DNA Protection Activity Research Articles

DNA-Protective, Antioxidant and Anti-Carcinogenic Potential of Meadowsweet (Filipendula ulmaria) Dry Tincture.

Nowadays, interest in natural antioxidants (especially phenolics) for the prevention of oxidative stress-related diseases is increasing due to their fewer side effects and more potent activity than some of their synthetic analogues. New chemical and pharmacological studies of well-known herbal substances are among the current trends in medicinal plant research. Meadowsweet (Filipendula ulmaria) is a popular herb used in traditional medicine to treat various diseases (including rheumatic-, inflammatory- and tumor-related disease, etc.). The dry tincture of Filipendulae ulmariae herba, collected from the Bulgarian flora, was analyzed using the HPLC method and bioassayed for antioxidant, antiproliferative and DNA-protective activities against oxidative damage. The HPLC phenolic profile showed 12 phenolics, of which salicylic acid (18.84 mg/g dry extract), rutin (9.97 mg/g de), p-coumaric acid (6.80 mg/g de), quercetin (4.47 mg/g de), rosmarinic acid (4.01 mg/g de) and vanillic acid (3.82 mg/g de) were the major components. The high antioxidant potential of the species was confirmed by using four methods, best expressed by the results of the CUPRAC assay (10,605.91 μM TE/g de). The present study reports for the first time the highly protective activities of meadowsweet dry tincture against oxidative DNA damage and its antiproliferative effect against hepatocellular carcinoma (HepG2 cell line). Meadowsweet dry tincture possesses great potential to prevent diseases caused by oxidative stress.

Investigation of Biological Activity of Squamarina cartilaginea (With.) P. James Species Distributed in Türkiye

In this study, the methanol extract of Squamarina cartilaginea, a species distributed in Türkiye, was investigated for its antimicrobial, antioxidant, cytotoxic, and DNA protective effects. The chemical composition of the extract was elucidated through spectroscopic determination of total phenols, total flavonoids, and chromatographic quantification of usnic acid. Antimicrobial activity was assessed using the disk diffusion method, revealing a significant zone of inhibition with a diameter of 17.5 mm against M. luteus and S. aureus. The antioxidant activity was evaluated through scavenging activities against DPPH and ABTS radicals, demonstrating a concentration-dependent potent scavenging activity against ABTS radicals. Cytotoxic activity was determined using the MTT method on DU-145 (Human Prostate Cancer Cell Line) and Colo 205 (Human Colon Cancer Cell Line) cell lines. The extract exhibited strong cytotoxic activity against the Colo 205 cell line, with a viability percentage of 33.16±2.01 at a concentration of 3.906 µg/mL. Furthermore, the S. cartilaginea extract demonstrated DNA protective activity on pBR322 plasmid DNA against UV and H2O2 exposure.

DNA interaction of selected tetrahydropyrimidine and its effects against CCl4-induced hepatotoxicity in vivo: Part II.

Tetrahydropyrimidine (compound A = methyl 4-[4'-(heptyloxy)-3'-methoxyphenyl]-1,6-dimethyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate) was chosen for in vivo studies after exhibiting noteworthy in vitro activity against the K562 and MDA-MB-231 cell lines, with IC50 values of 9.20 ± 0.14 µM and 12.76 ± 1.93 µM, respectively. According to experimental (fluorescence titration, viscosity, and differential scanning calorimetry) results, A interacts with DNA via the minor groove. In vivo, acute oral toxicity studies in Wistar albino rats proved no noticeable symptoms of either toxicity or death during the follow-up period. Genotoxic and antigenotoxic studies at three different concentrations of A (5, 10, and 20 mg/kg of body weight) in Wistar albino rats showed that the dose of 5 mg/kg body weight did not cause DNA damage and had a remarkable DNA protective activity against CCl4-induced DNA damage, with a percentage reduction of 78.7%. It is also important to note that, under the investigated concentrations of A, liver damage is not observed. Considering all experimental outcomes realized under various in vivo investigations (acute oral toxicity, genotoxicity, antigenotoxicity, and biochemical tests), compound A could be a promising candidate for further clinical testing.

