Antiinflamm Antiallergy Agents Med Chem [JOURNAL]
Sun
200 papers
Are there any Therapeutic Options Currently Available for Wuhan Coronavirus?
Carradori S
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 32213152 · Publisher ↗
Abstract loading — click title to view on PubMed.
Effects of Broad Spectrum Antibiotics on Measurement of Immunosuppressant Drugs.
Gönel A, Kirhan I
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32208127 · Publisher ↗
BACKGROUND: Antibiotics used parenterally can affect blood drug level measurements, as measured in diagnostic tests. OBJECTIVE: To investigate the effect of six different antibiotics commonly used in intensive care units...
BACKGROUND: Antibiotics used parenterally can affect blood drug level measurements, as measured in diagnostic tests. OBJECTIVE: To investigate the effect of six different antibiotics commonly used in intensive care units on tacrolimus, sirolimus, everolimus and cyclosporin A levels measured by mass spectrometry. METHODS: Ampicillin + sulbactam (AB1, IV, 1 g), imipenem + cilastatin sodium (AB2, IV, 500 mg), piperacillin + tazobactam (AB3, 4.5 g, IV), ertapenem (AB4, IV, 1 g), meropenem trihydrate (AB5, 500 mg, IV) and ceftriaxone (AB6, 1 g, IV) antibiotics were used for the interference assay. Measurements were performed on the Shimadzu 8045 (Japan) LC-MS/MS instrument. Bias values were calculated. RESULTS: The least affected immunosuppressant was cyclosporine A (between -6.88% and 3.40%). The most affected were everolimus and sirolimus. Ertapenem caused negative interference on the level of everolimus at the rate of -27.34% and sirolimus at the rate of -26.79%. Piperacillin + tazobactam and imipenem + cilastatin sodium caused positive interferences on sirolimus at the rate of 24.24% and 22.73%, respectively. Ampicillin + sulbactam, meropenem trihydrate and ceftriaxone affected the sirolimus levels at lower rates (-4.49%, 5.93% and 9.86%). Everolimus levels deviated at the rate of -11.21% to -16.99% due to imipenem + cilastatin sodium, meropenem trihydrate and ceftriaxone. CONCLUSION: This study demonstrated the potential of antibiotic use affecting immunosuppressant levels. Antibiotic interference, especially in transplant patients, may cause erroneous immunosuppression, increasing the likelihood of rejection.
The Trinity of Matrix Metalloproteinases, Inflammation, and Cancer: A Literature Review of Recent Updates.
Ozkan E, Bakar-Ates F
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 32178620 · Full text
The critical link between cancer and inflammation has been known for many years. This complex network was further complexed by revealing the association of the matrix metalloproteinase family members with inflammatory cy...
The critical link between cancer and inflammation has been known for many years. This complex network was further complexed by revealing the association of the matrix metalloproteinase family members with inflammatory cytokines, which were previously known to be responsible for the development of metastasis. This article summarizes the current studies which evaluate the relationship between cancer and inflammatory microenvironment as well as the roles of MMPs on invasion and metastasis together.
and Study: COX-2 Inhibition by Ethanol Extract of Dayak Onion Bulb ( Merr) as Treatment Innovation of Benign Prostatic Hyperplasia (BPH).
Sutapa H, Widodo MA, Purnomo BB … +2 more , Soebadi DM, Negara EP
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32129166 · Publisher ↗
INTRODUCTION: Benign Prostatic Hyperplasia (BPH) is a benign tumor in males, which is histopathologically known with an increase of epithelial cells and prostatic stroma. Androgens, estrogens, stroma-epithelial interacti...
INTRODUCTION: Benign Prostatic Hyperplasia (BPH) is a benign tumor in males, which is histopathologically known with an increase of epithelial cells and prostatic stroma. Androgens, estrogens, stroma-epithelial interactions, growth factors, and chronic inflammation play a key role in the occurrence of BPH. Chronic inflammation in BPH is characterized by excessive expression of COX-2, which will trigger the expression of Bcl-2 anti-apoptotic protein. Dayak onion (Eleutherine Americana Merr) is a typical Kalimantan plant that is known as the treatment for prostate disease. This plant contains flavonoids which can inhibit the COX-2 enzyme thus causing a reduction in the production of prostaglandin E2. METHODS: This research was experimental research computationally and in vitro laboratory experimental research to determine COX-2 inhibitory activity by ethanol extracts of Dayak onion. RESULTS AND DISCUSSION: In in silico flavonoid, it was strongly related to COX-2 receptor on the active side of TYR371. Thus, it had the potential to inhibit COX-2. COX-2 inhibitor would cause BCL-2 to be inactive so that apoptosis occurr in BPH. In the in vitro research using human whole blood assay, the Dayak Onion bulb ethanol extract had IC50 COX-2 of 40.57 ng/ml and IC50 COX-1 of 364.89 ng/ml. Therefore, the ratio of IC50 COX-2 to IC50 COX-1 was 0.11. CONCLUSION: Ethanol extract of Dayak onion bulb has an inhibitory activity against COX-2. Thus, it has a potential of being an innovation for BPH treatment. Patient Summary: A healthy male, age 25-35 years old (history taking, physical and laboratory examination), and not using NSAIDs for the past 2 weeks.
