OBJECTIVETo screen the antimalarial compounds of daphnetin derivatives against Plasmodium falciparum in vitro.

METHODPlasmodium faciparum (FCC1) was cultured in vitro by a modified method of Trager and Jensen. Antimalarial compounds were screened by microscopy-based assay and microfluorimetric method.

RESULTSDA79 and DA78 showed potent antimalarial activity against Plasmodium falciparum cultured in vitro.

CONCLUSIONThough the relationship between the structures of daphnetin derivatives and their antimalarial activities has not been clarified yet, this study may provide a new direction for discovery of more potential antimalarial compounds.

Animals ; Antimalarials ; chemistry ; pharmacokinetics ; pharmacology ; Plasmodium falciparum ; drug effects ; Umbelliferones ; chemistry ; pharmacokinetics ; pharmacology

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 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

Each diastereomer of 10-thiophenyl- and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10 beta-benzenesulfonyl-dihydroartemisinin showed stronger antimalarial activity than artemisinin.
Animals ; Antimalarials/chemistry/*pharmacology ; Artemisinins/chemistry/*pharmacology ; Chloroquine/pharmacology ; Drug Resistance ; Plasmodium falciparum/*drug effects ; Research Support, Non-U.S. Gov't

AIMTo establish 3D QSAR model of propenamides with anti-malarial activities.

METHODSChemical synthesis combined with comparative molecular field analysis (CoMFA).

RESULTSGenerated QSAR models for activities of inhibiting chloroquine resistive malaria (W2) and chloroquine sensitive malaria (D6).

CONCLUSIONThe activity of anti-W2 depends mostly on steric interaction and the activity of anti-D6 depends on both steric and electrostatic interaction.

Acrylamides ; chemical synthesis ; chemistry ; pharmacology ; Animals ; Antimalarials ; chemical synthesis ; chemistry ; pharmacology ; Chloroquine ; pharmacology ; Drug Resistance ; Molecular Conformation ; Molecular Structure ; Plasmodium ; drug effects ; Quantitative Structure-Activity Relationship

The aim of this study was to verify the trypanocidal effectiveness of aqueous, methanolic, and ethanolic extracts of Achyrocline satureioides against Trypanosoma evansi in vitro. A. satureioides extracts, known as macela, were used on trypomastigotes at different concentrations (1, 5, 10, 50, 100, 500, and 1,000 microg/ml) and exposure times (0, 1, 3, 6, and 9 hr). A dose-dependent effect was observed when the 3 extracts were tested. The concentrations of 1, 5, and 10 microg/ml were not able to kill trypomastigotes until 3 hr after exposure, and the highest concentrations (500 and 1,000 microg/ml) were able to kill all trypomastigotes after 1 hr. When the time of exposure was increased up to 9 hr, the concentrations at 50 and 100 microg/ml were 100% effective to 3 extracts. The chemical analysis of the extracts revealed the presence of flavonoids, a trypanocidal compound already described. Based on the results, we can conclude that the A. satureioides extracts exhibit trypanocidal effects.
Achyrocline/*chemistry ; Antimalarials/isolation & purification/*pharmacology ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Flavonoids/isolation & purification/pharmacology ; Plant Extracts/isolation & purification/*pharmacology ; Time Factors ; Trypanosoma/*drug effects

Animals ; Antimalarials ; chemical synthesis ; chemistry ; pharmacology ; Artemisinins ; chemical synthesis ; chemistry ; pharmacology ; Heterocyclic Compounds ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Plasmodium berghei ; drug effects ; Sesquiterpenes ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

OBJECTIVETo determine the free radical scavenging potentials pytochemical constituents of ethanol leaves extracts of Allamanda cathartica (A. cathartica) and Bixa orellana (B. orellana) and thus their effects in antimalarial activities.

METHODSBoth ethanol extracted plant samples were administered at 50 mg/mL, 100 mg/mL and 200 mg/mL to Albino rats and then administered with CCl4 at 1 mL/kg body weight, in liquid paraffin (1:1, v/v) for 2 days (negative control) and compared with 5% Tween 80 (placebo) and vitamin E (positive control) pretreatments. Thiobarbituric acid reactive substances (TBARS), glutathione (GSH) and catalase (CAT) activities in blood and liver tissues were assessed.

RESULTSIn CCl4 treated rats, TBARS levels significantly increased, while decreased GSH and CAT levels were recorded for both plant extracts. Generally, higher TBARS and GSH values were recorded for blood than for liver homogenates; with reverse trend observed for CAT level. Increased concentrations of A. cathartica extract recorded significant antioxidant levels similar to tocopherol (vitamin E). Reducing sugars, saponins, flavonoids were recorded for both species; alkaloids in A. cathartica and terpenoids in B. orellana.

CONCLUSIONSA. cathartica, possess phytochemicals that recorded significant antioxidative defense activities for blood and liver tissues with increasing concentration. However B. orellana did not record similar results.

Animals ; Antimalarials ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Bixaceae ; chemistry ; Catalase ; metabolism ; Dose-Response Relationship, Drug ; Enzyme Activation ; drug effects ; Glutathione ; metabolism ; Lipid Peroxidation ; drug effects ; Phytochemicals ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Rats ; Superoxide Dismutase ; metabolism

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

Resistance of Plasmodium spp. to anti-malarial drugs is the primary obstacle in the fight against malaria, and molecular markers for the drug resistance have been applied as an adjunct in the surveillance of the resistance. In this study, we investigated the prevalence of mutations in pvmdr1, pvcrt-o, pvdhfr, and pvdhps genes in temperate-zone P. vivax parasites from central China. A total of 26 isolates were selected, including 8 which were previously shown to have a lower susceptibility to chloroquine in vitro. For pvmdr1, pvcrt-o, and pvdhps genes, no resistance-conferring mutations were discovered. However, a highly prevalent (69.2%), single-point mutation (S117N) was found in pvdhfr gene. In addition, tandem repeat polymorphisms existed in pvdhfr and pvdhps genes, which warranted further studies in relation to the parasite resistance to antifolate drugs. The study further suggests that P. vivax populations in central China may still be relatively susceptible to chloroquine and sulfadoxine-pyrimethamine.
Antimalarials/*pharmacology ; China ; Chloroquine/pharmacology ; DNA, Protozoan/chemistry/genetics ; Drug Resistance/*genetics ; Folic Acid Antagonists/pharmacology ; Genotype ; Humans ; Malaria, Vivax/epidemiology/*parasitology ; Plasmodium vivax/drug effects/*genetics/isolation & purification ; Point Mutation ; Polymorphism, Single Nucleotide/*genetics ; Prevalence ; Protozoan Proteins/genetics ; Sequence Analysis, DNA ; Tandem Repeat Sequences/*genetics