Abstract:
:BACKGROUND The main strategy to control human malaria still relies on specific drug treatment, limited now by Plasmodium falciparum-resistant parasites, including that against artemisinin derivatives. Despite the large number of active compounds described in the literature, few of them reached full development against human malaria. Drug repositioning is a fast and less expensive strategy for antimalarial drug discovery, because these compounds are already approved for human use. OBJECTIVES To identify new antimalarial drugs from compounds commercially available and used for other indications. METHODS Accuvit®, Ginkgo® and Soyfit®, rich in flavonoids, and also the standard flavonoids, hesperidin, quercetin, and genistein were tested against blood cultures of chloroquine-resistant P. falciparum, as well as chloroquine, a reference antimalarial. Inhibition of parasite growth was measured in immunoenzymatic assay with monoclonal anti-P. falciparum antibodies, specific to the histidine-rich protein II. Tests in mice with P. berghei malaria were based on percent of parasitaemia reduction. These compounds were also evaluated for in vitro cytotoxicity. FINDINGS The inhibition of parasite growth in vitro showed that Accuvit® was the most active drug (IC50 5 ± 3.9 μg/mL). Soyfit® was partially active (IC50 13.6 ± 7.7 μg/mL), and Ginkgo® (IC50 38.4 ± 14 μg/mL) was inactive. All such compounds were active in vivo at a dose of 50 mg/kg body weight. Accuvit® and quercetin induced the highest reduction of P. berghei parasitaemia (63% and 53%, respectively) on day 5 after parasite inoculation. As expected, the compounds tested were not toxic. MAIN CONCLUSIONS The antimalarial activity of Accuvit® was not related to flavonoids only, and it possibly results from synergisms with other compounds present in this drug product, such as multivitamins. Multivitamins in Accuvit® may explain its effect against the malaria parasites. This work demonstrated for the first time the activity of these drugs, which are already marketed.
journal_name
Mem Inst Oswaldo Cruzjournal_title
Memorias do Instituto Oswaldo Cruzauthors
Penna-Coutinho J,Aguiar AC,Krettli\/ AUdoi
10.1590/0074-02760180279subject
Has Abstractpub_date
2018-12-06 00:00:00pages
e180279issue
12eissn
0074-0276issn
1678-8060pii
S0074-02762018001200301journal_volume
113pub_type
杂志文章abstract::The effects of radiation on the reproductive capacity and the longevity of Panstrongylus megistus were studied. An indirect correlation between longevity and radiation doses was observed. Males were more affected than females. Longevity of females submitted to 10 Gy was not different when compared to controls. Some of...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761993000200004
更新日期:1993-04-01 00:00:00
abstract::The current drug options for the treatment of chronic Chagas disease have not been sufficient and high hopes have been placed on the use of genomic data from the human parasite Trypanosoma cruzi to identify new drug targets and develop appropriate treatments for both acute and chronic Chagas disease. However, the lack...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762009000800006
更新日期:2009-12-01 00:00:00
abstract::Triatoma brasiliensis is composed of at least four geographic populations (brasiliensis, melanica, macromelasoma, and juazeiro) that have distinct chromatic, morphologic, biologic and ecologic patterns, and genetic composition. Reciprocal crosses between all pairwise combinations were carried out in order to evaluate ...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762003000500009
更新日期:2003-07-01 00:00:00
abstract::In the present study, some morphological structures of antennae, maxillary palps and caudal setae of fourth instar larvae of laboratory-reared phlebotomine sand flies (Lutzomyia longipalpis, L. migonei, L. evandroi, L. lenti, L. sericea, L. whitmani and L. intermedia) of the State of Ceará, Brazil, were examined under...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762001000800013
更新日期:2001-11-01 00:00:00
abstract::Angiostrongylus costaricensis is the causative agent of abdominal angiostrongyliasis, a zoonotic infection that may produce severe eosinophilic enterocolitis or hepatitis in humans. Parasites are usually not released in stools and serology has an important role in diagnosis. Since cross-reactivity is demonstrated betw...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760200201
更新日期:2020-09-21 00:00:00
abstract::Several factors appear to affect vertical HIV-1 transmission, dependent mainly on characteristics of the mother (extent of immunodeficiency, co-infections, risk behaviour, nutritional status, immune response, genetical make-up), but also of the virus (phenotype, tropism) and, possibly, of the child (genetical make-up)...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章,评审
doi:10.1590/s0074-02762001000100001
更新日期:2001-01-01 00:00:00
