DICP OpenIR
Discovery of beta(2)-adrenoceptor agonists in Curcuma zedoaria Rosc using label-free cell phenotypic assay combined with two-dimensional liquid chromatography
Zhou, Weijia1,2; Wang, Jixia1; Zhao, Yaopeng1; Yu, Long1; Fang, Ye3; Jin, Hongli1; Zhou, Han1; Zhang, Pengyu1; Liu, Yanfang1; Zhang, Xiuli1,4; Liang, Xinmiao1,4
Corresponding AuthorLiu, Yanfang(liuyanfang@dicp.ac.cn) ; Zhang, Xiuli(zhangxiuli@dicp.ac.cn) ; Liang, Xinmiao(liangxm@dicp.ac.cn)
KeywordCurcuma zedoaria Rosc beta(2)-adrenoceptor agonists Diarylheptanoids Label-free cell phenotypic assay Two-dimensional liquid chromatography
Source PublicationJOURNAL OF CHROMATOGRAPHY A
2018-11-23
ISSN0021-9673
DOI10.1016/j.chroma.2018.09.053
Volume1577Pages:59-65
Funding ProjectState Key Program of National Natural Science of China[U1508221] ; Project of National Science Foundation of China[81473436] ; Project of National Science Foundation of China[31670374] ; Project of National Science Foundation of China[81803706] ; DICP, CAS[DICP TMSR201601]
Funding OrganizationState Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS
WOS SubjectBiochemical Research Methods ; Chemistry, Analytical
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry
WOS KeywordFLIGHT MASS-SPECTROMETRY ; IDENTIFICATION ; EXTRACT ; CONSTITUENTS ; COMPONENTS ; INHIBITORS ; MEDICINE ; EFFICACY ; DRUGS
AbstractTraditional Chinese Medicines (TCMs) have been widely used in clinical practice, and provided a rich source for discovering new drug leads. However, efficient identification of active molecules responsible for the therapeutic effects of complex TCMs is still highly challenging. Here, we combined label-free cell phenotypic assay with two dimensional liquid chromatography (2DLC) to identify potential beta(2)-adrenoceptor (beta(2)-AR) agonists related to anti-asthmatic effect of Curcuma zedoaria Rosc (C.zedoaria), a commonly used TCM. The ethyl acetate extract of C.zedoaria was first fractionated into 26 fractions. Label free cell phenotypic profiling was then used to locate the active sites. Orthogonal second-dimensional (D2) separation was performed on two fractions displaying agonistic effect at the beta(2)-AR, combined with screening of the D2 fractions to track the activity. Finally, this approach led to the isolation of three known diarylheptanoids, among which diarylheptanoid b exhibited the most potent agonistic activity with an EC50 value of 5.93 mu M. This result was further demonstrated through the chemical synthesis of diarylheptanoid b. It is the first time to discover that diarylheptanoids could activate the beta(2)-AR, which may be responsible for the anti -asthmatic effect of C.zedoaria observed traditionally and in clinical application. This study also demonstrates the potential of this integrated strategy for identifying active ingredients and determining the basis of therapeutic materials in complex TCMs. (C) 2018 Elsevier B.V. All rights reserved.
Language英语
Funding OrganizationState Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS ; State Key Program of National Natural Science of China ; State Key Program of National Natural Science of China ; Project of National Science Foundation of China ; Project of National Science Foundation of China ; DICP, CAS ; DICP, CAS
WOS IDWOS:000452343500008
PublisherELSEVIER SCIENCE BV
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/166417
Collection中国科学院大连化学物理研究所
Corresponding AuthorLiu, Yanfang; Zhang, Xiuli; Liang, Xinmiao
Affiliation1.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100000, Peoples R China
3.Corning Inc, Biochem Technol Sci & Technol Div, Corning, NY 14831 USA
4.Nantong Univ, Coinnovat Ctr Neuroregenerat, Nantong 226019, Peoples R China
Recommended Citation
GB/T 7714
Zhou, Weijia,Wang, Jixia,Zhao, Yaopeng,et al. Discovery of beta(2)-adrenoceptor agonists in Curcuma zedoaria Rosc using label-free cell phenotypic assay combined with two-dimensional liquid chromatography[J]. JOURNAL OF CHROMATOGRAPHY A,2018,1577:59-65.
APA Zhou, Weijia.,Wang, Jixia.,Zhao, Yaopeng.,Yu, Long.,Fang, Ye.,...&Liang, Xinmiao.(2018).Discovery of beta(2)-adrenoceptor agonists in Curcuma zedoaria Rosc using label-free cell phenotypic assay combined with two-dimensional liquid chromatography.JOURNAL OF CHROMATOGRAPHY A,1577,59-65.
MLA Zhou, Weijia,et al."Discovery of beta(2)-adrenoceptor agonists in Curcuma zedoaria Rosc using label-free cell phenotypic assay combined with two-dimensional liquid chromatography".JOURNAL OF CHROMATOGRAPHY A 1577(2018):59-65.
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