己烯雌酚相关化合物对自发性高血压大鼠的降压作用及对不同尖孢镰刀菌物种的抗真菌活性。

Hypotensive effects on spontaneously hypertensive rats and antifungal activity on various species of Fusarium oxysporum of diethylstilbestrol-related compounds.

作者信息

Inamori Y, Ogawa M, Amino H, Tsuboi M, Yamaguchi S, Tsujibo H, Takemura S

机构信息

Osaka University of Pharmaceutical Sciences, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Jul;38(7):2045-6. doi: 10.1248/cpb.38.2045.

DOI:10.1248/cpb.38.2045

PMID:2176575

Abstract

The diethylstilbestrol-related compounds 3,3'-dihydroxy-alpha, beta-diethyldiphenylethane (I), diethylstilbestrol (II) and hexestrol (III) showed hypotensive effects on spontaneously hypertensive rats (SHR) and antifungal activities against all Fusarium oxysporum sp. tested. As previously reported, I had strong hypotensive action on normotensive rats at the dose of 10 mg/kg, while II and III showed weak hypotensive effects on these rats at the same dose. In this work, all three compounds also had hypotensive actions on SHR at the same dose. I showed the strongest hypotensive effect (-80.0 +/- 5.0 mmHg, 10 mg/kg, i.v.) on both SHR and normotensive rats. The three compounds also had antifungal activities against five kinds of Fusarium oxysporum sp. tested. Especially, II strongly inhibited the growth of Fusarium oxysporum f. sp. raphani IFO-9972 (minimum inhibitory concentration (MIC): 1.0 micrograms/ml).

摘要

己烯雌酚相关化合物3,3'-二羟基-α,β-二乙基二苯乙烷（I）、己烯雌酚（II）和己烷雌酚（III）对自发性高血压大鼠（SHR）显示出降压作用，并对所有测试的尖孢镰刀菌具有抗真菌活性。如先前报道，化合物I在剂量为10 mg/kg时对正常血压大鼠具有强烈的降压作用，而化合物II和III在相同剂量下对这些大鼠显示出较弱的降压作用。在本研究中，所有三种化合物在相同剂量下对SHR也具有降压作用。化合物I对SHR和正常血压大鼠均显示出最强的降压效果（-80.0±5.0 mmHg，10 mg/kg，静脉注射）。这三种化合物对五种测试的尖孢镰刀菌也具有抗真菌活性。特别是，化合物II强烈抑制萝卜尖孢镰刀菌IFO-9972的生长（最低抑菌浓度（MIC）：1.0微克/毫升）。