Phosphorus Sulfur and Silicon and The Related Elements, Jul 1, 2019
Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectr... more Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds were evaluated for their cytotoxicity against human breast cancer cell line MCF7 and prostate cancer cell line PC3 and nonmalignant fibroblast L929 cell line by MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) and 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) were found to display significant cytotoxicity with IC50 of 13.87 μM (against PC3 cell line) and 1.47 μM (against MCF7 cell line), respectively. These compounds were non-cytotoxic to normal cell line with IC50>100 μM. Western blotting studies demonstrated that compound 3f induced apoptosis and caused cell death in the MCF7 and PC3 cell lines via an increase in Bax protein expression and a slight decrease in Bcl-2 protein expression. The gene expression ratio Bax/Bcl-2 showed the induction of mitochondrial apoptosis in cancer cell lines. All of synthesized compounds have also been tested for antioxidant activity and all compounds achieved strong inhibition of the DPPH radical. These findings showed that compound 3f, displays potential to be further explored in the development of new anticancer agents. Graphical Abstract
Investigations in the discovery of tyrosinase enzyme inhibitors have the potential to design nove... more Investigations in the discovery of tyrosinase enzyme inhibitors have the potential to design novel anti-cancer drugs. A variety of novel bivalent pyrazolinyl triazoles 5-7 were synthesized and identified. The bis-acetyl triazole 3 was accomplished via two-step process first by preparation of diazide 2 followed its coupling reaction with acetylacetone in basic medium. The Claisen-Schmidt condensation reaction of 3 with two moles equivalent of benzaldehyde produces the corresponding bisα, β-unsaturated ketone 4. Treatment of Schiff base 4 with excess hydrazine hydrate in either acetic acid or ethanol/DMF afforded the bis-N-acetylpyrazline 5 or bis-pyrazoline 6, respectively. Finally, treatment of 6 with two derivatives of isothiocyanate analog gives the bis-N-thioamide pyrazolines 7a and 7b. The synthesized compounds were evaluated as anti-tumor candidates against three human cancer cell lines (MCF-7, HepG2, and HCT-116). The bioscreening evaluation showed that compounds 7a and 6 had a significant antineoplastic potencies (IC 50 : 32.26 and 57.06 µg/mL) against breast MCF-7 and hepatic HepG2 cancerous cell lines, respectively, in relative to the standard drug, 5-fluorouracil. Molecular docking studies of the synthesized compounds were investigated as VEGFR2 TK inhibitors.
Duzce Universitesi Tip Fakültesi Dergisi, Apr 30, 2019
Bu çalışmanın amacı, yeşil kimya yöntemiyle çinko oksit nanopartiküllerini (ZnONPs) sentezlemek v... more Bu çalışmanın amacı, yeşil kimya yöntemiyle çinko oksit nanopartiküllerini (ZnONPs) sentezlemek ve bu nanopartiküllerin anti-bakteriyel ve anti-kanser etkilerini incelemektir. Gereç ve Yöntemler: Çinko iyonları ve sulu enginar yaprağı (Cynara scolymus) ekstraktı kullanılarak ZnONPs yeşil kimya yöntemiyle sentezlendi. ZnONPs oluşumunun doğrulanması ve karakterizasyonu için morötesi-görünür bölge spektroskopisi (UV-Vis), Fourier dönüşümü kızılötesi spektroskopisi (FTIR), taramalı elektron mikroskobu (SEM), zetasizer ve Enerji dağınım X-ışını spektroskopisi (EDX) analizleri kullanıldı. ZnONPs'nin 4 farklı bakteri türü (E. coli, S. aureus, P. aeruginosa ve E. faecalis) üzerindeki antibakteriyel aktiviteleri, minimal inhibe edici konsantrasyon (MİK) ve kuyucuk difüzyon yöntemiyle ölçüldü. ZnONPs'nin HT-29 insan kolon kanseri hücreleri üzerindeki sitotoksik etkileri konsantrasyon ve zamana bağlı olarak olarak belirlendi. Bulgular: UV-Vis spektrumunda ZnO'ya spesifik olan 320-335 nm aralığında absorbans artışı gözlemlendi. FTIR spektrumunda 426 cm-1 ve 540 cm-1 'de ZnO'ya ait gerilme titreşimleri belirlendi. SEM analizinde partikül boyutu 276-309 nm ölçüldü. ZnONPs'nin zeta-sizer analizlerinde partikül büyüklüğü 137,8 nm ve partikül yükü-6,34 meV olarak bulundu. Antibakteriyel aktivite ölçümlerinde, sentezlenen nanopartiküllerin E. coli ve S. aureus'ta bakteriyel aktivite inhibisyonu sağladığı tespit edildi. ZnONPs HT-29 kolon kanseri hücreleri üzerinde 10 µg/mL'den daha yüksek konsantrasyonlarda sitotoksik etki gösterdi. Sonuç: ZnONPs'nin düşük maliyetle hazırlanabileceği ve klinik tedavilerde yeni ilaç formülasyonları için taşıyıcı sistem olarak kullanılma potansiyeline sahip olduğu bu çalışma ile gösterilmiştir.
