Publications
Title | Abstract | Year Filter | PMID(sorted ascending) Filter |
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the chemotherapy of rodent malaria, xxiii causal prophylaxis, part ii: practical experience with plasmodium yoelii nigeriensis in drug screening. | data are presented on the causal prophylactic action of about 100 compounds of various types against plasmodium yoelii nigeriensis n67 in mice. examples are given to show how action against pre-erythrocytic schizonts may be differentiated from action on emerging erythrocytic stages. in a series of 35 8-aminoquinolines, all but 10 showed definite causal prophylactic activity at tolerated doses. the data permit the compounds to be ranked in order of activity, and many are shown to be more active i ... | 1975 | 1098590 |
a comparison of pigment from schistosoma mansoni and plasmodium berghei. | the structures of malarial and schistosomal pigment within the parasites are distinct. the two pigments are distinguishable both before and after extraction from host liver. | 1975 | 1098591 |
antimalarials: screening of (orally administered) silver solfonamides against plasmodium berghei. | orally administered silver sulfadiazine is effective against plasmodium berghei. attempts to synthesize an active analogue with antimalarial activity failed. although several of the analogues were chemically stable (like silver sulfadiazine) in sodium chloride, none of the analogues were biologically active. this suggests that the antimalarial activity of silver sulfadiazine is stereo-specific. | 1975 | 1098869 |
thiosemicarbazones and hydrazones of alpha-methylchalkone as potential chemotherapeutic agents. | the effectiveness of chalkones and derivatives as antibacterial and antifungal agents stimulated our interest in the possibility of coupling this type of compound with certain hydrazines and thiosemicarbazides to determine the potential chemotherapeutic activity of these combinations as anticancer and antimalarial agents. accordingly, 18 hydrazine and thiosemicarbazide derivatives of alpha-methylchalkone (dypnone) have been synthesized for study as potential antitumor agents in animal tumor syst ... | 1975 | 1099024 |
alterations in the permeability of mouse erythrocytes infected with the malaria parasite, plasmodium berghei. | 1975 | 1099038 | |
antimalarial phenanthrene amino alcohols. 3. halogen-containing 9-phenanthrenemethanols. | a series of new 9-phenanthrene amino alcohols has been prepared in which each compound bears from one to five halogen or halogen-containing moieties. a number of these compounds are extremely active against plasmodium berghei in the mouse. some structural requirements for optimal efficacy are considered. | 1975 | 1099200 |
comparison of tritiated hypoxanthine, adenine and adenosine for purine-salvage incorporation into nucleic acids of the malarial parasite, plasmodium berghei. | this study was accomplished to examine the relative importance of different metabolic precursors of nucleic acid synthesis in the malarial parasite, p. berghei. three possible pathways for incorporation of adenine (type) compounds exist: 1) incorporation via hypoxanthine, 2) via adenine, or 3) via adenosine. the parasitized cell and erythrocyte-free malarial parasite were both examined because of possible metabolic differences that could be encountered. hypoxanthine was clearly the best precurso ... | 1975 | 1099747 |
mass isolation of anopheles stephensi salivary glands infected with malarial sporozoites. | 1975 | 1100801 | |
antimalarials. 7.2,8-bis(trifluoromethyl)-4-quinolinemethanols. | based on the high antilalarial activity of alpha-(2-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol, ten additional 2,8-bis(trifluoromethyl)-4-quinolinemethanols were prepared in which the amino alcohol side chain was structurally varied. synthesis of the compounds is described and antimalarial activity data against plasmodium berghei are presented and discussed in terms of the structure variations. | 1975 | 1100828 |
neutralizing antibody in rodent malaria. | small numbers of rat erythrocytes infected with viable p. berghei, when inoculated into susceptible rats together with hyperimmune rat serum (his), are fully neutralized. serum from convalescent rats delays the onset of patency but does not neutralize. the neutralizing efficiency of his rises in proportion to the number of successive reinoculations of hyperimmune rats. in contrast, mice inoculated with parasites together with either his or normal rat serum succumbed to the disease at the same ti ... | 1975 | 1101458 |
failure to protect mus musculus against plasmodium berghei with footpad injections of killed parasites incorporated in complete freund's adjuvant. | the stimulation of cell-mediated immunity by the injection of antigen from killed parasites incorporated in complete freund's adjuvant did not protect mus musculus from the erythrocytic stages of plasmodium berghei. agglutinating antibodies could not be detected, but delayed hypersensitivity was demonstrable. apparently thymocyte sensitization alone was not sufficient to afford protection. | 1975 | 1102649 |
enhanced trypanosoma musculi infections in mice with concomitant malaria. | 1975 | 1102992 | |
t-cell activation in murine malaria. | 1975 | 1102993 | |
the nature of age immunity to plasmodium berghei in the rat. | the intensity of plasmodium berghei infections decreases as the age of the rat host increases. the nature of this 'age immunity' was investigated. no experimental support was found for innate resistance involving either serum non-antibody factors or changes in the erythrocytes that inhibit parasites in older rats. a cross reacting immune response active against p. berghei was not found. evidence is presented which shows that rats less than 7 weeks old lack at least part of the functional immunol ... | 1975 | 1103066 |
[course of trypanosoma musculi infections in plasmodium berghi-infected mice (author's transl)]. | trypanosoma musculi brought into plasmodium berghei-infected mice in the later stages of the malaria infection shows rapid, approximately logarithmic multiplication in the peripheral blood. the trypanosome number increases by a factor of 2-9 per day, multiplication of the parasites kills most mice in a few days. many multiplicative forms of the trypanosomes and a few trypanosomes without nuclei are seen in blood smears. histologically and in touch preparations, masses of multiplicative forms of ... | 1975 | 1103389 |
[altered reproductive behaviour of trypanosoma musculi after several years of passage in mice (author's transl)]. | the modified strain multiplied less in pregnant and in plasmodium berghei-infected mice, more in heavily infected normal mice, and more or less in weakly infected normal mice. the discordant behaviour in weakly infected mice was due to the occurrence in some animals of a second phase of more rapid increase of the parasitemia. this behaviour could be seen occasionally in the original strain, too. in inbred mice (balb/chan) the length of parasitemia clearly depended on inoculum size and height of ... | 1975 | 1103390 |
