Browsing by Author "Cavus I."

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    Antileishmanial activity of selected Turkish medicinal plants
    (University of Benin, 2014) Ozbilgin A.; Durmuskahya C.; Kayalar H.; Ertabaklar H.; Gunduz C.; Ural I.O.; Zeyrek F.; Kurt O.; Cavus I.; Balcıoglu C.; Toz S.O.; Ozbel Y.
    Purpose: To determine the in vitro and in vivo anti-leishmanial activities of extracts obtained from Centaurea calolepis, Phlomis lycia, Eryngium thorifolium, Origanum sipyleum and Galium incanum ssp. centrale.; Methods: To estimate the cytotoxicity of plant extracts, WST-1 assay was used. Parasite inhibition in the presence of plant extracts (25-500 μg/ml) in comparision with control group and reference group (glucantime, 25 μg/ml) at 12-72 h were determined in vitro on L. tropica promastigotes. The in vivo leishmanicidal activity of the extracts was evaluated against L. tropica-infected mice with glucantime as reference drug.; Results: The chloroform extract of Galium incanum ssp. centrale showed the highest cytotoxicity with IC50 value of 0.0316 ± 0.005 μg/ml. In vitro parasite inhibition by the plant extracts ranged between 16.7 ± 0.01 % and 100 ± 0.00 % at 25 μg/ml concentration. The methanol extract of Eryngium thorifolium possessed the highest activity on promastigotes of L. tropica with 100 % inhibition at 25 μg/ml. The water and chloroform extracts of C. calolepis and water and methanol extracts of E. thorifolium at a dose of 100 mg/kg reduced parasitaemia in L. tropica infected mice.; Conclusion: Parasite viability results suggest that the methanol extract of Eryngium thorifolium, regarded as non-cytotoxic, is a promising candidate drug for treating L. tropica infection. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved.
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    Leishmaniasis in Turkey: Determination of Leishmania species by matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF MS)
    (Tehran University of Medical Sciences (TUMS), 2014) Culha G.; Akyar I.; Yildiz Zeyrek F.; Kurt Ö.; Gündüz C.; Özensoy Töz S.; Östan I.; Cavus I.; Gülkan B.; Kocagöz T.; Özbel Y.; Özbilgin A.
    Background: Cutaneous leishmaniasis (CL) is endemic in Southeastern Anatolia, mainly in Sanliurfa and Hatay provinces, and the causative agents are mostly Leishmania tropica and less frequently L. infantum. Here, we report the first MALDI-TOF analyses of Leishmania promastigotes obtained from the cultures of two CL cases from Osmaniye and Hatay provinces who were initially diagnosed by microscopy, culture and identified as L. infantum with Real-Time PCR (RT-PCR). Methods: Samples obtained from the skin lesions of patients were initially stained with Giemsa and cultivated in NNN medium. Examination of the smears and cultures revealed Leishmania amastigotes and promastigotes, respectively. The promastigotes (MHOM/TR/2012/CBU15 and MHOM/TR/2012/MK05) obtained from the cultures of both patients were used for RT-PCR targeting the ITS-1 region in the SSU of rRNA. The reference strains of four Leishmania species (L. infantum, L. donovani, L. tropica and L. major) were initially assessed with MALDI-TOF and their data were added to MALDI-TOF Biotyper Library. Results: Both RT-PCR and MALDI-TOF analyses indicated that the causative agent in both patient samples was L. infantum. Conclusion: Despite disadvantages such as requirement of culture fluid with nothing but promastigotes and high cost, MALDI-TOF analysis may be a fast, sensitive and specific diagnostic tool in especially large-scale research studies, where the cost declines, relatively.
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    In vivo antimalarial activity of methanol and water extracts of Eryngium thorifolium boiss (apiaceae family) against P. berghei in infected mice
    (University of Benin, 2014) Ural I.O.; Kayalar H.; Durmuskahya C.; Cavus I.; Ozbilgin A.
    Purpose: To investigate the in vivo antimalarial effect of Eryngium thorifolium, an endemic plant in Turkey. Methods: The methanol and water extracts were prepared and phytochemical analysis conducted on the extracts. Twenty four healthy Balb/c male mice, divided into 4 groups (n = 6), were infected intravenously with Plasmodium berghei and 100 - 250 mg/kg plant extracts administered orally in a single dose per day for 5 days. The untreated group of mice received normal saline solution and chloroquine (standard drug) served as reference drug. Results: The water extract group (250 mg/kg) prolonged the survival of the mice by 6 days compared with the untreated mice while the mice that received choloroquine treatment remained alive at the end of the study of the mice. In the untreated control group, maximum parasitaemia was observed on the 10th day of infection whereas The water extract exhibited some degree of antiplasmodial activity compared to untreated control group. The mice of chloroquine treated group remained alive at the end of the study with 100 % chemosuppression (p < 0.05). In the untreated control group, maximum parasitaemia was observed on the 10th day of infection whereas in the water extract group maximum parasitaemia was attained on the 16th day of infection. The water extract of the plant showed 45.85 % chemosuppression. Phytochemical screening of the water and methanol extracts revealed the presence of flavonoids, terpenoids and tannins. Anthraquinones were positive for water extract. Conclusions: The possible active compounds responsible for the observed chemosupression may be flavonoids, terpeneoids and anthraquinones which are present in the extract. This is the first report on the in vivo antimalarial activity of E. thorifolium. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved.
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    Design, synthesis, and in vitro biological evaluation of novel thiazolopyrimidine derivatives as antileishmanial compounds
    (Wiley-VCH Verlag, 2020) Istanbullu H.; Bayraktar G.; Akbaba H.; Cavus I.; Coban G.; Debelec Butuner B.; Kilimcioglu A.A.; Ozbilgin A.; Alptuzun V.; Erciyas E.
    A series of thiazolopyrimidine derivatives was designed and synthesized as a Leishmania major pteridine reductase 1 (LmPTR1) enzyme inhibitor. Their LmPTR1 inhibitor activities were evaluated using the enzyme produced by Escherichia coli in a recombinant way. The antileishmanial activity of the selected compounds was tested in vitro against Leishmania sp. Additionally, the compounds were evaluated for cytotoxic activity against the murine macrophage cell line RAW 264.7. According to the results, four compounds displayed not only a potent in vitro antileishmanial activity against promastigote forms but also low cytotoxicity. Among them, compound L16 exhibited an antileishmanial activity for both the promastigote and amastigote forms of L. tropica, with IC50 values of 7.5 and 2.69 µM, respectively. In addition, molecular docking studies and molecular dynamics simulations were also carried out in this study. In light of these findings, the compounds provide a new potential scaffold for antileishmanial drug discovery. © 2020 Deutsche Pharmazeutische Gesellschaft
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    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