DNA Protective Properties Research Articles

A novel sustainable and ecofriendly UV-Spectrophotometric method for the determination of Naringenin in bulk and vaginal niosomal nanoformulation

Naringenin, a flavonoid found in several fruits like oranges, grapefruit, and bergamot, exhibits a wide range of biological effects. These include antidiabetic, antidepressant, antiatherogenic, antitumor, immunomodulatory, anti-inflammatory, hypolipidemic, antioxidant, peroxisome proliferator-activated receptors (PPARs) activation, hepatoprotective properties, memory enhancement and DNA protective properties. The aim of this current study is to develop a simple and precise UV spectrophotometric technique for measuring Naringenin Active Pharmaceutical Ingredient (API) in bulk and vaginal niosomal nanoformulation using PBS (Phosphate buffer solution) pH 4.5. The absorption peak of Naringenin was identified at 287 nm, and it adhered to Beer's law within the concentration range of 2 to 14 µg/ml. The calibration curve demonstrates a linear relationship between absorbance and concentration within the range of 2 to 14 µg/ml. The determined limit of detection and limit of quantification were found to be 0.587672µg/mL and 1.780824µg/mL, respectively. The validity of the method was assessed for repeatability, accuracy and precision. The results obtained indicated minimal intraday and interday variation. The excipients in the nanoformulation did not interfere the analysis. The developed analytical UV spectrophotometric method is simple, rapid and consistent, making it suitable for estimating the drug in both bulk and nanoformulation.

Pumpkin seed oil lessens the colchicine-induced altered sex male hormone balance, testicular oxidative status, sperm abnormalities, and collagen deposition in male rats via Caspase3/Desmin/PCNA modulation

This study examined the efficiency of pumpkin seed oil (PSO) to rescue the colchicine (CHC)-induced adverse impacts on sperm characteristics, male sex hormones, testicular architecture, oxidative status, DNA content, collagen deposition, and immune expression of desmin and PCNA. Male Sprague Dawley rats were divided into four experimental groups (n = 10 each): control (distilled water), CHC (0.6 mg/kg b.wt), PSO (4 mL/kg b.wt), and CHC + PSO. After 60 days of dosing, CHC significantly reduced sperm motility (19%), sperm concentration (38%), estradiol (52%), testosterone (37%), luteinizing hormone (54%), and follicle-stimulating hormone (29%) compared to the control. Yet, the testicular tissues of CHC-administered rats exhibited elevated abnormal sperms (156%), malondialdehyde (354%), lactate dehydrogenase (73%), Caspase-3 (66%), and 8-hydroxyguanosine (65%) but lower reduced glutathione (74%), catalase (73%), and superoxide dismutase (78%) compared to the control group. Moreover, CHC induced testicular degeneration, distorted seminiferous tubules, apoptotic cells, exfoliated spermatogenic cells, reduced DNA content, decreased PCNA and desmin immune-expression, and increased collagen deposition. PSO effectively reversed the CHC-induced alterations in sperm quality and testicular function and architecture, likely through its antioxidant, antifibrotic, anti-apoptotic, and DNA-protective properties. These results suggest that PSO may be a beneficial intervention for long-term CHC users and may protect against CHC-induced male reproductive toxicity.

In Vitro Bioactivities and In Silico ADME Profile for Potential Biological Target Prediction of Selected Phytochemicals Using Six Nepeta Species

AbstractSeveral Nepeta species, used in traditional uses, represent sources of valuable phytochemical composition, as well as in vitro biological and in silico clinical activities. In the present study, the antioxidant and DNA protective properties of methanol: chloroform (1 : 1) extracts of six Nepeta species were evaluated by comparison with standards. In HPLC‐MS/MS analysis, the main components of the extracts were identified as rosmarinic acid, caffeic acid, chlorogenic acid, shikimic acid, and scutellarin. In the GC‐FID analysis, the highest components were palmitate and cis‐11‐eicosenoic acid. N. aristata has the greatest total phenol and flavonoid contents. N. baytopii, N. aristata, N. italica, N. stenantha, and N. nuda exhibited the highest antioxidant activities. The N. nuda, N. aristata, N. italica, and N. trachonitica extracts were shown to have the most potent DNA protection activity. According to the result of the GC‐FID and HPLC‐MS/MS analysis of Nepeta extracts, ADMET studies of the main components of the extracts were performed. It was evaluated that palmitic acid had BBB permeability, but oleic acid was toxic. The in vitro and in silico results confirmed that Nepeta L. extracts are potential natural products.

