| 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 (HY-D1056)-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. 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 model. 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. 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. 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. |
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| In Vitro | Palmatine (0-100 μM; 42 h) suppresses WNV with an EC50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC50 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. 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 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 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 h. Result: Induced apoptosis in a dose-dependent manner. |
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