Chaste tree (Vitex agnus-castus) – Pharmacology and clinical indications

Wuttke, W.; Jarry, H.; Christoffel, Volker; Spengler, Barbara A.; Seidlová-Wuttke, Dana

doi:10.1078/094471103322004866

Cited by 235 publications

(147 citation statements)

References 14 publications

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“…Many premenstrual syndromes, particularly premenstrual mastalgia (mastodynia), are associated with latent hyperprolactinemia [23][24][25] . In addition, casticin has been demonstrated to reduce abnormally high serum prolactin levels in vivo (Figure 2).…”

Section: Discussionmentioning

confidence: 99%

Casticin, a flavonoid isolated from Vitex rotundifolia, inhibits prolactin release in vivo and in vitro

Zhang

Zheng

et al. 2010

Acta Pharmacol Sin

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Aim: To investigate the anti-hyperprolactinemia activity of casticin, a flavonoid isolated from Vitex rotundifolia, and elucidate its molecular mechanism. Methods: Hyperprolactinemia (MIHP) was induced by administration of metoclopramide dihydrochloride (50 mg/kg, tid, ip, for 10 d) in SD rats and the primary pituitary cells were prepared from the pituitary glands of the SD rats. Prolactin concentrations were measured using a radioimmunoassay. Cell viability was measured using an MTT assay. The mRNA expression of estrogen receptor alpha and beta in rat pituitary cells was measured using semi-quantitative RT-PCR analysis. Results: The level of serum prolactin in the MIHP model group was 2.1 fold higher than that in the untreated control group (P<0.01). Casticin (10, 20, and 40 mg/kg, ip, for 7 d) reduced serum prolactin levels by 33.9%, 54.3%, and 64.7%, respectively (P<0.01). The positive control drug bromocriptine 1 mg/kg decreased the serum prolactin concentration in MIHP rats by 44.9%. 17β-Estradiol (E2) significantly increased the proliferation of pituitary cells and casticin (1 and 10 μmol/L) markedly inhibited E2-induced pituitary cell proliferation by 27.7% and 42.1%, respectively. Stimulation of pituitary cells with E2 increased prolactin secretion into the cell culture supernatants, and casticin (0.1, 1, and 10 μmol/L) significantly inhibited the prolactin release stimulated by E2 in a concentration-dependent manner. Casticin (1 and 10 μmol/L) significantly inhibited ERα mRNA expression in pituitary cells stimulated with E2 (P<0.01) but increased ERβ mRNA expression at a concentration of 10 μmol/L (P<0.01). However, casticin had no effects on proliferation and prolectin release of the unstimulated primary pituitary cells in vitro. Conclusion: Casticin inhibited the release of prolactin from pituitary cells of SD rats stimulated with E2 in vivo and in vitro. These effects might be related with inhibiting the ERα mRNA expression and increasing the ERβ mRNA expression.

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Section: Discussionmentioning

confidence: 99%

Casticin, a flavonoid isolated from Vitex rotundifolia, inhibits prolactin release in vivo and in vitro

Zhang

Zheng

et al. 2010

Acta Pharmacol Sin

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“…Today, the dried ripe fruit of V. agnus-castus is defined under the names Agnus Castus Fruit (ACF) and Chaste Tree, respectively, in the European Pharmacopoeia [7] and the United States Pharmacopeia [8]. ACF products are distributed as overthe-counter (OTC) drugs to treat premenstrual syndromes (PMS) and climacteric disorders based on clinical evidence in Europe [9,10]. Although ACF has been generally distributed as a health food product in Japan, a direct OTC drug derived from ACF was recently approved by the Ministry of Health, Labour and Welfare.…”

mentioning

confidence: 99%

Identification of New Diterpenes as Putative Marker Compounds Distinguishing Agnus Castus Fruit (Chaste Tree) from Shrub Chaste Tree Fruit (Viticis Fructus)

et al. 2016

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Agnus Castus Fruit is defined in the European Pharmacopoeia as the dried ripe fruit of Vitex agnus-castus. In Europe it is used as a medicine targeting premenstrual syndrome and climacteric disorder. In Japan, Agnus Castus Fruit is becoming popular as a raw material for over-the-counter drugs and health food products, though its congenic species, Vitex rotundifolia and Vitex trifolia, have been used as Shrub Chaste Tree Fruit in traditional medicines. Therefore, it is important to discriminate these Vitex plants from the viewpoint of regulatory science. Here we tried to identify putative marker compounds that distinguish between Agnus Castus Fruit and Shrub Chaste Tree Fruit. We analyzed extracts of each crude drug by liquid chromatography?mass spectrometry, and performed differential analysis by comparison of each chromatogram to find one or more peaks characteristic of Agnus Castus Fruit. A peak was isolated and identified as an equilibrium mixture of new compounds named chastol (1) and epichastol (1a). The planar structures of 1 and 1a were determined spectroscopically. Their relative configurations were revealed by nuclear Overhauser effect spectroscopy and differential nuclear Overhauser effect-NMR data. Since avoiding contamination from closely related species is needed for the quality control of natural pharmaceuticals, this information will be valuable to establish a method for the quality control of both, Agnus Castus Fruit and Shrub Chaste Tree Fruit products.

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“…The deficiency in progesterone and the dominance of estrogen in PCOS is the cause behind cyst formation in the ovaries. Vitex agnus leads to a mild inhibition in the release of FSH and the stimulation of LH release and ovulation, and it also increases progesterone levels (11,13,15). This compound selectively binds to estrogen receptor β and reduces circulating estrogen (15); it balances the estrogen-toprogesterone ratio (16,17).…”

Section: Introductionmentioning

confidence: 99%

“…Vitex agnus leads to a mild inhibition in the release of FSH and the stimulation of LH release and ovulation, and it also increases progesterone levels (11,13,15). This compound selectively binds to estrogen receptor β and reduces circulating estrogen (15); it balances the estrogen-toprogesterone ratio (16,17). Vitex agnus inhibits prolactin production through a direct connection with dopamine receptors (15).…”

Section: Introductionmentioning

confidence: 99%

The Effects of Combined Low-Dose Oral Contraceptives and Vitex Agnus on the Improvement of Clinical and Paraclinical Parameters of Polycystic Ovarian Syndrome: A Triple-Blind, Randomized, Controlled Clinical Trial

Shahnazi

Khalili

Hamdi

et al. 2016

Iran Red Crescent Med J

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Chaste tree (Vitex agnus-castus) – Pharmacology and clinical indications

Cited by 235 publications

References 14 publications

Casticin, a flavonoid isolated from Vitex rotundifolia, inhibits prolactin release in vivo and in vitro

Casticin, a flavonoid isolated from Vitex rotundifolia, inhibits prolactin release in vivo and in vitro

Identification of New Diterpenes as Putative Marker Compounds Distinguishing Agnus Castus Fruit (Chaste Tree) from Shrub Chaste Tree Fruit (Viticis Fructus)

The Effects of Combined Low-Dose Oral Contraceptives and Vitex Agnus on the Improvement of Clinical and Paraclinical Parameters of Polycystic Ovarian Syndrome: A Triple-Blind, Randomized, Controlled Clinical Trial

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