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

Background: The development of analgesic and anti-inflammatory drugs plays a crucial role in modern medicine, aiming to alleviate pain and reduce inflammation in patients. Opioids and nonsteroidal anti-inflammatory drugs are groups of drugs conventionally used to treat pain and inflammation, but a wide range of adverse effects and ineffectiveness in some pathological conditions leads us to search for new drugs with analgesic and anti-inflammatory properties.

Objectives: In this regard, the authors intend to investigate the ((2s,6s)-6-ethyl-tetrahydro-2h-pyran- 2-yl) methanol compound (LS20) on pain and acute inflammation.

Methods: Male Swiss mice were evaluated using acetic acid-induced abdominal writhing, formalin, and tail-flick as models of nociceptive evaluation and edema paw, air pouch and cell culture as models of inflammatory evaluation besides the rotarod test for assessment of motor impairment.

Results: The compound showed an effect on the acetic acid-induced abdominal writhing, formalin and tail-flick tests. Studying the mechanism of action, reversion of the antinociceptive effect of the compound was observed from previous intraperitoneal administration of selective and non-selective opioid antagonists on the tail flick test. In addition, the compound induced an antiedematogenic effect and reduced leukocyte migration and the production of pro-inflammatory cytokines in the air pouch model. LS20 was able to maintain cell viability, in addition to reducing cell production of TNF-α and IL-6.

Conclusion: In summary, the LS20 compound presented an antinociceptive effect, demonstrating the participation of the opioid system and an anti-inflammatory effect related to the inhibition of pro-inflammatory cytokine production. The compound also demonstrated safety at the cellular level.

Eczema is a systemic autoimmune disease characterized by inflammation and skin manifestation with a range of comorbidities that include physical and psychological disorders. Despite recent advancements in understanding the mechanisms involved in atopic dermatitis, current marketed products have shown varying results with more side effects. The present objective of the research studies is to develop new agents for eczema that cut down the cost of the novel drugs available and also improve the efficacy with the least adverse effects. Natural compounds and medicinal plants have been traditionally used since ancient civilizations. Nowadays, research in the herbal field is at its peak. One such natural compound, flavonoid, was found to be beneficial for the treatment of eczema. This review describes the use of certain flavonoid products to prepare preparations suitable for the treatment of prophylaxis or eczema. This is especially true for prophylaxis or atopic eczema treatment. These compounds exhibit anti-inflammatory, anti-inflammatory, anti-inflammatory, and anti-inflammatory properties and are, therefore, used in treatments to prevent allergies, inflammation, and irritation to the skin. We also dock the flavonoid derivatives used with the protein associated with the inhibition of eczema for better lead optimization. These preparations appear to be used for cosmetic, dermatological, or herbal remedies as a local application.

Background: Acquired immunity plays an important role in the prevention of viral infections. SARS-CoV-2 is an infection that leads to a pandemic. The development of specific anti-SARSCoV- 2 antibodies may play a vital role in disease prevention and control. Thus IgG antibody screening in the general population provides information on the immunological status of the community.

Aim: To clarify the SARS-CoV-2 immune status in the general population.

Methods: A cross-sectional study was conducted in Kirkuk province during the period from 15 May 2022 to 11 September 2022. The samples were collected from voluntary subjects and informed consent was taken from each participant before their enrolment in the study. SARS-CoV-2 IgG, SARSCoV- 2 IgM, 25-OH Vitamin D, Vitamin B12, and Folate were determined using the Electrochemiluminescence Immunoassay (eCLIA) technique with the instrument NIPIGON-Robot R1Automated ECL Analyzer (Canada).

Results: The overall IgG mean concentration was 37.75 ± 23.18 COI, with a median of 39.99 COI and a range of 0.25 - 87.23 COI. Additionally, 93% of tested samples were with concentrations of more than 1 COI. The highest frequency (18.2%) was for the IgG concentration of 51 to 60 COI, while the lowest frequency (1.3%) was for the concentration of 81 - 90 COI. The IgG was significantly higher (P = 0.046) in males (39.87 ± 24.04 COI) than that in females (35.12 ± 21.89 COI). The IgM overall concentration was 0.569 ± 0.456 COI, with a median of 0.489 COI and a range of 0.17 - 6.40 COI. The mean serum level of folic acid concentration was 9.03 ± 5.72 ng/ml, with a median of 7.476 ng/ml and a range of 0.60 - 20.00 ng/ml. The mean serum concentration of vitamin B12 was 462.65 ± 349.18 pg/ml, with a median of 353 pg/ml and a range of 13.05 - 2000 pg/ml. The mean serum concentration of vitamin D was 18.29 ± 18.42 ng/ml with a median of 12.44 ng/ml and a range of 3 - 100 ng/ml. IgG and IgM serum levels did not show a significant correlation with serum levels of folic acid, vitamin D, and vitamin B12. However, there was a significant correlation between folic acid and vitamin D (r = 0.197; P = 0.012); vitamin B12 and vitamin D (r = 0.253, P = 0.001). While there was a non-significant correlation between folic acid and vitamin D serum levels (r = 0.129, P = 0.10).

Conclusion: General population IgG antibody concentration reflects a high rate of herd immunity. Folic acid was with a mean value of about half of the upper normal limit and only 17.7% were with low values. Vitamin B12, only 6.3% of the population had values lower than normal. However, the range of vitamin B12 was wide. While vitamin D values were lower than the normal limit at 82.6%. However, a large scale well designed was warranted to evaluate COVID-19 national immune response.

An artificial glucocorticoid with anti-inflammatory and immunosuppressive properties is triamcinolone acetonide. It is abundantly used to treat redness, itching, and many other skin conditions like itching and psoriasis. As a result, there are several different triamcinolone acetonide formulations available. Each of these formulations must go through the correct phases of development and validation in order to identify the medications and other additives for safer use. This review article is just a representation of all the methods reported for the development and validation of triamcinolone acetonide in pure form to break down contaminants, in addition to other medications, and even in biological samples. The International Council for Harmonization (ICH) technical requirements for human use suggestions, which include a number of analytical parameters, have been followed in the validation of all the procedures. The present study also clarified the most significant drug combination.

The thiazole ring is a unique heterocyclic motif among heterocyclic compounds. This five-member ring with one nitrogen and one sulphur atom displays a wide array of pharmacological activities, including anti-inflammatory, antimicrobial, anticancer, antidiabetic, antiviral, etc., by acting on several targets. Its broad range of medical applications has inspired us to study this opulent heterocyclic molecule. The current review summarizes synthetic approaches for the preparation of thiazole derivatives in brief and discusses the promising biological activities of this scaffold. This review will be useful to the drug discovery community and will facilitate the synthesis and development of novel and potent thiazole derivatives, which may serve as lead molecules for the treatment of various diseases.

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.