The enzyme kinetic studies, DNA protection and antioxidant activities of furan/ thiophene-2-carboxamide derivatives

Three furan and/or thiophene-2-carboxamide compounds, namely N-(furan-2-ylmethyl)thiophene-2-carboxamide (1), N-(furan-2-carbonyl)furan-2-carboxamide (2), and N-(Thiophene-2-ylmethyl)furan-2-carboxamide (3) were investigated the enzyme kinetic studies by urease, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The inhibition constant (Ki) of Compound (CPD)3 by AChE was determined as 0.10 mM, and the Ki value by BChE was determined as 0.07 mM. In comparison, the Ki value of CPD1 by urease was determined as 0.10 mM. These CPDs were examined for antioxidant activity by the DPPH˙ scavenging method. CPD3 exhibited 98.93% DPPH scavenging activity compared to ascorbic acid, the positive control group. Furthermore, the DNA-protective activities of the compounds were investigated, and the DNA protection activity of CPD1 was observed to be 78%. The findings suggest that thiophene/furan carboxy amide-containing CPD1 and CPD3 might be exploited as potential structures for evaluating pharmaceuticals with greater potency.

Phytochemical profile, bioactivity, and molecular docking studies of natural edible mushrooms grown in Tokat and Sivas provinces of Turkey.

Mushrooms have been essential to the human diet because they contain balanced chemical components and some biologically active substances. In this work, we investigated the phenolics, essential oils, metal contents, antioxidant, antibacterial, DNA protective, and enzyme inhibition activities for Clitocybe geotropa, Ramaria aurea, Rhizopogon luteolus (RL), Russula delica (RD), Verpa bohemica, and Marasmius oreades mushrooms. Results exhibited a higher content for citric and succinic acids in all tested kinds. Further, we detected a high content of cis-9-oleic acid, linoleate, and cis-11-eicosanoate. All mushroom species contain a significant percentage of both Cu and Zn. Moreover, RL and RD recorded the highest phenolic and flavonoid contents. Furthermore, all samples showed standard to good antioxidant activity, and the same is true for the antibacterial and DNA protective activities. Enzyme inhibition activity was generally high and significantly higher against the urease than the thiourea. We applied molecular docking between the highest phenolic molecules with the urease to determine the mushroom extracts' high inhibition mechanism. In conclusion, all mushroom species revealed a variety in chemical content that is probably related to their multi-bioactivity.

Assessment of cytoprotective and genoprotective effects of Moringa oleifera and Tinospora cordifolia extracts in vitro.

Moringa oleifera and Tinospora cordifolia is extensively used as an ingredient of food and in traditional medicine for the management of a variety of diseases. The extracts of leaf of Moringa oleifera and stem of Tinospora cordifolia were assessed to examine their ability to inhibit the oxidative DNA damage (by DNA protection assay), cytoprotective and genoprotective potential (by Comet assay) in V79 cells individually and in combinations. It was found that these extracts could significantly inhibit the OH-dependent damage of pUC18 plasmid DNA. M. oleifera extract (160 and 320μg/mL) and Tinospora cordifolia extract (640, 1,280 and 2,560μg/mL) individually showed higher DNA protection activity. M. oleifera (1,280μg/mL) combined with Tinospora cordifolia (640μg/mL) showed best cytoprotective and genoprotective activities among different concentration combinations and various concentrations of individual plants in V79 cell line against hydrogen peroxide induced cytotoxicity and genotoxicity. This study demonstrates the cytoprotective and genoprotective activity of M. oleifera and Tinospora cordifolia individually or in combination.

