General

Scientific Names: Heliotropium indicum

Common Names:Da Wei Yao ,You Yu Cao, Ban Cao, Mao Wei Cao, Xiang Bi Guang, Xiang Bi Cao, Mo Yu Xu Cao.

BOTANICAL:

来 源： 为紫草科植物大尾摇 Heliotropium indicum L. 的全草或根。

植物特征： 一年生草本，高15—60厘米。根圆柱形，向下渐狭，长达13厘米，上部粗达0.7厘米，下部具少数分枝，干时黄褐色。茎粗壮，直立，具分枝，下部粗达1 厘米，被糙硬毛。叶片互生，稀近对生，叶片卵形、狭卵形或椭圆形，长4—10厘米，宽2—4厘米，先端急尖，基部骤然收缩并下延入叶柄，边缘呈不规则的波 状，两面疏被糙硬毛，第一次侧脉明显，每边5—6对，和中脉在背面凸起；叶柄长1—4厘米，具翅。蝎尾状花序长9—1 8厘米，通常单个顶生于茎及分枝先端，被糙硬毛；无苞片。花多数，于花序轴的一侧密集排列成二列；花萼绿色，长2—3毫米，疏被糙硬毛，5深裂，裂片披针 形，常不等；花冠白色或蓝色、紫色，高脚碟状，长3—4毫米，外面被细短毛，檐部5裂，裂片近圆形，芽时覆瓦状排列，管圆筒形，长2.5—3.5毫米；花 药长圆形，长不到1毫米，花丝细且短，着生于管基部上方；子房小，无毛，花柱长不到1毫米，中部以上增粗，柱头阔圆锥状，顶端平截。小坚果卵形，长3—4 毫米，无毛，2深裂，有纵肋，顶端开裂，每裂片分裂为有角状尖头，单种子的1对小坚果。花果期4—10月。

Pharmacology

化学成分: 大尾搖含生物鹼：大尾搖鹼 (indicine) ，乙醯大尾搖鹼 (acetylindicine) ，大尾搖寧鹼 (indicinine) ， N- 氧化大尾搖鹼 (indicine N-oxide) ，刺凌德草鹼 (echinatine) ，仰臥天芥菜鹼 (Supinine) ，歐天芥菜鹼 (heleurine) ，天芥菜鹼 (heliotrine) ，毛果天芥菜鹼 (lasiocarpine) ， N- 氧化毛果天芥菜鹼 (lasiocarpine N-oxide) 。種子油三醯甘油及氰類脂 (cyanolipid) 中均含 C 16 、 C 18 ，脂肪酸，氰類脂中 C 16 、 C 18 ，脂肪酸與 3 ， 3- 二羥甲基丙烯腈形成酯。

Efficacy

Indicine N-oxide is a pyrrolizidine alkaloid isolated from Heliotropium indicum, one of the widely used herbs in Ayurvedic medicine. Thirty-seven patients with solid tumors received the drug: 15 men and 22 women (mean age, 53 years). All had had prior chemotherapy, and 25 had had prior radiotherapy. Eighty-four percent had a performance status of 0-3 (Cancer and Leukemia Group B criteria). The drug was given as a short infusion over 15 minutes and repeated with a median interval of 4 weeks. Doses were escalated from 1 to 9 g/m2. A total of 55 courses were evaluable. Dose-limiting toxic effects were leukopenia and thrombocytopenia, and the toxicity was cumulative with repeated doses. Other toxic effects included nausea and vomiting, anemia, and hepatic dysfunction. The hematologic toxicity tended to be more pronounced in patients with hepatic dysfunction, poor marrow reserve, and heavy prior chemotherapy and radiotherapy. There were no complete or partial responses. One patient with skin melanoma and another with ovarian carcinoma had improvement lasting 2 months. The maximally tolerated dose is 9 g/m2 in our population. A recommended dose for therapeutic study is 7 g/m2. High-risk patients should be started at a dose of 5 g/m2. The treatment may be repeated at 4-week intervals with close monitoring of wbc and platelet counts. Dose reductions may be necessary for repeated courses. (source)

葉的提取物對小鼠 Schwartz 白血病 ( 腹水型 ) ，具有延長壽命的抗癌作用。從大尾搖分離的活性成分為大尾搖鹼及大尾搖鹼 N- 氧化物。大尾搖鹼對小鼠白血病 P388 ，有抗癌作用，但作用不如本品的 N- 氧化物。給白血病 P 388 ，小鼠腹腔內連續注射大尾搖鹼 N- 氧化物 50 ～ 800mg/kg ，有良好的治療效果，但口服和皮下注射無效；對黑色素瘤 B 16 也有效。本品用於臨床治療癌和白血病。

IN VITRO:

1. Kugelman M, et al., Indicine-N-oxide: the antitumor principle of Heliotropium indicum. Lloydia. 1976 Mar-Jun; 39(2-3):125-8.

CLINICAL:

1. Ohnuma T, et al., Phase I study of indicine N-oxide in patients with advanced cancer. Cancer Treat Rep. 1982 Jul; 66(7):1509-15.

Safety

用药忌宜： 孕婦慎服。

毒性： 水提取液對小鼠有輕微毒，性，醇提取液則無明顯毒性 ( 每鼠腹腔注射 1 ： 1 濃度 0.8ml 末引起死亡 ) 。大尾搖鹼對大鼠肝臟有毒性。小鼠腹腔注射大尾搖鹼 N- 氧化物 2000 ～ 3000mg/kg ，對心、脾、腎及十二指腸有毒性。