ABSTRACT
Background: Research on the development of reliable diagnostic targets is being conducted to overcome the high prevalence and difficulty in managing periodontitis. However, despite the development of various periodontitis target markers, their practical application has been limited due to poor diagnostic accuracy. In this study, we present an improved periodontitis diagnostic target and explore its role in periodontitis. Methods: Gingival crevicular fluid (GCF) was collected from healthy individuals and periodontitis patients, and proteomic analysis was performed. The target marker levels for periodontitis were quantified in GCF samples by enzyme-linked immunosorbent assay (ELISA). Mouse bone marrow-derived macrophages (BMMs) were used for the osteoclast formation assay. Results: LC-MS/MS analysis of whole GCF showed that the level of alpha-defensin 1 (DEFA-1) was higher in periodontitis GCF than in healthy GCF. The comparison of periodontitis target proteins galactin-10, ODAM, and azurocidin proposed in other studies found that the difference in DEFA-1 levels was the largest between healthy and periodontitis GCF, and periodontitis was more effectively distinguished. The differentiation of RANKL-induced BMMs into osteoclasts was significantly reduced by recombinant DEFA-1 (rDEFA-1). Conclusions: These results suggest the regulatory role of DEFA-1 in the periodontitis process and the relevance of DEFA-1 as a diagnostic target for periodontitis.
ABSTRACT
BACKGROUND: Although vaccination of nursing students in clinical practice is important due to the possibility of COVID-19 infection and subsequent transmission to patients, some nursing students are hesitant to get vaccinated. Thus, it is necessary to identify the actual intentions and motivations of nursing students who have been vaccinated for COVID-19, even if their decisions were driven by clinical practice policy. The purpose of this study was to understand the nature of COVID-19 vaccine hesitancy among vaccinated nursing students in clinical practice and to examine their reasons for getting vaccinated despite such hesitancy. METHOD: A cross-sectional, descriptive study was conducted at two tertiary hospitals in South Korea from November 20, 2021, to December 17, 2021. The study recruited a convenience sample of 125 nursing students who were vaccinated for COVID-19. Data were analyzed using the chi-square test, Fisher's exact test, and independent t-test. RESULTS: Of the 125 nursing students, 51 (40.8%) reported vaccine hesitancy, among whom 88.2% reported that their hesitancy was due to the adverse effects and instability of the vaccine. It was also found that 70.6% of nursing students in the vaccine-hesitant group were eventually vaccinated due to clinical practice policy, whereas 67.6% of nursing students in the non-hesitant group were vaccinated to protect their health. CONCLUSIONS: COVID-19 vaccine hesitancy is prevalent among nursing students. Therefore, specific efforts should be made to provide education focusing on the safety, benefits, and efficacy of COVID-19 vaccines, implement mandatory vaccination policies for clinical practice, and give priority to vaccination opportunities to nursing students in order to reduce the hesitancy of nursing students to vaccines.
Subject(s)
COVID-19 , Students, Nursing , Humans , COVID-19 Vaccines , Cross-Sectional Studies , COVID-19/epidemiology , COVID-19/prevention & control , VaccinationABSTRACT
The COVID-19 pandemic has changed the fitness-related field. More people started working out at home, and the use of fitness mobile apps that can measure the amount of exercise through a scientific method has increased compared to before the COVID-19 pandemic. This phenomenon is likely to continue even after the COVID-19 pandemic, and therefore this study aimed to investigate the importance of and satisfaction with a fitness app's functions according to consumers while using the fitness mobile app. Through this study, we intended to provide data for creating an environment where users can use fitness mobile apps consistently. A total of 420 questionnaires were distributed through Google Survey for about 3 months, from 13 September to 20 November 2020, and a total of 399 complete questionnaires were analyzed in this study. Regarding the data processing methods, frequency analysis, exploratory factor analysis, reliability analysis, descriptive statistical analysis, and IPA were used. The results are as follows. First, the first quadrant of the IPA matrix indicated the high importance of and satisfaction with the fitness mobile app, and included five attributes: cost-effectiveness, easy-to-understand information, ease of use and application, privacy protection, and compatibility with other devices. Second, the second quadrant of the matrix indicated relatively low satisfaction in association to high importance and included five attributes: accurate exercise information provision, design efficiency, daily exercise amount setting, convenient icons and interface, and provision of images and videos in appropriate proportions. Third, the third quadrant of the matrix, indicating low importance and low satisfaction, included five attributes: not sharing personal information, overall design composition and color, customer service, reliable security level, and providing information on goal achievement after exercising. Fourth, in the quadrant of the matrix, indicating low importance and high satisfaction, five attributes were included: exercise notification function, continuous service provision, step count and heart rate information, individual exercise recommendation, and individual body type analysis information.
