Anti-inflammatory & anti-allergy agents in medicinal chemistry最新文献

Background: The constant increase of arterial hypertension and the development of pathology at an earlier age are global healthcare problems that cause damage to vital organs and worsen patient prognosis. In recent years, studies have shown that galectin-3 plays a role in the development and progression of arterial hypertension and coronavirus disease (COVID-19).

Objective: The explanatory research study aimed to analyze the prognostic value of galectin-3 determination in the serum blood and lymphocytes of patients with arterial hypertension and coronavirus disease (COVID-19).

Methods: The patients were divided into two groups: Group 1 consisted of 36 individuals with AH, Group 2 included 35 patients with arterial hypertension and polysegmental COVID-19 pneumonia, and 16 practically healthy individuals were included in the control group. All patients underwent anthropometry, biochemical blood analysis, determination of galectin-3, level in serum and lymphocytes, IL-1β, IL-6, and echocardiography.

Results: The highest level of galectin-3 was found in patients of Group 1, while in patients of Group 2, the concentration of galectin-3 was significantly decreased, mostly due to the treatment of COVID-19, in addition to prolonged antihypertensive therapy.

Conclusion: The level of galectin-3 in serum and lymphocytes was significantly higher in patients of both groups compared to the control group (p<0.05). Arterial hypertension causes structural changes in the cardiovascular system that are associated with elevated levels of galectin-3 in serum and lymphocytes. It can be used as a marker of myocardial damage in the context of arterial hypertension and COVID-19.

Background: Quercetin belongs to the BCS Class IV of drugs, which means it exhibits low solubility and low permeability. Quercetin is a potent antioxidant drug candidate, but it has several drawbacks, such as a short half-life, poor stability, bioavailability, and solubility. These factors affect its reliability as a good wound-healing, anti-inflammatory, and antioxidant agent. Quercetin nanoparticles resolved these problems and offered high stability, high encapsulation efficacy, sustained and prolonged release, and enhanced accumulation at target sites with high therapeutic efficacy.

Methods: Banana starch and quercetin were used to formulate a new composition of nanoparticles. Formulated QBSN were evaluated for their antioxidant, wound healing, and anti-inflammatory potential.

Results: QBSN showed a good antioxidant effect against the DPPH free radical scavenging model. Inhibition of DPPH free radicals reached up to 98 percent at 40 μl. Histopathological studies of treated tissues (wound and paw edema) confirmed the potential of QBSN.

Conclusion: In the future, prepared nanoparticles may be the choice of drug formulation for wound healing, anti-inflammatory therapy, and antioxidant therapy.

The role of herbal medicines in the treatment of viruses and the identification of potential antiviral drugs has been the focus of researchers for decades. The control and treatment of viral diseases are very important due to the evolution of viruses and the emergence of new viruses compared to other pathogens such as fungi and bacteria. Astragalus membranaceus (AM) is a significant medicinal plant. The potential use of this plant and its chemical components in the treatment of inflammatory illnesses and viral diseases has been vigorously researched recently. Astragalus polysaccharides (APS) make up the majority of AM's ingredients. The main mechanisms of the antiviral effect of APS have been investigated in some studies. The results of these studies show that APS can exert its antiviral effect by enhancing type I IFN signaling, inhibiting the expression of Bax and Caspase-3 proteins in the apoptosis pathway, and other antiviral mechanisms such as anti-inflammatory activities. The most well-known inflammatory products of APS's antiviral effects are B-cell proliferation, antibody products, nuclear factor-kappa B (NF-κB), and IL(s). Although it has a known effectiveness, there are some limitations to this substance's use as medicine. The use of nanotechnology is removing these limitations and its ability to be used as an anti-virus agent. The purpose of this review is to emphasize the role of AM, especially APS, in controlling inflammatory pathways in the treatment of viral infections. With the emergence of these herbal medications, a new path has been opened in the control and treatment of viral infections.

Background: By comparing the histamine impact to the instant response to an injected foreign protein in previously sensitized animals, one might hypothesize that histamine may be involved in this reaction. Through all four of the recognized types of histamine receptors, histamine is also essential for the control of immunological function and acute and chronic allergic inflammation.

Methods: Recent evidence points to anti-IgE antibodies and specific antibodies to cytokines like IL-4 or IL-5 that are associated with allergic inflammation as probable causes of Allergic Rhinitis. The therapeutic advantage of antihistamines is a decrease in allergy symptoms and any other allergy-related symptoms. We research the many diseases and dose forms in which antihistamines are used. Pediatric age groups have never been thoroughly studied for firstgeneration antihistamines. Oral antihistamines are suggested as the first line of therapy for people with mild to severe intermittent Allergic Rhinitis symptoms.

Results: Currently, approximately 100 different antihistamine-containing medicines and around 20 different H1-receptor antagonists are available for therapeutic use. Antihistamines of the second generation are more efficient and secure than those of the first generation. We conducted a research on the sedative and non-sedative effects of antihistamines used to treat various diseases.

Conclusion: The present investigation highlights the use of antihistamines in various diseases at different ages, their sedative and non-sedative effect, and their utility in treating insomnia based on their safety and current use among the patient population, as well as our observation.

Background: The benefits of folic acid supplementation have been documented in several studies. However, while evidence exists regarding its benefits for growth and haematologic parameters, its possible effects on the brain have been less examined.

Objectives: The study aimed to examine the benefits of dietary folic acid supplementation (beginning in the prepubertal period) on neurobehaviour, oxidative stress, inflammatory parameters, and neurotransmitter levels in adult mice.

