This work aimed to characterize and evaluate the antihypertensive effect of the (-)-β-pinene/β-cyclodextrin
(βP/β-CD) complex. The complex was prepared through physical mixture and slurry complexation methods and was analyzed
through differential scanning calorimetry, thermogravimetry/derivative thermogravimetry, fourier transform infrared
spectroscopy, diffraction X-ray, docking and scanning electron microscopy. Normotensive or L-NAME-induced hypertensive
rats were used in pharmacological experiments. Mean arterial pressure (MAP) was determined with direct
blood pressure measurements from the abdominal aorta. The drugs were orally administrated and their effects were recorded
during 48 hours. Vascular effects of βP were evaluated in isolated ring of mesenteric artery. The physicochemical
characterization showed βP/β-CD complex formation. In hypertensive rats (MAP = 156±16 mmHg), the complex, but not
βP alone, promoted hypotension at 36 and 48 hours after administration (MAP = 124±3 and 110±5 mmHg, respectively).
In arterial rings, βP vasorelaxed rings precontracted with phenylephrine (Emax = 105±6%), which was not changed after
the removal of the vascular endothelium (Emax = 108±4%), after the pre-contraction with KCl 80 mM (Emax = 107±8%)
or S(-)-BayK8644 (Emax = 107±5%), or after incubation with TEA (Emax = 113±4%). Finally, βP inhibited CaCl2- and
sodium-orthovanadate-induced contractions. In conclusion, the slurry complexation method was the best among them.
Pharmacological results demonstrated that the complex promoted antihypertensive effect. Furthermore, βP induced endothelium-
independent vasorelaxation possibly caused by the inhibition of the Ca2+ influx through L-type Ca2+ channel associated
to a decrease in calcium sensitivity.