Antiinflamm Antiallergy Agents Med Chem [JOURNAL]
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200 papers
A Comprehensive Review on Insect Repellent Agents: Medicinal Plants and Synthetic Compounds.
Yadav DK, Rathee S, Sharma V … +1 more , Patil UK
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39415571 · Publisher ↗
Plant-based repellents have been used for generations as personal protection against mosquitoes. Ethnobotanical studies provide valuable knowledge for developing natural products. Commercial repellents with plant-based i...
Plant-based repellents have been used for generations as personal protection against mosquitoes. Ethnobotanical studies provide valuable knowledge for developing natural products. Commercial repellents with plant-based ingredients are popular, but insufficient studies follow Pesticide Evaluation Scheme WHO guidelines. Further standardized studies are needed to evaluate repellent compounds and develop high-repellency and safe products. Essential Oils (EOs) from aromatic plants have gained popularity as low-risk insecticides due to their low toxicity and short environmental persistence. These plant-derived EOs, produced through steam distillation, have repellent, insecticidal, and growth-reducing effects on various insects. They control phytophagous insects, bite flies, and home and garden insects. US registration is the main hurdle for new EOs. This review explores the use of essential oils from plants as a natural repellent, focusing on their effectiveness and synergistic effects. Essential oils are volatile mixtures of hydrocarbons with diverse functional groups, and their effectiveness is linked to monoterpenes and sesquiterpenes. Synergistic effects can improve their effectiveness, and the use of other natural products, like vanillin, can increase protection time. ., and are among the most promising plant families.
Dry-feed Added Quercetin Mitigates Cyclophosphamide-induced Oxidative Stress, Inflammation and Gonadal Fibrosis in Adult Male Rats.
Olofinnade AT, Ajifolawe OB, Onaolapo OJ … +1 more , Onaolapo AY
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39350549 · Publisher ↗
BACKGROUND: Cyclophosphamide (CYP), a widely used cancer chemotherapeutic agent has been linked with male gonadotoxicity, resulting in infertility. The notion that potent antioxidants could be beneficial in mitigating CY...
BACKGROUND: Cyclophosphamide (CYP), a widely used cancer chemotherapeutic agent has been linked with male gonadotoxicity, resulting in infertility. The notion that potent antioxidants could be beneficial in mitigating CYP-induced gonadotoxicity necessitated this research. Therefore, we examined the effects of feed-added quercetin on CYP-induced gonadotoxicity in male rats. METHODS: Male postpubertal rats were randomly assigned into six groups of 10 rats each. The normal control (fed standard rodent diet) and two groups fed quercetin-supplemented diet at 100 and 200 mg/kg of feed received normal saline intraperitoneally at 2 ml/kg daily. A fourth group which served as the CYP control (fed standard rodent diet) and the last two groups fed quercetin at 100 and 200 mg/kg of feed were administered CYP at 150 mg/kg/day. Rats were administered normal saline or CYP intraperitoneally on days 1 and 2, while standard diet or feed-added quercetin was administered daily for 21 days. On day 22, half of the animals were either sacrificed or paired with age-matched females for fertility assessment. Estimation of testosterone levels, antioxidant, anti-inflammatory markers, and histomorphological examination of the testis and epididymis was also assessed. RESULTS: The administration of CYP was associated with weight loss, decreased food intake, decreased antioxidant capacity, increased gonadosomatic index, increased lipid peroxidation, sub-fertility, and histological evidence of gonadal injury. However, administration of quercetin reversed CYP-induced changes. CONCLUSION: The result of this study suggests that dietary quercetin supplementation has the ability to mitigate CYP induced gonadotoxicity and mitigate subfertility in male rats. However, further studies are required to assess its possible use in humans.
Molecular Docking, Pharmacophore Modeling and ADMET Prediction of Novel Heterocyclic Leads as Glucokinase Activators.
Mehra A, Mittal A, Singh S
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39350548 · Publisher ↗
BACKGROUND: A pivotal impetus has driven the development of numerous small molecules aiming to improve therapeutic strategies for type 2 diabetes. Glucokinase (GK) activation has been offered a new realm of therapeutic a...
