Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight

doi:10.1007/s00210-022-02302-7

Review

. 2023 Feb;396(2):229-238.

doi: 10.1007/s00210-022-02302-7. Epub 2022 Oct 17.

Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight

Affiliations

¹ Department of Life Sciences, Presidency University, 86/1 College Street, Kolkata, -700073, West Bengal, India.
² Chemical and Biochemical Processing Division, ICAR-Central Institute for Research On Cotton Technology, Mumbai, 400019, Maharashtra, India.
³ School of Biological and Environmental Sciences, Shoolini University of Biotechnology and Management Sciences, Solan, 173229, Himachal Pradesh, India.
⁴ Department of Biomedical Sciences, School of Biosciences and Technology, Vellore Institute of Technology (VIT), Vellore, Tamil Nadu, 632014, India.
⁵ Department of Plant Biology, Institute of Environmental Biology, Wrocław University of Environmental and Life Sciences, Kożuchowska 5b, 51-631, Wrocław, Poland. jaroslaw.prockow@upwr.edu.pl.
⁶ Department of Life Sciences, Presidency University, 86/1 College Street, Kolkata, -700073, West Bengal, India. abhijit.dbs@presiuniv.ac.in.

PMID: 36251044
PMCID: PMC9574835
DOI: 10.1007/s00210-022-02302-7

Review

Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight

Champa Keeya Tudu et al. Naunyn Schmiedebergs Arch Pharmacol. 2023 Feb.

. 2023 Feb;396(2):229-238.

doi: 10.1007/s00210-022-02302-7. Epub 2022 Oct 17.

Affiliations

¹ Department of Life Sciences, Presidency University, 86/1 College Street, Kolkata, -700073, West Bengal, India.
² Chemical and Biochemical Processing Division, ICAR-Central Institute for Research On Cotton Technology, Mumbai, 400019, Maharashtra, India.
³ School of Biological and Environmental Sciences, Shoolini University of Biotechnology and Management Sciences, Solan, 173229, Himachal Pradesh, India.
⁴ Department of Biomedical Sciences, School of Biosciences and Technology, Vellore Institute of Technology (VIT), Vellore, Tamil Nadu, 632014, India.
⁵ Department of Plant Biology, Institute of Environmental Biology, Wrocław University of Environmental and Life Sciences, Kożuchowska 5b, 51-631, Wrocław, Poland. jaroslaw.prockow@upwr.edu.pl.
⁶ Department of Life Sciences, Presidency University, 86/1 College Street, Kolkata, -700073, West Bengal, India. abhijit.dbs@presiuniv.ac.in.

PMID: 36251044
PMCID: PMC9574835
DOI: 10.1007/s00210-022-02302-7

Abstract

Cryptolepine (1,5-methyl-10H-indolo[3,2-b]quinoline), an indoloquinoline alkaloid, found in the roots of Cryptolepis sanguinolenta (Lindl.) Schltr (family: Periplocaceae), is associated with the suppression of cancer and protozoal infections. Cryptolepine also exhibits anti-bacterial, anti-fungal, anti-hyperglycemic, antidiabetic, anti-inflammatory, anti-hypotensive, antipyretic, and antimuscarinic properties. This review of the latest research data can be exploited to create a basis for the discovery of new cryptolepine-based drugs and their analogues in the near future. PubMed, Scopus, and Google Scholar databases were searched to select and collect data from the existing literature on cryptolepine and their pharmacological properties. Several in vitro studies have demonstrated the potential of cryptolepine A as an anticancer and antimalarial molecule, which is achieved through inhibiting DNA synthesis and topoisomerase II. This review summarizes the recent developments of cryptolepine pharmacological properties and functional mechanisms, providing information for future research on this natural product.

Keywords: Anti-inflammatory; Antimalarial; Antitumor; Cryptolepine; Cryptolepis sanguinolenta; Hepatoprotective; Pharmacology.

PubMed Disclaimer

Conflict of interest statement

The authors declare no competing interests.