Subject(s)
COVID-19 , Mobile Applications , COVID-19/epidemiology , Exercise , Humans , Pandemics , Reproducibility of ResultsABSTRACT
BACKGROUND: To develop a warning system that can prevent or minimize laser exposure resulting in kidney and ureter damage during retrograde intrarenal surgery (RIRS) for urolithiasis. Our study builds on the hypothesis that shock waves of different degrees are delivered to the hand of the surgeon depending on whether the laser hits the stone or tissue. METHODS: A surgical environment was simulated for RIRS by filling the body of a raw whole chicken with water and stones from the human body. We developed an acceleration measurement system that recorded the power signal data for a number of hours, yielding distinguishable characteristics among three different states (idle state, stones, and tissue-laser interface) by conducting fast Fourier transform (FFT) analysis. A discrete wavelet transform (DWT) was used for feature extraction, and a random forest classification algorithm was applied to classify the current state of the laser-tissue interface. RESULTS: The result of the FFT showed that the magnitude spectrum is different within the frequency range of < 2500 Hz, indicating that the different states are distinguishable. Each recorded signal was cut in only 0.5-s increments and transformed using the DWT. The transformed data were entered into a random forest classifier to train the model. The test result was only measured with the dataset that was isolated from the training dataset. The maximum average test accuracy was > 95%. The procedure was repeated with random signal dummy data, resulting in an average accuracy of 33.33% and proving that the proposed method caused no bias. CONCLUSIONS: Our monitoring system receives the shockwave signals generated from the RIRS urolithiasis treatment procedure and generates the laser irradiance status by rapidly recognizing (in 0.5 s) the current laser exposure state with high accuracy (95%). We postulate that this can significantly minimize surgeon error during RIRS.
Subject(s)
Kidney Calculi , Ureter , Urolithiasis , Humans , Kidney Calculi/surgery , Machine Learning , Treatment Outcome , Urolithiasis/surgeryABSTRACT
AIM OF THE STUDY: The aim of this study was to test the anti-rheumatic effects of A. jaluense tubers in acute and chronic arthritis rats, and to assign its ingredients through UHPLC-TOF/MS. MATERIALS AND METHODS: Subcutaneous injection of carrageenan for acute arthritis and complete Freund's adjuvant (CFA) for chronic arthritis was carried out in the hind paw of SD rats. The paw volume was measured by a plethysmometer thermal hyperalgesia was tested using a thermal plantar tester, and mechanical hyperalgesia was evaluated by ankle flexion evoked vocalizations. The expression of c-Fos in the brain hippocampus was measured with the avidin-biotin-peroxidase technique. The ingredients were assigned by UHPLC-TOF/MS, chromatography was performed by UHPLC system with DAD detector and BEH C18 column, and spectroscopy was conducted by ESI-MS system. RESULTS AND DISCUSSION: The 80% ethanoic extract of A. jaluense tubers showed an acute anti-inflammatory effect by suppressing the edema volume in the hind paw of carrageenan-stimulated rats. In addition, A. jaluense tubers exerted an anti-rheumatic activity by reducing the secondary swelling volume from an immunological reaction in the left hind paw of CFA-induced chronic arthritis rats. Additionally, oral treatment with the 80% ethanoic extract -showed potent analgesic effects in the arthritis rats by recovering the paw withdrawal latency stimulated by the thermal hyperalgesia and by reducing the vocalization scores evoked by ankle flexion on both hind paws. Moreover, its treatment also indicated an anti-psychiatric effect by controlling the c-Fos protein expression of the brain hippocampus in CFA-stimulated arthritis rats. These results suggested that these therapeutic effects were exhibited by less toxic mono-esterified diterpenoid alkaloids (MDAs), and nontoxic non-esterified diterpenoid alkaloids (NDAs). CONCLUSION: A. jaluense tubers may act as viable therapeutic or preventive candidates for acute and chronic arthritis, particularly, for immune-inflammatory rheumatoid arthritis to suppress the pain and psychiatric condition.
