Search results for: inflammatory

Authors: Imen Abid, Rachel Calvet, Michel Baltas

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Flavonoids are secondary metabolites that belong to a polyphenolic class, present in fruits and vegetables, playing a significant role in biological systems. The structural variations of these flavonoids are associated with many biological and pharmacological activities (antioxidant, anti-inflammatory, anticancer, antibacterial, antifungal, antiviral, and antimalarial). Given their importance in plants and health-promoting roles in humans, significant efforts have been devoted towards their isolation of flavonoids and chemical elaboration (organic synthesis). But with the increasing public concern over environmental degradation and future resources, it is of great importance for chemists to come up with different approaches, less hazardous to human health and the environment. Being employed in large amounts, the solvents used in organic synthesis are high on the list of environmental pollutants. To overcome these problems, our approach is to develop unconventional processes involving solvent-free conditions. The application of mechanical forces to solvent-free or solvent-less reaction mixtures through the use of ball mills offers many advantages over traditional solvent-based strategies. It is one of the unconventional activation methods, which makes it possible to overcome the use of solvents, in the context of green chemistry and more respectful of the environment.

Keywords: organic synthesis, green chemistry, mecanochemistry, pharmaceutical molecules

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Authors: José Neves, M. Rosário Martins, Fátima Candeias, Diana Ferreira, Sílvia Arantes, Júlio Cruz-Morais, Guida Gomes, Joaquim Macedo, António Abelha, Henrique Vicente

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Some plants of genus Schinus have been used in the folk medicine as topical antiseptic, digestive, purgative, diuretic, analgesic or antidepressant, and also for respiratory and urinary infections. Chemical composition of essential oils of S. molle and S. terebinthifolius had been evaluated and presented high variability according with the part of the plant studied and with the geographic and climatic regions. The pharmacological properties, namely antimicrobial, anti-tumoural and anti-inflammatory activities are conditioned by chemical composition of essential oils. Taking into account the difficulty to infer the pharmacological properties of Schinus essential oils without hard experimental approach, this work will focus on the development of a decision support system, in terms of its knowledge representation and reasoning procedures, under a formal framework based on Logic Programming, complemented with an approach to computing centered on Artificial Neural Networks and the respective Degree-of-Confidence that one has on such an occurrence.

Keywords: artificial neuronal networks, essential oils, knowledge representation and reasoning, logic programming, Schinus molle L., Schinus terebinthifolius Raddi

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Authors: H. Boucheloukh, S. Rouissa, N. Aoun, M. Beloucifa, T. Sehili, F. Parrino, V. Loddo

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To optimize water purification and wastewater treatment by heterogeneous photocatalysis, we used NiFe₂O₄ as a catalyst and solar irradiation as a source of energy. In this concept, an organic substance present in many industrial effluents was chosen: naproxen ((S)-6-methoxy-α-methyl-2-naphthaleneacetic acid or 2-(6-methoxynaphthalenyl) propanoic), a non-steroidal anti-inflammatory drug. The main objective of this study is to degrade naproxen by an iron and nickel catalyst, the degradation of this organic pollutant by nickel ferrite has been studied in a heterogeneous aqueous medium, with the study of the various factors influencing photocatalysis such as the concentration of matter and the acidity of the medium. The photocatalytic activity was followed by HPLC-UV andUV-Vis spectroscopy. A first-order kinetic model appropriately fitted the experimental data. The degradation of naproxen was also studied in the presence of H₂O₂ as well as in an aqueous solution. The new hetero-system NiFe₂O₄/oxalic acid is also discussed. The fastest naproxen degradation was obtained with NiFe₂O₄/H₂O₂. In a first-place, we detailed the characteristics of the material NiFe₂O₄, which was synthesized by the sol-gel methods, using various analytical techniques: visible UV spectrophotometry, X-ray diffraction, FTIR, cyclic voltammetry, luminescent discharge optical emission spectroscopy.

Keywords: naproxen, nickelate, photocatalysis, oxalic acid

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Authors: I. L. Ibrahim, A. Mann, B. A. Adam

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This project involved screening for antibacterial activity, phytochemical and mineral properties of Leptadenia hastata by flame photometry. The result of phytochemical screening reveals that the presence of flavonoids, tannins, saponins, alkaloids, steroidal, and anthraquinones while the cardiac glycoside was absent. This justifies the plant been used as anti-bleeding and anti-inflammatory agents. The result of flame photometry revealed that 1.85 % (Na), 0.65% (K) and 1.85 % (Ca) which indicates the safe nature of the plant extract as such could be used to lower high blood pressure. The antibacterial properties of both the aqueous and ethanolic extract were studied against some bacteria, Escherichia coli, Bacillus Cercus, Pseudomonas aeruginas, and Enterobacter aerogegens, by disc diffusion method and the result reveals that there are very good activities against the organism while the ethanolic extract at concentration 1.0 – 1.2 mg/ml. the ethanolic extract showed in considerable zone inhibition against bacteria’s; Escherichia coli, Bacillus Cercus, pseudomonas aeruginosa andklebsellapnemuoniae. Minimum inhibitory concentration (MIC) and minimum Bacterial concentration (MBC) were conducted with fairly good significant effect of inhibition on the organism, therefore, plant extract could be a potential source of antibacterial agent.

