包天桐, 刘耕陶, 徐桂芳, 孙润华, 宋振玉. 二苯乙烯(芪)的一些药理作用J. 药学学报, 1979, 14(4): 227-233.
引用本文: 包天桐, 刘耕陶, 徐桂芳, 孙润华, 宋振玉. 二苯乙烯(芪)的一些药理作用J. 药学学报, 1979, 14(4): 227-233.
Bao Tiantong, Liu Gengtao, Xu Guifang, Sun Runhua , Song Zhenyu, . SOME PHARMACOLOGICAL PROPERTIES OF TRANS-STILBENEJ. Acta Pharmaceutica Sinica, 1979, 14(4): 227-233.
Citation: Bao Tiantong, Liu Gengtao, Xu Guifang, Sun Runhua , Song Zhenyu, . SOME PHARMACOLOGICAL PROPERTIES OF TRANS-STILBENEJ. Acta Pharmaceutica Sinica, 1979, 14(4): 227-233.

二苯乙烯(芪)的一些药理作用

SOME PHARMACOLOGICAL PROPERTIES OF TRANS-STILBENE

  • 摘要: 芪(二苯乙烯)通常用于化学工业,对其药理活性的研究很少。通过动物实验我们发现芪能明显保护CCl4引起的小鼠肝损害,表现在使高的SGPT及SGOT降低、BSP潴留减少、肝组织病变减轻等。芪明显促进肝糖元生成,此作用强度与可的松相近,但芪没有可的松那样的抗炎作用。在去肾上腺小鼠,芪仍能明显促进肝糖元生成,故此作用似乎不通过体内的垂体-肾上腺系统。芪对小鼠戊巴比妥睡眠时间影响不明显。根据实验资料分析,芪对CCl4肝损害的保护机制大概不是通过酶诱导,也不象某些抗氧化剂那样直接对抗CCl4的作用,但有可能与其促进肝糖元生成有某种关系。芪有微弱的雌激素作用(约为己烯雌酚的数万分之一)。芪的毒性很低,小鼠一次腹腔注射LD50为6.5 g/kg,灌胃LD50大于8 g/kg,但油溶液毒性较大(灌胃LD50为0.92g/kg)。长期大量给予芪,对雄小鼠的生长及睾丸发育有抑制作用,给狗服芪50 mg/kg/天连续一个月以上未见明显异常反应。

     

    Abstract: Trans-stilbene, a chemical reagent, was found to be effective in protecting the liver from CCl4 injury. In the first series of experiments, mice were given orally two doses of stilbene (100 mg/kg for each dose) in the first day and a dose of GCl4 (0.01 ml/kg) the next day. The SGPT and SGOT levels as well as BSP retention were significantly lower in stilbene pre-treated mice than in the CCl4 controls determined 16 hrs after injection of the liver poison. Histological examination revealed that lesions of the liver of stilbene pre-treated mice were less severe than those of CCl4 controls. In the second series of experiments, a dose of CCl4 was given to the mice and 40 hrs later the mice were given orally stilbene at dosages of 50 or 100 mg/kg twice a day for two days. The repair of injured liver tissue seemed to be accelerated since the liver weights and SGPT levels were statistically lower in the stilbene treated mice. These findings are parallel to the pathological observations.Since this compound did not show any effect in lowering either the SGPT levels or the GPT levels of liver tissue in normal mice at the dosage as high as 1000 mg/kg, the possibility of inhibition of the enzymes may be excluded.In the third series of experiments, mice fasted for 24 hrs were used. An hour after a dose of stilbene (100 or 200 mg/kg), mice were injected with 10% glucose (20ml/kg) and sacrificed 2 hours thereafter for the determination of liver glycogen. The results showed that glycogenesis was stimulated by the oral administration of stilbene. In adrenalectomized mice this action was even more significant: the liver glycogen in the stilbene (200 mg/kg) pre-treated mice was found to be twice as high as controls—a potency approximating 100 mg/kg of cortisone.No significant effect was found either on the pentobarbital sleeping time in mice (stilbene 200 mg/kg, p o) or on cotton pellet granuloma response in rats (stilbene 100 mg/kg/day p o for 7 days). However, the compound exhibited a very weak estrogenic activity as shown in the immature mice uterus assay.The toxicity of stilbene is low. When suspended in starch, the ip LD50 was found to be 6.50±0.76 g/kg in mice. No death was recorded in 10 mice given an oral dose of 8.0 g/kg. When dissolved in oil the toxicity of stilbene increased sharply, the po LD50 of its peanut oil solution was found tO he 0.92±0.14 g/kg. Four dogs (two males and two females) were fed stilbene 10~50 mg/kg for 30 days. No change in behavior, liver and kidney functions and blood counts was found.

     

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