Browsing by Author "Zengin G."

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A broad-spectrum biological activities of Heracleum humile extracts: A first report of the antiviral, anti-cancer and chemical properties
(2024-12-01) Ocal M.; Duran Yelken S.; Altunoglu Y.C.; Baloglu M.C.; Soomro S.I.; Zengin G.; Angeloni S.; Mustafa A.M.; Caprioli G.; Paksoy M.Y.
A multidirectional perspective for novel functional products: In vitro pharmacological activities and in silico studies on Ononis natrix subsp. hispanica
(2017-09-01) Yerlikaya S.; Zengin G.; Mollica A.; Baloglu M.C.; Altunoglu Y.C.; Aktumsek A.
The genus Ononis has important value as traditional drugs and foods. In the present work, we aimed to assess the chemical profiles and biological effects of Ononis natrix subsp. hispanica extracts (ethyl acetate, methanol, and water). For chemical profile, total and individual phenolic components were detected. For biological effects, antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (against cholinesterase, tyrosinase, α-amylase and α-glucosidase), antimicrobial, DNA protection and cytotoxic abilities were tested. The predominant phenolics were apigenin, luteolin, and quercetin in the tested extracts. Generally, the ethyl acetate and methanol extracts were noted as the most active in the antioxidant and enzyme inhibitory assays. Water extract with different concentrations indicated high level of DNA protection activity. Methanol and ethyl acetate extracts showed antibacterial effect against to Staphylococcus aureus and Staphylococcus epidermidis strains. The cytotoxic effects of O. natrix subsp. hispanica extracts on the survival of HeLa and PC3 cells were determined by MTT cell viability assay. Water and methanol extracts caused initiation of apoptosis for PC3 cell line. Furthermore, molecular docking was performed to better understand interactions between dominant phenolic compounds and selected enzymes. Our results clearly indicate that O. natrix subsp. hispanica could be considered a potential candidate for designing novel pharmaceuticals, cosmeceuticals and nutraceuticals.
Anticancer and biological properties of leaf and flower extracts of Echinacea purpurea (L.) Moench
(2021-06-01) Mohamed Sharif K.O.; Tufekci E.F.; Ustaoglu B.; Altunoglu Y.C.; Zengin G.; Llorent-Martínez E.J.; Guney K.; Baloglu M.C.
Echinacea purpurea (L.) Moench is an important medicinal herb; its roots, leaves and, flowers have been used by the food and pharmaceutical industries. In this study, DNA protection, antimicrobial, antioxidant-enzyme inhibition, and antiproliferative activities of water, methanol (MeOH), and ethyl acetate (EA) extracts of leaves and flowers of E. purpurea were evaluated. In addition, total phenolics and flavonoids, as well as individual compounds, were identified using colorimetric assays and HPLC-ion trap mass spectrometry, respectively. Chicoric acid and its isomer were the most abundant natural compounds, with concentrations similar to previous studies of E. purpurea. All extracts had antimicrobial activity against a broad range of bacteria, particularly Enterococcus faecalis. The antiproliferative activity of the extracts on the HeLa cells was shown. The lowest value of IC50 (73 μg/ml) came from the 24 h MeOH extract of flowers. The water extract of leaves showed strong antioxidant activity with the DPPH, ABTS, CUPRAC, and FRAP assays. EA and MeOH extracts of leaves showed a significant inhibition ability of cholinesterase and tyrosinase, respectively. The presented study suggested that E. purpurea extracts had promising therapeutic properties. Further investigation at the cellular level could be done to highlight the mechanism behind these biological activities.
Chemical characterization, computational analysis and biological views on Daphne gnidioides Jaub. & Spach extracts: Can a new raw material be provided for biopharmaceutical applications?
(2020-08-01) Can T.H.; Tufekci E.F.; Altunoglu Y.C.; Baloglu M.C.; Llorent-Martínez E.J.; Stefanucci A.; Mollica A.; Cichelli A.; Zengin G.