abstract::BACKGROUND Paracoccidioides spp. causes paracoccidioidomycosis (PCM), an important and frequent systemic mycosis that occurs in Latin America. The infectious process begins with contact between the fungus and lung cells, and the molecular pattern of this interaction is currently poorly understood. MicroRNAs (miRNAs) a...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760200238
更新日期:2020-01-01 00:00:00
abstract::Three Yersinia pestis strains isolated from humans and one laboratory strain (EV76) were grown in rich media at 28 degrees C and 37 degrees C and their outer membrane protein composition compared by sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS-PAGE). Several proteins with molecular weights ranging f...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761990000100018
更新日期:1990-01-01 00:00:00
abstract::Coronavirus disease 2019 (COVID-19) caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly contagious infection that may break the healthcare system of several countries. Here, we aimed at presenting a critical view of ongoing drug repurposing efforts for COVID-19 as well as discussing ...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760200254
更新日期:2020-10-02 00:00:00
abstract::An unusually high incidence of microcephaly in newborns has recently been observed in Brazil. There is a temporal association between the increase in cases of microcephaly and the Zika virus (ZIKV) epidemic. Viral RNA has been detected in amniotic fluid samples, placental tissues and newborn and fetal brain tissues. H...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760160085
更新日期:2016-05-01 00:00:00
abstract::Citral, the main constituent of lemongrass (Cymbopogon citratus) essential oil, was added to Trypanosoma cruzi cultures grown in TAU3AAG medium to observe the effect on the epimastigote-to-trypomastigote differentiation process (metacyclogenesis). Our results showed that citral (20 μg/mL) did not affect epimastigote v...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762010000800012
更新日期:2010-12-01 00:00:00
abstract::The yield as well as phenotypic and functional parameters of canine peripheral blood monocyte-derived macrophages were analyzed. The cells that remained adherent to Teflon after 10 days of culture had high phagocytic activity when inoculated with Leishmania chagasi. Flow cytometric analysis demonstrated that more than...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762005000500012
更新日期:2005-08-01 00:00:00
abstract::To compare the epidemiological profile and socioeconomic factors associated to the infection by Schistosoma mansoni in a rural and an urban endemic area a cross-sectional study was performed in Agua Branca de Minas (rural area) and Bela Fama (urban area), both situated in the State of Minas Gerais, Brazil. Two hundred...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761997000500001
更新日期:1997-09-01 00:00:00
abstract::A pleiotropic response to the calpain inhibitor MDL28170 was detected in the tomato parasite Phytomonas serpens. Ultrastructural studies revealed that MDL28170 caused mitochondrial swelling, shortening of flagellum and disruption of trans Golgi network. This effect was correlated to the inhibition in processing of cru...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760160270
更新日期:2017-01-01 00:00:00
abstract::In many helminth infected hosts the number of eosinophils increases dramatically, often without any concurrent increases in the number of other leukocytes, so that eosinophils become the dominant cell type. Many experimental investigations have shown that the eosinophilia is induced by interleukin-5 (IL-5) but its fun...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章,评审
doi:10.1590/s0074-02761997000800013
更新日期:1997-01-01 00:00:00
abstract::The vaccine Bacillus of Calmette Guérin (BCG) was originally developed in France as an oral vaccine against tuberculosis. The oral use of this vaccine was replaced by the parenteral route in almost all countries after the Lubeck disaster. In contrast, Brazil retained the oral delivery of the vaccine until the mid-seve...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 历史文章,杂志文章,评审
doi:10.1590/s0074-02762005000500002
更新日期:2005-08-01 00:00:00
abstract::The invasion of the erythrocyte by Plasmodium falciparum depends on the ability of the merozoite to move through the membrane invagination. This ability is probably mediated by actin dependent motors. Using affinity columns with G-actin and F-actin we isolated actin binding proteins from the parasite. By immunoblottin...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762000000300007
更新日期:2000-05-01 00:00:00
abstract::This study objective was to evaluate the cytokines associated with early events of hepatic fibrosis in schistosomiasis mansoni. Hepatic fibrosis was classified by ultrasonography in 94 patients. Immunological evaluation was performed by measurement of secreted cytokines (interleukin IL-5, IL-10, IL-13, interferon-gamm...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762004000900004
更新日期:2004-01-01 00:00:00