The Role of Serum Procalcitonin Level as an Early Marker of Ascitic Fluid Infection in Post Hepatitic Cirrhotic Patients.
Abu Rahma MZ, Mahran ZG, Shafik EA … +6 more , Mohareb DA, Abd El-Rady NM, Mustafa MA, Khalil M, Abo-Amer YE, Abd-Elsalam S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32124702 · Publisher ↗
AIMS & BACKGROUND: The early diagnosis of spontaneous bacterial peritonitis (SBP) has been considered important in the overall patient's survival. Ascitic fluid culture examination performance, in the emergency setting,...
AIMS & BACKGROUND: The early diagnosis of spontaneous bacterial peritonitis (SBP) has been considered important in the overall patient's survival. Ascitic fluid culture examination performance, in the emergency setting, is time-consuming and not always available, so there is a need for easy to apply, rapid and reliable markers for diagnosis of patients with ascites. The present prospective study aimed to determine the early diagnostic value of serum procalcitonin (PCT) levels in decompensated cirrhotic patients (DCPs) with SBP. METHODS: 47 HCV cirrhotic patients with ascites were enrolled for this prospective study. The severity of cirrhosis was classified based on the Child-Pugh criteria. All patients were subjected to paracentesis and ascitic fluid (AF) culture. Serum PCT levels were measured using enzyme-linked fluorescence analysis (ELFA). RESULTS: The diagnostic value of serum PCT levels and WBC/PLT ratios for detecting infections were serum PCT levels (3.63 ± 3.47 ng/mL) in DCPs with infections which were significantly higher than in DCPs without infections (0.505 ± 0.230 ng/mL); p < 0.05. The cut-off value for serum PCT levels was 0.7 ng/mL for the diagnosis of infections in DCPs, for which the sensitivity and specificity were 93.1% and 73.2%, respectively. The AUC was 0.91 (95% CI: 0.83-0.99). CONCLUSION: Serum procalcitonin seems to provide satisfactory diagnostic biomarkers in SBP.
3,4,5-Trihydroxybenzoic Acid Attenuates Ligature-Induced Periodontal Disease in Wistar Rats.
Karatas O, Gevrek F
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32026787 · Publisher ↗
BACKGROUND: 3,4,5-Trihydroxybenzoic acid, which is also known as gallic acid, is an antiinflammatory agent that could provide beneficial effects in preventing periodontal inflammation. The present study aimed to evaluate...
BACKGROUND: 3,4,5-Trihydroxybenzoic acid, which is also known as gallic acid, is an antiinflammatory agent that could provide beneficial effects in preventing periodontal inflammation. The present study aimed to evaluate the anti-inflammatory effects of gallic acid on experimental periodontitis in Wistar rats. Alveolar bone loss, osteoclastic activity, osteoblastic activity, and collagenase activity were also determined. METHODS: Thirty-two Wistar rats were used in the present study. Study groups were created as following: Healthy control (C,n=8) group; periodontitis (P,n=8) group; periodontitis and 30 mg/kg gallic acid administered group (G30,n=8); periodontitis and 60 mg/kg gallic acid administered group (G60,n=8). Experimental periodontitis was created by placing 4-0 silk sutures around the mandibular right first molar tooth. Morphological changes in alveolar bone were determined by stereomicroscopic evaluation. Mandibles were undergone histological evaluation. Matrix metalloproteinase (MMP)-8, tissue inhibitor of MMPs (TIMP)-1, bone morphogenetic protein (BMP)-2 expressions, tartrateresistant acid phosphatase (TRAP) positive osteoclast cells, osteoblast, and inflammatory cell counts were determined. RESULTS: The highest alveolar bone loss was observed in the periodontitis group. Both doses of gallic acid decreased alveolar bone loss as compared to the P group. TRAP-positive osteoclast cell counts were higher in the P group, and gallic acid successfully lowered these counts. Osteoblast cells also increased in gallic acid administered groups. Inflammation in the P group was also higher than those of C, G30, and G60 groups supporting the role of gallic acid in preventing inflammation. 30 and 60 mg/kg doses of gallic acid decreased MMP-8 levels and increased TIMP-1 levels. BMP levels increased in gallic acid administered groups, similar to several osteoblasts. CONCLUSION: Present results revealed an anti-inflammatory effect of gallic acid, which was indicated by decreased alveolar bone loss and collagenase activity and increased osteoblastic activity.
