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Öğe Antimicrobial and anti-quorum sensing activities of giant fennel (Ferula elaeochytris Korovin) from the Hatay region(Selçuk Üniversitesi, 2020) Tüfekci, Enis Fuat; Alkateeb, Anfal; Akar, Sarah; Çorum, Orhan; Altunoğlu, Yasemin Çelik; Baloğlu, Mehmet Cengiz; Kiraz, Muammer; Çöplü, NilayAmaç: Günümüzde giderek artan antibiyotik direnci, bilim dünyasını yeni antimikrobiyal moleküllerin keşfine veya alternatif mücadele yöntemlerinin geliştirilmesi üzerine odaklamıştır. Bu alternatif mücadele yöntemlerinden bir tanesinin bakterilerde quorum sensing (QS; çoğunluğu algılama) inhibisyonu olacağı öngörülmektedir. Çünkü QS sistemi bakterilerde virülans faktörlerinin sentezinde önemli bir rol oynar. Medikal öneme sahip birçok bitkinin umut verici antimikrobiyal ve anti-QS aktivitelere sahip olduğu bilinmektedir. Bu bitkilerden birisinin de Anadolu'da yıllardır yaygın olarak kullanılan çakşır otu (Ferula elaeochytris Korovin) olabileceğini düşünmekteyiz. Bu nedenle, bu çalışmada F. elaeochytris Korovin’in kök özütünün antimikrobiyal ve anti-QS aktivitelerinin araştırılması amaçlanmıştır. Gereç ve Yöntem: Özütün antimikrobiyal aktivitesi, çeşitli mikroorganizmalara karşı disk difüzyon yöntemi ile taranmıştır. Özütün etkili suş veya suşlara karşı minimum inhibitör konsantrasyonu (MİK) ve minimum bakterisidal konsantrasyonu (MBK) değerleri sıvı mikrodilüsyon yöntemi ile belirlenmiştir. Anti-QS aktivite, Pseudomonas aeruginosa ve Chromobacterium violaceum biyoraportör suşlarında sırasıyla piyosiyanin ve viyolasin pigmentleri üretiminin inhibisyonu üzerine araştırılmıştır. Bulgular: Özütün sadece Staphylococcus aureus suşuna karşı antimikrobiyal aktivitesi (zon çapı = 9.3±0.6 mm) tespit edilmiştir. MİK ve MBK değerleri sırasıyla 4.4±1.9 mg/mL ve >105 mg/mL olarak saptanmıştır. Viyolasin üretimi inhibisyonu belirlenmemiştir. Özütün MİK altı konsantrasyon değerleri (1.64 µg/mL ve 3.28 µg/mL) bakteri üremesini baskılamadan piyosiyanin üretimini sırasıyla %60 ve %82 oranında inhibe etmiştir. Öneri: Bu çalışmanın sonuçları F. elaeochytris Korovin'in kök özütünün antistafilokokal ve anti-QS ajanların geliştirilmesi için iyi bir aday olabileceğini göstermektedir.Öğe DNA protection, antioxidant, antibacterial and enzyme inhibition activities of heartwood and sapwood extracts from juniper and olive woods(ROYAL SOC CHEMISTRY, 2015) Özkan, Osman Emre; Zengin, Gökhan; Akça, Mehmet; Baloğlu, Mehmet Cengiz; Olgun, Cağrı; Altuner, Ergin Murat; Ateş, SaimIn this study, DNA protective, antioxidant, antibacterial and enzyme inhibiting properties of methanol extracts obtained from juniper and olive heartwood and sapwood were determined. These extracts were tested by five antioxidant methods (DPPH scavenging, FRAP, CUPRAC, metal chelating and phosphomolybdenum). Generally, heartwood extracts of both species are more efficient for DPPH radical scavenging activity, cupric ion reducing activity, ferric reducing antioxidant power and metal chelating activity than sapwood extracts. When compared to heartwood extracts, sapwood extracts have larger inhibition zone in disk diffusion test. In addition, all extracts showed high antibacterial activity against Staphylococcus aureus. DNA protection of both extracts had a capacity to inhibit the DNA damage arisen from Fenton's reagent. The highest DNA protective activity was observed in juniper sapwood extract with 84%. Furthermore, other extracts also indicated more than 60% of DNA protective activity. Olive wood extracts displayed the strongest enzyme inhibition activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Although juniper heartwood extracts showed highest anti-amylase, anti-glucosidase and anti-tyrosinase effects, they had no ability for inhibition BChE. The methanol extracts of olive samples demonstrated the most antioxidant activity (DPPH, CUPRAC and FRAP). In addition, juniper samples showed the highest anti-amylase, anti-tyrosinase, metal chelating and DNA protective activity. According to these results, the extracts of juniper and olive wood can be considered as a source of natural bio active agents for dietary, pharmacological and medicinal applications. This research will also serve as a base for future studies about biological activities of wood extracts.