Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin, has recently shown antitumor activity in various cancer cells including cancers of cervix, pancreas, prostate, liver and neuroblastoma. Numerous studies in vivo and in vitro indicate that DHA possesses unique antitumor features and appears to be a promising chemotherapeutic agents. Here we systematically review the advances in research of anticancer of dihydroartemisinin, as well as summarize the mechanisms of its inducing apoptosis,delay cell-cycle, inhibitory cell proliferation and downregulate angiogenesis.
Animals ; Antineoplastic Agents ; pharmacology ; Artemisinins ; pharmacology ; Humans

Artemisinins ; pharmacology ; Drug Discovery ; Humans ; Nobel Prize

Antimalarials ; pharmacology ; Artemisinins ; pharmacology ; Humans ; Medicine, Chinese Traditional

To study the growth effects of differing concentrations of artemisinin on green algae and to evaluate the ecological risk. The effects of artemisinin on the growth and the content change of chlorophyll, protein, oxygen, conductivity, SOD, CAT, MDA in Chlorella pyrenoidosa and Scenedesmus oblique were studied through 96 h toxicity tests. Artemisinin accelerated the growth of algae at a lower concentration ( <40 microg . L-1) with content increase of chlorophyll or protein and so on, and it inhibited the growth of algae at higher concentration ( >80 microg . L-1). The content of chlorophyll or protein in algae cells reduced with the increasing concentration of artemisinin, exhibiting the good concentration-effect relationship. SOD and CAT activity was stimulated at low concentrations ( <40 microg . L-1 ) and inhibited at high concentrations ( >80 microg . L- 1). However, MDA content increased significantly with the increase of concentration. According to the seven kinds of indicators changes, the time-response and dose-response suggested that the surfactant first hurt in Ch. pyrenoidosa was damaging membrane by changing membrane lipid molecules soluble. And primary mechanism on Chlorophyta cells might be related to the oxidation damage of lipid and other biological large molecules caused by artemisinin. The large-scale intensive planting of Artemisia annua may reduce the surrounding water productivity.
Artemisinins ; pharmacology ; Chlorophyll ; metabolism ; Chlorophyta ; drug effects ; metabolism

Microbial transformation is an efficient enzymatic approach for the structural modification of exogenous compounds to obtain derivatives. Compared with traditional chemical synthesis, the microbial transformation has in fact the undoubtable advantages of strong region-and stereo-selectivity, and a low environmental and economic impact on the production process, which can achieve the reactions challenging to chemical synthesis. Because microbes are equipped with a broad-spectrum of enzymes and therefore can metabolize various substrates, they are not only a significant route for obtaining novel active derivatives, but also an effective tool for mimicking mammal metabolism in vitro. Artemisinin, a sesquiterpene with a peroxy-bridged structure serving as the main active functional group, is a famous antimalarial agent discovered from Artemisia annua L. Some sesquiterpenoids, such as dihydroartemisinin, artemether, and arteether, have been developed on the basis of artemisinin, which have been successfully marketed and become the first-line antimalarial drugs recommended by WHO. As revealed by pharmacological studies, artemisinin and its derivatives have exhibited extensive biological activities, including antimalarial, antitumor, antiviral, anti-inflammatory, and immunomodulatory. As an efficient approach for structural modification, microbial transformation of artemisinin and its derivatives is an increasingly popular strategy that attracts considerable attention recently, and numerous novel derivatives have been discovered. Herein, this paper reviewed the microbial transformation of artemisinin and its artemisinin, including microbial strains, culture conditions, product isolation and yield, and biological activities, and summarized the advances in microbial transformation in obtaining active derivatives of artemisinin and the simulation of in vivo metabolism of drugs.
Animals ; Antimalarials/pharmacology* ; Antiviral Agents ; Artemether ; Artemisinins ; Mammals

