scholarly journals Anti-inflammatory properties of the combination of meloxicam and N-acetyl-L-proline

Author(s):  
A. U. Vauchok ◽  
B. V. Dubovik

The anti-inflammatory properties of the combination of meloxicam and atypical NSAID N-acetyl-L-proline (Groceprol®) after intragastric administration in a model of carrageenan paw edema in mice were studied. The average effective dose of N-acetyl-L-proline calculated by the regression analysis method in this model was 414 mg/kg, and the average effective dose of meloxicam was 2.85 mg/kg. In the combination in a ratio of 40:1, the activity of the compounds increases significantly, the ED50 of meloxicam decreases to 1 mg/kg, a similar value of N-acetyl-L-proline becomes 43 mg/kg. The same trend was also observed with another mass ratio of components of 20:1. The analysis of the pharmacodynamics of the combination of drugs according to the T. Chou method showed an additive type of interaction, typical for compounds with different mechanisms of primary action. It was established that a combination of N-acetyl-L-proline and meloxicam in the weight ratios of 40:1 and 20:1 demonstrate synergism, allowing to reduce the dose of the components in 2.7–9.6 times as compared with the effect of the drugs individually.The results of the study are the experimental justification for the use of anti-inflammatory synergistic combination of N-acetyl-L-proline and meloxicam.

2014 ◽  
Vol 0 (2) ◽  
Author(s):  
I. M. Belay ◽  
E. O. Mihayluk ◽  
V. V. Parchenko ◽  
O. I. Panasenko ◽  
E. G. Knysh

2021 ◽  
Vol 14 (4) ◽  
pp. 309-316

Abstract: The aim of the current study was to measure indoor radon concentration levels and its resulting doses received by the students and staff in schools of the directorate of education in the north of Hebron region- Palestine, during the summer months from June to September (2018), using CR-39 detectors. In this study, a total of 567 CR-39-based radon detectors were installed in the selected schools. The average radon concentrations were found to be 90.0, 66.5 and 58.0 Bqm-3 in Halhul, Beit Umar and Alarrub camp schools, respectively. Based on the measured indoor radon data, the overall average effective dose for the studied area was found to be 0.31 mSvy-1. Reported values for radon concentrations and corresponding doses are lower than ICRP recommended limits for workplaces. The results show no significant radiological risk for the pupils and staff in the schools under investigation. Consequently, the health hazards related to radiation are expected to be negligible. Keywords: Radon concentration, Alpha particles, Annual effective dose, Schools. PACs: 29.40.−n.


2021 ◽  
Vol 30 (3) ◽  
pp. 26-31
Author(s):  
L.T. Fahrtdinova ◽  
◽  
M.K. Sadigova ◽  
T.V. Kirillova ◽  
Yu. T. Saidullaeva ◽  
...  

The article presents the results of a study on the development of a recipe for semi‑finished custard based on gluten‑free raw materials. The ratio of components in the gluten‑free mixture was optimized using the regression analysis method. The influence of gluten‑free raw materials on the rheological properties of the semi‑ finished product is studied. The variants of the experiment differed in the composition of the composite mixture (the ratio of corn, rice flour and corn starch). The chemical composition and the ratio of the components of the mixture determine the rheological properties of the semi‑finished product. The experimental version with the ratio of rice flour, corn flour and corn starch 50:40:10 most corresponds to the rheological properties of the control version and is characterized by high consumer properties.


