Central nervous system activities of two diterpenes isolated from Aloysia virgata

作者：Wasowski Cristina; Marder Mariel^*

来源：Phytomedicine, 2011, 18(5): 393-401.

DOI：10.1016/j.phymed.2010.08.017

• Aloysia virgata
• Phyllocladane diterpenoids
• Anxiety
• GABA(A) receptor
• Benzodiazepine binding site ligand

Using the guide of a competitive assay for the benzodiazepine binding site in the gamma-aminobutyric acid type A receptor (GABA(A)), two active diterpenes were isolated from the aerial parts of Aloysia virgata (Ruiz & Pavon) A.L. Jussieu var. platyphylla (Briquet) Moldenke. These compounds, identified as (16R)-16,17,18-trihydroxyphyllocladan-3-one (1) and (16R)-16,17-dihydroxyphyllocladan-3-one (2) on the basis of spectral data, competitively inhibited the binding of [(3)H]-FNZ to the benzodiazepine binding site with K(i) +/- S.E.M. values of 56 +/- 19 mu M and 111 +/- 13 mu M, respectively. The behavioral actions of these diterpenes, intraperitoneally (i.p.) administered in mice, were examined in the plus-maze, holeboard, locomotor activity and light/dark tests. Compound 1 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters measured in the holeboard test (the number of head dips at 0.3 mg/kg and 3 mg/kg, the rears at 1 mg/kg and the time spent head-dipping at 3 mg/kg), in the plusmaze assay (the percentage of open arm entries at 1 mg/kg) and in the light/dark test (the time in light and the number of transitions at 1 mg/kg). Compound 2 augmented the number of rearings in the holeboard apparatus (at 0.3 mg/kg and 1 mg/kg) and the locomotor activity (at 1 mg/kg). These results reveal the presence of neuroactive compounds in Aloysia virgata.

• 出版日期2011-3-15