General

Scientific Names: Alisma orientale (Sam.) Juzep.

Common Names:Ze Xie, Tian E Dan, Ru Yi Cai, Shui Ze, Che Zhan Cai, Tian Tu.

 

BOTANICAL:

泽泻

来 源: 为泽泻科多年生沼泽植物泽泻Alisma orientalis(Sam.) Juzep.的块茎。

植物特征: 多年生沼生草本,高50~100cm。块茎球形。叶丛生,叶柄长5~50cm,基部鞘状;叶片椭圆形、卵状椭圆形至宽卵形,长2.5~18cm,宽1~10cm,基部心形、圆形或楔形,全缘,叶脉5~7条。花茎由叶丛中生出,花序通常为大形的轮生状圆锥花序;花两性;外轮花被片3,萼片状,广卵形,内轮花被片3,花瓣状,白色;雄蕊6枚;心皮多数、轮生。瘦果多数,倒卵形,扁平,花柱宿存。花期6~8月,果期7~9月。

生药材鉴定: 泽泻呈类圆形、长圆形或倒卵形,长4~7cm,直径3~5cm表面黄白色,未去尽粗皮者显淡棕色,有不规则横向环状浅沟纹,并散有多数细小突起的须根痕,于块茎底部尤密。质坚实,破折面黄白色,颗粒性,有多数细孔。气微,味微苦。

 

 

Pharmacology

化学成分: 泽泻块茎中含挥发油(内含糖醛)、小量生物碱、天门冬素、一种植物甾醇苷、脂肪酸(棕榈酸、硬脂酸、油酸、亚油酸)、树脂、蛋白质、淀粉和5种三萜类化合物[泽泻醇(alisol)A、B,乙酸泽泻醇A酯、B酯,表泽泻醇A];4种倍半萜A~D、尿苷、tymidine、 β- 谷甾醇3-O-硬脂酸酯、正二十三烷、 β- 谷甾醇、1-硬脂酸甘油酯、胡萝卜苷6-O-硬脂酸酯、大黄素、泽泻醇C单醋酸酯和环氧泽泻烯(alismoxide)等。

 

 

Efficacy

Herbal drugs were screened for their activity in reversing multidrug resistance (MDR) in P-glycoprotein (P-gp) over-expressing cancer cells. Through bio-assay guided fractionation an active compound was isolated from Rhizoma Alismatis, the underground part of Alisma orientale and the chemical structure of the isolate compound was confirmed by HPLC, LC-MS and NMR as Alisol B 23-acetate (ABA). ABA restored the sensitivity of MDR cell lines HepG2-DR and K562-DR to anti-tumor agents that have different modes of action but are all P-gp substrates. It restored the activity of vinblastine, a P-gp substrate, in causing G2/M arrest in MDR cells. In a dose-dependent manner, ABA increased doxorubicin accumulation and slowed down the efflux of rhodamin-123 from MDR cells. ABA inhibited the photoaffinity labeling of P-gp by [125I]iodoarylazidoprazosin and stimulated the ATPase activity of P-gp in a concentration-dependent manner, suggesting that it could be a transporter substrate for P-gp. In addition, ABA was also a partial non-competitive inhibitor of P-gp when verapamil was used as a substrate. Our results suggest that ABA may be a potential MDR reversal agent and could serve as a lead compound in the development of novel drugs. (source)

IN VITRO:

  1. Wang C, et al., Reversal of P-glycoprotein-mediated multidrug resistance by Alisol B 23-acetate. Biochem Pharmacol. 2004 Sep 1; 68(5):843-55.
  2. Chou CC, et al., Pharmacological evaluation of several major ingredients of Chinese herbal medicines in human hepatoma Hep3B cells. Eur J Pharm Sci. 2003 Aug; 19(5):403-12.

 

 

 

Safety

毒性和副作用 : T对小鼠iv的LD50为780mg/kg,ip为1 270mg/kg,po为4 000mg/kg。泽泻含有刺激性物质,内服可引起胃肠炎,贴于皮肤引起发泡。另有临床报告,服用、接触泽泻出现过敏反应者。


 
   
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