Öğe Investigation of chemical profile, biological properties of Lotus corniculatus L. extracts and their apoptotic-autophagic effects on breast cancer cells(ELSEVIER, 2019) Yerlikaya, Şerife; Baloğlu, Mehmet Cengiz; Diuzheva, Alina; Jeko, Jozsef; Cziaky, Zoltan; Zengin, GökhanThis study aimed to reveal chemical profiles and biological activities of ethyl acetate (EA), methanol (MeOH), and water extracts of Lotus corniculatus. Ethnobotanical reports have indicated the importance of phytochemical properties of the genus Lotus. In this study, the effects of medicinal plant extracts on antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (on cholinesterase, tyrosinase, a-amylase and a-glucosidase), DNA protection and anticancer properties (including anti-proliferative, cell death and telomerase activity marker gene analysis, apoptotic DNA fragmentation analysis, cell migration test) were evaluated. According to chemical analysis, quercetin derivatives geraldol, isorhamnetin and kaempferol-O-coumaroylhexoside-O-deoxyhexoside isomers were dominant in the extracts. MeOH extracts showed the highest total flavonoids capacity with 21.13 mg RE/g. EA extract showed the strongest anti-amylase activity among the tested extracts. Water extract had the most protective activity against plasmid DNA. To indicate cell survival, MIT test was performed against human MCF-7 and MDA-MB-231 breast cancer cells. Half-maximal inhibitory concentration for cells were calculated and used for detection of mechanisms behind the cancer cell death. EA extract showed up-regulation of Bax proapoptotic gene and apoptotic DNA fragmentation activity on highly invasive MDA-MB-231 cells. Beclin-1 and LC3-II autophagy genes were higly expressed after treatment of MCF-7 cells with EA extracts. EA and MeOH extracts inhibited cell migration ability of both cancer cells. Linoleamide, was dominant component in EA extract and caused apoptosis on MDA-MB-231 breast cancer cells via increasing intranuclear Ca2+. The detailed mechanism behind the anticancer properties should be further investigated. (C) 2019 Elsevier B.V. All rights reserved.Öğe Multi-targeted potential of Pittosporum senacia Putt.: HPLC-ESI-MSn analysis, in silico docking, DNA protection, antimicrobial, enzyme inhibition, anticancer and apoptotic activity(ELSEVIER SCI LTD, 2019) Mahomoodally, Mohamad Fawzi; Picot-Allain, Carene; Hosenally, M.; Uğurlu, Aslı; Mollica, Adriano; Stefanucci, Azzurra; Llorent-Martinez, E. J.; Baloğlu, Mehmet Cengiz; Zengin, GökhanPittosporum senacia (PS) Putt. (Pittosporaceae), indigenous to the Mascarene Islands, is a common ingredient in traditional medicines. However, there is currently a dearth of studies to validate some of these traditional claims. Given the broad traditional uses of PS against several diseases, we aimed to provide a comprehensive insight into the biological and chemical profile of P. senacia. The antioxidant, enzyme inhibitory activity, anticancer, and phytochemical composition of the methanolic extract of P. senacia leaf extracts were studied. The possible interaction and binding mode of the most abundant phytochemicals were studied via in silico docking experiments on tyrosinase and alpha-glucosidase. The mechanism behind the cytotoxic property of P. senacia extract for MDA-MB-231 was also examined using different methods including 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell viability test checking apoptosis-associated genes, and wound healing assays. Twenty-six compounds were identified, of which caffeoylquinic acid derivatives, ferulic acid derivative, cinnamoylquinic acid