Browsing by Author "Zengin, Gokhan"

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Chemical characterization, computational analysis and biological views on Daphne gnidioides Jaub. & Spach extracts: Can a new raw material be provided for biopharmaceutical applications?
(2020-05-13T00:00:00Z) Can, Tevfik Hasan; Tufekci, Enis Fuat; Altunoglu, Yasemin Celik; Baloglu, Mehmet Cengiz; Llorent-Martínez, Eulogio J; Stefanucci, Azzurra; Mollica, Adriano; Cichelli, Angelo; Zengin, Gokhan
The scientific world tends to turn to natural products such as medicinal and aromatic plants because of the inadequacy of commercially available synthetic drugs as antibiotics or anticancer, and their adverse effects on healthy tissues. One of these plants is Daphne gnidioides Jaub. & Spach, which belongs to the Thymelaeaceae family, and there is no data in the literature on its biological activity. This study is aimed to elucidate the chemical profiles and in vitro anticancer, antibacterial and DNA protection and enzyme inhibitory properties of methanol extracts of root, stem, and leaf of D. gnidioides Jaub. & Spach. Polyphenolic components of the extracts were characterized by HPLC-MS/MS. The highest phenolic content was detected in the leaf extract (TIPC = 43.5 ± 0.5 mg/g DE), followed by stem (TIPC = 27.3 ± 0.7 mg/g DE) and root (TIPC = 18.3 ± 0.2 mg/g DE) extracts. Vicenin-2 and 3-O-p-coumaroyl-5-O-caffeoylquinic acid were the main identified compounds in leaf and both root and stem extracts, respectively. The extracts did not show any protective effect on DNA against experimental Fenton's reagent. The minimum inhibitory concentration and the minimum bactericidal concentration values for the root and leaf extracts against tested bacterial strains ranged from 31.25 to 500 μg/mL. After 48 h interaction of the cancer cell lines with the extracts, only the stem extract had significant cytotoxicity on HeLa cells (IC = 86.16 μg/mL). No remarkable activity of the extracts, which was tested against MDA-MB-231, was detected (IC > 1000 μg/mL). These data showed that D. gnidioides Jaub. & Spach stem extract inhibited the survival of HeLa cells in a time-dependent manner. After the treatment of IC concentration of stem extract with HeLa cells, an increase in LC3-II autophagic gene expression was detected. Also, the extracts exhibited significant tyrosinase inhibitory effects which were confirmed by molecular docking. To sum up, the tested extracts could be used as a starting point for the development of new multifunctional drugs.
Chemical fingerprints, antioxidant, enzyme inhibitory, and cell assays of three extracts obtained from Sideritis ozturkii Aytaç & Aksoy: An endemic plant from Turkey.
(2019-07-15T00:00:00Z) Zengin, Gokhan; Uğurlu, Asli; Baloglu, Mehmet Cengiz; Diuzheva, Alina; Jekő, József; Cziáky, Zoltán; Ceylan, Ramazan; Aktumsek, Abdurrahman; Picot-Allain, Carene Marie Nancy; Fawzi Mahomoodally, M
This study was geared towards assessing the possible antioxidant, enzyme inhibitory, and cytotoxic activities of ethyl acetate, methanol, and water extracts of Sideritis ozturkii Aytaç & Aksoy. The phytochemical profiles of the studied extracts were characterised by HPLC-MS/MS. The methanol extract, rich in phenolics (78.04 mg gallic acid equivalent/g), exhibited the strongest antioxidant activities. However, the ethyl acetate extract was the most active extract in the enzyme inhibitory assays. The water extract of S. ozturkii (1 mg/ml, 48 h incubation) slightly inhibited (22%) growth of human breast cancer cell line (MDA-MB-231 cells). On the other hand, the ethyl acetate and methanol extracts showed strong inhibition (98% and 97%, respectively) of MDA-MB-231 cells and caused apoptotic cell death. Scientific data generated from this study further appraises the multiple biological activities of plants belonging to the Sideritis genus. In addition, preliminary evidence gathered from the current investigation advocates for further studies geared towards the preparation of therapeutic formulations from S. ozturkii.