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 (IC50 = 86.16 μg/mL). No remarkable activity of the extracts, which was tested against MDA-MB-231, was detected (IC50 > 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 IC50 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
(2019-07-15) Zengin G.; Uğurlu A.; Baloglu M.C.; Diuzheva A.; Jekő J.; Cziáky Z.; Ceylan R.; Aktumsek A.; Picot-Allain C.M.N.; 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
(2022-07-01) Ocal M.; Altunoglu Y.C.; Angeloni S.; Mustafa A.M.; Caprioli G.; Zengin G.; Paksoy M.Y.; Baloglu M.C.
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 48th hour (IC50:97.94 μg/mL), followed by the MCF-7 cell lines at the 24th hour (IC50:103.9 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.
Comprehensive approaches on chemical composition and biological properties of Daphne pontica L. extracts
(2022-01-01) Celik Altunoglu Y.; Can T.H.; Tufekci E.F.; Altunoglu B.D.; Baloglu M.C.; Llorent-Martínez E.J.; Zengin G.
The genus Daphne presents great interest as a valuable source of natural agents in traditional medicine of various countries, including Turkey. In the current work, we investigated the phytochemical composition and biological properties of Daphne pontica L. extracts. Methanol extracts of roots, stems and leaves were prepared. The chemical characterization was performed by HPLC-ESI-MSn, observing that flavonoids and phenolic acids were the main compounds. Biological properties were studied in terms of antimicrobial, DNA protection, anticancer, and enzyme inhibitory properties (cholinesterases, tyrosinase, amylase and glucosidase). Methanol extracts of roots, leaves, and stems of D. pontica had antimicrobial effects against a broad range of bacteria. In addition, methanol extract of roots of D. pontica exhibited a promising anticancer activity that was shown to be dose- and time-dependent for HeLa cells with an IC50 value of 203.9 μg/mL. Generally, the leaf extracts exhibited the best enzyme inhibitory properties on the tested enzymes. According to our results, D. pontica might be regarded as a valuable source of natural agents to combat cancer, infectious diseases, and metabolic diseases.
DNA protection, antioxidant, antibacterial and enzyme inhibition activities of heartwood and sapwood extracts from juniper and olive woods
(2015-08-21) Özkan O.E.; Zengin G.; Akça M.; Baloʇlu M.C.; Olgun Ç.; Altuner E.M.; Ateş S.; Aktümsek A.; Vurdu H.
In 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.
Evaluation of the Potential Therapeutic Properties of Liquidambar orientalis Oil
(John Wiley and Sons Inc, 2023) Baloglu, M.C.; Ozer L.Y.; Pirci B.; Zengin G.; Ibrahim Uba A.; Celik Y.A.
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′-azinobis(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 48 h 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 of Coronilla varia L. extracts as a source of high-value natural agents: Chemical profiles and biological connections
(2021-12-01) Yerlikaya S.; Baloglu M.C.; Altunoglu Y.C.; Diuzheva A.; Jekő J.; Cziáky Z.; Zengin G.
Pharmacological studies have indicated that flavonoids are crucial compounds to eliminate drug resistance. In this report, the activity of ethyl acetate (EAE), methanol (ME) and water (WE) extracts of Coronilla varia L. on antioxidant and enzyme inhibitory activities, DNA protective effects, antiproliferative activities, apoptotic; autophagic and telomerase gene activity analysis in breast cancer cells and inhibitory effects on cell migration ability of malignant breast cancer cells were examined. In addition, HPLC-MS-MS was used for detection of chemical profiles of all extracts. Results showed that the highest concentration of the bioactive components was detected in EAE (50.86 mg GAE/g for phenolics and 25.66 mg RE/g for flavonoid). Also, EAE displayed significant antioxidant properties in radical scavenging and reducing power assays. Regarding enzyme inhibitory effects, EAE and ME were more active than WE. Some significant compounds such as, vitamin B5, riboflavin, citric acid, and isoflavonoid derivate – medicarpin, noscapine were detected only in WE. Apigenin was determined in all extracts. WE indicated the most shield effect on pDNA against oxidative damage. Half-maximal inhibitory concentrations of extracts on breast cancer cells were calculated with MTT cell viability test. Bax gene was up-regulated and anti-apoptotic gene known as Bcl-2 was down-regulated on MDA-MB-231 cells after treated with WE. TERT-1 gene was down-regulated after treated with EAE and ME for MDA-MB-231 and MCF-7 cells, respectively. Cell migration ability of both MDA-MB-231 and MCF-7 cells was prevented with EAE and ME. A more effective treatment strategy can be applied by combining these extracts with commercial chemotherapy drugs which cause apoptosis and cell migration inhibition in vitro.
