| 生物活性 | Palmatine hydroxide is an orally active and irreversibleindoleamine 2,3-dioxygenase1 (IDO-1)inhibitor withIC50s 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 proteasein an uncompetitive manner with anIC50of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5]. |
| IC50& Target | IDO-1 3 μM (IC50, HEK 293-hIDO-1) | IDO-1 157 μM (IC50, rhIDO-1) | WNV NS2B-NS3 96 μM (IC50) |
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体外研究
(In Vitro) | Palmatine (0-100 μM; 42 h) suppresses WNV with an EC50value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC50values of 26.4 μM and 7.3 μM, respectively[3].
Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation[5].
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[5].
Cell Proliferation Assay[5] | 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[5] | 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[5] | 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[5] | 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. |
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体内研究
(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 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[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, withScopolamine(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. |
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| 来源 | - Plants
- Rutaceae
- Phellodendron amurenseRupr.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 15.62 mg/mL(42.28 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.7070 mL | 13.5351 mL | 27.0702 mL | | 5 mM | 0.5414 mL | 2.7070 mL | 5.4140 mL | | 10 mM | 0.2707 mL | 1.3535 mL | 2.7070 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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