Comprehensive evaluation of Ixoroside: An iridoid glycoside from Nepeta aristata and N. baytopii, assessing antioxidant, antimicrobial, enzyme inhibitory, DNA protective properties, with computational and pharmacokinetic analyses

Ixoroside, an iridoid glycoside, was isolated from two endemic plants, Nepeta aristata and Nepeta baytopii and its structure was elucidated by comprehensive analysis with NMR and mass spectrophotometers. It was observed that the compound exhibited strong antioxidant activity in phosphomolybdenum-reducing power (55.65±0.02 μg/mL), H2O2 (2.97±0.50 μg/mL), and superoxide anion scavenging (11.31±0.19 μg/mL) activities. It has also been noted that the ixoroside molecule has enzyme inhibitor (7.01±0.001 μg/mL for urease, 19.06±0.51 μg/mL for AChE, 9.90±0.5 μg/mL for BChE, 16.87±0.08 μg/mL for α-amylase, 4.11±0.36 μg/mL for α-glucosidase and 2.23±0.001 μg/mL for tyrosinase) and DNA protective effect (55.14% for Form I) and antibacterial (10 mm against K. pneumoniae, 9.00 mm against E. faecalis and 11.00 mm against S. aureus, 128 μg/mL against E. coli and E. faecalis). In silico studies, density functional theory (DFT) and molecular docking were performed to elucidate ixoroside interaction with enzymes. In enzyme inhibition kinetics, ixoroside exhibited strong interaction with urease (Ki, 0.11 mM, mixed-uncompetitive), α-glucosidase (Ki, 0.10 mM, noncompetitive) and tyrosinase (Ki, 0.10 mM, noncompetitive). Additionally, BChE was observed to interact strongly with α-glucosidase and tyrosinase with binding constants of 0.49, 1.19 and 3.15 μM in molecular docking. Moreover, the pharmacological properties of ixoroside examined by adsorption, distribution, metabolism, excretion and toxicity (ADMET) showed that the molecule has drug-like properties.

Molecular characterization, cytoprotective, DNA protective, and immunological assessment of peroxiredoxin-1 (Prdx1) from yellowtail clownfish (Amphiprion clarkii)

Peroxiredoxin-1 (Prdx1) is a thiol-specific antioxidant enzyme that detoxifies reactive oxygen species (ROS) and regulates the redox status of cells. In this study, the Prdx1 cDNA sequence was isolated from the pre-established Amphiprion clarkii (A. clarkii) (AcPrdx1) transcriptome database and characterized structurally and functionally. The AcPrdx1 coding sequence comprises 597 bp and encodes 198 amino acids with a molecular weight of 22.1 kDa and a predicted theoretical isoelectric point of 6.3. AcPrdx1 is localized and functionally available in the cytoplasm and nucleus of cells. The TXN domain of AcPrdx1 comprises two peroxiredoxin signature VCP motifs, which contain catalytic peroxidatic (Cp-C52) and resolving cysteine (CR-C173) residues. The constructed phylogenetic tree and sequence alignment revealed that AcPrdx1 is evolutionarily conserved, and its most closely related counterpart is Amphiprion ocellaris. Under normal physiological conditions, AcPrdx1 was ubiquitously detected in all tissues examined, with the most robust expression in the spleen. Furthermore, AcPrdx1 transcripts were significantly upregulated in the spleen, head kidney, and blood after immune stimulation by polyinosinic:polycytidylic acid (poly (I:C)), lipopolysaccharide (LPS), and Vibrio harveyi injection. Recombinant AcPrdx1 (rAcPrdx1) demonstrated antioxidant and DNA protective properties in a concentration-dependent manner, as evidenced by insulin disulfide reduction, peroxidase activity, and metal-catalyzed oxidation (MCO) assays, whereas cells transfected with pcDNA3.1(+)/AcPrdx1 showed significant cytoprotective function under oxidative and nitrosative stress. Overexpression of AcPrdx1 in fathead minnow (FHM) cells led to a lower viral copy number following viral hemorrhagic septicemia virus (VHSV) infection, along with upregulation of several antiviral genes. Collectively, this study provides insights into the function of AcPrdx1 in defense against oxidative stressors and its role in the immune response against pathogenic infections in A. clarkii.