Keywords: antibacterial activity, Leptadenia hastata, infectious diseases, phytochemical screening

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Authors: Florge Francis A. Sy

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Acute pancreatitis (AP) is an inflammatory condition of the pancreas with local and systemic complications. Severe acute pancreatitis (SAP) has a higher mortality rate. Laboratory parameters like the neutrophil-to-lymphocyte ratio (NLR), red cell distribution width (RDW), and mean platelet volume (MPV) have been associated with SAP but with conflicting results. This study aims to determine the predictive value of these parameters on the severity and in-hospital mortality of AP. This retrospective, cross-sectional study was done in a private hospital in Cebu City, Philippines. One-hundred five patients were classified according to severity based on the modified Marshall scoring. The admitting hemogram, including the NLR, RDW, and MPV, was obtained from the complete blood count (CBC). Cut-off values for severity and in-hospital mortality were derived from the ROC. Association between NLR, RDW, and MPV with SAP and mortality were determined with a p-value of < 0.05 considered significant. The mean age for AP was 47.6 years, with 50.5% being male. Most had an unknown cause (49.5%), followed by a biliary cause (37.1%). Of the 105 patients, 23 patients had SAP, and 4 died. Older age, longer in-hospital duration, congestive heart failure, elevated creatinine, urea nitrogen, and white blood cell count were seen in SAP. The NLR was associated with in-hospital mortality using a cut-off of > 10.6 (OR 1.133, 95% CI, p-value 0.003) with 100% sensitivity, 70.3% specificity, 11.76% PPV and 100% NPV (AUC 0.855). The NLR was not associated with SAP. The RDW and MPV were not associated with SAP and mortality. The admitting NLR is, therefore, an easily accessible parameter that can predict in-hospital mortality in acute pancreatitis. Although the present study did not show an association of NLR with SAP nor RDW and MPV with both SAP and mortality, further studies are suggested to establish their clinical value.

Keywords: acute pancreatitis, mean platelet volume, neutrophil-lymphocyte ratio, red cell distribution width

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Authors: Bilal Ahmad

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Alzheimer’s disease (AD) is one of the most common neurodegenerative illnesses. However, how Gut-microbiota plays a role in the pathogenesis of AD is not well elucidated. The purpose of this literature review is to summarize and understand the current findings that may elucidate the gut microbiota's role in the development of AD. Methods: A literature review of all the relevant papers known to the author was conducted. Relevant articles, abstracts and research papers were collected from well-accepted web sources like PubMed, PMC, and Google Scholar. Results: Recent studies have shown that Gut-microbiota has an important role in the progression of AD via Gut-Microbiota-Brain Axis. The onset of AD supports the ‘Hygiene Hypothesis’, which shows that AD might begin in the Gut, causing dysbiosis, which interferes with the intestinal barrier by releasing pro-inflammatory cytokines and making its way up to the brain via the blood-brain barrier (BBB). Molecular mechanisms lipopolysaccharides and serotonin kynurenine (tryptophan) pathways have a direct association with inflammation, the immune system, neurodegeneration, and AD. Conclusion: The studies helped to analyze the molecular basis of AD, other neurological conditions like depression, autism, and Parkinson's disease and how they are linked to Gut-microbiota. Further, studies to explore the therapeutic effects of probiotics in AD and cognitive enhancement should be warranted to provide significant clinical and practical value.

Keywords: gut-microbiota, Alzheimer’s disease, second brain aging, lipopolysaccharides, short-chain fatty acids

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Authors: Niranjan Koirala, Sumangala Darsandhari, Hye Jin Jung, Jae Kyung Sohng

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Sakuranetin, an antifungal agent and genkwanin, an anti-inflammatory agent, are flavonoids with several potential pharmaceutical applications. To produce such valuable flavonoids in large quantity, an Escherichia coli cell factory has been created. E. coli harboring O-methyltransferase (SaOMT2) derived from Streptomyces avermitilis was employed for regiospecific methylation of naringenin and apigenin. In order to increase the production via biotransformation, metK gene was overexpressed and the conditions were optimized. The maximum yield of sakuranetin and genkwanin under optimized conditions was 197 µM and 170 µM respectively when 200 µM of naringenin and apigenin were supplemented in the separate cultures. Furthermore, sakuranetin was purified in large scale and used as a substrate for in vitro glycosylation by YjiC to produce glucose and galactose derivatives of sakuranetin for improved solubility. We also found that unlike naringenin, sakuranetin effectively inhibits α-melanocyte stimulating hormone (α-MSH)-stimulated melanogenesis in B16F10 melanoma cells. In addition, genkwanin more potently inhibited angiogenesis than apigenin. Based on our findings, we speculate that these compounds warrant further investigation in vivo as potential new therapeutic anti-carcinogenic, anti-melanogenic and anti-angiogenic agents.

Keywords: anti-carcinogenic, anti-melanogenic, glycosylation, methylation

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Authors: Naela Nabiela, Ahmad Hilmi Fahmi, M. Sukron, Ayu Elita Sari, Yusran, Suparmi

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Aspirin is one of NSAIDs (non-steroid inflammatory drugs), can cause gastric ulcer as an side effect of prolonged consumption. The effort to prevent the increase of gastric HCl level can by treating with amylopectin was reported that can cover the gastric mucose. However, the effect of amylopectin in starch from Manihot utilissima which is believed as traditional treatment gastric ulcer have not been clear yet. This study was conducted to determine the effect of starch formed as syrup to HCl level and gastric histopatology. This experiment post test only control group design used 42 male wistar rats divided into 7 groups. All groups, except first group, were induced by 60 mg/100gBW/day aspirin for 3 days. The following day for 2 days each group was treated by starch syrup at dosed 0.45% w/v, 0.9% w/v, 1.8% w/v, 0% w/v, and sucralfate. Respectively, HCl level were measured by acidi-alkalimetri titration method, while the gastric histopathology were prepared by hematoxylin-eosin staining. The result shows that aspirin induction can increase the HCl level as 0,00767 N. Starch syrup at dose 1.8% w/v was effective to reduce HCl level and the grade of second gastric necrosis. It can be conclude that starch syrup is potention as a treatment to cure gastric ulcer caused by NSAIDs side effect.