Omalizumab in the Treatment of Chronic Urticaria: The Effect of Drug Co-Administration and Co-Morbidities.
Tagka A, Lambrou GI, Nicolaidou E … +4 more , Nakou E, Makris M, Stratigos A, Katsarou A
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32013838 · Publisher ↗
BACKGROUND: Chronic Spontaneous Urticaria (CSU) is a disease presenting typical wheals characterized by itching, angioedema or both. Although CU is, by appearance, a relatively "simple" disease, yet it has a devastating...
BACKGROUND: Chronic Spontaneous Urticaria (CSU) is a disease presenting typical wheals characterized by itching, angioedema or both. Although CU is, by appearance, a relatively "simple" disease, yet it has a devastating effect on those suffering due to its immense social implications. AIMS: The aim of the present study was to investigate the effect of omalizumab in the treatment of CSU. In particular, gender, co-administration of drugs and comorbidities were taken into account. MATERIALS AND METHODS: 108 patients (25 Males/83 Females) admitted to our department were diagnosed with CSU and were treated for 30 months. CSU was estimated on a score basis, which was used in order to define disease severity. The mean total CSU score and the mean CSU score of the first trimester, as well as the first semester, were calculated. Patients were treated with omalizumab, and in several cases, with co-administration of dapsone, cyclosporine and anti-histamines. RESULTS: Females manifested significantly higher scores as compared to males. Further on, patients who relapsed manifested significantly higher scores during the whole time course, as well as at the end of the first semester. CONCLUSION: Females are more prone to CSU. Although CSU scores in patients with remission, relapse and poor response manifested no significant difference at diagnosis, relapsed patients manifested higher CSU scores in the first semester. Therefore, the first semester of treatment is probably critical for the final patient outcome. Further studies are necessary in order to understand the mechanisms of CSU for better treatment and prognosis.
Quercetin Decreased Alveolar Bone Loss and Apoptosis in Experimentally Induced Periodontitis Model in Wistar Rats.
Taskan MM, Gevrek F
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31976849 · Publisher ↗
BACKGROUND: Quercetin is a flavonoid which has potent anti-inflammatory, antibacterial, and antioxidant effect. Purpose of this study was to evaluate effects of quercetin on alveolar bone loss and histopathological chang...
BACKGROUND: Quercetin is a flavonoid which has potent anti-inflammatory, antibacterial, and antioxidant effect. Purpose of this study was to evaluate effects of quercetin on alveolar bone loss and histopathological changes in ligature-induced periodontitis in rats. METHODS: Wistar rats were divided into four experimental groups: non-ligated control (C, n=8) group; periodontitis (P, n=8) group; ligature and low dose quercetin group (75 mg/kg/day quercetin, Q75 group, n=8); ligature and high dose quercetin group (150 mg/kg/day quercetin, Q150 group, n=8). Silk ligatures were placed at gingival margin of lower first molars of mandibular right quadrant. Study duration was 15 days, and animals were sacrificed end of this period. Changes in alveolar bone levels were clinically measured and tissues were immunohistochemically examined, matrix metalloproteinase 8 (MMP 8), inducible nitric oxide synthase (iNOS), tissue inhibitor of metalloproteinase 1 (TIMP 1), Cysteine-aspartic proteases 3 (Caspase 3), and tartrate-resistant acid phosphatase (TRAP) positive osteoclast cells, osteoblast, and neutrophil counts were also determined. RESULTS AND DISCUSSION: Alveolar bone loss was highest in P group, and differences among P, Q75, and Q150 groups were significant. Both doses of quercetin decreased TRAP+ osteoclast cells and increased osteoblast cells. Inflammation in P group was also higher than those of C, Q75, and Q150 groups indicating anti-inflammatory effect of quercetin. iNOS, MMP-8, and caspase-3 levels were highest, and TIMP-1 expression was lowest in P group; differences were statistically significant. CONCLUSION: Within limits of this study, it can be suggested that quercetin administration may reduce alveolar bone loss by increasing osteoblastic activity, decreasing osteoclastic activity, apoptosis, and inflammation in an experimental model of periodontitis.