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts ... more In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts of Cynara scolymus (Artichoke) using microwave irradiation and the evaluation of its anti-cancer potential with photodynamic therapy (PDT). Silver nanoparticles formation was characterized by scanning electron microscopy with energy dispersive x-ray spectroscopy and Fourier transform infrared (FTIR) spectroscopy. Silver nanoparticles formation was also investigated the surface charge, particle size and distribution using zetasizer analysis. The cytotoxic effect of AgNPs and/or PDT was studied by MTT assay and migration by the scratch assay. The apoptotic inducing ability of the AgNPs and/or PDT was investigated by intracellular ROS analysis, antioxidant enzyme levels (SOD, CAT, GPx and GSH), Hoechst staining and Bax/Bcl-2 analysis using western blotting. The mean particle size of produced AgNPs was found 98.47±2.04 nm with low polydispersity (0.301±0.033). Zeta potential values of AgNPs show-32.3± 0.8 mV. These results clearly indicate the successful formation of AgNPs for cellular uptake. Mitochondrial damage and intracellular ROS production were observed upon treatment with AgNPs (10μg/mL) and PDT (0.5 mJ/cm 2) showed significant reducing cell migration, expression of Bax and suppression of Bcl-2. Significantly, biosynthesized AgNPs showed a broad-spectrum anti-cancer activity with PDT therapy and therefore represent promoting ROS generation by modulating mitochondrial apoptosis induction in MCF7 breast cancer cells.
In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts ... more In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts of Cynara scolymus (Artichoke) using microwave irradiation and the evaluation of its anti-cancer potential with photodynamic therapy (PDT). Silver nanoparticles formation was characterized by scanning electron microscopy with energy dispersive x-ray spectroscopy and Fourier transform infrared (FTIR) spectroscopy. Silver nanoparticles formation was also investigated the surface charge, particle size and distribution using zetasizer analysis. The cytotoxic effect of AgNPs and/or PDT was studied by MTT assay and migration by the scratch assay. The apoptotic inducing ability of the AgNPs and/or PDT was investigated by intracellular ROS analysis, antioxidant enzyme levels (SOD, CAT, GPx and GSH), Hoechst staining and Bax/Bcl-2 analysis using western blotting. The mean particle size of produced AgNPs was found 98.47±2.04 nm with low polydispersity (0.301±0.033). Zeta potential values of AgNPs show-32.3± 0.8 mV. These results clearly indicate the successful formation of AgNPs for cellular uptake. Mitochondrial damage and intracellular ROS production were observed upon treatment with AgNPs (10μg/mL) and PDT (0.5 mJ/cm 2) showed significant reducing cell migration, expression of Bax and suppression of Bcl-2. Significantly, biosynthesized AgNPs showed a broad-spectrum anti-cancer activity with PDT therapy and therefore represent promoting ROS generation by modulating mitochondrial apoptosis induction in MCF7 breast cancer cells.