Keywords: concentration of HCl stomach, gastric histopathology, gastritis, starch

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Authors: Najwa Othman, Norhidayah Suleiman, Gun Hean Chong

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Palm fatty acid distillate (PFAD) is a by-product of palm oil refineries which contains valuable compounds such as phytosterols, squalene, polycosanol, co-enzyme Q10 and vitamin E (tocopherols and tocotrienols). Approximately 0.7-1.0% of vitamin E accumulates in PFAD, and it functions as antioxidants and anti-inflammatory. The objective of this research is to evaluate the effect of manipulated variables in supercritical carbon dioxide towards the recovery of tocotrienols in PFAD. The vitamin E concentrate isolated varies depending on the pre-treatment of sample and extraction techniques. In this research, tocotrienols in PFAD was concentrated by removing the extraneous matters, especially free fatty acid (FFA) and acylglycerols. Pre-treatment method such as enzymatic hydrolysis by using lipase from Candida rugosa as an enzyme was used to remove FFA and improve recovery of vitamin E. After that, treated PFAD was extracted by using supercritical fluid extraction in co-current glass beads packed column (22 cm x 75 cm i.d) at different temperatures (40-60°C) and pressures (100-300 bar) for 5 hours. After the extraction, the sample was analyzed by using high-pressure liquid chromatography (HPLC) system to quantify the tocotrienols. The results indicated that a combined pressure (200 bar) and temperature (60°C) was predicted to provide highest tocotrienols yield and the extraction yield obtained was 106.45%.

Keywords: enzymatic hydrolysis, palm fatty acid distillate, supercritical fluid extraction, tocotrienols

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Authors: A. Jafarzadeh, G. R. Hashemi Tabar

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Campylobacteriosis is caused by Campylobacter organisms. This is most commonly caused by C. jejuni, It is among the most common bacterial infections of humans, often a foodborne illness. It produces an inflammatory, sometimes bloody, diarrhea or dysentery syndrome, mostly including cramps, fever and pain. It is found in cattle, swine, and birds, where it is non-pathogenic. But the illness can also be caused by C. coli (also found in cattle, swine, and birds) C. upsaliensis (found in cats and dogs) and C. lari (present in seabirds in particular). Infection with a Campylobacter species is one of the most common causes of human bacterial gastroenteritis. For instance, an estimated 2 million cases of Campylobacter enteritis occur annually in the U.S., accounting for 5-7% of cases of gastroenteritis. Furthermore, in the United Kingdom during 2000 Campylobacter jejuni was involved in 77.3% in all cases of foodborne illness. 15 out of every 100,000 people are diagnosed with campylobacteriosis every year, and with many cases going unreported, up to 0.5% of the general population may unknowingly harbor Campylobacter in their gut annually. A large animal reservoir is present as well, with up to 100% of poultry, including chickens, turkeys, and waterfowl, having asymptomatic infections in their intestinal tracts. An infected chicken may contain up to 109 bacteria per 25 grams, and due to the installations, the bacteria is rapidly spread to other chicken. This vastly exceeds the infectious dose of 1000-10,000 bacteria for humans. In this article this disease is fully discussed in human and animals.

Keywords: campylobacteriosis, human, animal, zoonosis

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Authors: Lynda Golea, Rachid Chebaki

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Schiff bases contain heterocyclic structural units with N and O donor atoms which plays an important role in coordination chemistry. Azomethine groups are a broad class of widely used compounds with applications in many fields, including analytical, inorganic chemistry and biological. Schiff's base is of promising research interest due to the widespread antibacterial resistance in medical science. In addition, the research is essential to generate Schiff base metal complexes with various applications. Schiff complexes have been used as drugs and have antibacterial, antifungal, antiviral, and anti-inflammatory properties. The various donor atoms they contain offer a special ability for metal binding. In this research on the physicochemical properties of azomethine groups, we synthesized and studied the Schiff base compounds by a condensation reaction of tryptamines and acetophenone in ethanol. The structure of the prepared compound was interpreted using 1H NMR, 13C NMR, UV-vis and FT-IR. A computational analysis at the level of DFT with functional B3LYP in conjunction with the base 6-311+G (d, p) was conducted to study its electronic and molecular structure. The biological study was performed on three bacterial strains usually causing infection, including Gram-positive and Gram-negative, for antibacterial activity. Results showed moderate biological activity and proportional activity with increasing concentration.