effects of lowered environmental temperature on the growth of exoerythrocytic stages of plasmodium berghei. | the effect of lowered host-environmental temperature upon the development and maturation of the preerythrocytic tissue stages of rodent malaria parasites has been investigated in two strains of plasmodium berghei originating from the highlands of katanga. young albino rats inoculated with massive sporozoite doses of p. berghei nk 65 and maintained for 48 hours at 12 degrees c developed small, stunted tissue schizonts, averaging 11 x 15 microns, of a distinct morphology. control rats kept at room ... | 1975 | 1103642 |
detection of antibody in white mice infected with plasmodium berghei by means of the indirect immunofluorescence test. | experiments have been conducted in order to test the efficacy of the immunofluorescence test in the detection of antibody in mice infected with plasmodium berghei vincke et zips, 1948. this method enables the detection of antibody in subclinical and latent cases when an occasional parasite only is present in the blood cells. of the various methods used for the preparation of antigen, and of the various fixatives, a satisfactory immunofluorescence reaction was obtained if unfixed erythrocytes wit ... | 1975 | 1104419 |
evaluation of a method for in vitro ookinete development of the rodent malarial parasite, plasmodium berghei. | 1975 | 1104798 | |
chloroquine resistance in malaria: variations of substrate-stimulated chloroquine accumulation. | the response of [14c]chloroquine accumulation to the provision of substrate was evaluated using washed erythrocytes infected with plasmodium berghei cs (chloroquine-susceptible), with p. berghei cr (chloroquine-resistant), with plasmodium vinckei cs, with p. vinckei cr, or with a strain of p. berghei spontaneously resistant to chloroquine, plasmodium berghei yoelii 17x. erythrocytes infected with chloroquine-resistant parasites had a blunted response, particularly to low glucose concentrations. ... | 1975 | 1104805 |
antimalarials. synthesis and antimalarial activity of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine and derivatives. | the preparation and activity against plasmodium berghei of derivatives of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine are described. replacement of the cinnamoyl group was accomplished by acylation or alkylation of 1-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine. modifications of the 5-phenyl group were prepared either by a sequence of reactions involving mandelic ester-pemoline-piperazine pemoline or by the reaction of 5-aryl-2-thio-2,4-oxazolidinedione with piperazine or n ... | 1975 | 1104830 |
antimalarials. 3. 3-substituted 1-naphthalenemethanols. | the synthesis and antimalarial activity of 22 3-substituted 1-naphthalenemethanols whose substitution was patterned after the antimalarial 2-substituted 4-quinolinemethanols are described. the compounds were active against plasmodium berghei in mice, the most active being 6-chloro-alpha-(dibutylaminomethyl)-3-(3,4-dichlorophenyl)-1-naphthalenemethanol hydrochloride (3b). the naphthalenemethanols tested, 1b and 2b, were not photosensitizing to albino mice. structure-activity relationships between ... | 1975 | 1104831 |
antimalarials. 10. substituted 3-halo- and 3-methoxy-2-aryl-4-quinoline(di-n-butylaminomethyl)methanols. | four 2-aryl-4-quinoline(di-n-butylaminomethyl)methanols with br, cl, f, or ome in position 3 were synthesized by modifications of standard reactions. the antimalarial activity decreased with increased size of the 3-substituent. the 3-f-4',6,8-cl3 compound was the most active (at 2.5 mg/kg) and was completely curative at 80 mg/kg against p. berghei in mice. | 1975 | 1104832 |
intramuscular immunization of mice with irradiated plasmodium berghei sporozoites. enhancement of protection with albumin. | 1975 | 1106231 | |
[immunosuppression in protozoan infections]. | 1975 | 1107126 | |
antimalarial amino alcohols ii: anthraceneaminoethanols and anthraceneaminopropanols (1- and 9-substituted). | the syntheses of seven anthracene amino alcohols with one, two, or three additional substituents are described. these compounds include three 1-aminoethanols, two 9-aminoethanols, and two 9-aminopropanols, prepared from substituted anthraquinones or from 10-chloro-9-anthraldehydes. the antimalarial activity of these compounds, as well as tentative structure-activity relationships, is discussed in the light of previously published work. | 1975 | 1107515 |
synthesis of 2-pyridyl-alpha-toluenesulfonates as antimalarials. | a series of substituted 2-pyridyl-alpha-toluenesulfonates was synthesized for antimalarial testing. they were prepared by treating various 2-pyridinols with alpha-toluenesulfonyl chlorides in the presence of an alkali. in tests against plasmodium berghei in mice at 640 mg/kg, only 3,5-dichloro-2-pyridyl-alpha-toluenesulfonate was considered active, i.e., doubled the mean survival time. | 1975 | 1107516 |
difference in antimalarial activity between certain amino alcohol diastereomers. | a striking difference in antimalarial activity between the diastereomers of 6-bromo-alpha-[2-(1-methylpiperidyl)]-9-phenanthrenemethanol, alpha-(3-peperidyl)-3,6-bis(trifluoromethyl)-9-phenanthrenemethanol, and alpha-(3-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol was observed. a possible explanation involving the n-o distance and active site binding requirements is suggested. | 1976 | 1107548 |
pharmacology of the malaria parasite--a study of dose-response relationships in chloroquine-induced autophagic vacuole formation in plasmodium berghei. | 1975 | 1108883 | |
monoclonal antibodies recognize a processing dependent epitope present in the mature cs protein of various plasmodial species. | in the present paper, we have characterized the specificity of a series of monoclonal antibodies (moabs) against plasmodium berghei sporozoites, selected for their lack of reactivity with the repeat domain of the circumsporozoite (cs) protein. we found that these moabs recognize pb44, the mature membrane form of the cs protein, but they do not react with pb54, its precursor. furthermore, these moabs do not react with any of the synthetic peptides representing the linear sequence of the p. berghe ... | 1992 | 1279504 |
pathology of fatal and resolving plasmodium berghei cerebral malaria in mice. | cba/t6 and balb/c mice inoculated with plasmodium berghei anka strain (pba) died from cerebral malaria 6-8 days post-inoculation. dba/2j mice similarly inoculated developed a non-fatal cerebral malaria, with mild temporary cerebral symptoms, and died between days 15 and 22 from other malaria-related complications. when inoculated with p. berghei k173 (pb) these mouse strains did not develop a cerebral malaria but died between days 15 and 22 from other malaria-related complications. these mouse s ... | 1992 | 1280805 |
