Description:
<jats:title>Abstract</jats:title>
<jats:p>More than a decade ago, we initiated a research program on the molecular pharmacology of phytochemicals derived from Chinese medicinal herbs. Bioactive plant extracts have been fractionated by chromatographic techniques. We isolated bioactive compounds and elucidated their chemical structures by nuclear magnetic resonance and mass spectrometry. A promising compounds was artemisinin from Artemisia annua L. and its semisynthetic compound artesunate. Artemisinin and artesunate are anti-malarial drugs. Our data indicated profound activity against cancer cells, but also against various viruses, Schistosoma, Trypanosoma, and even plant crown gall tumors. To elucidate the molecular mode of actions against cancer, we applied molecular biological and pharmacogenomic approaches in vitro and in vivo. Different signaling pathways were identified not only in cancer cells but also in cells infected with viruses, e.g. HCMV, HSV1 and others. To translate the experimental results in cell lines and animals to the bedside, we report on the compassionate use of artesunate in single cancer patients as well as on our efforts to initiate several clinical phase I/II trials in veterinary tumors as well as in human cervix or colorectal carcinoma. These pilot studies indeed indicate that artesunate is not only useful as antimalarial drug, but also exerts activity against cancer and viral diseases. Clinical results will also be presented that not only artesunate as semisynthetic chemical derivative of artemisinin, but also herbal extracts from Artemisia annua are active in veterinary and human tumor patients. Artesunate represents an illustrative example for the therapeutic potential of medicinal herbs and drugs derived from traditional Chinese medicine.References 1. Efferth et al.: Journal of Molecular Medicine 2002;80:233-42. 2. Efferth: Drug Resistance Updates 2005;8:85-97. 3. Efferth et al.: Molecular Cancer Therapeutics 2008;7:152-61. 4. Li et al.: Cancer Research 2008;68:4347-51. 5. Shapira et al.: Clinical Infectious Diseases 2008;46:1455-7. 6. Efferth et al.: Clinical Infectious Diseases 2008;47:804-11. 7. Krishna et al.: Ebiomedicine 2014;2:82-90. 8. Saeed et al.: Pharmacological Research 2016;110:216-226.</jats:p>
<jats:p>Citation Format: Thomas A. Efferth. Beyond malaria: Second career of artesunate as cancer drug [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5109. doi:10.1158/1538-7445.AM2017-5109</jats:p>