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review · RSC Advances

Incredible use of plant-derived bioactives as anticancer agents

202530 citationsOpen accessJimma University

In plain language

Plant-derived substances such as alkaloids, glycosides, terpenes, flavones, and polyphenols present significant potential as anticancer agents. These naturally occurring compounds act against cancer cells by causing DNA damage, activating apoptosis-inducing enzymes, arresting cell cycles, and reducing proliferation and angiogenesis. Specific bioactives target distinct molecular pathways across multiple cancer types. For instance, capsaicin, ouabain, and lycopene act via the STAT-3 pathway in conditions including breast, lung, and colorectal cancers. Epigallocatechin gallate and emodin target JNK proteins in skin, breast, and lung cancers, whereas berberine, evodiamine, lycorine, and astragalin operate through the PI3K/Akt and Ras/MAP-kinase pathways. A comprehensive assessment compiles the biological activities, molecular mechanisms, and clinical trials of 144 natural compounds and their synthetic analogues, providing a structured foundation for developing plant-derived cancer therapeutics.

Key takeaways

  • Plant-derived secondary metabolites suppress cancer cells through DNA damage, apoptosis activation, and cell cycle arrest.
  • Compounds such as capsaicin, ouabain, and lycopene exert anticancer effects across multiple tumour types via the STAT-3 signalling pathway.
  • Bioactives including berberine, evodiamine, and astragalin disrupt cancer progression through PI3K/Akt and Ras/MAP-kinase pathways.
  • The compiled evidence reviews the mechanisms, anticancer efficacy, and clinical trial status of 144 bioactive compounds and synthetic analogues.

Why it matters

Despite therapeutic advances, global cancer treatment still faces substantial limitations. Plant-derived compounds offer alternative mechanisms to target diverse cancers, ranging from leukaemia to breast and lung malignancies. Systematically charting how 144 natural molecules and their analogues affect key cellular pathways helps researchers identify viable drug candidates to address existing gaps in conventional cancer therapy.

Commercialisation angle

The findings are relevant to pharmaceutical developers and oncology researchers seeking early-stage leads and clinically evaluated candidates for drug discovery. By detailing 144 plant-derived bioactives and synthetic analogues alongside their clinical trial status, the evidence supports translational pipelines ranging from laboratory screening to clinical evaluation. However, the work represents a synthesis of existing trial and laboratory data rather than a newly tested commercial formulation.

AI-generated from the published abstract. Always read the original work before citing.

Abstract

Cancer is a major global concern. Despite considerable advancements in cancer therapy and control, there are still large gaps and requirements for development. In recent years, various naturally occurring anticancer drugs have been derived from natural resources, such as alkaloids, glycosides, terpenes, terpenoids, flavones, and polyphenols. Plant-derived substances exhibit their anticancer potential through antiproliferative activity, cytotoxicity, apoptosis, angiogenesis and cell cycle arrest. Natural compounds can affect the molecular activity of cells through various signaling pathways, like the cell cycle pathway, STAT-3 pathway, PI3K/Akt, and Ras/MAP-kinase pathways. Capsaicin, ouabain, and lycopene show their anticancer potential through the STAT-3 pathway in breast, colorectal, pancreatic, lung, cervical, ovarian and colon cancers. Epigallocatechin gallate and emodin target the JNK protein in skin, breast, and lung cancers, while berberine, evodiamine, lycorine, and astragalin exhibit anticancer activity against breast, liver, prostate, pancreatic and skin cancers and leukemia through the PI3K/Akt and Ras/MAP-kinase pathways. <i>In vitro</i>/<i>in vivo</i> investigations revealed that secondary metabolites suppress cancer cells by causing DNA damage and activating apoptosis-inducing enzymes. After a meticulous literature review, the anti-cancer potential, mode of action, and clinical trials of 144 bioactive compounds and their synthetic analogues are included in the present work, which could pave the way for using plant-derived bioactives as anticancer agents.

Research topics

  • Chemical synthesis and alkaloids
  • Phytochemistry and Bioactivity Studies
  • Phytochemistry and Biological Activities

Read the original research

This page summarises published work. The authoritative version sits with the publisher.

DOI: 10.1039/d4ra05089d

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