ArticleChinese medicine2016
Inhibition of IKK-β by epidioxysterols from the flowers of Calotropis gigantea (Niu jiao gua).
Article in Chinese medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed, 23 citations in OpenAlex.
- From traditional uses to biochemical evidence: phytochemical diversity and bioactivities of Calotropis gigantea-a comprehensive update since 2013.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- HPLC-MS standardization and validation methods for determination of calactin content in dichloromethane fraction ofHeliyon · 2025Article
- A Phytotoxin with Selective Herbicidal Activity and Related Metabolites from the Phytopathogenic FungusMolecules (Basel, Switzerland) · 2024Article
- Enniatins from a marine-derived fungus Fusarium sp. inhibit biofilm formation by the pathogenic fungus Candida albicans.Journal of natural medicines · 2023Article
- Apoptosis induced by 9,11‑dehydroergosterol peroxide from Ganoderma Lucidum mycelium in human malignant melanoma cells is Mcl‑1 dependent.Molecular medicine reports · 2018Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundCalotropis gigantea (Asclepiadaceae) (Niu jiao gua) has been used as a poultice in Chinese medicine for treating inflammatory skin diseases, e.g., neurodermatitis. This study aims to isolate the epidioxysterols from the flowers of C. gigantea, elucidate their structures and evaluate their possible inhibitory effects on the NF-κB pathway.
methodsThe two epidioxysterols 9,11-dehydroergosterol peroxide (1) and ergosterol peroxide (2) were isolated from the powdered flowers of C. gigantea by ultrasonic-assisted extraction, followed by the purification of the crude extract by column chromatography (i.e., silica gel and MCI-gel CHP 20P open columns). The chemical structures of these compounds were identified through a comparison of their HRMS, (1)H and (13)C NMR data with those in the literature. The in vitro IKK-β inhibitory activities of compounds 1 and 2 (1-100 µM) were evaluated using an IKK α and β Assay/Inhibitor Screening Kit, which is a single-site, semi-quantitative immunoassay. Berberine was used as a positive control. The IKK-β inhibitory activities between compounds 1 and 2 were compared by a two-tailed Student's t test to summarize the structure activity relationship.
resultsCompounds 1 and 2 exhibited a dose-dependent inhibitory activity towards IKK-β in a similar manner to that of berberine. The IKK-β inhibitory activities of these two epidioxysterols were significantly stronger (P = 0.001 for compound 1 and P = 0.028 for compound 2) than that of berberine at the concentration of 100 µM. Furthermore, at the same concentration the suppressive effect of compound 1 towards IKK-β was greater than that of compound 2 (P = 0.041), while their activities at 10 and 50 µM were comparable. The difference in the results at 100 µM therefore suggested that the double bond between C-9 and C-11 in compound 1 could be responsible for its higher inhibitory activity towards IKK-β at this concentration.
conclusions9,11-dehydroergosterol peroxide (1) and ergosterol peroxide (2) were isolated from the flowers of C. gigantea and exhibited in vitro inhibitory activities towards IKK-β.
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