculosis (Mtb) H37Rv, multidrug-resistant, and extensively drug-resistant clinical isolates with mean minimum inhibitory concentrations of 25, 100, and 100 µg/mL, respectively. 3,6-DHF bound Mtb β-ketoacyl-acyl carrier protein synthase III (mtKASIII) with high affinity through hydrogen bonding of 3,6-DHF of A-ring 6-hydroxyl and C-ring 3-hydroxyl groups with Tyr304 and Gly209 of mtKASIII. Comparison of 3,6-DHF and 3,6,3′,4′-tetrahydroxyflavone (3,6,3′,4′-THF) activities revealed that 3,6,3′,4′-THF did not have anti-tuberculosis (TB) activity, implying that increased hydrophilicity decreases TB membrane permeabilization. 3,6-DHF reduced tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-12, IL-1β, and matrix metalloproteinase (MMP)-1 mRNA levels and suppressed phosphorylation levels of extracellular signal-regulated kinase (ERK) in LPS-stimulated MRC-5 cells. These data indicate that 3,6-DHF could be developed as a potential anti-TB drug, which also suppresses lung inflammation.
Rhamnetin Exhibits Anti-Tuberculosis Activity and Protects against Lung Inflammation
Min Jun Kim,전다솜,곽철희,Sungweon Ryoo,김양미 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.10
Rhamnetin, a natural flavonoid found in cloves and berries has been reported to show anti-inflammatory activities in lipopolysaccharide-stimulated RAW264.7 cells and may be a potent inhibitor for extracellular signal-regulated kinase 1 (ERK1) and c-Jun N-terminal kinase. Here, we showed that rhamnetin has antimycobacterial effects on Mycobacterium tuberculosis (MT) H37Rv, multi-drug-, and extensively drug-resistant clinical isolates. We also investigated the effect of rhamnetin on interferon (IFN)-γ-stimulated human lung fibroblast MRC-5 cells, since MT infection causes intensive lung inflammation. Rhamnetin suppressed mRNA levels of tumor necrosis factor-α, interleukin (IL)-1β, IL-6, IL-12, and matrix metalloproteinase-1. Furthermore, it inhibited IFN-γ-mediated stimulation of ERK1 and p38 mitogen-activated protein kinase in MRC-5 cells. These results showed that rhamnetin has potent anti-tuberculosis activities and effectively suppresses lung inflammation, implying that rhamnetin can be a potent anti-tuberculosis dietary agent.
전다솜,Binu Jacob,곽철희,김양미 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.11
Papiliocin is a 37-residue antimicrobial peptide, with Trp2 and Phe5 previously reported as key residues necessary for its antibacterial activity. This study determined the essential length of the N-terminal fragment of papiliocin necessary to retain its biological activity. We designed and synthesized an array of seven peptides from the N-terminal helix (PapN), with longest peptide with 22 residues and the shortest peptide consisting of the first 10 residues. The minimum inhibitory concentration (MIC) values and cytotoxicity measurement revealed that a PapN-12mer containing a three-turn, amphipathic helix was the shortest peptide exhibiting antibacterial activity without cytotoxicity. Additionally, PapN-20mer peptide containing two isoleucines at the C-terminus represented the shortest peptide exhibiting potent anti-inflammatory activities by inhibiting nitric oxide production and inflammatory cytokine production in lipopolysaccharide-stimulated mouse macrophage RAW264.7 cells. These results provided valuable insights into the design of short, potent peptide analogs of papiliocin.