Subject(s)
Aconitum/chemistry , Analgesics/pharmacology , Antirheumatic Agents/pharmacology , Plant Extracts/pharmacology , Analgesics/isolation & purification , Animals , Antirheumatic Agents/isolation & purification , Arthritis, Experimental/drug therapy , Disease Models, Animal , Freund's Adjuvant , Hyperalgesia/drug therapy , Male , Plant Roots , Rats , Rats, Sprague-DawleyABSTRACT
The aim of this study was to examine the most cost-effective strategy of screening and vaccinating measles- and varicella-susceptible health care workers (HCWs). A retrospective cost-effectiveness analysis was conducted at a tertiary hospital in Korea with 300 HCWs who were at high risk of infection. Self-reported histories of vaccinations, infectious diseases, and contact with such cases were collected. Serological tests for immunoglobulin G titers of measles and varicella were performed. Data were analyzed using analysis of variance, Kruskal-Wallis test, χ2 test, and Fisher exact test. Seropositivity rates were 96.3% for measles and 95.7% for varicella. Four different strategies (cases) for vaccination were investigated. Considering the progressive decline in antibody concentrations and the false-positive responses in self-reported histories, case 3, which involved administering 2-dose vaccinations to susceptible HCWs demonstrated by antibody screening tests for both measles and varicella, was the most cost-effective strategy. Health care facilities should establish mandatory immunization policies that reduce the risk of transmission of vaccine-preventable diseases.
Subject(s)
Chickenpox , Health Personnel , Mass Screening , Measles , Vaccination , Chickenpox/prevention & control , Cost-Benefit Analysis , Health Personnel/statistics & numerical data , Humans , Mass Screening/statistics & numerical data , Measles/prevention & control , Retrospective Studies , Vaccination/statistics & numerical dataABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: The young branches of C. cassia Blume (Cinnamomi Ramulus; Guizhi; ; C. cassia twigs) have long been used as an anti-pyretic, anti-rheumatic, anti-spasmodic and stomachic in traditional medicine. AIM OF THE STUDY: The aim of this study was to test the anti-inflammatory, anti-nociceptive, and anti-arthritic effects of Cinnamomum cassia twigs in acute and chronic arthritis rats. MATERIALS AND METHODS: Subcutaneous injection of carrageenan for acute inflammation and complete Freund's adjuvant (CFA) for chronic arthritis was carried out in the hind paw of SD rats. The paw volume was measured by a plethysmometer; thermal hyperalgesia was tested using a thermal plantar tester; hyperalgesia was evaluated by ankle flexion evoked vocalizations. The c-Fos expression in the lumbar spinal cord was measured with the avidin-biotin-peroxidase technique. The nitric oxide (NO) generation in lipopolysaccharide (LPS)-induced RAW 264.7 cells was tested by Griess assay. RESULTS AND DISCUSSION: An 80% ethanoic extract of the C. cassia twigs exhibited chronic anti-inflammatory and anti-arthritic activities by reducing the edema volume in the paws of CFA-induced chronic arthritis in rats. In addition, it showed analgesic effects through the recovery of the paw withdrawal latency stimulated by thermal hyperalgesia, and suppressing the vocalization scores evoked by ankle flexion in the hind paws of the arthritis rats. It also controlled c-Fos expression in the lumbar spinal cord of the arthritis rats. Moreover, the addition its 80%-ethanoic extract, specifically, its ethyl acetate fraction, powerfully suppressed the paw swelling in carrageenan-stimulated arthritis and the NO production in LPS-induced murine immune cells. CONCLUSION: C. cassia twigs may act as a viably sufficient therapeutic or preventive candidate for osteoarthritis and rheumatoid arthritis; additionally, it could prevent gastrointestinal damage with its gastric protection.