derivative and two other polyphenols (oleuropeine and isoramnetin glucoside) being abundant, have been tested using in silico studies, against alpha-glucosidase and tyrosinase. The extract (IC50 = 118.8 mu g/ml) exhibited time and dose dependent anti-proliferative effect on human breast cancer cell line, MDA-MB-231. According to the expression profile of apoptosis inhibitors and apoptosis promoters genes, expression of Bar and Bak genes were significantly increased compared to Bcl-2 and Birc5 genes. Based on wound healing analysis, cell migration was inhibited after the application of the plant extract. The present findings suggested that PS might be a good candidate as sources of bioactive compounds for designing functional applications.Öğe Multidirectional insights on Chrysophyllum perpulchrum leaves and stem bark extracts: HPLC-ESI-MSn profiles, antioxidant, enzyme inhibitory, antimicrobial and cytotoxic properties(ELSEVIER SCIENCE BV, 2019) Baloğlu, Mehmet Cengiz; Llorent-Martinez, Eulogio J.; Aumeeruddy, Muhammad Zakariyyah; Mahomoodally, Mohamad Fawzi; Altunoğlu, Yasemin Çelik; Ustaoğlu, Buket; Öçal, Mustafa; Gürel, Songül; Bene, Kouadio; Sinan, Kouadio Ibrahime; Zengin, GökhanCluysophyllum perpulchrum Mildbr. ex Hutch. & Dalziel has been reported to possess several therapeutic properties in African traditional medicine. However, its pharmacological properties have not been fully studied. Herein, we focused on the evaluation of the antioxidant, enzyme inhibitory, antimicrobial and cytotoxic effects of three solvent extracts (ethyl acetate, methanol, and water) of the stem bark and leaves. Polyphenolic components of the extracts were also identified by high-performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC-ESI-MSn). The methanolic stem bark extract possess the highest DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging, ferric and molybdenum (VI) reducing, and the highest inhibitory effect against acetylcholinesterase and butyrylcholinesterase. The aqueous stem bark extract displayed the highest ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)) scavenging and cupric reducing power. In contrast, the leaf ethyl acetate extract was the most effective metal chelator and a-amylase inhibitor while the leaf methanolic extract exhibited the highest tyrosinase and alpha-glucosidase inhibition. The highest total phenolic content (131.58 mg GAE/g extract) was recorded from the methanolic stem bark extract while the leaf methanolic extract was the richest in total flavonoid content (30.43 mg RE/g extract). Flavan-3-ols were main group in the methanol extracts. The minimum inhibitiory concentration values for the methanolic stem bark extract against Gram positive and negative bacteria strains ranged between 62.5-125 mu g/ml. Bark extracts of C. petpulchrtun were very effective against Salmonella kentucky, Proteus vulgaris and Staphylococcus aureus at 62.5 mu g/ml. In addition, cytotoxic activity of stem bark samples was evident at lower concentration than those of leaf extracts. Stem bark extracts displayed the highest prevention against to HeLa cell line (IC50 = 264 mu g/mL after 48 h). In light of the above, C. perpulcluum might provide health benefits against oxidative stress and the associated chronic diseases. Nonetheless, the detailed mechanism of action is yet to be further investigated.Öğe Novel in vitro and in silico insights of the multi-biological activities and chemical composition of Bidens tripartita L.