Palmatine hydroxide

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC 50 s 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 IC 50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities In Vitro Palmatine (0-100 μM; 42 h) suppresses WNV with an EC 50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC 50 values of 26.4 μM and 7.3 μM, respectively. Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation . Palmatine (0-704 μM; 24 h) reduces AURKA protein levels, induces G2/M phase arrest, and induces apoptosis in colon cancer cells via the mitochondrial associated pathway . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: HCT-116, SW480, HT-29 Concentration: 0, 88, 176, 352, and 704 μM (HCT-116, SW480); 0, 141, 282, 564, and 1128 μM (HT-29) Incubation Time: 24, 48 and 72 h Result: Decreased cell viability in a dose-dependent manner. Western Blot Analysis Cell Line: HCT-116, SW480, HT-29 Concentration: 100 nM for HCT-116, 500 nM for SW480 and HT-29 Incubation Time: 24, 48 and 72 h Result: Promoted the expression of apoptosis markers such as P53 / P73, Caspase3, and Caspase9. Reduced AURKA protein levels. Increased cyt. c in the cytoplasm while reduced Bcl2 and Bcl-xl in a dose-dependent manner. Cell Cycle Analysis Cell Line: HCT-116, SW480 Concentration: 88, 176, 352 and 704 μM Incubation Time: 24, 48 and 72 h Result: Induced G2/M phase arrest in a dose-dependent manner. Apoptosis Analysis Cell Line: HCT-116, SW480 Concentration: 88, 176, 352 and 704 μM Incubation Time: 24, 48 and 72 h Result: Induced apoptosis in a dose-dependent manner. 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 . Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/ Lipopolysaccharides -induced fulminant hepatic failure in mice. Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice. Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: DSS- induced Colitis BALB/c mice model (8-week-old) 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 100 mg/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 modelDosage: 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 - and diazepam-induced amnesia modelDosage: 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 modelDosage: 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. Form:Solid IC50& Target:IDO-1 3 μM (IC 50 , HEK 293-hIDO-1) IDO-1 157 μM (IC 50 , rhIDO-1) WNV NS2B-NS3 96 μM (IC 50 )

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