General

Scientific Names: Sophora subprostrata

Common Names: Guang Dou Gen, Shan Dou Gen, Shan Da Dou Gen, Huang Jie, Ku Dou Gen.

BOTANICAL:

来 源： 为豆科物柔枝槐sophora subprostrata Chun et T.Chen的根。

植物特征：灌木，高1～2m。羽状复叶互生，小叶11～17，卵形或长圆状卵形，长1～2.5cm，宽0.5～1.5cm，顶瑞一小叶较大，上面疏生短柔毛，下面密生灰棕色短柔毛；小叶柄短，被毛。总状花序顶生及腋生，有毛；花萼阔钟形；花冠蝶形，黄白色；雄蕊10；子房密生柔毛，花柱弯曲，柱头上簇生长柔毛。荚果连珠状。花期5～6月，果期7～8月。

资源分布：生于石灰岩山地或岩石缝中。主产广西。

生药材鉴定： 根茎呈不规则结节状，顶端残留茎基或茎痕，下面着生根数条。根长圆柱形，略弯曲，长10～35cm，直径0.3～1.5cm；表面棕色至棕黑色，有纵皱纹及横长皮孔。质坚硬，断面皮部淡棕色，木部黄白色。微有豆腥气，味极苦。

Pharmacology

化学成分: 根含总生物碱约0.93%，其中苦参碱(matrine)0.52%，氧化苦参碱(oxyma-trine)0.35%, 以及微量的臭豆碱(anagyrine)和甲基金雀花碱(methylcytisne)；并含槐果碱 (sophocarpine)。黄酮类化合物有紫檀素(pterocarpin)和l-三叶豆高丽槐甙(l-trifolirhizin,l- maackioin-β-D-glucoside),后者经酶水解得l-高丽槐素（l-maackiain）,均为紫檀素类化合物，有抗癌作用，其作用甙比甙元强，右旋体比左旋体强。另含山豆根素(sophoranone)、山豆根查耳酮(sophoradin)、山豆根色烯素 (sophoranochromene)、山豆根色烯查耳酮(sophoradochromene)、山豆根色烯素 (sophoranochromene)、山豆根色烯查耳酮(sophoradochromene)、山豆根色满素（2-[{3′- hydroxy-2′,2′-dimethyl-8′-(3-methy-2-butenyl)}chroman-6′-yl]-7-hydroxy-8-(3- methyl-2-butenyl)chroman-4-one）、山豆根苯并二氢呋喃素(2-[{2′-(l-hydroxy-l- methylethyl)-7′-(3-methyl-2-butenyl)-2′,3′-dihydrobenzofuran}-5′-yl]-7- hydroxy-8-(3-methyl-2-butenyl)chroman-4-one)、大豆素（daiazein）、山豆根苯并吡喃素（2-[(7′-hydroxy-2′-dimethyl-2H-benzopyran)-6′-yl]-7-hydroxy-8-(3-methyl-2- butenyl)chroman-4-one）、4′，7-二羟基-6,8-双（3-甲基-2-丁烯）二氢黄酮（4′,7- trihydroxy-6,8-bis-(3-methyl-2-butenyl)flavanone）、2′,4′，7-三羟基-6,8-双（3- 甲基-2-丁烯）二氢黄酮（2′,4′,7-trihydroxy-6,8-bis-(3-methyl-2- butenyl)flavanone）、山豆根新色烯查耳酮（6-[3-(2′，4′- dihydroxyphenyl)acryloyl]-7-hydroxy-2,2-dimethyl-8-(3-methyl-2-butenyl)2H- benzopyrane）、山豆根新色烯素(2-(2′，4′-dihydroxyphenyl)-8,8-dimethyl-10-(3- methyl-2-butenyl)-8H-pyreano[2,3-d]chroman-4-one）及柒料木素；其所含酚性物质，水解得咖啡酸和长链醇（CnH2n+1OH，n=20,21,23,24,25,26）其中以C26为主，占72.4%；此外，尚含羽扇豆醇、β-谷甾醇、维生素C和维生素B1。有报道，中性多糖由D-半乳糖和D-葡萄糖组成，其分子比为1:1。

Efficacy

抗肿瘤作: 小鼠灌服广豆根浸剂60克/公斤/日，共16 ～21天，对于接种的子宫颈癌有明显的抑制作用。对肉瘤－180的抑制率也达到25%以上。从广豆根中分离出来的苦参碱，对小鼠艾氏腹水癌无论试管试验或整体动物试验都有效，氧化苦参碱则无效，对小鼠肉瘤－180则都有效。氧化苦参碱的化疗系数为自力霉素（Mitomycin C)的7.8倍。山豆根中所含的紫檀素类（Pterocarpoid)、槐树素（Sophoiaponicin)对肉瘤－180也有抑制作用，其母核Chromanocoumaran则无效，一般讲右旋异构体比左旋者活性强，甙的活性比甙元强。应用白血病人的白细胞，以美蓝脱色测定脱氢酶的活性，或用瓦伯呼吸器测定白细胞呼吸，山豆根（未鉴定品种）对急性淋巴细胞型白血病和急性粒细胞型白血病患者白细胞的脱氢酶均有抑制作用，对前者的呼吸有轻度抑制作用。

　　 红车轴草根甙能抑制感染植物的真菌。柔枝槐素色烯能预防鼠生胃溃疡。

　　 日本山豆根（ Euchresta japonica Benth.)对恶性肿瘤有显著效果，副作用小，安全，且不使白细胞减少。试验动物一般状态良好，认为可在临床上试用。 (source)

Sophoranone inhibited cell growth and induced apoptosis in various lines of cells from human solid tumors, with 50% inhibition of growth of human stomach cancer MKN7 cells at 1.2 +/- 0.3 microM. The growth-inhibitory and apoptosis-inducing activities of sophoranone for leukemia U937 cells were very much stronger than those of other flavonoids, such as daidzein, genistein and quercetin. At the early stages of treatment of U937 cells with sophoranone, reactive oxygen species were formed, mitochondrial permeability pores were opened and cytochrome c was released from mitochondria. Cytochrome c was also released upon treatment of isolated mitochondria with sophoranone. Inhibitors of complexes III and IV, but not complexes I and II, of the mitochondrial respiratory chain prevented the release of cytochrome c from isolated mitochondria by sophoranone, as well as the induction of apoptosis in U937 cells in response to sophoranone. Our results indicate that sophoranone might be a unique apoptosis-inducing anticancer agent that targets mitochondria. (source)

IN VITRO:

1. Kajimoto S, et al., Sophoranone, extracted from a traditional Chinese medicine Shan Dou Gen, induces apoptosis in human leukemia U937 cells via formation of reactive oxygen species and opening of mitochondrial permeability transition pores. Int J Cancer. 2002 Jun 20; 99(6):879-90.
2. Kojima R, et al., Antitumor activity of Leguminosae plants constituents. I. Antitumor activity of constituents of Sophora subprostrata. Chem Pharm Bull (Tokyo). 1970 Dec; 18(12):2555-63.
   
   

Safety

用药忌宜: 脾胃虚寒泄泻者忌服。①《本草经疏》：“虚寒者勿服。”②《本草汇》：“脾虚食少而泻者，切勿沾唇。”③《得配本草》：“虚火炎肺、咽喉肿痛者禁用。”