BACKGROUND: A pivotal impetus has driven the development of numerous small molecules aiming to improve therapeutic strategies for type 2 diabetes. Glucokinase (GK) activation has been offered a new realm of therapeutic antidiabetic activity with novel heterocyclic derivatives. In the context of antidiabetic drug design, GK is an interesting and newly validated target. A key enzyme needed for blood glucose homeostasis is Glucokinase, which is dysfunctional in individuals with type 2 diabetes. Heterocyclic derivatives are utilized in this innovative approach to activate GK enzymes as medicinal agents that will significantly improve type 2 diabetes management. OBJECTIVES: To address type 2 diabetes, as well as minimize unwanted side effects, this research endeavor aimed to develop activators of glucokinase. METHODS: A rigorous scrutiny was conducted of the Maybridge online repository, which houses a formidable collection of 53,000 lead compounds. A collection of 125 compounds that contain the thiazolidinedione core was selected from this extensive collection. The structures were generated using ChemDraw 2D, stabilized conformation with ChemBioDraw Ultra, and docked using Auto Dock Vina 1.5.6 in this methodology. In addition, log P was predicted online using the Swiss ADME algorithm. The PKCSM software was used to predict the toxicity of the leading compounds. RESULTS: The highest binding affinity was found for AS72 and AS108 to GK receptors. GI absorption and excretion of these compounds were efficient due to Lipinski's Rule of Five compliance. When compared with the standard drugs Dorzagliatin (GKA) and MRK (co-crystallized ligand), these substances demonstrated a notable lack of AMES toxicity, skin sensitization, and hepatotoxicity. CONCLUSION: In recent studies, lead molecules that possess enhanced pharmacokinetic profiles, increased binding affinity, and lower toxicity were developed to act as glucokinase activators.
based Designing of benzothiazol-2-amine Derivatives as Analgesic and Anti-inflammatory Agents.
Mishra AK, Thajudeen KY, Singh M … +5 more , Rasool G, Kumar A, Singh H, Sharma K, Mishra A
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39162282 · Publisher ↗
BACKGROUND: Benzo[d]thiazoles represent a significant class of heterocyclic compounds renowned for their diverse pharmacological activities, including analgesic and antiinflammatory properties. This molecular scaffold ho...
BACKGROUND: Benzo[d]thiazoles represent a significant class of heterocyclic compounds renowned for their diverse pharmacological activities, including analgesic and antiinflammatory properties. This molecular scaffold holds substantial interest among medicinal chemists owing to its structural versatility and therapeutic potential. Incorporating the benzo[d]thiazole moiety into drug molecules has been extensively investigated as a strategy to craft novel therapeutics with heightened efficacy and minimized adverse effects. AIMS: The aim of the present research work was to design, synthesize and characterize the new benzo[d]thiazol-2-amine derivatives as potent analgesic and anti-inflammatory agents. MATERIALS AND METHODS: The synthesis of the presented benzo[d]thiazol-2-amine derivatives was performed by condensing-(4-chlorobenzylidene) benzo[d]thiazol-2-amine with a number of substituted phenols in the presence of potassium iodide and anhydrous potassium carbonate in dry acetone. IR spectroscopy, 1HNMR spectroscopy, 13CNMR spectroscopy and Mass spectroscopy methods were used to characterize the structural properties of all 13 newly synthesized derivatives. The molecular properties of these newly synthesized derivatives were estimated to study the attributes of drug-like candidates. Benzo[d]thiazol-2-amine derivatives were molecularly docked with selective enzymes COX-1 and COX-2. Analgesic and anti-inflammatory activities of synthesized compounds were evaluated by using albino rats. RESULTS: Findings of the research suggested that compounds G3, G4, G6, G8 and G11 possess higher binding affinity than diclofenac sodium, when docking was performed with enzyme COX-1. Compounds G1, G3, G6, G8 and G10 showed lower binding affinity than Indomethacin when docking was performed with enzyme COX-2. evaluation of the COX-1 and COX-2 enzyme inhibitory activities was performed for synthesized compounds. DISCUSSION: Compounds G10 and G11 exhibited significant COX-1 and COX-2 enzyme inhibitory action with an IC value of 5.0 and 10 μM, respectively. Using the hot plate method and the carrageenan-induced rat paw edema model, the synthesized compounds were screened for their biological activities, including analgesic and anti-inflammatory activities. Highest analgesic action was exhibited by derivative G11 and the compound G10 showed the highest anti-inflammatory response. Inhibition of COX may be considered as a mechanism of action of these compounds. CONCLUSION: It was concluded that synthesized derivatives G10 and G11 exhibited significant analgesic and anti-inflammatory effect; therefore, the said compounds may be subjected to further clinical investigation for establishing these as future compounds for the treatment of pain and inflammation.
Corrigendum to: Anti- SARS-CoV-2 IgG and IgM Levels in Iraqi General Population.