Comparative Content, Biological and Anticancer Activities of Heracleum humile Extracts Obtained by Ultrasound-Assisted Extraction Method.
(2022-07-01T00:00:00Z) Ocal, Mustafa; Altunoglu, Yasemin Celik; Angeloni, Simone; Mustafa, Ahmed M; Caprioli, Giovanni; Zengin, Gokhan; Paksoy, Mehmet Yavuz; Baloglu, Mehmet Cengiz
As the safety and effectiveness of synthetic drugs remain in doubt, researchers are trying to develop natural medicines from medicinal plants. Herein, ethyl acetate, methanol and water extracts from the Heracleum humile plant were obtained by an ultrasonic-assisted extraction process and the aim was to evaluate some biological effects of the extracts due to the limited data on the pharmacological properties of Heracleum humile in the literature. Weak antibacterial activity was observed on tested bacterial species. The minimum inhibitory concentration and the minimum bactericidal concentration values ranged from 250 to 500 μg/mL. In addition, cytotoxic activity was determined using the MTT test. The strongest findings were determined for ethyl acetate extract on the MDA-MB-231 cell lines at the 48 hour (IC :97.94 μg/mL), followed by the MCF-7 cell lines at the 24 hour (IC :103.9 μg/mL). All extracts of Heracleum humile contained mainly flavonoids, phenolic acids and their derivatives, i. e., well-known compounds that possess numerous biological activities such as antioxidant, anti-inflammatory, anticancer, antimicrobial etc. The study results could provide important information that Heracleum humile could be a potential candidate as a natural enzyme inhibitor. It can be concluded that these extracts could be useful in the elementary step of improving novel plant-derived multifunctional pharmaceuticals.
Evaluation of the Potential Therapeutic Properties of Liquidambar orientalis Oil.
(2023-09-12) Baloglu, Mehmet Cengiz; Yildiz Ozer, Lutfiye; Pirci, Buket; Zengin, Gokhan; Uba, Abdullahi Ibrahim; Celik Altunoglu, Yasemin
Liquidambar orientalis Mill., commonly called the Anatolian sweetgum or Sigla tree, is endemic to southwestern Turkey. It has been historically significant in traditional medicine. In our research, we delved into the therapeutic attributes of its oil, emphasizing its antioxidant, antimicrobial, and antitumor properties. The primary chemical constituent of the gum is styrene, accounting for 78.5%. The gum demonstrated antioxidant capabilities in several assays, including in 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP). It displayed bactericidal actions against various gram-positive bacteria, such as Staphylococcus aureus, and gram-negative strains, including Escherichia coli. Additionally, the oil showcased potent antitumor effects against breast (MDA-MB-231), lung (A549), and prostate (PC3) cancer cell lines. These effects were found to be both time- and dose-dependent. L. orientalis Mill. oil showed the best antitumor activity against breast, lung, and prostate cancer cell lines after the 24 h and 48h treatment. Its oil might induce autophagy in the PC3 prostate cancer cell line, whereas its cytotoxicity against MDA-MB-231 and A549 cancer cell lines might not be correlated with autophagy or apoptosis pathways. In conclusion, the oil from the Sigla tree offers promising therapeutic potential and warrants further exploration.
Exploring the Nutraceutical Potential of Dried Pepper L. on Market from Altino in Abruzzo Region.
