Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors

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 TSL...

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Detalles Bibliográficos
Autores principales: Park, Bernie Byunghoon, Choi, Jae Wan, Park, Dawon, Choi, Doyoung, Paek, Jiwon, Kim, Hyun Jung, Son, Se-Young, Mushtaq, Ameeq Ul, Shin, Hyeji, Kim, Sang Hoon, Zhou, Yuanyuan, Lim, Taehyeong, Park, Ji Young, Baek, Ji-Young, Kim, Kyul, Kwon, Hongmok, Son, Sang-Hyun, Chung, Ka Young, Jeong, Hyun-Ja, Kim, Hyung-Min, Jung, Yong Woo, Lee, Kiho, Lee, Ki Yong, Byun, Youngjoo, Jeon, Young Ho
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6584507/
https://www.ncbi.nlm.nih.gov/pubmed/31217492
http://dx.doi.org/10.1038/s41598-019-44853-5
Descripción
Sumario: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.

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