(PERGAMON-ELSEVIER SCIENCE LTD, 2018) Uysal, Şengül; Uğurlu, Aslı; Zengin, Gökhan; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Mollica, Adriano; Custodio, LuisaBidens tripartita L. is a traditional phyto-remedy used in several countries, yet there is still a paucity of data on its biological potential. We aimed to provide new insights on the pharmacological potential of extracts prepared from B. tripartita via highlighting its antioxidant, key enzymes inhibitory potency, and DNA protecting effects. Phytochemical profile was established using High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) and bioactive compound(s) docked against target enzymes using in silica methods. Cytotoxicity against three cancer cell lines was assessed using the methylthiazolyldiphenyl-tetrazolium bromide (MTT) cell viability test. The main compounds were luteolin-7-glucoside (cynaroside), chlorogenic acid, and epicatechin in the extracts. The methanol extract exhibited the highest radical scavenging activity. Ethyl acetate extract showed strongest a-amylase inhibitory activity, while the best a-glucosidase inhibitory effect recorded for the methanol extract. Molecular docking showed that cynaroside strongly interact to a-glucosidase cavity by establishing six hydrogen bonds. B. tripartita extracts were found to protect supercoiled form of pUC19 plasmid (>70%) and also showed anti-proliferative properties. Results amassed in the present study add on to a growing body of literature on the multi-pharmacological potency of B. tripartita which can be applied to bio-products development geared towards management of common diseases.Öğe Pharmacological and polyphenolic profiles of Phyllanthus phillyreifolius var. comrnersonii Mull. Arg: An unexplored endemic species from Mauritius(ELSEVIER SCIENCE BV, 2019) Mahomoodally, Mohamad Fawzi; Yerlikaya, Şerife; Llorent-Martinez, Eulogio J.; Uğurlu, Aslı; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Mollica, Adriano; Dardenne, Kurty Kersley; Aumeeruddy, Muhammad Zakariyyah; Puchooa, Daneshwar; Zengin, GökhanPhyllanduts phillyreifolius var. conunersonii Mfill. Arg is an endemic plant of Mauritius. To date, no study has been performed concerning its polyphenolic profile and pharmacological properties. In this study, a decoction (water), ethyl acetate and methanol extracts of the aerial parts of P. phillyreifolius, obtained from different extraction procedures (maceration and Soxhlet), were studied for antibacterial, antioxidant, anticancer, and enzyme inhibitory properties along with their polyphenolic profile. The ethyl acetate macerated extract showed high antibacterial activity against B. cereus (MIC = 0.293 mg/mL) and E. coil (MIC = 0.417 mg/mL) while S. epidermidis was most susceptible to the ethyl acetate-Soxhlet extract (MIC = 0.521 mg/mL). The methanolSoxhlet extract displayed the most potent cupric and ferric reducing power, and metal chelating effect, while the macerated methanolic extract was the most effective DPPH and ABTS scavenger, and BChE inhibitor. Only the ethyl acetate-Soxhlet extract exhibited alpha-glucosidase inhibition. All extracts exhibited a strong anti-tyrosinase activity, which was further investigated by molecular docking and molecular dynamic. After 48 h exposure to the extracts for HeLa cell lines, the ethyl acetate-Soxhlet extract showed the highest inhibition (IC50 = 533.1 pg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC50 = 337.4 pg/mL). Treatment of cancer cell lines with all P. phillyreifolius extracts resulted in a time-dependent reduction of cell viability for HeLa and dose-and time-dependent reduction for MDA-MB-231. Gene expression ratio of Bcl-2 to Bax was higher for all Soxhlet-extracts. Total phenolics (TPC) and flavonoids (TFC) content were highest in the decoction and methanol-Soxhlet extract, respectively (122.43 mg GAE/g extract and 31.28 mg RE/g extract, respectively). The extracts were abundant in ellagitannins, although phenolic acids and flavonoids were also detected. Granatin B was detected for the first time in Phyllanthus species. Overall, the aerial parts of P. phillyreifolius exemplify a potent reservoir of bioactive phytochemicals for therapeutic applications.