Exploring the nutraceutical potential of dried pepper capsicum annuum L. on market from altino in abruzzo region
(2020-05-01) Valle A.D.; Dimmito M.P.; Zengin G.; Pieretti S.; Mollica A.; Locatelli M.; Cichelli A.; Novellino E.; Ak G.; Yerlikaya S.; Baloglu M.C.; Altunoglu Y.C.; Stefanucci A.
Sweet pepper is a typical type of Capsicum annuum 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.
Integration of in vitro and in silico approaches to assess three Astragalus species from Turkey flora: A novel spotlight from lab bench to functional applications
(2022-10-01) Zengin G.; Uba A.I.; Ocal M.; Sharifi-Rad M.; Caprioli G.; Angeloni S.; Altunoglu Y.C.; Baloglu M.C.; Yıldıztugay E.
Members of the genus Astragalus have a great interest as a source of natural bioactive compounds on a scientific platform. To provide multidirectional insights into three Astragalus species (A. setulosus, A. anthylloides, and A. ovalis), the current work focused on the chemical characterization and biological properties of their extracts (aerial parts and roots). The chemical characterization of the extracts was detected by HPLC-MS/MS analysis. The biological properties were evaluated by antioxidant, enzyme inhibitory, and cytotoxic parameters. Assays for radical quenching, reducing capacity, and metal chelation were also used to evaluate antioxidant properties. To test the enzyme inhibitory effects of the extracts, cholinesterases, tyrosinase, α-amylase, and α-glucosidase were utilized as target enzymes. Two cancer cell lines, (MCF-7 (human breast cancer cell line) and HeLa (Human cervix cancer cell line), were selected to evaluate cytotoxic effects. Generally, 5- caffeoylquinic acid (2.43–283.92 μg/g extract), hyperoside (4.33–216.22 μg/g extract) and rutin (1.09–184.98 μg/g extract) were the main constituents. The extracts from aerial parts and roots of A. anthylloides showed stronger radical scavenging and reducing power abilities compared to A. setulosus and A. ovalis. The best AChE and BChE inhibitory effects were determined in the aerial parts of A. setulosus (2.18 mg GALAE/g) and roots of A. ovalis (4.76 mg GALAE/g), respectively. The extracts of A. ovalis had the highest tyrosinase inhibitory abilities. The extract from aerial parts of A. setulosus showed stronger cytotoxic effects compared to other extracts. Pearson's correlation analysis revealed that the presence of some compounds (resveratrol, p-coumaric, 5-caffeoylquinic, and ferulic acids, etc) was linked to the observed biological activities. Molecular docking was also provided for the possible interaction of enzymes as well as protein targets of the tested cell lines. Our findings provide a scientific basis for the Astragalus species, which may serve as a source of naturally occurring bioactive compounds for health-promoting applications.
Investigation of chemical profile, biological properties of Lotus corniculatus L. extracts and their apoptotic-autophagic effects on breast cancer cells
(2019-09-10) Yerlikaya S.; Baloglu M.; Diuzheva A.; Jekő J.; Cziáky Z.; Zengin G.
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
(2018-10-01) Locatelli M.; Yerlikaya S.; Baloglu M.; Zengin G.; Altunoglu Y.; Cacciagrano F.; Campestre C.; Mahomoodally M.; Mollica A.
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 Boerhavia diffusa extracts: A potential raw material for functional applications
(2021-12-01) Sinan K.I.; Akpulat U.; Aldahish A.A.; Altunoglu Y.C.; Baloğlu M.C.; Zheleva-Dimitrova D.; Gevrenova R.; Lobine D.; Mahomoodally M.F.; Etienne O.K.; Zengin G.; Mahmud S.; Capasso R.
Boerhavia diffusa 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 B. diffusa. 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 B. diffusa as a potential candidate for functional applications in the preparation.