Keywords: azomethine, HOMO, LUMO, RMN, molecular docking

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Authors: Sourabh Jain, Vikas Jain, Dharmendra Kumnar

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The present study investigated the antidiabetic potential of Cedrus deodara heart wood aqueous extract and its relationship in alloxan-induced diabetic rats. Aqueous extract of Cedrus deodara was found to reduce blood sugar level in alloxan induced diabetic rats. Reduction in blood sugar could be seen from 5th day after continuous administration of the extract and on 21st day sugar levels were found to be reduced by 40.20%. Oxidative stress produced by alloxan was found to be significantly lowered by the administration of Cedrus deodara aqueous extract (500 mg/kg). This was evident from a significant decrease in lipid per oxidation level in liver induced by alloxan. The level of Glutathione, Catalase, Superoxide dismutase and Glutathione-S-Transferase in liver, kidney and pancreas tissue were found to be increased significantly after drug administration. The results obtained in the present study suggest that the Cedrus deodara aqueous extract effectively and significantly reduced the oxidative stress induced by alloxan and produced a reduction in blood sugar level.

Keywords: Cedrus deodara, heartwood, antioxidant, anti-diabetic, anti-inflammatory

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Authors: Lourdes Hanna, Edward Poluyi, Chibuikem Ikwuegbuenyi, Eghosa Morgan, Grace Imaguezegie

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Background: Degeneration of the central nervous system (CNS), also known as neurodegeneration, describes an age-associated progressive loss of the structure and function of neuronal materials, leading to functional and mental impairments. Main body: Neuroinflammation contributes to the continuous worsening of neurodegenerative states which are characterised by functional and mental impairments due to the progressive loss of the structure and function of neu-ronal materials. Some of the most common neurodegenerative diseases include Alzheimer’s disease (AD), Parkinson’s disease (PD) and amyotrophic lateral sclerosis (ALS). Whilst neuroinflammation is a key contributor to the progression of such disease states, it is not the single cause as there are multiple factors which contribute. Theoretically, non-steroidal anti-inflammatory drugs (NSAIDs) have potential to target neuroinflammation to reduce the severity of disease states. Whilst some animal models investigating the effects of NSAIDs on the risk of neurodegenerative diseases have shown a beneficial effect, this is not the same finding. Conclusion: Further investigation using more advanced research methods is required to better understand neuroinflammatory pathways and understand if there is still a potential window for NSAID efficacy.

Keywords: intervention, central nervous system, neurodegeneration, neuroinflammation

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Authors: Arezou Hajhashemi, Karim Asgari, Masoud Etemadifar, Maryam Keyvani, Ali Hekmatnia

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Multiple Sclerosis (MS) is one of the most prevalent demyelinating diseases in CNS. As in other chronic cerebral diseases, impairment in cognitive functioning and in memory is popular. Because of the inflammatory and demyelinating nature of the disease, the localization of plaques in different parts of the Prefrontal and Limbic System, may lead to memorial symptoms. This investigation was intended to study relationship between frequency of plaques and memorial symptoms arising from dysfunction limbic system and prefrontal of patients with MS. The sample was selected randomly from patients with MS with memory problem, who have been referred to Isfahan Multiple Sclerosis Society. Brain System Test and Memory Test was administered to the sample, and their MRI's were analyzed by specialist in order to indentify two different parts of plaques. The data was analyzed by SPSS. The results showed that there were significant relationship between MS plaques and prefrontal's dysfunction and memorial symptom related to prefrontal area; however, there were no significant relationship between MS plaques and limbic system's dysfunction and memorial symptoms related to limbic system area. The results of this study suggest that memorial symptoms due to injury regions of the brain have the most significant relationship to prefrontal. Better judgment about these results needs more studies in future.

Keywords: multiple sclerosis, magnetic image, brain injury, behavior disorder

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Authors: Leila Anoosheh

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Aim: The aim of this study was to assess The effects of aerobic training on microRNA let-7a expression and levels of tumor tissue IL-6 in mice with breast cancer. Method: Twenty BALB/c c mice (4-5 weeks,17 gr mass) were cancerous by injection of estrogen-dependent receptor breast cancer cells MC4-L2 and divided into two groups: tumor-training(TT) and tumor-control(TC) group. Then TT group completed aerobic training for 6 weeks, 5 days per week (14-18 m/min). After tumor emersion, tumor width and length were measured by digital caliper every week. 48 hours after the last exercise subjects were killed. Tissue sampling were collected and stored in -70ᵒ. Tumor tissue was homogenized and let-7a expression and IL-6 levels were accounted with Real time-PCR and ELISA Kit respectively. Statistical analysis of let-7a was conducted by the REST software. Repeated measures and independent tests were used to assess tumor size and IL-6, respectively. Results: Tumor size and IL-6 levels were significantly decreased in TT group compare with TC group (p<0.05). microRNA let-7a was increased significantly in TT against control group respectively (p=0/000). Conclusion: Reduction in tumor size, followed by aerobic exercise can be attributed to the loss of inflammatory factors such as IL-6; It seems that regarding to up regulation effects of aerobic exercise training on let-7a and down regulation effects of that on IL-6 in mice with breast cancer, This type of training can be used as adjuvant therapy in conjunction with other therapies for breast cancer.

Keywords: breast cancer, aerobic training, microRNA let-7a, IL-6

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Authors: Muhamad Syafiq Hakimi Kamaruddin, Norhidayah Suleiman

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Ginger extracts (Zingiber officinale Rosc.) have been attributed therapeutic properties primarily as antioxidant, anticancer, and anti-inflammatory properties. Conventional extractions including Soxhlet and maceration are commonly used to extract the bioactive compounds from plant material. Nevertheless, high energy consumption and being non-environmentally friendly are the predominant limitations of the conventional extractions method. Herein, green technology, namely supercritical carbon dioxide (scCO2) extraction, is used to study process variables' effects on extract yields. Herein, green technology, namely supercritical carbon dioxide (scCO2) extraction, is used to study process variables' effects on extract yields. A pressure (10-30 MPa), temperature (40-60 °C), and median particle size (300-600 µm) were conducted at a CO2 flow rate of 0.9 ± 0.2 g/min for 120 mins. The highest overall yield was 4.58% obtained by the scCO2 extraction conditions of 300 bar and 60 °C with 300µm of ginger powder for 120 mins. In comparison, the yield of the extract was increased considerably within a short extraction time. The results show that scCO2 has a remarkable ability over ginger extract and is a promising technology for extracting bioactive compounds from plant material.

