ArticleChinese medicine2023
Prenylated chromones and flavonoids isolated from the roots of Flemingia macrophylla and their anti-lung cancer activity.
Article in Chinese medicine, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 7 citations in OpenAlex.
- Quantitative Structure-Activity Relationship Approaches for Exploring the Anticancer Potential of Flavonoids.Chemistry & biodiversity · 2026Review
- Naturally occurring prenylated flavonoids from AfricanRSC advances · 2025Review
- Integrated bioinformatics and network pharmacology to identify and validate macrophage polarization related hub genes in the treatment of osteoarthritis with Astragalus membranaceus.Journal of orthopaedic surgery and research · 2025Article
- High-quality assembly of the chromosomal genome for Flemingia macrophylla reveals genomic structural characteristics.BMC genomics · 2025Article
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundThe successful launch of icaritin, a therapeutic drug for liver cancer derived from Epimedium brevicornu, has provided new impetus for the development of prenylated flavonoids in the field of oncology. Flemingia macrophylla is reported to contain characteristic prenylated flavonoids which can regulate the p53 protein. We aimed to isolate these constituents and conduct activity evaluation, structure-activity relationship, and mechanism studies to provide candidate compounds for antitumor drug development.
methodsIn this study, chromatographic techniques combined with spectroscopic methods were used to separate, purify, and identify the constituents of Flemingia macrophylla methanol extract. The cytotoxic activity of the constituents was evaluated using an MTT assay with A549 and H1975 cells as the model. The binding mechanism between the compounds and the p53 protein was investigated with molecular docking and validated with cellular thermal shift assay (CETSA). Western blotting (WB) was employed to detect the expression of p53 protein and apoptosis-related proteins in cells.
resultsChiral HPLC separation of racemates 1 and 7 provided two pairs of undescribed enantiomers (1a/1b and 7a/7b), along with eight known compounds (2 - 9) isolated from Flemingia macrophylla roots. Their structures were elucidated by spectroscopic analysis, and the absolute configurations of the enantiomers were determined from experimental and calculated electronic circular dichroism data. Compounds 1 - 7, and the non-prenyl analogues 10 - 13, were evaluated for cytotoxic activity against the human lung cancer A549 and H1975 cell line. Compounds 5 - 7 displayed better cytotoxicity than the positive control icaritin in A549 and H1975, with IC
conclusionThis study demonstrates that Flemingia macrophylla is rich in prenylated flavonoid constituents, among which compounds 5 and 7 exhibited significant cytotoxic activity against A549 cells and served as reference candidates for the design and development of prenylated compounds as antitumor therapeutic drugs.
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Registered trials
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