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The volatile constituents of Artemisia annua L. plants, grown in the field in The Netherlands from seeds of Chinese and Vietnamese origin, were investigated using GC and GC–MS (EI, NICI) analysis. The plants grown from Chinese seeds contained 4.0% (v/w) essential oil on a dry weight (DW) basis, those from Vietnamese seeds, 1.4% (v/w). More than forty compounds were identified. The principal component of the Chinese oil was artemisia ketone (63.9%); other major constituents included artemisia alcohol (7.5%), myrcene (5.1%), α‐guaiene (4.7%) and camphor (3.3%). In the Vietnamese oil the main components were camphor (21.8%) and germacrene‐D (18.3%); other important constituents were β‐caryophyllene (5.6%), trans‐β‐farnesene (3.8%) and 1,8‐cineole (3.1%). In the Vietnamese variety the terpenoid biosynthesis proceeded further towards sesquiterpenes, whereas in the Chinese predominantly monoterpenes were formed. This was also reflected in the artemisinin contents, found in dichloromethane extracts of the herbaceous plant material: 0.17% (DW) in Chinese and 1.00% (DW) in Vietnamese plants. We suggest that the differences in the essential oil composition may be ascribed to the existence of different A. annua chemotypes. In a dichloromethane extract of the roots several non‐volatile sesquiterpenes were found. The main constituent was a new compound, which was identified tentatively as arteannuic alcohol.
The volatile constituents of Artemisia annua L. plants, grown in the field in The Netherlands from seeds of Chinese and Vietnamese origin, were investigated using GC and GC–MS (EI, NICI) analysis. The plants grown from Chinese seeds contained 4.0% (v/w) essential oil on a dry weight (DW) basis, those from Vietnamese seeds, 1.4% (v/w). More than forty compounds were identified. The principal component of the Chinese oil was artemisia ketone (63.9%); other major constituents included artemisia alcohol (7.5%), myrcene (5.1%), α‐guaiene (4.7%) and camphor (3.3%). In the Vietnamese oil the main components were camphor (21.8%) and germacrene‐D (18.3%); other important constituents were β‐caryophyllene (5.6%), trans‐β‐farnesene (3.8%) and 1,8‐cineole (3.1%). In the Vietnamese variety the terpenoid biosynthesis proceeded further towards sesquiterpenes, whereas in the Chinese predominantly monoterpenes were formed. This was also reflected in the artemisinin contents, found in dichloromethane extracts of the herbaceous plant material: 0.17% (DW) in Chinese and 1.00% (DW) in Vietnamese plants. We suggest that the differences in the essential oil composition may be ascribed to the existence of different A. annua chemotypes. In a dichloromethane extract of the roots several non‐volatile sesquiterpenes were found. The main constituent was a new compound, which was identified tentatively as arteannuic alcohol.
Artemisia annua L. contains artemisinin, an endoperoxide sesquiterpene lactone, mainly in its leaves and inflorescences. This compound and a series of derivatives have attracted attention because of their potential value as antimalarial drugs. In this review a survey of the currently available literature data is given. It includes phytochemical aspects, such as constituents of A. annua, the artemisinin content during the development of the plant and its biosynthesis, isolation, analysis and stability. Total chemical synthesis of artemisinin is referred to, as well as structure-activity relationships of derivatives and simplified analogues. Pharmacological studies are summarized, including the mechanism of action, interaction of the antimalarial activity with other drugs, possible occurrence of resistance to artemisinin, clinical results, toxicological aspects, metabolism and pharmacokinetics. Finally, plant cell biotechnology is mentioned as a possible means to obtain plants and cell cultures with higher artemisinin contents, allowing an industrial production of pharmaceuticals containing this novel drug.
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