Browsing by Author "Perk N.E."

Now showing 1 - 2 of 2
  • No Thumbnail Available
    Item
    Comparison of liver extract medium with novy-macneal-nicolle medium and the molecular method for the diagnosis of leishmaniasis; [Layşmanyaz tanısı için karaciğer ekstreli besiyerinin novy-macneal-nicolle besiyeri ve moleküler yöntemle karşılaştırılması]
    (AVES, 2020) Özbilgin A.; Tünger Ö.; İnanır I.; Çavuş İ.; Perk N.E.; Özel Y.
    Objective: Diagnosis of Leishmaniasis is based on culture, mi-croscopic examination, serological tests, molecular methods. Novy-MacNeal-Nicolle (NNN) medium is mostly used for culture all over the world. The use of molecular methods for diagnostic purposes led to the questioning of the sensitivity of NNN medium. In this study, it is aimed to compare the performance of a new culture medium with those of NNN medium and the molecular method. Methods: Samples of 22 patients with suspected cutaneous leishmaniasis (CL) and 4 patients with suspected visceral leishmaniasis (VL) were sent to Manisa Celal Bayar University Faculty of Medicine Department of Medical Parasitology for diagnosis or confirmation from Kilis, Osmaniye, Bitlis, Gazian-tep and Manisa provinces. Pre-prepared media were sent to the health centers in these provinces and inoculation of these media with clinical samples was requested. Needle aspiration fluid for CL and bone marrow samples for VL were cultured simultaneously on NNN medium and newly developed liver extracted medium (LEM), and were sent to our institution with their smears. Smears were examined by staining with Giemsa method. In addition, parasite DNA was identified with real-time polymerase chain reaction method in these materials. Results: Leishmania amastigotes were detected in 14 of 26 samples. Promastigote proliferation was observed in 8 and 24 of the samples cultured in NNN and LEM respectively. No proliferation was detected by either method in samples of 2 patients with suspected CL. L. tropica, L. major and L. infantum/donovani were detected among isolates showing dermotropic location, and L. tropica and L. infantum/don-ovani were detected among isolates with viscerotropic location by genotyping. Conclusions: NNN medium, which is widely used in leishmaniasis di-agnosis, is not sensitive enough for the diagnosis of some Leishmania strains in Turkey. Therefore, an enrichment medium such as liver extract medium which we have presented in this study should be used for di-agnosis. However our results should be confirmed with more studies. Klimik Dergisi 2020; 33(2): 137-41. © 2020, AVES. All rights reserved.
  • No Thumbnail Available
    Item
    Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition
    (Elsevier Masson s.r.l., 2023) Istanbullu H.; Bayraktar G.; Karakaya G.; Akbaba H.; Perk N.E.; Cavus I.; Podlipnik C.; Yereli K.; Ozbilgin A.; Debelec Butuner B.; Alptuzun V.
    The leishmaniasis are a group of vector-borne diseases caused by a protozoan parasite from the genus Leishmania. In this study, a series of thiazolopyrimidine derivatives were designed and synthesized as novel antileishmanial agents with LmPTR1 inhibitory activity. The final compounds were evaluated for their in vitro antipromastigote activity, LmPTR1 and hDHFR enzyme inhibitory activities, and cytotoxicity on RAW264.7 and L929 cell lines. Based on the bioactivity results, three compounds, namely L24f, L24h and L25c, were selected for evaluation of their in vivo efficacy on CL and VL models in BALB/c mice. Among them, two promising compounds, L24h and L25c, showed in vitro antipromastigote activity against L. tropica with the IC50 values of 0.04 μg/ml and 6.68 μg/ml; against L. infantum with the IC50 values of 0.042 μg/ml and 6.77 μg/ml, respectively. Moreover, the title compounds were found to have low in vitro cytotoxicity on L929 and RAW264.7 cell lines with the IC50 14.08 μg/ml and 21.03 μg/ml, and IC50 15.02 μg/ml and 8.75 μg/ml, respectively. LmPTR1 enzyme inhibitory activity of these compounds was determined as 257.40 μg/ml and 59.12 μg/ml and their selectivity index (SI) over hDHFR was reported as 42.62 and 7.02, respectively. In vivo studies presented that L24h and L25c have a significant antileishmanial activity against footpad lesion development of CL and at weight measurement of VL group in comparison to the reference compound, Glucantime®. Also, docking studies were carried out with selected compounds and other potential Leishmania targets to detect the putative targets of the title compounds. Taken together, all these findings provide an important novel lead structure for the antileishmanial drug development. © 2022 Elsevier Masson SAS