Helenalin is a selective inhibitor of transcription factor NF-κB by direct targeting of p65. It is an anti-inflammatory sesquiterpene lactone compound with alkylating activity. Through its ability to target the cysteine sulfhydryl groups in the p65 subunit of NF-κB, helenalin effectively inhibits its DNA binding.

8-epi-Helenalin, a sesquiterpene lactone with anti-tumor properties, is derived from Inula britannica L. var. chinensis (Rupr.) Reg. It demonstrates cytotoxic activity against a range of cancer cell lines, with ED50 values of 12.2 μM for HL-60, 53.8 μM for A549, 9.1 μM for MCF7, 8.7 μM for HCT-15, 18.7 μM for SK-OV-3, and 8.3 μM for Malme-3M, indicating its potential for anti-tumor research [1].

Helenalin Acetate is an anti-inflammatory and anti-cancer agent, disrupting the cooperation of CCAAT-box/enhancer-binding protein beta (C/EBPß) and co-activator p300.