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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- No. CAS: 480-26-2
- Fòrmula: C16H12N2
- Peso molecular:232.29
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
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p38 MAPK |
Topoisomerase II |
hAChE 485 nM (IC50) |
BChE 699 nM (IC50) |
eel AChE 267 nM (IC50) |
HIF-1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
1.05 μM
Compound: 13
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
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[PMID: 34710743] |
| Erythrocyte | IC50 |
19.65 nM
Compound: 59
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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
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[PMID: 35985254] |
| KB | IC50 |
1.5 μM
Compound: 2a
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In vitro cell survival assay on cancer KB cell lines
In vitro cell survival assay on cancer KB cell lines
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[PMID: 11300877] |
| MCF7 | IC50 |
0.63 μM
Compound: 13
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Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
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[PMID: 34710743] |
| MRC5 | IC50 |
1.5 μM
Compound: crytolepine
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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
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[PMID: 12139461] |
| Vero | IC50 |
3.2 μg/mL
Compound: Cryp
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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
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[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.
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Cell Line:A375, Hs294t
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Concentration:2.5, 5.0, 7.5 μM
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Incubation Time:24 h
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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.
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Cell Line:human hepatoma HepG2 cells treated with IL-6
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Concentration:0.5,1,2 μM (in the presence of 200 ng/mL IL-6)
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Incubation Time:24 h
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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.
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Cell Line:T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells
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Concentration:1-20 μM
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Incubation Time:24 h under hypoxia
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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 (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.
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Animal Model:athymic nude mice (female, 4–5 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 3 days/week; 24 days
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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.
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Animal Model:Swiss albino (TO strain, male, mean weight 25 g, Eperythrozoon-free, Plasmodium berghei-infected)[3]
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Dosage:7.0, 14.1, 28.2, 56.3, 112.6 mg/kg/d
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Administration:s.c.; daily; 4 days
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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.
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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]
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Dosage:10, 20, 40 mg/kg
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Administration:i.p.; single dose 1 hour before carrageenan injection
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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.
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Animal Model:BALB/c (female, 4–6 weeks old, 18–22 g, 4T1 tumor xenograft model)[8]
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Dosage:5, 10, 20 mg/kg
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Administration:i.p.; once every 2 days; seven injections
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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.
Chemical Information
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No. CAS 480-26-2
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Peso molecular 232.29
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Fòrmula C16H12N2
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SMILES
N1=C2C=CC=CC2=C3C1=CC=4C=CC=CC4N3C
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Pal HC, et al. Cryptolepine inhibits melanoma cell growth through coordinated changes in mitochondrial biogenesis, dynamics and metabolic tumor suppressor AMPKα1/2-LKB1. Sci Rep. 2017;7(1):1498. Published 2017 May 4. [Content Brief]
[2]. Ferguson G, et al. Computational Insight into the Intercalating Properties of Cryptolepine. ACS Omega. 2025;10(18):18283-18290. Published 2025 Apr 28. [Content Brief]
[4]. Tudu CK, et al. Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight. Naunyn Schmiedebergs Arch Pharmacol. 2023;396(2):229-238. [Content Brief]
[5]. Mensah KB, et al. Cryptolepine, the Main Alkaloid of the Antimalarial Cryptolepis sanguinolenta (Lindl.) Schlechter, Induces Malformations in Zebrafish Embryos. Biochem Res Int. 2019;2019:7076986. Published 2019 Jul 8. [Content Brief]
[6]. Domfeh SA, et al. Cryptolepine inhibits hepatocellular carcinoma growth through inhibiting interleukin-6/STAT3 signalling. BMC Complement Med Ther. 2021;21(1):161. Published 2021 Jun 2. [Content Brief]
[7]. Olajide OA, et al. Anti-inflammatory properties of cryptolepine. Phytother Res. 2009;23(10):1421-1425. [Content Brief]
[8]. Zheng Z, et al. Cryptolepine suppresses breast adenocarcinoma via inhibition of HIF-1 mediated glycolysis. Biomed Pharmacother. 2022;153:113319. [Content Brief]
[9]. Amissah JN, et al. Mineral Fertilization Influences the Growth, Cryptolepine Yield, and Bioefficacy of Cryptolepis sanguinolenta (Lindl.) Schlt. Plants (Basel). 2022;11(1):122. Published 2022 Jan 1. [Content Brief]
[10]. Domfeh SA, et al. The Pharmacologically Active Alkaloid Cryptolepine Activates a Type 1 Interferon Response That Is Independent of MAVS and STING Pathways. J Immunol Res. 2022;2022:8873536. Published 2022 Jul 26. [Content Brief]
[11]. Amissah JN, et al. Increasing the planting density of Cryptolepis sanguinolenta (Lindl.) Schlt increased root biomass and cryptolepine yield. Heliyon. 2024;10(10):e30932. Published 2024 May 9. [Content Brief]
[12]. Forkuo AD, et al. In vitro anti-malarial interaction and gametocytocidal activity of cryptolepine. Malar J. 2017;16(1):496. Published 2017 Dec 28. [Content Brief]
[13]. Quarshie JT, et al. Cryptolepine Suppresses Colorectal Cancer Cell Proliferation, Stemness, and Metastatic Processes by Inhibiting WNT/β-Catenin Signaling. Pharmaceuticals (Basel). 2023;16(7):1026. Published 2023 Jul 19. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cryptolepine Related Classifications
HY-W800535 Related Classifications
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