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RESEARCH PRODUCT

Novel Developments on Artemisinin and Its Derivatives for Cancer Therapy

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The lack of effective long-term anticancer therapy highlights the necessity to identify new potent anticancer compounds. Many biocompounds of naturally occurring medicinal plants have pharmacological activities and, thus, represent a source of molecules that may have anti-proliferative effects on a variety of cancers. During the past 10 years, we have systematically analyzed medicinal plants used in traditional Chinese medicine and focused our interest on Artemisia annua (sweet wormwood herb). The active principle of sweet wormwood herb is Artemisinin, a sesquiterpene, which exerts not only anti-malarial activity but also profound cytotoxicity against tumour cells. The anti-tumour mechanism shares similarities to the anti-malarial mechanism: the Artemisinin molecule contains an endoperoxide bridge that reacts with an iron atom to form free radicals causing macromolecular damage and cell death. The anticancer activity of artesunate, a semi-synthetic derivative of Artemisinin, has also been shown in human xenograft tumours in mice and dogs. First encouraging experience in the clinical treatment of patients suffering from laryngeal carcinoma, uveal melanoma, pituitary macroadenoma and non-small cell lung cancer calls for comprehensive clinical trials with artesunate for cancer treatment in the near future. In this chapter, we summarize novel developments on Artemisinin and its derivatives concerning mode of action, metabolism, toxicity, in vivo effects, clinical application and biotechnological production methods.