Academic Journal
Identification of anti-NSCLC bioactive compounds from Euphorbia helioscopia L. through integrated pharmacological classification and metabolomics analysis.
| Τίτλος: | Identification of anti-NSCLC bioactive compounds from Euphorbia helioscopia L. through integrated pharmacological classification and metabolomics analysis. |
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| Συγγραφείς: | Yu X; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Bai C; School of Basic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China., Wang T; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Yang Y; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Deng Y; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Li C; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Hu W; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China., Li R; School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China. Electronic address: lirui@cdutcm.edu.cn., Yang J; School of Basic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China. Electronic address: yangjiahui@cdutcm.edu.cn., Hu K; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, China. Electronic address: kaifenghu@cdutcm.edu.cn. |
| Πηγή: | Journal of pharmaceutical and biomedical analysis [J Pharm Biomed Anal] 2026 Oct 15; Vol. 279, pp. 117586. Date of Electronic Publication: 2026 May 27. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Science Country of Publication: England NLM ID: 8309336 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-264X (Electronic) Linking ISSN: 07317085 NLM ISO Abbreviation: J Pharm Biomed Anal Subsets: MEDLINE |
| Imprint Name(s): | Publication: <2006->: London : Elsevier Science Original Publication: Oxford ; New York : Pergamon Press, c1983- |
| Ιατρικοί όροι (MeSH): | Euphorbia*/chemistry , Lung Neoplasms*/drug therapy , Lung Neoplasms*/metabolism , Lung Neoplasms*/pathology , Carcinoma, Non-Small-Cell Lung*/drug therapy , Carcinoma, Non-Small-Cell Lung*/metabolism , Carcinoma, Non-Small-Cell Lung*/pathology , Antineoplastic Agents, Phytogenic*/pharmacology , Antineoplastic Agents, Phytogenic*/isolation & purification , Plant Extracts*/pharmacology , Plant Extracts*/chemistry, Metabolomics/methods ; Apoptosis/drug effects ; Chromatography, High Pressure Liquid/methods ; Cell Proliferation/drug effects ; Humans ; Cell Line, Tumor |
| Περίληψη: | Euphorbia helioscopia L. (commonly known as Zeqi) has been reported to possess anti-tumor potential, however, its bioactive constituents and underlying molecular mechanisms against non-small cell lung cancer (NSCLC) remain to be elucidated. This study aimed to systematically identify anti-NSCLC components and explore their associated mechanisms through integrated pharmacological classification and metabolomics analysis. Zeqi samples exhibiting distinct in vitro antiproliferative activities were first classified into relatively higher-activity (RHA) and relatively lower-activity (RLA) group, and then subjected to metabolomics profiling using ultra performance liquid chromatography-high resolution mass spectrometry (UPLC-HRMS) and subsequent univariate and multivariate statistical analysis. Four compounds (fraxetin, 2''-O-galloylhyperoside, isofraxidin and myricitrin 3-O-galactoside) were identified as candidate bioactive constituents associated with the antiproliferative activity of Zeqi. Among these, fraxetin exhibited the most potent inhibitory effect against NSCLC cells. Flow cytometric analysis revealed a dose-dependent increase in apoptotic rates. Transcriptomic analysis indicated that fraxetin regulates the expression of apoptosis-related genes and activates apoptotic pathways. Further reverse transcription quantitative polymerase chain reaction (RT-qPCR) and Western blot analyses confirmed that fraxetin-induced apoptosis in NSCLC cells might be associated with its ability to upregulate Noxa and downregulate Mcl-1 at both transcriptional and translational levels. In conclusion, the successful application of integrated pharmacological classification and metabolomics analysis not only enabled the identification of anti-NSCLC active components in Zeqi but also provides a robust methodological framework for efficient discovery of bioactive lead compounds from complex traditional Chinese medicine (TCM) systems. (Copyright © 2026 Elsevier B.V. All rights reserved.) |
| Competing Interests: | Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: Euphorbia helioscopia L.; Fraxetin; Metabolomics; Non-small cell lung cancer; Pharmacological classification |
| Substance Nomenclature: | 0 (Antineoplastic Agents, Phytogenic) 0 (Plant Extracts) |
| Entry Date(s): | Date Created: 20260528 Date Completed: 20260610 Latest Revision: 20260610 |
| Update Code: | 20260611 |
| DOI: | 10.1016/j.jpba.2026.117586 |
| PMID: | 42208414 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1873-264X |
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| DOI: | 10.1016/j.jpba.2026.117586 |