Subject(s)
Arthritis, Experimental/drug therapy , Cinnamomum aromaticum/chemistry , Inflammation/drug therapy , Plant Extracts/pharmacology , Analgesics/isolation & purification , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Antirheumatic Agents/isolation & purification , Antirheumatic Agents/pharmacology , Carrageenan , Freund's Adjuvant , Hyperalgesia/drug therapy , Male , Mice , RAW 264.7 Cells , Rats , Rats, Sprague-DawleyABSTRACT
BACKGROUND: Valid and reliable methods for measurement of lesion sizes during endoscopy have not been established. METHODS: We developed a novel software program (ENDOVER; Poinbionics, Seoul, Republic of Korea) to measure lesions sizes and assessed its validity and reliability. To validate the program, we measured standard coin sizes and estimated measurement errors. To assess program reliability, 32 pictures of endoscopically resected specimens were used to measure tissue sizes six times in a 24-h interval by two examiners. Intraclass correlation coefficients (ICCs) were used to assess intraobserver and interobserver agreements. Agreement between the program and pathological measurements was assessed by absolute differences. RESULTS: The nominal standard sizes of 10-won, 100-won, and 500-won coins were 18.0, 24.0, and 26.5 mm, and the calculated sizes were 18.09, 24.48, and 26.31 mm, respectively. ICCs of the long and short diameters were, respectively, 0.92 [95% confidence interval (CI) 0.87-0.95] and 0.93 (CI 0.89-0.96) for examiner 1 and 0.88 (CI 0.81-0.93) and 0.92 (CI 0.87-0.95) for examiner 2. Interobserver ICCs of the long and short diameters were 0.97 (CI 0.94-0.99) and 0.97 (CI 0.94-0.99), respectively. The mean absolute differences between the program and pathological measurements were 4.4 and 4.7 mm for the long and short diameters, respectively. CONCLUSIONS: Our findings indicate that the novel measurement program is a valid and reliable method for estimation of lesion sizes from endoscopic findings during and after examination.
Subject(s)
Endoscopy/standards , Gastrointestinal Neoplasms/diagnostic imaging , Gastrointestinal Neoplasms/pathology , Humans , Observer Variation , Reproducibility of Results , Severity of Illness Index , SoftwareABSTRACT
Performing diverse application tests on synthesized metal oxides is critical for identifying suitable application areas based on the material performances. In the present study, Ni-oxide@TiO2 core-shell materials were synthesized and applied to photocatalytic mixed dye (methyl orange + rhodamine + methylene blue) degradation under ultraviolet (UV) and visible lights, CO oxidation, and supercapacitors. Their physicochemical properties were examined by field-emission scanning electron microscopy, X-ray diffraction analysis, Fourier-transform infrared spectroscopy, and UV-visible absorption spectroscopy. It was shown that their performances were highly dependent on the morphology, thermal treatment procedure, and TiO2 overlayer coating.
ABSTRACT
Five lignans were isolated from the ethyl acetate extracts of Saururus chinensis rhizomes and evaluated for anti-HIV-1 activity. Their structures were elucidated as two dilignans, manassantin A (1), manassantin B (2), two sesquilignans, saucerneol B (3) and saucerneol C (4), and a new lignan, saururin B (5) by spectroscopic analysis. Of these components, manassantin A (1) and saururin B (5) showed dose-dependent inhibitory activities on HIV-1 protease with IC(50) values of 38.9 and 5.6 microM. In addition, manassantins A (1), B (2) and saucerneol B (3) inhibited HIV-1-induced cytopathic effects in a human T lymphoblastoid cell line with IC(100) values of 1.0, 1.0 and 0.2 microM, respectively. Of these active constituents, saucerneol B (3) showed the most potent and selective anti-HIV-1 activity (IC(100) of 0.2 microM, CC(0) of >125.0 microM, and SI of >520.8).
Subject(s)
HIV Protease Inhibitors/isolation & purification , HIV Protease Inhibitors/pharmacology , HIV-1/drug effects , Lignans/pharmacology , Rhizome/chemistry , Saururaceae/chemistry , Cell Line , Cytopathogenic Effect, Viral/drug effects , Dose-Response Relationship, Drug , HIV Protease Inhibitors/chemistry , Humans , Inhibitory Concentration 50 , Lignans/chemistry , Lignans/isolation & purification , Molecular Structure , Spectrum Analysis , T-Lymphocytes/virologyABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Alpinia officinarum Hance (Zingiberaceae) is an annual plant. Its rhizome has long been used as an anti-inflammatory, an analgesic, a stomachic and a carminative in traditional medicine. OBJECTIVE: The aim of this study was to test the anti-inflammatory effects of Alpinia officinarum rhizomes on acute and chronic arthritis in SD rats. METHODS: Alpinia officinarum rhizomes were extracted by refluxing using 80% ethanol. The fractions were