Alobaidi AH, Mustafa HI, Salih AM … +1 more , Alsamarai AM
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39162123 · Publisher ↗
A typographical error in the Reference No. 175 appeared erroneously in the References List of the article titled "Anti- SARSCoV- 2 IgG and IgM Levels in Iraqi General Population", 2023; 22(2) [1]. Original: Barassi, A.;...
A typographical error in the Reference No. 175 appeared erroneously in the References List of the article titled "Anti- SARSCoV- 2 IgG and IgM Levels in Iraqi General Population", 2023; 22(2) [1]. Original: Barassi, A.; Pezzilli, R.; Mondoni, M.; Rinaldo, R.F.; Dav, I.M.; Cozzolino, M. Vitamin D in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) patients with non-invasive ventilation support. Panminerva Med., 2021, ••• Corrected: Barassi, A.; Pezzilli, R.; Mondoni, M.; Rinaldo, R.F.; Davì, M.; Cozzolino, M. Vitamin D in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) patients with non-invasive ventilation support. Panminerva Med., 2023, 65(1), 23-29. We apologize to the readers for the inconvenience caused due to this error. The original article can be found online at: https://www.eurekaselect.com/article/135111.
Ferulic Acid: A Review of Mechanisms of Action, Absorption, Toxicology, Application on Wound Healing.
Werneck Cerqueira AFL, de Mello Brandão H, Tavares GD … +1 more , Rodarte MP
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39108119 · Publisher ↗
UNLABELLED: Ferulic acid is a widely distributed phenolic substance with diverse bioactive properties, which has been widely used in the pharmaceutical, food, and cosmetic industries. Wounds are complex skin lesions to t...
UNLABELLED: Ferulic acid is a widely distributed phenolic substance with diverse bioactive properties, which has been widely used in the pharmaceutical, food, and cosmetic industries. Wounds are complex skin lesions to treat and their treatment is long and costly. This encourages the search for alternative treatments, especially in the area of bioactive substances of natural origin. AIMS: This work aims to make a bibliographic survey on studies of the use of ferulic acid in the treatment of wounds. RESULTS: The studies found show that ferulic acid acts through different mechanisms of action such as antioxidant, anti-inflammatory, antimicrobial, collagen production, angiogenic, and reepithelialization effects. These properties act synergistically in different stages of healing, which differentiates it from conventional treatments. In addition, ferulic acid has dermal absorption, low skin metabolism, and low toxicity. CONCLUSION: Studies in this area are recent and further research is needed to expand the possibilities and therapeutic efficiency of ferulic acid in wound healing.
Using Quality by Design Tools to Study Gel Formulation from Leaves and Conducting its Molecular Docking, and ADMET Analyses.
Kanakal MM, Abbas SA, Khan A … +7 more , Sultana S, Fatima H, Tabasssum R, Ahmed MG, Sultana R, Mohammed JS, Salfi R
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39082166 · Publisher ↗
INTRODUCTION: This research aims to create a gel formulation of Brassica juncea leaf extract and assess its anti-inflammatory properties using an study. The anti-inflammatory activity has been compared with Diclofenac m...
INTRODUCTION: This research aims to create a gel formulation of Brassica juncea leaf extract and assess its anti-inflammatory properties using an study. The anti-inflammatory activity has been compared with Diclofenac molecules in PDB id: 4Z69. Further, the Absorption, Distribution, Metabolism, Excretion, and Toxicity analysis has been performed to ensure the therapeutic potential and safety of the drug development process. The Quality by Design tool has been applied to optimize formulation development. METHODS: The extracted gel is characterized by performing Fourier transformer infrared, zeta potential, particle size, Scanning Electron Microscope, and entrapment efficiency. Further, the formulation is evaluated by examining its viscosity, spreadability, and pH measurement. An study of all nine extract suspensions was conducted to determine the drug contents at 276 nm. RESULTS: The optimized suspension has shown the maximum percentage of drug release (82%) in 10 hours of study. Animal study for anti-inflammatory activity was performed, and results of all five groups of animals compared the % inhibition of paw edema at three hours; gel (56.70%), standard (47.86%), and (39.72%) were found. CONCLUSION: The research could conclude that the anti-inflammatory activity of gel formulation is high compared to extract, and a molecular docking study validates the anti-inflammatory therapeutic effects. ADMET analysis ensures the therapeutic effects and their safety.
The Influence of Phytoconstituents for the Management of Antipsoriatic Activity in Various Animal Models.
Yadav R, Yadav T, Upadhayay A … +4 more , Alam MS, Dubey G, Kumar V, Sahu A
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39082165 · Publisher ↗
It is possible for psoriasis to manifest at any point in a person's life, regardless of their age, gender, or geographic location. It is a chronic immune-linked inflammatory skin illness that affects individuals of vario...
