ABSTRACT
This study examines the potential of herniarin from tarragon, as an agent with multifaceted effects on bladder cancer cells and investigates herniarin's impact on cell viability, migration, cell cycle regulation, apoptosis induction, and Erk signaling pathways in bladder cancer cell lines, including RT-112 (gradeâ 1, non-invasive), HTB9 (gradeâ 2, invasive), and HT1376 (gradeâ 3, invasive), through comprehensive inâ vitro experiments. The compound causes cell cycle arrest at distinct phases in different cell lines: G1/S arrest in RT112 cells, G2/M arrest in HTB9 cells, and S phase arrest in HT1376 cells. Furthermore, herniarin induces caspase-mediated apoptosis in various cell lines and simultaneously modulates protein levels of apoptotic and anti-apoptotic proteins, indicating its potential as a therapeutic agent. Herniarin's influence also extends to Erk signaling, a crucial pathway that regulates cell growth and differentiation. In conclusion, this study reveals herniarin's potential as a versatile agent in the treatment of bladder cancer.
Subject(s)
Apoptosis , Umbelliferones , Urinary Bladder Neoplasms , Humans , Cell Survival , Cell Line, Tumor , G2 Phase Cell Cycle Checkpoints , Cell Cycle , Urinary Bladder Neoplasms/drug therapy , Urinary Bladder Neoplasms/metabolism , Cell Proliferation , Cell Cycle CheckpointsABSTRACT
In this study, methanol, ethanol, methanol-dichloromethane (1 : 1, v/v), acetone, ethyl acetate, diethyl ether, and chloroform extracts of lavender (Lavandula stoechas L. subsp. stoechas) were prepared by maceration, and the ursolic acid contents in the extracts were determined quantitatively by HPLC analyses. The present results show that the methanol-dichloromethane (1 : 1, v/v) solvent system is the most efficient solvent system for the extraction of ursolic acid from the plant sample with the highest yield (2.22â g/100â g plant sample). In the present study, a new practical method for the isolation of ursolic acid from polar extracts was also demonstrated for the first time. The inhibition effects of the extracts and ursolic acid were also revealed on α-glycosidase, acetylcholinesterase, butyrylcholinesterase, and human carbonic anhydrase I and II enzymes by determining IC50 values for the first time. The extracts and ursolic acid acted as potent antidiabetic agents by strongly inhibiting the α-glycosidase activity, whereas they were found to be very weak neuroprotective agents. In view of the present results, L. stoechas and its major metabolite, ursolic acid, can be recommended as a herbal source to control postprandial blood sugar levels and prevent diabetes by delaying the digestion of starch in food.
Subject(s)
Lavandula , Oils, Volatile , Triterpenes , Humans , Oils, Volatile/pharmacology , Methanol , Acetylcholinesterase , Butyrylcholinesterase , Methylene Chloride , Triterpenes/pharmacology , Plant Extracts/pharmacology , Solvents , Glycoside Hydrolases , Ursolic AcidABSTRACT
In the study, water, ethanol, methanol, dichloromethane, and acetone extracts of Asparagus officinalis L. were obtained by maceration. DPPHâ , ABTSâ + , FRAP, and CUPRAC methods determined the antioxidant capacities of all extracts. Moreover, the inâ vitro effects of extracts on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase (CA)-I, CA-II and α-Glycosidase were investigated. At a 10â µg/ml concentration, the extract with the highest Fe3+ reduction capacity was ethanol (AE), and the extract with the highest Cu2+ reduction capacity was acetone (AA). AE for AChE (IC50 =21.19â µg/ml) and α-Glycosidase (IC50 : 70.00â µg/ml), methanol (AM) for BChE (IC50 =17.33â µg/ml), CA-I and II (IC50 =79.65 and 36.09â µg/ml, respectively) showed the most potent inhibition effect. The content analysis of acetone extract was performed with LC/MS-MS, the first three phytochemicals found most were p-Coumaric acid, rutin, and 4-hydroxybenzoic acid (284.29±3.97, 135.39±8.19, and 102.06±5.51â µg analyte/g extract, respectively).