prepared by the fractionation of ethyl acetate (EtOAc), n-butanol, and water. This extract was administrated to rats by peroral injection. Acute arthritis was induced by a subcutaneous injection of carrageenan into the hind paw of SD rats. Chronic arthritis was stimulated by a subcutaneous injection of complete Freund's adjuvant (CFA) into the hind paw of SD rats. The paw volume was measured using a plethysmometer, thermal hyperalgesia was tested using a thermal plantar tester, hyperalgesia was evaluated by ankle flexion evoked vocalizations, and the expression of c-Fos in the brain hippocampus was measured with the avidin-biotin-peroxidase technique. Nitric oxide (NO) production was evaluated on nitrite by a Griess assay in lipopolysaccharide (LPS)-induced murine macrophage RAW 264.7 cells. RESULTS: An 80% ethanolic extract showed acute anti-inflammatory activity that it reduced the edema volume in carrageenan-stimulated arthritis and inhibited NO generation in LPS-induced RAW 264.7 cells. In addition, this extract showed chronic anti-rheumatic and analgesic activities by suppressing the swelling volume, by recovering the paw withdrawal latency, and by inhibiting the flexion scores in CFA-induced arthritis. Particularly, this medicine had potent meaningful effects on the second signal of the left hind paw in the form of an immunological reaction compared to its effects on the first signal in the right hind paw after the CFA treatment. This also shows an anti-psychiatric effect through control of the expression of the c-Fos protein of the brain hippocampus in CFA-stimulated arthritis. On the other hand, each fraction showed acute anti-inflammatory effects; the action of the EtOAc fraction may have resulted from the suppression of NO production. CONCLUSIONS: Alpinia officinarum rhizomes may be viable therapeutic or preventive candidates for the treatment of acute and chronic arthritis.
Subject(s)
Alpinia , Analgesics/therapeutic use , Anti-Inflammatory Agents/therapeutic use , Arthritis/drug therapy , Hippocampus/drug effects , Plant Extracts/therapeutic use , Proto-Oncogene Proteins c-fos/metabolism , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Arthritis/chemically induced , Carrageenan , Edema/drug therapy , Freund's Adjuvant , Hippocampus/metabolism , Macrophages/drug effects , Models, Animal , Nitric Oxide/antagonists & inhibitors , Phytotherapy , Plant Extracts/pharmacology , Rats , Rats, Sprague-Dawley , RhizomeABSTRACT
Eight compounds were isolated from the CH (2)Cl (2) extracts of ERYTHRINA SENEGALENSIS to assess HIV-1 protease (PR) activity inhibition. The prenylated isoflavone structures, identified by spectroscopic analysis, were 8-prenylluteone ( 1), auriculatin ( 2), erysenegalensein O ( 3), erysenegalensein D ( 4), erysenegalensein N ( 5), derrone ( 6), alpinumisoflavone ( 7), and 6,8-diprenylgenistein ( 8). The constituents showed dose-dependent inhibitory activities on HIV-1 PR with IC (50) values from 0.5 to 30.0 muM. Compounds 1 - 5 possessing two hydroxy groups in the 2' and 4' positions of the B ring, potently inhibited HIV-1 PR activity. In addition, 6,8-diprenylgenistein ( 8) with two prenyl groups in the 6 and 8 positions of the A ring and one hydroxy group in the 4' position of B-ring was the most potent HIV-1 PR inhibitor.
Subject(s)
Erythrina/chemistry , HIV Protease Inhibitors/pharmacology , HIV-1/drug effects , Plant Extracts/pharmacology , Dose-Response Relationship, Drug , HIV Protease Inhibitors/chemistry , HIV Protease Inhibitors/isolation & purification , Isoflavones/chemistry , Isoflavones/isolation & purification , Isoflavones/pharmacology , Molecular Structure , Plant Bark , Plant Extracts/chemistry , Plant StemsABSTRACT
An herbal mixture prepared with Cinnamomi Ramulus, Anemarrhenae Rhizoma and Alpiniae Officinari Rhizoma (CAA) is used in oriental medicine for treating several ailments. The purpose of this study was to determine the mechanisms by which CAA elicits an antiinflammatory effect on nitric oxide (NO) production in the mouse macrophage cell line RAW 264.7 cells. The results indicated that lipopolysaccharide (LPS)-induced NO production was inhibited by CAA in a dose-dependent manner. Western blotting and RT-PCR analysis demonstrated that CAA decreased LPS-induced inducible nitric oxide synthase (iNOS) protein and gene expression in RAW 264.7 cells. Furthermore, CAA inhibited the LPS-induced DNA binding activity of nuclear factor-kappa B (NF-kappaB) and this effect was mediated through inhibiting the degradation of inhibitory factor-kappaBalpha (IkappaBalpha). Therefore, the results demonstrate that CAA inhibits LPS-induced production of NO and expression of iNOS by blocking NF-kappaB activation. CAA might be a potential therapeutic candidate for treating inflammatory diseases such as arthritis.