Green solvent-based extraction of three Fabaceae species: A potential antioxidant, anti-diabetic, and anti-leishmanial agents

The Fabaceae is renowned for its diverse range of chemical compounds with significant biological activities, making it a valuable subject for pharmacological studies. The chemical composition and biological activities of three Fabaceae species were investigated using methanol separately and in combination with dimethyl sulfoxide (DMSO) and glycerol for extraction. The results revealed the highest phenolic (49.59 ± 0.38 mg gallic acid equivalent/g), flavonoid (29.16 ± 0.39 mg rutin equivalent/g), and alkaloid (14.23 ± 0.54 mg atropine equivalent/g) contents in the Caesalpinia decapetala methanol extracts. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and DNA protection activity were the highest (0.88 ± 0.43 μg/mL IC50 and 2149.26 band intensity) in Albizia julibrissin methanol extracts. The α-amylase activity was highest in all methanol extracts (<15 μg/mL IC50 values), while the α-glucosidase inhibition potential was highest (<1 μg/mL IC50 value) in the methanol–glycerol and methanol–DMSO extracts. Pearson coefficient analysis showed a strong positive correlation between the DPPH and α-amylase assays and phytochemicals. Anti-leishmanial activity was observed in decreasing order: A. julibrissin (74.75 %) > C. decapetala (70.86 %) > Indigofera atropurpurea (65.34 %). Gas chromatography-mass spectrometry revealed 33 volatile compounds and, aamong these (Z)-9-octadecenamide was detected in the highest concentration ranging from 21.85 to 38.61 %. Only the methanol extracts of the examined species could be assessed for in vivo studies for immediate applications.

Effects of Separation and Purification Methods on Antioxidation, Hypoglycemic and DNA Protection Activity of Fenugreek Polysaccharide.

Six low molecular weight fenugreek polysaccharides (FP) were isolated and purified by ethanol stepwise precipitation (EFP-20, EFP-40, and EFP-60) and DEAE-52 cellulose column method (DFP-0, DFP-0.15, and DFP-0.3), respectively. The effects of different separation and purification techniques on the preliminary properties and biological activities of fenugreek polysaccharides were compared. The results showed that the DEAE-52 cellulose-eluted fractions had a higher total sugar content and displayed a looser structure. The molecular weights of all six fractions were in the range of 4-19 kDa, with significant changes in the ratio of galactose to mannose. All six fractions contained α-D-galactopyranose and β-D-mannopyranose structures. Activity tests showed that all six fractions possessed antioxidant, hypoglycemic and DNA-protective activities. Among them, the DFP-0 fraction showed the highest activity. Overall, different isolation and purification methods lead to changes in the properties and bioactivities of FP, which provides a theoretical basis for the development and application of FP in functional foods and drugs.

A novel glycoglycerolipid from Holotrichia diomphalia Bates: Structure characteristics and protective effect against DNA damage

A lipidated polysaccharide, HDPS-2II, was isolated from the dried larva of Holotrichia diomphalia, which is used in traditional Chinese medicine. The molecular weight of HDPS-2II was 5.9 kDa, which contained a polysaccharide backbone of →4)-β-Manp-(1 → 4,6)-β-Manp-(1 → [6)-α-Glcp-(1]n → 6)-α-Glcp→ with the side chain α-Glcp-(6 → 1)-α-Glcp-(6 → linked to the C-4 of β-1,4,6-Manp and four types of lipid chains including 4-(4-methyl-2-(methylamino)pentanamido)pentanoic acid, 5-(3-(tert-butyl)phenoxy)hexan-2-ol, N-(3-methyl-5-oxopentan-2-yl)palmitamide, and N-(5-amino-3-methyl-5-oxopentan-2-yl)stearamide. The lipid chains were linked to C-1 of terminal α-1,6-Glcp in carbohydrate chain through diacyl-glycerol. HDPS-2II exhibited DNA protective effects and antioxidative activity on H2O2- or adriamycin (ADM)-induced Chinese hamster lung cells. Furthermore, HDPS-2II significantly ameliorated chromosome aberrations and the accumulation of reactive oxygen species (ROS), reduced γ-H2AX signaling and the expressions of NADPH oxidase (NOX)2, NOX4, P22phox, and P47phox in ADM-induced cardiomyocytes. Mechanistically, HDPS-2II suppressed ADM-induced up-regulation of NOX2 and NOX4 in cardiomyocytes, but not in NOX2 or NOX4 knocked-down cardiomyocytes, indicating that HDPS-2II could relieve intracellular DNA damage by regulating NOX2/NOX4 signaling. These findings demonstrate that HDPS-2II is a new potential DNA protective agent.