It is possible for psoriasis to manifest at any point in a person's life, regardless of their age, gender, or geographic location. It is a chronic immune-linked inflammatory skin illness that affects individuals of various racial and ethnic origins. It is recognized to be a longlasting condition. Because of the significant contribution that natural products have made, there has been a significant advancement in the treatment of skin illnesses such as psoriasis. The biggest number of phytochemicals derived from a wide range of plants and herbs are now being used in a variety of applications throughout the whole world. Additionally, a number of phytochemicals, including aloe-emodin, psoralen, curcumin, and others, have been effectively extracted in pure or clear form, and they have shown a great deal of efficacy in the treatment of psoriasis illness. There is evidence that few herbal remedies are effective, and the occurrence of these phytochemicals provides more proof. When synthetic medications are used for chronic therapy, they may cause a variety of adverse consequences; hence, the exploration of natural pharmaceuticals can give a successful natural treatment with a minimal amount of adverse effects. Within the scope of this concise review, a number of plant sources that possess anti-psoriatic activity are investigated, and the antipsoriatic effects of these plant sources are shown on a number of animal models using particular pathways.
Topical Administration of Nanostructured Lipid Carriers as a Viable Approach to Reduce Inflammation: A Review.
Rajak P, Karmakar A, Sarma S … +1 more , Bhuyan B
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39082164 · Publisher ↗
This review seeks to assess the potential of nanomaterials, specifically Nano-structured Lipid Carriers (NLCs), in mitigating challenges associated with inflammation-related disorders, with a particular emphasis on chron...
This review seeks to assess the potential of nanomaterials, specifically Nano-structured Lipid Carriers (NLCs), in mitigating challenges associated with inflammation-related disorders, with a particular emphasis on chronic ailments like arthritis. A comprehensive literature review spanning Web of Science, PubMed, and other scholarly repositories from 2000 to 2023 is conducted. Articles are selected based on their focus on NLCs and inflammation management, utilizing keywords, such as "nanomaterials," "targeted drug delivery," and "arthritis." Exclusion criteria involve non-English studies or those lacking adequate detail on NLCs. Synthesized data provide an overview of the advantages, challenges, and prospects of NLCs in addressing chronic inflammatory disorders. This review also examines the therapeutic applications of nanotechnology, including targeted drug delivery and tissue engineering, particularly focusing on the intricate biological responses in chronic inflammation, often involving Non-steroidal Anti-inflammatory Drugs (NSAIDs). Moreover, the exploration extends to topical delivery methods to enhance control over medication concentration, with a review of lipid nanoparticles, such as liposomes and solid-lipid nanoparticles, highlighting their potential in augmenting drug permeation while addressing challenges like inadequate drug loading. NLCs have emerged as promising candidates for overcoming drug delivery challenges, particularly in arthritis treatment, with a focus on their advantages across diverse lipid compositions. The review underscores significant strides in inflammation management through NLC utilization, offering insights into future research directions. Moreover, it contributes to ongoing advancements in nanomedicine, emphasizing the pivotal role of NLCs in developing innovative therapeutic approaches for inflammation-related disorders, particularly arthritis. NLCs represent a promising avenue for effective interventions, signaling progress in nanotechnology-enabled therapeutics.
Naringenin: A Promising Immunomodulator for Anti-inflammatory, Neuroprotective and Anti-cancer Applications.
Solanki S, Vig H, Khatri N … +5 more , Singh BP, Khan MS, Devgun M, Wal P, Wal A
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39076091 · Publisher ↗
BACKGROUND: Inflammatory, immune, and neurodegenerative diseases constitute a category of persistent and debilitating conditions affecting millions worldwide, with intertwined pathophysiological pathways. Recent research...