2016 ◽  
Vol 57 (4) ◽  
pp. 422-430 ◽  
Author(s):  
Masahiro Hosoda ◽  
Shinji Tokonami ◽  
Yasutaka Omori ◽  
Tetsuo Ishikawa ◽  
Kazuki Iwaoka

Abstract Due to the Fukushima Daiichi Nuclear Power Plant (FDNPP) accident, the evacuees from Namie Town still cannot reside in the town, and some continue to live in temporary housing units. In this study, the radon activity concentrations were measured at temporary housing facilities, apartments and detached houses in Fukushima Prefecture in order to estimate the annual internal exposure dose of residents. A passive radon–thoron monitor (using a CR-39) and a pulse-type ionization chamber were used to evaluate the radon activity concentration. The average radon activity concentrations at temporary housing units, including a medical clinic, apartments and detached houses, were 5, 7 and 9 Bq m −3 , respectively. Assuming the residents lived in these facilities for one year, the average annual effective doses due to indoor radon in each housing type were evaluated as 0.18, 0.22 and 0.29 mSv, respectively. The average effective doses to all residents in Fukushima Prefecture due to natural and artificial sources were estimated using the results of the indoor radon measurements and published data. The average effective dose due to natural sources for the evacuees from Namie Town was estimated to be 1.9 mSv. In comparison, for the first year after the FDNPP accident, the average effective dose for the evacuees due to artificial sources from the accident was 5.0 mSv. Although residents' internal and external exposures due to natural radionuclides cannot be avoided, it might be possible to lower external exposure due to the artificial radionuclides by changing some behaviors of residents.


2015 ◽  
Vol 167 (4) ◽  
pp. 671-677 ◽  
Author(s):  
Vitalija Samerdokiene ◽  
Albinas Mastauskas ◽  
Vydmantas Atkocius

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Ge Lu ◽  
Qian Wang ◽  
Zi-Jing Xie ◽  
Shang-Jie Liang ◽  
Hong-Xiao Li ◽  
...  

Diminished ovarian reserve (DOR) is an increasingly emerging reproductive disorder that disturbs reproductive-aged women, which is closely linked with inflammation. In clinic, moxibustion has already been applied for reproductive problems. In the present study, we examined the involvement of inflammation in DOR and investigated the effect of moxibustion for its anti-inflammatory activities. Methods. DOR rat model was established using tripterygium glycosides A tablets (TGs) suspension by intragastric administration and was then treated with either moxibustion or hormone replacement therapy (HRT), respectively. Estrus cycles were observed through vaginal cytology. Ovarian morphological alterations were observed by HE staining. The serum levels of follicle-stimulating hormone (FSH), estradiol (E2), anti-Müllerian hormone (AMH), tumor necrosis factor alpha (TNF-α), and interleukin-10 (IL-10) were measured through ELISA. The expression levels of Nrf2, HO-1, and NLRP3 were detected using immunohistochemistry. Nrf2, HO-1, and NLRP3 mRNA were examined by RT-PCR. Results. Moxibustion improved estrus cycles, FSH, E2, and AMH levels relative to DOR rats as well as HRT, while also inhibiting ovarian tissue injury. Anti-inflammatory cytokine IL-10 in peripheral blood was upregulated, and proinflammatory factor TNF-α was decreased after treatment with moxibustion. Moxibustion enhanced the expression of mRNA and protein of nuclear factor erythroid 2-related factor (Nrf2) and heme oxygenase-1 (HO-1); in the mean time, nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3) was suppressed. Conclusions. We demonstrated that moxibustion could ameliorate the ovarian reserve in rats induced by TGs. Overall, the effect of moxibustion was comparable to that of HRT. The underlying mechanism could be attributed to the anti-inflammatory effects of moxibustion, which suppressed NLRP3 activation by upregulating Nrf2/HO-1 signaling pathway.


2020 ◽  
Vol 11 ◽  
Author(s):  
Ye Yu ◽  
Dong-Ming Wu ◽  
Jing Li ◽  
Shi-Hua Deng ◽  
Teng Liu ◽  
...  