highly diverse t cell recognition of a single plasmodium berghei peptide presented by a series of mutant h-2kd molecules. | we have tested 21 independent ctl clones for recognition of a single peptide derived from the plasmodium berghei circumsporozoite protein in the context of 13 mutants of the murine mhc class i molecule h-2kd. in this series of kd mutants, amino acid residues located on the upper surface of the alpha-helices were individually substituted by alanine. remarkably, most clones displayed individual recognition patterns on the kd mutants. we had previously found that this series of ctl clones was likew ... | 1992 | 1281196 |
the chemotherapy of rodent malaria. xlvii. studies on pyronaridine and other mannich base antimalarials. | the activities of mannich base antimalarials, including pyronaridine, have been explored against drug-sensitive (plasmodium berghei n) and chloroquine-resistant (plasmodium yoelii ns) rodent malaria parasites in vivo. lines of these parasites have been developed with resistance to pyronaridine, amodiaquine, or wr 228,258. the responses and patterns of cross-resistance of these lines to mannich bases and other blood schizontocides are inconsistent. it is concluded that some mannich bases may prov ... | 1992 | 1288426 |
[antimalarial effect of n-hentriacontanol isolated from cuatresia sp (solanaceae)]. | the antimalarial activity of the fatty alcohol, n-hentriacontanol, isolated from the bolivian solanaceae, cuatresia sp, is investigated in vivo through a classical four-day suppressive test against plasmodium berghei and p. vinckei in mice. this product markedly reduced the virulence of experimentally induced p. vinckei infection. n-hentriacontanol belongs to a new class of antimalarial natural compounds to be exploited for therapeutic purposes. | 1992 | 1294019 |
role of free radicals in plasmodium berghei infected mastomys natalensis brain. | lipid peroxide, lipid hydroperoxide, reduced glutathione, oxidised glutathione, lipofuscin contents and the activity of the enzyme superoxide dismutase were assessed in p. berghei infected m. natalensis brain. the results showed significant increase in the levels of lipid peroxides, lipid hydroperoxides and lipofuscin in brain subcellular fractions of p. berghei infected m. natalensis. furthermore, a depressed superoxide dismutase activity was observed along with regulation in glutathione conten ... | 1992 | 1294484 |
studies on the infectivity of gametocytes of plasmodium berghei (nk 65) in anopheles stephensi. | the infectivity of gametocytes of plasmodium berghei (nk 65) has been studied in laboratory bred anopheles stephensi. mosquitoes were fed daily on infected male and female mastomys natalensis and subsequent development of the oocysts was monitored in the midguts. maximum number of oocysts were found in mosquitoes which were fed on infected female mastomys on d8 and in male mastomys on d7 post-inoculation. during the next peak of gametocytaemia, very few oocysts developed. these findings suggest ... | 1992 | 1296945 |
spectrophotometric assay of the interaction of plasmodium berghei infected erythrocyte lysates and neutral red. | in order to reveal by absorption spectrophotometry the redox differences between the plasmodium berghei infected erythrocyte lysates (mel) and the healthy ones (hel) we studied their interaction with the neutral red (nr) redox dye. the variation of the dye absorption intensity at 540 nm as a function of the hemoglobin content of the samples was attributed to the redox potential variation of the different hemoglobin aggregates formed in the samples containing different hemoglobin quantities. by s ... | 1992 | 1297467 |
[studies on the antimalarial action of gelatin capsule of artemisia annua]. | the pharmacological and clinical effects of gelatin capsule of artemisia annua (gcaa) were investigated. the results revealed that the ld50 was 162.5 +/- 10.1g (crude drug)/kg and ed50 was 11.9 +/- 2.4g (crude drug) for clearance of parasitemia in mice infected with plasmodium berghei therapeutic index being 13.6, which was 3.5 times more than that of artemisinin. the cure rate of coea for plasmodium berghei and p. vivax infections was 100%, as well as just like that of the extract tablets of ar ... | 1992 | 1303339 |
localization of a 230-kd parasitophorous vacuole membrane antigen of plasmodium berghei exoerythrocytic schizonts (lsa-2) by immunoelectron and confocal laser scanning microscopy. | using antiserum to a 230-kd parasitophorous vacuole membrane (pvm) antigen of plasmodium berghei exoerythrocytic schizonts as a specific probe for the pvm, we studied the three-dimensional structure of this membrane within infected host cells by immunoelectron microscopy and confocal laser scanning microscopy at 3, 4, and 50 hr after sporozoite invasion. fluorescent label was not detected at 3 hr, but was associated with the cytoplasm of 24-hr-old exoerythrocytic parasites. specific labeling of ... | 1992 | 1318005 |
[involvement of cellular immunity in pathology. neuromalaria]. | murin cerebral malaria (mcm) with plasmodium berghei anka and the cba/ca mice is the result of an immunopathological process. an overproduction of tnf is implicated in its pathogenesis. recent datas concerning tnf production during the course of plasmodium vinckei vinckei infection, and analysis of relationships between mcm and experimental allergic encephalomyelitis (eae) raise the hypothesis of the involvement of an auto-immune process in the murin disease. the role of cellular immunity in hum ... | 1992 | 1327351 |
gamete development in plasmodium berghei regulated by ionic exchange mechanisms. | ionic regulation in the induction of exflagellation of plasmodium berghei was investigated by culturing the parasites in various isotonic media. of the salts tested, nahco3 exhibited the highest activity in inducing exflagellation, whereas khco3 showed no activity. in the absence of hco3-, media containing monovalent cation (na+, k+, cs+, rd+, choline+, lysine+, arginine+) and cl- also induced exflagellation, but their activities were lower than that of nahco3. anions of br- or no3- could be sub ... | 1992 | 1329079 |
host resistance assays as predictive models in styrene immunomodulation. | three infection models namely an oncogenic virus encephalomyocarditis (emcv), a rodent strain of malaria, plasmodium berghei, and a rodent hookworm parasite, nippostrongylus brasiliensis, were used to confirm the in vivo immunotoxic potential of styrene reported in our previous communication. the altered host resistance to these challenge infections was evaluated in rodents pre-treated with 0, 0.02, 0.03 or 0.05 x ld50 dose of styrene (5 days/week) for 4 weeks. significantly increased mortality ... | 1992 | 1330943 |
[an evaluation of the effect of phytobacteriomycin on the malarial parasite in the mosquito]. | 1992 | 1331733 | |