(2020-05-08T00:00:00Z) Della Valle, Alice; Dimmito, Marilisa Pia; Zengin, Gokhan; Pieretti, Stefano; Mollica, Adriano; Locatelli, Marcello; Cichelli, Angelo; Novellino, Ettore; Ak, Gunes; Yerlikaya, Serife; Baloglu, Mehmet Cengiz; Celik Altunoglu, Yasemin; Stefanucci, Azzurra
Sweet pepper is a typical type of from Abruzzo region, recognized as a traditional and local product, traditionally cultivated in the town of Altino (Abruzzo region, Italy). The aim of this study is to compare the sweet type of peppers from Altino with the hot pepper cultivated in the same area, in order to delineate their different phytochemical and biological profiles in vitro and in vivo. In this study, we elucidated their phytochemical composition, fatty acids composition and phenolic/flavonoid contents in extracts. Then antioxidant and enzyme inhibition assays were performed to evaluate their biological properties, together with in vitro cell assay and in vivo anti-inflammatory activity. Microwave (1000 mg/mL) extract of hot pepper showed the best inhibition value on in vitro cell growth assay; in fact, the number of survived cells was about 20% and 40% for microwave and Soxhlet extracts, respectively. In vivo anti-inflammatory assay revealed good activity for both species, which, when associated with in vitro cell inhibition results, could explain the protective effect on human prostatic hyperplasia.
Investigation of chemical profile, biological properties of Lotus corniculatus L. extracts and their apoptotic-autophagic effects on breast cancer cells.
(2019-09-10T00:00:00Z) Yerlikaya, Serife; Baloglu, Mehmet Cengiz; Diuzheva, Alina; Jekő, József; Cziáky, Zoltán; Zengin, Gokhan
This 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, MTT 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.
Investigations into the therapeutic potential of Asphodeline liburnica roots: In vitro and in silico biochemical and toxicological perspectives.
(2018-10-01T00:00:00Z) Locatelli, Marcello; Yerlikaya, Serife; Baloglu, Mehmet Cengiz; Zengin, Gokhan; Altunoglu, Yasemin Celik; Cacciagrano, Francesco; Campestre, Cristina; Mahomoodally, Mohamad Fawzi; Mollica, Adriano
This study aims to establish the biological and chemical profile of Asphodeline liburnica (Scop.) Rchb. root. The antioxidant, antimicrobial, enzyme inhibitory, DNA protection, apoptotic DNA ladder fragmentation analysis, and anti-proliferative of A. liburnica were established using standard assays. In silico study was also performed to understand interactions between quantified anthraquinones and key enzymes of clinical relevance. Total phenolic and flavonoid contents were found to be 9.67 mgGAE/g and 1.48 mgRE/g extract, respectively. Chrysophanol was detected as a major anthraquinone. The extract exhibited radical scavenging ability against DPPH and ABTS with values of 13.23 and 66.99 mgTE/g extract, respectively. Good inhibitory activity against tyrosinase was recorded. In silico experiments showed that the anthraquinones were able to establish coordinative bonds with the copper atoms present in the enzymatic cavity of tyrosinase. MTT cell viability test on MDA-MB-231 cells showed that at 0.1 and 1 μg of extracts induced anti-proliferative effect. Apoptotic DNA fragmentation analysis indicated nuclear condensation resulting in DNA fragmentation, which exhibited apoptotic cell death in the presence of A. liburnica. This study has provided insights on the potential usage of A. liburnica which could open new avenues for research and stimulate future interest for the development of safe novel biopharmaceuticals.
LC-MS/HRMS Analysis, Anti-Cancer, Anti-Enzymatic and Anti-Oxidant Effects of Extracts: A Potential Raw Material for Functional Applications.