Multiple sclerosis (MS), an autoimmune and degenerative disease, is characterized by demyelination and chronic neuroinflammation. Bixin is a carotenoid isolated from the seeds of Bixa orellana that exhibits various potent pharmacological activities, including antioxidant, anti-inflammatory, and anti-tumor properties. However, the effects of bixin on MS have not yet been examined. To evaluate the effects and underlying molecular mechanisms of bixin on MS, experimental autoimmune encephalomyelitis (EAE) was established in C57BL/6 mice, which were treated via intragastric administration of bixin solutions. To evaluate the molecular mechanisms of bixin, quantitative reverse-transcription PCR, western blot, immunohistochemistry, flow cytometry, and enzyme-linked immunosorbent assay analyses were performed. We found that bixin significantly improved the symptoms and pathology in EAE mice, reduced the release of inflammatory cytokines TNF-α, IL-6, IL-8, IL-17, and IFN-γ, and increased the expression of the anti-inflammatory cytokine IL-10. And bixin reduced the proportion of Th1 and Th17 cells in the spleen and CNS, and suppressed microglia aggregation, and TXNIP/NLRP3 inflammasome activity by scavenging excessive reactive oxygen species (ROS) in EAE mice. Furthermore, bixin inhibited inflammation and oxidative stress via activating nuclear factor erythroid 2-related factor 2 (NRF2), and its downstream genes in EAE mice, meanwhile, these effects were suppressed upon treatment with an NRF2 inhibitor, ML385. Bixin prevented neuroinflammation and demyelination in EAE mice primarily by scavenging ROS through activation of the NRF2 signaling pathway. Taken together, our results indicate that bixin is a promising therapeutic candidate for treatment of MS.


Author(s):  
A. A. Spasov ◽  
D. S. Yakovlev ◽  
D. V. Maltsev ◽  
M. V. Miroshnikov ◽  
K. T. Sultanova ◽  
...  

Thearticlepresentstheresultsofastudyoftheneurotoxicologicalprofileofanew5-HT2A-antagonist(compoundI) using the method of multi-test observation by «S. Irwin». The test parameters were evaluated in parallel groups, receiving the compound in doses beginning with the average effective dose (ED50) and with a multiple increase of 2, 5, 7.5 and 10 times.The study revealed that the neurotoxicological properties of compound I are characterized by dose-dependent activity. It has been shown that neurotoxicological changes in the behavior of the animals did not occur with the administration of compound I at average effective dose of 10 mg / kg and doses, exceeding the effective by 2 and 5 times; the animals welfare corresponds to that of the control group. The most significant effects by the administration of the studied compound developed in high doses, exceeding the effective by 7.5 and 10 times. The limits of the minimum toxic dose (TDmin) for compound I by oral administration has been found to be 50 mg / kg <TDmin≤75 mg / kg.


Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 20-25 ◽  
Author(s):  
Xinyao Yang ◽  
Xiaoli Gao ◽  
Yuan Cao ◽  
Qiang Guo ◽  
Shanshan Li ◽  
...  

AbstractThe anti-inflammatory effects of boldine and reticuline isolated from Litsea cubeba were evaluated by using xylene-induced ear edema and carrageenan-induced paw edema in mice and rats. Our results demonstrated that intragastric administration with boldine and reticuline significantly mitigated ear weight in mice and decreased paw volume in rats. A combination administration of boldine (0.5 mg/kg) + reticuline (0.25 mg/kg) resulted in a potentiated inhibition in these two models. In parallel, boldine or reticuline reduce the infiltration of neutrophil leukocytes in rat paw tissue, respectively, and the combination of the two groups performed a better anti-inflammatory activity as shown in histopathologies. Boldine, reticuline, and their combination notably inhibited mRNA expressions of TNF-α, and IL-6 and reduced the phosphorylation levels of Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3). Beyond that, their combination also can reduce the phosphorylation levels of p65 and IκBα in the pathological tissues of animals, as observed by real-time PCR and western blot analyses, respectively. These findings indicate for the first time that boldine and reticuline have not only anti-inflammatory activity but also potential synergistic effects in vivo. The underlying mechanism may relate to the inhibition on the expression of pro-inflammatory cytokines, such as TNF-α and IL-6, which may be a consequence of JAK2/STAT3 and NF-κB pathway involvements. This study provides useful data for further exploration and application of boldine and reticuline as potential anti-inflammatory medicines.


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