Bioinfo Chem

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Harmine: A Natural β-Carboline with Promising Multi-Targeted Anticancer Potential

Noshin Tasnim Yana1, Md. Nasimul Haque Shipon1, Md Emran Hossain2, Md. Sakib Al Hasan1*, Md. Tahmidur Rahman1, Emon Mia1

+ Author Affiliations

Bioinfo Chem 7 (1) 1-8 https://doi.org/10.25163/bioinformatics.7110455

Submitted: 22 October 2025 Revised: 22 December 2025  Accepted: 27 December 2025  Published: 29 December 2025 


Abstract

Cancer remains a major global health challenge, driving an urgent search for safer and more effective therapeutics from natural sources. Harmine (HRM), a β-carboline alkaloid found predominantly in Peganum harmala and Banisteriopsis caapi, has long been valued in traditional medicine for its diverse pharmacological properties. This study systematically reviewed preclinical and computational evidence to evaluate HRM’s anticancer potential, safety, and pharmacological suitability. Data were collected from PubMed, ScienceDirect, Springer, and Web of Science databases up to February 2025, focusing on in vitro and in vivo studies of HRM’s effects on various cancer types. Additionally, SwissADME and ProTox-II were used to assess drug-likeness and toxicity profiles. Results revealed that HRM inhibits cancer cell proliferation, migration, and invasion while inducing apoptosis, autophagy, and cell cycle arrest across a broad spectrum of cancers—including breast, colon, gastric, liver, lung, thyroid, and skin malignancies. Mechanistically, HRM activates caspase-3/-9 and PARP cleavage, upregulates pro-apoptotic proteins (Bax, p53), and downregulates oncogenic regulators (cyclin D1, p-Akt, and Bcl-2). In silico analyses indicated favorable physicochemical and pharmacokinetic characteristics, with compliance to all major drug-likeness rules and moderate oral bioavailability. Toxicological predictions suggested manageable safety risks, though potential hepatotoxicity and MAO-A inhibition warrant cautious evaluation. In conclusion, harmine demonstrates potent, multi-targeted anticancer properties with strong preclinical evidence supporting its advancement as a natural therapeutic lead. Further pharmacokinetic optimization and clinical validation are essential to confirm its safety and efficacy in humans.

Keywords: Harmine, Anticancer activity, Apoptosis, Cytotoxicity, Natural product

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