Multi-targeted potential of Pittosporum senacia Putt.: HPLC-ESI-MSⁿ analysis, in silico docking, DNA protection, antimicrobial, enzyme inhibition, anti-cancer and apoptotic activity
(2019-12-01) Mahomoodally M.; Picot-Allain C.; Hosenally M.; Ugurlu A.; Mollica A.; Stefanucci A.; Llorent-Martínez E.; Baloglu M.; Zengin G.
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 (IC50 = 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.
Multidirectional insights on Chrysophyllum perpulchrum leaves and stem bark extracts: HPLC-ESI-MS ⁿ profiles, antioxidant, enzyme inhibitory, antimicrobial and cytotoxic properties
(2019-08-01) Baloglu M.C.; Llorent-Martínez E.J.; Aumeeruddy M.Z.; Mahomoodally M.F.; Altunoglu Y.C.; Ustaoglu B.; Ocal M.; Gürel S.; Bene K.; Sinan K.I.; Zengin G.
Chrysophyllum 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-MS n) . 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 α-amylase inhibitor while the leaf methanolic extract exhibited the highest tyrosinase and α-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 μg/ml. Bark extracts of C. perpulchrum were very effective against Salmonella kentucky, Proteus vulgaris and Staphylococcus aureus at 62.5 μg/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 (IC 50= 264 μg/mL after 48 h). In light of the above, C. perpulchrum might provide health benefits against oxidative stress and the associated chronic diseases. Nonetheless, the detailed mechanism of action is yet to be further investigated.
New perspectives into the chemical characterization of Sida acuta Burm. f. extracts with respect to its anti-cancer, antioxidant and enzyme inhibitory effects
(2021-06-01) Uysal S.; Gevrenova R.; Sinan K.I.; Bayarslan A.U.; Altunoglu Y.C.; Zheleva-Dimitrova D.; Ak G.; Baloglu M.C.; Etienne O.K.; Lobine D.; Mahomoodally M.F.; Zengin G.
The chemical components, in vitro antioxidant capacities and enzyme inhibitory effects of dichloromethane (DCM), ethyl acetate (EA), methanol (MeOH) and water extracts of the medicinal plant, Sida acuta Burm. f. were evaluated. The individual phenolic components were assessed via ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS). In terms of chemical composition, phenolics (hydroxybenzoic and hydroxycinnamic acids) and flavonoids were identified as main groups. The antioxidant capacities were evaluated using a panoply of cell-free bioassays and the enzymatic inhibitory potentials against key enzymes involved in human diseases were also determined. The water extract exhibited the strongest scavenging abilities on DPPH (IC50: 1.05 mg/mL) and ABTS (IC50: 1.02 mg /mL). The best cholinesterase inhibitory abilities were observed with the methanol extract (IC50: 0.51 and 0.52 mg/mL for AChE and BChE, respectively), while DCM exhibited the strongest α-amylase (IC50: 1.21 mg/mL) and α-glucosidase (IC50: 0.62 mg/mL) inhibitory effects. The anti-cancer effects of methanol and water extracts were tested on human breast cancer cells, MDA-MB-231, and the methanol extract showed the best anti-cancer effect with an IC50 value of 102.4 μg/mL. In conclusion, the experimental data have demonstrated promising pharmacological activities of S. acuta extracts obtained using different solvents, thereby providing a scientific basis for the validation of the traditional medicinal uses of this plant.
Novel in vitro and in silico insights of the multi-biological activities and chemical composition of Bidens tripartita L.
(2018-01-01) Uysal S.; Ugurlu A.; Zengin G.; Baloglu M.C.; Altunoglu Y.C.; Mollica A.; Custodio L.; Neng N.R.; Nogueira J.M.F.; Mahomoodally M.F.
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
(2019-01-01) Mahomoodally M.F.; Yerlikaya S.; Llorent-Martínez E.J.; Uğurlu A.; Baloglu M.C.; Altunoglu Y.C.; Mollica A.; Dardenne K.K.; Aumeeruddy M.Z.; Puchooa D.; Zengin G.
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 (IC50 = 533.1 μg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC50 = 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.