Methods: Forty-eight prepubertal male mice were assigned into four groups of 12 animals each. Mice were grouped into normal control (fed standard diet) and three groups fed folic acid supplemented diet at 2.5, 5, and 10 mg/kg of feed. Animals were fed a standard diet or folic acid-supplemented diet for eight weeks during which food intake and body weight were assessed. On postnatal day 78, animals were exposed to the open-field, Y-maze, radial arm maze, elevated plus maze, bar test, and models of behavioural despair. 24 hours after the last behavioural test, animals were made to fast overnight and then sacrificed by cervical dislocation. Blood was then taken for the assessment of blood glucose, leptin, and insulin levels. Homogenates of brain tissue were prepared and used for the assessment of biochemical parameters.

Results: Results showed a concentration-dependent increase in body weight, and improved antioxidant status, memory scores, and acetylcholine levels. Also, a decrease in food intake, blood glucose, insulin, and leptin levels was observed. A reduction in open-field behaviour, anxiety-related behaviour, and proinflammatory markers, was also observed.

Conclusion: The beneficial effect of prepubertal continuous dietary folate fortification on the brain (as the animal ages) has been shown in this study.

Background: Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by inflammation of the joints, leading to pain, swelling, and joint deformity. Effective management of RA involves the use of disease-modifying drugs that can slow down disease progression and alleviate symptoms. Among the potential targets for RA treatment is Bruton's tyrosine kinase (BTK), which plays a crucial role in B-cell signalling and contributes to the pathogenesis of RA.

Aims: QSARINS (QSAR-INSUBRIA) is software used for the development and validation of Quantitative Structure-Activity Relationship (QSAR) analysis. In the present work, this software was explored for pharmacophore optimization of the pyrrolo-pyrimidine nucleus for anti-rheumatoid activity.

Methods: A series of pyrrolo-pyrimidine derivatives were used to build the QSAR models. These models were generated to identify structural features that correlate significantly with the activity. We followed the assessment of statistical parameters to ensure thorough validation of all the QSAR models. The QSAR models demonstrating better statistical performance were selected, and descriptors of these models were analysed.

Results: The results showed that the QSAR models were highly statistically robust and exhibited a strong external predictive ability. Their structural features were also deduced.

Conclusion: This QSAR study provided crucial information about the specific molecular features that can be used for the optimization of the pharmacophores. This research provides valuable insights into the structural features essential for BTK inhibition and paves the way for the design and development of novel anti-rheumatic agents targeting BTK in RA.

Background: The Capparidaceae family includes the medicinal herb Capparis herbacea Willd. The aerial and underground parts of plant C.herbacea were studied for their chemical composition, antioxidant, and cytotoxic properties.

Methods: Using gas chromatography with mass spectrometric detection (7890A/5975C), 94 chemicals were identified in ethanol extract from leaves, roots, seeds, and stems of C. herbacea. Main components were (leaves) phytol 18.16%, hexanedioic acid, bis(2-ethylhexyl) ester 16.75%, vitamin E 11.95%, (roots) sucrose 13.94%, hexadecanoic acid, ethylester 22.80%, octadecanoic acid, ethylester 37.77%; (seeds) hexadecanoic acid, ethylester 13.96%, ethyl9.cis.,11.trans.-octadecadienoate 48.54%, bis(2-ethylhexyl) phthalate 9.77%; (stems) 1-propene-1,2,3-tricarboxylic acid, tributyl ester 42.69%, and tributylacetylcitrate 19.63%. Nine components were identified in the makeup of the C. herbacea sample's essential oil using the method of chromatography-mass spectrometry.

Results: The main components were (in%): T-cadinol (29.56), meta-cymene (16.12), pulegone (14.11), and σ-amorphene (12.26). Chloroform and methanol extracts of Capparis herbacia roots at concentrations of 1 mg/ml showed higher average antioxidant activity, while ethyl acetate root extract at concentrations of 0.75 and 1 mg/ml showed higher average antioxidant activity compared to gallic acid AOA.

Conclusion: In addition, plant extracts have cytotoxic activity. Essential oils of leaves and stems, fruit and roots of Capparis herbacia plants exhibited cytotoxicity, all larvae died, and larval mortality was 96%.

Background: Endothelial nitric oxide synthase (eNOS) is known to be expressed in endothelium and smooth muscle cells of arteries. The aim of this study was to investigate the expression of eNOS in intimal and medial layer of aorta from rats fed with a high salt diet and its modulation by losartan and tempol.

Methods: Rats were fed during three weeks with: normal salt diet (NS, 0.4% NaCl); high salt diet (HS, 8% NaCl); NS plus tempol 1 mM (NS-T); HS plus tempol (HS-T); NS plus losartan 40mg.kg-1 (NS-L) and HS plus losartan (HS-L). Systolic blood pressure was recorded by the tail cuff method. Rats were then anaesthetized and the thoracic aorta and small arteries (bronchial branches of aorta) were processed to evaluate the expression of eNOS and aquaporin-1 (AQP-1) by immunohistochemistry.

Results: HS group showed increased systolic blood pressure, increased eNOS and AQP-1 immunoexpression in the aorta intimal layer, and decreased eNOS immunoexpression in the aorta medial layer, respect to NS group. Losartan and tempol prevented hypertension and changes in the expression of eNOS and AQP-1 of the intimal layer. However, only tempol increased the expression of eNOS elicited by sodium overload in the medial layer of the aorta and small arteries respect to HS group.

Conclusions: A high salt diet decreases eNOS expression in vascular smooth muscle layers of aorta and small arteries, which is reversed by tempol. These results suggest an adverse effect of oxidative stress on vascular eNOS in rats fed a high salt diet independently of hypertension.