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Natural products are highly useful as sources of drugs and as tools for fundamental biomedical research. Phytomedicines based on medicinal plants and herbal extracts are used worldwide. Using three examples from our lab, we have shown different approaches to explore the biological and pharmacological properties of herbal extracts and new natural product leads. Our emphasis has been on global effects and multiple rather than single targets, whereby cell- and mechanism-based in vitro assays, in vivo pharmacology, cell biology and transcriptional profiling were employed.