Subject(s)
Macrophages/drug effects , NF-kappa B/metabolism , Nitric Oxide/metabolism , Plant Extracts/pharmacology , Animals , Asparagaceae/chemistry , Blotting, Western , Cell Line , Cell Survival/drug effects , Dose-Response Relationship, Drug , Lauraceae/chemistry , Lipopolysaccharides/pharmacology , Macrophages/cytology , Macrophages/metabolism , Mice , Nitric Oxide Synthase Type II/genetics , Nitric Oxide Synthase Type II/metabolism , Plant Extracts/chemistry , Protein Binding/drug effects , Reverse Transcriptase Polymerase Chain Reaction , Zingiberaceae/chemistryABSTRACT
Oleanolic acid (OA) and ursolic acid (UA), triterpene acids having numerous pharmacological activities including anti-inflammatory, anti-cancer, and hepato-protective effects, were tested for their ability to modulate the activities of several cytochrome P450 (CYP) enzymes using human liver microsomes. OA competitively inhibited CYP1A2-catalyzed phenacetin O-deethylation and CYP3A4-catalyzed midazolam 1-hydroxylation, the major human drug metabolizing CYPs, with IC50 (Ki) values of 143.5 (74.2) microM and 78.9 (41.0) microM, respectively. UA competitively inhibited CYP2C19-catalyzed S-mephenytoin 4'-hydroxylation with an IC50 (Ki) value of 119.7 (80.3) microM. However, other CYPs tested showed no or weak inhibition by both OA and UA. The present study demonstrates that OA and UA have inhibitory effects on CYP isoforms using human liver microsomes. It is thus likely that consumption of herbal medicines containing OA or UA, or administration of OA or UA, can cause drug interactions in humans when used concomitantly with drugs that are metabolized primarily by CYP isoforms. In addition, it appears that the inhibitory effect of OA on CYP1A2 is, in part, related to its anti-inflammatory and anticancer activities.
Subject(s)
Cytochrome P-450 Enzyme Inhibitors , Enzyme Inhibitors/pharmacology , Microsomes, Liver/drug effects , Plant Preparations , Triterpenes/pharmacology , Chromatography, High Pressure Liquid , Cytochrome P-450 Enzyme System/metabolism , Dose-Response Relationship, Drug , Humans , Inhibitory Concentration 50 , Isoenzymes/antagonists & inhibitors , Isoenzymes/metabolism , Microsomes, Liver/enzymology , Plant Preparations/chemistry , Plant Preparations/metabolism , Triterpenes/analysis , Ursolic AcidABSTRACT
Harpagophytum procumbens (Pedaliaceae) has been used for the treatment of pain and arthritis. The effect of Harpagophytum procumbens against lipopolysaccharide-induced inflammation was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, reverse transcription-polymerase chain reaction, prostaglandin E(2) (PGE(2)) immunoassay, and nitric oxide detection on mouse fibroblast cell line L929. The aqueous extract of Harpagophytum procumbens was shown to suppress PGE(2) synthesis and nitric oxide production by inhibiting lipopolysaccharide-stimulated enhancement of the cyclooxygenase-2 and inducible nitric oxide synthase (iNOS) mRNAs expressions in L929 cells. These results suggest that Harpagophytum procumbens exerts anti-inflammatory and analgesic effects probably by suppressing cyclooxygenase-2 and iNOS expressions.
