CAS |
315-22-0 |
Chinese Name |
野百合碱 |
English Name |
Crotaline |
Synonyms |
Monocrotaline |
Molecular Formula |
C16H23NO6 |
Molecular Weight |
325.36 |
Solubility |
Soluble in DMSO ≥10mg/mL |
Purity |
HPLC≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 628-506-2 |
MDL |
MFCD00084656 |
SMILES |
O=C(O[C@]1([H])CCN2[C@]1([H])C(CO3)=CC2)[C@H](C)[C@@](C)(O)[C@@](C)(O)C3=O |
InChIKey |
QVCMHGGNRFRMAD-XFGHUUIASA-N |
InChI |
InChI=1S/C16H23NO6/c1-9-13(18)23-11-5-7-17-6-4-10(12(11)17)8-22-14(19)16(3,21)15(9,2)20/h4,9,11-12,20-21H,5-8H2,1-3H3/t9-,11+,12+,15+,16-/m0/s1 |
PubChem CID |
9415 |
Target Point |
Others |
Passage |
Others |
Background |
It is a pyrrolizidine alkaloid, which has inhibitory effect on various tumors, and is considered to be an alkylating agent, which exerts anticancer activity through the alkylation of DNA. |
In Vitro |
野百合碱(MCT)是一种11元大环吡咯里西啶生物碱(PA),来源于猪屎豆(Crotalaria spectabilis)植物的种子[1]。野甘露碱是一种天然配体,具有剂量依赖性细胞毒性,具有强大的抗肿瘤活性。野百合碱的体外细胞毒性证实为IC50为24.966μg/ mL,2 X IC50对HepG2细胞的遗传毒性[2]。 |
In Vivo |
MCT引起大鼠肺血管综合征,其特征为增殖性肺血管炎,肺动脉高压(PH)和肺心病[3]。在肺动脉高压(PAH)的临床前模型中,野百合碱动物模型提供了模拟人PAH几个关键方面的优势,包括血管重塑,平滑肌细胞增殖,内皮功能障碍,炎性细胞因子上调和右心室衰竭,需要单次注射药物[4]。通过注射野百合碱观察到与PH发展相关的多种途径的变化,包括活化的糖酵解,增加的增殖标记,肉毒碱稳态的破坏,炎症和纤维化生物标志物的增加以及谷胱甘肽生物合成的减少[5]。 |
Animal Experiment |
大鼠:在该研究中使用总共20只雄性Sprague Dawley大鼠(SD; 220-270g)(每组n = 10)。对照组接受野百合碱(MCT)的载体。肺动脉高压前期(PH)组单次注射MCT(60 mg / kg ip)诱导并在14天后处死[5]。 |
Data Literature Source |
[1]. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012 Feb 15; 302 (4) :L363-9. [2]. Kusuma SS, et al. Antineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem. 2014; 14 (9) :1237-48. [3]. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992; 22 (5-6) :307-25. [4]. Nogueira-Ferreira R, et al. Exploring the monocrotaline animal model for the study of pulmonary arterial hypertension: A network approach. Pulm Pharmacol Ther. 2015 Dec; 35:8-16. [5]. Rafikova O,et al. Metabolic Changes Precede the Development of Pulmonary Hypertension in the Monocrotaline Exposed RatLung. PLoS One. 2016 Mar 3; 11 (3) :e0150480. |
Unit |
Bottle |
Specification |
20mg 10mM*1mL in DMSO 100mg |