General

Scientific Names: Gelsemium elegans (Gardn. et Champ.) Benth.

Common Names: Da Cha Yao, Hu Man Teng, Duan Chang Cao, Gou Wen, Ye Ge.

BOTANICAL:

别名大茶叶、断肠草、毒根、烂肠草、野葛、胡蔓藤等，系马钱科常绿藤本植物胡蔓藤Gelsemium elegans (Gardn.efchamp) Benth. 的根、茎及叶。产于江南各省。

藤本植物，長3-12米，全株無毛。葉對生，卵形或卵狀披針形。花黃色或橙黃色，花冠漏斗狀，5裂。果為蒴果，卵形或橢圓形。花期5-11月。生於低丘陵坡地或灌木叢中。全株有毒，尤以嫩葉毒性最大。嚼食三片葉即可致人死亡。花的蜜腺亦有毒。

Pharmacology

化学成分: 从根、茎、叶中已分得16种生物碱：钩吻素甲（gelsemine）、钩吻素丙（sempervirine）、钩吻素丁（koumicine）、钩吻素戊（koumidine，即C16（S）-normacusine）、钩吻素己（gelsenicine）、钩吻素庚（gelseni-dine）、N1-甲氧基钩吻素（N1-methoxygelsemine）、11-去甲氧基钩吻素乙（gelsedine）、钩吻素子（koumine）、钩吻素寅（kouminicine）、钩吻素卯（kouminidine）、钩吻素辰（kounidine）、胡蔓藤碱甲（humantenmine）、胡蔓藤碱乙（humantennine）、胡蔓藤碱丙（humantenidine）和胡蔓藤碱丁（humantenirine）。此外，尚得到gelsevirine。这些生物碱中以钩吻素子的含量最高，1931年就有报道，但其结构直到1986年才最后确定。另钩吻素丑为不纯物，从中分离到钩吻素甲。

  1. Rujjanawate C, et al., Pharmacological effect and toxicity of alkaloids from Gelsemium elegans Benth. J Ethnopharmacol. 2003 Nov; 89(1):91-5.
  2. Zhang L, et al., [Advances in the study on chemical constituents and pharmacology of Gelsemium elegans (Gardn. et Champ.) Benth.]. Zhong Yao Cai. 2003 Jun; 26(6):451-3. Review.
  3. Kitajima M, et al., Structure reinvestigation of gelsemoxonine, a constituent of Gelsemium elegans, reveals a novel, azetidine-containing indole alkaloid. Org Lett. 2003 Jun 12; 5(12):2075-8.
  4. Schun Y, et al., Cytotoxic steroids of Gelsemium sempervirens. J Nat Prod. 1987 Mar-Apr; 50(2):195-8.
  5. Yang JS, et al., [Chemical studies on the alkaloids from hu-man-teng (Gelsemium elegans Benth.). II. The structure of humantenidine]. Yao Xue Xue Bao. 1984 Jun; 19(6):437-40.
  6. Yang JS, et al., [Chemical studies on the alkaloids of Hu-Man-Teng (Gelsemium elegans Banth.). I. Isolation of the alkaloids and structure of humantenmine]. Yao Xue Xue Bao. 1983 Feb; 18(2):104-12.
  7. Janot MM, et al., [Chemical study of Gelsemium elegans Benth. (Loganiaceae): isolation of sempervirine.]. Ann Pharm Fr. 1953 Sep-Oct; 11(9-10):602-8.


Efficacy

主治： 肝癌、食管癌、胃癌等消化系统肿瘤及淋巴肉瘤、骨肉瘤、皮肤癌等。胡蔓藤含有钩吻素子（即阔胺）、钩吻素寅、钩吻素丙、丁、戍、丑、卯等多种生物碱等成份。其中钩吻素寅有剧毒。钩吻总生物碱对动物移植性肿瘤、小鼠肉瘤 180 有抑制作用；钩吻素甲对小鼠有镇痛作用，对止癌痛亦有效。