Phosphorus Sulfur and Silicon and The Related Elements, Jul 1, 2019
Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectr... more Abstract A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds were evaluated for their cytotoxicity against human breast cancer cell line MCF7 and prostate cancer cell line PC3 and nonmalignant fibroblast L929 cell line by MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) and 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) were found to display significant cytotoxicity with IC50 of 13.87 μM (against PC3 cell line) and 1.47 μM (against MCF7 cell line), respectively. These compounds were non-cytotoxic to normal cell line with IC50>100 μM. Western blotting studies demonstrated that compound 3f induced apoptosis and caused cell death in the MCF7 and PC3 cell lines via an increase in Bax protein expression and a slight decrease in Bcl-2 protein expression. The gene expression ratio Bax/Bcl-2 showed the induction of mitochondrial apoptosis in cancer cell lines. All of synthesized compounds have also been tested for antioxidant activity and all compounds achieved strong inhibition of the DPPH radical. These findings showed that compound 3f, displays potential to be further explored in the development of new anticancer agents. Graphical Abstract
Investigations in the discovery of tyrosinase enzyme inhibitors have the potential to design nove... more Investigations in the discovery of tyrosinase enzyme inhibitors have the potential to design novel anti-cancer drugs. A variety of novel bivalent pyrazolinyl triazoles 5-7 were synthesized and identified. The bis-acetyl triazole 3 was accomplished via two-step process first by preparation of diazide 2 followed its coupling reaction with acetylacetone in basic medium. The Claisen-Schmidt condensation reaction of 3 with two moles equivalent of benzaldehyde produces the corresponding bisα, β-unsaturated ketone 4. Treatment of Schiff base 4 with excess hydrazine hydrate in either acetic acid or ethanol/DMF afforded the bis-N-acetylpyrazline 5 or bis-pyrazoline 6, respectively. Finally, treatment of 6 with two derivatives of isothiocyanate analog gives the bis-N-thioamide pyrazolines 7a and 7b. The synthesized compounds were evaluated as anti-tumor candidates against three human cancer cell lines (MCF-7, HepG2, and HCT-116). The bioscreening evaluation showed that compounds 7a and 6 had a significant antineoplastic potencies (IC 50 : 32.26 and 57.06 µg/mL) against breast MCF-7 and hepatic HepG2 cancerous cell lines, respectively, in relative to the standard drug, 5-fluorouracil. Molecular docking studies of the synthesized compounds were investigated as VEGFR2 TK inhibitors.
Duzce Universitesi Tip Fakültesi Dergisi, Apr 30, 2019
Bu çalışmanın amacı, yeşil kimya yöntemiyle çinko oksit nanopartiküllerini (ZnONPs) sentezlemek v... more Bu çalışmanın amacı, yeşil kimya yöntemiyle çinko oksit nanopartiküllerini (ZnONPs) sentezlemek ve bu nanopartiküllerin anti-bakteriyel ve anti-kanser etkilerini incelemektir. Gereç ve Yöntemler: Çinko iyonları ve sulu enginar yaprağı (Cynara scolymus) ekstraktı kullanılarak ZnONPs yeşil kimya yöntemiyle sentezlendi. ZnONPs oluşumunun doğrulanması ve karakterizasyonu için morötesi-görünür bölge spektroskopisi (UV-Vis), Fourier dönüşümü kızılötesi spektroskopisi (FTIR), taramalı elektron mikroskobu (SEM), zetasizer ve Enerji dağınım X-ışını spektroskopisi (EDX) analizleri kullanıldı. ZnONPs'nin 4 farklı bakteri türü (E. coli, S. aureus, P. aeruginosa ve E. faecalis) üzerindeki antibakteriyel aktiviteleri, minimal inhibe edici konsantrasyon (MİK) ve kuyucuk difüzyon yöntemiyle ölçüldü. ZnONPs'nin HT-29 insan kolon kanseri hücreleri üzerindeki sitotoksik etkileri konsantrasyon ve zamana bağlı olarak olarak belirlendi. Bulgular: UV-Vis spektrumunda ZnO'ya spesifik olan 320-335 nm aralığında absorbans artışı gözlemlendi. FTIR spektrumunda 426 cm-1 ve 540 cm-1 'de ZnO'ya ait gerilme titreşimleri belirlendi. SEM analizinde partikül boyutu 276-309 nm ölçüldü. ZnONPs'nin zeta-sizer analizlerinde partikül büyüklüğü 137,8 nm ve partikül yükü-6,34 meV olarak bulundu. Antibakteriyel aktivite ölçümlerinde, sentezlenen nanopartiküllerin E. coli ve S. aureus'ta bakteriyel aktivite inhibisyonu sağladığı tespit edildi. ZnONPs HT-29 kolon kanseri hücreleri üzerinde 10 µg/mL'den daha yüksek konsantrasyonlarda sitotoksik etki gösterdi. Sonuç: ZnONPs'nin düşük maliyetle hazırlanabileceği ve klinik tedavilerde yeni ilaç formülasyonları için taşıyıcı sistem olarak kullanılma potansiyeline sahip olduğu bu çalışma ile gösterilmiştir.