[a spectrophotometric study of the interaction of neutral red with lysates of erythrocytes infected with plasmodium berghei]. | 1992 | 1340261 | |
immunopathology of malaria: role of cytokine production and adhesion molecules. | 1992 | 1342724 | |
deletion, insertion and translocation of dna sequences contribute to chromosome size polymorphism in plasmodium berghei. | extensive chromosome size polymorphism arises in plasmodium berghei during in vivo mitotic multiplication. size differences between homologous chromosomes mainly involve rearrangements in the subtelomeric regions while internal chromosomal regions are more conserved. size differences are almost exclusively due to differences in the copy number of a 2.3 kb subtelomeric repeat unit. not only deletion of 2.3 kb repeats occurs, but addition of new copies of this repeat sometimes results in the forma ... | 1992 | 1343732 |
interrelationship between schistosomiasis and concomitant diseases. | the biological literature contains many examples of mutual influences between different species of parasites, especially with respect to concomitant helminth infections. several situations are known in which the association of infection by schistosoma mansoni with other pathogens in the same host results in a type of disease which differs from the simple summation of the individual effects of each infection. the present study concerns concomitant infections involving s. mansoni and enterobacteri ... | 1992 | 1343911 |
distinct t cell specificities are induced with the authentic versus recombinant plasmodium berghei circumsporozoite protein. | plasmodium berghei sporozoite (spz)-immune lymph node (ln) cells obtained from mice of different h-2 haplotypes were analyzed for the presence of circumsporozoite (cs) protein-reactive t cells in proliferative assays. although lymphocytes from each strain responded in vitro to the priming ag and to the soluble rcs protein, they did not respond to cs protein synthetic peptides. parallel analysis of rcs protein-primed ln cells revealed that the two ag are unequal in generating t cell specificities ... | 1992 | 1348519 |
antimalarial activity of orotate analogs that inhibit dihydroorotase and dihydroorotate dehydrogenase. | dihydroorotase and dihydroorotate dehydrogenase, two enzymes of the pyrimidine biosynthetic pathway, were purified from plasmodium berghei to apparent homogeneity. orotate and a series of 5-substituted derivatives were found to inhibit competitively the purified enzymes from the malaria parasite. the order of effectiveness as inhibitors on pyrimidine ring cleavage reaction for dihydroorotase was 5-fluoro orotate greater than 5-amino orotate, 5-methyl orotate greater than orotate greater than 5-b ... | 1992 | 1348618 |
the role of t cells in pathogenesis and protective immunity to murine malaria. | t-cell-mediated immunity to a virulent strain of plasmodium berghei nk65 (pb nk65) and to an attenuated derivative (pb xat) of the strain were examined in cba mice by the administration of monoclonal antibodies against t-cell subsets or interferon-gamma (ifn-gamma). the injection of anti-cd8+ or anti-ifn-gamma delayed the mortality of mice infected with pb nk65, although it did not affect the parasitaemia. in the late stage of pb nk65 infection, t cells, especially cd8+ t cells, were increased i ... | 1992 | 1350570 |
mini- and micro-satellites in the genome of rodent malaria parasites. | higher eukaryotes contain within their dna numerous arrays of repetitive dna, many of which are known as satellite dnas and display extensive variability. the presence of these repeats has been demonstrated for various species and they have been used for genetic identification and classification. here, it is demonstrated that southern hybridisation of dna from rodent malaria parasites allows detection of micro- and minisatellite sequences in the genome of plasmodium species. closely related line ... | 1992 | 1355061 |
attenuation of malaria infection, paralysis and lesions in the central nervous system by low protein diets in rats. | young wistar rats developed a fulminant infection when inoculated with the rodent malaria parasite plasmodium berghei. rats that died during the infection exhibited a progressive paralysis of the extremities, a rapidly decreasing body temperature and minute haemorrhages in the brain. increasing the level of protein in the diet from 4 to 8 and 16% was accompanied by an increase in morbidity and mortality from 15 to 40 and 90% respectively on day 6 of the infection. increasing the level of dietary ... | 1992 | 1356299 |
inhibition of the growth of plasmodium falciparum and plasmodium berghei in vitro by an extract of cochlospermum angolense (welw.). | an extract of cochlospermum angolense (welw.) is used in the traditional medicine of angola for the therapy of icterus and for the prophylaxis of malaria. from the roots of this plant red crystalline substances have been isolated and tested for their effect on plasmodium falciparum in vitro and on the dna and protein synthesis of plasmodium berghei. the multiplication of p. falciparum was decreased to 50% of the control in the presence of 10 micrograms/ml extracted material and there was a total ... | 1992 | 1356304 |
most residues on the floor of the antigen binding site of the class i mhc molecule h-2kd influence peptide presentation. | a panel of 15 single alanine substitutions on the floor of the peptide binding groove of the murine class i histocompatibility molecule h-2kd has been analyzed. all but two mutant molecules were expressed on the cell surface, and were tested for peptide binding and presentation to specific cytotoxic t lymphocytes. eleven out of 13 mutant molecules appeared to be functionally altered. five of the substituted residues were involved in the presentation of all peptides tested. three participated in ... | 1992 | 1358191 |
identification and quantification of rodent malaria strains and species using gene probes. | a dna probe pcsv4 and a subclone thereof pcsv4.1, hybridize specifically to rodent malaria dna. dna purified from a small volume (10 microliters) of infected mouse blood was used to determine the composition of the parasite population present. the hybridization signal following pcsv4 probing of slot-blotted dna correlated directly with parasitaemia. the hybridization pattern and intensity, resulting from probing restriction enzyme digested and southern-blotted genomic dna, determined the identit ... | 1992 | 1359498 |
a protective monoclonal antibody with dual specificity for plasmodium falciparum and plasmodium berghei circumsporozoite proteins. | an igm monoclonal antibody (mab 36) which reacts with the circumsporozoite (cs) proteins of both p. falciparum and p. berghei was isolated from plasmodium falciparum sporozoite-immunized mice. in assays of biological activity, mab 36 induces the cs precipitation reaction with live sporozoites and blocks the invasion of hepatoma cells by sporozoites in vitro at concentrations much lower than those observed for previously reported cs protein-specific monoclonal antibodies. mab 36 also provided com ... | 1992 | 1375561 |
