Vitex rotundifolia L. is widely distributed along the sea coast of China. The aim of this study was to investigate the anti-nociceptive and anti-
hyperprolactinemia activities of substances isolated from Fructus Viticis (the fruit of Vitex rotundifolia), which may be effective in the treatment of pre-menstrual symptoms, using
acetic-acid-induced writhing and
metoclopramide-dihydrochloride-induced
hyperprolactinemia in mice. The fractions effective in terms of anti-nociceptive and anti-
hyperprolactinemia activities were obtained from Fructus Viticis by elution through macro-porous resin, and
polyamide and
silica gel column chromatography. The standardization of the fractions obtained from the separation procedures was carried out by means of high-performance liquid chromatography (HPLC)-fingerprint. In this study, the
flavone-enriched fraction (Fraction 6) showed a higher inhibitory rate than
indomethacin (69.4% vs. 56.4%) at a dose of 50 mg/kg body wt., and significantly reduced the
prolactin level as compared to HPRL-treated mice (8.2 ng/ml vs. 25.5 ng/ml). Furthermore, this fraction showed anti-nociceptive activity in a dose-dependent manner (10-50 mg/kg body wt., i.g.). On further purification with
silica gel,
Casticin was isolated from this fraction and it decreased abnormal serum levels of
prolactin by approximately 50% (p < 0.01). Using bioassay-screening methods, our results indicate that the presence of
flavonoids such as
Casticin in this plant may be responsible for the activity effects.
Casticin has potent
analgesic and anti-
hyperprolactinaemia properties, is likely to be one of the active components of Fructus Viticis, and may have a role in treating PMS (premenstrual syndrom).