Subject(s)
Antioxidants , Asparagus Plant , Antioxidants/chemistry , Butyrylcholinesterase , Acetylcholinesterase , Plant Extracts/pharmacology , Plant Extracts/chemistry , Tandem Mass Spectrometry , Methanol , Acetone , Phytochemicals/pharmacology , Phytochemicals/chemistry , Ethanol , Glycoside HydrolasesABSTRACT
INTRODUCTION: Tomentosin, the characteristic component of Inula viscosa (L.) is an important sesquiterpene lactone with anticarcinogenic effects. Methods of obtaining pure tomentosin are not sufficient for anticancer drug research. OBJECTIVES: This study aims to develop a specific method to isolate tomentosin from I. viscosa with high yield. It also aims to investigate the inhibitory effects of tomentosin on human carbonic anhydrase I (hCAI), human carbonic anhydrase II (hCAII), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glucosidase, and α-amylase enzymes. MATERIAL AND METHODS: Tomentosin was purified by a specific column chromatography method. The content of tomentosin in dichloromethane, dichloromethane by Soxhlet method, ethanol and ethanol by Soxhlet method extracts of I. viscosa was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Half maximal inhibitory concentration (IC50 ) and inhibition constant (Ki ) values were calculated to determine in vitro enzyme inhibition effects. RESULTS: Tomentosin was isolated in high yield (0.64%). The IC50 and Ki values for tomentosin were calculated as 5.00 ± 0.19 (r = 0.9688) and 4.62 ± 0.10 µM for hCAI, 5.40 ± 0.26 (r = 0.9677) and 5.22 ± 0.31 µM for hCAII, 6.75 ± 0.208 (r = 0.9891) and 3.75 ± 0.27 µM for AChE, 6.67 ± 0.307 (r = 0.9820) and 0.51 ± 0.11 µM for BChE, 26.61 ± 0.236 (r = 0.9815) and 2.61 ± 0.71 µM for α-glucosidase and 26.89 ± 1.54 µM (r = 0.9670) for α-amylase, respectively. CONCLUSION: Tomentosin was isolated in high yield from the paste-like extract of I. viscosa compared to the positive controls, it was determined that tomentosin was weakly effective against hCAI, hCAII, AChE and BChE, but thoroughly effective against α-glucosidase and α-amylase. These results suggested that tomentosin has α-glucosidase and α-amylase inhibitor potential.
Subject(s)
Inula , Sesquiterpenes , Acetylcholinesterase , Butyrylcholinesterase , Carbonic Anhydrase II , Chromatography, Liquid , Ethanol , Inula/chemistry , Lactones/pharmacology , Methylene Chloride , Plant Extracts/pharmacology , Sesquiterpenes/pharmacology , Tandem Mass Spectrometry , alpha-Amylases , alpha-GlucosidasesABSTRACT
This study was designed to investigate the effects of emulsion formulations of oleuropein isolated from ethanol extract of olive leaf in streptozotocin-diabetic rats. The rats were treated with the administration of the emulsion containing oleuropein at a low (150 mg/kg b.wt.) and high (225 mg/kg b.wt.) dose for 30 days. At the end of the study, blood samples were drawn from the heart of the rats to determine blood glucose, alanine transaminase, and aspartate transaminase levels. In addition, their liver tissues were dissected to determine the levels of glutathione and thiobarbituric acid-reactive substances, and superoxide dismutase activity. According to the results for both dose treatments, a statistically significant increase in superoxide dismutase activities and glutathione levels of the treated diabetic rats was observed when compared with those of the diabetic control rats. On the other hand, a statistically significant decrease in the levels of thiobarbituric acid-reactive substances, aspartate transaminase and alanine transaminase of the treated diabetic rats was determined. It should be highlighted that the administrations at the high dose were more effective compared to that of the low dose. Furthermore, a substantial decrease in the blood glucose levels of the diabetic rats exposed to the high dose was observed.
Subject(s)
Diabetes Mellitus, Experimental , Iridoids , Olea , Plant Extracts , Animals , Antioxidants , Blood Glucose , Catalase , Ethanol , Iridoid Glucosides , Iridoids/pharmacology , Liver , Plant Extracts/pharmacology , Plant Leaves , Rats , Rats, Wistar , Superoxide DismutaseABSTRACT
In this study, we investigated whether jervine (J) could prevent gastrointestinal (GI) side effects of abdominopelvic radiotherapy (RT) in Wistar-Albino female rats. Rats were divided into five groups: control (C), J only (J), J administered at 5 mg/kg/days for 7 days, RT only (RT), J before RT (J + RT), J administered for seven days before RT, J both before and after RT (J + RT + J), and J administered for 7 days before RT and after RT for 3 days. The weights of rats were measured on the 1st, 7th, and 10th days of the study. Rats were sacrificed to obtain tissues from the liver and intestine, which was followed by taking blood samples intracardially. In addition, the tissues were stained with pyruvate dehydrogenase (PDH) immunohistochemically. In our study, J supplementation markedly reduced weight loss, and histopathological, immunohistochemical, biochemical results suggest that J had a protective effect on GI toxicity following RT.
