This study is to investigate the effect of artesunate on transforming growth factor-beta1 (TGF-beta1) induced epithelial-mesenchymal transition (EMT) and its possible mechanism. After the in vitro cultured RLE-6TN cells were treated with TGF-beta1 then artesunate intervened on it, after 24 h, expression of the markers of mesenchymal cell was assayed using Western blotting and real-time PCR analysis. Western blotting was also used to detect the effect of TGF-beta1 on the Smad3 and Smad7 expressions of RLE-6TN cells. Morphological alterations were examined by phase-contrast microscope, and ultrastructure changes by electron microscope. Incubation of RLE-6TN cells with TGF-beta1 resulted in the up-regulation of the expression of the mesenchymal cell markers, after artesunate intervened on it, resulted in the down-regulation of the expression. Meanwhile, incubation with artesunate intervened on RLE-6TN cells could lead to the apparent down-regulation of the expression of Smad3 and up-regulation of Samd7 and the transition of RLE-6TN cells to mesenchymal-like by TGF-beta1 induction, after artesunate intervened on it, RLE-6TN cells to epithelial-like. TGF-beta1 induced epithelial-mesenchymal transition process; artesunate can inhibit TGF-beta1-induced epithelial-mesenchymal transition process, the possible mechanism is up-regulation of the expression of Smad7 and down-regulation of the expression of Smad3, meanwhile inhibits phosphorylation of Smad3.
Actins ; genetics ; metabolism ; Animals ; Artemisia ; chemistry ; Artemisinins ; isolation & purification ; pharmacology ; Cell Line ; Cell Proliferation ; drug effects ; Epithelial Cells ; cytology ; metabolism ; Epithelial-Mesenchymal Transition ; drug effects ; Idiopathic Pulmonary Fibrosis ; pathology ; Plants, Medicinal ; chemistry ; Pulmonary Alveoli ; cytology ; RNA, Messenger ; metabolism ; Rats ; Smad3 Protein ; genetics ; metabolism ; Smad7 Protein ; genetics ; metabolism ; Transforming Growth Factor beta1 ; pharmacology ; Vimentin ; genetics ; metabolism

Dihydroartemisinin is an important derivative of artemisinin. We used dihydroartemisinin as the starting material, through esterification, amination and acylation, a series of novel piperazine-sulfonamide contained dihydroartemisinin derivatives were firstly synthesized and their chemical structures were confirmed by IR, 1H NMR, 13C NMR and HR-MS. X-diffraction was used to determine the final configuration of the compound 3c. And the in vitro anti-HeLa activities of compounds 3 were analyzed with CCK-8 method. The preliminary bioassay test shows that compound 3 showed the best inhibition activities against HeLa with IC50 values of 0.14 micromol x L(-1).
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Artemisinins ; chemical synthesis ; chemistry ; pharmacology ; Cell Proliferation ; drug effects ; HeLa Cells ; Humans ; Inhibitory Concentration 50 ; Molecular Structure ; Piperazines ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship ; Sulfonamides ; chemistry

This study is to elucidate the immunoregulation mechanisms of artesunate (AST) on allergic contact dermatitis (ACD). Pharmacodynamics analyses, HE staining, semi-quantitative RT-PCR and Western blotting were used to explore the effects of AST on the related cytokines, transcription factor and signaling molecule of ACD respectively. The results indicated that topical administration of AST not only reduced the increase of ear swelling, spleen index and inflammatory cells infiltration in ACD mice, but also inhibited remarkably the expression of IFN-gamma, T-bet and NF-kappaB p65. It's suggested that AST could exhibit suppressive effects on inflammatory response and immune function of ACD, which indicates the possibility of developing AST as a novel immunoregulatory agent in the treatment of ACD and other immune-related diseases.
Administration, Topical ; Animals ; Artemisinins ; administration & dosage ; chemistry ; pharmacology ; Dermatitis, Allergic Contact ; immunology ; metabolism ; pathology ; Ear ; pathology ; Female ; GATA3 Transcription Factor ; genetics ; metabolism ; Hypersensitivity, Delayed ; drug therapy ; Immunosuppressive Agents ; administration & dosage ; chemistry ; pharmacology ; Interferon-gamma ; genetics ; metabolism ; Interleukin-4 ; genetics ; metabolism ; Mice ; Mice, Inbred ICR ; Molecular Structure ; NF-kappa B ; metabolism ; RNA, Messenger ; metabolism ; T-Box Domain Proteins ; genetics ; metabolism