abstract::In a recent issue of Memórias do Instituto Oswaldo Cruz, published in Rio de Janeiro in February 2014 (109: 87-92), Adami et al. have published a survey reporting Mansonella parasite prevalence in the Amazon Region. This report makes a useful contribution to the existing knowledge of filarial parasite distribution wit...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-0276140079
更新日期:2014-07-01 00:00:00
abstract::The main purpose of the present study was to examine if there is difference in terms of incidence rates of congenital toxoplasmosis among populations assisted in public and private hospitals from Uberlândia, state of Minas Gerais, Brazil. A total of 805 serum samples from cord blood were collected, being 500 from publ...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762004000100002
更新日期:2004-02-01 00:00:00
abstract::A list of 41 Apoidea (Hymenoptera) type specimens deposited in the Entomological Collection of the Instituto Oswaldo Cruz, Rio de Janeiro, RJ, Brazil is presented. The types previously belonged to the Zikán and Schrottky private collections. A total of 11 holotypes and 30 paratypes are listed with their respective dat...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761997000300009
更新日期:1997-05-01 00:00:00
abstract::Aedes albopictus was found in six of the 10 departments of Haiti and in 14 of the 35 communes surveyed. The survey found the larvae of Ae. albopictus in 13 different types of containers. Used tires and tins were by far the most common breeding sites used by this mosquito species. At the breeding sites, Ae. albopictus ...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762012000200020
更新日期:2012-03-01 00:00:00
abstract::Through its life cycle from the insect vector to mammalian hosts Trypanosoma cruzi has developed clever strategies to reach the intracellular milieu where it grows sheltered from the hosts' immune system. We have been interested in several aspects of in vitro interactions of different infective forms of the parasite w...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761999000700014
更新日期:1999-01-01 00:00:00
abstract::Respiratory failure (RF) is the main cause of hospital admission in HIV/AIDS patients. This study assessed comorbidities and laboratory parameters in HIV/AIDS inpatients with RF (N = 58) in relation to those without RF (N = 36). Tuberculosis showed a huge relative risk and platelet counts were slightly higher in HIV/A...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/0074-02760200082
更新日期:2020-09-14 00:00:00
abstract::Two new species of the Culicoides paraensis species group, C. diversus Felippe-Bauer and C. peruvianus Felippe-Bauer, are described and illustrated based on female specimens from Amazonian region of Peru. A systematic key, table with numerical characters of females, and distribution of species of the C. paraensis grou...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762003000800014
更新日期:2003-12-01 00:00:00
abstract::A shift from large to small average sizes was observed in Triatoma infestans and Rhodnius domesticus between field and domestic (or laboratory) conditions of life. It was more pronounced in the female specimens, leading to a subsequent reduction of sexual size dimorphism. This feature is discussed in terms of genetic ...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761999000400024
更新日期:1999-07-01 00:00:00
abstract::The great difficulties in treating people and animals suffering from cryptosporidiosis have prompted the development of in vitro experimental models. Due to the models of in vitro culture, new extracellular stages of Cryptosporidium have been demonstrated. The development of these extracellular phases depends on the t...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02762007005000071
更新日期:2007-08-01 00:00:00
abstract::Mycobacteria, specially Mycobacterium tuberculosis are among the micro-organisms that are increasing dramatically the number of infections with death, all over the world. A great number of animal experimental models have been proposed to investigate the mechanisms involved in the host response against these intracellu...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章,评审
doi:10.1590/s0074-02761997000800033
更新日期:1997-01-01 00:00:00
abstract::An important point in paleoparasitology is the correct diagnosis of the origin of coprolites found in archaeological sites. The identification of human and animal coprolites, through the study of the shape, size, characteristics after rehydration, alimentary contents, and the presence of parasites, has proved to be ac...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章
doi:10.1590/s0074-02761989000200007
更新日期:1989-04-01 00:00:00
abstract::A rational method of search for natural neolignans of desired structures is outlined. This involves consultation of a collection of chemical profiles of plant families. The profiles are assembled considering the biosynthetic class (in the present case lignoids), subclass (neolignans), structural types (neolignan skele...
journal_title:Memorias do Instituto Oswaldo Cruz
pub_type: 杂志文章,评审
doi:10.1590/s0074-02761991000600009
更新日期:1991-01-01 00:00:00