标签归档：黄藤素

Palmatine (Synonyms: 黄藤素)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Palmatine  (Synonyms: 黄藤素)

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。

Palmatine (Synonyms: 黄藤素)

Palmatine Chemical Structure

CAS No. : 3486-67-7

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Palmatine 的其他形式现货产品:

Palmatine chloride Palmatine hydroxide

Palmatine 相关产品

•同靶点产品:

•同靶点蛋白产品:

生物活性

Palmatine 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 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 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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Palmatine 相关抗体:

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].

Shanghai Jinpan Biotech Co Ltd 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)[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, 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.

分子量

352.40

Formula

C21H22NO4+
CAS 号

3486-67-7
性状

固体

颜色

Light yellow to yellow

中文名称

黄藤素
结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
初始来源
  • 植物
  • 芸香科
  • 黄柏
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
Data Sheet (544 KB) SDS (393 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Zhang XJ, et al. Palmatine ameliorated murine colitis by suppressing tryptophan metabolism and regulating gut microbiota.Pharmacol Res. 2018 Nov;137:34-46.  [Content Brief]

    [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.  [Content Brief]

    [3]. Jia F, et al. Identification of palmatine as an inhibitor of West Nile virus. Arch Virol. 2010 Aug;155(8):1325-9.  [Content Brief]

    [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.  [Content Brief]

    [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.  [Content Brief]

    [6]. Long J, et al. Palmatine: A review of its pharmacology, toxicity and pharmacokinetics. Biochimie. 2019 Jul;162:176-184.  [Content Brief]

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