{"title":"Molecular Docking, Pharmacophore Modeling and ADMET Prediction of Novel Heterocyclic Leads as Glucokinase Activators.","authors":"Anuradha Mehra, Amit Mittal, Shivangi Singh","doi":"10.2174/0118715230325278240821053346","DOIUrl":"10.2174/0118715230325278240821053346","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Objectives: </strong>To address type 2 diabetes, as well as minimize unwanted side effects, this research endeavor aimed to develop activators of glucokinase.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>In recent studies, lead molecules that possess enhanced pharmacokinetic profiles, increased binding affinity, and lower toxicity were developed to act as glucokinase activators.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"57-74"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142335936","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}
Mohammed M Al-Mahadeen, Areej M Jaber, Jalal A Zahra, Belal O Al-Najjar, Mustafa M El-Abadelah, Monther A Khanfar
{"title":"Discovery and Chemical Exploration of Spiro[Benzofuran-3,3'-Pyrroles] Derivatives as Innovative FLT3 Inhibitors for Targeting Acute Myeloid Leukemia.","authors":"Mohammed M Al-Mahadeen, Areej M Jaber, Jalal A Zahra, Belal O Al-Najjar, Mustafa M El-Abadelah, Monther A Khanfar","doi":"10.2174/0118715230343474241009112335","DOIUrl":"10.2174/0118715230343474241009112335","url":null,"abstract":"<p><strong>Aims: </strong>This study aimed at the synthesis of several spiro[benzofuran-3,3'-pyrroles] derivatives by a three-component reaction conducted by mixing DMAD, <i>N</i>-bridgehead heterocycles, and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. Moreover, <i>in vitro</i> evaluation of their cytotoxicity affinities against FMS-like tyrosine kinase 3 was carried out.</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 spiro[benzofuran-3,3'-pyrroles] derivatives.</p><p><strong>Methods: </strong>A novel set of spiro[benzofuran-3,3'-pyrroles] ((11-13)a-e) was synthesized by a one-pot three-component reaction involving dimethyl acetylenedicarboxylate, <i>N</i>-bridgehead heterocycles and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. The compounds were analyzed using NMR <sup>1</sup>H, <sup>13</sup>C, 2D-NMR (COSY, HMQC, HMBC), and HRMS. Docking simulations were conducted to elucidate the anticancer activity of synthesized compounds on FLT3 protein, with Gilteritinib as a reference for comparison.</p><p><strong>Results: </strong>This study demonstrated the successful design, synthesis, and biological evaluation of spiro[benzofuran-3,3'-pyrroles] derivatives as FLT3 inhibitors for AML treatment. The synthesized compounds demonstrated promising binding affinities and significant inhibitory activity against FLT3 kinase. The inhibitors (11a, 11b, 11c, 12d, and 12e) exhibited excellent selectivity profiles against FLT3. Particularly, compound 12e showed strong binding affinity and potent inhibitory activity (IC<sub>50</sub> = 2.5 μM).</p><p><strong>Conclusion: </strong>Fifteen new synthetic spiro[benzofuran-3,3'-pyrroles] were prepared, characterized, and evaluated for cytotoxicity affinities against FMS-like tyrosine kinase 3. Compound 12e showed strong binding affinity and potent inhibitory activity (IC<sub>50</sub> = 2.5 μM), making it a promising candidate for further development as a therapeutic option for AML treatment. These findings lay the groundwork for further optimization and development of spiro[benzofuran-3,3'-pyrroles] derivatives as potential therapeutics for AML treatment. Further studies are needed to explore their efficacy and safety profiles in preclinical and clinical settings.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"127-138"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142796772","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}
