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Palmatine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Palmatine图片
CAS NO:3486-67-7
包装与价格:
包装价格(元)
250mg电议
1 g电议

产品名称
黄藤素
产品介绍
Palmatine 是一种具有口服活性的、不可逆的IDO-1抑制剂,对 HEK 293-hIDO-1 和 rhIDO-1 的IC50分别为 3 μM 和 157 μM。Palmatine 也能非竞争性抑制西尼罗病毒 (WNV)NS2B-NS3蛋白酶,IC50为 96 μM。Palmatine 具有抗癌、抗炎、神经保护、抗细菌、抗病毒活性。
生物活性

Palmatine 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 can also inhibit West Nile virus (WNV)NS2B-NS3 proteasein an uncompetitive manner with anIC50of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

IC50& Target[1]

IDO-1

3 μM (IC50, HEK 293-hIDO-1)

IDO-1

157 μM (IC50, rhIDO-1)

WNV NS2B-NS3

96 μM (IC50)

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 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 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 h
Result:Induced apoptosis in a dose-dependent manner.
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.
分子量

352.40

Formula

C21H22NO4+

CAS 号

3486-67-7

中文名称

黄藤素

结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
来源
  • Plants
  • Rutaceae
  • Phellodendron amurenseRupr.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.