临床上有以本品为未，每天服125毫克，治疗38例原发性肝癌，结果特效1例，显效3例，有效19例，平均生存8个月以上，其中存活2年以上者8例。用本品治疗食管癌、肝癌、宫颈癌等多种肿瘤26例，结果12例缓解，9例不变。也有用本品治疗恶性淋巴瘤19例，基本治愈4例，好转12例；淋巴肉瘤9例，基本治愈3例，好转6例。

广东梅县地区人民医院用断肠草总生物碱制剂综合治疗食管癌、肝癌、肺癌、胃癌、贲门癌、直肠癌等及淋巴造血系统恶性肿瘤共26例，除5例死亡外，绝大部份患者临床症状均获改善，止痛效果明显，其中4例宫颈癌见肿块缩小，宫颈局部光滑、萎缩、子宫旁浸润好转。6例肝癌均未出现高度腹水或浮肿。但此药的副作用是肌肉注射5-10分钟或静脉点滴过程中可出现头晕、眼花、视力模糊、复视、眼睑下垂、口干等情况，个别病例有腹部不适，排尿困难，但均于2-3天自然消失。多数病例用药一段时间后反应减轻或无反应。广西医学院以钩吻干粉50毫克/次，每日3次服用，3天后若无反应增加至100-150毫克/次，连续长期服，报道8例肝癌有效病例，除1例服药3个月外，均服1年以上，有的服药2-3年，其中1例加用石山芋，另两例用过少量喜树混悬液，用药1-2个月后病情均有明显好转，疼痛减轻或消失，食欲增加，体重增加，有6例肝脏缩小50%以上，缩小不足50%者2例；AFP阳性4例均转为阴性，病情缓解，治疗后生存期30-87个月，中数生存期41个月。现已知钩吻共有11-12种，中毒后可引起眩晕，咽食剧痛，口吐泡沫，瞳孔散大，下腭脱落，肌肉无力，最后因心脏及呼吸衰竭而死亡，应慎用及预防中毒。 (Source)

 

IN VITRO:

After koumine (50 mmol/L) treatment in vitro, the LoVo cells were examined under light microscope, transmission electron microscope and fluoroscope respectively for apoptosis, and the cell cycle distribution was analyzed using flow cytometry. The percentage of apoptotic cells increased in a time-dependent manner after the cells were treated with koumine, whose action exhibited remarkable cell cycle specificity. The percentage of LoVo cells in G(0)/G(1) phase rose from 31.3% to 42.3% and the percentage of cells in S phase fells from 62.0% to 38.7%. Therefore, Koumine can induce apoptosis of LoVo cells in a time-dependent manner and inhibit the DNA synthesis in LoVo cells, thereby blocking the cell cycle from G1 to S phase. (Source)

The inhibitory effect of gelsemium alkaloids exstract (GAA) on HepG2 cells in vitro were studied by crystal violet dyeing method. The morphological change of HepG2 cells were observed with optical microscope. The alterations of cell cycle induced by GAA were analyzed with flow cytometry. The results showed that HepG2 cells exposed to GAA 10 micrograms/ml was inhibited significantly (P < 0.05). The inhibitory effect appeared in a dose- and time-dependent manner. HepG2 cells showed nuclear chromosome segmentation and condensation after GAA treatment. There emerged obvious Sub-G1 peak in the DNA histogram of HepG2 cells. GAA has a significant inhibition on HepG2 cells in vitro. The mechanism of antitumor action may be related to their apoptosis inducing activity. (Source)

  1. Chi DB, et al., [Study of koumine-induced apoptosis of human colon adenocarcinoma LoVo cells in vitro]. Di Yi Jun Yi Da Xue Xue Bao. 2003 Sep; 23(9):911-3. Chinese.
  2. Wang Y, et al., [Inhibitory effect of gelsemium alkaloids extract on hepatic carcinoma HepG2 cells in vitro]. Zhong Yao Cai. 2001 Aug; 24(8):579-81. Chinese.

Safety

毒性：钩吻碱静脉注射对小鼠（雌雄各半）的LD50为1.56mg/kg, 腹腔注射对雌性小鼠的LD50为1.5mg/kg，腹腔注射对雄性大鼠的LD50为1.2mg/kg。

　

 
   
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