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

Bernie Byunghoon Park; Jae Wan Choi; Dawon Park; Doyoung Choi; Jiwon Paek; Hyun Jung Kim; Se Young Son; Ameeq Ul Mushtaq; Hyeji Shin; Sang Hoon Kim; Yuanyuan Zhou; Taehyeong Lim; Ji Young Park; Ji Young Baek; Kyul Kim; Hongmok Kwon; Sang Hyun Son; Ka Young Chung; Hyun Ja Jeong; Hyung Min Kim; Yong Woo Jung; Kiho Lee; Ki Yong Lee; Youngjoo Byun; Young Ho Jeon

doi:10.1038/s41598-019-44853-5

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

Bernie Byunghoon Park, Jae Wan Choi, Dawon Park, Doyoung Choi, Jiwon Paek, Hyun Jung Kim, Se Young Son, Ameeq Ul Mushtaq, Hyeji Shin, Sang Hoon Kim, Yuanyuan Zhou, Taehyeong Lim, Ji Young Park, Ji Young Baek, Kyul Kim, Hongmok Kwon, Sang Hyun Son, Ka Young Chung, Hyun Ja Jeong, Hyung Min KimYong Woo Jung, Kiho Lee, Ki Yong Lee, Youngjoo Byun, Young Ho Jeon

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

Abstract

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.

Original language	English
Article number	8762
Journal	Scientific Reports
Volume	9
Issue number	1
DOIs	https://doi.org/10.1038/s41598-019-44853-5
State	Published - 1 Dec 2019

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Park, B. B., Choi, J. W., Park, D., Choi, D., Paek, J., Kim, H. J., Son, S. Y., Mushtaq, A. U., Shin, H., Kim, S. H., Zhou, Y., Lim, T., Park, J. Y., Baek, J. Y., Kim, K., Kwon, H., Son, S. H., Chung, K. Y., Jeong, H. J., ... Jeon, Y. H. (2019). Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors. Scientific Reports, 9(1), Article 8762. https://doi.org/10.1038/s41598-019-44853-5

@article{89edabde412343f9ace0f94007b016f5,

title = "Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors",

abstract = "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.",

author = "Park, \{Bernie Byunghoon\} and Choi, \{Jae Wan\} and Dawon Park and Doyoung Choi and Jiwon Paek and Kim, \{Hyun Jung\} and Son, \{Se Young\} and Mushtaq, \{Ameeq Ul\} and Hyeji Shin and Kim, \{Sang Hoon\} and Yuanyuan Zhou and Taehyeong Lim and Park, \{Ji Young\} and Baek, \{Ji Young\} and Kyul Kim and Hongmok Kwon and Son, \{Sang Hyun\} and Chung, \{Ka Young\} and Jeong, \{Hyun Ja\} and Kim, \{Hyung Min\} and Jung, \{Yong Woo\} and Kiho Lee and Lee, \{Ki Yong\} and Youngjoo Byun and Jeon, \{Young Ho\}",

note = "Publisher Copyright: {\textcopyright} 2019, The Author(s).",

year = "2019",

month = dec,

day = "1",

doi = "10.1038/s41598-019-44853-5",

language = "English",

volume = "9",

journal = "Scientific Reports",

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Park, BB, Choi, JW, Park, D, Choi, D, Paek, J, Kim, HJ, Son, SY, Mushtaq, AU, Shin, H, Kim, SH, Zhou, Y, Lim, T, Park, JY, Baek, JY, Kim, K, Kwon, H, Son, SH, Chung, KY, Jeong, HJ, Kim, HM, Jung, YW, Lee, K, Lee, KY, Byun, Y & Jeon, YH 2019, 'Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors', Scientific Reports, vol. 9, no. 1, 8762. https://doi.org/10.1038/s41598-019-44853-5

TY - JOUR

T1 - Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors

AU - Park, Bernie Byunghoon

AU - Choi, Jae Wan

AU - Park, Dawon

AU - Choi, Doyoung

AU - Paek, Jiwon

AU - Kim, Hyun Jung

AU - Son, Se Young

AU - Mushtaq, Ameeq Ul

AU - Shin, Hyeji

AU - Kim, Sang Hoon

AU - Zhou, Yuanyuan

AU - Lim, Taehyeong

AU - Park, Ji Young

AU - Baek, Ji Young

AU - Kim, Kyul

AU - Kwon, Hongmok

AU - Son, Sang Hyun

AU - Chung, Ka Young

AU - Jeong, Hyun Ja

AU - Kim, Hyung Min

AU - Jung, Yong Woo

AU - Lee, Kiho

AU - Lee, Ki Yong

AU - Byun, Youngjoo

AU - Jeon, Young Ho

PY - 2019/12/1

Y1 - 2019/12/1

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/85068401290

U2 - 10.1038/s41598-019-44853-5

DO - 10.1038/s41598-019-44853-5

M3 - Article

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AN - SCOPUS:85068401290

SN - 2045-2322

VL - 9

JO - Scientific Reports

JF - Scientific Reports

IS - 1

M1 - 8762

ER -

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

Abstract

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