Molecular Modelling, Synthesis and Evaluation of Flavone and Flavanone Scaffolds as Anti-inflammatory Agents.
Kiruthiga N, Alagumuthu M, Selvinthanuja C … +2 more , Srinivasan K, Sivakumar T
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 31899683 · Publisher ↗
OBJECTIVE: The objective of the study was to develop new Cyclooxygenase-2 inhibitors as anti-inflammatory agents from the synthetic route. MATERIALS AND METHODS: The 2-phenyl-4H-chromen-4-one and 2-phenyl-2,3-dihydro-4H-...
OBJECTIVE: The objective of the study was to develop new Cyclooxygenase-2 inhibitors as anti-inflammatory agents from the synthetic route. MATERIALS AND METHODS: The 2-phenyl-4H-chromen-4-one and 2-phenyl-2,3-dihydro-4H-chromenone hybrids were synthesised and characterised by using UV, IR, H-NMR, and mass spectrometry. An attempt was made for consolidated lead flavones and flavanones scaffolds by determining ADME/ T properties. Molecular docking simulations were performed by using Autodock.4 to understand the binding interaction over the targeted enzyme Cyclooxygenase-2. The titled compounds were evaluated for various in-vitro models for antioxidant and anti-inflammatory activities and based upon the IC values, the selected compounds were screened for in vivo anti-inflammatory activity by both acute and chronic models. RESULTS AND DISCUSSION: Twenty titled compounds were synthesised and elucidated their structure for confirmation of their functional groups by various spectroscopic techniques. Among the synthesized compounds, flavone derivatives such as HFc (7-hydroxy-3-(4-methoxy phenyl)-4H-chromen-4- one), HF (2-(2,4-di methoxy-phenyl)-7-hydroxy-4H-chromen-4-one) and HFe (7-hydroxy-2- (thiophen-2-yl)-4H-chromen-4-one) produced higher potency. Flavanone derivatives HFAc (7- hydroxy-2-(4-hydroxy-3-methoxy phenyl)-2,3-dihydro-4H-chromen-4-one), HFAb (7-hydroxy-2-(4- methoxy phenyl)-2,3-dihydro-4H-chromen-4-one) and HFA (7-hydroxy-2-(thiophen-2-yl)-2,3- dihydro-4H-chromen-4-one) showed significant anti-inflammatory activity compared to the standard COX-2 inhibitors. CONCLUSION: The flavone and flavanone scaffolds possess their excellent inhibitory action over the Cyclooxygenase-2 and act as a potential anti-inflammatory agent. The results of computational studies were also significantly correlated and concluded that those naturally mimicking flavonoid analogues were tremendous candidates to fight against the inflammatory diseases in drug discovery.
New Inhibition Detection Method to Evaluate the Human Salivary Alphaamylase Activity of Some Drugs, Molecular Docking, and SAR Studies.
Samira N, Khedidja B, Manel L … +2 more , Israa S, Mohamed Y
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 31899682 · Publisher ↗
BACKGROUND: For the first time, the investigation of six anti-inflammatory drugs and six antihistaminic drugs for inhibitory activities against alpha-amylase has been evaluated using a new inhibition detection method in...
BACKGROUND: For the first time, the investigation of six anti-inflammatory drugs and six antihistaminic drugs for inhibitory activities against alpha-amylase has been evaluated using a new inhibition detection method in order to find new treatments for some diseases caused by α-amylase. OBJECTIVE: The first part of this work was devoted to the evaluation of the inhibition activity of these drugs on salivary α-amylase in vitro. Then to study the nature of interactions and structure-activity relationship, using the Autodockvina program for molecular docking. MATERIALS AND METHODS: The evaluation of the inhibitory activity of our drugs is achieved using a new method that has proved its sensitivity, quickness, and effectiveness. RESULTS: The results of this study show that betamethasone and loratadine are potent α-amylase inhibitors with IC50 values 0.7mg/ml and 1.03 mg/ml, respectively compared to acarbose with IC50=5.6 μg/ml. CONCLUSION: The results showed that the loratadine and the betamethasone have a strong potential to inhibit the alpha-amylase.
Therapeutic Approach of Probiotics in Children with Atopic Dermatitis.
Huidrom S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 31899681 · Publisher ↗
Pediatric atopic dermatitis (AD) is a chronic, relapsing inflammatory skin disease, affecting 20% of children all over the world especially in developed countries. The global prevalence of AD in children has been increas...