Molecular docking, molecular dynamics, MM/PBSA approaches and bioactivity studies of nepetanudoside B isolated from endemic Nepeta aristata

Nepetanudoside B (NNB) was isolated from aerial parts of endemic Nepeta aristata crude extract (CH3OH-CHCl3) using silica gel (n-hexane, methanol, ethyl acetate, and dichlorometane, respectively) and sephadex LH-20 (65% Methanol-35% Chloroform) column chromatographies. Preparative-HPLC was used to purify NNB after activity-guided isolation of methanol sub-fractions with enzyme inhibitory and DNA protective properties. The NNB was determined using 1H,13C, COSY, HSQC, HMBC, and LC-MS/MS. The study compared the effects of NNB with conventional drugs in terms of its ability to inhibit enzymes such as urease, α-amylase, carbonic anhydrase (CA), lipase, α-glucosidase, and tyrosinase, as well as its ability to protect DNA. Enzyme kinetic and molecular docking were also used to evaluate this. NNB exhibited the best inhibitory activity on urease (1.28 ± 0.00 µg/mL), lipase (5.83 ± 0.10 µg/mL), BChE (3.73 ± 0.46 µg/mL), tyrosinase (7.39 ± 0.00 µg/mL), α-glucosidase (10.95 ± 0.00 µg/mL), α-amylase (22.11 ± 1.03 µg/mL) and AChE (25.68 ± 3.32 µg/mL), respectively. NNB has higher MolDock scores with binding energy in α-glucosidase (-233) and BChE (-8.90 kcal/mol). In enzyme kinetics studies, it was determined that urease, AChE, α-glucosidase, lipase, and CA were non-competitive , while BChE and tyrosinase were competitive inhibition mechanisms. Their Ki values were calculated as 0.09, 0.24, 0.09, 0.10, 0.08, 0.05, and 0.07 mM, respectively. Molecular dynamics simulation studies were performed for the interactions of NNB-BChE with MM/PBSA binding free energey RMSD, RMSF, Rg, SASA, and also the number of hydrogen bonds was calculated. The suitability and effectiveness of NNB have been proven in the food and pharmaceutical industries. The NNB molecule may lead to development studies as a BChE inhibitor. Communicated by Ramaswamy H. Sarma

An Overview of Chemical Constituents, Medicinal Properties, Clinical Trials, and Patents of Twigs of Morus alba (Ramulus Mori)

Abstract The rich chemical constituents and diverse pharmacological properties of Ramulus Mori (RM) or the twig of Morus alba with evidence supported by clinical trials and patents are reviewed. Known as Sangzhi in Chinese, RM is widely used in traditional Chinese medicine to treat gout, arthritis, and rheumatism. Chemical constituents include flavonoids, benzofurans, alkaloids, stilbenes, chalcones, phenolic acids, and coumarins. Bioactivities of RM include antidiabetic, anti-obesity, anti-inflammatory, antityrosinase, neuroprotective, antioxidant, hepatoprotective, cytoprotective, renoprotective, antihyperuricemic, analgesic, antifungal, DNA protective, anticancer, gastroprotective, cardioprotective, anti-hair aging, anti-arthritic, and antiplatelet aggregation properties. The most active compounds from RM are mulberrin, oxyresveratrol, and mulberroside A. All four clinical trials on RM are focused on the treatment of diabetes. The patents entail using RM extracts as cosmetics for skin whitening and as agents for hypoglycemia. Topics for further research on RM are suggested.

The Bioactivity of a Hydroxytyrosol-Enriched Extract Originated after Direct Hydrolysis of Olive Leaves from Greek Cultivars.

