Natural Product-Based Cancer Therapeutics
Summary
Natural products have long served as a cornerstone of cancer drug discovery, offering structurally diverse compounds that act on a spectrum of malignant processes. Plant-derived agents such as taxanes and vinca alkaloids pioneered microtubule-targeted chemotherapy, while microbial metabolites and marine-sourced molecules have expanded therapeutic modalities to include DNA-intercalators, epigenetic regulators and signal-pathway modulators. Advances in high-throughput screening, multiomics profiling and synthetic biology have accelerated the elucidation of active scaffolds, enabled the generation of tailored analogues and supported sustainable supply through microbial fermentation or semi-synthesis. Chemical optimisation has yielded second-generation derivatives with improved solubility, potency and selectivity, while combination regimens seek to overcome resistance and enhance tolerability. Global efforts now address biodiversity access, scalable production and equitable benefit sharing, underscoring the strategic importance of natural product pipelines in meeting unmet needs across diverse tumour types.
Research from Nature Portfolio
Recent studies have highlighted the vast potential of deep-sea ecosystems as reservoirs of chemically novel anticancer leads. A comprehensive analysis of marine gene patents revealed thousands of protein-coding sequences linked to bioactive scaffolds, with deep-sea microbes emerging as prolific sources for therapeutic discovery and patent applications. This work underscores the importance of maritime bioprospecting for enriching anticancer libraries and guiding sustainable exploitation of ocean biodiversity. In parallel, a synthetic withanolide analogue named orpinolide has been shown to exert potent antileukaemic effects by targeting oxysterol-binding protein (OSBP). Multiomic and CRISPR–Cas9 screens demonstrated that orpinolide disrupts Golgi–endoplasmic reticulum lipid exchange, triggering Golgi collapse and apoptotic programmes. These findings reaffirm sterol transport as an actionable metabolic dependency in leukaemia and illustrate how natural product mimetics can reveal new therapeutic vulnerabilities.
Natural Product-Based Cancer Therapeutics publication trend
The graph below shows the total number of articles in natural product-based cancer therapeutics across all publications each year (not limited to Nature Index journals).
Technical terms
Natural product: A bioactive compound produced by living organisms, often serving as a lead for drug development.
Phytochemical: A plant-derived secondary metabolite with potential therapeutic activity.
Withanolide: A class of steroidal lactones, typically isolated from Solanaceae species, with diverse bioactivities.
Oxysterol-binding protein (OSBP): A lipid-transfer protein that regulates cholesterol and phosphoinositide transport between cellular membranes.
Marine bioprospecting: The systematic exploration of marine biodiversity to discover novel compounds for therapeutic or industrial use.
References
- Growing prominence of deep-sea life in marine bioprospecting. Nature Sustainability (2024).
- Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting OSBP. Nature Chemical Biology (2024).
- Phytochemicals in Cancer Treatment: From Preclinical Studies to Clinical Practice. Frontiers in Pharmacology (2020).
- Plant Secondary Metabolites as Anticancer Agents: Successes in Clinical Trials and Therapeutic Application. International Journal of Molecular Sciences (2018).
- Marine Natural Products: A Source of Novel Anticancer Drugs. Marine Drugs (2019).
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