Abstract:
:Leishmaniasis is an epidemic in various countries, and the parasite Leishmania donovani is developing resistance against available drugs. In the present study the antileishmanial action of piperolactam A (PL), isolated after bioactivity guided fractionation from root extracts of Piper betle was accentuated in detail. Activity potentiation was achieved via cyclodextrin complexation. Crude hydro-ethanolic extract (PB) and three fractions obtained from PB and fabricated PL-hydroxypropyl-β-cyclodextrin (HPBCD) nanoparticles were evaluated for antileishmanial activity. Tests were performed against L. donovani wild-type, sodium stibogluconate, paromomycin and field isolated (GE1) resistant strains in axenic amastigote and amastigote in macrophage models. PL-HPBCD complex was characterized and FITC loaded HPBCD nanoparticles were assessed for macrophage internalization in confocal microscopic studies. Isolated and purified PL from most potent, alkaloid rich ethyl acetate fraction of PB showed high level of antileishmanial activities in wild-type (IC50=36 μM), sodium stibogluconate resistant (IC50=103 μM), paromomycin resistant (IC50=91 μM) and field isolated resistant (IC50=72 μM) strains together with cytotoxicity (CC50=900 μM) in mouse peritoneal macrophage cells. Inclusion of PL in HPBCD nanoparticles resulted in 10-fold and 4-10-fold increase in selectivity indexes (CC50/IC50) for wild-type and drug resistant strains, respectively. Drug-carrier interactions were clearly visualized in FT-IR studies. Complete incorporation of PL in HPBCD cavity was ascertained in DSC and XRD analyses. 180nm size stable nanospheres showed macrophage internalization within 1h of incubation. Piperolactam A (PL), a representative of the inchoate skeleton of aristolactam chassis might be the source of safe and affordable antileishmanial agents for the cure of deadly Leishmania infections.
journal_name
Acta Tropjournal_title
Acta tropicaauthors
Bhattacharya P,Mondal S,Basak S,Das P,Saha A,Bera Tdoi
10.1016/j.actatropica.2016.02.017subject
Has Abstractpub_date
2016-06-01 00:00:00pages
97-106eissn
0001-706Xissn
1873-6254pii
S0001-706X(16)30079-1journal_volume
158pub_type
杂志文章相关文献
ACTA TROPICA文献大全abstract::This study was conducted to determine the effects of increased water temperatures on the development of Aedes aegypti immatures under laboratory conditions in Trinidad, West Indies using temperature regulated water baths to cover a range of temperatures from 24-25°C to 34-35°C at a relative humidity of 80%. Two experi...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2011.04.004
更新日期:2011-07-01 00:00:00
abstract::Eighty Leishmania isolates from patients who contracted cutaneous leishmaniasis in the Manaus region, Amazonas State, Brazil, were identified as Leishmania (Viannia) guyanensis by the electrophoretic profiles of six enzymes. None reacted with the species-specific monoclonal antibody B19. Two L. (V.) guyanensis subpopu...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/s0001-706x(02)00002-5
更新日期:2002-04-01 00:00:00
abstract::Free Living Amoebae (FLA) of Acanthamoeba genus are widely distributed in the environment and can be found in the air, soil and water; and have also been isolated from air-conditioning units. In humans, they are causative agents of a sight-threating infection of the cornea, Acanthamoeba keratitis (AK) and a fatal infe...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2013.10.006
更新日期:2014-02-01 00:00:00
abstract::Cysticercosis caused by the larvae of Taenia solium is a serious and emerging threat to public health in the endemic areas as well as in the non-endemic areas. Neurocysticercosis, an affection of the central nervous system is a leading cause of epilepsy in endemic areas. This study was carried out to investigate human...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2015.12.019
更新日期:2017-01-01 00:00:00
abstract::Loop-mediated isothermal amplification (LAMP) is a novel molecular method that accelerates and facilitates DNA amplification and detection under isothermal conditions. It represents a revolution in molecular biology by reducing the high cost, turnaround time and technicality of polymerase chain reaction and other ampl...
