The American Journal of Tropical Medicine and Hygiene
Artemisia annua L. (annual wormwood) contains the antimalarial artemisinin. Aqueous preparations of the dried herb are included in the pharmacopoeia of the People's Republic of China for treatment of fever and malaria. Fourteen healthy male volunteers received one liter of tea prepared from nine grams of Artemisia annua leaves. Blood samples were taken and artemisinin was detected by reversed phase high-performance liquid chromatography.
Artemisinin, a sesquiterpene lactone endoperoxide derived from the plant Artemisia annua, forms the basis of the most important treatments of malaria in use today. In an effort to elucidate the biosynthesis of artemisinin, an expressed sequence tag approach to identifying the relevant biosynthetic genes was undertaken using isolated glandular trichomes as a source of mRNA.
INTRODUCTION: This paper reviews recent trends in the production, supply and price of the active ingredients as well as finished ACT products. Production and cost data provided in this paper are based on an ongoing project (Artepal). Stability data are derived from a development project on rectal artesunate. DISCUSSION: The artemisinin raw material and its derivatives appear to be very stable compared to the finished products.
Artemisinin (an antimalaric compound) is isolated as the active compound of the medicinal plant Artemisia annua L. A simple, rapid, and high-efficient method of extraction is developed, in which it is extracted by matrix solid-phase dispersion (MSPD) and directly analyzed by post-column derivatization high-performance liquid chromatography (HPLC). The quantitation results from the MSPD method are compared with two conventional liquid solvent extraction processes, Soxhlet and ultrasonic wave by F-test, and the result indicates no significant difference.
At some point during biosynthesis of the antimalarial artemisinin in glandular trichomes of Artemisia annua, the Delta11(13) double bond originating in amorpha-4,11-diene is reduced. This is thought to occur in artemisinic aldehyde, but other intermediates have been suggested. In an effort to understand double bond reduction in artemisinin biosynthesis, extracts of A. annua flower buds were investigated and found to contain artemisinic aldehyde Delta11(13) double bond reductase activity.
BACKGROUND: Due to the global occurrence of multi-drug-resistant malarial parasites (Plasmodium falciparum), the anti-malarial drug most effective against malaria is artemisinin, a natural product (sesquiterpene lactone endoperoxide) extracted from sweet wormwood (Artemisia annua). However, artemisinin is in short supply and unaffordable to most malaria patients. Artemisinin can be semi-synthesized from its precursor artemisinic acid, which can be synthesized from simple sugars using microorganisms genetically engineered with genes from A. annua.
Artemisinin the sesquiterpene endoperoxide lactone extracted from the herb Artemisia annua, remains the basis for the current preferred treatment against the malaria parasite Plasmodium falciparum. In addition, artemisinin and its derivatives show additional anti-parasite, anti-cancer, and anti-viral properties. Widespread use of this valuable secondary metabolite has been hampered by low production in vivo and high cost of chemical synthesis in vitro. Novel production methods are required to accommodate the ever-growing need for this important drug.
BACKGROUND AND AIMS: The resurgence of malaria, particularly in the developing world, is considerable and exacerbated by the development of single-gene multi-drug resistances to chemicals such as chloroquinone. Drug therapies, as recommended by the World Health Organization, now include the use of antimalarial compounds derived from Artemisia annua--in particular, the use of artemisinin-based ingredients. Despite our limited knowledge of its mode of action or biosynthesis there is a need to secure a supply and enhance yields of artemisinin.
BACKGROUND: Glandular trichomes produce a wide variety of commercially important secondary metabolites in many plant species. The most prominent anti-malarial drug artemisinin, a sesquiterpene lactone, is produced in glandular trichomes of Artemisia annua. However, only limited genomic information is currently available in this non-model plant species. RESULTS: We present a global characterization of A. annua glandular trichome transcriptome using 454 pyrosequencing.
The antimalarial sesquiterpene, artemisinin, is in short supply; demand is not being met, and the role of artemisinin in the plant is not well established. Prior work showed that addition of dimethyl sulfoxide (DMSO) to seedlings increased artemisinin in their shoots and this study further investigated that serendipitous observation. When in vitro-cultured Artemisia annua rooted shoots were fed different amounts of DMSO (0-2.0% v/v), artemisinin levels doubled and showed biphasic optima at 0.25 and 2.0% DMSO.