Pediatric atopic dermatitis (AD) is a chronic, relapsing inflammatory skin disease, affecting 20% of children all over the world especially in developed countries. The global prevalence of AD in children has been increasing over recent years. This chronic inflammatory skin disease causes economic and social burden to the family. The exact cause of AD is not known, however recent studies suggest that the imbalance of microflora present in the gut leads to AD. The current treatment of AD involves the application of moisturizer, topical corticosteroids, antihistamines and antibiotics. This line of treatment of AD in children has many side effects. An alternative novel therapeutic approach has to be explored to combat this chronic skin disease. In recent years, there has been increasing interest in the use of probiotics in the modulation of gut microbiota for the management of AD. Many research studies showed that the administration of probiotics gives positive results in the prevention and treatment of AD in children, however, the results are not consistent and conclusive. In this review, the phenomenon that the dysbiosis of the gut flora contributes to the development of AD is addressed and clinical evidence of probiotics in the prevention and treatment of AD children is also summarised.
Pro- and Anti-Inflammatory Cytokine Expression Levels in Macrophages; An Approach to Develop Indazolpyridin-Methanones as a Novel Inflammation Medication.
Alagumuthu M, Srivastava V, Shah M … +3 more , Arumugam S, Sonaimuthu M, Arumugam NA
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31878864 · Full text
BACKGROUND: Macrophages play a serious part in the instigation, upkeep, and resolution of inflammation. They are activated or deactivated during inflammation progression. Activation signals include cytokines (IF-γ, granu...
BACKGROUND: Macrophages play a serious part in the instigation, upkeep, and resolution of inflammation. They are activated or deactivated during inflammation progression. Activation signals include cytokines (IF-γ, granulocyte-monocyte colonystimulating factor (GM-CSF), and TNF-α), extracellular matrix proteins, and other chemical mediators. Activated macrophages are deactivated by anti-inflammatory cytokines (IL- 10 and TGF-β (transforming growth factor-beta) and cytokine antagonists that are mainly produced by macrophages. Based on this, the present study aimed to develop novel (E)- Benzylidene-indazolpyridin methanones (Cpd-1-10) as effective anti-inflammatory agents by analyzing pro- and anti-inflammatory cytokine levels in macrophages. OBJECTIVES: To determine the anti-inflammatory effect of indazolpyridin-methanones by examining pro- and anti-inflammatory interleukin levels in J77A.1 macrophages. METHODS: Expression of cytokines such as TNF-α, IL-1β, IL-6 and IL-10 serum levels measured by ELISA method. Anti-cancer and cytotoxicity studies were carried out by MTT assay. COX-2 seems to be associated with cancers and atypical developments in the duodenal tract. So, a competitive ELISA based COX-2 inhibition assay was done. To validate the inhibitory potentials and to get more insight into the interaction of COX-2 with Cpd1-10, molecular docking was performed. RESULTS: Briefly, the COX-2 inhibitory relative activity was found to be in between the range of 80-92% (Diclofenac showed 84%, IC50 0.95 μM). CONCLUSION: Cytotoxicity effect of the compounds against breast cancer cell lines found excellent and an extended anticancer study ensured that these compounds are also alternative therapeutic agents against breast cancer. Among all the tested cancer cell lines, the anti- cancer effect on breast cancer was exceptional for the most active compounds Cpd5 and Cpd9.
Mitigation of Radiation-induced Gastrointestinal System Injury using Resveratrol or Alpha-lipoic Acid: A Pilot Histopathological Study.
Farhood B, Hassanzadeh G, Amini P … +7 more , Shabeeb D, Musa AE, Khodamoradi E, Mohseni M, Aliasgharzadeh A, Moradi H, Najafi M
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31713500 · Publisher ↗
AIM: In this study, we aimed to determine possible mitigation of radiationinduced toxicities in the duodenum, jejunum and colon using post-exposure treatment with resveratrol and alpha-lipoic acid. BACKGROUND: After the...