Subject(s)
Fibroblasts/drug effects , Harpagophytum , Isoenzymes/antagonists & inhibitors , Nitric Oxide Synthase/antagonists & inhibitors , Animals , Cell Line , Cyclooxygenase 2 , Dose-Response Relationship, Drug , Fibroblasts/enzymology , Gene Expression Regulation, Enzymologic/drug effects , Gene Expression Regulation, Enzymologic/physiology , Isoenzymes/biosynthesis , Lipopolysaccharides/pharmacology , Mice , Nitric Oxide Synthase/biosynthesis , Nitric Oxide Synthase Type II , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Prostaglandin-Endoperoxide Synthases/biosynthesisABSTRACT
BACKGROUND: Chelidonii herba is classified as Papaver somniferum L. Aqueous extract from C. herba is traditionally used for disorders with symptoms like pain, bloating, abdominal cramp after meals. METHODS: Modulation of C. herba on glycine-activated and glutamate-activated ion currents in the acutely dissociated periaqueductal gray (PAG) neurons was investigated by the nystatin-perforated patch-clamp technique. RESULTS: C. herba inhibited glycine-activated ion current and increased glutamate-activated ion current. C. herba-induced inhibition on glycine-activated ion current is implicated in opioid receptors and GTP-binding proteins (G-proteins). Increased glutamate-activated ion current induced by C. herba is linked neither by opioid receptors nor GTP-binding proteins. CONCLUSIONS: Suppressed glycine-induced response and elevated glutamate-induced response by C. herba may increase neuronal excitability in PAG, results in activation of descending pain control system, and this mechanism can be suggested as one of the analgesic actions of C. herba.
Subject(s)
Chelidonium/chemistry , Neurons/drug effects , Periaqueductal Gray/drug effects , Plant Extracts/pharmacology , Animals , Dose-Response Relationship, Drug , Ethylmaleimide/pharmacology , Female , Glutamic Acid/pharmacology , Glycine/pharmacology , Ion Channel Gating/physiology , Male , Membrane Potentials/drug effects , Naltrexone/pharmacology , Neurons/physiology , Nystatin/pharmacology , Patch-Clamp Techniques , Periaqueductal Gray/cytology , Periaqueductal Gray/physiology , Rats , Rats, Sprague-DawleyABSTRACT
Chloroquine has been used for many decades in the prophylaxis and treatment of malaria. It is metabolized in humans through the N-dealkylation pathway, to desethylchloroquine (DCQ) and bisdesethylchloroquine (BDCQ), by cytochrome P450 (CYP). However, until recently, no data are available on the metabolic pathway of chloroquine. Therefore, the metabolic pathway of chloroquine was evaluated using human liver microsomes and cDNA-expressed CYPs. Chloroquine is mainly metabolized to DCQ, and its Eadie-Hofstee plots were biphasic, indicating the involvement of multiple enzymes, with apparent Km and Vmax values of 0.21 mM and 1.02 nmol/min/mg protein 3.43 mM and 10.47 nmol/min/mg protein for high and low affinity components, respectively. Of the cDNA-expressing CYPs examined, CYP1A2, 2C8, 2C19, 2D6 and 3A4/5 exhibited significant DCQ formation. A study using chemical inhibitors showed only quercetin (a CYP2C8 inhibitor) and ketoconazole (a CYP3A4/5 inhibitor) inhibited the DCQ formation. In addition, the DCQ formation significantly correlated with the CYP3A4/5-catalyzed midazolam 1-hydroxylation (r = 0.868) and CYP2C8-catalyzed paclitaxel 6alpha-hydroxylation (r = 0.900). In conclusion, the results of the present study demonstrated that CYP2C8 and CYP3A4/5 are the major enzymes responsible for the chloroquine N-deethylation to DCQ in human liver microsomes.
Subject(s)
Aryl Hydrocarbon Hydroxylases/biosynthesis , Chloroquine/metabolism , Cytochrome P-450 Enzyme System/biosynthesis , Microsomes, Liver/metabolism , Aryl Hydrocarbon Hydroxylases/antagonists & inhibitors , Biotransformation , Cytochrome P-450 CYP2C8 , Cytochrome P-450 CYP3A , Cytochrome P-450 Enzyme Inhibitors , DNA, Complementary/analysis , Enzyme Inhibitors/pharmacology , Humans , Microsomes, Liver/enzymologyABSTRACT
To investigate whether bee venom (BV) induces apoptosis, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, terminal deoxynucleotidyl transferase- mediated dUTP nick end-labeling assay, 4,6-diamidino-2-phenylindole staining, flow cytometric analysis, and DNA fragmentation assay were performed on NCI-H1299 lung cancer cells treated with BV. Through morphological and biochemical analyses, it was demonstrated that NCI-H1299 cells treated with BV exhibit several features of apoptosis. In addition, reverse transcription-polymerase chain reaction and prostaglandin E(2) (PGE(2)) immunoassay were performed to verify whether BV possesses an inhibitory effect on the expression of cyclooxygenase (COX) and PGE(2 )synthesis. Expression of COX-2 mRNA and synthesis of PGE(2) were inhibited by BV. These results suggest the possibility that BV may exert an anti-tumor effect on human lung cancer.