Tsumura Research Laboratory, Ami-Machi, Inashiki-Gun, Ibaraki, Japan.
J Ethnopharmacol. 2009 Oct 29;126(1):96-101. doi: 10.1016/j.jep.2009.08.005. Epub 2009 Aug 12.
Luteinizing hormone-releasing hormone (LH-RH) has been suggested as an inducer of centrally mediated elevation of skin temperature, and calcitonin gene-related peptide (CGRP) is one of the potent vasodilator neuropeptides that has been suggested as an inducer of peripherally mediated elevation of skin temperature. We investigate the effect of the Japanese herbal medicine Tokaku-jyoki-to using two rat-models for menopausal hot flash.
Tokaku-jyoki-to used in present study was prepared as a spray-dried powder from hot-water extract. Skin temperature was measured by thermister thermometer. Estrogen receptor (ER) binding assay of Tokaku-jyoki-to extract was performed using human recombinant ERalpha or ERbeta.
Oral Tokaku-jyoki-to (1000 mg/kg) restored skin temperature rise induced by LH-RH or CGRP in ovariectomized (OVX) rats as well as subcutaneous 17beta-estradiol (0.010 mg/kg) did. Tokaku-jyoki-to did not affect the lower concentration of plasma estradiol and the decreased uterine weight due to ovariectomy, although the hormone replacement of 17beta-estradiol restored them. In estrogen receptor ligand-binding study, Tokaku-jyoki-to extract bound to human ERalpha poorly and did not bound to human ERbeta.
These results suggest that Tokaku-jyoki-to, which appears to contain organ-specific selective estrogen receptor modulator, may be useful for the treatment of hot flashes in patients for whom estrogen replacement therapy is contraindicated as well as menopausal women.
促黄体激素释放激素(LH-RH)已被认为是中枢介导皮肤温度升高的诱导剂,而降钙素基因相关肽(CGRP)是一种强效血管扩张神经肽,被认为是诱导皮肤温度外周介导升高的诱导剂。我们使用两种绝经后潮热的大鼠模型来研究日本草药当药的作用。
本研究中使用的当药是由热水提取物制成的喷雾干燥粉末。皮肤温度通过热敏电阻温度计测量。使用人重组 ERalpha 或 ERbeta 进行当药提取物的雌激素受体(ER)结合测定。
口服当药(1000mg/kg)可恢复 LH-RH 或 CGRP 诱导的去卵巢(OVX)大鼠皮肤温度升高,如皮下 17β-雌二醇(0.010mg/kg)。当药对因卵巢切除而导致的低浓度血浆雌二醇和子宫重量下降没有影响,尽管 17β-雌二醇的激素替代可以恢复这些。在雌激素受体配体结合研究中,当药提取物与人 ERalpha 结合较弱,与人 ERbeta 不结合。
这些结果表明,当药似乎含有器官特异性选择性雌激素受体调节剂,可用于治疗对雌激素替代疗法有禁忌的患者以及绝经后妇女的潮热。