General
Scientific Names: Inula britannica L.
Common Names: Xu Fu Hua,
Fei Tian Rui, Jin Qian Hua, Ye You Hua, Di Di Jin, Xia Ju, Jin Qian Ju, Ai Ju, Die Luo Huang, Man Tian Xing, Liu Yue Ju, Huang Shu Hua, Fu Hua Quan Fu Hua.
BOTANICAL:
 
来 源：
为菊科植物旋复花（Inula britannica L.var. chinensis (Rupr.) Reg.）、线叶旋复花（Inula linariaefolia Turcz.）或大花旋或大花旋复花（Inula britannica L.）等的头状花序。
植物特征：
多年生草本，高20一70cm。根状茎短，横走或斜升。茎单生或簇生，基部常有不定根。基部叶花期枯萎；中部叶长椭圆形，基部宽大；上部叶渐小。头状花序单生或多数；总苞半球形；舌状花黄色；管状花冠毛1轮，白色。瘦果圆锥形，被短毛。花期6一l0月，果期9一11月。
生药材鉴定：
呈扁球形或类球形，直径1～2cm。总苞由多数苞片组成，呈覆瓦状排列，苞片披针形或条形，灰黄色，长4～11mm；总苞基部有时残留花梗，苞片及花梗表面被白色茸毛，舌状花1列，黄色，长约1cm，多卷曲，常脱落，先端3齿裂；管状花多数，棕黄色，长约5mm，先端5齿裂；子房顶端有多数白色冠毛，长5～6mm。有的可见椭圆形小瘦果。体轻，易散碎。气微，味微苦。
Pharmacology
化学成分: 大花旋复花开花时期的地上部分含倍半萜内酯化合物大花旋复花素(Britanin)和旋复花素(Inulicin)。花含槲 皮素(Quercetin)、异槲皮素(Isoquereetin)、咖啡酸(Caffeieacid)、绿原酸(lorogenicacid)、菊糖及蒲公英甾醇(Taraxasterol)等多种甾醇。花含蒲公英甾醇(taraxasterol,inusterol A-)；地上部分分离得旋覆花内酯 (inulicin)，另分得脱乙酰旋覆花内酯(desacetylinulicin)。
Efficacy
Treatment with ergolide, a sesquiterpene lactone from Inula britannica var chinensis, caused the induction of apoptosis in Jurkat T cells, which was confirmed by DNA fragmentation, caspase-3 activation and cleavage of poly(ADP-ribose) polymerase in response to ergolide. Furthermore, mitochondrial dysfunction appeared to be associated with ergolide-induced apoptosis, because Bax translocation and cytochrome c release were stimulated by ergolide. In parallel, the nuclear factor-kappaB (NF-kappaB) signaling pathway was significantly inhibited by ergolide, which was accompanied by down-regulation of cell survival molecules, such as X-chromosome-linked inhibitor of apoptosis and Bcl-2. In addition, the JNK signaling pathway was involved in ergolide-induced apoptosis. Collectively, our results identified a new mechanism for the anti-cancer property of ergolide, attributable to the induction of apoptosis through down-regulation of cell survival signal molecules resulting from inhibition of the NF-kappaB signaling pathway. (source)
We isolated and identified two known sesquiterpenelactones, O, O-diacetylbritannilactone (OODABL) and O-acetylbritaanilactone (OABL) from the flowers of the medicinal plant Inula britannica and studied their mechanism of anti-tumor effects. To determine the biological significance of Bcl-2 phosphorylation, we used a baby rat kidney (BRK-p53) cell line that was transformed with EIA and a temperature-sensitive mutant p53. The BRK-p53 cell line was transfected with either a vector with wild type Bcl-2 or a vector in which Bcl-2 had mutations in the paclitaxel phosphorylation sites (pcDNA3.1 V5/His Bcl-2 S70, 87A). OODABL and OABL induced phosphorylation of Bcl-2 in breast, ovary and prostate cancer cell lines and induced G2/M cell cycle arrest. Using the BRK cells with mutant Bcl-2 (BRK-Bcl-2-mt) and control (BRK-Bcl-2-wt), we found that OODABL induced phosphorylation of Bcl-2 at sites similar to paclitaxel. Phosphorylation of Bcl-2 was important for OODABL-induced cytotoxicity, since the abrogation of phosphorylation in BRK-Bcl-2-mt cells decreased OODABL-induced cytotoxicity. We concluded that OODABL is cytotoxic in multiple tumor cell lines, and the cytotoxicity is dependent, at least in part, on the phosphorylation of Bcl-2. (source)
The extracts of Inula britannica have anti-inflammatory, anti-bacterial, anti-hepatitic, and anti-tumor activities. Various sesquiterpene lactones with cytotoxic properties including 1-O-acetylbritannilactone (1) have been isolated from this Chinese medicinal plant. Eight derivatives of 1-O-acetylbritannilactone, (2-O-alkyloxime-3-phenyl)-propionyl-1-O-acetylbritannilactone esters were designed and synthesized. Four of these compounds were tested to show inhibitory activity on the growth of human leukemia HL-60 and cancer Bel-7402 cell lines. (source)
IN VITRO:
- Song YJ, et al.,
Apoptotic potential of sesquiterpene lactone ergolide through the inhibition of NF-kappaB signaling pathway.
J Pharm Pharmacol. 2005 Dec; 57(12):1591-7.
- Rafi MM, et al.,
A sesquiterpenelactone from Inula britannica induces anti-tumor effects dependent on Bcl-2 phosphorylation.
Anticancer Res. 2005 Jan-Feb; 25(1A):313-8.
- Liu S, et al.,
Design, synthesis, and anti-tumor activity of (2-O-alkyloxime-3-phenyl)-propionyl-1-O-acetylbritannilactone esters.
Bioorg Med Chem. 2005 Apr 15; 13(8):2783-9.
Safety
宜忌:《本草衍义补遗》：“病人涉虚者不宣多服，利大肠，戒之。” 《本经逢原》：“阴虚劳嗽，风热燥咳，不可误用。”
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