{"title":"<i>In-vitro</i> Antioxidant and <i>In-vivo</i> Analgesics and Anti-inflammatory Activity of <i>Allamanda blanchetii</i> Leaf Extract in Rats.","authors":"Achla Vyas, Revathi Gupta, Rakesh Jatav","doi":"10.2174/0118715230340178241008163943","DOIUrl":"10.2174/0118715230340178241008163943","url":null,"abstract":"<p><strong>Objectives: </strong>This study assessed the In-vitro Antioxidant and In-vivo Analgesics and Anti-inflammatory Activity of <i>Allamanda blanchetii</i> Leaf Extract in Rats.</p><p><strong>Introduction: </strong>Diverse pharmacological applications of plants from the Apocynaceae family are reported in the literature. <i>Allamanda blanchetii</i>; an ornamental species belonging to the Apocynaceae family, is characterized by diverse biological activities, i.e. antioxidant, cytotoxic, thrombolytic, membrane-stabilizing, antimicrobial, and anti-proliferative effects. This species represents a perennial flora that thrives in tropical and subtropical climates.</p><p><strong>Materials and methods: </strong>Ultrasonication-assisted method used for plant extraction. The extracts were subjected to phytochemical screening tests, followed by total phenolic content analysis, using gallic acid as a standard. The antioxidant activity was examined by DPPH scavenging and FRAP assays. The acetic acid-induced writhing test, tail flick, and Hot plate method were used for the determination of analgesic activity. Anti-inflammatory activity by following carrageenan-induced paw edema.</p><p><strong>Results: </strong>ABLE treatments show analgesic effectiveness against the acid-induced pain source, tail flick, and hot plate methods at different doses of ABLE 400,200,100 mg/kg results showed respectively- 55.32, 38.67, and 22.85 (% inhibition), 89.47%, 62.57 %, 49.57%, and 100%, 92.40%, 65.33% response after 180 min of drug administration. ABLE 400 and 200 mg/kg exhibit effective results (1.43± 0.005 and 1.50± 0.008) against carrageenan- induced intoxication.</p><p><strong>Discussion: </strong>The fundamental components of antioxidants that can aid in the reduction of free radicals include phenol, flavonoids, and polyphenols. Applying DPPH and FRAP, ABLE exhibits remarkable antioxidant activity. When it comes to both centrally and peripherally acting analgesics, ABLE exhibits highly effective activity. Methanolic ABLE had a noticeable impact on paw edema caused by carrageenan. Antioxidants, alkaloids, and glycosides were present in methanolic ABLE, which allowed it to efficiently combat inflammatory mediators and the cause of pain.</p><p><strong>Conclusion: </strong>Ultrasonic assistance is beneficial in isolating active metabolites in plants, with phenolic compounds exhibiting antioxidant activity. ABLE, a plant with 55% squalene, effectively combats inflammatory mediators and pain. Further investigation is needed to identify biomarkers in the plant.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"114-126"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142840726","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}
Dionisia P Ferreira, Fabrício H Holanda, Swanny F Borges, Ryan da S Ramos, Victoria Mae T Shinkai, Gisele C De Souza, José Carlos T Carvalho, Raphael S Pimenta, José Luiz M Do Nascimento, Irlon M Ferreira
{"title":"Toxicity and anti-inflammatory effects of Eleutherine bulbosa (Miller) Urb, ethanolic extract, in zebrafish (Danio rerio).","authors":"Dionisia P Ferreira, Fabrício H Holanda, Swanny F Borges, Ryan da S Ramos, Victoria Mae T Shinkai, Gisele C De Souza, José Carlos T Carvalho, Raphael S Pimenta, José Luiz M Do Nascimento, Irlon M Ferreira","doi":"10.2174/0118715230352701241130053455","DOIUrl":"https://doi.org/10.2174/0118715230352701241130053455","url":null,"abstract":"<p><strong>Introduction: </strong>Eleutherine bulbosa (Miller) Urb, popularly known as \"marupa-zinho\", is frequently used in traditional medicine for treating various diseases, including hypertension, ulcers, constipation, and intestinal infection. However, there is little scientific knowledge available regarding the pharmacological effects of this species. Thus in vivo and in silico phytochemical studies are required to establish whether this plant has these effects. Further tests were necessary to evaluate the pharmacological activity of the compounds found in this plant, and demonstrate results related to the anti-inflammatory process, which will serve as the basis for future research in this area.