2. NF-κB MAPK/ERK Pathway PI3K/Akt/mTOR Cell Cycle/DNA Damage Epigenetics Apoptosis Neuronal Signaling Metabolic Enzyme/Protease Stem Cell/Wnt
  3. NF-κB p38 MAPK mTOR Topoisomerase AMPK Apoptosis Cholinesterase (ChE) HIF/HIF Prolyl-Hydroxylase β-catenin
  4. Cryptolepine

Cryptolepine 是一种口服有效的多活性生物碱，具有抗癌、抗菌、抗病毒、抗疟疾、抗炎、抗高血糖、缓解疼痛等多种特性。Cryptolepine 可作为 c-Myc、mTOR、NF-κB、HIF-1、MAPK 抑制剂及 AMPKα1/2 激活剂，能嵌入 DNA、抑制拓扑异构酶 II (Top II)，破坏线粒体动力学并诱导细胞凋亡 (apoptosis)。Cryptolepine 同时具有抗疟原虫及胆碱酯酶抑制活性。Cryptolepine 可用于肿瘤 (黑色素瘤、肝细胞癌、乳腺腺癌等)、疟疾、炎症性疾病及糖尿病的相关研究，特别是抑制肿瘤生长与抗疟原虫感染。

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Cryptolepine

Cryptolepine Chemical Structure

CAS No. : 480-26-2

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Cryptolepine 相关抗体

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cryptolepine is an orally active multi-potent alkaloid with anti-cancer, anti-bacterial, anti-viral, anti-malarial, anti-inflammatory, anti-hyperglycemic, relieve pain and other properties. Cryptolepine acts as an inhibitor of c-Myc, mTOR, NF-κB, HIF-1, MAPK and an activator of AMPKα1/2. It intercalates into DNA, inhibits topoisomerase II (Top II), disrupts mitochondrial dynamics and induces cell apoptosis (apoptosis). Cryptolepine also exhibits anti-plasmodial and cholinesterase inhibitory activities. Cryptolepine can be used in research related to tumors (melanoma, hepatocellular carcinoma, mammary adenocarcinoma, etc.), malaria, inflammatory diseases and diabetes, particularly in studies focused on inhibiting tumor growth and anti-plasmodial infection[1][2][3][4][6][7][8][9][10][11][12][13][14].
IC50 & Target

p38 MAPK

 

Topoisomerase II

 

hAChE

485 nM (IC50)

BChE

699 nM (IC50)

eel AChE

267 nM (IC50)

HIF-1α

 

体外研究
(In Vitro)

Cryptolepine (2.5-7.5 μM；24 h) 以浓度依赖的方式诱导 A375 和 Hs294t 黑色素瘤细胞发生线粒体耗竭，并激活 AMPKα1/2-LKB1通路[1]。
Cryptolepine (2.5-10 μM) 可抑制 LPS 诱导的 RAW 264.7 细胞中一氧化氮的生成，并通过抑制 NF-κB 激活过程中的 DNA 结合活性来发挥抗炎作用[4]。
Cryptolepine (0.5-2 μM；24 h) 以剂量依赖的方式抑制经 200 ng/mL IL-6 处理 24 h 的人肝癌 HepG2 细胞中 p-STAT3 和 IL-23 的水平[6]。
Cryptolepine (1-20 μM；缺氧条件；24 h) 以时间和剂量依赖的方式降低 T47D、4T1、MCF-7 和 MDA-MB-231 乳腺癌细胞中缺氧诱导的 HIF-1α 蛋白水平[8]。
Cryptolepine (0-100 μg/mL；72 h)，提取自Cryptolepis sanguinolenta，对 Jurkat 白血病细胞系具有细胞毒性，其 CC50值<62.56 μg/mL[9]。
Cryptolepine (10 µM-1.69×10−4 µM；48 h) 抑制恶性疟原虫 (NF54) IV/V 期晚期配子体的活力，IC50为 1965 nM[12]。
Cryptolepine (0.5-1.2 μM；48 h) 可在 IC30 (0.5 μM) 和 IC50 浓度下强效抑制未受刺激及受 WNT3a 刺激的 DLD1 结直肠癌细胞的迁移[14]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cryptolepine 相关抗体:

Western Blot Analysis[1]

Cell Line: A375, Hs294t
Concentration: 2.5, 5.0, 7.5 μM
Incubation Time: 24 h
Result: Caused a concentration-dependent decrease in protein levels of Mfn1, Mfn2, Opa1, and Drp1 compared to vehicle-treated controls.\n
Reduced total and phosphorylated mTOR protein levels, as well as phosphorylation of p70S6K and 4E-BP1 (downstream targets) in a concentration-dependent manner; total p70S6K and 4E-BP1 levels were unaffected.\n
Reduced levels of PGC-1α, SIRT1, Opa1, and c-Myc proteins in a concentration-dependent manner.

ELISA Assay[6]

Cell Line: human hepatoma HepG2 cells treated with IL-6
Concentration: 0.5,1,2 μM (in the presence of 200 ng/mL IL-6)
Incubation Time: 24 h
Result: Suppressed p-STAT3 and IL-23 levels in a dose-dependent fashion.
Additively suppressed p-STAT3 and IL-23 levels when co-treated with 5 μM niclosamide at 0.5 μM.

