Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors.
Bernie Byunghoon ParkJae Wan ChoiDawon ParkDoyoung ChoiJiwon PaekHyun Jung KimSe-Young SonAmeeq Ul MushtaqHyeji ShinSang Hoon KimYuanyuan ZhouTaehyeong LimJi Young ParkJi-Young BaekKyul KimHongmok KwonSang-Hyun SonKa Young ChungHyun-Ja JeongHyung-Min KimYong Woo JungKiho LeeKi Yong LeeYoungjoo ByunYoung Ho JeonPublished in: Scientific reports (2019)
Thymic stromal lymphopoietin (TSLP) plays an important role in the differentiation and proliferation of Th2 cells, resulting in eosinophilic inflammation and numerous allergic diseases. Baicalein (1), a major component of Scutellaria baicalensis, was found to be the first small molecule to block TSLP signaling pathways. It inhibited effectively eosinophil infiltration in house dust mite-induced and ovalbumin-challenged mouse models. Structure-activity relationship studies identified compound 11a, a biphenyl flavanone analog, as a novel human TSLP inhibitor for the discovery and development of new anti-allergic drugs.
Keyphrases
- small molecule
- signaling pathway
- induced apoptosis
- allergic rhinitis
- structure activity relationship
- endothelial cells
- oxidative stress
- mouse model
- high glucose
- cell cycle arrest
- diabetic rats
- protein protein
- pi k akt
- drug induced
- high throughput
- bone marrow
- cell death
- induced pluripotent stem cells
- human health
- risk assessment
- health risk assessment
- polycyclic aromatic hydrocarbons
- single cell
- drinking water
- chronic rhinosinusitis