Şaban Tekin

Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives

In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80.51-97.02% compared to 5-FU. Some of the compounds exhibited anti-microbial activity. Also, they evaluated for inhibition effects against human carbonic anhydrase I, and II isoenzymes (hCA I and II) with Ki values in the range of 405.26-635.68pM for hCA I, and 245.40-489.60pM for hCA II, respectively. These results demonstrated that 3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives could be used in different biomedical applications.

Simple and convenient preparation of novel 6,8-disubstituted quinoline derivatives and their promising anticancer activities

A short and easy route is described for 6,8-disubstituted derivatives of quinoline and 1,2,3,4-tetrahydroquinoline from 6,8-dibromoquinolines 2 and 7 by various substitution reactions. While copper-promoted substitution of 6,8dibromide 2 produced monomethoxides 3 and 4, a prolonged reaction time mainly afforded dimethoxide 6 instead of 5, whose aromatization with DDQ and substitution reaction of dibromide 7 with NaOMe in the presence of CuI also gave rise to dimethoxide 6. Several 6,8-disubstituted quinolines were obtained by treatment of 6,8-dibromoquinoline (7) with n -BuLi followed by trapping with an electrophile [Si(Me)3Cl, S2 (Me)2, and DMF]. Furthermore, 7 was also converted to mono and dicyano derivatives. The anticancer activities of compounds 2, 7, 6, 12, 13, 15, and 16 against HeLa, HT29, and C6 tumor cell lines were tested, and 6,8-dibromo-1,2,3,4-tetrahydroquinoline (2) and 6,8-dimethoxyquinoline (6) showed significant anticancer activities against the tumor cell lines.

Synthesis and characterization of two novel dicyanidoargentate(I) complexes containing N-(2-hydroxyethyl)ethylenediamine exhibiting significant biological activity

Two novel cyanido-bridged bimetallic polymeric complexes, [Ni(hydeten)2Ag(CN)2] [Ag(CN)2]·H2O (C1) and [Cd2(hydeten)2Ag4(CN)8]·H2O (C2) (hydeten: N-(2-hydroxyethyl)ethylenediamine) were synthesized and characterized by elemental, FT-IR, X-ray (C2), thermal and variable temperature magnetic measurement (C1) techniques. Their anticancer, antibacterial and antifungal effects were also investigated. The crystallographic analyses showed that C2 crystallizes in the monoclinic space group P21/c and shows a 3D 6,4 ladder-type polymeric chain in which the CdII centers are linked by [Ag(CN)2]− units. The Ag⋯Ag distance exhibits a short value of 3.1365(9) A. It features a rare linear pentameric unit of [Ag(CN)2]− ions assembled via d10–d10 interaction as building blocks. Both complexes exhibited outstanding antibacterial, antifungal and anticancer activities against ten different bacterial strains, two plant pathogenic fungi (Alternaria solani and Rhizoctonia solani) and four tumor cell lines (HT-29, HeLa, C6 and Vero), respectively.

Gene expression analysis of metallothionein and mineral elements uptake in tomato (Solanum lycopersicum) exposed to cadmium

Heavy metals such as Cd are considered to be the most important pollutants in soil contamination. Cd is a non-essential element adversely affecting plant growth and development, and it has caused some physiological and molecular changes. Metallothioneins (MTs) are low molecular weight, cysteine-rich, and metal binding proteins. In this study, we aimed to evaluate the MT gene expression levels and minerals uptake in the tissues of Solanum lycopersicum exposed to Cd. The transcriptional expression of the MT genes was determined by real-time quantitative PCR. The MT genes were regulated by the Cd and the mineral elements uptake changed tissue type and applied doses. The MT1 and MT2 transcript levels increased in the roots, the leaves and the fruits of the tomato. The MT3 and MT4 transcript pattern changed according to the tissue types. The Cd treatment on the growth medium increased the Mg, Ca, and Fe content in both the leaves and fruits of the tomato. However, the Cd affected the mineral levels in the roots depending on the mineral types and doses. Also, the Cd content increased in the roots, the leaves, and the fruits of the tomato, respectively. The results presented in this study show that Cd has synergistic and/or antagonistic effects on minerals depending on the tissue types. These results indicate that the MT1 and MT2 expression pattern increased together with the Mg, Ca, and Fe content in both the leaves and the fruits of the tomato.