Öğe Syzgium coriaceum Bosser & J. Gueho-An endemic plant potentiates conventional antibiotics, inhibits clinical enzymes and induces apoptosis in breast cancer cells(ELSEVIER, 2020) Mahomoodally, Mohamad Fawzi; Uğurlu, Aslı; Liorent-Martinez, Eulogio J.; Nagamootoo, Meenathee; Picot-Allain, Marie Carene Nancy; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Hosenally, Muzzammil; Zengin, GökhanSyzygium species are renowned for being important reservoirs of phytochemicals with pharmaceutical and biomedical potential. However, no attempt has been made to delineate the pharmacological potential and phytochemical profile of Syzgtturt coriaceum Bosser & J. Gueho, an endemic plant to Mauritius. The present study aimed to determine the antibacterial, antioxidant, cytotoxicity, enzyme inhibitory and phytochemical profile of the ethyl acetate and methanol extracts of S. coriaceum. Preliminary qualitative phytochemical study of the extracts showed the presence of phenol, tannins, and alkaloids. Chemical characterisation showed the presence of derivatives of tannins, gallic acids, quercetin, and kaempferol. Potentiating activity between S. coriaceum extracts and antibiotics (ampicillin and streptomycin) using the checkerboard method showed additive interaction. The extracts showed potent 2,2-diphenyl-1-picrylhydrazyl (DPPH) (2.95 and 2.93 mmol trolox equivalent (TE)/g sample for ethyl acetate and methanol extracts, respectively) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) (4.09 and 3.83 mmol TE/g sample for ethyl acetate and methanol extracts, respectively) scavenging abilities. Syzygium coriaceum extracts were active inhibitors of alpha-glucosidase (about 47 mmol acarbose equivalent/g sample for ethyl acetate and methanol extract). S. coriaceum methanol extract caused maximum inhibition against human breast adenocarcinoma (MDA-MB-231) cancer cells after 48 h treatment with the IC50 value of 53.41 mu g/mL. Expression of anti-apoptotic Bcl2 and BIRCS genes were down-regulated. It can be concluded that S. coriaceum extracts lead to YIDA-MB-231 cells apoptosis. This investigation has provided a comprehensive report of the biological and chemical profile of S. coriaceum. Collected scientific evidences can open new avenues for research and contributes towards establishing primary data on Syzygium species endemic to Mauritius for bioprospection of novel phytopharmaceuticals.Öğe Utilisation of Rhododendron luteum Sweet bioactive compounds as valuable source of enzymes inhibitors, antioxidant, and anticancer agents(PERGAMON-ELSEVIER SCIENCE LTD, 2020) Mahomoodally, Mohamad Fawzi; Sieniawska, Elwira; Sinan, Kouadio Ibrahime; Picot-Allain, Marie Carene Nancy; Yerlikaya, Şerife; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Şenkardeş, İsmail; Rengasamy, Kannan R. R.; Zengin, GökhanEthnobotanical evidences report the use of Rhododendron luteum Sweet (Ericaceae) in traditional medicinal systems. However, R. luteum has been associated to the occurrence of 'mad honey' poisoning. In the present study, the ethyl acetate, methanol, and water extracts of R. luteum were investigated for their in vitro antioxidant, enzyme inhibition, and cytotoxic properties. The cytotoxicity of R. luteum extracts on A549 lung cancer cell line was evaluated using MTT cell viability assay. Besides, HPLC-ESI-MSn approach was employed to elucidate the secondary metabolite profiles of R. luteum in order to establish any structure-activity relationship. Methanol and water extracts of R. luteum possessed highest radical scavenging and reducing properties while the ethyl acetate extract showed highest metal chelating properties. In terms of enzyme inhibition, the methanol and ethyl acetate extracts of R. luteum, possessing epigallocatechin, were active inhibitors of cholinesterase enzymes, a-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 mu g/ml IC50 value. Though R. luteum has received little scientific attention due to the occurrence of grayanotoxins in the plant, however, data presented in this work shows promising biological activity of R. luteum and highlighted its role as a potential source of antioxidant and key enzyme inhibitors.