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.

Chemical Constituents and Bioactivities of Nepeta Taxa Essential Oils from Turkey: Principal Component Analysis, Molecular Docking Study, Molecular Dynamics, MM‐PBSA and Drug‐Likeness Estimation

AbstractNepeta taxa are popular plants and sources of traditional Turkish medicine. Chemical constituents in the essential oils (EOs) hydrodistilled from above‐ground parts of Nepeta aristata (NA), N. baytopii (NB), N. italica (NI), N. nuda (NN), and N. stenantha (NS) were determined using GC‐MS. The pharmacological activities of EOs, such as biological activities, were evaluated in vitro. DNA protection activities of NS‐EO were found to be the most effective. The NA‐EO, NI‐EO, and NS‐EO were more potent urease inhibitors, while the NS‐EO exhibited potent AChE inhibitors. Their molecular docking, molecular dynamics and enzyme inhibition results were compatible with the major components. Furthermore, MolDock and binding affinity results were found to be high. Moreover, AChE‐tau‐cadinol, BChE‐tau‐cadinol and tyrosinase‐Caryophyllene oxide complexes showed stability when simulated for 100 ns, with high MM‐PBSA energy values. In addition, the main components′ pharmacokinetic properties were observed to be effective. The present study showed that EOs may be valuable natural products for future pharmacological research, food, and the cosmetic industry according to in vitro and in silico values.

The Phytochemical constituents and biological activities of sungkai (Peronema canescens Jack) leaves hydroethanolic extracts

Peronema canescens, Jack commonly known as "sungkai," has been traditionally used as a herbal medicine for various health conditions. This study aimed to explore the bioactive compound of the P. canescens leaves hydroethanolic extract, along with assessing its antioxidant and antimutagenic properties. Liquid chromatography-mass spectrometry (LC-MS) was utilized for phytochemical analysis of the hydroethanolic extracts, while antioxidant activity was evaluated through the DPPH radical scavenging method. Quantification of total phenolic and flavonoid content was achieved via colorimetric analysis. Furthermore, the DNA protection activity was assessed using plasmid pBR322 subjected to free radical treatment. The primary bioactive compounds identified in the P. canescens hydroethanolic extracts belonged to the alkaloid and flavonoid groups. The antioxidant activity of P.canescens leaves hydroethanolic extracts showed an IC50 value of 0.02±0.00 µg/mL. Additionally, the total flavonoid and phenolic content were measured at 33,769±3,626 µg QE/mL and 638,924±6,683 µg GAE/mL, respectively. Notably, P.canescens exhibited significant potential in mitigating DNA damage. In conclusion, the P. canescens leaves hydroethanolic extracts demonstrate promising attributes as a herbal medicine, highlighting notable antioxidant and antimutagenic effects.

Ailanthus altissima Seed Oil-A Valuable Source of Lipid-Soluble Components with DNA Protective and Antiproliferative Activities.

The present study is focused on the chemical and lipid composition of seed oil of the European ornamental and invasive wood plant Ailanthus altissima (Simaroubaceae). Total lipids, proteins, carbohydrates, ash, and moisture in the seeds were determined. A high yield of glyceride oil (30.7%) was found, as well as a high content of fibers (29.6%) and proteins (18.7%). Physicochemical properties of the oil define it as semi-dry (129.4 g I2/100 g Iodine value) with oxidative stability, refractive index, saponification value, and relative density similar to widely used oils with nutritional value and health benefits. The composition of the seed oil was determined chromatographically. Unsaturated fatty acids (95.3%) predominated in the seed oil, of which linoleic acid (48.6%) and oleic acid (44.8%) were the major ones. The main lipid-soluble bioactive components were β-sitosterol (72.6%), γ-tocopherol (74.6%), phosphatidylinositol (29.5%), and phosphatidic acids (25.7%). The proven in vitro DNA-protective ability of seed oil is reported for the first time. The seed oil exhibited a weak antiproliferative effect on HT-29 and PC3 tumor cell lines and showed no cytotoxicity on the BALB/c 3T3 cell line. In brief, the present study reveals that A. altissima seed oil can be used as a healthy food.

