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quinidine polygalacturonate

Names

[ CAS No. ]:
27555-34-6

[ Name ]:
quinidine polygalacturonate

[Synonym ]:
Cinchonan-9-ol, 6'-methoxy-, (9S)-, compd. with D-galacturonic acid (1:1)
(9S)-6'-Methoxycinchonan-9-ol - D-galacturonic acid (1:1)

Biological Activity

[Description]:

Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Research Areas >> Cardiovascular Disease
Research Areas >> Infection
Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[In Vitro]

Quinidine polygalacturonate shows cytotoxicity against MES-SA cells, and induces apoptosis[4]. Apoptosis Analysis[4] Cell Line: MES-SA and MESSA/DX5 cells Concentration: 10 μM Incubation Time: 24 hours Result: Increased the apoptotic portion sub-G1 DNA contents induced by paclitaxel, while paclitaxel had no effect on sub-G1 DNA contents undergoing apoptosis. Cell Cytotoxicity Assay[4] Cell Line: MES-SA and MESSA/DX5 cells Concentration: 10 μM Incubation Time: 24 hours Result: Showed cytotoxicity against MES-SA cells in a concentration-dependent manner.

[In Vivo]

Quinidine polygalacturonate shows effects on the PTZ-induced seizure threshold[5]. Animal Model: Male mice of the NMRI strain (age 5-6 weeks and weight 25-30 g)[5] Dosage: 10, 20, and 30 mg/kg Administration: Intraperitoneal injection; 10, 20, and 30 mg/kg; once Result: Increased the threshold dose for the onset to tonic hind limb extension at a dose of 30 mg/kg, compared to the saline-treated control group (p<0.05).

[References]

[1]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991 Jul;103(3):1807-13.

[2]. Roden DM, et al. Class I antiarrhythmic agents: quinidine, procainamide and N-acetylprocainamide, disopyramide. Pharmacol Ther. 1983;23(2):179-91.

[3]. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS and immunoassay findings in rat urine. J Anal Toxicol. 1990 Sep-Oct;14(5):311-7.

[4]. Sang-Yun Lee, et al. Hydrocinchonine, cinchonine, and quinidine potentiate paclitaxel-induced cytotoxicity and apoptosis via multidrug resistance reversal in MES-SA/DX5 uterine sarcoma cells. Environ Toxicol. 2011 Aug;26(4):424-31.

[5]. Hassan Jamali, et al. Effect of dextromethorphan/quinidine on pentylenetetrazole- induced clonic and tonic seizure thresholds in mice. Neurosci Lett. 2020 Jun 11;729:134988.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H34N2O9

[ Molecular Weight ]:
518.556

[ Exact Mass ]:
518.226440


Related Compounds