AIM: In this study, we aimed to determine possible mitigation of radiationinduced toxicities in the duodenum, jejunum and colon using post-exposure treatment with resveratrol and alpha-lipoic acid. BACKGROUND: After the bone marrow, gastrointestinal system toxicity is the second critical cause of death following whole-body exposure to radiation. Its side effects reduce the quality of life of patients who have undergone radiotherapy. Resveratrol has an antioxidant effect and stimulates DNA damage responses (DDRs). Alpha-lipoic acid neutralizes free radicals via the recycling of ascorbic acid and alpha-tocopherol. OBJECTIVE: This study is a pilot investigation of the mitigation of enteritis using resveratrol and alpha-lipoic acid following histopathological study. METHODS: 60 male mice were randomly assigned to six groups; control, resveratrol treatment, alpha-lipoic acid treatment, whole-body irradiation, irradiation plus resveratrol, and irradiation plus alpha-lipoic acid. The mice were irradiated with a single dose of 7 Gy from a cobalt-60 gamma-ray source. Treatment with resveratrol or alpha-lipoic acid started 24 h after irradiation and continued for 4 weeks. All mice were sacrificed after 30 days for histopathological evaluation of radiation-induced toxicities in the duodenum, jejunum and colon. RESULTS AND DISCUSSION: Exposure to radiation caused mild to severe damages to vessels, goblet cells and villous. It also led to significant infiltration of macrophages and leukocytes, especially in the colon. Both resveratrol and alpha-lipoic acid were able to mitigate morphological changes. However, they could not mitigate vascular injury. CONCLUSION: Resveratrol and alpha-lipoic acid could mitigate radiation-induced injuries in the small and large intestine. A comparison between these agents showed that resveratrol may be a more effective mitigator compared to alpha-lipoic acid.
Synthesis and Biological Activity of a Bis-steroid-Methanocyclobutanaphthalene- dione Derivative against Ischemia/Reperfusion Injury via Calcium Channel Activation.
Lauro FV, Francisco DC, Marcela RN … +6 more , Virginia MA, Alejandra GE, Maria LR, Lenin HH, Yaritza BB, Jhair CT
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31580254 · Full text
BACKGROUND: There is some experimental data on the effect exerted by some steroid derivatives against ischemia/reperfusion injury; however, the molecular mechanism is very confusing, perhaps this phenomenon could be due...
BACKGROUND: There is some experimental data on the effect exerted by some steroid derivatives against ischemia/reperfusion injury; however, the molecular mechanism is very confusing, perhaps this phenomenon could be due to the protocols used and/or differences in the chemical structure of each one of the steroid derivatives. OBJECTIVES: The aim of this study was to synthesize a new bis-steroid-methanocyclobutanaphthalene- dione derivative using some tools chemical. METHODOLOGY: The biological activity exerted by the bis-steroid-methanocyclobutanaphthalene- dione derivative against ischemia/reperfusion injury was evaluated in an isolated heart model using noradrenaline, milrinone, dobutamine, levosimendan, and Bay-K- 8644 as controls. In addition, other alternative experiments were carried out to evaluate the biological activity induced by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure in the absence or presence of nifedipine. RESULTS: The results showed that 1) the bis-steroid-methanocyclobuta-naphthalene-dione derivative significantly decreases the ischemia-reperfusion injury translated as a decrease in the the infarct area in a similar manner to levosimendan drug; 2) both bis-steroidmethanocyclobuta- naphthalene-dione and Bay-K-8644 increase the left ventricular pressure and 3) the biological activity exerted by bis-steroid-methanocyclobuta-naphthalenedione derivative against left ventricular pressure is inhibited by nifedipine. CONCLUSION: In conclusion, the bis-steroid-methanocyclobuta-naphthalene-dione derivative decreases the area of infarction and increases left ventricle pressure via calcium channels activation; this phenomenon could constitute a new therapy for ischemia/reperfusion injury.
Anti-inflammatory Property of AMP-activated Protein Kinase.
Noor HB, Mou NA, Salem L … +7 more , Shimul MFA, Biswas S, Akther R, Khan S, Raihan S, Mohib MM, Sagor MAT
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31530260 · Full text
BACKGROUND: One of the many debated topics in inflammation research is whether this scenario is really an accelerated form of human wound healing and immunityboosting or a push towards autoimmune diseases. The answer req...
BACKGROUND: One of the many debated topics in inflammation research is whether this scenario is really an accelerated form of human wound healing and immunityboosting or a push towards autoimmune diseases. The answer requires a better understanding of the normal inflammatory process, including the molecular pathology underlying the possible outcomes. Exciting recent investigations regarding severe human inflammatory disorders and autoimmune conditions have implicated molecular changes that are also linked to normal immunity, such as triggering factors, switching on and off, the influence of other diseases and faulty stem cell homeostasis, in disease progression and development. METHODS: We gathered around and collected recent online researches on immunity, inflammation, inflammatory disorders and AMPK. We basically searched PubMed, Scopus and Google Scholar to assemble the studies which were published since 2010. RESULTS: Our findings suggested that inflammation and related disorders are on the verge and interfere in the treatment of other diseases. AMPK serves as a key component that prevents various kinds of inflammatory signaling. In addition, our table and hypothetical figures may open a new door in inflammation research, which could be a greater therapeutic target for controlling diabetes, obesity, insulin resistance and preventing autoimmune diseases. CONCLUSION: The relationship between immunity and inflammation becomes easily apparent. Yet, the essence of inflammation turns out to be so startling that the theory may not be instantly established and many possible arguments are raised for its clearance. However, this study might be able to reveal some possible approaches where AMPK can reduce or prevent inflammatory disorders.