use of human universally antigenic tetanus toxin t cell epitopes as carriers for human vaccination. | synthetic constructs were assembled as multiple ag peptide systems containing repetitive sequences of plasmodium falciparum and plasmodium berghei, the causative agents of human and murine malaria respectively, and two universal human tetanus toxin t cell epitopes 830-843 and 947-967. these constructs were tested for antibody production in mice and for their capacity to stimulate human pbl and tetanus toxin-specific t cell clones. a high antibody titer can be obtained in mice when multiple ag pe ... | 1992 | 1378079 |
h-2-restricted cytolytic t lymphocytes specific for hla display t cell receptors of limited diversity. | we previously showed that h-2kd-restricted cytotoxic t lymphocyte (ctl) clones specific for a single nonapeptide derived from the plasmodium berghei circumsporozoite (pbcs) protein displayed t cell receptors (tcrs) of highly diverse primary structure. we have now analyzed the tcr repertoire of ctls that recognize a peptide derived from the human class i major histocompatibility complex (mhc) molecule hla-cw3 in association with the same murine class i mhc molecule h-2kd. we first sequenced the t ... | 1992 | 1380061 |
immunogenic properties of multiple antigen peptide systems containing defined t and b epitopes. | immunization with chemically defined synthetic polymers, multiple ag peptide (map) systems, containing t and b epitopes of the circumsporozoite protein of p. berghei induce high levels of circulating antibodies that are detectable several months after boosting. the anti-map secondary antibody response is characterized by an increase in the levels of circulating igg and a concomitant decrease in the igm levels. in vitro and in vivo experiments indicated that th epitopes included in the map are re ... | 1992 | 1382101 |
t helper epitopes enhance the cytotoxic response of mice immunized with mhc class i-restricted malaria peptides. | we have previously derived mhc class i (h-2kd) restricted cytotoxic t lymphocytes (ctl) from balb/c mice immunized with irradiated sporozoites from plasmodium (p.) berghei and p. yoelii. the ctl recognize synthetic peptides corresponding to a region of the circumsporozoite (cs) protein that is homologous in the two species. in the present study, we have attempted to induce cs-specific ctl by immunization with those peptides in incomplete freund's adjuvant. only a low level ctl response was detec ... | 1992 | 1383348 |
[the blood schizontocidal effects of pyronaridine, amodiaquine, mefloquine and qinghaosu on mice infected with plasmodium berghei]. | the asexual stages of p. berghei anka were completely eliminated as revealed in a "4-day suppressive test" with the daily dose of pyronaridine 12.5 mg base/kg or amodiaquine 25 mg base/kg. mefloquine 25 mg base/kg and qinghaosu 100 mg/kg though exerted obvious suppressive effect, the cure rates were only 50% and 0%, respectively. in treating chloroquine-sensitive p. berghei anka strain pyronaridine exhibited the best therapeutic activity, which was followed by amodiaquine, mefloquine and quingha ... | 1992 | 1394908 |
[observation of ultrastructure and drug sensitivity of in vitro cultured exoerythrocytic form of plasmodium berghei]. | the ultrastructure of in vitro cultured exoerythrocytic stage (ee) of plasmodium berghei (p. b.) was observed under transmission electron microscope (tem). the drug sensitivity of ee was also measured in vitro. the ee was cultured in monolayer host cell, fixed and embedded in situ. the ultrathin sections were prepared and examined by routine methods. the tem pictures showed that the fine structure of in vitro cultured ee was similar with that of ee grown in rat hepatocytes in vivo, as described ... | 1992 | 1394909 |
synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2h,10h)-acridinediones and related structures. | to improve upon the activity and properties of the 3-aryl-7-chloro-3,4- dihydro-1,9(2h,10h)-acridinediones, a variety of 1-[(alkylamino)alkylene]imino derivatives (3) were prepared and shown to be highly active antimalarial agents in both rodents and primates. among structural modifications prepared, including n10-alkyl and c2-substituted analogs, removal of the c9 oxygen, and introduction of an imino side chain at c9, the imines of the n10-h acridinediones were the most active compounds obtaine ... | 1992 | 1404226 |
extensive turnover of telomeric dna at a plasmodium berghei chromosomal extremity marked by a rare recombinational event. | the dynamics of telomere turnover were studied in plasmodium, whose telomeric structures consist of linear, recognisable sequences of two distinct repeats (tttaggg and ttcaggg). independent recombinant clones containing a well-defined chromosomal extremity of plasmodium berghei, both before and after a rare insertion event took place, were obtained from clonal parasite populations and analysed. the insertion, which splits the original telomere and causes a significant reduction in the size of th ... | 1992 | 1408751 |
development of a model ribosomal rna hybridization assay for the detection of sarcocystis and other coccidia. | two regions of the primary structure of the small subunit rrna of sarcocystis muris bradyzoites were compared with nucleotide sequences of s. gigantea, toxoplasma gondii, plasmodium berghei and mus musculus and used to design genus- and species-specific probes for the detection and identification of coccidia. total cellular rna of purified s. muris, s. cruzi, t. gondii and eimeria nieschulzi and coccidia-infected tissues of mouse, ox, sheep and pig, were assayed using twenty-base oligomers label ... | 1992 | 1423056 |
plasmodium berghei: sporozoites are sensitive to human serum but not susceptible host serum. | human complement was activated by rodent malaria, plasmodium berghei, sporozoites through the alternative pathway, as revealed by c3 deposition on sporozoites using the fluorescent antibody technique. sporozoites exposed to fresh human serum decreased in infectivity to hepg2 cells, but those exposed to heated or c3-deficient human serum showed normal infectivity to hepg2 cells. in contrast, c3 deposition was not observed on the sporozoites treated with mouse or rat serum even in the presence of ... | 1992 | 1426138 |
immunization against cerebral pathology in plasmodium berghei-infected mice. | the development of cerebral lesions in plasmodium berghei-infected mice was dependent on the strain of mice and the size of the infectious inoculum. in particular, c57bl/6j mice develop cerebral lesions when infected with low numbers of parasitized erythrocytes. by increasing the number of parasites in the infectious inoculum, the percentage of animals that develop cerebral malaria is decreased. varying degrees of protection against the development of cerebral malaria can be obtained by several ... | 1992 | 1437278 |