Investigation of phenolic contents and in vitro biological activities of Inula helenium subsp. pseudohelenium extracts

AbstractThe purpose of the present study was to investigate the phenolic profile, antioxidant capacity, and biological activity of Inula helenium subsp. pseudohelenium extracts, for the first time. Phenolic substances in leaf ethanol (L-EtOH), leaf pure water (L-PW), root ethanol (R-EtOH), and root pure water (R-PW) extracts of I. helenium subsp. pseudohelenium plant were investigated by HPLC. Also, the antimicrobial (hollow agar), antioxidant, antiproliferative, and DNA protective activities of the samples were examined in vitro. Gallic acid was not detected in the extracts, the presence of curcumin was detected only in EtOH extracts. L-EtOH exhibited the best antimicrobial activity. According to the antioxidant results, the L-EtOH extract had an activity profile close to the standard antioxidants in general. It was also found that the L-EtOH extract stabilised the DNA by disrupting the scavenging effect of H2O2+DMSO. According to the antiproliferative activity results, EtOH extracts exhibited the strongest effect, especially against MCF7 cancer cell lines. When evaluated in general terms, it was found that L-EtOH extract showed better activity than other extracts. It is important to conduct more in vivo and in vitro studies after isolating the active components of extracts e.g. L-EtOH, which have good effects in terms of biological activity.

In vitro bioactivities and in silico enzyme interactions of abietatrien-3β-ol by bio-guided isolation from Nepeta italica subsp. italica

Abietatrien-3β-ol (ATO) was isolated from the aerial part of the Nepeta italica subsp. italica methanol-chloroform extract and studied antioxidant, enzyme inhibition, and DNA protection activities. The plant extract was fractionated by silica gel column chromatography using four different solvents. After the active chloroform fraction was divided into six subfractions under the guidance of bioactivity, ATO was isolated from the fourth active subfraction. The molecular structure of ATO was determined by the NMR techniques and confirmed with literature data. In the antioxidant test, ATO showed excellent DPPH˙ (IC50-1.18 ± 0.11 µg/mL), ABTS˙+ (IC50-1.82 ± 0.00 µg/mL), metal chelating (IC50-2.90 ± 0.05 µg/mL), superoxide anion scavenging (IC50-11.59 ± 0.27 µg/mL), reducing power (A0.5-21.09 ± 1.42 µg/mL), H2O2 (A0.5-57.81 ± 4.54 µg/mL), and phosphomolybdenum reducing (A0.5-124.23 ± 0.69 µg/mL) activities when compared to standards. The DNA protection potential was also found to be strong in Form I (47.89%) and Form II (4.56%) formations. ATO had high inhibitions in AChE (IC50-1.25 ± 0.04 µg/mL), BChE (IC50-1.26 ± 0.03 µg/mL), lipase (IC50-7.58 ± 0.27 µg/mL), and tyrosinase (IC50-9.60 ± 0.03 µg/mL). In molecular docking studies, ATO had a high binding affinity with α-amylase (−8.80 kcal/mol), tyrosinase (−8.10 kcal/mol), and urease (−8.10 kcal/mol) enzymes. In addition, by detailing the interaction of ATO with key enzymes that give the best interactions through molecular docking studies, with molecular dynamics studies, and by performing ADMET and DFT calculations, it was tried to explain that it could be a suitable drug candidate. In light of these studies, ATO is thought to be an effective enzyme inhibitor and a protective molecule against oxidation with its active antioxidant properties. Communicated by Ramaswamy H. Sarma