Subject(s)
Gastrointestinal Agents/therapeutic use , Radiation Injuries/pathology , Radiation Injuries/prevention & control , Veratrum Alkaloids/therapeutic use , Animals , Gastrointestinal Agents/chemistry , Gastrointestinal Agents/pharmacology , Rats , Rats, Wistar , Veratrum Alkaloids/chemistry , Veratrum Alkaloids/pharmacologyABSTRACT
Curcumin, a bioactive and pharmacologically efficient component isolated from Curcuma longa has attracted considerable attention because of its ability to modulate diverse cellular and physiological pathways. WNT, TGF/SMAD, NOTCH, and SHH are fundamentally different signaling cascades, but their choreographed activation is strongly associated with cancer development and progression. In this review we have attempted to set spotlight on regulation of different cell signaling pathways by curcumin in different cancers. We partition this multi-component review into in-depth biological understanding of various signal transduction cascades and how curcumin targets intracellular signal transducers of deregulated pathways to inhibit cancer development and progression. Rapidly broadening landscape of both established and candidate oncogenic driver mutations identified in different cancers is a major stumbling block in the standardization of drugs having significant clinical outcome. Intra and inter-tumor heterogeneity had leveraged the complexity of therapeutic challenges to another level. Multi-pronged approach and molecularly guided treatments will be helpful in improving the clinical outcome.
Subject(s)
Antineoplastic Agents, Phytogenic/therapeutic use , Curcumin/therapeutic use , Mutation , Neoplasm Proteins , Neoplasms , Signal Transduction , Translational Research, Biomedical/methods , Animals , Humans , Neoplasm Proteins/genetics , Neoplasm Proteins/metabolism , Neoplasms/drug therapy , Neoplasms/genetics , Neoplasms/metabolism , Neoplasms/pathology , Signal Transduction/drug effects , Signal Transduction/genetics , Translational Research, Biomedical/trendsABSTRACT
PURPOSE: To evaluate clinical periodontal findings and GCF levels of tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6) and interleukin 8 (IL-8) in patients with overhang amalgam restorations before and after overhang restoration removal. METHODS: 22 volunteer subjects (age range: 22-42 years old) with 22 overhang Class II amalgam restorations were selected. GCF samples were obtained from adjacent and contralateral teeth for IL-6, IL-8 and TNF-α measurements and analyzed using enzyme-linked immunosorbent assay (ELISA) kits. The amalgam overhangs were removed and the readings were repeated at the end of 1 week. Clinical periodontal assessments, including gingival index (GI) and plaque index (PI) were performed at baseline and after 1 week. Data were analyzed using the paired t-test and independent sample t-test at a significance level of 0.05. Correlations were investigated using Pearson correlation analysis. RESULTS: A significant reduction in GI and PI was observed after removal of the overhanging restoration on Day 7. (P< 0.05) However, there was no significant difference between IL-6 (P= 0.857), IL-8 (P= 0.579) and TNF-α (P= 0.958) levels before and after overhang restoration removal. There were no significant correlations between laboratory findings and clinical parameters. CLINICAL SIGNIFICANCE: Dental restorations may produce periodontal disease and may alter tooth form, surface integrity, relationship with the periodontium and adjacent teeth. The marginal edge located in the gingival sulcus is likely the cause of the inflammatory reaction. This study showed significant improvement in clinical periodontal parameters after removing the overhangs of restorations.