journal_title:Acta tropica
pub_type: 杂志文章,评审
doi:10.1016/j.actatropica.2012.02.004
更新日期:2012-06-01 00:00:00
abstract::Two high-throughput assays for the identification of members of the Anopheles gambiae sensu lato species complex have recently been reported. These methods, are based on TaqMan single nucleotide polymorphism (SNP) genotyping that enables rapid scoring of mosquito DNA samples in real-time PCR reactions. Unfortunately, ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2008.04.009
更新日期:2008-07-01 00:00:00
abstract::The identification and characterization of Leishmania are relevant to diagnosis, treatment, eco-epidemiology studies, prophylactic measures and control of the disease. Two strains of Leishmania (MHOM/BR/1971/BH49 and MHOM/BR/1971/BH121), isolated from human cutaneous leishmaniasis, were studied using biological and mo...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2009.07.026
更新日期:2009-12-01 00:00:00
abstract::The chewing lice (Mallophaga) are common parasites of different animals. Most of them infest terrestrial and marine birds, including pigeons, doves, swans, cormorants and penguins. Mallophaga have not been found on marine mammals but only on terrestrial ones, including livestock and pets. Their bites damage cattle, sh...
journal_title:Acta tropica
pub_type: 杂志文章,评审
doi:10.1016/j.actatropica.2017.05.031
更新日期:2018-01-01 00:00:00
abstract::The Kato-Katz technique is the method routinely used for diagnosing human schistosomiasis mansoni by estimating faecal egg burdens. To improve the sensitivity of faecal diagnosis, we established and validated a novel separation technique based upon the greater density of viable schistosome eggs relative to faecal mate...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/s0001-706x(02)00089-x
更新日期:2002-08-01 00:00:00
abstract::Antigen-detection enzyme immunoassays (ELISA) were used for the diagnosis of Trypanosoma vivax, T. congolense and T. brucei in N'Dama cattle in Gabon, Central Africa. The assays are based on monoclonal antibodies which recognise trypanosome antigens specific for each of the three species and animals were termed 'antig...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/0001-706x(91)90068-u
更新日期:1991-11-01 00:00:00
abstract::The anthelmintic activity of 11 benzimidazole derivatives (A1-A11) and 2 thioureides N,N'-disubstituted (B1-B2) was determined. Each compound and albendazole was tested in vitro against Toxocara canis larvae and in vivo against Hymenolepis nana adult. Compounds A1-A6 and B1-B2 were designed as albendazole prodrugs. Co...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2008.11.014
更新日期:2009-03-01 00:00:00
abstract::We report results of Trypanosoma cruzi infection and parasite genotypes in the wild Octodon degus and synantropic reservoir Rattus rattus from an endemic area with sylvatic Triatoma infestans as the only detected vector. The infection status was determined by hemi-nested PCR directed to minicircles DNA and genotyping ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2009.02.010
更新日期:2009-07-01 00:00:00
abstract::In Triatominae, female fecundity and fertility may be affected by age, adult nutritional status (i.e., blood meal source and amount of blood ingested) and number of matings. Triatoma infestans (Klug) is the main vector of Chagas disease in southern South America and considering that reproductive success is intimately ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2011.05.015
更新日期:2011-08-01 00:00:00
abstract::Several approaches have been developed for diagnosis of Theileria equi infection in horses and donkeys but all of them have limitations in practice. Due to numerous strengths including easy operation, cheapness and high sensitivity and specificity, LAMP has been already extensively used for surveillance of a number of...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2013.05.007
更新日期:2013-09-01 00:00:00
abstract::Three Entamoeba spp. including E. suis, zoonotic E. polecki, and E. histolytica, have been described in pigs to date. However, little is known about the molecular epidemiology of these neglected parasites in pigs globally. In this study we surveyed the occurrence and molecular epidemiology of porcine Entamoeba spp. in...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2018.06.020
更新日期:2018-09-01 00:00:00
abstract::Essential oils (EOs) are potential tools for controlling Musca domestica L. In a fumigant assay, M. domestica adults treated with Citrus sinensis EO (LC50=3.9mg/dm(3)), with (4R)(+)-limonene (95.1%) being its main component, died within 15min or less. The terpenes absorbed by the flies and their metabolites, analyzed ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2013.03.009
更新日期:2013-07-01 00:00:00
abstract::A case of ectopic lesion of Schistosoma haematobium of the penis with extensive tissue destruction, simulating an early carcinoma of the penis and almost resulting in an autoamputation of the crown of the penis, is presented. The penis was surgically repaired and the patient treated with ambilhar. In schistosoma endem...
