
Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown
Published: April 23, 2024
Language: Английский
Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown
Published: April 23, 2024
Language: Английский
Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown
Published: Jan. 23, 2025
Pulmonary inflammation is the main cause of lung injury. Phosphodiesterase 4 (PDE4) a promising anti-inflammatory target for treatment respiratory diseases. Herein, we designed and synthesized 43 compounds in two novel series benzimidazole derivatives as PDE4 inhibitors. Among them, compound A5 showed highly selective inhibition PDE4, good safety, liver microsomal stability vitro. administration remarkably attenuated inflammatory infiltration pathologic injury models acute mice chronic obstructive pulmonary disease (COPD) mice. In addition, enhanced sputum secretion, relieved cough mice, inhibited phosphorylation p38 MAP kinase, an important protein regulation Overall, A5, effective inhibitor without toxicity gastrointestinal reaction, may be potent candidate
Language: Английский
Citations
0Current Issues in Molecular Biology, Journal Year: 2025, Volume and Issue: 47(4), P. 262 - 262
Published: April 8, 2025
A characteristic of Chronic Obstructive Pulmonary Disease (COPD) is the inflammation respiratory pathway. Inflammatory regulators affected in COPD include cyclooxygenase-2 (COX-2), tumor necrosis factor-alpha (TNF-α), interleukin (IL-1β), and interleukin-6 (IL-6). Therefore, this systematic review aimed to investigate biological activity Indonesian medicinal plants as anti-inflammation through vitro, silico, vivo studies. digital search was conducted using Scopus, Google Scholar, PubMed online databases find relevant articles by applying specific keywords related subject interest. The results showed 18 studies that reported five proven inhibit regulation. were sambiloto (Andrographis paniculata), legetan warak (Adenostemma lavenia), kersen (Muntingia calabura), babadotan (Ageratum conyzoides), sembung rambat (Mikania micrantha Kunth). In vitro studies, A. paniculata, lavenia, M. calabura can suppress levels pro-inflammatory cytokines, such TNF-α, IL-1β, IL-6, LPS-stimulated RAW 264.7 cells. silico compounds have strong binding bind inflammatory receptors are andrographiside contained paniculata; ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid lavenia; 7-Hydroxyflavone calabura; 22,23-Dihydrospinasterol conyzoides. extracts calabura, conyzoides, reduce lung tissue animal models (hamsters, mice, rats). This might help develop treatment build scientifically natural products from for future investigations.
Language: Английский
Citations
0Biomaterials, Journal Year: 2024, Volume and Issue: 317, P. 123061 - 123061
Published: Dec. 26, 2024
Language: Английский
Citations
0Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown
Published: April 23, 2024
Language: Английский
Citations
0