Subject(s)
Dental Amalgam/adverse effects , Dental Amalgam/chemistry , Dental Restoration, Permanent/adverse effects , Gingival Crevicular Fluid/metabolism , Interleukin-6/metabolism , Interleukin-8/metabolism , Tumor Necrosis Factor-alpha/metabolism , Adult , Dental Plaque Index , Enzyme-Linked Immunosorbent Assay , Female , Humans , Male , Periodontal IndexABSTRACT
The dried rhizomes of Veratrum album were individually extracted with CHCl3 , acetone, and NH4 OH/benzene to test the toxic effects against the Colorado potato beetle, Leptinotarsa decemlineata, which is an important agricultural pest. Fifteen compounds in various amounts were isolated from the extracts using column and thin-layer chromatography. The chemical structures of 14 compounds were characterized as octacosan-1-ol (1), ß-sitosterol (2), stearic acid (3), diosgenin (4), resveratrol (5), wittifuran X (6), oxyresveratrol (7), ß-sitosterol 3-O-ß-D-glucopyranoside (8), diosgenin 3-O-α-L-rhamnopyranosyl-(1 â 2)-ß-D-glucopyronoside (9), oxyresveratrol 3-O-ß-D-glucopyranoside (10), jervine (11), pseudojervine (13), 5,6-dihydro-1-hydroxyjervine (14), and saccharose (15) using UV, IR, MS, (1) H- and (13)C-NMR, and 2D-NMR spectroscopic methods. However, the chemical structure of 12, an oligosaccharide, has not fully been elucidated. Compounds 4, 6, 9, and 10 were isolated from V. album rhizomes for the first time in the current study. The toxic effects of three extracts (acetone, CHCl3 , and NH4 OH/benzene) and six metabolites, 2, 2+4, 5, 7, 8, and 11, were evaluated against the Colorado potato beetle. The assay revealed that all three extracts, and compounds 7, 8, and 11 exhibited potent toxic effects against this pest. This is the first report on the evaluation of the toxic effects of the extracts and secondary metabolites of V. album rhizomes against L. decemlineata. Based on these results, it can be concluded that the extracts can be used as natural insecticides.
Subject(s)
Coleoptera/drug effects , Insecticides/chemistry , Insecticides/pharmacology , Veratrum/chemistry , Animals , Chromatography, Thin Layer , Insecticides/isolation & purification , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/pharmacology , Rhizome/chemistry , Veratrum/metabolismABSTRACT
In this study, the pesticide (acetamiprid, deltamethrin, and pyridaben) removal and physicochemical quality improvement of vine (Vitis vinifera) leaf were examined using ultrasonic and traditional cleaning for 5, 10, and 15 min. After an ultrasonic cleaning procedure at 37 kHz for 10 min, acetamiprid, deltamethrin, and pyridaben in vine leaf were reduced by 54.76, 58.22, and 54.55 %, respectively. Furthermore, the total phenolic content (TPC) in vine leaf increased to 13.45 mg GAE/g DW compared to that in control samples using traditional cleaning (10.37 mg GAE/g DW), but there were no significant differences in DPPH radical scavenging activity. After 15 min of conventional cleaning, the total chlorophyll and total carotenoid content of leaves were found to be lowest among all samples, at 6.52 mg/kg and 0.48 mg/kg, respectively. In conclusion, when compared to conventional cleaning methods, ultrasonic cleaning with no chemicals or heat treatment has proven to be a successful and environmentally friendly application in reducing commonly used pesticides and improving the physicochemical qualities of leaves.
Subject(s)
Pesticides , Vitis , Vitis/chemistry , Pesticides/analysis , Phenols/analysis , Plant Leaves/chemistry , Plant Extracts/chemistry , Antioxidants/chemistryABSTRACT
Increased pro-inflammatory cytokines and oxidative stress contribute to the pathophysiology of ulcerative colitis (UC). Inula viscosa is a plant with antioxidant and anti-inflammatory properties. We investigated the effect of an ethanolic extract of I. viscosa on an experimental UC model created using acetic acid. Rats were divided into four groups of eight: group 1, control; group 2, 3% acetic acid group; group 3, 100 mg/kg sulfasalazine + 3% acetic acid group; group 4, 400 mg/kg I. viscosa + 3% acetic acid. I. viscosa and sulfasalazine were administered by oral gavage and 3% acetic acid was administered per rectum. We found that I. viscosa treatment decreased colon malondialdehyde, tumor necrosis factor-α, interleukin-1 beta and nuclear factor kappa B levels; it increased reduced glutathione, nuclear factor erythroid 2-related factor 2, heme oxygenase-1 and kelch-like ECH-associated protein 1 levels and glutathione peroxidase enzyme activity. Group 1 colon exhibited normal histological structure. Slight inflammatory cell infiltration and edema and insignificant slight erosion in crypts were detected in colon tissues of group 4. We found that I. viscosa reduced oxidative stress and inflammation, which was protective against UC by inducing the Nrf-2/Keap-1/HO-1 pathway in the colon.