Nowadays, olive leaf polyphenols have been at the center of scientific interest due to their beneficial effects on human health. The most abundant polyphenol in olive leaves is oleuropein. The biological properties of oleuropein are mainly due to the hydroxytyrosol moiety, a drastic catechol group, whose biological activity has been mentioned many times in the literature. Hence, in recent years, many nutritional supplements, food products, and cosmetics enriched in hydroxytyrosol have been developed and marketed, with unexpectedly positive results. However, the concentration levels of hydroxytyrosol in olive leaves are low, as it depends on several agricultural factors. In this study, a rapid and easy methodology for the production of hydroxytyrosol-enriched extracts from olive leaves was described. The proposed method is based on the direct acidic hydrolysis of olive leaves, where the extraction procedure and the hydrolysis of oleuropein are carried out in one step. Furthermore, we tested the in vitro bioactivity of this extract using cell-free and cell-based methods, evaluating its antioxidant and DNA-protective properties. Our results showed that the hydroxytyrosol-enriched extract produced after direct hydrolysis of olive leaves exerted significant in vitro antioxidant and geno-protective activity, and potentially these extracts could have various applications in the pharmaceutical, food, and cosmetic industries.

Synergistic interaction between Bambusa arundinacea and Euphorbia hirta leaf extract on antioxidant, antiglycation and DNA protective properties.

Oxidative stress and enhanced non-enzymatic protein glycation result in the pathogenesis of various disorders in humans, including diabetes mellitus. This study examined the synergistic action of Bambusa arundinacea with Euphorbia hirta leaf extract for anti-oxidant potential, antiglycation effect on fructose-mediated proteins, and DNA-protective properties. The methanolic extract shows significantly (P<0.01) higher total phenolic and flavonoid content when compared with ethyl acetate and hexane extract in both plants. The combined methanolic extract (CME) of both plants exhibits higher antioxidant potential, as indicated by the lower IC50 values obtained for DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity (4.82 μg/ml) and NO (nitric oxide) scavenging activity (3.94 μg/ml) with stronger Trolox equivalent antioxidant capacity when compared to B. arundinacea and E. hirta individually. The antiglycation analysis revealed that CME is more potent to inhibit fructose-mediated glycation of human serum albumin (HSA) at the early and middle stages. In addition to this, CME more effectively inhibits protein glycation in the late phase, which was confirmed by declining fluorescence intensity. Furthermore, a high degree of positive correlation was obtained between antioxidant and antiglycation capacities through Pearson’s correlation coefficient. The results also demonstrated that CME displays a synergistic effect in protecting DNA from oxidative damage and preventing the formation of glycation of DNA.

Palm Fruit (Phoenix dactylifera L.) Pollen Extract Inhibits Cancer Cell and Enzyme Activities and DNA and Protein Damage.

Palm fruit pollen extract (PFPE) is a natural source of bioactive polyphenols. The primary aim of the study was to determine the antioxidant, antimicrobial, anticancer, enzyme inhibition, bovine serum albumin (BSA), and DNA-protective properties of PFPE and identify and quantify the phenolic compounds present in PFPE. The results demonstrated that PFPE exhibited potent antioxidant activity in various radical-scavenging assays, including (2,2-diphenyl-1-picrylhydrazyl) (DPPH•), 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS•), nitric oxide (NO), ferric-reducing/antioxidant power (FRAP), and total antioxidant capacity (TAC). PFPE also displayed antimicrobial activity against several pathogenic bacteria. Similarly, PFPE reduced acetylcholinesterase, tyrosinase, and α-amylase activities. PFPE has been proven to have an anticancer effect against colon carcinoma (Caco-2), hepatoma (HepG-2), and breast carcinoma (MDA) cancer cells. Apoptosis occurred in PFPE-treated cells in a dose-dependent manner, and cell cycle arrest was observed. Furthermore, in breast cancer cells, PFPE down-regulated Bcl-2 and p21 and up-regulated p53 and Caspase-9. These results show that PFPE constitutes a potential source of polyphenols for pharmaceutical, nutraceutical, and functional food applications.