Keywords: conventional, ginger, non-environmentally, supercritical carbon dioxide, technology

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Authors: Ezaldin A. M. Mohammed, Youssef K. H. Abdalhafid, Masoud. M. Zatout

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The study aims to clarify the toxic effect of plant hormones, which are widely used in agriculture. One of these is the plant hormones (indole acetic acid); has been ٳata hormone to rats at 100 ppm salt solution of 0.2 per day after day for a period of forty days before conception until the fourteenth day or sixteenth or childbirth. Treatment brought about a marked shortage in the rate of increase in the weight of mice., And a percentage of the weight of the liver there was a distinct increase in the relative weight of the liver. As well as the increase in pathological changes and increase the size of the nuclei and Kupffer cell, as noted widespread and dense clusters of inflammatory cells accompanied by about the erosion of liver tissue and blood ٳrchah. Biochemical analyzes showed a marked decrease of the liver in antioxidant enzymes and an increase in the rate of free radicals. It was also noted an increase in cases of abortion. The owner of so many birth defects. It was also noted the lack of body weight in fetuses and increase the absorption rate of embryos in fetuses of mothers treatment compared to the control group. Showed microscopic examinations of the liver of mice born in the transaction and the decay in the presence of hepatic cells and edema, blood vessels and increase the rate of cell death.

Keywords: indol acetic acid, liver, pathological changes, albino rats

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Authors: Daniel Motlhanka, Neo Kerebotswe

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The strong and long history of use of medicinal plants in Botswana to address existing and emerging health threats provides undebatable evidence for their potential as innovative therapeutic tools. The prevalence of emerging health threats, such as COVID-19 and hard-to-treat non-communicable diseases, warrants the scientific community to revisit and exploit ethnopharmacology for its potential as a source of therapeutic tools. Many studies conducted on bioactivity-guided bioassays of ethnobotanical resources have proved a number of health beneficial properties of these plants, such as free radical scavenging, anti-inflammatory, antimicrobial and, most importantly, the capability of medicinal plants to alleviate oxidative stress. In this work, a number of medicinal plants used in Botswana traditional medicine were investigated for both their free radical scavenging capability and total phenolic contents using the Free Radical Scavenging Power (FRSP) and Folin Ciocalteau (FC) method. At 100 micrograms/ml all the studied plants expressed above 90% Scavenging power and expressed total phenolic contents between 5000- 8890 mg/L.GAE. These plants are promising tools for engineering active therapeutic tools against life-threatening diseases of oxidative stress origin.

Keywords: oxidative stress, non-communicable diseases, total phenolics, ethnobotanicals

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Authors: Muhammad Mustaqeem, Musa Kaleem Baloch, Irfan Ullah, Ammarah Luqman, Afshan Ahmad

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Flurbiprofen is one of the most potent nonsteroidal anti-inflammatory drugs. It is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrhea. However, its aqueous solubility is very low and hinders the skin permeation. Thus, it is imperative to develop such a drug delivery systems which can improve its aqueous solubility and hence improve the skin permeation and therapeutic compliance. Microemulsions have been also proven to increase the cutaneous absorption of lipophilic drugs as compared to conventional vehicles. Micro-emulsion is thermodynamically stable emulsion that has the capacity to ‘hide/solubilize’ water-insoluble molecules within a continuous oil phase. Therefore, flurbiprofen was converted to Easters through chemical reactions with alcohols such as methanol, ethanol, propanol and butanol. The product was further treated with hydrazine to get hydrazide. The solubility of the parent drug Flurbiprofen and the products were solubilized in microemulsions formed using various surfactants like ionic, non-ionic and zwitterions. It has been concluded that the product was more soluble than the parent compound. The biological activities of these were also investigated. The outcome was very promising and the product was more active than the parent compound. It, therefore, concluded that in this way, we can not only enhance the solubility of the drug and increase its bioactivity, but also reduce the risk of stomach cancer.

Keywords: Flurbiprofen, microemulsion, surfactants, hyrazides

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Authors: Katharigatta N. Venugopala, Melendhran Pillay, Bander E. Al-Dhubiab

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Tuberculosis (TB) infection is caused mainly by Mycobacterium tuberculosis (MTB) and it is one of the most threatening and wide spread infectious diseases in the world. Benzothiazole derivatives are found to have diverse chemical reactivity and broad spectrum of pharmacological activity. Some of the important pharmacological activities shown by the benzothiazole analogues are antitumor, anti-inflammatory, antimicrobial, anti-tubercular, anti-leishmanial, anticonvulsant and anti-HIV properties. Keeping all these facts in mind in the present investigation it was envisaged to synthesize a series of novel {2-(benzo[d]-thiazol-2-yl-methoxy)-substitutedaryl}-(substitutedaryl)-methanones (4a-f) and characterize by IR, NMR (1H and 13C), HRMS and single crystal x-ray studies. The title compounds are investigated for in vitro anti-tubercular activity against two TB strains such as H37Rv (ATCC 25177) and MDR-MTB (multi drug resistant MTB resistant to Isoniazid, Rifampicin and Ethambutol) by agar diffusion method. Among the synthesized compounds in the series, test compound {2-(benzo[d]thiazol-2-yl-methoxy)-5-fluorophenyl}-(4-chlorophenyl)-methanone (2c) was found to exhibit significant activity with MICs of 1 µg/mL and 2 µg/mL against H37Rv and MDR-MTB, respectively when compared to standard drugs. Single crystal x-ray studies was used to study intra and intermolecular interactions, including polymorphism behavior of the test compounds, but none of the compounds exhibited polymorphism behavior.

