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Artemisinin (qinghaosu), a sesquiterpenoid lactone peroxide constituent of annual wormwood (Artemisia annuaL. # ARTAN) that is used as an antimalarial drug, was tested for phytotoxic properties. It inhibited germination of lettuce (Lactuca sativaL.) and annual wormwood, and growth of roots and shoots of lettuce, redroot pigweed (Amaranthus retroflexusL. # AMARE), pitted morningglory (Ipomoea lacunosaL. # IPOLA), annual wormwood, and common purslane (Portulaca oleraceaL. # POROL) was inhibited at 33 μM. No effects of 33 μM artemisinin were detected on growth of velvetleaf (Abutilon theophrastiMedik. # ABUTH) and grain sorghum [Sorghum bicolor(L.) Moench.]. Chlorophyll content was not affected in lettuce, and chlorosis was not observed in any species tested. The probable biosynthetic precursors of artemisinin, arteannuin B and qinghao acid, had no effect on growth or chlorophyll content of lettuce; however, they inhibited lettuce seed germination. Artemisinin and cinmethylin {exo-1-methyl-4-(1-methylethyl)-2-[(2-methylphenyl)methoxy]-7-oxabicyclo [2.2.1] heptane} were equally effective in reducing growth of lettuce; however, cinmethylin had no effect on germination. Respiration of lettuce roots or cotyledons was not inhibited by artemisinin. Artemisinin only marginally increased the mitotic index of lettuce root tips at 33 μM. At the ultrastructural level, however, chromosomes were less condensed during mitosis in artemisinin-treated than control meristematic cells. The growth-inhibiting ability of artemisinin could not be reduced by feeding the plants with hydrolyzed protein or treatment with putrescine. Artemisinin is a selective phytotoxin that reduces growth by a mechanism other than mitotic disruption or inhibition of protein synthesis.

Microbial metabolism of the sesquiterpene lactone antimalarial drug artemisinin [1] was studied. Screening studies have shown a number of microorganisms capable of metabolizing artemisinin [1]. Scale-up fermentation with Nocardia corallina (ATCC 19070) and Penicillium chrysogenum (ATCC 9480) have resulted in the production of two major microbial metabolites that have been characterized with the use of 2D-nmr techniques. These metabolites have been identified as deoxyartemisinin [2] and 3 alpha-hydroxydeoxyartemisinin [3].

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