The clinical or experimental study proves that Chinese medicine such as Tripteryglum wilfordii, Lignum Sappan, Caulis Sinomenii, Radix Trichosanthis and Herba Artemisiae Annuae have good immunosuppressive activity. Further researches on the immunosuppressive active components from Chinese medicine have been the main direction in recent years. The recent researches on immunosuppressive effect and possible mechanisms for the monomers such as triperine, triptolide, bazilein, potosappanin A, sinomenine, trichosanthin and artemisinin extracted from those Chinese medicine are introduced in this review.
Animals ; Artemisinins ; pharmacology ; therapeutic use ; Diterpenes ; pharmacology ; therapeutic use ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Epoxy Compounds ; pharmacology ; therapeutic use ; Humans ; Immunosuppressive Agents ; pharmacology ; therapeutic use ; Morphinans ; pharmacology ; therapeutic use ; Phenanthrenes ; pharmacology ; therapeutic use ; Plants, Medicinal ; chemistry ; Trichosanthin ; pharmacology ; therapeutic use

OBJECTIVETo breed and spread a new cultivar of Artemisia annua.

METHODThe excellent germplasm resources of A. annua in the main production area of Artemisia were collected, and the improved germplasm were screened, the content of artemisinin was determined, and yield per plant was measured. The systematically maternal line and seed production techniques of mass selection were applied combined with the variety test, variety regional test trials and production trials for breeding and spreading the new cultivars of artemisia.

RESULTThe popularization and experiment illustrated the production of the new species reached 3 000 kg x hm(-2), compared with wild A. annua it increased 10% -14%. The content of artemisinin reached more than 1%, increased more than 0.2%.

CONCLUSIONIt is proved that the systematically maternal line and seed production techniques of mass selection can significantly improve the quality of A. annua and it is an acceptable way to cultivate new variety. By production verification, it is practicable and high technical and economic benefits to popularize the new cultivar "Yu-Qing No. 1" of A. annua.

Antimalarials ; analysis ; pharmacology ; Artemisia annua ; chemistry ; genetics ; growth & development ; Artemisinins ; analysis ; pharmacology ; Breeding ; methods

To investigate the antitumor mechanism of artemisninin, a flexible docking analysis was used to score all kinds of functions of 11 Qinghaosu derivatives and transferrin with different resolutions. The distances of Asp-63, Tyr-188, His-249, Arg-124 and Lys-296 with Qinghaosu were less than 0.5 nm, separately. Meanwhile, the higher is the activity of Qinghaosu derivatives the higher is the score. Our model explains that Fe2+ is more feasible to react with Qinghaosu, and not involved in other metabolism in presence of transferrin. Docking results unveil that Iron(II)-transferrin increased the cytotoxicity of Qinghaosu derivatives and provide a rational basis for further design and synthesis of novel Qinghaosu derivatives.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; pharmacology ; Artemisinins ; chemical synthesis ; chemistry ; pharmacology ; Catalytic Domain ; Drug Discovery ; Models, Chemical ; Molecular Structure ; Protein Binding ; Transferrin ; chemistry

OBJECTIVETo study the effect of water content in soil on physiological characters and yield of Artemisia annua.

METHODThe pot experiment was applied and activity of protective enzyme, biomass and artemisinin accumulation were measured under different water treatments.

