金合欢素，一种从牡荆(Vitex rotundifolia)中分离得到的类黄酮，能够在体内和体外抑制催乳素的释放。
Casticin, a flavonoid isolated from Vitex rotundifolia, inhibits prolactin release in vivo and in vitro.
机构信息
Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
出版信息
Acta Pharmacol Sin. 2010 Dec;31(12):1564-8. doi: 10.1038/aps.2010.178. Epub 2010 Nov 1.
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 micromol/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 micromol/L) significantly inhibited the prolactin release stimulated by E2 in a concentration-dependent manner. Casticin (1 and 10 micromol/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 micromol/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.
目的
研究从牡荆Vitex rotundifolia中分离得到的类黄酮化合物牡荆素（Casticin）的抗高泌乳素血症（hyperprolactinemia，MIHP）活性，并阐明其分子机制。
方法
用盐酸甲氧氯普胺（50mg/kg，tid，ip，共 10d）诱导 SD 大鼠发生高泌乳素血症（MIHP），并从 SD 大鼠的垂体中制备原代垂体细胞。采用放射免疫法测定催乳素浓度。采用 MTT 法测定细胞活力。采用半定量 RT-PCR 分析检测大鼠垂体细胞中雌激素受体 alpha 和 beta 的 mRNA 表达。
结果
MIHP 模型组大鼠血清催乳素水平比未处理对照组高 2.1 倍（P<0.01）。牡荆素（10、20 和 40mg/kg，ip，共 7d）分别降低血清催乳素水平 33.9%、54.3%和 64.7%（P<0.01）。阳性对照药物溴隐亭 1mg/kg 使 MIHP 大鼠血清催乳素浓度降低 44.9%。17β-雌二醇（E2）显著增加垂体细胞的增殖，牡荆素（1 和 10μmol/L）显著抑制 E2 诱导的垂体细胞增殖，抑制率分别为 27.7%和 42.1%。E2 刺激垂体细胞后，催乳素分泌到细胞培养上清液中，牡荆素（0.1、1 和 10μmol/L）呈浓度依赖性显著抑制 E2 刺激的催乳素释放。牡荆素（1 和 10μmol/L）显著抑制 E2 刺激的垂体细胞中 ERαmRNA 表达（P<0.01），但在 10μmol/L 浓度时增加 ERβmRNA 表达（P<0.01）。然而，牡荆素对体外未受刺激的原代垂体细胞的增殖和催乳素释放没有影响。
结论
牡荆素抑制体内和体外 E2 刺激的 SD 大鼠垂体细胞催乳素的释放。这些作用可能与抑制 ERαmRNA 表达和增加 ERβmRNA 表达有关。
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