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Monocrotaline

CAS No. : 315-22-0

MCE 国际站：Monocrotaline

产品活性：Monocrotaline 是一种 11 元大环吡咯利西啶生物碱。Monocrotaline 对 OCT-1 和 OCT-2 有抑制作用，其 IC₅₀ 值分别为 36.8 µM 和 1.8 mM。Monocrotaline 具有抗肿瘤活性，对肝癌细胞有一定的细胞毒性。Monocrotaline 用于在啮齿动物中诱导肺动脉高压模型。

研究领域：Others

作用靶点：Others

结构分类：生物碱  |  吡咯类生物碱  |  结构分类

来源：植物  |  豆科  |  猪屎豆

In Vitro: Monocrotaline a natural ligand exhibits dose-dependent cytotoxicity with potent antineoplastic activity. The in vitro cytotoxicity of monocrotaline is proved at IC₅₀ 24.966 µg/mL and genotoxicity at 2 X IC₅₀ against HepG2 cells.

In Vivo: Monocrotaline can be used in animal modeling to construct a rat model of hypertension.

MCT causes a pulmonary vascular syndrome in rats characterized by proliferative pulmonary vasculitis, pulmonary hypertension (PH), and cor pulmonale. Among preclinical models of pulmonary arterial hypertension (PAH), monocrotaline animal model offers the advantage of mimic several key aspects of human PAH, including vascular remodeling, proliferation of smooth muscle cells, endothelial dysfunction, upregulation of inflammatory cytokines, and right ventricle failure, requiring a single drug injection. Changes in multiple pathways associated with the development of PH, including activated glycolysis, increased markers of proliferation, disruptions in carnitine homeostasis, increased inflammatory and fibrosis biomarkers, and a reduction in glutathione biosynthesis are observed with the injection of monocrotaline.
Monocrotaline (60 mg/kg; i.p.; single dose), followed by Astragaloside (ASIV) (10 and 30 mg/kg/day for 21 days), significantly increases pulmonary artery pressure and promotes pulmonary artery structural remodeling and right ventricular hypertrophy in rats.
Monocrotaline (60 mg/kg; i.p.; single dose) causes Pulmonary arterial hypertension (PAH) in rat models in 3-4 weeks.
Monocrotaline (60 mg/kg; i.p. Single dose), 7 days after surgery, exhibits dose-dependent cytotoxicity and shows potent antitumor activity in a rat model of left pneumonectomy .
NOTE: Monocrotaline is dissolved in 1 N HCl, diluted in sterile saline and adjusted to pH 7.4 with 1 N NaOH.

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