Dibenzo[a,g]quinolizinium,5,6-dihydro-2,3,9,10-tetramethoxy-, hydroxide (9CI)

Product NameDibenzo[a,g]quinolizinium,5,6-dihydro-2,3,9,10-tetramethoxy-, hydroxide (9CI)
CAS131-04-4
MFC21H22NO4.HO
MW369.41102
EINECS
MOL File131-04-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO : 15.62 mg/mL (42.28 mM; ultrasonic and warming and heat to 60°C)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

Uses

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

Safety Profile

Experimental reproductive effects. When heated to decomposition it emits toxic fumes of NOx.

in vivo

Palmatine (50 or 100 mg/kg; p.o.; daily for 7 days) ameliorates DSS (dextran sulfate sodium)-induced colitis and prevents infiltration of inflammatory cells^[1]. Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/Lipopolysaccharides (HY-D1056)-induced fulminant hepatic failure in mice^[2]. Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice^[4]. Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice^[5].

Animal Model:	DSS- induced Colitis BALB/c mice model (8-week-old)^[1]
Dosage:	50 or 100 mg/kg
Administration:	Orally, daily, for 7 days
Result:	Ameliorated DSS-induced colitis and prevented infiltration of inflammatory cells; remarkably extended the colon length; significantly suppressed the colonic MPO activity. Decreased the levels of colonic inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); Protected mucosal integrity by modulating TJs protein and apoptosis proteins; Restored DSS-induced decreases of TJ protein ZO-1, ZO-2 and claudin-1; Reduced Bax expression and enhanced Bcl-2 expression at the dose of 100mg/kg, prevented epithelial apoptosis and improved intestinal integrity. Prevented DSS-induced changes of gut microbiota in colitis mice.

Animal Model:	Male ICR mice (20–22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant hepatic failure model^[2]
Dosage:	25, 50, 100, or 200 mg/kg
Administration:	Intraperitoneal injection, 1 h before the GalN/LPS treatment
Result:	Attenuated the mortality and serum aminotransferase activities increased by GalN/LPS. Prevented the increase of serum TNF-α and augmented that of serum IL-10. Decreased the TNF-a mRNA expression and increased the IL-10 mRNA expression. Attenuated the apoptosis of hepatocytes.

Animal Model:	Swiss young male albino mice, with Scopolamine (HY-N0296)- and diazepam-induced amnesia model^[4]
Dosage:	0.1, 0.5, 1 mg/kg
Administration:	Intraperitoneal injection, 10 days
Result:	Significantly improved learning and memory of mice at 0.5 and 1 mg/kg and did not show any significant effect on locomotor activity of the mice. Significantly reversed scopolamine- and diazepam-induced amnesia in mice. Significantly reduced brain acetylcholinesterase activity of mice.

Animal Model:	BALB/c-nude mice, HCT-116 xenograft model^[5]
Dosage:	33.75, 67.5 and 135 mg/kg
Administration:	Oral administration, once a day for 26 days
Result:	The tumor volume and weight of the treatment group were significantly reduced.

IC 50

IDO-1: 3 μM (IC₅₀, HEK 293-hIDO-1); IDO-1: 157 μM (IC₅₀, rhIDO-1); WNV NS2B-NS3: 96 μM (IC₅₀)

References

[1] Zhang XJ, et al. Palmatine ameliorated murine colitis by suppressing tryptophan metabolism and regulating gut microbiota.Pharmacol Res. 2018 Nov;137:34-46. DOI:10.1016/j.phrs.2018.09.010
[2] Lee WC, et al. Palmatine attenuates D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mice. Food Chem Toxicol. 2010 Jan;48(1):222-8. DOI:10.1016/j.fct.2009.10.004
[3] Jia F, et al. Identification of palmatine as an inhibitor of West Nile virus. Arch Virol. 2010 Aug;155(8):1325-9. DOI:10.1007/s00705-010-0702-4
[4] Dhingra D, et al. Memory-enhancing activity of palmatine in mice using elevated plus maze and morris water maze. Adv Pharmacol Sci. 2012;2012:357368. DOI:10.1155/2012/357368
[5] Liu X, et al. Palmatine induces G2/M phase arrest and mitochondrial-associated pathway apoptosis in colon cancer cells by targeting AURKA. Biochem Pharmacol. 2020 May;175:113933. DOI:10.1016/j.bcp.2020.113933
[6] Long J, et al. Palmatine: A review of its pharmacology, toxicity and pharmacokinetics. Biochimie. 2019 Jul;162:176-184. DOI:10.1016/j.biochi.2019.04.008

Preparation Products And Raw materials

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