General

Scientific Names: Podophyllum emodi Wall. Var chinense Sprague

Common Names: Gui Jiu, Tao Er Qi, Xiao Ye Lian, Xi Zhang Gui Jiu.

BOTANICAL:

来 源： 为植物小薜科鬼臼Podophyllum enosi Wall.var.chinense sprague的根状茎。

植物特征： 多年生草本，高 10～17cm。根茎粗壮，结节状，少分枝。茎生叶常为2，盾状，近圆形，长16～22cm，宽12～19cm,8～9浅裂，裂片边缘有叶状细齿；叶柄长 10～15cm。花5～8朵着生于叶柄上方近叶片处，下垂，花梗长达到.8cm；萼片6；花瓣6，紫红色；雄蕊6；雌蕊1，子房上位。浆果近球形。花期 5～6月，果期9～10月。

生药材鉴定： 本品呈椭圆形或近球形，多压扁，长3～5.5cm，直径2～4cm。表面紫红色或紫褐色，皱缩，有的可见露出的种子。顶端稍尖，果梗黄棕色，多脱落。果皮与果肉粘连成薄片，易碎，内具多数种子。种子近卵形，长约4mm；表面红紫色，具细皱纹，一端有小突起；质硬。种仁白色，有油性。气微，味酸甜、涩；种子味苦。

Pharmacology

化学成分: 鬼臼毒素（podophyllotoxin）、去甲鬼臼毒素（demerty-podophyllotoxin）、鬼臼苦素、山荷叶素（diphyllin）、黄酮类等。

Efficacy

Podophyllotoxin is a natural product isolated from Podophyllum peltatum and Podophyllum emodi and has long been known to possess medicinal properties. Etoposide (VP-16), a podophyllotoxin derivative, is currently in clinical use in the treatment of many cancers, particularly small cell lung carcinoma and testicular cancer. This compound arrests cell growth by inhibiting DNA topo-isomerase II, which causes double strand breaks in DNA. VP-16 does not inhibit tubulin polymerization, however, its parent compound, podophyllotoxin, which has no inhibitory activity against DNA topoisomerase II, is a potent inhibitor of microtubule assembly. In addition to these two mechanisms of action, an unknown third mechanism of action has also been proposed for some of the recent modifications of podophyllotoxins. Owing to its severe toxic side effects a number of modifications have been done on podophyllotoxin structure. Some of the congeners exhibited potent antitumor actiivity, of which etoposide and teniposide are in clinical use, NK 611 is in phase II clinical trials and many compounds are in the same line. Recent developments on podophyllotoxins have led structure-activity correlations which have assisted in the design and synthesis of new podophyllotoxin derivatives of potential antitumor activity. Modification of the A-ring gave compounds having significant activity but less than that of etoposide, whereas modification of the B-ring resulted in the loss of activity. One of the modifications in the D-ring produced GP-11 which is almost equipotent with etoposide. E-ring oxygenation did not affect the DNA cleavage which led to the postulation of the third mechanism of action. It has also been observed that free rotation of E-ring is necessary for the antitumor activity. The C4-substituted aglycones have a significant place in these recent developments. Epipodophyllotoxin conjugates with DNA cleaving agents such as distamycin increased the number of sites of cleavage. The substitution of a glycosidic moiety with arylamines produced enhanced activity. Modification in the sugar ring resulted in the development of the agent, NK 611 which is in clinical trial at present. (source)

用于治疗骨癌、脑癌、鼻咽癌、宫颈癌等。鬼臼毒素对小鼠和大鼠的多种肿瘤模型有抑制作用，包括急性白血病、转移淋巴瘤、局部淋巴瘤、腺瘤和黑色素瘤等。对人体鼻咽癌（KB）细胞也有抑制作用。鬼臼毒素及其衍生物，主要阻止细胞分裂前期（G 2 期），或从G 2 期进入分裂期的过程，故属于细胞周期特异性药物。

用鬼臼制剂局部敷用试治宫颈癌5例，其中1例Ⅰ期菜花型宫颈癌患者，经治疗2个月后，局部肿瘤消失，宫颈恢复正常。另4例Ⅱ期宫颈癌患者治疗3个月后，3例菜花型局部肿瘤明显缩小变平，另1例结核型患者肿瘤缩小不明显。一般用药7～14天后开始显效。 鬼臼乙叉甙（VP-16）为鬼臼毒素衍生物，对未接受过化疗的病人，有效率可达20%～65%，平均43%，但对曾经化疗过的病人疗效则低。常规用量为240mg/天，第1、3、5天用药，3周重复1次[刘静，内蒙古医学杂志，1988,33(1):46]。 (source)

败毒抗癌，用于癌瘤积毒：宫颈癌 桃耳七醇浸液20%用消毒棉球浸附后全面敷布于宫颈癌灶，24小时后除去，每日或隔日上药1次，3次后，局部分泌物增多，可与消炎生肌散交替敷用，以改善由于肿瘤坏死引致的炎性现象，并促进宫颈正常组织的恢复，用药后对粘膜有刺激作用或可引致轻度腹泻，经对症处理后即消失。治疗2个月后，局部肿瘤消失，宫颈恢复光滑。亦治阴茎癌，可使肿瘤全部消失，获近期痊愈。乳腺癌 桃耳七50克，八角莲、黄杜鹃各15克，紫背天葵30克 用白酒100毫升浸渍7天后，每服15毫升，日3次。局部用消毒棉球蘸药酒湿敷患处，能使癌肿消除。亦治皮肤癌，可使缩小变平，获得痊愈。 (source)

IN VITRO:

1. Damayanthi Y, et al., Podophyllotoxins: current status and recent developments. Curr Med Chem. 1998 Jun; 5(3):205-52. Review.
2. Sinkule JA. Etoposide: a semisynthetic epipodophyllotoxin. Chemistry, pharmacology, pharmacokinetics, adverse effects and use as an antineoplastic agent. Pharmacotherapy. 1984 Mar-Apr; 4(2):61-73. Review.
3. Von Krogh G. Topical treatment of penile condylomata acuminata with podophyllin, podophyllotoxin and colchicine. A comparative study. Acta Derm Venereol. 1978; 58(2):163-8.
4. Sanchez-Parareda J, et al., [Isolation and antimitotic activity of lactones extracted from Podophyllum emodi].Rev Esp Fisiol. 1970 Sep; 26(3):257-68. Spanish.
   
   
   
   

Safety

宜忌: 有轻度胃肠道反应，如食欲不振，恶心，呕吐，腹泻。骨髓抑制。

毒 性 : 主要有上腹不適﹑輕度腹瀉﹑下腹疼痛﹑頭痛頭暈, 大劑量會引起昏迷﹑休克﹑四肢癱瘓和腦部嚴重受損。