plasmodium falciparum and p. berghei: detection of sporozoites and the circumsporozoite proteins in the saliva of anopheles stephensi mosquitoes. | sporozoites and free circumsporozoite (cs) protein were stained immunoenzymatically in 1-min saliva samples collected from anopheles stephensi mosquitoes infected with either plasmodium berghei or p. falciparum. the number of sporozoites in 1-min saliva-streak samples significantly increased as the salivary gland index rose from 3+ to 4+. for p. berghei-infected mosquitoes from which saliva had been collected before 30 days postfeed, the median sporozoite counts for 3+ and 4+ gland indexes were ... | 1992 | 1438147 |
appearance of adherent cells suppressive to erythropoiesis during an early stage of plasmodium berghei infection in mice. | we examined the effect of adherent cells from bone marrow or spleen of mice infected with plasmodium berghei on dyserythropoiesis. significant reduction in number of erythroid progenitors (erythroid colony-forming units: cfu-e and erythroid burst-forming units: bfu-e) was observed in bone marrow as early as 1 day after p. berghei infection. when adherent cells were removed from bone marrow or spleen cells of infected mice, the number of cfu-e and bfu-e was clearly increased. furthermore, additio ... | 1992 | 1439968 |
purification and ligand binding of a soluble class i major histocompatibility complex molecule consisting of the first three domains of h-2kd fused to beta 2-microglobulin expressed in the baculovirus-insect cell system. | a recombinant baculovirus encoding a single-chain murine major histocompatibility complex class i molecule in which the first three domains of h-2kd are fused to beta 2-microglobulin (beta 2-m) via a 15-amino acid linker has been isolated and used to infect lepidopteran cells. a soluble, 391-amino acid single-chain h-2kd (sc-kd) molecule of 48 kda was synthesized and glycosylated in insect cells and could be purified in the absence of detergents by affinity chromatography using the anti-h-2kd mo ... | 1992 | 1447172 |
placental pathology in plasmodium berghei-infected rats. | the pathologic changes in placentae of pregnant rats infected with plasmodium berghei at different stages of gestation were studied using light and electron microscopy and immunohistochemistry. the major changes observed were thickening and duplication of the trophoblastic basement membrane, and accumulation of parasitized erythrocytes and occasional mononuclear cells in the maternal blood space. immunohistochemical examination of nine placentae revealed that six stained positively for igg, two ... | 1992 | 1449205 |
the effect of malaria infection on 3'-azido-3'-deoxythymidine and paracetamol glucuronidation in rat liver microsomes. | the effect of malaria infection on udp-glucuronosyltransferase (udpgt) activity was investigated in rat liver microsomes using 3'-azido-3'-deoxythymidine and paracetamol. the michaelis-menten parameters, km and vmax were calculated and intrinsic clearance values were estimated for normal and infected livers. the results show that malaria infection alters the activity of udpgt. | 1992 | 1449539 |
electron microscopic analysis of circumsporozoite protein trail formation by gliding malaria sporozoites. | immunoelectron microscopic techniques were utilized to characterize the morphology of circumsporozoite protein-containing trails deposited on various substrates by gliding plasmodium berghei and plasmodium falciparum sporozoites. the basic components of the trails are beadlike particles, 25 to 90 nm in diameter, which are devoid of unit membrane and have an electron-lucent center. trails were captured on formvar-covered grids coated with anticircumsporozoite protein monoclonal antibodies and com ... | 1992 | 1453354 |
reversal of chloroquine resistance with verapamil in p. berghei in vivo. | the effects of verapamil on the parasite susceptibility to chloroquine were examined in mice infected with chloroquine-sensitive and chloroquine-resistant lines of plasmodium berghei. verapamil in a dose of 10-50 mg/kg daily s.c. for 4 days did not affect the growth of both sensitive and resistant parasites. when verapamil in the same dose range was combined with 1.5 mg/kg chloroquine diphosphate, the chloroquine-sensitive parasites became more susceptible to chloroquine. similarly, verapamil se ... | 1992 | 1459299 |
effect of picroliv on glutathione metabolism in liver and brain of mastomys natalensis infected with plasmodium berghei. | administration of picroliv, the active principle from picrorhiza kurrooa, at a dose of 6 mg/kg, po for two weeks showed significant protection against changes in liver and brain glutathione metabolism of plasmodium berghei infected mastomys natalensis. the depletion of reduced glutathione level and inhibition of glutathione-s-transferase, glutathione reductase and glutathione peroxidase activities due to p. berghei infection were markedly recovered by picroliv. the increased levels of lipid pero ... | 1992 | 1459651 |
plasmodium berghei and plasmodium chabaudi chabaudi: development of simple in vitro erythrocyte invasion assays. | erythrocyte invasion assays are described for two species of rodent malaria, namely plasmodium berghei and p.c. chabaudi. these invasion assays are simple, are carried out using a candle jar and allow a number of assays to be performed simultaneously. our results demonstrate that both rodent malaria species show an in vitro preference for reticulocytes although the preference of p. c. chabaudi for these cells is not as marked as that of p. berghei. the details of our invasion assays and our resu ... | 1992 | 1461676 |
assessment of parasite population dynamics in mixed infections of rodent plasmodia. | cloned lines of the four rodent plasmodium species can be differentiated by the rflp pattern generated following southern blotting and probing with pcsv4.1, a probe derived from a p. chabaudi chabaudi genomic library. groups of cba/ca mice were inoculated simultaneously with cloned lines from two parasite species or strains. six mixed species and three mixed strain infections using rodent malaria lines were initiated. the composition of the parasite population in each group was determined qualit ... | 1992 | 1461677 |
heme polymerase: modulation by chloroquine treatment of a rodent malaria. | the biosynthesis of the beta-hematin of malarial pigment (hemozoin) is catalyzed by a newly discovered enzyme, heme polymerase, which is described for plasmodium berghei in this report. this novel enzyme is present in the insoluble fraction of hemolysates of infected erythrocytes but is not present in normal erythrocytes. the substrate is ferriprotoporphyrin ix (fp) released from hemoglobin. at ph 5 and 37 degrees c the enzyme is saturated by 100 microm fp. the ph optimum is between 5 and 6 and ... | 1992 | 1474861 |