BACKGROUND: Inflammatory, immune, and neurodegenerative diseases constitute a category of persistent and debilitating conditions affecting millions worldwide, with intertwined pathophysiological pathways. Recent research has spotlighted naturally occurring compounds like naringenin for potential therapeutic applications across multiple ailments. OBJECTIVES: This review offers an encompassing exploration of naringenin's anti-inflammatory, immune-protective, and neuroprotective mechanisms, elucidating its pharmacological targets, signal transduction pathways, safety profile, and insights from clinical investigations. METHODS: Data for this review were amassed through the scrutiny of various published studies search engines such as PubMed and Google Scholar. Content from reputable publishers including Bentham Science, Taylor and Francis, Nature, PLOS ONE, among others, was referenced. RESULTS: Naringenin exhibits substantial anti-inflammatory effects by restraining the NF-κB signaling pathway. It activates Nrf2, renowned for its anti-inflammatory properties, inducing the release of hemeoxynase-1 by macrophages. Furthermore, naringenin treatment downregulates the expression of Th1 cytokines and inflammatory mediators. It also impedes xanthine oxidase, counteracts reactive oxygen species (ROS), scavenges superoxide radicals, mitigates the accessibility of oxygen-induced K+ erythrocytes, and reduces lipid peroxidation. Naringenin's antioxidant prowess holds promise for addressing neurological conditions. CONCLUSION: Extensive research has been undertaken to establish the anti-inflammatory, immunomodulatory, and neuroprotective attributes of naringenin across various medical domains, lending credence to its pharmacological utility. The principal obstacle to naringenin's adoption as a therapeutic agent remains the dearth of in vivo data. Efforts should focus on rendering naringenin delivery patient-friendly, economically viable, and technologically advanced.
Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer.
Kumari V, Bajpai M
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39069701 · Publisher ↗
INTRODUCTION: Emulgel dosage form is an advanced form of transdermal drug delivery. It is a combination of emulsion and gel in a definite ratio. Emulsions are incorporated into the gel with proper mixing. The emulsion pr...
INTRODUCTION: Emulgel dosage form is an advanced form of transdermal drug delivery. It is a combination of emulsion and gel in a definite ratio. Emulsions are incorporated into the gel with proper mixing. The emulsion present in emulgel can be either oil/water or water/oil, which is thickened by mixing it with a gelling agent. MATERIALS AND METHODS: On the basis of the solubility of lornoxicam in various oils, a surfactant and a co-surfactant were selected for further research. For the preparation of emulgel, the emulsion was prepared with Smix (surfactant and co-surfactant) in a ratio of 1:2. The prepared emulsion was incorporated into different concentrations of carbapol 934 in a 1:1 ratio to make a homogenous emulgel. RESULTS: The emulgel was inspected visually to see if it had any phase behaviour, spreadability, or grittiness by applying it to a slide. All formulations were evaluated for pH, physical properties, drug content, spreadability, extrudability, swelling index, viscosity, and centrifugation. Franz diffusion cell was used to perform release of formulation with the help of egg membrane. Among all formulations, F3 showed 83% release after 6 hours and showed acceptable physical properties like homogeneity, colour, consistency, pH value, spreadability, extrudability, and drug content. DISCUSSION: Thus, emulgel can be regarded as a more feasible drug delivery system for hydrophobic drugs (lornoxicam) than the currently marketed formulation. Optimized emulgel formulation consists of a microemulsion of lornoxicam, 1% of carbopol 934, propylene glycol, sodium benzoate, lemon grass oil, glycerin, and distilled water. In the release studies, pH 7.4 phosphate buffer emulgel formulation (F3) showed 83% after 6 hours. Emulgel was found to be stable under stable conditions. CONCLUSION: The emulgel of the poorly water-soluble drug (lornoxicam) was formulated. The components and their optimum ratio for the formulation of microemulsion were obtained by solubility studies and droplet size analysis. Thus, microemulsion can be regarded as a more feasible dose delivery system for lornoxicam than the currently marketed tablet, capsule, and injection formulations. Optimized microemulsion of lornoxicam was incorporated into the gel base. Therefore, it may be concluded that emulgel of lornoxicam can be used as a controlledrelease dosage form of the drug for local application in rheumatoid arthritis.
Evaluation of Spirooxindole-3,3'-pyrrolines-incorporating Isoquinoline Motif as Antitumor, Anti-inflammatory, Antibacterial, Antifungal, and Antioxidant Agents.
Jaber AM, Zahra JA, El-Abadelah MM … +4 more , Al-Mahadeen MM, Sabri SS, Kasabri V, Haddadin RN
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 39069700 · Publisher ↗
BACKGROUND: A series of novel 2-(isoquinolin-1-yl)-spiro[oxindole-3,3'-pyrrolines] were synthesized by a one-pot three-component reaction involving dimethyl acetylenedicarboxylate, 3-phenylimidazo[5,1-a]isoquinoline and...
