General

Scientific Names: Epimedium sagittatum (Sieb. Et Zucc.) Maxim .

Common Names: Jian Ye Yin Yang Huo, San Zhi Jiu Ye Cao.

BOTANICAL:

来 源： 为小檗科植物箭叶淫羊藿 Epimedium sagittatum (Sieb.et Zucc.)Maxim. 的地上部分。

植物特征： 多年生草本，高30～50cm。根茎匍匐，呈结节状，质硬，有多数纤细须根。基生叶1～3，三出复叶，有长柄；小叶片卵形、狭卵形至卵状披针形，长4～9cm，宽2.5～5cm，先端急尖或渐尖，边缘有细刺毛，基部深心形，侧生小叶基部显著不对称，外侧形斜而较长，呈尖耳状，内侧较短，近圆形，叶片革质，上面灰绿色，无毛，下面色较浅，被紧贴的刺毛或细毛。茎生叶常2，生于茎顶，形与基生叶相似。花多数，聚成总状花序或下部分枝而成圆锥花序，长约7.5cm；花序轴和花梗无毛或被少数腺毛；花较小，直径6～8mm；萼片8，外轮4片卵形，较小，外有紫色斑点，易脱落，内轮4片较大，白色，花瓣状；花瓣4，囊状，有短于内轮萼片的距，或近于无距。蓇葖果卵圆形，先端具宿存花柱，呈短嘴状；种子数粒，肾形，黑色，有脉纹。花期2～3月，果期4～5月。

生药材鉴定： 一回三出复叶，小叶片长卵形至卵状披针形，长4～12cm,宽2.5～5cm；先端浙尖，两侧小叶基部明显偏斜，外侧呈箭形。下表面疏被粗短伏毛或近无毛。叶片革质。

Pharmacology

化学成分: 茎叶含淫羊藿甙 (icariin) 、淫羊藿糖甙A (epinedoside A) ；根茎及根含去甲淫羊藿甙 (noricarliin) 、淫羊藿脂素 (icariresinol) 。

Efficacy

Reports elsewhere demonstrated that Epimedin C, a constituent isolated from the leaves of Epimedium sagittatum, possessed anti-tumor activity. However, its mechanism of action remains unresolved. Using SK-Hep-1 cells, a poorly-differentiated hepatoma subline, as an experimental model, we present evidence here that the anti-tumor activity of Epimedin C may involve cell cycle blockage. Immunoblotting analyses demonstrated that Epimedin C caused a decreased expression of hyperphosphorylated retinoblastoma (Rb) protein, cyclin D1, c-Myc, and c-Fos. In parallel, we measured the kinase activities and found that CDK2 and CDK4 were suppressed with commensurate increased levels of CDK inhibitors, p21(Cip1) and p27(Kip1). These data suggested that Epimedin C arrested the proliferation of these cells at G0/G1 phase through inhibition of CDK2 and CDK4 activities via an increased induction of p21(Cip1) and p27(Kip1). Alternatively, we investigated whether the anti-proliferative effect of Epimedin C on these cells might involve MAP kinase cascade. Using western blotting technique, we demonstrated that Epimedin C also selectively decreased ERK1/2 phosphorylation. Among the downstream effectors of ERK examined, we found that Epimedin C selectively decreased the expression of c-Fos, but not c-Jun. By EMSA assay, we further demonstrated that decreased c-Fos resulted in the downregulation of AP-1/DNA binding activity. Taken together, the molecular mechanisms of anti-tumor activity of Epimedin C may be proceeded by the combined effects of the cell cycle blockage via either the inhibition of CDK2 and CDK4 activities, with commensurate increase in their inhibitors, p21(Cip1) and p27(Kip1) or negatively modulates the ERK/c-Fos/AP-1 signaling pathway. (source)

The present study was conducted to evaluate the cytotoxic effects of Coptis chinensis and Epimedium sagittatum extracts and their major constituents on hepatoma and leukaemia cells in vitro. Four human liver cancer cell lines, namely HepG2, Hep3B, SK-Hep1 and PLC/PRF/5, and four leukaemia cell lines, namely K562, U937, P3H1 and Raji, were used in the present study. Of the two crude drugs, C. chinensis exhibited the strongest activity against SK-Hep1 (IC50 = 7 microg/mL) and Raji (IC50 = 4 microg/mL) cell lines. The IC50 values for C. chinensis on HepG2, Hep3B and PLC/PRF/5 cell lines were 20, 55 and 35 microg/mL, respectively. The IC50 values for C. chinensis on K562, U937 and P3H1 cell lines were 29, 29 and 31 microg/mL, respectively. With the exception of HepG2 and Hep3B, the E. sagittatum extract inhibited the proliferation of all cell lines (SK-Hep1, PLC/PRF/5, K562, U937, P3H1 and Raji), with IC50 values of 15, 57, 74, 221, 40 and 80 microg/mL, respectively. Interestingly, the two major compounds of C. chinensis, berberine and coptisine, showed a strong inhibition on the proliferation of both hepatoma and leukaemia cell lines, with IC50 values varying from 1.4 to 15.2 microg/mL and from 0.6 to 14.1 microg/mL, respectively. However, icariin (the major compound of E. sagittatum) showed no inhibition of either the hepatoma or leukaemia cell lines. The results of the present study suggest that the C. chinensis extract and its major constituents berberine and coptisine possess active antihepatoma and antileukaemia activities. (source)

IN VITRO:

1. Liu TZ, et al., Molecular mechanism of cell cycle blockage of hepatoma SK-Hep-1 cells by Epimedin C through suppression of mitogen-activated protein kinase activation and increased expression of CDK inhibitors p21(Cip1) and p27(Kip1). Food Chem Toxicol. 2006 Feb; 44(2):227-35. Epub 2005 Aug 19.
2. Lin CC, et al., Cytotoxic effects of Coptis chinensis and Epimedium sagittatum extracts and their major constituents (berberine, coptisine and icariin) on hepatoma and leukaemia cell growth. Clin Exp Pharmacol Physiol. 2004 Jan-Feb; 31(1-2):65-9.
   
   
   
   
   
   
   

Safety

宜忌: 阴虚火旺阳强易举者禁服。