ultrastructural changes in the blood-brain barrier of mice infected with plasmodium berghei. | mice infected with the rodent malaria parasite plasmodium berghei exhibit ultrastructural changes of the blood-brain barrier during the course of infection. firm adherence including cellular interdigitation of infected cells or leucocytes and even clusters of cells to the vascular-endothelial lining is repeatedly observed early during infection. ghosts and membrane remnants can be found engulfed in the surface of the endothelial cells. frequently leucocytes migrate between endothelial cells and ... | 1992 | 1485495 |
application of a simple culture of plasmodium berghei for assessment of antiparasitic activity. | mouse erythrocytes infected with plasmodium berghei were incubated for a short period in microplate wells. the parasites changed morphologically from the immature ring form to mature schizonts, and free merozoites were released. however, reinvasion of the erythrocytes appeared not to be possible in this system. this intraerythrocytic one-step growth of the parasite could be determined quantitatively by counting incorporation of 3h-hypoxanthine. the incorporation was markedly decreased by additio ... | 1992 | 1487372 |
peptide binding to mhc class i proteins measured with a novel fluorescent technique. | an n-dansylated peptide derived from the plasmodium berghei circumsporozoite protein (pbcs 253-260) bound in an allele-specific manner to a single-chain kd molecule (sc-kd), and its binding resulted in significant fluorescent enhancement. the binding kinetics of unlabelled peptides could be determined by pre-incubating dansylated pbcs with a concentrated suspension of sc-kd, and then diluting this mixture in the presence of unmodified peptide. the time-dependence of the ensuing fluorescence decr ... | 1992 | 1493573 |
cyclical transmission of plasmodium berghei (coccidiida: plasmodiidae) by anopheles omorii (diptera: culicidae). | anopheles omorii, a tree-hole breeding anopheline collected in japan, transmitted a rodent malaria, plasmodium berghei anka strain, in the laboratory. mice with 0.2-15% parasitemia, 0.01-1.5% gametocytemia, and 0.001-0.5% exflagellations were used as infective hosts. oocyst numbers ranged from 2 to 171 (mean 44) on the midgut 8-16 d after the blood meal. several to hundreds of sporozoites were detected in the salivary glands 14 d after feeding. the mosquitoes were infective to mice from 13 to 40 ... | 1992 | 1495055 |
immunoprotection in mice susceptible to waning memory against the pre-erythrocytic stages of malaria after validated immunisation with irradiated sporozoites of plasmodium berghei. | the induction of immunity by irradiated sporozoites has been a bench-mark of immunological protection against the malaria parasite. herein we confirm that different mouse strains exhibit different susceptibilities to sporozoite-induced infection of plasmodium berghei. we note, however, that after hepatic schizogony, early parasite growth in the blood demonstrates no strain preference between c57bl/6 and balb/c mice. sporozoite-susceptible c57bl/6 mice, although initially protected by irradiated ... | 1992 | 1495922 |
dispiro-1,2,4,5-tetraoxanes: a new class of antimalarial peroxides. | dispiro-1,2,4,5-tetraoxanes 2-4 were synthesized as potential peroxide antimalarial drugs. they had curative activity against plasmodium berghei in vivo at single doses of 320 and 640 mg/kg which confirms earlier unpublished data. moreover, artemisinin (1) and 4 had equivalent ed50's against p. berghei in vivo in the multiple-dose thompson test; neither showed any evidence of acute toxicity at total doses of more than 12 g/kg. dispiro-1,2,4,5-tetraoxane 4 had ic50's comparable to those of 1 agai ... | 1992 | 1501229 |
[the search for new antiparasitic agents. 10. the synthesis, toxicological and antimalarial properties of nitrogen-containing heterocycles with a 4-(4-alkylpiperazinyl-1) phenylamine substituent (the preparation quinoprazine)]. | synthesis is described and acute toxicity and antimalaria action is studied in new derivatives of quinoline and benzo(g)quinoline containing a 4-(4-alkylpiperazinyl-1)phenylamine substitute. only the derivatives of benzo(g)quinoline were found to have a high antimalaria effect and to have advantages over the standard agent chloroquine on their tolerance and protective action. one of the compounds, 4-[4-(4-ethylpiperazinyl-1)phenylamino] benzo(g)quinoline, named quinoprazine, showed some action a ... | 1992 | 1508078 |
cytokines inhibit the development of liver schizonts of the malaria parasite plasmodium berghei in vivo. | the effect of induction of an acute-phase response and its mediators on the development of liver schizonts of the rodent malaria parasite plasmodium berghei was investigated in brown norway rats. subcutaneous injection of turpentine oil 24 h or 5 min before inoculation of sporozoites resulted in 80% and 35% reduction of schizont development, respectively. turpentine oil induced high plasma levels of interleukin-6 (il-6). intraperitoneal administration of il-1, il-6 or both, significantly reduced ... | 1992 | 1516619 |
a t cell clone directed at the circumsporozoite protein which protects mice against both plasmodium yoelii and plasmodium berghei. | clone b is a cytotoxic t cell clone induced by immunization with plasmodium yoelii sporozoites which recognizes an epitope on both the p. yoelii and plasmodium berghei circumsporozoite proteins. it is cd8, uses the v beta 8.1 tcr, and is kd restricted. when adoptively transferred, it protects mice against infection by both species of malaria sporozoites, and this protection is dependent on ifn-gamma. clone b cells are more broadly reactive and protective than previously described murine t cell c ... | 1992 | 1517574 |
binding of malarial circumsporozoite protein to sulfatides [gal(3-so4)beta 1-cer] and cholesterol-3-sulfate and its dependence on disulfide bond formation between cysteines in region ii. | region ii of the malaria circumsporozoite (cs) protein is highly conserved between the cs proteins of different species of malaria. amino acid sequences homologous to that of region ii are found in thrombospondin, properdin, von willebrand factor and a few other proteins. we show here that the native cs protein from the rodent parasite plasmodium berghei, and recombinant plasmodium vivax and plasmodium falciparum cs proteins containing region ii, but not recombinant proteins lacking region ii, s ... | 1992 | 1518521 |
comparison of effects of pyronaridine, amodiaquine, mefloquine and qinghaosu on rodent malaria. | blood schizontocidal effect of antimalarials were compared by 4-day suppressive test with an extended observation period of 31 days. on a drug-sensitive plasmodium berghei anka strain, pyronaridine (pnd) exhibited the best effect, followed by amodiaquine (adq), mefloquine (mfq), and qinghaosu (qhs). on a moderately chloroquine-resistant p. berghei ns line, the order of effects was the same, pnd greater than adq greater than mfq greater than qhs. on a highly pyronaridine-resistant p. berghei rp l ... | 1992 | 1523480 |
