TY - JOUR
T1 - Opioidergic mechanisms underlying the actions of Vitex agnus-castus L.
AU - Webster, Donna E.
AU - He, Ying
AU - Chen, Shao Nong
AU - Pauli, Guido F.
AU - Farnsworth, Norman R.
AU - Wang, Zaijie Jim
N1 - Funding Information:
This research was funded by NIH grants AT002406 , AT003647 , AT003476 , and AT000155 . Donna Webster was supported by an NIH predoctoral fellowship (F31AT002669). The contents are solely the responsibility of the authors and do not necessarily represent the official views of the NCCAM, ODS, or NIH.
PY - 2011/1/1
Y1 - 2011/1/1
N2 - Vitex agnus-castus (VAC) has been used since ancient Greek times and has been shown clinically to be effective for the treatment of pre-menstrual syndrome. However, its mechanism of action has only been partially determined. Compounds, fractions, and extracts isolated from VAC were used in this study to thoroughly investigate possible opioidergic activity. First, an extract of VAC was found to bind and activate μ- and δ-, but not κ-opioid receptor subtypes (MOR, DOR, and KOR respectively). The extract was then resuspended in 10% methanol and partitioned sequentially with petroleum ether, CHCl3, and EtOAc to form four fractions including a water fraction. The highest affinity for MOR was concentrated in the CHCl3 fraction, whereas the highest affinity for DOR was found in the CHCl3 and EtOAc fractions. The petroleum ether fraction had the highest agonist activity at MOR and DOR. Several flavonoids from VAC were found to bind to both MOR and DOR in a dose-dependent manner; however only casticin, a marker compound for genus Vitex, was found to have agonist activity selective for DOR at high concentrations. These results suggest VAC may exert its therapeutic effects through the activation of MOR, DOR, but not KOR.
AB - Vitex agnus-castus (VAC) has been used since ancient Greek times and has been shown clinically to be effective for the treatment of pre-menstrual syndrome. However, its mechanism of action has only been partially determined. Compounds, fractions, and extracts isolated from VAC were used in this study to thoroughly investigate possible opioidergic activity. First, an extract of VAC was found to bind and activate μ- and δ-, but not κ-opioid receptor subtypes (MOR, DOR, and KOR respectively). The extract was then resuspended in 10% methanol and partitioned sequentially with petroleum ether, CHCl3, and EtOAc to form four fractions including a water fraction. The highest affinity for MOR was concentrated in the CHCl3 fraction, whereas the highest affinity for DOR was found in the CHCl3 and EtOAc fractions. The petroleum ether fraction had the highest agonist activity at MOR and DOR. Several flavonoids from VAC were found to bind to both MOR and DOR in a dose-dependent manner; however only casticin, a marker compound for genus Vitex, was found to have agonist activity selective for DOR at high concentrations. These results suggest VAC may exert its therapeutic effects through the activation of MOR, DOR, but not KOR.
KW - Botanical
KW - Menopause
KW - Pain
KW - Plant
KW - Premenstrual syndrome
UR - http://www.scopus.com/inward/record.url?scp=78549246146&partnerID=8YFLogxK
U2 - 10.1016/j.bcp.2010.09.013
DO - 10.1016/j.bcp.2010.09.013
M3 - Article
C2 - 20854795
AN - SCOPUS:78549246146
SN - 0006-2952
VL - 81
SP - 170
EP - 177
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 1
ER -