BACKGROUND: A series of novel 2-(isoquinolin-1-yl)-spiro[oxindole-3,3'-pyrrolines] were synthesized by a one-pot three-component reaction involving dimethyl acetylenedicarboxylate, 3-phenylimidazo[5,1-a]isoquinoline and N-alkylisatins in chloroform at ∼60°C for 24 h. AIMS: This study aimed at the synthesis of novel spirooxindole-3,3'-pyrrolines derivatives and in vitro evaluation of cytotoxicity affinities in cross-correlations with their anti-inflammation and radical scavenging capacities. OBJECTIVES: The objective of this study was to use a one-pot, three-component reaction to synthesize a novel set of spirooxindole-3,3'-pyrrolines derivatives. METHODS: A novel set of spirooxindole-3,3'-pyrrolines (8a-i) was synthesized by a one-pot three-component reaction involving dimethyl acetylenedicarboxylate, 3-phenylimidazo[5,1- a]isoquinoline and N-alkylisatins in chloroform at ∼60°C for 24 h. These new compounds were characterized by HNMR, C-NMR, and HRMS spectral data and screened for their antitumor, anti-inflammatory, antibacterial, antifungal, and antioxidant activities. RESULTS: The new synthetic spirooxindole-3,3'-pyrrolines (8a-i)-tested compounds displayed significant anti-inflammatory properties and were noncytotoxic on PDL fibroblasts. However, they lacked antioxidative-DPPH radical scavenging capabilities. Notably, Doxorubicin and cisplatin demonstrated antiproliferative effects on various cancer monolayers. Moreover, compounds 8b, 8d, 8f, 8h, and 8i exhibited pronounced viability reduction properties in colorectal and pancreatic cancer monolayers, as well as across skin, lung, prostate, and cervical adenocarcinomas, with higher cytotoxicity in mammary cancer cells MCF7 and T47D. None of the tested compounds had significant antibacterial activity against or . However, compounds 8c, 8d, and 8f exhibited notable antifungal properties, indicating potential for further investigation. CONCLUSION: Eight new synthetic spiro[indoline-3,3-pyrroles] were prepared, characterized, and evaluated for their anti-inflammatory and cytotoxic properties. The compounds showed significant anti-inflammatory effects and promising cytotoxicity against various cancer monolayers, especially in colorectal and pancreatic cancers. Some compounds also exhibited antifungal properties. However, they did not exhibit significant antibacterial activity.
Potential of Natural Products as Therapeutic Agents for Inflammatory Diseases.
Aundhia C, Parmar G, Talele C … +3 more , Sadhu P, Sen AK, Rana P
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38984571 · Publisher ↗
Inflammation is a complex biological response that plays a pivotal role in various pathological conditions, including inflammatory diseases. The search for effective therapeutic agents has led researchers to explore natu...
Inflammation is a complex biological response that plays a pivotal role in various pathological conditions, including inflammatory diseases. The search for effective therapeutic agents has led researchers to explore natural products due to their diverse chemical composition and potential therapeutic benefits. This review comprehensively examines the current state of research on natural products as potential therapeutic agents for inflammatory diseases. The article discusses the antiinflammatory properties of various natural compounds, their mechanisms of action, and their potential applications in managing inflammatory disorders. Additionally, formulation and delivery systems, challenges and future prospects in this field are also highlighted.
Novel Dual COX-2/5-LOX Inhibitory Activity by Chalcone Derivatives: A Safe and Efficacious Anti-inflammatory Agent.
Mittal R, Sharma S, Mittal A … +1 more , Kushwah AS
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38939991 · Publisher ↗
BACKGROUND: Non-communicable diseases are chronic systemic inflammation in humans that occurs because of enhanced inflammatory mediators of the arachidonic acid cascade. We aimed to explore whether the lead chalcone comp...
BACKGROUND: Non-communicable diseases are chronic systemic inflammation in humans that occurs because of enhanced inflammatory mediators of the arachidonic acid cascade. We aimed to explore whether the lead chalcone compounds could exhibit anti-inflammatory activity via dual blockage of COX-2/5-LOX enzymes and their regulatory mechanism. METHODS: RAW 264.7 macrophages were collected from NCC, Pune, for in-vitro experiments. The IC values of chalcone compounds C45 and C64 were calculated. RAW 264.7 macrophages were treated with C45 and C64 (10%, 5%, 2.5%, 0.125%, and 0.0625% concentration). The cell viability was carried out with an MTT assay. The COX-1, COX-2, 5-LOX, PGE2, and LTB4 levels were detected by ELISA-based kits. The in-vivo evaluation was carried out in Male Wistar rats (250-300 g, 7-8 weeks old) with acute and chronic anti-inflammatory models and histopathological studies on the stomach, liver, and kidney. RESULTS: The present study described the in-vitro and in-vivo biological evaluation of dual COX-2/5-LOX inhibitors in chalcone derivatives (C45 and C64) compounds showed the most effective COX-2 and 5-LOX inhibition with IC50 values 0.092 and 0.136 μM respectively. Simultaneously, compound C64 showed comparable selectivity towards COX-2 with a Selectivity Index (SI) of 68.43 compared to etoricoxib, with an SI of 89.32. In-vivo carrageenaninduced rat paw oedema activity, the compound C64 showed a significant reduction in oedema with 78.28% compared to indomethacin with 88.07% inhibition. Furthermore, cotton pelletinduced granuloma activity revealed that compound C64 significantly reduced 32.85% compared with standard 40.13% granuloma inhibition. CONCLUSION: The chalcone compound C64, (E)-1-(4-Amino-2-hydroxyphenyl)-3-(3,4,5-trimethoxyphenyl)- prop-2-en-1-one was proved to be a potent and novel Dual COX-2/5-LOX inhibitor with improved gastric safety profiling.
