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

Background: Previous studies have experimentally validated and reported that chemical constituents of marine sponges are a source of natural anti-inflammatory substances with the biotechnological potential to develop novel drugs.

Aims: Therefore, the aim of this study was to perform a systematic review to provide an overview of the anti-inflammatory substances isolated from marine sponges with therapeutic potential.

Methods: This systematic review was performed on the Embase, PubMed, Scopus and Web of Science electronic databases. In total, 613 were found, but 340 duplicate studies were excluded, only 100 manuscripts were eligible, and 83 were included.

Results: The results were based on in vivo and in vitro assays, and the anti-inflammatory effects of 251 bioactive compounds extracted from marine sponges were investigated. Their anti-inflammatory activities include inhibition of pro-inflammatory mediators, such as tumor necrosis factor- α (TNF-α), interleukin-6 (IL-6), nitrite or nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin 1β (IL-1β), prostaglandin E2 (PGE2), phospholipase A2 (PLA2), nuclear transcription factor-kappa B (NF-κB), leukotriene B4 (LTB4), cyclooxygenase- 1 (COX-1), and superoxide radicals.

Conclusion: In conclusion, data suggest (approximately 98% of articles) that substances obtained from marine sponges may be promising for the development of novel anti-inflammatory drugs for the treatment of different pathological conditions.

Background: The combination of two drugs may lead to better results while reducing the need for each medication.

Objective: This study aimed to explore the synergistic benefits of combination therapy by suboptimal dose of niacin (Nic.) and prednisolone (Pred.) in an experimental model of Rheumatoid arthritis (RA).

Methods: About 50 male Wistar rats (weighing 150 - 160 grams) were randomly divided into five groups of ten, including healthy and RA groups treated with Nic. (80 mg/kg-orally), or Pred. (2 mg/kg-orally), and/or co-administration of Nic. and Pred. (half doses with each one-orally). RA was induced by the injection of complete Freund's adjuvant into the hind paw of each rat. All treatments were initiated on the fifth day following the induction and continued until day 30 post-induction.

Results: The combined Nic. and Pred. at half doses promoted a significant regression in the severity of the established RA, which is more pronounced than full doses of either drug alone. Combination therapy promoted a reduction in some hematological and biochemical RA parameters, like neutral red uptake by phagocytic cells, myeloperoxidase, nitric oxide, and C-reactive protein, more profound than each drug alone. Combined treatment caused a greater decrease in IFN-γ expression than other treatments in the area of plantar joints. All treatments were effective in increasing the expression of the IL-10 in the area of plantar joints. Prednisolone was less effective in reducing the expression of the TNF-α in the area of plantar joints than the other group.

Conclusion: This combination may be a useful approach to controlling RA.

Background: Oral strip is very similar to thin strip of postage stamp in shape, size and thickness. The strip is designed to be placed on the tongue or any oral mucosal tissue which immediately gets wet and hydrated after being in contact with the saliva. Desloratadine is one of the better- known second-generation antihistamines that has been studied for being effective in relieving the allergic nasal and skin symptoms.

Objective: The aim of this study is to develop desloratadine orodispersible film (ODF) with fast disintegration time and suitable mechanical strength to treat allergic symptoms in geriatric patients in order to increase compliance and convenience.

Methods: Solvent casting method using hydroxypropyl methylcellulose (HPMC) as the film forming polymer was applied. Polyethylene glycol 400 (PEG 400) and glycerol (Gly) were used as the plasticizers and citric acid (CA) was used as saliva stimulating agent. The resultant films were evaluated for disintegration time, folding endurance, surface pH, weight variation, thickness, surface morphology using scanning electron microscopy, drug content, content uniformity, moisture loss, moisture uptake, and drug-excipient compatibility using DSC and FT-IR.

Results: All the selected films started to disintegrate in less than 14 seconds. Selected optimum films exhibited good mechanical properties with a folding endurance value greater than 100. The uniformity in weight, thickness, and drug content in the selected films was obtained. Surface pH was within the normal range (6.4 - 6.8). A smooth surface of the films was obtained and drugexcipient compatibility was proved using DSC and FT-IR. The dissolution test was done for optimum film formulations by simulating the oral cavity physiological conditions using the conventional dissolution test apparatus. More than 87% of the drug was released by the 4th minute.

Conclusion: Orodispersible film of desloratadine was successfully prepared by solvent casting method in order to improve the disintegration/dissolution of the drug in oral cavity and hence better patient compliance and effective therapy.

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.