Subject(s)
Colitis, Ulcerative , Inula , Rats , Animals , Colitis, Ulcerative/chemically induced , Colitis, Ulcerative/drug therapy , Colitis, Ulcerative/metabolism , Sulfasalazine/pharmacology , Inula/metabolism , Acetic Acid , Antioxidants/pharmacology , Antioxidants/metabolismABSTRACT
Impact of various ultrasound pretreatment and microwave drying parameters on the qualitative and antioxidant characteristics of Inula viscosa (L.) was investigated in this study. The leaves of Inula viscosa (L.) were sonicated for 10, 20, and 30 min in an ultrasonic bath (37 kHz, 150 Watts). Microwave drying was done at three distinct times (1, 3, and 5 min) and with three different microwave power levels (100, 180, and 300 Watts). Microwave dried samples were tested for color characteristics (L*, a*, b*), chlorophyll, carotenoid, total phenol, and antioxidant content. All dried samples were prepared by infusing them in hot water as tea, and the sensorial properties of teas including odor, color, aroma, and overall acceptability were evaluated by panelists. For 10, 20, and 30 min of ultrasound pretreatment, the L* values of leaves varied from 37.70 to 49.76, 34.97 to 46.25, and 27.88 to 43.34, respectively. The total carotenoid concentration ranged from 0.12 to 0.32 mg/g DW, while the total chlorophyll content was from 0.44 to 0.94 mg/g DW. The antioxidant activity of Inula viscosa (L.) leaves that were dried at 300 Watts for 5 min did not change significantly as a result of ultrasound pretreatment. There was a significant positive correlation between aroma and TPC, as well as between color and overall acceptability. The darkest-colored teas were deemed preferable by the panelists.
Subject(s)
Antioxidants , Inula , Microwaves , Ultrasonics , Carotenoids , Chlorophyll , ColorABSTRACT
The protective effects of the ethanol extract of Smilax excelsa L. (SE) leaves were investigated on testicular tissue of rats with a torsion model in this study. The chemical composition of the extract was detected by means of liquid chromatography with tandem mass spectrometry (LC-MS/MS). SE extract was given for 21 days before torsion was created in the treatment group. The sperm parameters of the torsion group were impaired, and there was an increase in MDA level as well as a decrease in GSH level and GPx activity compared to the control group. TNF-α and NF-κB levels in the torsion group increased as compared to those in the control group. The expression levels of Nrf-2 and HO-1 were lower in the torsion group than those in the control group. The SE pretreatment group has improved sperm, oxidative stress, and inflammatory markers when compared to the torsion group, and the Nrf-2/HO-1 pathway was activated. PRACTICAL APPLICATIONS: Smilax excelsa L. is a plant with economic value used in traditional medicine in the treatment of stomachache, bloating, and breast cancer in Northwest Anatolia. It has an antioxidant effect due to the flavonoids and anthocyanins it contains. The protective effect against ischemia-reperfusion-induced tissue and reproductive damage in testicular tissue were demonstrated with the study. When the histological examinations of the tissues were evaluated, it was found that morphological structure of the tissues was retained in the treatment group. The findings indicate that SE prevents tissue damage in the torsion model by antioxidant and anti-inflammatory effects and activating Nrf-2/HO-1 pathway.
Subject(s)
Reperfusion Injury , Smilax , Spermatic Cord Torsion , Animals , Anthocyanins/metabolism , Anti-Inflammatory Agents/metabolism , Anti-Inflammatory Agents/pharmacology , Antioxidants/metabolism , Chromatography, Liquid , Humans , Male , Plant Extracts/metabolism , Plant Extracts/pharmacology , Rats , Reperfusion Injury/drug therapy , Reperfusion Injury/metabolism , Reperfusion Injury/prevention & control , Seeds/metabolism , Spermatic Cord Torsion/drug therapy , Spermatic Cord Torsion/metabolism , Spermatic Cord Torsion/pathology , Tandem Mass Spectrometry , TestisABSTRACT
Acute lung injury (ALI) is one of the most common causes of death in diseases with septic shock. Oleuropein, one of the important components of olive leaf, has antioxidant and anti-inflammatory effects. The objective of this study was to investigate the effects of oleuropein on lipopolysaccharide (LPS)-induced ALI in rats. Oleuropein was administered to rats at a dose of 200 mg/kg for 20 days and LPS was given through intratracheal administration to induce ALI. The study was terminated after 12 h. The results showed that in the group treated with oleuropein, inflammatory cytokines and oxidative stress decreased in serum, bronchoalveolar lavage fluid (BALF), and lung tissue, and there were significant improvements in the picture of acute interstitial pneumonia (AIP) caused by LPS in histopathological examination. Based on the findings of the present study, oleuropein showed protective effects against LPS-induced ALI.