Figures

**Fig. 1**
Chemical structure of 1 cryptolepine and 2 neocryptolepine/cryptotackieine

**Fig. 2**
Diagram with the relevant pharmacological properties of cryptolepine and its analogues, derivatives, and their potential mechanism of actions

See this image and copyright information in PMC

Cited by

Cryptolepine Analog Exhibits Antitumor Activity against Ehrlich Ascites Carcinoma Cells in Mice via Targeting Cell Growth, Oxidative Stress, and PTEN/Akt/mTOR Signaling Pathway.
El-Aarag B, Shalaan ES, Ahmed AAS, El Sayed IET, Ibrahim WM. El-Aarag B, et al. Anticancer Agents Med Chem. 2024;24(6):436-442. doi: 10.2174/0118715206274318231128072821. Anticancer Agents Med Chem. 2024. PMID: 38305388
The Emerging Role of Natural Products in Cancer Treatment.
Ghosh S, Das SK, Sinha K, Ghosh B, Sen K, Ghosh N, Sil PC. Ghosh S, et al. Arch Toxicol. 2024 Aug;98(8):2353-2391. doi: 10.1007/s00204-024-03786-3. Epub 2024 May 25. Arch Toxicol. 2024. PMID: 38795134 Review.
Cytotoxic leuconoxine-type diazaspiroindole alkaloids isolated from Cryptolepis dubia.
Ren Y, Kaweesa EN, Henkin JM, Sydara K, Xayvue M, Pandey P, Chittiboyina AG, Ali Z, Ferreira D, Soejarto DD, Burdette JE, Kinghorn AD. Ren Y, et al. Bioorg Med Chem Lett. 2024 Mar 15;101:129650. doi: 10.1016/j.bmcl.2024.129650. Epub 2024 Feb 9. Bioorg Med Chem Lett. 2024. PMID: 38341161
Investigating the Anti-inflammatory Effect of Quinoline Derivative: N1-(5-methyl-5H-indolo[2,3-b]quinolin-11-yl)benzene-1,4-diamine Hydrochloride Loaded Soluble Starch Nanoparticles Against Methotrexate-induced Inflammation in Experimental Model.
Medhat D, El-Bana MA, El-Tantawy El-Sayed I, Ahmed AAS, El-Naggar ME, Hussein J. Medhat D, et al. Biol Proced Online. 2024 Jun 3;26(1):16. doi: 10.1186/s12575-024-00240-7. Biol Proced Online. 2024. PMID: 38831428 Free PMC article.
One-Pot Synthesis of Polynuclear Indole Derivatives by Friedel-Crafts Alkylation of γ-Hydroxybutyrolactams.
Abaev VT, Aksenov NA, Aksenov DA, Aleksandrova EV, Akulova AS, Kurenkov IA, Leontiev AV, Aksenov AV. Abaev VT, et al. Molecules. 2023 Apr 2;28(7):3162. doi: 10.3390/molecules28073162. Molecules. 2023. PMID: 37049924 Free PMC article.

References

1. Wright CW, Addae-Kyereme J, Breen AG, Brown JE, Cox MF, Croft SL, Gökçek Y, Kendrick H, Phillips RM, Pollet PL. Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents. J Med Chem. 2001;44(19):3187–3194. doi: 10.1021/jm010929+. - DOI - PubMed
1. Zhu H, Gooderham NJ. Mechanisms of induction of cell cycle arrest and cell death by cryptolepine in human lung adenocarcinoma A549 cells. Toxicol Sci. 2006;91(1):132–139. doi: 10.1093/toxsci/kfj146. - DOI - PubMed
1. Abacha YZ, Forkuo AD, Gbedema SY, Mittal N, Ottilie S, Rocamora F, Winzeler EA, van Schalkwyk DA, Kelly JM, Taylor MC, Reader J (2022) Semi-synthetic analogues of cryptolepine as a potential source of sustainable drugs for the treatment of malaria, Human African Trypanosomiasis and Cancer - PMC - PubMed
1. Ameyaw EO, Koffuor GA, Asare KK, Konja D, Du-Bois A, Kyei S, Forkuo AD, Mensah RNAO. Cryptolepine, an indoloquinoline alkaloid, in the management of diabetes mellitus and its associated complications. J Intercult Ethnopharmacol. 2016;5(3):263. doi: 10.5455/jice.20160606124435. - DOI - PMC - PubMed
1. Ansha C, Mensah KB. A review of the anticancer potential of the antimalarial herbal Cryptolepis sanguinolenta and its major alkaloid cryptolepine. Ghana Med J. 2013;47(3):137–147. - PMC - PubMed