Tegaserod for the Treatment of Irritable Bowel Syndrome.
Madia VN, Messore A, Saccoliti F … +8 more , Tudino V, De Leo A, De Vita D, Bortolami M, Scipione L, Pindinello I, Costi R, Di Santo R
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31518227 · Full text
BACKGROUND: Tegaserod (Zelnorm®) is a 5-hydroxytryptamine (serotonin) type 4 receptor agonist for the treatment of hypomotility disorders of the lower gastrointestinal tract associated with the irritable bowel syndrome w...
BACKGROUND: Tegaserod (Zelnorm®) is a 5-hydroxytryptamine (serotonin) type 4 receptor agonist for the treatment of hypomotility disorders of the lower gastrointestinal tract associated with the irritable bowel syndrome with constipation (IBS-C). OBJECTIVE: The authors provide the reader with a better understanding on tegaserod mechanism of action, on its pharmacodynamics and pharmacokinetic properties, on safety and tolerability, with a summary of the key published clinical trials conducted in patients with irritable bowel syndrome (IBS). Its effects on colon inflammation have also been described. RESULTS: Tegaserod was withdrawn in 2007 due to increased risks of cardiovascular adverse effects. The manufacturer denied this, because pre-existing cardiovascular disease or risk factors were attributed to all affected patients. Thus, no causal relationship between tegaserod use and cardiovascular events was clearly shown. A matched case-control study of tegaserod-treated with untreated patients found no association between tegaserod and adverse cardiovascular outcomes. Despite its adverse effects, tegaserod resulted to be effective in treating chronic constipation in adult women aged < 65 years with IBS-C, while the safety and effectiveness of tegaserod in men with IBS-C have not been established. Tegaserod was resubmitted to the Food and Drug Administration in 2018 for use in a low-risk population. Moreover, tegaserod has also been shown to improve symptoms, enhance gastric accommodation and significantly attenuate visceral pain arising from the colon in functional dyspepsia patients. Treatment with tegaserod seems also to exert a protective effect in inflamed colons, reducing the severity of colitis in animal models.
In silico and in vitro Study of the Inhibitory Effect of Antiinflammatory Drug Betamethasone on Two Lipases.
Samira N, Khedidja B, Zahra AF … +2 more , Elyakine CKN, Mohamed Y
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31518226 · Full text
BACKGROUND: For the first time, the anti-inflammatory drug betamethasone is investigated for its inhibitory activity against lipase. OBJECTIVE: This work aims to demonstrate the in vitro and in silico inhibitory effect o...
BACKGROUND: For the first time, the anti-inflammatory drug betamethasone is investigated for its inhibitory activity against lipase. OBJECTIVE: This work aims to demonstrate the in vitro and in silico inhibitory effect of the anti-inflammatory drug betamethasone on the enzymatic activity of two lipases. METHODS: In vitro study using p-nitrophenyllaurate as lipase substrate is used to determine inhibition potency. Molecular Docking is performed using the Autodock Vina for drug molecule and two enzymes Candida rugosa lipase and human pancreatic lipase. RESULTS: Betamethasone represents a moderate inhibition effect with a value of IC50 of 0.36±0.01 mg/ml. Molecular docking allowed us to understand inhibitory - enzyme interactions and to confirm in vitro obtained results. CONCLUSION: These experiments showed that betamethasone can be used in the treatment of diseases related to lipase activity.
Protection from Radiation-induced Damage in Rat's Ileum and Colon by Combined Regimens of Melatonin and Metformin: A Histopathological Study.
Najafi M, Cheki M, Hassanzadeh G … +3 more , Amini P, Shabeeb D, Musa AE
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31438832 · Full text
BACKGROUND: Radiation-induced enteritis and proctitis are common side effects of abdominopelvic cancers among patients that undergo radiotherapy for prostate, colorectal or urinary cancers. Exposure of these tissues to h...