Subject(s)
Acute Lung Injury/prevention & control , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Iridoid Glucosides/pharmacology , Lung/drug effects , Acute Lung Injury/chemically induced , Acute Lung Injury/metabolism , Acute Lung Injury/pathology , Animals , Cytokines/metabolism , Disease Models, Animal , Inflammation Mediators/metabolism , Lipopolysaccharides , Lung/metabolism , Lung/pathology , Male , Neutrophil Infiltration/drug effects , Oxidative Stress/drug effects , Rats, WistarABSTRACT
BACKGROUND: The aims of this study were to examine the chemical composition of the essential oils and hexane extracts of the aerial parts of Satureja spicigera (C. Koch) Boiss., Thymus fallax Fisch. & CA Mey, Achillea biebersteinii Afan, and Achillea millefolium L. by GC and GC-MS, and to test antibacterial efficacy of essential oils and n-hexane, chloroform, acetone and methanol extracts as an antibacterial and seed disinfectant against 25 agricultural plant pathogens. RESULTS: Thymol, carvacrol, p-cymene, thymol methyl ether and gamma-terpinene were the main constituents of S. spicigera and T. fallax oils and hexane extracts. The main components of the oil of Achillea millefolium were 1,8-cineole, delta-cadinol and caryophyllene oxide, whereas the hexane extract of this species contained mainly n-hexacosane, n-tricosane and n-heneicosane. The oils and hexane extracts of S. spicigera and T. fallax exhibited potent antibacterial activity over a broad spectrum against 25 phytopathogenic bacterial strains. Carvacrol and thymol, the major constituents of S. spicigera and T. fallax oils, also showed potent antibacterial effect against the bacteria tested. The oils of Achillea species showed weak antibacterial activity. Our results also revealed that the essential oil of S. spicigera, thymol and carvacrol could be used as potential disinfection agents against seed-borne bacteria. CONCLUSION: Our results demonstrate that S. spicigera, T. fallax oils, carvacrol and thymol could become potentials for controlling certain important agricultural plant pathogenic bacteria and seed disinfectant.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Disinfectants/pharmacology , Magnoliopsida/chemistry , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Achillea/chemistry , Anti-Bacterial Agents/isolation & purification , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plant Extracts/chemistry , Satureja/chemistry , Seeds/microbiology , Thymus Plant/chemistryABSTRACT
Helichrysum plicatum species are used in Turkish folk medicine as lithagogue, diuretic, and nephritic. Research on the methanol (MeOH) extract of flowers of H. plicatum DC. subsp. plicatum resulted in the isolation of eight known compounds (1-8). The chemical structures of the compounds were determined as ß-sitosterol (1), apigenin (2), nonacosanoic acid (3), astragalin (4), ß-sitosterol-3-O-ß-D-glucopyranoside (5), helichrysin A (6), helichrysin B (7), and isosalipurposide (8) by spectroscopic and chromatographic/spectrometric methods, including 1D and 2D nuclear magnetic resonance and liquid chromatography-tandem mass spectrometry. Nonacosanoic acid (3) was isolated for the first time from H. plicatum DC. subsp. plicatum. The MeOH extract and isolated compounds were evaluated for their in vitro human carbonic anhydrase I (hCAI) and II (hCAII), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase inhibitory activities. The IC50 values of H. plicatum DC. subsp. plicatum MeOH extract for hCAI, hCAII, AChE, BChE, and α-glycosidase were found to be 77.87, 52.90, 115.50, 117.46, and 81.53 mg/mL, respectively. The compounds showed IC50 values of 1.43-4.47, 1.40-4.32, 1.69-2.90, 1.09-3.89, and 1.61-3.80 µM against hCAI, hCAII, AChE, BChE, and α-glycosidase, respectively. In summary, H. plicatum DC. subsp. plicatum secondary metabolites demonstrated strong inhibitory effects especially against hCAI and hCAII, whereas the MeOH extract showed a weak inhibitory effect on all enzymes.