(2021-12-16T00:00:00Z) Sinan, Kouadio Ibrahime; Akpulat, Uğur; Aldahish, Afaf A; Celik Altunoglu, Yasemin; Baloğlu, Mehmet Cengiz; Zheleva-Dimitrova, Dimitrina; Gevrenova, Reneta; Lobine, Devina; Mahomoodally, Mohamad Fawzi; Etienne, Ouattara Katinan; Zengin, Gokhan; Mahmud, Shafi; Capasso, Raffaele
is a great tropical plant and is widely used for various traditional purposes. In the present study, we examined the influence of solvents (dichloromethane, ethyl acetate, methanol and infusion (water)) on chemical composition and biological capabilities of . An UHPLC-HRMS method was used to determine the chemical characterization. The biological ability was examined for antioxidant, enzyme inhibitory and anti-cancer effects. To evaluate antioxidant effects, different chemical methods (ABTS, DPPH, CUPRAC, FRAP, metal chelating and phosphomolybdenum) were applied. With regard to enzyme inhibitory properties, cholinesterases, amylase, glucosidase and tyrosinase were used. The MDA-MB-231 breast cancer cell line was chosen to determine anticancer activity. Based on the UHPLC-HRMS analysis, 37 specialized metabolites were dereplicated and identified in the studied extracts. Results revealed the presence of 15 hydroxybenzoic, hydroxycinnamic, acylquinic acids, and their glycosides, one rotenoid, seven flavonoids, 12 fatty acids and two other glycosides. Among the tested extracts, the methanol extract showed a stronger antioxidant ability compared with other extracts. The methanol extract also showed the best inhibitory effects on tyrosinase and glucosidase. In the anti-cancer evaluation, the methanol extract showed stronger anticancer effects compared with water extract. In summary, our observations can contribute to the establishment of as a potential candidate for functional applications in the preparation.
Multi-targeted potential of Pittosporum senacia Putt.: HPLC-ESI-MS analysis, in silico docking, DNA protection, antimicrobial, enzyme inhibition, anti-cancer and apoptotic activity.
(2019-12-01T00:00:00Z) Mahomoodally, Mohamad Fawzi; Picot-Allain, Carene; Hosenally, M; Ugurlu, Asli; Mollica, Adriano; Stefanucci, Azzurra; Llorent-Martínez, E J; Baloglu, Mehmet Cengiz; Zengin, Gokhan
Pittosporum 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 α-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 α-glucosidase and tyrosinase. The extract (IC = 118.8 μg/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 Bax 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.
Novel in vitro and in silico insights of the multi-biological activities and chemical composition of Bidens tripartita L.
(2018-01-01T00:00:00Z) Uysal, Sengul; Ugurlu, Asli; Zengin, Gokhan; Baloglu, Mehmet Cengiz; Altunoglu, Yasemin Celik; Mollica, Adriano; Custodio, Luisa; Neng, Nuno R; Nogueira, José M F; Mahomoodally, M Fawzi
Bidens 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 silico 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 α-amylase inhibitory activity, while the best α-glucosidase inhibitory effect recorded for the methanol extract. Molecular docking showed that cynaroside strongly interact to α-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.
Pharmacological and polyphenolic profiles of Phyllanthus phillyreifolius var. commersonii Müll. Arg: An unexplored endemic species from Mauritius.
(2019-01-01T00:00:00Z) Mahomoodally, Mohamad Fawzi; Yerlikaya, Serife; Llorent-Martínez, Eulogio J; Uğurlu, Asli; Baloglu, Mehmet Cengiz; Altunoglu, Yasemin Celik; Mollica, Adriano; Dardenne, Kurty Kersley; Aumeeruddy, Muhammad Zakariyyah; Puchooa, Daneshwar; Zengin, Gokhan
Phyllanthus phillyreifolius var. commersonii Müll. 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. coli (MIC = 0.417 mg/mL) while S. epidermidis was most susceptible to the ethyl acetate-Soxhlet extract (MIC = 0.521 mg/mL). The methanol-Soxhlet 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 α-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 (IC = 533.1 μg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC = 337.4 μg/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.
Utilisation of Rhododendron luteum Sweet bioactive compounds as valuable source of enzymes inhibitors, antioxidant, and anticancer agents.
(2020-01-01T00:00:00Z) Mahomoodally, Mohamad Fawzi; Sieniawska, Elwira; Sinan, Kouadio Ibrahime; Nancy Picot-Allain, Marie Carene; Yerlikaya, Serife; Cengiz Baloglu, Mehmet; Altunoglu, Yasemin Celik; Senkardes, Ismail; Rengasamy, Kannan Rr; Zengin, Gokhan
Ethnobotanical 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-MS 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, α-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 μg/ml IC 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.