摘要:Highlights•In this study seven previously reported compounds (1–7) were isolated and identified from the root extract ofEuphorbia grandicornisfor the first time.•Isolated compounds were evaluated for cytotoxic activities against MCF-7, HCC70 and MCF-12A cell lines.•Of the pure compounds isolated from the root extract, only hexyl (E)−3-(4‑hydroxy-3-methoxyphenyl)−2-propenoate (7) exhibited significant toxicity against MCF-7 (IC50 = 23.41 µM), HCC70 (29.45 µM) and MCF-12A (27.01 µM).AbstractEuphorbia grandicornisBlanc is widely utilized in traditional medicine for a variety of ailments including body pains associated with skin irritations, inflammation, and snake or scorpion bites. Compounds fromE. grandicorniswere characterized using spectroscopic techniques, NMR, IR, MS, and melting points and alongside the extracts were evaluated forin vitroanticancer activity against several cancer cell lines. The root extract afforded known, β-glutinol (1), β-amyrin (2), 24-methylenetirucalla-8-en-3β-ol (3), tirucalla-8,25-diene-3β,24R-diol (4), stigmasterol (5), sitosterol (6), and hexyl (E)-3-(4‑hydroxy-3-methoxyphenyl)-2-propenoate (7) based on their NMR spectroscopic data for the first report inE. grandicornis. The extracts and isolated compounds were evaluated for anticancer activities against hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. The CH2Cl2extract exhibited potent, cytotoxicity against MCF-7, HCC70, and MCF-12A cells. The aerial extract exhibited IC50values of 1.03, 0.301, and 1.68 µg/mL, and root extract displayed IC50values of 0.83, 0.83 and 3.98 µg/mL against MCF-7, HCC70, and MCF-12A cells, respectively. The root extract thus showed selectivity for the cancer cell lines over the non-cancerous control cell line (SI = 4.80). Hexyl (E)-3-(4‑hydroxy-3-methoxyphenyl)-2-propenoate (7) showed significant activity with IC50values of 23.41, 29.45 and 27.01 µM against MCF-7, HCC70 and MCF-12A cells, respectively, suggesting non-specific cytotoxicity.Graphical abstractDisplay Omitted