Pyrazoles as Anti-inflammatory and Analgesic Agents: and Studies.
Chahal G, Monga J, Rani I … +4 more , Saini S, Devgun M, Husain A, Lal Khokra S
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38828869 · Publisher ↗
BACKGROUND: Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There a...
BACKGROUND: Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There are well-known marketed drugs having pyrazole moiety as celecoxib, and lonazolac as COX-II inhibitors. AIMS: We aim to synthesize better anti-inflammatory than existing ones. Thiophene is also known for its analgesic and anti-inflammatory action. Thus, the fusion of both gives better anti-inflammatory agents. In the present studies, derivatives from two series of pyrazole were prepared by reacting substituted chalcone (3a-3f) derivatives prepared from 2-acetyl thiophene. They substituted aromatic aldehydes with phenyl hydrazine to form (5a-5f) and with 2, 4-dinitro phenyl hydrazine giving compounds (6a-6f) separately. METHODS: Purified and characterized pyrazoles have been analyzed for analgesic and anti-inflammatory activities by using standard methods. Compounds 5e, 5f, and 6d were proved to be potent analgesics and series (5a-5f) was found to have anti-inflammatory action, which was further validated using docking and ADME studies. RESULTS: The ADME profile of synthesized compounds was found to be satisfactory. CONCLUSION: The synthesized compounds can serve as lead for further drug designing.
Flavonoids as Potential Natural Compounds for the Prevention and Treatment of Eczema.
Khan J, Yadav S, Bhardwaj D … +2 more , Kumar A, Okanlawon MU
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38721791 · Publisher ↗
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 t...
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.
Decades Long Involvement of THP-1 Cells as a Model for Macrophage Research: A Comprehensive Review.
Sharma P, Venkatachalam K, Binesh A
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38676532 · Publisher ↗
Over the years, researchers have endeavored to identify dependable and reproducible models for examining macrophage behavior under controlled conditions. The THP-1 cell line has become a significant and widely employed...
Over the years, researchers have endeavored to identify dependable and reproducible models for examining macrophage behavior under controlled conditions. The THP-1 cell line has become a significant and widely employed tool in macrophage research within these models. Originating from the peripheral blood of individuals with acute monocytic leukemia, this human monocytic cell line can undergo transformation into macrophage-like cells, closely mirroring primary human macrophages when exposed to stimulants. Macrophages play a vital role in the innate immune system, actively regulating inflammation, responding to infections, and maintaining tissue homeostasis. A comprehensive understanding of macrophage biology and function is crucial for gaining insights into immunological responses, tissue healing, and the pathogenesis of diseases such as viral infections, autoimmune disorders, and neoplastic conditions. This review aims to thoroughly evaluate and emphasize the extensive history of THP-1 cells as a model for macrophage research. Additionally, it will delve into the significance of THP-1 cells in advancing our comprehension of macrophage biology and their invaluable contributions to diverse scientific domains.
Immunoregulatory Effects of the Active Form of Vitamin D (Calcitriol), Individually and in Combination with Curcumin, on Peripheral Blood Mononuclear Cells (PBMCs) of Multiple Sclerosis (MS) Patients.
Fasihi M, Samimi-Badabi M, Robat-Jazi B … +6 more , Bitarafan S, Moghadasi AN, Mansouri F, Yekaninejad MS, Izad M, Saboor-Yaraghi AA
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38566376 · Publisher ↗
OBJECTIVES: Multiple sclerosis (MS) is a chronic autoimmune inflammatory disease affecting the central nervous system. Immune cell subsets, notably T helper (Th) 17 and Th1, exert important roles in MS pathogenesis. Wher...
