General

Scientific Names: Stellera chamaejasme L.

Common Names: Rui Xiang Lang Du, Hong Tou Cai Tou Hua, Lang Du.

BOTANICAL:

来 源： 为瑞香科植物瑞香狼毒Stellera chamaejasma L. 的干燥根。

植物特征： 多年生草本。根粗大，圆锥形，不分枝或少分枝，表面红棕色或浅褐色。茎丛生，直立，不分枝，无毛，基部木质化。叶互生，较密，椭圆状披针形至卵状披针形，先端急尖，基部楔形或近圆形，全缘，两面无毛；叶柄基部具关节。头状花序顶生，具多数花；花萼筒紫红色，裂片5，粉红色，具紫红色脉纹；无花瓣；雄蕊10，2轮，着生于花萼筒喉部和中部稍上；子房上部密生细毛。小坚果卵形，包藏于宿存萼筒内。花期6-7月，果期7-8月。

生药材鉴定： 本品呈纺锤形、圆锥形或长圆柱形，稍弯曲，单一或有分枝,长短不等,根头部有地上茎残迹，表面棕色至棕褐色，有扭曲的纵沟及横生隆起的皮孔和侧根痕，栓皮剥落处露出白色柔软纤维。体轻，质韧，不易折断，断面呈纤维状。皮部类白色，木部淡黄色。气微，味微辛。

Pharmacology

化学成分: 植物主要含有双黄酮、木脂素、香豆素、二萜等成分,其中瑞香烷型二萜具有较强的抗肿瘤作用。

Efficacy

Thirteen compounds were isolated from roots of Stellera chamaejasme L. (Thymelaeaceae). They are 3-sitosterol (2), simplexin (3), pimelea factor P2 (4), daucosterol (5), (+)-3-hydroxy-1,5-diphenyl-1-pentanone (6), 4-ethoxy-benzoic acid (7), 2,4,6-Trimethoxy-benzoic acid (8), (+)-afzelechin (9), fumaric acid (10), N,N-dimethyl-L-aspartic acid (11), umbelliferone (12), daphniretin (13) and a novel bicoumarin named bicoumastechamin (1). Among the known compounds, 7, 8, 9, 10 and 11 were first isolated from this plant, and 6 was first isolated from the natural resources. Their structures have been elucidated on the basis of spectral data. In vitro bioassays showed that 4 inhibited cancer cell growth, 13 exhibited immunomodulatory activity, and 6 exhibited both immunomodulatory and anti-tumor activity. (source)

The daphnane-type diterpene gnidimacrin, isolated from the root of the Chinese plant, Stellera chamaejasme L., was found to strongly inhibit cell growth of human leukemias, stomach cancers and non-small cell lung cancers in vitro at concentrations of 10(-9) to 10(-10) M. On the other hand, even at 10(-6) to 10(-5) M, the small cell lung cancer cell line H69 and the hepatoma cell line HLE were refractory to gnidimacrin. The agent showed significant antitumor activity against murine leukemias and solid tumors in an in vivo system. In K562, a sensitive human leukemia cell line, gnidimacrin induced blebbing of the cell surface, which was completely inhibited by staurosporine at concentrations above 10(-8) M, and arrested the cell cycle transiently to G2 and finally the G1 phase at growth-inhibitory concentrations. It inhibited phorbol-12,13-dibutyrate(PDBu) binding to K562 cells and directly stimulated protein kinase C (PKC) activity in the cells in a dose-dependent manner (3-100 nM). Although activation of PKC isolated from refractory H69 cells was observed only with 100 nM gnidimacrin, the degree of activation was lower than that produced by 3 nM in K562 cells. Our results suggest that gnidimacrin acts as a PKC activator for tumor cells and that this mechanism may be responsible for its antitumor activity. (source)

Gnidimacrin, a diterpene compound, isolated from the methanol extract of Stellera chamaejasme L, showed significant antitumor activities against mouse leukemia P-388 and L-1210 in vivo. At the dosages of 0.02-0.03mg/kg ip, the in increase in life span (ILS) was 70% and 80%, respectively. Gnidimacrin was also active against murine solid tumors in vivo, such as Lewis lung carcinoma, B-16 melanoma and colon cancer 26. It showed ILSs of 40%, 49% and 41% at the dosages of 0.01-0.02mg/kg ip, respectively. Gnidimacrin strongly inhibited cell proliferation of human cancer cell lines such as leukemia K562, stomach cancers Kato-III, MKN-28, MKN-45, and mouse L-1210 by the MTT assay and colony forming assay in vitro. The IC50 of gnidimacrin was 0.007-0.00012microgram/ml. It is concluded that gnidimacrin is the principal antitumor element in Stellera chamaejasme L. with strong antitumor activities. (source)

体外抗肿瘤活性研究采用MTT比色法和集落形成法测定, 靶细胞采用人胃癌细胞SGC-7901、人肝癌细胞BEL-7402和人白血病细胞HL-60; 通过提取物对小鼠的移植性肿瘤S180和H22生长的影响来评价体内抗肿瘤作用. 结果: 瑞香狼毒总黄酮提取物对体外培养的肿瘤细胞有较强的抑制作用, 体外抗肿瘤活性高于长春新碱; 瑞香狼毒总黄酮提取物急性毒性较小, 对小鼠移植性肿瘤S180和H22的生长也有显著的抑制作用, 并和剂量正相关, 高剂量组对小鼠移植性肿瘤S180的抑制率为45.64%, H22的为47.59%, 与阳性对照组环磷酰胺的抑制率接近. 结论: 瑞香狼毒总黄酮提取物具有较强的体内和体外抗肿瘤作用. (source)

IN VITRO:

1. Xu ZH, et al., A new bicoumarin from Stellera chamaejasme L. J Asian Nat Prod Res. 2001; 3(4):335-40.
2. Yoshida M, et al., Antitumor activity of daphnane-type diterpene gnidimacrin isolated from Stellera chamaejasme L. Int J Cancer. 1996 Apr 10; 66(2):268-73.
3. Feng W, et al., [The antitumor activities of gnidimacrin isolated from Stellera chamaejasme L]. Zhonghua Zhong Liu Za Zhi. 1995 Jan; 17(1):24-6. Chinese.
   
   

Safety

宜忌: 　 本品为三毒药之一，内服宜慎；孕妇禁用。