Keywords: benzothiazole analogues, characterization, crystallography, anti-TB activity

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Authors: Anusha Bhardwaj, Shekhar Shinde

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Nitric oxide (NO•) has been documented in research papers as one of the most versatile player in the therapeutics. It is identified as a biological multifunctional messenger molecule which is synthesized by the action of nitric oxide synthase (NOS) enzyme from L-arginine. The protective and the toxic effect in conjunction form the complete picture of the biological function of nitric oxide in humans. The dual nature is because of various factors such as concentration of NO, the isoform of NOS involved, type of cells in which it is synthesized, reaction partners like proteins, reactive oxygen intermediates, prosthetic groups, thiols etc., availability of the substrate L-arginine, intracellular environment in which NO is produced and generation of guanosine 3, 5’- cyclic monophosphate (cGMP). Activation of NOS through infection or trauma leads to one or more systemic effects including enhanced immune activity against invading pathogens, vaso/bronchodilatation in the cardiovascular and respiratory systems and altered neurotransmission which can be protective or toxic. Hence, NO affects the balance between healthy signaling and neurodegeneration in the brain. In lungs, it has beneficial effects on the function of airways as a bronchodilator and acts as the neurotransmitter of bronchodilator nerves. Whereas, on the other hand, NO may have deleterious effects by amplifying the asthmatic inflammatory response and also act as a vasodilator in the airways by increasing plasma exudation. But NOS Inhibitors and NO donors hamper the signalling pathway and hence a therapeutic application of NO is compromised.

Keywords: nitric oxide, multifunctional, dual nature, therapeutic applications

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Authors: So Youn Park, Yi Sle Lee, Ki Whan Hong, Chi Dae Kim

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The role of metabolism in the pathogenesis of osteoarthritis is an emerging field. Metabolic alterations may be a role in osteoarthritis (OA) pathogenesis, and these changes influence joint destruction via several cytokine. Especially, in OA patients, levels of IL-1β are elevated in the synovial fluid, synovial membrane, subchondral bone, and cartilage. The IL-1β is activated by NLRP3 inflammasomes, and NLRP3 inflammasomes are cytosolic complexes that drive the production of other inflammatory cytokines, including IL-1β. In this study, we examined that SIRT1 suppresses IL-1β through inhibiting NLRP3 inflammasomes and SIRT1 ameliorates osteoarthritis. OA fibroblasts were isolated from synovium of OA patients. IL-1β and NLRP3 were detected in synovium of OA patients by immunohistochemistry. Lipopolysaccharides (LPS) stimulated the expression of active IL-1β mRNA in OA fibroblasts and combination of LPS, and adenosine triphosphate increased more the expression of active IL-1β in OA fibroblasts. The level of IL-1β was measured by western blot and ELISA assay. NLRP3 inflammasomes complex were measured by western blot. SIRT1 did not inhibit expression of NLRP3 inflammasome. So caspase-1, apoptotic speck-like protein containing a caspase recruitment domain (ASC) and NLRP3 protein were expressed in OA fibroblasts. But SIRT1 suppressed activation of IL-1β by inhibiting activity of caspase-1 via NLRP3 inflammasome in OA fibroblasts under LPS plus ATP stimulation. These results suggest that SIRT1 is a modulator of NLRP3 inflammasomes in OA fibroblasts and ameliorate IL-1β, so expression of SIRT1 in OA fibroblast may be a potential strategy for OA inflammation treatment.

Keywords: osteoarthritis, inflammasome, SIRT1, IL-1beta

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Authors: Chowdhury Md. Navim Kabir

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Renal impairment is one of the most severe non-communicable diseases around the world. Especially patients with diagnosed/newly diagnosed renal impairment who need surgery are more focused on preoperative and postoperative preparation. Serum creatinine is the prime biochemical marker for assessing renal function, and the level of impairment is widely measured by this marker as well as Glomerular Filtration Rate (GFR). Objective: Factors responsible for fluctuating serum creatinine during preoperative and postoperative periods and minimizing the process of serum creatinine is the ultimate goal of this study. Method: 37 patients participated in this cross-sectional study who were previously diagnosed/newly diagnosed. They were admitted to different tertiary-level hospitals for emergency or elective surgery. Fifteen patients were admitted in the renal function impairment stage and 22 were admitted as normal patients’. Values of creatinine at the pre-admission stage and 2nd/3rd post-admission follow-up were compared. Results: 0.41 was the average of 22 patients' creatinine between pre-admission and 2nd/3rd follow-up. The responsible factor like prolonged staying, immobilization, co-morbidities, different preoperative antibiotics and Non-Steroidal Anti Inflammatory Drugs (NSAIDs) were also inducers for creatinine elevation. After postoperative hemodialysis rapid decrease of creatinine is seen in normal patients, but this decrease is very much minor in Chronic Kidney Disease (CKD) diagnosed patients.