Five novel dicyanidoaurate(I)-based complexes exhibiting significant biological activities: synthesis, characterization and three crystal structures

Five new cyanido-bridged coordination polymers having closed formulae [Ni(hydeten)Au2(CN)4] (C1), [Ni(hydeten)2Au2(CN)4]·H2O (C2), [Cu(hydeten)2Au2(CN)4]·CH3OH (C3), [Zn(hydeten)2 Au2(CN)4]·H2O (C4), and [Cd(hydeten)2Au2(CN)4]·H2O (C5) (hydeten: N-(2-hydroxyethyl)-ethylenediamine) have been prepared and characterized by elemental, thermal, FT-IR and XRD (C3, C4 and C5) measurement techniques. The anticancer, antibacterial and antifungal activities of the complexes are also investigated. The C3, C4 and C5 units according to XRD analyses are linked to each other via –CN–M(hydeten)–NC–Au(1)–CN–M(hydeten)–CN– chains (MII = Cu, Zn and Cd) and aurophilic interacted –Au(1)(CN)2–Au(2)(CN)2–Au(1)(CN)2–Au(2)(CN)2– zig-zag shaped chains along the a axis. C1, C2 and C4 show significant antifungal effects against several plant pathogenic fungi, while surprisingly C3 exhibits a considerable antibacterial effect against Gram negative E. coli. The studies of the antiproliferative activity on Hela, HT29 and C6 tumor cell lines indicated the anticancer potential of these complexes even at low doses.

Biological Property of Fritillaria imperialis L. Extract

A preliminary in vitro screening revealed the therapeutic status of extracts of Fritillaria imperialis L. that belongs to the Liliaceae family. Its tendrilled bulbs are consumed fresh or prepared in a powdered form and used as a home remedy for cough and phlegm, high fever, hemorrhage, lack of milk, treatment of abscesses, asthma, rheumatism, and eye disease. Herein, we investigated the antiproliferative, cytotoxic effects and antibacterial activities of Fritillaria imperialis L. extracts on three cancer cell lines (HeLa, HT29, and C6), and a non-cancer cells (Vero). The potential antiproliferative and cytotoxic impact of Fritillaria imperialis L. extracts were investigated in vitro through MTT and LDH measurement techniques, and its antimicrobial effects were studied with MIC and disc-zone test. The extracts of Fritillaria imperialis L. have been shown to exhibit poor antiproliferative effects and antibacterial activities on some cancer cell lines and bacteria, respectively, at even high concentration. These data suggest that Fritillaria imperialis L. extracts are low cytotoxic to cancer cell lines and Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922). Our results indicate that clinic consideration of Fritillaria imperialis extracts for the treatment of malignant and bacterial disease needs to be re-evaluated due to its different extraction and isolation methods.

Yapı Aktivite İlişkisi (SAR): Bromlanmış 8-hidroksikinolin ve ftalonitril türevlerinin çeşitli kanser hücre hatları üzerine antiproliferatif aktivitelerinin incelenmesi

In this study, phthalonitriles 6, 7 and their corresponding bromo derivatives 8, 9 were synthesized from 8hydroxyquinoline to investigate antiproliferative and cytotoxic activities on C6 (rat brain tumor), HeLa (human cervix carcinoma) and HT29 (human colon carcinoma) cancer cell lines of these molecules. The antiproliferative and apoptotic effects of 7-bromoand 5,7-dibromo-8-hydroxyquinoline derivatives (2 and 3) and phthalonitrile 6, 7 and their brominated derivatives 8, 9 were compared in terms of Structure Activity Relationship (SAR). Although bromohydroxyquinoline derivatives 2 and 3 exhibited high antiproliferative * Sorumlu Yazar / Corresponding Author 1 Kırıkkale Üniversitesi, Eğitim Fakültesi, Matematik ve Fen Bilimleri Eğitimi Bölümü, Yahşihan, Kırıkkale, sokten@gmail.com 2 Gaziosmanpaşa Üniversitesi, Fen Edebiyat Fakültesi, Biyoloji Bölümü, Tokat, tugbakul_koprulu@hotmail.com 3 İstanbul Gelişim Üniversitesi, Sağlık Bilimleri Yüksekokulu, Avcılar, İstanbul, cakmak.osman@gmail.com 4 Gen Mühendisliği ve Biyoteknoloji Enstitüsü, Tübitak MAM, Gebze, Kocaeli, sabant@yahoo.com 1300 Sakarya Üniversitesi Fen Bilimleri Enstitüsü Dergisi, 21 (6), 1300~1306, 2017