Compounds from aerial parts of Isodon lophanthoides and their effects of cytotoxicity and LPS-induced IL-1β and IL-10 production in RAW 264.7 macrophages

The bioassay-guided isolation of compounds from the aerial parts of Isodon lophanthoides (IL) resulted in the identification of five compounds (1–5). The chemical structures of 1–5 were determined through spectral analyses and compared to those identified in the literature to be 4-hydroxybenzoic acid (1), protocatechuic acid (2), rosmarinic acid (3), coetsoidin B (4), and coetsoidin A (5). Compounds 1, 4, and 5 were found for the first time in the aerial parts of IL. Compounds 1 and 2 displayed potent cytotoxic activity against A549, MCF-7, HepG2, and HL60 cancer cell lines, with IC₅₀ values ranging from 13.93 to 18.69 µm and from 11.97 to 18.30 µm, respectively. Compounds 1‒5 significantly inhibited LPS-induced IL-1β production in RAW 264.7 macrophages compared to the LPS 5 ng/mL control group, resulting in IL-1β concentrations ranging from 34.92 to 46.91 pg/mL. Additionally, compounds 1‒5 exhibited notable stimulation of IL-10 production, with IL-10 levels ranging from 358.77 to 478.23 pg/mL, compared to the LPS 5 ng/mL control group. These findings highlight the potential of compounds 1‒5 and the IL extracts for the cytotoxic effects on cancer cell lines and on LPS-induced IL-1β and IL-10 production in RAW 264.7 macrophages.