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts ... more In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts of Cynara scolymus (Artichoke) using microwave irradiation and the evaluation of its anti-cancer potential with photodynamic therapy (PDT). Silver nanoparticles formation was characterized by scanning electron microscopy with energy dispersive x-ray spectroscopy and Fourier transform infrared (FTIR) spectroscopy. Silver nanoparticles formation was also investigated the surface charge, particle size and distribution using zetasizer analysis. The cytotoxic effect of AgNPs and/or PDT was studied by MTT assay and migration by the scratch assay. The apoptotic inducing ability of the AgNPs and/or PDT was investigated by intracellular ROS analysis, antioxidant enzyme levels (SOD, CAT, GPx and GSH), Hoechst staining and Bax/Bcl-2 analysis using western blotting. The mean particle size of produced AgNPs was found 98.47±2.04 nm with low polydispersity (0.301±0.033). Zeta potential values of AgNPs show-32.3± 0.8 mV. These results clearly indicate the successful formation of AgNPs for cellular uptake. Mitochondrial damage and intracellular ROS production were observed upon treatment with AgNPs (10μg/mL) and PDT (0.5 mJ/cm 2) showed significant reducing cell migration, expression of Bax and suppression of Bcl-2. Significantly, biosynthesized AgNPs showed a broad-spectrum anti-cancer activity with PDT therapy and therefore represent promoting ROS generation by modulating mitochondrial apoptosis induction in MCF7 breast cancer cells.
In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts ... more In this study, we report on the synthesis of silver nanoparticles (AgNPs) from the leaf extracts of Cynara scolymus (Artichoke) using microwave irradiation and the evaluation of its anti-cancer potential with photodynamic therapy (PDT). Silver nanoparticles formation was characterized by scanning electron microscopy with energy dispersive x-ray spectroscopy and Fourier transform infrared (FTIR) spectroscopy. Silver nanoparticles formation was also investigated the surface charge, particle size and distribution using zetasizer analysis. The cytotoxic effect of AgNPs and/or PDT was studied by MTT assay and migration by the scratch assay. The apoptotic inducing ability of the AgNPs and/or PDT was investigated by intracellular ROS analysis, antioxidant enzyme levels (SOD, CAT, GPx and GSH), Hoechst staining and Bax/Bcl-2 analysis using western blotting. The mean particle size of produced AgNPs was found 98.47±2.04 nm with low polydispersity (0.301±0.033). Zeta potential values of AgNPs show-32.3± 0.8 mV. These results clearly indicate the successful formation of AgNPs for cellular uptake. Mitochondrial damage and intracellular ROS production were observed upon treatment with AgNPs (10μg/mL) and PDT (0.5 mJ/cm 2) showed significant reducing cell migration, expression of Bax and suppression of Bcl-2. Significantly, biosynthesized AgNPs showed a broad-spectrum anti-cancer activity with PDT therapy and therefore represent promoting ROS generation by modulating mitochondrial apoptosis induction in MCF7 breast cancer cells.
Uploads
Papers by Muruvvet ABBAK