Artemisinin was isolated from traditional Chinese herb Artemisia annua for treating malaria. A series of derivatives,like dihydroartemisinin,artesunate,artemether,artether,had the same core chemical structure,and sesquiterpene lactone containing peroxide bridge constitute the basic chemical structure. Besides anti-malaria,artemisinin family drugs were found to ameliorate many different diseases,which have attracted wide attention in recent years. Among different diseases,artemisinin family drugs were found to have T lymphocytes immunomodulation effects,including activation,proliferation,differentiation,apoptosis and subsets function. Because T cell immunologic response is the key point of many diseases,and impact the pathogenic process,therapeutic effect and prognosis,the drug studies with it as the target have become hotspots in recent years. Studies of artemisinin family drug on T cell immunomodulation were still at the initial stage and involved in different disease; furthermore,T cell immune process involves complicated molecular mechanism,it is imperative to summarize the advance of current studies for further systematic explanation and exploration of their characteristics and mechanisms. This article will summarize the research progress of artemisinin family drugs for malaria,autoimmune disease,hypersensitivity reaction,tumor,schistosomiasis and AIDS relating to T cell immune modulation,so as to provide basic and professional reference for related research and application.
Antimalarials ; Artemisia annua ; Artemisinins/pharmacology* ; Immunomodulation ; T-Lymphocytes

OBJECTIVEIn order to enhance the yield of artemisinin, makes out the Artemisia annua adaptive area regional assignment in Guangxi. To ensure the nicety in study, on the base of literature study and experience on the spot, the article inspect the division result.

METHODBy document analysis and colleted data of A. annua, make out sample collect proceed and inspect the result of artemisinin content rank distribution in Guangxi.

RESULT AND CONCLUSIONResult of A. annua regional assignment is checked out in the article, the result passes the check by AQL (32, 4). The conclusions insure subsequence study and the A. annua sample collect. The result of artemisinin content rank distribution in Guangxi can be used in artemisinin production.

Antimalarials ; analysis ; pharmacology ; Artemisia annua ; chemistry ; Artemisinins ; analysis ; pharmacology ; China ; Plant Extracts ; analysis ; pharmacology

OBJECTIVETo explore the effects of micro-elements fertilizers on the quality and yields of Artemisia annua.

METHODField experiments were conducted according to the method of random blocks design. After the harvest the yield was calculated and the content of artemisinin was determined.

RESULTBy applying 0.1%-0.5% Mn and 0.1%-0.5% Zn the dried leaf output and artemisinin content were increased.

CONCLUSIONThe suitable ranges of Mn and Zn can increased the yield and artemisinin content of A. annua.

Artemisia annua ; drug effects ; metabolism ; Artemisinins ; metabolism ; Boron ; pharmacology ; Manganese ; pharmacology ; Zinc ; pharmacology

Artemisinin is a key anti-malarial drug and few clinically meaningful resistant cases about its application have so far been reported. The World Health Organization (WHO) officially recommended the use of ACT (Artemisinin-based Combination Therapy) as the first line antimalarial application to increase its inhibitory efficacy and prevent the likely resistance development. Based on our current understanding of artemisinin, a set of compounds were selected to study their interaction with artemisinin by using the yeast (S. cerevisiae) model, in the hope that knowledge gained might provide some references for clinical investigations. In this research, yeast strain (BY4742) was cultured in the nonfermentable YPGE solid medium with 4 μmol · L(-1) artemisinin and one of the selected compounds for 48 hours, and the combined drug efficiency was evaluated by the inhibition of yeast growth. The compounds belong to the categories of oxygenants, antioxidants, metal ions, ion chelators and uncouplers. Among them, 0.2 mmol L(-1) FeCl3, 60 μmol · L(-1) BPS, 1 mmol · L(-1) CuCl2, 0.75 mmol · L(-1) VE and 1 mmol · L(-1) VC antagonized the action of artemisinin, while 40 μmol · L(-1) DNP, 0.1 μmol · L(-1) CCCP and 0.25 mmol · L(-1) H2O2 had synergistic effects. These results suggested that redox-active and mitochondria-dysfunctional compounds could affect artemisinin's potency, supporting our prior proposed mitochondrial model for artemisinin's action. This research in addition provided a convenient method to screen likely artemisinin-interacting compounds.
Artemisinins ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Saccharomyces cerevisiae ; drug effects ; growth & development

Animals ; Artemisinins ; pharmacology ; Cricetinae ; Leishmania donovani ; drug effects ; Male ; Mesocricetus ; Sesquiterpenes ; pharmacology