Biofilm formation and auto-aggregation abilities of novel targeted aqua-probiotics

Background: The probiotics’ auto-aggregation and biofilm formation abilities have a significant role in the development of biotechnological processes.Objective: The aim of this study was to evaluate the biofilm formation and auto-aggregation abilities of novel, targeted aqua-probiotics isolated from aquatic organisms.Methods: The biofilm formation abilities of Lactobacillus delbrueckii str. UZ-1, Lactiplantibacillus plantarum str. R3, Lactococcus str. UZ-2, Enterococcus faecium str. R2, Pediococcus acidilactici str. N from the culture collection of the Microbiology of the Academy of Sciences of the Republic of Uzbekistan, Bacillus subtilis str. 1R, Bacillus amyloliquefaciens str. 4R and from the culture collection of the Southern Federal University of Russa and Lacticaseibacillus rhamnosus str. 1A and Enterococcus str. 9-3 from the culture collection of the Armenian National Agrarian University were assessed.Results: According to the investigations, the biofilm formation abilities of Lactobacillus delbrueckii str. UZ-1, Lactiplantibacillus plantarum str. R3, Lactococcus str. UZ-2, Enterococcus faecium str. R2, Pediococcus acidilactici str. N, Bacillus subtilis str. 1R, Bacillus amyloliquefaciens str. 4R, Bacillus amyloliquefaciens str. 5R, Lacticaseibacillus rhamnosus str. 1A and Enterococcus str. 9-3 were 0.119 ± 0.05D, 0.113 ± 0.065D, 0.196 ± 0.04D, 0.116 ± 0.01D, 0.152 ± 0.05D, 0.74 ± 0.15D, 2.621± 0.55D, 1.831 ± 0.45D, and 0.227 ± 0.04D and 0.483 ± 0.15D respectively. The highest rate of auto-aggregation was shown by Bacillus amyloliquefaciens str. 5R, and Bacillus amyloliquefaciens str. 4R was the strain with the highest ability to form biofilm. These two Bacillus strains are also distinguished by the highest DNA protective properties and relatively low antioxidant activity. Despite the fact that Bacillus amyloliquefaciens str. 5R showed the highest rate of auto-aggregation after 2 hours, this strain showed the lowest level of auto-aggregation among the studied strains after 24 hours. The Enterococcus str. 9-3 strain with the highest antioxidant activity showed 0.483 ± 0.15D biofilm formation ability.Conclusion: The novel targeted aquaprobiotics have distinct biofilm formation and aggregation properties, which are important to consider when planning appropriate biotechnological processes, requiring specific membrane properties of probiotics.Graphical Abstract: Membrane properties of novel targeted aquaprobiotics.Keywords: Lactobacilli, aqua-probiotic, antioxidant activity, biofilm formation, aggregation, Enterococcus str. 9-3

Evaluation of DNA Protective and Antimicrobial Properties of some Cladonia Species

The present study evaluated the DNA protective properties and antimicrobial activities of the methanol extracts of nine Cladonia species, namely C. pocillum, C. subulata, C. pyxidata, C. coniocraea, C. foliacea, C. firma, C. furcata, C. fimbriata and C. rangiformis collected in Turkey. DNA protection properties efficiency of Cladonia extracts was evaluated using pBR322 plasmid DNA. In vitro antimicrobial activities of methanol extracts against two Gram-negative bacteria (Escherichia coli and Proteus mirabilis), three Gram-positive bacteria (Staphylococcus aureus, Micrococcus luteus and Bacillus subtilis) and two fungal strains (Candida glabrata and Candida albicans) were examined using the disc diffusion method and through the determination of minimal inhibitory concentrations (MIC). DNA protective studies, all Cladonia extracts protected pBR322 plasmid DNA against damage caused by the hydrogen peroxide (H2O2) with ultraviolet (UV). The results demonstrated that the inhibition zones in the disc diffusion method ranged from 6.5 to 19.0 mm. MIC results were ranged from 3.12 to 6.25 mg/mL. Cladonia extracts show a better antimicrobial effect against bacterial strains than fungal strains. The highest antimicrobial effect among lichen species was demonstrated by Cladonia pocillum. Our results demonstrated that tested Cladonia extracts had strong antibacterial and DNA protective effects. This is the first comprehensive study to evaluate the DNA protective properties activity of Cladonia extracts.

Antioxidant and antimutagenic properties of probiotic Lactobacilli determined using LUX-biosensors

The initial screening of probiotic strains in vitro, carried out by different methods, may omit strains that are promising from the point of view of biotechnology or, conversely, mark as promising strains those that will lose activity when transferred in vivo. It is known that the release of metabolites by probiotic bacteria, in particular, lactobacilli, is highly dependent on the biochemical context. In this work, we modified the method that was previously successfully used for the selection of probiotics for poultry, based on their antioxidant and DNA-protective properties. A comparison was made of this activity on standard media and on an artificial intestinal medium that mimics the intestines of a bird. As a result, three Lactobacillus strains were selected, which not only exhibit antioxidant and DNA-protective properties but also do not lose these activities in an artificial intestinal medium.