BACKGROUND: Radiation-induced enteritis and proctitis are common side effects of abdominopelvic cancers among patients that undergo radiotherapy for prostate, colorectal or urinary cancers. Exposure of these tissues to high doses of radiation leads to damage to villous, inflammation, pain, ulcer and bleeding, which may cause malabsorption and gastrointestinal disorders. To date, several procedures such as pharmaceutical treatment have been proposed for protection and mitigation of gastrointestinal toxicity following radiotherapy. AIMS: In the current study, we aimed to investigate the possible radioprotection of ileum and colon in rats using a combination of melatonin and metformin. METHODS: In this experimental study, 30 male Wistar rats were randomly assigned to six groups: control, melatonin (100 mg/kg) treatment, melatonin (100 mg/kg) plus metformin (100 mg/kg) treatment, radiation (10 Gy to whole body) group, radiation + melatonin (100 mg/kg) treatment, and radiation + melatonin (100 mg/kg) plus metformin (100 mg/kg) treatment. After 3.5 days, rats were sacrificed and their ileum and colon tissues carefully removed. Histopathological evaluations were conducted on these tissue samples. RESULTS: Histological evaluations reported moderate to severe damages to ileum and colon following whole body irradiation. Melatonin administration was able to protect the ileum remarkably, while the combination of melatonin and metformin was less effective. Interestingly, for the colon, melatonin was less effective while its combination with metformin was able to protect against radiation toxicity completely. CONCLUSION: For the ileum, melatonin was a more effective radioprotector compared to its combination with metformin. However, the combination of melatonin and metformin can be proposed as an ideal radioprotector for the colon.
Human Toxocara Infection: Allergy and Immune Responses.
Zibaei M, Shayesteh Z, Moradi N … +1 more , Bahadory S
Antiinflamm Antiallergy Agents Med Chem · 2019 · PMID 31379304 · Publisher ↗
BACKGROUND: Toxocariasis is a cosmopolitan infection that occurs in various regions worldwide, more frequently in developing countries. Chronic infections with Toxocara species in humans are associated with the productio...
BACKGROUND: Toxocariasis is a cosmopolitan infection that occurs in various regions worldwide, more frequently in developing countries. Chronic infections with Toxocara species in humans are associated with the production of high levels of specific and non-specific antibodies of all isotypes and IgG subclasses and a cytokine response characterized by the production of Th2 cytokines including IL-4, IL-5 and IL-13 by Peripheral Blood Monocytes (PBMCs) and Leukocytes (PBLs) in whole blood cultures. Other Th2 effector responses are also prominent during infection, reflected by elevated numbers of peripheral blood eosinophils and increased expression of eosinophil degranulation products. The production of IFN-γ by PBMCs/PBLs stimulated with Toxocara-secreted proteins is not prominent in toxocariasis but IL-10 production may be increased in infected individuals. The relationship between Toxocara species with allergic reactions was reported in the recent century. Experimental and epidemiological investigations revealed that toxocariasis with this parasite led to the development of allergic symptoms, such as asthma. However, the findings are conflicting since in other investigations no association between these two immunopathologies has been reported. CONCLUSION: The present review endeavours to summarize the data on Toxocara species and findings from studies on the relationship of toxocariasis with symptoms and signs of allergy. Furthermore, the mechanisms of immune responses and the factors associated between allergy and Toxocara infection are discussed.
Progranulin Regulates Inflammation and Tumor.
Liu C, Li J, Shi W … +5 more , Zhang L, Liu S, Lian Y, Liang S, Wang H
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31339079 · Full text
Progranulin (PGRN) mediates cell cycle progression and cell motility as a pleiotropic growth factor and acts as a universal regulator of cell growth, migration and transformation, cell cycle, wound healing, tumorigenesis...
Progranulin (PGRN) mediates cell cycle progression and cell motility as a pleiotropic growth factor and acts as a universal regulator of cell growth, migration and transformation, cell cycle, wound healing, tumorigenesis, and cytotoxic drug resistance as a secreted glycoprotein. PGRN overexpression can induce the secretion of many inflammatory cytokines, such as IL-8, -6,-10, TNF-α. At the same time, this protein can promote tumor proliferation and the occurrence and development of many related diseases such as gastric cancer, breast cancer, cervical cancer, colorectal cancer, renal injury, neurodegeneration, neuroinflammatory, human atherosclerotic plaque, hepatocarcinoma, acute kidney injury, amyotrophic lateral sclerosis, Alzheimer's disease and Parkinson's disease. In short, PGRN plays a very critical role in injury repair and tumorigenesis, it provides a new direction for succeeding research and serves as a target for clinical diagnosis and treatment, thus warranting further investigation. Here, we discuss the potential therapeutic utility and the effect of PGRN on the relationship between inflammation and cancer.
About
- Frequency
- Sun
- Papers found
- 200
- RSS feed
- Subscribe