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

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In-vitro and In Silico Assessment of Anti-inflammation Properties of Saponarin Extracted from Hordeum Vulgare. 从大麦中提取的皂苷抗炎特性的体外和体内评估
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230284334240101100450
Revathi Boyina, Sreya Kosanam, Sasidhar Bhimana, Raveendra Babu Gudimitla, Dhachinamoorthi Duraiswamy
{"title":"<i>In-vitro</i> and <i>In Silico</i> Assessment of Anti-inflammation Properties of Saponarin Extracted from Hordeum Vulgare.","authors":"Revathi Boyina, Sreya Kosanam, Sasidhar Bhimana, Raveendra Babu Gudimitla, Dhachinamoorthi Duraiswamy","doi":"10.2174/0118715230284334240101100450","DOIUrl":"10.2174/0118715230284334240101100450","url":null,"abstract":"<p><strong>Background: </strong>Hordeum vulgare, commonly known as Barley grass, is a historically significant cultivated plant with profound implications for societies, agricultural sciences, and human nutrition. It has been valued for both sustenance and its potential medicinal properties.</p><p><strong>Objectives: </strong>This study aims to comprehensively investigate the medicinal properties of Hordeum vulgare, focusing on its potential therapeutic benefits and anti-inflammatory properties. Additionally, we seek to quantify and compare the phytochemical content of two distinct extracts: Barley Grass Hexane Extract (BGHE) and Barley grass aqueous extract (BGAQ).</p><p><strong>Methods: </strong>We quantified the phytochemical contents of BGHE and BGAQ and evaluated their anti-inflammatory effects using UV spectroscopy at 560 nm, coupled with the RBC membrane stabilization technique. Subsequently, we conducted <i>in silico</i> studies to assess the <i>in vitro</i> anti-inflammatory potential of Barley grass leaf extracts.</p><p><strong>Results: </strong>Both BGHE and BGAQ demonstrated significant inhibitory effects on inflammation compared to the control group. However, BGHE exhibited superior anti-inflammatory efficacy when compared to BGAQ, suggesting its role as a potential anti-inflammatory agent. <i>In silico</i> studies further supported the anti-inflammatory potential of Barley grass leaf extracts.</p><p><strong>Conclusion: </strong>Hordeum vulgare, or Barley grass, offers a wealth of health benefits, including anti-inflammatory, anti-diabetic, anti-cancer, antioxidant, anti-acne, and anti-depressant properties. These properties contribute to improved immunity, reduced cardiovascular disorders, and alleviation of fatigue. The distinct extracts, BGHE and BGAQ, both exhibit promising anti-inflammatory capabilities, but BGHE shows better anti-inflammatory activity. This research sheds light on the therapeutic potential of Barley grass, making it a valuable candidate for further exploration in the field of natural medicine.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"14-20"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139521906","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The Influence of Phytoconstituents for the Management of Antipsoriatic Activity in Various Animal Models. 植物成分对各种动物模型抗银屑病活性管理的影响
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230320581240711063558
Ravina Yadav, Tejpal Yadav, Ashutosh Upadhayay, Md Sabir Alam, Gaurav Dubey, Vikram Kumar, Adarsh Sahu
{"title":"The Influence of Phytoconstituents for the Management of Antipsoriatic Activity in Various Animal Models.","authors":"Ravina Yadav, Tejpal Yadav, Ashutosh Upadhayay, Md Sabir Alam, Gaurav Dubey, Vikram Kumar, Adarsh Sahu","doi":"10.2174/0118715230320581240711063558","DOIUrl":"10.2174/0118715230320581240711063558","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"215-229"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141857544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer. 含柠檬草油作为渗透促进剂的洛诺昔康乳胶凝胶的配制与表征
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230289163240703075629
Vibha Kumari, Meenakshi Bajpai
{"title":"Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer.","authors":"Vibha Kumari, Meenakshi Bajpai","doi":"10.2174/0118715230289163240703075629","DOIUrl":"10.2174/0118715230289163240703075629","url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Materials and methods: </strong>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.</p><p><strong>Results: </strong>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 <i>in-vitro</i> 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.</p><p><strong>Discussion: </strong>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 <i>in-vitro</i> release studies, pH 7.4 phosphate buffer emulgel formulation (F3) showed 83% after 6 hours. Emulgel was found to be stable under stable conditions.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"164-173"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141790763","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Pyrazoles as Anti-inflammatory and Analgesic Agents: In-vivo and In-silico Studies. 吡唑作为消炎镇痛剂:体内和微观研究。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230275741231207115011