Publication types

Actions
Actions

MeSH terms

Actions
Actions
Actions
Actions
Actions
Actions
Actions

Substances

Actions
Actions
Actions
Actions
Actions

LinkOut - more resources

Full Text Sources

[1] Wright CW, Addae-Kyereme J, Breen AG, Brown JE, Cox MF, Croft SL, Gökçek Y, Kendrick H, Phillips RM, Pollet PL. Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents. J Med Chem. 2001;44(19):3187–3194. doi: 10.1021/jm010929+. - DOI - PubMed

[2] Wright CW, Addae-Kyereme J, Breen AG, Brown JE, Cox MF, Croft SL, Gökçek Y, Kendrick H, Phillips RM, Pollet PL. Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents. J Med Chem. 2001;44(19):3187–3194. doi: 10.1021/jm010929+. - DOI - PubMed

[3] Zhu H, Gooderham NJ. Mechanisms of induction of cell cycle arrest and cell death by cryptolepine in human lung adenocarcinoma A549 cells. Toxicol Sci. 2006;91(1):132–139. doi: 10.1093/toxsci/kfj146. - DOI - PubMed

[4] Zhu H, Gooderham NJ. Mechanisms of induction of cell cycle arrest and cell death by cryptolepine in human lung adenocarcinoma A549 cells. Toxicol Sci. 2006;91(1):132–139. doi: 10.1093/toxsci/kfj146. - DOI - PubMed

[5] Abacha YZ, Forkuo AD, Gbedema SY, Mittal N, Ottilie S, Rocamora F, Winzeler EA, van Schalkwyk DA, Kelly JM, Taylor MC, Reader J (2022) Semi-synthetic analogues of cryptolepine as a potential source of sustainable drugs for the treatment of malaria, Human African Trypanosomiasis and Cancer - PMC - PubMed

[6] Abacha YZ, Forkuo AD, Gbedema SY, Mittal N, Ottilie S, Rocamora F, Winzeler EA, van Schalkwyk DA, Kelly JM, Taylor MC, Reader J (2022) Semi-synthetic analogues of cryptolepine as a potential source of sustainable drugs for the treatment of malaria, Human African Trypanosomiasis and Cancer - PMC - PubMed

[7] Ameyaw EO, Koffuor GA, Asare KK, Konja D, Du-Bois A, Kyei S, Forkuo AD, Mensah RNAO. Cryptolepine, an indoloquinoline alkaloid, in the management of diabetes mellitus and its associated complications. J Intercult Ethnopharmacol. 2016;5(3):263. doi: 10.5455/jice.20160606124435. - DOI - PMC - PubMed

[8] Ameyaw EO, Koffuor GA, Asare KK, Konja D, Du-Bois A, Kyei S, Forkuo AD, Mensah RNAO. Cryptolepine, an indoloquinoline alkaloid, in the management of diabetes mellitus and its associated complications. J Intercult Ethnopharmacol. 2016;5(3):263. doi: 10.5455/jice.20160606124435. - DOI - PMC - PubMed

[9] Ansha C, Mensah KB. A review of the anticancer potential of the antimalarial herbal Cryptolepis sanguinolenta and its major alkaloid cryptolepine. Ghana Med J. 2013;47(3):137–147. - PMC - PubMed

[10] Ansha C, Mensah KB. A review of the anticancer potential of the antimalarial herbal Cryptolepis sanguinolenta and its major alkaloid cryptolepine. Ghana Med J. 2013;47(3):137–147. - PMC - PubMed

Save citation to file

Email citation

Add to Collections

Add to My Bibliography

Your saved search

Create a file for external citation management software

Your RSS Feed

Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight

Affiliations

Unravelling the pharmacological properties of cryptolepine and its derivatives: a mini-review insight

Authors

Affiliations

Abstract

Conflict of interest statement

Figures

Similar articles

Cited by

References

Publication types

MeSH terms

Substances

LinkOut - more resources

Full Text Sources

Abstract

Conflict of interest statement

Figures

Similar articles

Cited by

References

Publication types

MeSH terms

Substances

Related information

LinkOut - more resources

Full Text Sources