Keywords: CKD, Meropenam, NSAID, comorbidities, immobilized

Procedia PDF Downloads 49

Authors: W. G. Kim, J. M. Chang, W. S. Kim

Abstract:

Immunologically non-treated and acellularized porcine xenografts were implanted as an arterial graft in goats and comparatively analyzed for the explanted grafts with gross observation, as well as light microscopy and immunohistochemistry, following the predetermined periods. For immunologically non-treated xenografts, bilateral porcine carotid arteries were harvested, and after short-term freezing at -70°C, were implanted into goats. The preparation of acellularized xenograft vessels has been performed with Nacl-SDS solution and stored at the freezer until use. The goats were randomly assigned for three periods of observation (3, 6, and 12 months after implantation), four animals were observed at each of these times. Periodic ultrasonographic examinations were performed during observation period. Following the predetermined periods, the explanted grafts were analyzed. Among 12 animals, one goat died prematurely, and a total of 22 grafts were evaluated. Gross observations revealed non-thrombotic patent smooth lumens. Microscopic examinations of the explanted grafts showed satisfactory cellular reconstruction up to the 12-month observation period. The proportions of CD3 positive T lymphocytes among inflammatory cells infiltrations were very low. In conclusion, these findings, as a whole, suggest that porcine vessel xenografts can be clinically acceptably implanted in the goats as a form of small-diameter vascular graft, regardless of the acellularized xenograft or immunologically non-treated xenograft.

Keywords: xenograft, arterial graft, long-term survival animals, immunology

Procedia PDF Downloads 319

Authors: Turker Yardan, Bahattin Avci, S. Sirri Bilge, Ayhan Bozkurt

Abstract:

Sinapic acid (SA) is a phenylpropanoid compound with anti-inflammatory, antioxidant, and neuroprotective activities. The purpose of this study was to characterize the possible protective effect of sinapic acid on chlorpyrifos (CPF), a common organophosphorus pesticide used worldwide, induced toxicity in rats. Forty male and female rats (240-270 g) were used in this study. Each group was composed of 5 male and 5 female rats. Sinapic acid (20 mg/kg or 40 mg/kg) or vehicle (olive oil, 1 ml ⁄ rat) were given orally for 5 days. CPF (279 mg/kg) or vehicle (peanut oil, 2 ml ⁄ kg, s.c.) was administered on the sixth day, immediately after the recording of the body weight of the animals. Twenty four hours following CPF administration body weight, body temperature and locomotor activity values were recorded before decapitation of the animals. Trunk blood, brain, and liver samples were collected for biochemical examinations. Chlorpyrifos administration decreased butyrylcholinesterase activity in blood, brain, and liver, while it increased malondialdehyde (MDA) levels and advanced oxidation protein products (AOPPs) (p < 0.01 - 0.001). Additionally, CPF administration reduced the body weight, body temperature, and locomotor activity values of the animals (p < 0.01 - 0.001). All these physiological and biochemical changes induced by CPF were reduced with the 40 mg/kg dose of SA (p < 0.05 - 0.001). Our results suggest that SA administration ameliorates CPF induced toxicity in rats, possibly by supporting the antioxidant mechanism.

Keywords: antioxidant, Chlorpyrifos, poisoning, sinapic acid

Procedia PDF Downloads 154

Authors: Francesca La Rosa , Marina Saresella, Mario Clerici, Michael Heneka

Abstract:

Neuroinflammation plays a key role in the modulation of the pathogenesis of neurodegenerative disorder such as Alzheimer's Disease (AD). Microglia, the main immune effector of the brain, are able to migrate to sites of Amyloid-beta (Aβ) deposition to eliminate Aβ phagocytosis upon activation by multiple receptors: Toll like receptors and scavenger receptors. The issue of whether microglia are able to eliminate pathological lesions such as neurofibrillary tangles or senile plaques from AD brain still remains the matter of controversy. Recent data suggest that the Nod Like Receptor 3 (NLRP3), multiprotein inflammasome complexes, plays a role in AD, as its activation in the microglia by Aβ triggers. IL-1β is produced as a biologically inactive pro-form and requires caspase-1 for activation and secretion. Caspase-1 activity is controlled by inflammasomes. We investigate about the importance of inflammasomes complex in the Aβ phagocytosis and its degradation. The preliminary results of phagocytosis assay and immunofluorescent experiment on primary Microglia cells to lipopolysaccharide (LPS) an Aβ exposure show that a previous treatment with LPS reduce Aβ phagocytosis. Different results were obtained in Primary Microglia wild type, NLRP3 and ASC Knockout suggesting a real inflammasomes involvement in Alzheimer's pathology. Inflammasomes inactivation reduces the production of inflammatory cytokines prolonging the protective activity of microglia and Aβ clearance, featuring a typical microglia phenotype of the early stage of AD disease.