Subject(s)
Carbonic Anhydrase Inhibitors/pharmacology , Cholinesterase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/pharmacology , Helichrysum/chemistry , Phytochemicals/pharmacology , Acetylcholinesterase/metabolism , Butyrylcholinesterase/metabolism , Carbonic Anhydrase I/metabolism , Carbonic Anhydrase II/metabolism , Carbonic Anhydrase Inhibitors/chemistry , Cholinesterase Inhibitors/chemistry , Chromatography, Liquid , Flowers/chemistry , GPI-Linked Proteins/metabolism , Gene Expression Regulation, Enzymologic/drug effects , Glycoside Hydrolase Inhibitors/chemistry , Humans , Molecular Structure , Phytochemicals/chemistry , Secondary Metabolism , Tandem Mass SpectrometryABSTRACT
The aim of this study was to investigate the effects of extracts and pure Artemisia dracunculus L. (tarragon) metabolites on the antimonoamine oxidase and anticholinesterase activities. The compounds were characterized as stigmasterol (1), herniarin (2), (2E,4E)-1-(piperidin-1-yl)undeca-2,4-diene-8,10-diyn-1-one (3), (2E,4E)-N-isobutylundeca-2,4-dien-8,10-diynamide (4), 3,4-dehydroherniarin (5) and skimmin (6) by 1H-NMR, 13C-NMR, 1D and 2D NMR methods. The compounds 5 and 6 were isolated from tarragon for the first time. The extracts and pure compounds have inhibitory effects on the human monoamine oxidase (hMAO) A and B enzymes, whereas they did not exhibit any anticholinesterase activities. Among the tarragon compounds, only 2 and 6 compounds showed the inhibitory effects against hMAO A (IC50 = 51.76 and 73.47 µM, respectively) and hMAO B (IC50 = 0.84 and 1.63 mM, respectively). In the study, herniarin content in the extracts was also analysed by high-performance liquid chromatography and it was found that there was a relationship between the inhibition effects of the extracts and their herniarin content.
Subject(s)
Artemisia/chemistry , Coumarins/pharmacology , Monoamine Oxidase/drug effects , Umbelliferones/pharmacology , Enzyme Inhibitors/pharmacology , Humans , Monoamine Oxidase Inhibitors/pharmacologyABSTRACT
This study was aimed to investigate the antihemorrhoidal effects of ethanol (CBE) and water extracts (CBW) of Capsella bursa-pastoris, an edible plant and a precipitant (CBW-1) obtained from the CBW in croton oil (CO)-induced hemorrhoid model in rats. CBW-1 was contain three organic acids, citric acid (36.09%), malic acid (35.56%), and quinic acid (17.73%). Hemorrhoids were evaluated by histopathology of recto-anal tissues and biochemical parameters in plasma and recto-anal tissues of rats. CBW, CBE, and CBW-1 significantly reduced hemorrhagic necrotic enteritis induced by CO. CO also increased the cytokines and lipid peroxidation (LPO) in serum, and myeloperoxidase (MPO) activity and LPO in recto-anal tissues, and reduced the GSH, CAT, GPx, and SOD levels in serum and recto-anal tissues. However, CBE, CBW, and CBW-1 ameliorated the levels of the cytokines, LPO, MPO, and the antioxidants. Our results conclude that the curative effect of Capsella bursa-pastoris is closely related with its organic acids constituents, citric, malic, and quinic acids. PRACTICAL APPLICATIONS: The fresh leaves of Capsella bursa-pastoris are edible, eaten raw or cooked, and also used in salad. It has a widespread traditional usage in the treatment of the hemorrhoids in the Anatolia and in the Middle East Countries. According to our literature survey, any scientific evidence has not been found in the literature that C. bursa-pastoris could be used in the treatment of hemorrhoids. Therefore, in the current study, we aimed to investigate the antihemorrhoidal and antioxidant effects of ethanol and water extracts, and a precipitant (CBW-1) obtained from the CBW of C. bursa-pastoris in croton oil (CO)-induced hemorrhoid model in rats. The current results showed that its water extract and CBW-1 containing three organic acids, citric acid (36.09%), malic acid (35.56%), and quinic acid (17.73%) significantly reduced the hemorrhagic necrotic enteritis induced by CO ameliorating the levels of the cytokines, LPO, MPO, and the antioxidants. Our results conclude that the curative effect of C. bursa-pastoris is closely related with its organic acids constituents, citric, malic, and quinic acids.
