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 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 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.

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Cryptolepine

Cryptolepine Chemical Structure

CAS No. : 480-26-2

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Cryptolepine Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Topoisomerase Topo I Topo II DNA gyrase

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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HIF-1α HIF

  • Biological Activity

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Description

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 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

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.05 μM
Compound: 13
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
[PMID: 34710743]
Erythrocyte IC50
19.65 nM
Compound: 59
Antiplasmodial activity against Plasmodium falciparum NF54 gametocytes infected in human erythrocyte assessed as inhibition of parasite growthVincubated for 48 hrs by SYBR Green dye based fluorescence assay
Antiplasmodial activity against Plasmodium falciparum NF54 gametocytes infected in human erythrocyte assessed as inhibition of parasite growthVincubated for 48 hrs by SYBR Green dye based fluorescence assay
[PMID: 35985254]
KB IC50
1.5 μM
Compound: 2a
In vitro cell survival assay on cancer KB cell lines
In vitro cell survival assay on cancer KB cell lines
[PMID: 11300877]
MCF7 IC50
0.63 μM
Compound: 13
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
[PMID: 34710743]
MRC5 IC50
1.5 μM
Compound: crytolepine
Cytotoxicity against human diploid embryonic lung cell line MRC-5 using MTT assay
Cytotoxicity against human diploid embryonic lung cell line MRC-5 using MTT assay
[PMID: 12139461]
Vero IC50
3.2 μg/mL
Compound: Cryp
Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay
[PMID: 21134759]
In Vitro

Cryptolepine (2.5-7.5 μM; 24 h) induces mitochondrial depletion in A375 and Hs294t melanoma cells in a concentration-dependent manner and activates the AMPKα1/2-LKB1 pathway[1].
Cryptolepine (2.5-10 μM) inhibits nitric oxide production in LPS-induced RAW 264.7 cells and exerts anti-inflammatory effects by suppressing the DNA-binding activity during NF-κB activation[4].
Cryptolepine (0.5-2 μM; 24 h) dose-dependently inhibits the levels of p-STAT3 and IL-23 in human hepatocellular carcinoma HepG2 cells treated with 200 ng/mL IL-6 for 24 h[6].
Cryptolepine (1-20 μM; hypoxic conditions; 24 h) reduces hypoxia-induced HIF-1α protein levels in T47D, 4T1, MCF-7 and MDA-MB-231 breast cancer cells in a time- and dose-dependent manner[8].
Cryptolepine (0-100 μg/mL; 72 h), extracted from Cryptolepis sanguinolenta, exhibits cytotoxicity against the Jurkat leukemia cell line, with a CC50 value of <62.56 μg/mL[9].
Cryptolepine (10 μM-1.69×10-4 μM; 48 h) inhibits the viability of late stage IV/V gametocytes of Plasmodium falciparum (NF54), with an IC50 of 1965 nM[12].
Cryptolepine (0.5-1.2 μM; 48 h) potently inhibits the migration of unstimulated and WNT3a-stimulated DLD1 colorectal cancer cells at IC30(0.5 μM) and IC50 concentrations[14].

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

Cryptolepine Related Antibodies

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.
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.
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.
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.
In Vivo

Cryptolepine (10 mg/kg; i.p.; three times per week; for 24 consecutive days) inhibits melanoma tumor growth in athymic nude mice by disrupting mitochondrial dynamics and biogenesis, resulting in a 68% reduction in tumor volume and a 61% reduction in tumor weight[1].
Cryptolepine (7.0-112.6 mg/kg/d; s.c.; daily, for 4 days) does not significantly reduce the parasitemia level of P. berghei in mice[3].
Cryptolepine (10-40 mg/kg; i.p. or p.o.; daily; 4 days) exhibits dose-dependent anti-inflammatory activity in a rat model of acute inflammation without inducing gastric injury[4].
Cryptolepine (10-40 mg/kg; i.p.) exhibits dose-dependent anti-inflammatory activity in carrageenan-induced rat paw edema models, such as inhibiting LPS-induced microvascular permeability; Cryptolepine (10-40 mg/kg; i.p.) also shows dose-dependent analgesic activity in acetic acid-induced mouse writhing models[7].
Cryptolepine (5-20 mg/kg; i.p.; once every 2 days; total 7 administrations) dose-dependently inhibits the growth of 4T1 tumors in BALB/c mice, with the tumor growth inhibition (TGI) rate reaching 71.5% in the 20 mg/kg dose group. Its mechanism of action involves the inhibition of HIF-1-mediated glycolysis and ATP production[8].

MedChemExpress (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: 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.
Molecular Weight

232.29

Formula

C16H12N2
CAS No.
SMILES

N1=C2C=CC=CC2=C3C1=CC=4C=CC=CC4N3C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Cryptolepine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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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