Keywords: Alzheimer disease, innate immunity, neuroinflammation, NLRP3

Procedia PDF Downloads 424

Authors: Tuong Thi Van Thuy, Dao Van Toan, Nguyen Duc Phuc

Abstract:

Mesenchymal stem cells (MSCs) were discovered in the 1970s with their unique properties of differentiation, immunomodulation, multiple secreting, and homing factors to injured organs. MSC-based therapies have emerged as a promising strategy for various diseases such as cancer, tissue regeneration, or immunologic/inflammatory-related diseases. This study evaluated the clinical application of MSCs for cancer therapy in trials registered on Clinical Trial as of July 2022. The results showed 40 clinical trials used MSCs in various cancer conditions. 62% of trials used MSCs for therapeutic purposes to minimize the side effects of cancer treatment. Besides, 38% of trials were focused on using MSCs as a therapeutic agent to treat cancer directly. Most trials (38/40) are ongoing phase I/II, and 2 are entering phase III. 84% of trials used allogeneic MSCs compared with 13% using autologous sources and 3% using both. 25/40 trials showed participants received a single dose of MSCs, while the most times were 12 times in a pancreatic cancer treatment trial. Conclusion: MSC-based therapy for cancer in clinical trials should be applied to (1) minimize the side effects of oncological treatments and (2) directly affect the tumor via selectively delivering anti-cancer payloads to tumor cells. Allogeneic MSCs are a priority selected in clinical cancer therapy.

Keywords: mesenchymal stem cells, MSC-based therapy, cancer condition, cancer treatment, clinical trials

Procedia PDF Downloads 62

Authors: Njeim Pressila, Hajj-Boutros Guy, Antony D. Karelis

Abstract:

Background: Acute resistance exercise is associated with an elevated inflammation response, which could lead to delayed onset muscle soreness (DOMS). There is evidence that suggests that ingesting foods that have anti-inflammation properties may help reduce DOMS. A vegan diet has also been shown to be an anti-inflammatory diet which could, in turn, decrease DOMS. Objective and hypothesis: The purpose of the present study will be to compare markers of DOMS between vegans and omnivores after acute resistance exercise in young females. We hypothesize that vegans will have a better recovery of DOMS markers after a resistance exercise session compared to omnivores. Methods: Population: We will recruit30 vegans and 30 omnivores to participate in this study. Allvolunteers will follow either a vegan or an omnivore diet for at least 2 years. Anthropometric measurements, body composition, musclestrength (leg and chest press), markers of DOMS (swelling, pain, and stiffness), and dietary factors, as well as a wellness and anxiety questionnaire will be measured. All participants will also perform an acute resistance exercise session in order to induce DOMS. Pertinence: This project will give us a better understanding on the recovery process of vegans after a resistance training session and, as such, provide useful information to health professionals and athletes/coaches (kinesiologists and nutritionists)

Keywords: vgeans, omnivores, delayed onset muscle soreness, pain, stifness

Procedia PDF Downloads 105

Authors: Janneth Gonzalez, Marco Avila, George Barreto

Abstract:

GRP78 participates in multiple functions in the cell during normal and pathological conditions, controlling calcium homeostasis, protein folding and unfolded protein response. GRP78 is located in the endoplasmic reticulum, but it can change its location under stress, hypoxic and apoptotic conditions. NF-κB represents the keystone of the inflammatory process and regulates the transcription of several genes related with apoptosis, differentiation, and cell growth. The possible relationship between GRP78-NF-κB could support and explain several mechanisms that may regulate a variety of cell functions, especially following brain injuries. Although several reports show interactions between NF-κB and heat shock proteins family members, there is a lack of information on how GRP78 may be interacting with NF-κB, and possibly regulating its downstream activation. Therefore, we assessed the computational predictions of the GRP78 (Chain A) and NF-κB complex (IkB alpha and p65) protein-protein interactions. The interaction interface of the docking model showed that the amino acids ASN 47, GLU 215, GLY 403 of GRP78 and THR 54, ASN 182 and HIS 184 of NF-κB are key residues involved in the docking. The electrostatic field between GRP78-NF-κB interfaces and molecular dynamic simulations support the possible interaction between the proteins. In conclusion, this work shed some light in the possible GRP78-NF-κB complex indicating key residues in this crosstalk, which may be used as an input for better drug design strategy targeting NF-κB downstream signaling as a new therapeutic approach following brain injuries.

Keywords: computational biology, protein interactions, Grp78, bioinformatics, molecular dynamics

Procedia PDF Downloads 322

Authors: Tunca Gul Altuntas, Aziz Baydar, Cemre Acar, Sezen Yılmaz, Tulay Coban

Abstract:

Free radicals, which are generated in many bioorganic redox processes, play a role in the pathogenesis of several diseases including cancer, arthritis, hemorrhagic shock, inflammatory, cardiovascular, neurodegenerative diseases and age-related degenerative brain diseases. Exposures of normal cell to free radical damages several structures, oxidizes nucleic acids, proteins, lipids, or DNA. Compounds interfere with the action of reactive oxygen species might be useful in prevention and treatment of these pathologies. A series of indole compounds containing piperazine ring were synthesized. Coupling of indole-2-carboxylic acid with monosubstituted piperazines was accomplished with 1,1’-carbonyldiimidazole (CDI) in a good yield. The structures of prepared compounds were verified in good agreement with their 1H NMR (nuclear magnetic resonance), MS (mass spectrophotometry), and IR (infrared spectrophotometry) characteristics. In this work, all synthetized indole derivatives were screened in vitro for their antioxidative potential against vitamin E (α-tocopherol) using different antioxidant assays such as superoxide anion formation, lipid peroxidation levels in rat liver, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable radical scavenging activity. The synthesized compounds showed various levels of inhibition compared to vitamin E. This may give promising results for the development of new antioxidant agents.

Keywords: antioxidant, indoles, piperazines, reactive oxygen species

Procedia PDF Downloads 210