Subject(s)
Capsella , Hemorrhoids , Animals , Croton Oil , Lipid Peroxidation , Plant Leaves , RatsABSTRACT
The antioxidant and cardioprotective effects of oleuropein have been reported in several studies; however, its effect on ketamine cardiotoxicity has not been known yet. The aim of this study was to investigate the effects of oleuropein in ketamine-induced cardiotoxicity model in rats. A total of 28 male Wistar Albino rats were included in the study and they were randomly divided into four groups, each having seven rats. Group 1 (control): rats were given 1 mL of DMSO by oral gavage method for 7 days. Group 2 (ketamine): on the seventh day of the study, 60 mg/kg ketamine was administered intraperitoneally. Then, 60 mg/kg ketamine was administered intraperitoneally every 10 min for 3 h. Group 3 (oleuropein): rats were given 200 mg/kg/day oleuropein by oral gavage method for 7 days. Group 4 (oleuropein + ketamine): rats were given 1 × 200 mg/kg oleuropein by oral gavage method for 7 days. Furthermore, 60 mg/kg ketamine was administered intraperitoneally on the seventh day of the experiment. Then, 60 mg/kg ketamine was administered intraperitoneally every 10 min for 3 h. Serum cardiac marker (TnI, CK-MB and CK) levels were measured. Histopathological analysis was performed on a portion of the cardiac tissue. Cardiac tissue oxidative stress and antioxidant markers (MDA, GSH, GSH.Px and CAT), TNF-α, IL-6, NF-κB, COX-2 and Nrf-2 gene expressions, and protein conversion levels of related genes were determined. Data obtained showed that ketamine administration increased MDA (p < 0.001), TNF-α (p < 0.01), IL-6 (p < 0.01), COX-2 (p < 0.001) and NF-κB (p < 0.001) levels, as well as serum TnI (p < 0.001), CK-MB (p < 0.001) and CK (p < 0.01) levels whereas decreased GSH (p < 0.05) and Nrf-2 (p < 0.05) levels, as well as GSH-Px (p < 0.001) and CAT (p < 0.05) enzyme activities. Oleuropein administration was observed to decrease MDA, TNF-α, IL-6, COX-2, NF-κB, TnI, CK-MB and CK levels close to the control group and to increase GSH levels and GSH-Px and CAT enzyme activities close to the control group. This study showed that oleuropein administration reversed the increased oxidative stress and inflammation as a result of the use of ketamine and had protective effects on the heart.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Heart Diseases/prevention & control , Inflammation Mediators/metabolism , Iridoid Glucosides/pharmacology , Myocytes, Cardiac/drug effects , Oxidative Stress/drug effects , Animals , Cardiotoxicity , Disease Models, Animal , Heart Diseases/chemically induced , Heart Diseases/metabolism , Heart Diseases/pathology , Ketamine , Male , Myocytes, Cardiac/metabolism , Myocytes, Cardiac/pathology , Rats, Wistar , Signal TransductionABSTRACT
BACKGROUND: Veratrum, hellebore is an important plant species of the Liliaceae family and jervine is the characteristic steroidal alkaloid constituent of Veratrum album. PURPOSE: In the current study, anti-inflammatory and antioxidant effects of jervine isolated from NH4OH-benzene extract of V. album rhizomes were investigated on CAR induced paw edema in rats. METHODS/STUDY DESIGN: In inflammatory study, 50, 100, 200 and 400⯠mg/kg doses of jervine, 25⯠mg/kg doses of DIC and IND were orally administered, and the volume of the foots were measured up to their knee arthrosis by plethismometer. After one hour of the oral administration of the all treatments, 0.1â¯ml of CAR solution (1%) was injected into the foot of the all rat groups and the volume of the foots were measured during 5 h after CAR injection. GPx, SOD, GR, MPO, CAT enzymes activities and GSH, LPO levels of the supernatants of paw homogenates and inflammation biomarkers such as TNF-α and IL-1ß in the rats serums were also estimated. RESULTS: According to the present results, jervine exerted 50.4-73.5% anti-inflammatory effects in carrageenan induced paw edema. Inflammation biomarkers such as TNF-α, IL-1ß and MPO that increased by CAR injection were suppressed by the administrations of all doses of jervine, IND and DIC. In all paw tissues, LPO levels as indicator of oxidative tissue damage were found to be high in CAR-treated group and it was found to be decreased in all doses of jervine. CONCLUSION: Jervine, DIC and IND reduced the negative effects of CAR due to increasing effects on the SOD, CAT, GSH, GPx and GR antioxidants.