OBJECTIVES: Multiple sclerosis (MS) is a chronic autoimmune inflammatory disease affecting the central nervous system. Immune cell subsets, notably T helper (Th) 17 and Th1, exert important roles in MS pathogenesis. Whereas, Treg cells modulate the disease process. Calcitriol, the active form of vitamin D, and curcumin, a bioactive compound derived from turmeric, play immunomodulatory effects relevant to autoimmune disorders, including MS. The objective of this study is to investigate the effects of calcitriol and Curcumin on Peripheral blood mononuclear cells (PBMCs) of individuals with MS. METHODS: PBMCs from twenty MS patients were isolated, cultured, and exposed to 0.004 μg/mL of calcitriol and 10 μg/mL of curcumin. The cells underwent treatment with singular or combined doses of these components to assess potential cumulative or synergistic immunomodulatory effects. Following treatment, the expression levels of genes and the cellular population of Treg, Th1 and Th17 were evaluated using Real-time PCR and flow cytometry. RESULTS: Treatment with curcumin and calcitriol led to a significant reduction in the expression levels of inflammatory cytokines and transcription factors related to Th1 and Th17 cells, including , and . Furthermore, the frequency of these cells decreased following treatment. Additionally, curcumin and calcitriol treatment resulted in a significant upregulation of the FOXP3 gene expression and an increase in the frequency of Treg cells. CONCLUSION: This study demonstrates that curcumin and calcitriol can effectively modulate the inflammatory processes intrinsic to MS by mitigating the expression of inflammatory cytokines by Th1 and Th17 cells while concurrently enhancing the regulatory role of Treg cells. Moreover, the combined treatment of curcumin and calcitriol did not yield superior outcomes compared to single-dosing strategies.
Development and Evaluation of Celecoxib Emulgel by Using Natural Oil.
Rajput A, Gaur R, Kulshreshtha M … +2 more , Jadaun SS, Kumari V
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38409718 · Publisher ↗
BACKGROUND: Emulgel combines the qualities of an emulsion with those of a gel. In order to create an emulgel w/o or o/w, emulsions have to be formulated, which are then combined with a gelling agent, resulting in a dual-...
BACKGROUND: Emulgel combines the qualities of an emulsion with those of a gel. In order to create an emulgel w/o or o/w, emulsions have to be formulated, which are then combined with a gelling agent, resulting in a dual-control drug release. Celecoxib exhibits analgesic, antipyretic and anti-inflammatory activities and is used to treat osteoarthritis, severe pain, rheumatoid arthritis, and other medical conditions. METHODS: Celecoxib Emulgel was developed and evaluated by using natural oil and carbopol- 940 as a gelling agent in different concentrations. The screening of various oils, co-surfactants and surfactants was performed to determine the solubility. The essential oils (eucalyptus oil and turpentine oil) were used as penetration modifiers. Studies on compatibility with polymers have been conducted, and the results indicate that there should be no physical or chemical interactions between the polymers and the drug substance. For the preparation of emulgel, various emulsions were prepared with Smix (cosurfactant and surfactant) ratios (1:1, 2:1 and 3:1). The selection of a gelling agent was done by incorporating the selected emulsion system ratio of 1:1 with the combinations of polymers carbapol 940, carbapol 934, and HPMC (0:1:0, 0:0.5:1, 0:0:3, 0.5:0:1, 1:0:0) gel base to make a homogenous emulgel. RESULTS: The emulgel was examined visually to see if it had any phase behaviour, feel, spreadability, and grittiness by applying its thin layer to a slide. Then, all six formulations of emulgel were prepared with the selected gelling agent. All emulgels were evaluated for pH, physical properties (consistency, homogeneity, colour, texture), drug content, spreadability, extrudability, swelling index, viscosity, stability and centrifugation. A Franz diffusion cell and an egg membrane were used to perform drug release. CONCLUSION: Among all prepared formulations, EG1 had a better release, higher viscosity, higher drug content, and a higher swelling index than the others. The formulation EG1 showed higher drug release (91.25%) within 8 hours.
Analgesic and Anti-inflammatory Potential of the New Tetrahydropyran Derivative (2s,6s)-6-ethyl-tetrahydro-2h-pyran-2-yl) Methanol.
Castro GNS, de Souza RDN, da Silva ACM … +5 more , Laureano-Melo R, da Silva Côrtes W, Capim SL, de Almeida Vasconcellos MLA, Marinho BG
Antiinflamm Antiallergy Agents Med Chem · 2024 · PMID 38409717 · Publisher ↗
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...
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.
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