Geeta Chahal, Jyoti Monga, Isha Rani, Shubham Saini, Manish Devgun, Asif Husain, Sukhbir Lal Khokra
{"title":"Pyrazoles as Anti-inflammatory and Analgesic Agents: <i>In-vivo</i> and <i>In-silico</i> Studies.","authors":"Geeta Chahal, Jyoti Monga, Isha Rani, Shubham Saini, Manish Devgun, Asif Husain, Sukhbir Lal Khokra","doi":"10.2174/0118715230275741231207115011","DOIUrl":"https://doi.org/10.2174/0118715230275741231207115011","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Aims: </strong>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.</p><p><strong>Methods: </strong>Purified and characterized pyrazoles have been analyzed for <i>in-vivo</i> 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.</p><p><strong>Results: </strong>The ADME profile of synthesized compounds was found to be satisfactory.</p><p><strong>Conclusion: </strong>The synthesized compounds can serve as lead for further drug designing.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"23 1","pages":"39-51"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141200815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Dual COX-2/5-LOX Inhibitory Activity by Chalcone Derivatives: A Safe and Efficacious Anti-inflammatory Agent. 查尔酮衍生物的新型 COX-2/5-LOX 双重抑制活性:一种安全有效的抗炎剂
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230301176240605072113
Roopal Mittal, Shailesh Sharma, Amit Mittal, Ajay Singh Kushwah
{"title":"Novel Dual COX-2/5-LOX Inhibitory Activity by Chalcone Derivatives: A Safe and Efficacious Anti-inflammatory Agent.","authors":"Roopal Mittal, Shailesh Sharma, Amit Mittal, Ajay Singh Kushwah","doi":"10.2174/0118715230301176240605072113","DOIUrl":"10.2174/0118715230301176240605072113","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Methods: </strong>RAW 264.7 macrophages were collected from NCC, Pune, for in-vitro experiments. The IC<sub>50</sub> 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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"174-186"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141474367","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Using Quality by Design Tools to Study Gel Formulation from Brassica juncea Leaves and Conducting its In vitro, In vivo, Molecular Docking, and ADMET Analyses. 利用设计质量工具研究甘蓝叶凝胶配方,并进行体外、体内、分子对接和 ADMET 分析。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230309053240718122527
Mahibub Mahamadsa Kanakal, Syed Atif Abbas, Abdullah Khan, Saleha Sultana, Humaira Fatima, Ruheena Tabasssum, Mohammed Gulzar Ahmed, Rokeya Sultana, Jaffer Sadik Mohammed, Roshan Salfi
{"title":"Using Quality by Design Tools to Study Gel Formulation from <i>Brassica juncea</i> Leaves and Conducting its <i>In vitro, In vivo,</i> Molecular Docking, and ADMET Analyses.","authors":"Mahibub Mahamadsa Kanakal, Syed Atif Abbas, Abdullah Khan, Saleha Sultana, Humaira Fatima, Ruheena Tabasssum, Mohammed Gulzar Ahmed, Rokeya Sultana, Jaffer Sadik Mohammed, Roshan Salfi","doi":"10.2174/0118715230309053240718122527","DOIUrl":"10.2174/0118715230309053240718122527","url":null,"abstract":"<p><strong>Introduction: </strong>This research aims to create a gel formulation of Brassica juncea leaf extract and assess its anti-inflammatory properties using an <i>in silico</i> 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.</p><p><strong>Methods: </strong>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 <i>In vitro</i> study of all nine extract suspensions was conducted to determine the drug contents at 276 nm.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"187-204"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141857561","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cinnamic Acid Ameliorates Acetic Acid-induced Inflammatory Response through Inhibition of TLR-4 in Colitis Rat Model. 肉桂酸通过抑制 TLR-4 改善乙酸诱导的大鼠结肠炎模型炎症反应
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230278980231212103709
Zahra Rezaei, Saeideh Momtaz, Pardis Gharazi, Mahban Rahimifard, Maryam Baeeri, Ali Reza Abdollahi, Mohammad Abdollahi, Amirhossein Niknejad, Danial Khayatan, Mohammad Hosein Farzaei, Amir Hossein Abdolghaffari
{"title":"Cinnamic Acid Ameliorates Acetic Acid-induced Inflammatory Response through Inhibition of TLR-4 in Colitis Rat Model.","authors":"Zahra Rezaei, Saeideh Momtaz, Pardis Gharazi, Mahban Rahimifard, Maryam Baeeri, Ali Reza Abdollahi, Mohammad Abdollahi, Amirhossein Niknejad, Danial Khayatan, Mohammad Hosein Farzaei, Amir Hossein Abdolghaffari","doi":"10.2174/0118715230278980231212103709","DOIUrl":"10.2174/0118715230278980231212103709","url":null,"abstract":"<p><strong>Background: </strong>Cinnamic acid, an active compound in cinnamon spp., has anti-inflammatory and antioxidant characteristics and is favorable in managing inflammatory bowel diseases.</p><p><strong>Objectives: </strong>Evaluate cinnamic acid's effects on colitis in rats.