Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy

Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines

Ampelographic and molecular characterisation of grapevine varieties in the gene bank of the experimental vineyard ‘Radmilovac’ – Serbia

Characterisations of thirty grapevine varieties (Vitis vinifera L.) from the experimental vineyard ‘Radmilovac’ were conducted using a large number of OIV descriptors and eight highly polymorphic microsatellite loci. The ampelographic description contained 45 features. Molecular characterisation of selected microsatellite loci was performed using capillary electrophoresis fragment analysis. Dendrograms based on ampelographic and genetic data resulted in three groups of varieties. Qualitative ampelographic characteristics tended to manifest significant differences. The most common deviation among varieties within the group was in the characteristic OIV 051 (colouration of the upper side of a young leaf). Genetic characterisation of SSR markers through analyses of a large number of varieties contributes to better organisation of grapevine collections and simpler identification of varieties, as well as data exchange. When identifying the varieties, the results of the DNA analysis should be combined with the ampelographic descriptors, in order to select grapevine varieties with desirable viticultural and oenological traits. Integration of the obtained genetic data with the ampelographic data is of utmost importance for accurate identification of the varieties and offers a significant means for the preservation and use of the varieties

Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374

Supplementary material for: [https://doi.org/10.1021/acs.jmedchem.5b01374]Related to published version: [http://cherry.chem.bg.ac.rs/handle/123456789/2036

Confirming infection of hop plants inoculated with Verticilium nonalfalfae

Hop (Humulus lupulus L.) is grown mostly as flavouring and bittering ingredient for beer and is also appreciated in the herbal and cosmetic industry, as well as in pharmacology. Among several diseases that damage hop growing, the most devastating in European hop production is verticillium wilt, caused by the soil-borne fungal pathogen Verticillium nonalfalfae. Colonization pattern and differential expression of selected genes after artificial infection of susceptible and resistant hop cultivars with V. nonalfalafae in stems and roots have been analysed recently Svara et al., 2019. Here, we present the dataset related to verification of plant samples infections after artificial inoculation (fungi- and mock-inoculated). After inoculation plant samples were tested for the positive infection by PCR amplification of the V. nonalfalfae ITS DNA region with species specific primers developed and optimised for this purpose. For more insight please see the article “Temporal and spatial assessment of defence responses in resistant and susceptible hop cultivars during infection with Verticillium nonalfalfae”