Artemisinin, a natural compound from Artemisia annua, is highly effective in treating drug-resistant malaria. Because chemical synthesis of this natural terpenoid is not economically feasible, its only source remains as the native plant which produces only small quantities of it, resulting in a supply that is far short of demand. Extensive efforts have been invested in metabolic engineering for the biosynthesis of artemisinin precursors in microbes. However, the production of artemisinin itself has only been achieved in plants. Since, A. annua possesses only poorly developed genetic resources for traditional breeders, molecular breeding is the best alternative. In this review, we describe the efforts taken to enhance artemisinin production in A. annua via transgenesis and advocate metabolic engineering of the complete functional artemisinin metabolic pathway in heterologous plants. In both cases, we emphasize the need to apply state-of-the-art synthetic biology approaches to ensure successful biosynthesis of the drug.

青蒿素是一种来自青蒿的天然化合物，在治疗耐药性疟疾方面非常有效。由于这种天然萜类化合物的化学合成在经济上不可行，它的唯一来源仍然是仅生产少量它的本地植物，导致供应远远供不应求。在微生物中青蒿素前体生物合成的代谢工程中投入了大量努力。然而，青蒿素本身的生产只能在植物中实现。由于青蒿对传统育种者的遗传资源开发不足，分子育种是最好的选择。在这次审查中，我们描述所作的努力，以提高青蒿素生产的青蒿通过转基因并提倡对异源植物中完整的功能性青蒿素代谢途径进行代谢工程。在这两种情况下，我们都强调需要应用最先进的合成生物学方法来确保药物的成功生物合成。