General

Scientific Names: Tripterygium hypoglaucum Hutch.

Common Names: Kun Ming Shan Hai Tang.

BOTANICAL:

来 源： 为卫矛科植物昆明山海棠Tripterygium hypoglaucum(LevL)Hutch.的干燥根。

植物特征： 落叶披散或蔓生灌木，长 2～3 m。根圆柱状，黄红色。小枝有棱，红褐色，有圆形小瘤状突起。单叶互生，卵形或宽椭圆形，边缘有细锯齿，叶上面绿色，下面粉白色，侧脉6～7对，两面突起。圆锥花序顶生，有灰褐色毛；花白色，花萼、花瓣、雄蕊均为5；心皮3。翅果具3翅，翅膜质，赤红色。

Pharmacology

化学成分: 昆明山海棠含有萜类、生物碱、甙类、糖类、有机酸、齐墩果酸、多糖、β-谷甾醇等多种成分。

Efficacy

To investigate the effects of total alkaloids of Tripterygium hypoglaucum Hutch (THH) on the tk gene of mouse lymphoma cells. L5178Y cells were infected with total alkaloids of THH with different concentrations and put into single-cell wells at different time phases. Then the numbers of positive wells were counted and the cell plating efficiency, relative suspension growth and mutation frequency were determined. Total alkaloids of THH (0.1-2.0 g x L(-1)) induced tk locus mutation with mutation frequency 2-9 times higher than that of spontaneous mutation frequency of L5178Y cells. There were two different phenotypes of mutation colonies, large colony and small colony, but the main colony was large colony. This phenomenon might be related with the mutagenesis of THH. Total alkaloids of THH can exert toxicity and mutagenic effects on tk gene in L5178Y cells, and there may be range limit in gene mutation. (source)

The genotoxicity and cytotoxicity of a Chinese medicinal herb, Tripterygium hypoglaucum (level) Hutch (THH), was investigated in human promyelocytic leukemia (HL-60) cells using the hypoxanthine-guanine phosphoribosyltransferase mutation assay. THH showed clear cytotoxicity and mutagenicity in HL-60 cells at concentrations between 6.7 and 20.0 mg/ml. When the mutants were characterized by techniques based on multiplex PCR, 46.6% of induced mutants were found to have deletions, whereas only 7.7% of spontaneous mutants showed deletions. The rest were not characterized, but were assumed to be mainly point mutations. Mapping of all intragenic deletion breakpoints showed a random distribution of breakpoints in nine exons. Deletion of exon 1 appeared as the only whole gene deletion, while deletions of exon 7/8 and 9 often occurred concomitantly (71.4%). It is concluded that THH is mutagenic in HL-60 cells, predominantly inducing deletions. Since this herb is widely used as a traditional medicine, its genotoxicity should be assessed in vivo in treated humans. (source)

昆明山海棠 （六方藤，紫金藤，紫金皮，火把花，721） Tripterygium hypoglaucum(Le,vl)Hutch 本品为卫矛科雷公藤 （Tripterygium) 属植物，从中分离出三个微量化学成分即雷公藤甲 （雷公藤內酯，Triptolide), 雷公藤乙 （雷公藤羟内酯，Tripdiolide), 雷公酮 （雷公藤碳内酯，triptonide), 为萜类化合物.[性状]雷公藤内酯， 溶点226-227度。 羥内酯， 熔点210-211度。碳内酯，熔点251-252度。 本品民间有用以治疗肿瘤的经验。雷滕素甲， 乙， 丙对动物实验肿瘤有很高的活性，国内1977年报道从昆明山海棠中分离得到雷公藤素甲，经动物实验，0.25毫克/公斤对小鼠L615有很好的效果。 国内以昆明山海棠试用与32例鼻咽癌， 肺癌等，16例获得缓解。 (source)

1972年， Kupchan SM 等从台湾产的雷公藤样品中分离出3个二萜内酯的三环氧化合物，雷藤素甲（Triptolide）、雷藤素乙（Tripdiolide）和雷藤酮（Triptonide），其得率均为0.001%。因对小鼠白血病瘤谱和人体鼻咽癌细胞有很高的抗癌活性而引起人们的注意。随后，云南省植物研究所植化室 [5] 用95%的乙醇抽提昆明山海棠根粉，再用有机溶剂划分为4个不同的部位，并做了抗癌活性筛选。其中 T-II，T-III 部位对白血病瘤谱Ｌ 615 表现有抗癌活性，小鼠生存时间延长率分别为43%及30%（Ｐ<0.001）；将 T-II 部位过一次氧化铝柱后，再过一次硅胶柱层析，即可从中分离得雷藤素甲（Ｃ 20 Ｈ 24 Ｏ 6 ）得率约为0.0005%，药理试验结果表明对小鼠Ｌ 615 有很好的抗癌活性（0.25mg/kg），动物生存时间延长率在159%以上。 (source)

IN VITRO:

1. Wan CK, et al., Triptolide induces Bcl-2 cleavage and mitochondria dependent apoptosis in p53-deficient HL-60 cells. Cancer Lett. 2005 Nov 25.
2. Liu J, et al., Triptolide suppresses CD80 and CD86 expressions and IL-12 production in THP-1 cells. Acta Pharmacol Sin. 2005 Feb; 26(2):223-7.
3. Liu SX, et al., [Effects of total alkaloids of Tripterygium hypoglaucum Hutch on tk gene of mouse lymphoma cells]. Zhongguo Zhong Yao Za Zhi. 2003 Oct; 28(10):954-7. Chinese.
4. Liu SX, et al., Molecular analysis of Tripterygium hypoglaucum (level) Hutch-induced mutations at the HPRT locus in human promyelocytic leukemia cells by multiplex polymerase chain reaction. Mutagenesis. 2003 Jan; 18(1):77-80.
   
   
   
   
   
   
   
   
   
   

Safety

宜忌: 肾功能不全者慎用。