Eryngium Billardieri F. Dolaroche'den (Boğa Dikeni) Hazırlanan Ekstraktlarin Fenolik İçerikleri Ve Biyolojik Özellikleri

In this study, Eryngium billardieri was collected from Patnos district of Ağrı province during the vegetation period. While some of the collected plant was stored fresh in a -86oC freezer, the other part was preserved as herbarium material. After the species of the plant were identified, methanol and pure water extracts were prepared from the aerial parts of the fresh and herbarium samples. The phenolic contents of the extracts were determined by using HPLC. Moreover, various in vitro antioxidant properties and DNA protective properties of the relevant extracts were tested. The comparison of the test results showed that the phenolic compounds of the fresh plant extracts were more than that of herbarium extracts. Although both extracts showed good antioxidant activities, their activity was lower than the standart antioxidants. Moreover, herbarium extracts were seen to have a relatively better effect on the pUC18 DNA stabilization, irrespective of the presence of H2O2 in the environment. Having considered that there is limited number of studies on E.billardieri in the literature, this study will offer important insights into the studies in this area.

Role of Glucosinolates in the Nutraceutical Potential of Selected Cultivars of Brassica rapa.

Brassica rapa L. subsp. rapa (turnip greens), a traditionally consumed vegetable, is well-known due to its high content of glucosinolates, which are secondary metabolites with a positive biological activity for human health. Our hypothesis has been based on the relation between B. rapa glucosinolate content and its healthy properties, and our aim is to establish guidelines for safe B. rapa vegetable consumption. Three B. rapa cultivars (143N5, 143N7 and 163N7) have been characterized by HPLC analysis of purified extracts from leaf samples in order to determine their glucosinolate content and to relate this content to beneficial effects on DNA protection, lifespan extension and chemoprevention. In order to ascertain the heath properties in vitro and in vivo, toxicity activities were assayed in the Drosophila melanogaster and leukaemia cell models; genomic safety was also assessed in both models using genotoxicity, fragmentation and comet assay. The Drosophila model has also been used to study the antioxidative activity and the longevity induction. Our results showed a relationship between B. rapa glucosinolate content and its safety and benefices in its consumption. Gluconapin, the main B. rapa glucosinolate, was directly related with these wholesome effects. The relevant conclusion in the present research is focused on B. rapa cultivar 163N7 due to its high gluconapin content and low progoitrin content, which exert anti-cancer and DNA protection properties and could be recommended as being safe and healthy for human consumption.

Cytotoxicity and DNA protective effects of the Terfezia and Picoa species from the eastern region of Turkey

Background and Aims: This study aims to investigate the cytotoxicity and DNA protective effects of semi-arid, arid, or desert truffles such as the Terfezia and Picoa species. Methods: The DNA protective effects of the Terfezia and Picoa species was evaluated using plasmid pBR322 DNA treated with UV and H2O2. The cytotoxic effects of water and methanol extracts of the Terfezia and Picoa species on H1299 and HUVEC cells were evaluated using the MTT assay. Results: Higher concentrations of T. olbiensis and P. lefebvrei extracts have demonstrated a DNA protective effect. The water extract of P. juniperi only at a 40 mg/mL concentration demonstrated a DNA-protective effect, whereas T. boudieri extract did not show any DNA-protective effect at all concentrations tested. H1299 cells showed more sensitivity to the water extract of T. olbiensis (4.66%), P. juniperi (12.04%), P. lefebvrei (21.93%), and the methanol extract of T. boudieri (20.93%). In general, the water and methanol extracts of the Terfezia and Picoa species demonstrated the least cytotoxic effects on HUVEC cells, except for the water extract of P. juniperi (38.46%). Conclusions: In conclusion, results obtained from this study show that the Terfezia and Picoa truffle species have potential DNA protective and cancer prevention properties.

