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

Park, Bernie Byunghoon; Choi, Jae Wan; Park, Dawon; Choi, Doyoung; Paek, Jiwon; Kim, Hyun Jung; Son, Se-Young; Ul Mushtaq, Ameeq; 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

doi:10.1038/s41598-019-44853-5

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

Park, Bernie Byunghoon;
Choi, Jae Wan;
Park, Dawon;
Choi, Doyoung;
Paek, Jiwon;
... Jung, Yong Woo;
... Lee, Kiho;
... Lee, Ki Yong;
... Byun, Youngjoo;
... Jeon, Young Ho;
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초록

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.

키워드

THYMIC STROMAL LYMPHOPOIETIN; INNATE LYMPHOID-CELLS; BIOLOGICAL EVALUATION; TYPE-2 IMMUNITY; DERIVATIVES; FLAVONOIDS; CYTOKINE; BINDING; INFLAMMATION; CHALCONES

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

저자: Park, Bernie Byunghoon; Choi, Jae Wan; Park, Dawon; Choi, Doyoung; Paek, Jiwon; Kim, Hyun Jung; Son, Se-Young; Ul Mushtaq, Ameeq; 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

DOI: 10.1038/s41598-019-44853-5

발행일: 2019-06-19

유형: Article

저널명: Scientific Reports

권: 9