</p><p><strong>Methods: </strong>To induce colitis in experimental rats, excluding the sham group, a 4% intrarectal solution of acetic acid was administered. The rats were then given oral doses of cinnamic acid at 30, 45, and 90 mg/kg for two days. The animals were assessed for macroscopic and microscopic changes, and the levels of inflammatory mediators such as tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and myeloperoxidase (MPO) were measured using Eliza kits. Additionally, real-time PCR was performed to examine the gene level of toll-like receptor 4 (TLR-4) in the colon.</p><p><strong>Results: </strong>Effective reduction of inflammation in acetic acid-induced colitis was achieved through Cinnamic acid administration at doses of 45 and 90 mg/kg. The decrease was achieved by inhibiting the activities of TNF-α, IL-6, and MPO while downregulating the expression of TLR-4. It is important to note that macroscopic and microscopic evaluations were significant in determining the effectiveness of cinnamic acid in reducing inflammation.</p><p><strong>Conclusion: </strong>Downregulation of inflammatory cytokines and TLR-4 expression may contribute to cinnamic acid's anti-inflammatory effect.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"21-30"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139743049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of Spirooxindole-3,3'-pyrrolines-incorporating Isoquinoline Motif as Antitumor, Anti-inflammatory, Antibacterial, Antifungal, and Antioxidant Agents. 评估含有异喹啉基团的螺吲哚-3,3'-吡咯烷类抗肿瘤、抗炎、抗菌、抗真菌和抗氧化剂。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230322113240705071750
Areej M Jaber, Jalal A Zahra, Mustafa M El-Abadelah, Mohammed M Al-Mahadeen, Salim S Sabri, Violet Kasabri, Randa N Haddadin
{"title":"Evaluation of Spirooxindole-3,3'-pyrrolines-incorporating Isoquinoline Motif as Antitumor, Anti-inflammatory, Antibacterial, Antifungal, and Antioxidant Agents.","authors":"Areej M Jaber, Jalal A Zahra, Mustafa M El-Abadelah, Mohammed M Al-Mahadeen, Salim S Sabri, Violet Kasabri, Randa N Haddadin","doi":"10.2174/0118715230322113240705071750","DOIUrl":"10.2174/0118715230322113240705071750","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Aims: </strong>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.</p><p><strong>Objectives: </strong>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.</p><p><strong>Methods: </strong>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 <sup>1</sup>HNMR, <sup>13</sup>C-NMR, and HRMS spectral data and screened for their antitumor, anti-inflammatory, antibacterial, antifungal, and antioxidant activities.</p><p><strong>Results: </strong>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 <i>S. aureus</i> or <i>E. coli</i>. However, compounds 8c, 8d, and 8f exhibited notable antifungal properties, indicating potential for further investigation.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"261-272"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141790762","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and Evaluation of Celecoxib Emulgel by Using Natural Oil. 利用天然油脂开发和评估塞来昔布凝胶
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230276597240207070306
Aarti Rajput, Rishabh Gaur, Mayank Kulshreshtha, Sumedha Singh Jadaun, Vibha Kumari
{"title":"Development and Evaluation of Celecoxib Emulgel by Using Natural Oil.","authors":"Aarti Rajput, Rishabh Gaur, Mayank Kulshreshtha, Sumedha Singh Jadaun, Vibha Kumari","doi":"10.2174/0118715230276597240207070306","DOIUrl":"10.2174/0118715230276597240207070306","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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 <i>in-vitro</i> drug release.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"129-137"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139975350","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ferulic Acid: A Review of Mechanisms of Action, Absorption, Toxicology, Application on Wound Healing. 阿魏酸:阿魏酸:作用机制、吸收、毒理学、伤口愈合应用综述。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-01-01 DOI: 10.2174/0118715230309592240723105514
Ana Flávia Lawall Werneck Cerqueira, Humberto de Mello Brandão, Guilherme Diniz Tavares, Mirian Pereira Rodarte
{"title":"Ferulic Acid: A Review of Mechanisms of Action, Absorption, Toxicology, Application on Wound Healing.","authors":"Ana Flávia Lawall Werneck Cerqueira, Humberto de Mello Brandão, Guilherme Diniz Tavares, Mirian Pereira Rodarte","doi":"10.2174/0118715230309592240723105514","DOIUrl":"10.2174/0118715230309592240723105514","url":null,"abstract":"<p><p>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.</p><p><strong>Aims: </strong>This work aims to make a bibliographic survey on studies of the use of ferulic acid in the treatment of wounds.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>Studies in this area are recent and further research is needed to expand the possibilities and therapeutic efficiency of ferulic acid in wound healing.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"205-214"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141899330","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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