Western Blot Analysis[8]

Cell Line: T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells
Concentration: 1-20 μM
Incubation Time: 24 h under hypoxia
Result: Reduced hypoxia-induced HIF-1α protein levels in T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells.
Dose-dependently suppressed hypoxia-induced protein expression of GLUT-1, LDHA, PFKFB3, p-PFKFB3, and PFK-1.\n
Dose-dependently decreased the phosphorylation of Ras, p-c-Raf, p-MEK1/2, p-ERK1/2 (MAPK pathway), p-mTOR, p-p70S6K, p-4E-BP1, and p-eIF4E (mTOR pathway and eIF4E phosphorylation); increased p-AMPKα and p-TSC2.
体内研究
(In Vivo)

Cryptolepine (10 mg/kg；i.p.；每周 3 次；持续 24 天) 通过破坏线粒体动力学与生物发生，抑制无胸腺裸鼠的黑色素瘤肿瘤生长[1]。
Cryptolepine (7.0-112.6 mg/kg/d；s.c.；每日，4 天) 未显著降低小鼠体内 P. berghei 的原虫血症水平[3]。
Cryptolepine (10-40 mg/kg；i.p. or p.o.；每日；4 天) 在大鼠急性炎症模型中表现出剂量依赖性抗炎活性，且不会诱发胃损伤[4]。
Cryptolepine (10-40 mg/kg；i.p.) 在角叉菜胶诱导的大鼠足肿胀模型中呈现剂量依赖性抗炎活性，如抑制 LPS 诱导的微血管通透性；Cryptolepine (10-40 mg/kg; i.p.) 还在乙酸诱导的小鼠扭体模型中表现出剂量依赖性镇痛活性[7]。
Cryptolepine (5-20 mg/kg；i.p.；每 2 天 1 次；共 7 次) 可剂量依赖性地抑制 BALB/c 小鼠体内 4T1 肿瘤的生长，其中 20 mg/kg 剂量组的肿瘤生长抑制率 (TGI) 达 71.5%，其作用机制为抑制HIF-1介导的糖酵解与 ATP 生成[8]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: athymic nude mice (female, 4–5 weeks of age)[1]
Dosage: 10 mg/kg
Administration: i.p.; 3 days/week; 24 days
Result: Reduced tumor volume by 68%; reduced average wet tumor weight by 61%; reduced tumor ATP content by 32%; reduced levels of phosphorylated Drp1, c-Myc, SIRT1, and PGC-1α proteins; enhanced phosphorylation of AMPKα1/2; reduced phosphorylation of 4E-BP1.
Animal Model: Swiss albino (TO strain, male, mean weight 25 g, Eperythrozoon-free, Plasmodium berghei-infected)[3]
Dosage: 7.0, 14.1, 28.2, 56.3, 112.6 mg/kg/d
Administration: s.c.; daily; 4 days
Result: Showed no significant effect on P. berghei parasitaemia, with mean parasitaemia values ranging from 33.04% to 46.44% and no significant reduction compared to control mice.
Animal Model: not specified strain[4]
Dosage: 10, 40 mg/kg (i.p. for paw edema; p.o. daily for 4 days for microvascular permeability)
Administration: i.p. (paw edema); p.o.; daily; 4 days (microvascular permeability)
Result: Exhibited dose-dependent anti-inflammatory activity in carrageenan-induced paw edema; inhibited LPS-induced microvascular permeability without causing gastric lesions
Animal Model: carrageenan-induced paw oedema model, LPS-induced microvascular permeability model, and acetic acid-induced writhing model in Wistar rats (male, 120–200 g) [7]
Dosage: 10, 20, 40 mg/kg
Administration: i.p.; single dose 1 hour before carrageenan injection
Result: 1. Produced statistically significant inhibition of paw oedema formation in a dose-dependent manner at the third hour (oedema peak).
2. Significantly inhibited LPS-induced microvascular permeability in a dose-dependent manner.
3. Inhibited carrageenan-induced pleurisy by 23.6%, 35.3%, and 51.2% at 10, 20, and 40 mg/kg, respectively, in a dose-dependent manner.
4. Significantly inhibited writhing in a dose-dependent manner.
Animal Model: BALB/c (female, 4–6 weeks old, 18–22 g, 4T1 tumor xenograft model)[8]
Dosage: 5, 10, 20 mg/kg
Administration: i.p.; once every 2 days; seven injections
Result: Reduced tumor weight with tumor growth inhibition (TGI) values of 45.8% (10 mg/kg) and 71.5% (20 mg/kg).
Dose-dependently decreased HIF-1α protein expression in tumors; reduced tumor lactic acid levels by 54.1% (10 mg/kg) and 68.4% (20 mg/kg).
Dose-dependently reduced tumor ATP production.
Decreased the ratio of phosphorylated eIF4E to total eIF4E in tumors at 10 and 20 mg/kg doses.
分子量

232.29

Formula

C16H12N2
CAS 号
结构分类
初始来源
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
参考文献

Cryptolepine 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Cryptolepine480-26-2NF-κBp38 MAPKmTORTopoisomeraseAMPKApoptosisCholinesterase (ChE)HIF/HIF Prolyl-Hydroxylaseβ-cateninNuclear factor-κBNuclear factor-kappaBMammalian target of RapamycinAMP-activated protein kinaseHypoxia-inducible factorsHIFsHIF-PHBeta cateninA375Plasmodium falciparumAMPKα1/2LKB1Cryptolepis sanguinolentaTopoisomerase IIc-MycHepG2Inhibitorinhibitorinhibit

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