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ABSTRACT: Complexations between three oridonin derivatives and β-cyclodextrin (βCD) were studied by nuclear magnetic resonance (NMR) method. Job's plots for complexes were depicted by (1) H NMR spectra chemical shifts, which proved the 1:1 stoichiometry inclusion complex formation between each derivative and βCD. Two-dimensional rotating frame overhauser effect spectroscopy (2D ROESY) support the above conclusion and also proved that ring A of each oridonin derivative deeply enters into hydrophobic cavity from the wider rim and the other parts are outside the cavity. Apparent formation constants (K(a) ) of complexes between three oridonin derivatives and two CDs are calculated according to Scott's equation. Copyright © 2011 John Wiley & Sons, Ltd.