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Monocrotaline

MCE China：Monocrotaline

Brand：MedChemExpress (MCE)

Cat. No.HY-N0750

CAS：315-22-0

Synonyms：Crotaline

Purity：99.88%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].

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[2].

In Vivo：.f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of chronic progressive pulmonary hypertension (PH) Background Pulmonary arterial hypertension (PAH) is characterized by vascular remodeling of the distal pulmonary arterial circulation. PAH remodeling includes apoptosis and proliferation of pulmonary vascular endothelial cells, muscularization of distal pulmonary arterioles, deposition of extracellular matrix proteins, and perivascular inflammation; it is accompanied by increased pulmonary vascular resistance, leading to right ventricular (RV) failure and death. However, the cause of pulmonary vascular remodeling in PAH is still unclear. Monocrotaline induces right ventricular hypertrophy (RVH) and pulmonary vascular remodeling. Specific Mmodeling Methods Rat[10]: male • adult Sprague Dawley rats • 300-350 gAdministration: 60 mg/kg • sc for single dose • control group: saline solutionMcie[11]: male • C57BL/6 mice • 6-8 weeks oldAdministration: 600 mg/kg • sc • once weekly for 4 weeks Note 1. Monocrotaline-induced pulmonary hypertension can be reversed by tail vein injection of 25 μg mouse mesenchymal stem cells in 100 μL PBS three hours after each injection. 2. Extracellular vesicles (EVs) isolated from the circulation or lungs of mice with monocrotaline-induced pulmonary hypertension induce right ventricular hypertrophy (RVH) and pulmonary vascular remodeling when injected into healthy mice. Modeling Record Molecular changes: ↑ expression of 5-HTR2A, 5-HTR2B and 5-HTT in lung homogenate; ↑ expression of IL-1b, IL6, TNF-a and MCP-1; ↑ levels of total collagen fibers and total pulmonary vascular collagen. Physiological indicators: Increased right ventricular systolic pressure, right heart hypertrophy, gas exchange; collagen deposition in the pulmonary artery. Correlated Product(s): Terguride[10]

IC50 & Target：OCT1 36.8 μM (IC50) OCT2 1852.6 μM (IC50)

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References：

[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.  [Content Brief]

[2]. Wu XH, et al. Experimental animal models of pulmonary hypertension: Development and challenges. Animal Model Exp Med. 2022 Sep; 5(3):207-216.  [Content Brief]

[3]. Kusuma SS, et al. Antineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem. 2014;14(9):1237-48.  [Content Brief]

[4]. Jin H, et al. Astragaloside IV blocks monocrotaline‑induced pulmonary arterial hypertension by improving inflammation and pulmonary artery remodeling. Int J Mol Med. 2021 Feb;47(2):595-606.  [Content Brief]

[5]. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22(5-6):307-25.  [Content Brief]

[6]. Chen JY, et al. An in vitro study on interaction of anisodine and monocrotaline with organic cation transporters of the SLC22 and SLC47 families. Chin J Nat Med. 2019 Jul;17(7):490-497.  [Content Brief]

[7]. 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.  [Content Brief]

[8]. Zhao J, et al. Effects of paclitaxel intervention on pulmonary vascular remodeling in rats with pulmonary hypertension. Exp Ther Med. 2019 Feb;17(2):1163-1170.  [Content Brief]

[9]. 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.  [Content Brief]

[10]. Dumitrascu R, Kulcke C, Königshoff M, Kouri F, Yang X, Morrell N, Ghofrani HA, Weissmann N, Reiter R, Seeger W, Grimminger F, Eickelberg O, Schermuly RT, Pullamsetti SS. Terguride ameliorates monocrotaline-induced pulmonary hypertension in rats. Eur Respir J. 2011 May;37(5):1104-18.  [Content Brief]

[11]. Aliotta JM, Pereira M, Wen S, Dooner MS, Del Tatto M, Papa E, Goldberg LR, Baird GL, Ventetuolo CE, Quesenberry PJ, Klinger JR. Exosomes induce and reverse monocrotaline-induced pulmonary hypertension in mice. Cardiovasc Res. 2016 Jun 1;110(3):319-30.  [Content Brief]