Drug intelligence / Profile preview

cryptolepine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral (experimental, Animal Studies)[1][3], Intraperitoneal (animal Studies)[4], Not Approved For Human Administration
01

Overview

Cryptolepine is a natural indoloquinoline alkaloid found predominantly in the roots of Cryptolepis sanguinolenta and other plants[1][2]. It exhibits a wide range of pharmacological activities, including antimalarial, anticancer, anti-inflammatory, antidiabetic, antiprotozoal, antibacterial, antifungal, anti-hyperglycemic, antipyretic, antimuscarinic, and acetylcholinesterase/butyrylcholinesterase inhibitory effects[1][2][3][4][6][7]. Cryptolepine operates via multiple mechanisms: it intercalates into DNA (particularly between cytosine-guanine base pairs), inhibits topoisomerase II, suppresses DNA synthesis[1][3][8], and blocks key oncogenic and inflammatory pathways such as p53, STAT3, and PI3K/Akt[3]. It has promising activity against malaria, several protozoal and bacterial infections, as well as a variety of cancers, including breast cancer[3][6]. Additionally, it functions as a multi-target cholinesterase inhibitor, relevant for neurodegenerative diseases such as Alzheimer’s disease[1].

Other names
cryptolepine5-methylindolo[3,2-b]quinoline5H-Quindoline, 5-methyl-CCRIS 9019CCRIS9019CCRIS-9019
02

Targets

AcetylcholinesteraseButyrylcholinesteraseDNATOP2A (DNA topoisomerase II)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)STAT3 (Signal Transducer and Activator of Transcription 3)

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