Chelerythrine (Synonyms: 白屈菜红碱)

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Chelerythrine  (Synonyms: 白屈菜红碱)

Chelerythrine 是一种天然生物碱,为有效、选择性的 Ca2+/磷脂依赖性 PKC 拮抗剂,IC50 值为 0.7 μM。Chelerythrine 具有抗肿瘤、抗糖尿病、抗炎的活性。Chelerythrine 抑制 BclXL-Bak BH3 肽结合,IC50 为 1.5 μM,并从 BclXL 取代了 Bax。 Chelerythrine 诱导细胞凋亡和自噬。

Chelerythrine                                          (Synonyms: 白屈菜红碱)

Chelerythrine Chemical Structure

CAS No. : 34316-15-9

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Chelerythrine 的其他形式现货产品:

Chelerythrine chloride

Chelerythrine 相关产品

同靶点产品:

同靶点蛋白产品:

生物活性

Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity[2]. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy[3][4].

IC50 & Target[1]

PKC

0.7 μM (IC50)

体外研究
(In Vitro)

Chelerythrine (48 小时) 抑制 L-1210 细胞的生长 (IC50: 0.53 uM)[1]
Chelerythrine (0-20 μM,24 小时) 可抑制 A549 和 NCI-H1299 细胞的细胞活力,诱导细胞凋亡和自噬[4]
Chelerythrine (0-5 μM,24 或 48 小时) 可诱导 BclXL 过表达的 SH-SY5Y 细胞凋亡[3]
Chelerythrine (2.5-10 μM,16 小时) 可诱导 SH-SY5Y 细胞线粒体去极化 (线粒体电位降低),并刺激分离的线粒体释放 CytC[4]
Chelerythrine (0-100 ng/mL,24 小时) 可减少 LPS 诱导的原代巨噬细胞中 NO 和 TNF-α 的产生[5]
Chelerythrine (MIC: 0.156 mg/mL) 对革兰氏阳性菌、金黄色葡萄球菌 (SA)、MRSA 和超广谱 β-内酰胺酶金黄色葡萄球菌 (ESBLs-SA) 具有抗菌活性[6]

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

Chelerythrine 相关抗体:

Western Blot Analysis[4]

Cell Line: A549 and NCI-H1299 cells
Concentration: 10, 15, 20 μM
Incubation Time: 24 h
Result: Induced expression of LC3-II in a beclin 1-dependent way.

体内研究
(In Vivo)

Chelerythrine (5 mg/kg,腹腔注射,每日) 可减轻新生大鼠中部分单侧输尿管梗阻 (UUO) 引起的肾损伤,并恢复肾功能[2]
Chelerythrine (1-10 mg/kg,腹腔注射,注射 100 μg/kg LPS 前 24 小时和 1 小时) 在 LPS 诱导的小鼠内毒素休克中显示出抗炎作用 (提高存活率、降低血清亚硝酸盐和 TNF-α 水平)[5]

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

Animal Model: Unilateral ureteral obstruction (UUO) induced neonatal rats[2]
Dosage: 5 mg/kg
Administration: i.p., daily
Result: Attenuated kidney injury (Increased kidney weight and restored renal function).
Inhibited UUO-induced upregulated kidney injury molecule-1 expression, apoptosis, and renal fibrosis.

分子量

348.37

Formula

C21H18NO4

CAS 号

34316-15-9

中文名称

白屈菜红碱;白屈菜赤碱

结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
初始来源
  • 植物
  • 罂粟科
  • 博落回
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.

纯度 & 产品资料
Data Sheet (542 KB) 产品使用指南 (1538 KB)

参考文献
  • [1]. Herbert JM, et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1990 Nov 15;172(3):993-9.  [Content Brief]

    [2]. Shi B, et al. Protein kinase C inhibitor chelerythrine attenuates partial unilateral ureteral obstruction induced kidney injury in neonatal rats. Life Sci. 2019 Jan 1;216:85-91.  [Content Brief]

    [3]. Chan SL, et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6.  [Content Brief]

    [4]. Tang ZH, et al.Induction of reactive oxygen species-stimulated distinctive autophagy by chelerythrine in non-small cell lung cancer cells.Redox Biol. 2017 Aug;12:367-376.  [Content Brief]

    [5]. Li W, et al. Effect of chelerythrine against endotoxic shock in mice and its modulation of inflammatory mediators in peritoneal macrophages through the modulation of mitogen-activated protein kinase (MAPK) pathway. Inflammation. 2012 Dec;35(6):1814-24.  [Content Brief]

    [6]. He N, et al. Antibacterial mechanism of chelerythrine isolated from root of Toddalia asiatica (Linn) Lam. BMC Complement Altern Med. 2018 Sep 26;18(1):261.  [Content Brief]

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