Isolation, characterization and evaluation of oxypeucedanin and osthol from local endemic Prangos aricakensis Behçet and Yapar root as antioxidant, enzyme inhibitory, antibacterial and DNA protection: molecular docking and DFT approaches

Prangos species were previously used against many disorders due to their chemical component. Prangos aricakensis Behçet & Yapar is a newly discovered local endemic species in Turkey’s eastern region, and there is no research on P. aricakensis in the literature. In this work, oxypeucedanin and osthol molecules have been isolated from the root part of P. aricakensis for the first time. Oxypeucedanin and osthol structures were elucidated by 1D and 2D NMR analysis. For the bioactivities determination, antioxidant (DPPH· and ABTS·+ scavenging), enzyme inhibition (AChE, BChE, tyrosinase, and urease), antibacterial and DNA protection activity studies were applied for both molecules and compared with standard drug molecules, after applying enzyme kinetic assays and in silico approaches to clarify the mechanism of action for both molecules with enzymes, using molecular docking and density functional theory (DFT). Oxypeucedanin (2.19 ± 0.38 µg/mL) and osthol (4.57 ± 1.28 µg/mL) exhibited better activity than standards in DPPH∙ scavenging activity. Osthol (11.76 ± 0.59 µg/mL) showed a better tyrosinase inhibition effect than kojic acid (12.82 ± 0.91 µg/mL), and oxypeucedanin (3.03 ± 0.01 µg/mL) showed better urease inhibition effect than thiourea (5.37 ± 1.86 µg/mL). Our results showed that the osthol molecule was an excellent skin protective agent while the oxypeucedanin molecule could be a remarkable antiulcer agent. Therefore, although this study is the first in its field, it remained in the in vitro and in silico stages and is thought to pave the way for in vivo studies in the future. Communicated by Ramaswamy H. Sarma

Thespesia lampas mediated green synthesis of silver and gold nanoparticles for enhanced biological applications

The present study investigated the synthesis and biological applications of green, economical, and multifunctional silver and gold nanoparticles (TSAgNPs and TSAuNPs) using the ethnomedical important medicinal plant Thespesia lampas for biological activities. Relatively higher levels of antioxidant components were measured in T. lampas compared to the well-known Adhatoda vasica, and Diplocyclos palmatus suggested the potential of T. lampas for the study. Synthesized TSAgNPs and TSAuNPs were characterized through UV-Vis, XRD, SEM-EDS, HR-TEM, SAED, and FTIR techniques. SEM revealed that TSAgNPs and TSAuNPs were predominantly spherical in shape with 19 ± 7.3 and 43 ± 6.3 nm crystal sizes. The sizes of TSAgNPs and TSAuNPs were found to be12 ± 4.8 and 45 ± 2.9 nm, respectively, according to TEM measurements. The FTIR and phytochemical analyses revealed that the polyphenols and proteins present in T. lampas may act as bio-reducing and stabilizing agents for the synthesis. Synthesized NPs exhibited enhanced scavenging properties for ABTS and DPPH radicals. TSAgNPs and TSAuNPs were able to protect DNA nicking up to 13.48% and 15.38%, respectively, from oxidative stress. TSAgNPs possessed efficient antibacterial activities in a concentration-dependent manner against human pathogenic bacteria, such as E. coli, B. subtilis, P. vulgaris, and S. typhi. Furthermore, TSAgNPs and TSAuNPs showed significant cytotoxicity against FaDu HNSCC grown in 2D at 50 and 100 μg mL-1. Tumor inhibitory effects on FaDu-derived spheroid were significant for TSAgNPs > TSAuNPs at 100 μg mL-1 in 3D conditions. Dead cells were highest largely for TSAgNPs (76.65% ± 1.76%), while TSAuNPs were non-significant, and Saq was ineffectively compared with the control. However, the diameter of the spheroid drastically reduced for TSAgNPs (3.94 folds) followed by TSAuNPs (2.58 folds), Saq (1.94 folds), and cisplatin (1.83 folds) at 100 μg mL-1. The findings of the study suggested the bio-competence of TSAgNPs and TSAuNPs as multi-responsive agents for antioxidants, DNA protection, antibacterial, and anti-tumor activities to provide a better comprehension of the role of phytogenic nanoparticles in healthcare systems.