RESULT AND CONCLUSIONThe results showed that contents of osmotic adjustable substances, activity of protective enzyme, biomass and artemisinin accumulation were greatly affected by water content in the soil. Under water stress the water content in leave decreased, relative plasmalemma permeability increased, proline quickly accumulated to promote water retaining capability of cell, POD, CAT and SOD cooperated to reduce lipid peroxidation and reduced cell damage, and biomass decreased. At the seedling stage, the content of artemisinin and yield reached the maximal when the water content in soil was between 50%-55%. At the beginning of the branching stage, the content of artemisinin was the highest at the water content of 50%-55%, while the yield reached the maximal at the water content of 70%-75%. At the end of branching stage, the content of artemisinin was the highest at the water content of 40%-45%, while the yield reached the maximal at the water content of 60%-65%. In conclusion, the optimum water content in soil was between 50%-55% at the seedling stage, at the branching stage, higher water content was beneficial for the higher yield.

Antimalarials ; analysis ; pharmacology ; Artemisia annua ; chemistry ; physiology ; Artemisinins ; analysis ; Biomass ; Plant Leaves ; chemistry ; Plant Transpiration ; Seedlings ; Soil ; analysis ; Water ; Water Movements

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 observe the effect of artemisinin on the ischemia/reperfusion injury of the iisolated rat myocardium and to preliminarily study the possible mechanism.

METHODFifty Wistar rats were randomly divided into 5 groups: a control group, an ischemia/reperfusion (I/R) group, and 3 artemisinin (AS) groups (10, 100, 1000 micromol x L(-1)), 10 rats in each group. Ischemia/reperfusion injury of the isolated rat myocardium was induced by a Langendorff system. The electrocardiogram, the cardiac functional parameters, coronary flow, and the activities of LDH (lactate dehydrogenase), CPK (creatine phosphokinase), SOD (superoxide dis-mutase) and the level of malondiadehyde (MDA) in myocardial tissue, and the myocardial ultrastructures were investigated.

RESULTAS (10,100 micromol x L(-1)) could significantly improve the index of the myocardial function (+/- dp/dt(max), LVSP) after the ischemia/reperfusion, increase the coronary flow, decrease the leakage of LDH and CPK, and increase the SOD activity and decrease the MDA level in cardiac tissues, and alleviate the myocardial ultrastructure injury. But, AS (1000 micromo x L(-1)) did not have the above effects.

CONCLUSIONAS (10, 100 micromol x L(-1)) alleviate the myocardial ischemia/reperfusion injury in rats. The mechanism may be related to its functions of antioxidation and scavenging free radicals.

Animals ; Antioxidants ; pharmacology ; Artemisia ; chemistry ; Artemisinins ; isolation & purification ; pharmacology ; Coronary Circulation ; drug effects ; Female ; Free Radical Scavengers ; pharmacology ; Heart ; physiopathology ; Male ; Myocardial Reperfusion Injury ; metabolism ; pathology ; physiopathology ; Myocardium ; pathology ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Wistar

The different components of crude mycelium of the predominant endophytic Colletotrichum gloeosporioides of Artemisa annua have been extracted by the methods of acid hydrolysate. We compared the effect of the isolated components on artemisin biosynthesis in hairy root cultures. Therefore, the oligosaccharide elicitor from C. gloeosporioides has been partially purified by column chromatography of Sephadex G25. The isolated oligosaccharide B II (elicitor, MW < 2500) has been revealed to promote the production of artemisinin in Artemisia annua hairy root cultures. When hairy roots of 23-day old cultures (later growth phase) were exposed to the elicitor at 0.4 mg/mL for 4 days, the maximum production of artemisinin reached to 13.51 mg/L, a 51.63% increase over the control. This is the first report on the stimulation of artemisinin production in hairy roots by the oligosaccharide elicitor from an endophytic fungus of A. annua.
Artemisia annua ; drug effects ; growth & development ; metabolism ; Artemisinins ; metabolism ; Bioreactors ; Colletotrichum ; chemistry ; Mycelium ; chemistry ; Oligosaccharides ; isolation & purification ; pharmacology ; Plant Roots ; drug effects ; growth & development ; metabolism