journal_title:Acta tropica
pub_type: 杂志文章
doi:
更新日期:1978-09-01 00:00:00
abstract::It has been reported a higher seroprevalence of HBV and HCV in leprosy patients than in the general population, but the reasons for these findings are not yet clear. On the other hand, there is evidence that these viruses may influence the onset of leprosy reactional episodes, an important cause of neurological sequel...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2017.04.024
更新日期:2017-08-01 00:00:00
abstract::The semiargenteus-subgroup of the Tabanus bovinus species group is reviewed. The known distribution area of the three previously known species could be significantly increased. T. semiargenteus Olsufjev, 1937 was for the first time recorded from Syria and Iran, T. olsufjevi Hauser, 1960 from Iraq and Iran and T. sarba...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2014.04.027
更新日期:2014-09-01 00:00:00
abstract::The efficacy of a 5-day treatment with intramuscular artemether (3.2-mg/kg loading dose followed by 1.6 mg/kg daily) was compared to that of the standard 7-day treatment with quinine (20-mg/kg loading dose followed by 10 mg/kg every 8 h) in a randomised clinical trial including 103 children aged 12-60 months with cere...
journal_title:Acta tropica
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0001-706x(99)00031-5
更新日期:1999-10-15 00:00:00
abstract::A simple, rapid and inexpensive method for the extraction of DNA from filarial vector, Culex quinquefasciatus, useful in Ssp I PCR assay for xenomonitoring of infection with Wuchereria bancrofti is presented. The DNA extracted by this method was found suitable for PCR detection of W. bancrofti infection in pools of 10...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/s0001-706x(02)00267-x
更新日期:2003-04-01 00:00:00
abstract::The incidence of Echis carinatus (saw-scaled or carpet viper) bite and its mortality have been investigated in the Nigerian savanna region. A geographical area was defined in which the snake was particularly abundant and bites were frequent. Perennial and seasonal fluctuations in incidence and mortality, the circumsta...
journal_title:Acta tropica
pub_type: 杂志文章
doi:
更新日期:1976-01-01 00:00:00
abstract::Sm14 and paramyosin are two major Schistosoma mansoni vaccine candidate antigens. Recently, we have identified Sm14 and paramyosin epitopes that are recognized by T cells of resistant individuals living in endemic areas for schistosomiasis. Herein, mice were immunized with these peptides separately or in association i...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2008.03.003
更新日期:2008-06-01 00:00:00
abstract::Chronic malaria severely affects the immune system and causes polyclonal B-cell activation, as evidenced by the presence of hypergammaglobulinemia, elevated levels of autoantibodies, loss of B-cell memory and the frequent occurrence of Burkitt's lymphomas (BL) in children living in malaria endemic areas. Previous stud...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2011.05.005
更新日期:2011-08-01 00:00:00
abstract::In sub-Saharan Africa, tick infestation and tick-borne infections together with tsetse-transmitted trypanosomosis arguably constitute the main parasitological disease complex constraining livestock production. Resistance to tick attack and tick-borne micro-organisms (TBMs) varies among different breeds of cattle. The ...
journal_title:Acta tropica
pub_type: 杂志文章,评审
doi:10.1016/s0001-706x(00)00063-2
更新日期:2000-05-31 00:00:00
abstract::A large-scale control trial against Glossina palpalis palpalis was carried out in the Congo using a new trapping technique. In the same way a test related to the experimental utilization of sentinel animals was performed, concurrently to the classical epidemiological and entomological evaluation. 564 domestic animals ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:
更新日期:1988-12-01 00:00:00
abstract::Manipulating the endogenous immune responses of the mosquito such as temporal and spatial expression of antimicrobial peptides may help in the development of a refractory mosquito, unable to transmit malaria. In mosquito several small antimicrobial peptides are activated locally in the midgut and salivary glands upon ...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2008.01.001
更新日期:2008-04-01 00:00:00
abstract::Accumulation, degradation and excretion by the host of helminth metabolic end products, such as branched-chain volatile fatty acids are poorly studied although they play an appreciable role in host-parasite interactions and, being detectable in excreta, provide a reliable diagnostic test for at least some helminthiase...
journal_title:Acta tropica
pub_type: 杂志文章
doi:
更新日期:1981-12-01 00:00:00
abstract::Cattle were exposed to natural trypanosome challenge in an area of high Glossina density (Samandéni, Burkina Faso) for various periods of time during 1982, 1983, 1984 and 1985. All of 30 Zebu proved to be sensitive to trypanosomiasis i.e. they died or were treated in extremis in 10 +/- 4 weeks. Twenty-one (31%) Baoulé...
journal_title:Acta tropica
pub_type: 杂志文章
doi:
更新日期:1987-03-01 00:00:00
abstract::Historically, the whole of Burkina Faso was considered to be endemic for onchocerciasis (except a small area in the far north of the country) with prevalence rates 60-80%, but all endemic areas were included in the World Health Organisation Onchocerciasis Control Programme, which operated a system of vector control by...
journal_title:Acta tropica
pub_type: 杂志文章
doi:10.1016/j.actatropica.2018.05.013
更新日期:2018-09-01 00:00:00