Chemical Composition, Antimicrobial, and DNA Protection Activity of Essential Oils from Citrus Species of Northeast India

Chemical Composition, Antimicrobial, and DNA Protection Activity of Essential Oils from Citrus Species of Northeast India

Bioactive Component Analysis of Dices of Pomegranate Fruits in Different Phenotype

Pomegranate fruit is a type of fruit belonging to the family of Lythraceae, consisting of shell, kernel, grains and dice. In this study, pomegranates of 3 different genotypes (local name: deve dişi, hicaz and nuz ekşisi) harvested (October-December), which are widely cultivated in the province of Gaziantep, Oğuzeli, were collected, and after identification, the dice sections were removed and dried in the shade. Total antioxidant and total oxidant levels, animicrobial activities, DNA protective activity and total flavanoid and total phenolic content were determined in 18 extracts in 3 different solvents (methanol, ethanol and DMSO) with solid-liquid extraction. Kirby-Bauer disc diffusion method was used to determine antimicrobial properties. According to the results obtained, 100% of Escherichia coli, Stenotrophomonas maltophilia, Staphylococcus aureus strains were resistant to all membrane extracts. While antioxidant levels of all membrane extracts were found highly and oxidant levels were found to be low. It was determined that the extracts have the potential to protect DNA against oxidative damage caused by UV and H2O2. Total phenolic determination by Folin-Ciocalteu method; Total flavonoid amount was measured by AlCl3 using colorimetric method. Compared to the solvent and extraction methods used, high results were obtained in both phenolic and flavonoid determinations in all extracts, although they differed slightly among themselves. While the pomegranate fruit is consumed as food, the dice and shell parts are discarded. According to our study results, it is thought that alternative new products that can be used in complementary medicine can be obtained from pomegranate membranes that have a rich bioactive composition.

DNA protection, molecular docking, enzyme inhibition and enzyme kinetic studies of 1,5,9-epideoxyloganic acid isolated from Nepeta aristata with bio-guided fractionation

1,5,9-epideoxyloganic acid (ELA) was isolated from the aerial parts of endemic Nepeta aristata Boiss Et Kotschy Ex Boiss crude extract (methanol:chloroform) using silica gel (hexane, chloroform, ethyl acetate, and methanol) and sephadex LH-20 (65% methanol-35% chloroform) columns. Activity-guided isolation was performed on methanol sub-fractions with DNA protection and enzyme inhibitory activities, and then the ELA was purified by prep-HPLC. The ELA structure, bio-guided isolate, was determined via 1H NMR, 13C NMR, and MS spectrometry. ELA's enzyme inhibition and DNA protection activities were investigated and compared with standard drugs. The inhibition capacity of ELA against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), urease, carbonic anhydrase (CA), α-glucosidase, α-amylase, lipase, and tyrosinase enzymes was evaluated by kinetic and molecular docking results. The ELA displayed the best inhibitory activity on AChE, BChE, α-glucosidase, urease, α-amylase, and tyrosinase with IC50 values of 2.53 ± 0.27, 3.75 ± 0.11, 3.98 ± 0.07, 4.40 ± 0.01, 6.43 ± 0.54 and 7.39 ± 0.00 µg/mL, respectively. ELA acted as a competitive inhibitor against BChE and α-glucosidase and a non-competitive inhibitor against AChE. The ELA’s binding affinity values on AChE, BChE, and α-glucosidase were −7.70, −8.50, and −8.30 kcal/mol, respectively. DNA protection activity of the ELA molecule was determined as 57.53% for form I and 53.57% for form II. In conclusion, the inhibitory activity of ELA demonstrated its effectiveness in terms of its suitability in the pharmaceutical industry. Communicated by Ramaswamy H. Sarma