gametocytocidal and sporontocidal activity of antimalarials against plasmodium berghei anka in icr mice and anopheles stephensi mosquitoes. | the gametocytocidal and sporontocidal activity of three 8-aminoquinolines (primaquine, wr-238605, and wr-242511), three dihydroacridine-diones (floxacrine, wr-250547, and wr-250548), a 1,4-naphthoquinone (menoctone), a synthetic aminoalcohol (halofantrine), and a guanide (wr-182393) was determined against a cloned line of plasmodium berghei anka. gametocytocidal activity was assessed by treating mice with a single intraperitoneal inoculation of a given compound (25 mg base drug/kg mouse body wei ... | 1992 | 1539752 |
antimalarial properties of n-3 and n-6 polyunsaturated fatty acids: in vitro effects on plasmodium falciparum and in vivo effects on p. berghei. | the polyunsaturated fatty acids docosahexaenoic acid (c22:6,n-3), eicosapentaenoic acid, arachidonic acid, and linoleic acid caused marked in vitro growth inhibition of plasmodium falciparum, assessed by a radiometric assay. in contrast, negligible parasite killing was seen with oleic acid or docosanoic acid. parasite killing was significantly increased when oxidized forms of polyunsaturated fatty acids were used. antioxidants greatly reduced the fatty acid-induced killing. mice infected with p. ... | 1992 | 1541684 |
immunization with synthetic peptides containing a defined malaria epitope induces a highly diverse cytotoxic t lymphocyte response. evidence that two peptide residues are buried in the mhc molecule. | in the present study, we have explored ways of inducing a ctl response to a previously defined h-2kd mhc class i restricted epitope in the circumsporozoite (cs) protein of plasmodium berghei, and studied in detail the fine specificity of the response. we found that the s.c. injection of a variety of synthetic peptides emulsified in freund's adjuvant efficiently induced a specific ctl response in (balb/c x c57bl/6)f1 (h-2d x h-2b) mice. in contrast, balb/c mice responded only marginally, consiste ... | 1992 | 1541825 |
immunoenzymatic labeling of multiple plasmodial salivary gland sporozoites in a single test. | a direct, double- and triple-staining immunoenzymatic method detected and differentiated sporozoites by color in anopheles stephensi salivary glands and in mixed sporozoite slide preparations. a double-staining method used beta-galactosidase- and alkaline phosphatase-labeled monoclonal antibodies to the circumsporozoite (cs) proteins of plasmodium berghei and p. falciparum in mosquito salivary glands. the cs proteins were distinguished clearly by the blue-green and red substrate products of beta ... | 1992 | 1558271 |
effect of malaria on phenol conjugation pathways in perfused rat liver. | the effect of malaria infection (mi) on sulphation and glucuronidation of phenol was investigated in single-pass perfused livers from rats infected with the rodent malaria parasite plasmodium berghei. at a hepatic inflow (cin) phenol concentration of 1 microgram/ml in controls, 52% was metabolized to sulphate conjugate and 37% to glucuronide conjugate at steady state. at this cin, mi had no effect on phenol clearance (cl) (control: 9.63 +/- 0.38 vs mi: 9.65 +/- 0.36 ml/min; p greater than 0.05) ... | 1992 | 1562275 |
defined medium supporting development of cleansed plasmodium berghei ookinetes in anopheles stephensi. | hamsters blood infected with plasmodium berghei was cultured in vitro for the development of ookinetes. the ookinetes were separated from blood components, suspended in various defined media and fed to anopheles stephensi through a membrane. the development of the oocysts and infective sporozoites was recorded. mosquitoes infected with ookinetes suspended in l15 formulated into l15-b, l15-d (a medium specially modified for this purpose), ipl-41 or 199 media with no proteins added, developed at l ... | 1992 | 1563917 |
a comparative study of the kinetic changes of hemopoietic stem cells in mice infected with lethal and non-lethal malaria. | the kinetic changes of hemopoietic stem cells in bone marrow and spleen were compared between lethal plasmodium berghei- and non-lethal p. yoelii 17x-infected mice. p. yoelii 17x-infected mice showed more severe splenomegaly than those infected with p. berghei. p. yoelii 17x-infected mice also showed a greater degree of sustained increase in number of multipotent hemopoietic stem cells (colony-forming units in spleen: cfu-s) and committed stem cells for granulocytes and macrophages (cfu-gm) and ... | 1992 | 1563919 |
embryotoxic and growth-retarding effects of malaria on pregnant mice. | the effect of the malaria parasite, plasmodium berghei berghei, on reproductive physiology was studied in mice. three groups of randomly bred mice consisting of two groups of pregnant females and one group of nonpregnant females were used for the study. blood-induced infections in mice were used. endocrinologic evidence was found of an imbalance in endocrine function in the mice with infections. although there was an elevation in white blood cell counts, the red blood cell counts decreased as th ... | 1992 | 1564714 |
dietary fish-oil supplementation in experimental gram-negative infection and in cerebral malaria in mice. | dietary fish-oil supplementation interferes with eicosanoid production and appears to decrease production of interleukin-1 (il-1) and tumor necrosis factor (tnf). the effect of fish oil was investigated in an intramuscular klebsiella pneumoniae infection in swiss mice and in cerebral malaria induced by plasmodium berghei in c57b1/6 mice. after a low inoculum of k. pneumoniae, 90% of fish oil-fed mice survived; survival in control mice fed equal amounts of corn or palm oil or normal chow was 30%, ... | 1992 | 1569340 |
development of plasmodium berghei ookinetes to young oocysts in vitro. | the mosquito stage of plasmodium berghei was cultivated in vitro, with special attention to ookinete transformation into early oocyst. the ookinetes were obtained by in vitro culture of gametocytes taken from infected mice, purified by density gradient of metrizoic acid or a lymphocyte separation medium, and incubated either in acellular culture or in co-cultivations with mosquito cells. in acellular culture, the ookinetes were found to aggregate with each other and transformed from banana to ro ... | 1992 | 1578408 |
antimalarial activity of new dihydroartemisinin derivatives. 5. sugar analogues. | a series of dihydroartemisinin derivatives containing a sugar moiety was prepared in the search for analogues with good water solubility and high antimalarial activity. the preparation of the new compounds was achieved by treatment of dihydroartemisinin (2) with chlorotrimethylsilane in pyridine solution at -10 degrees c to give a nearly quantitative yield of 10-o-(trimethylsilyl)dihydroartemisinin (3), which was then condensed with 1-hydroxypolyacetylated sugars 5 to give dihydroartemisinin der ... | 1992 | 1578492 |