Hypericum beanii , a traditional folk medicine plant, has been employed in the treatment of various inflammation-related diseases and has demonstrated promising potential as an herbal remedy for cancer. In this study, we isolated 29 compounds from the roots of H. beanii . We evaluated their cytotoxic effects on five human cancer cell lines, which revealed that the ethanol extract, along with compounds 4 and 14 , exhibited significant cytotoxic activity. Additionally, we assessed their anti-inflammatory properties by measuring the inhibition of nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages. Our findings showed that the ethanol extract (IC 50 ?=?7.41?±?0.38?μg/mL), compound 4 (IC 50 ?=?7.82?±?0.42?μM), and compound 14 (IC 50 ?=?3.05?±?0.06?μM) displayed substantial anti-inflammatory activity. ELISA assays and qPCR analysis revealed that compounds 4 and 14 may exert their anti-inflammatory and antitumor effects by inhibiting the expression of iNOS, TNF- α , IL-1 β , and IL-6 mRNA, shedding light on their role in cancer-related inflammation.
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