Antiproliferative properties and structural analysis of newly synthesized Schiff bases bearing pyrazole derivatives and molecular docking studies

New pyrazole Schiff bases containing azo groups were synthesized using the condensation reaction between p-nitrobenzaldehyde and (E)-4-(phenyl)-1-H-pyrazole-3,5-diamine in the molar ratio of 1:2. Characterization of the compounds was performed by spectroscopic techniques, including IR, UV-Vis, 1H-NMR and 13C-NMR. Biological activity of the compounds was evaluated by analyzing DNA protection, antimicrobial and anticancer properties. Compound 4 was effective for Salmonella typhimurium with the MIC concentration of 62.5 µg/mL. Moreover, this compound had the highest protection activity on DNA. Cytotoxic activity of compound 4 was determined on the HeLa cancer cell line with the IC50 concentration of 976.6 µM. The anti-cancer characteristic of compounds 4 and 5 for HeLa cancer was theoretically analyzed by molecular docking study as well. Among the tested compounds, compound 4 possessed significant results due to its in vitro cytotoxic properties. Therefore, it may be considered as a potential bioactive agent for cancer treatment studies. In addition, further in vivo analysis can be performed to indicate its anticancer property.

Some biological properties of ethanol extract prepared from the aerial parts of Scutellaria albida L. subsp. condensata (Rech.f.) J.R. Edm.

Moderate effects of some plants with proven biological properties in the treatment of various diseases have increased the importance of them and the interest in alternative medicine. The members of the Lamiaceae family are one of the widely used in alternative medicine and agriculture due to their metabolite content. In order to gain valuable biological data for alternative medicine and new studies, Scutellaria albida subsp. Candensest a member of the Lamiaceae family was collected from a height of 1500 meters in Bitlis province in Turkey. Ethanol (EtOH) extract was prepared by using the aerial parts of the plant and used in all stages of the study. Firstly, the phenolic content of the extract was determined by HPLC. Myricetin and 4-Hydroxybenzoic acid at the highest concentrations were detected, but ascorbic acid, gallic acid, quercetin, and 3,4-Dihydroxybenzoic acid could not be determined in the extract. In order to test the antioxidant properties based on phenolic content, several in vitro antioxidant tests were performed and DNA protective properties were investigated. In the biological activity results, the extract was determined to have a similar antioxidant effect to standards or lower than them and exhibited relatively DNA protective activity at high concentration. Finally, the effects of the extract on some types of bacteria and fungi were investigated by the hollow agar method and 150 µL volume of the extract was shown to have better activity than ampicillin and Amikacin. Due to the limited studies on Scutellaria albida subsp Candensest, it is thought that this study will contribute to the literature.

Comprehensive approaches on chemical composition and biological properties of Daphne pontica L. extracts

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 .

Simultaneous study of antioxidant activity, DNA protection and anti-inflammatory effect of Vernonia amygdalina leaves extracts.

Vernonia amygdalina (VA) has been reported to have antioxidant potential; however, its DNA protection and anti-inflammatory properties remain unclear. We aimed to investigate whether aqueous (WEVAL) and alcoholic (EEVAL) VA extracts exert similar antioxidant, DNA protection and anti-inflammatory effects and attempted to explore the mechanism underlying the anti-inflammatory effects. These results demonstrated that WEVAL had greater polyphenolic and flavonoid contents, as well as a stronger reducing power, DPPH radical scavenging and DNA protective activity. Moreover, both extracts reduced lipopolysaccharide (LPS)-induced expression of COX-II, iNOS, pro-inflammatory factors, including NO, TNF-α, IL-1β, and IL-10. Compared with WEVAL, EEVAL was a more potent inflammatory inhibitor. Both extracts similarly inhibited LPS-induced MAPK (p38) and NF-κB expression. Our findings indicate that WEVAL and EEVAL have diverse antioxidant and anti-inflammatory effects. WEVAL had a stronger antioxidant and DNA protection activity; contrastingly, EEVAL had a stronger anti-inflammatory ability. The anti-inflammatory activity involves reduced pro-inflammatory cytokines through NF-κB down-regulation and MAPK inhibition. These results demonstrated that production of WEVAL and EEVAL from VA leaves may provide a safe and efficacious source of pharmaceutical applications, with antioxidant, DNA protective and anti-inflammation activities.