Abstract
High-performance liquid chromatography, liquid chromatography–mass spectrometry, and gas chromatography–mass spectrometry methods were developed to analyze the process waste streams of Artemisia Annua extraction. Results from these methods suggested that the final waste from the extraction process could serve as a source of dihydroartemisinic acid (DHAA) that could be converted to additional artemisinin. Two additional impurities were isolated and identified in the waste material as well as in A. annua leaf samples. That these impurities also appear as side-products in chemical transformations of DHAA to artemisinin supports the conclusion that the in vivo transformation proceeds as nonspecific oxidations. These impurities do not appear in isolated artemisinin. A simple, high-yielding procedure for recovery of DHAA from the primary waste stream was developed.
Highlights
Artemisinin is a natural product that serves as the starting material for antimalarial active pharmaceutical ingredients in artemisinin combination therapy treatments
In the semisynthetic approach (Scheme 1), AA produced by Scheme 1 fermentation is reduced selectively to dihydroartemisinic acid (2) (DHAA), which is converted to artemisinin via a chemical conversion which mimics the synthetic pathway used by the plant.[3]
Using higher performance liquid chromatography (HPLC), it was found that leaves from three different batches contained artemisinin between 1.0 and 1.4 wt %, together with 0.24 to 0.36 wt % of DHAA and 0.04 to 0.09 wt % of AA
Summary
Artemisinin is a natural product that serves as the starting material for antimalarial active pharmaceutical ingredients in artemisinin combination therapy treatments. Its supply and price may be subject to disruptive price fluctuations In response to these concerns about the impact of price fluctuations on efforts to treat and even eradicate malaria, the Bill and Melinda Gates Foundation funded a cooperative effort to develop an alternate source of artemisinin. The results of the research toward semisynthetic artemisinin (SSA) represent a technical tour de force encompassing development of fermentation processes[1] to produce artemisinic acid (AA, 1) and a chemical conversion to artemisinin developed by Sanofi[2] (3). This means that DHAA needs to be at most $75/kg Because this does not seem to be possible from current fermentation routes, alternative sources should be explored
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