Abstract
In this report, a new cytotoxic group, a 15-oxo-16α-H-17-methoxy (or ethoxy)- unit, was suggested from the structure-activity relationship analyses of 39 ent-kaurane diterpenoids, including 17 new compounds (neolaxiflorins I–Y, 1–17) isolated from the leaves of Isodon eriocalyx var. laxiflora using an in vitro cytotoxicity assay against HL-60, SMMC-7721, A-549, MCF-7, and SW-480 human cancer cell lines. This discovery is counter to the rule that the α,β-unsaturated ketone (C-15-C-16-C-17) unit is indispensable for cytotoxicity of the ent-kauranoids. Furthermore, portions of the isolates exhibited inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. The NF-κB inhibitory activity assay suggests a potential novel cytotoxic mechanism for compounds 9 and 22.
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