</p><p><strong>Methods: </strong>Therefore, our study aimed to determine the acute toxicity levels of the hexanoic fraction of the ethanolic extract of Eleutherine bulbosa (referred to as ExtHF) using adult zebrafish, with the determination of the LD50, behavioral and histopathological evaluations, as well as the anti-inflammatory potential of ExtHF, at different doses, in abdominal edema induced by carrageenan. The acute toxicity study and histopathological analysis in zebrafish showed that ExtHF has a high toxic potential, with an LD50 of 346.74 mg/kg. However, ExtHF showed an anti-inflammatory effect by inhibiting abdominal edema at all doses tested.</p><p><strong>Results: </strong>The inhibition rate of 66.2% and 62.4%, respectively, was observed with the 2.5 mg/kg dose, respectively, indicating that ExtHF is safe in terms of acute toxicity based on behavioral changes, mortality rate, and histopathological examination. Therefore, ExtHF has an acceptable level of safety for acute toxicity, defined by the analysis of behavioral changes, mortality, and histopathology, showing a significant anti-inflammatory effect in zebrafish at all doses, showing that ExtHF was very efficient in preventing the formation of edema, in addition, it was also revealed that ExtHF has a great effect in reversing the edema which is already installed.</p><p><strong>Conclusion: </strong>Molecular docking studies revealed that the eleutherol molecule isolated from E. bulbosa has a dual inhibition profile against cyclooxygenase-1 and 2.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142934153","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}
Mahdieh Fasihi, Mahsa Samimi-Badabi, Behrouz Robat-Jazi, S. Bitarafan, A. Moghadasi, Fatemeh Mansouri, Mir Saeed Yekaninejad, M. Izad, A. Saboor-Yaraghi
{"title":"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.","authors":"Mahdieh Fasihi, Mahsa Samimi-Badabi, Behrouz Robat-Jazi, S. Bitarafan, A. Moghadasi, Fatemeh Mansouri, Mir Saeed Yekaninejad, M. Izad, A. Saboor-Yaraghi","doi":"10.2174/0118715230293847240314073359","DOIUrl":"https://doi.org/10.2174/0118715230293847240314073359","url":null,"abstract":"OBJECTIVES\u0000Multiple 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.\u0000\u0000\u0000METHODS\u0000PBMCs 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 immunomod-ulatory 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.\u0000\u0000\u0000RESULTS\u0000Treatment 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, includ-ing IFN-γ, T-bet, IL-17, and RORC. Furthermore, the frequency of these cells decreased follow-ing treatment. Additionally, curcumin and calcitriol treatment resulted in a significant upregu-lation of the FOXP3 gene expression and an increase in the frequency of Treg cells.\u0000\u0000\u0000CONCLUSION\u0000This 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.","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"195 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140768821","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}
Syed A Abbas, Abdullah Khan, Mehraj Fatima, Anandarajagopal Kalusalingam, Mahibub M Kanakal, Shiva K Inamdar, Vijay Kotra, Long C Ming, Ashok K M Dastapur, Tazneem Bachi
{"title":"Gas Chromatography-Mass Spectrometry (GC-MS) Analysis of <i>Scaphium Affine</i> Seed Extract and Assessment of Its Anti-hemorrhoidal Efficacy.","authors":"Syed A Abbas, Abdullah Khan, Mehraj Fatima, Anandarajagopal Kalusalingam, Mahibub M Kanakal, Shiva K Inamdar, Vijay Kotra, Long C Ming, Ashok K M Dastapur, Tazneem Bachi","doi":"10.2174/0118715230285370240131111539","DOIUrl":"10.2174/0118715230285370240131111539","url":null,"abstract":"<p><strong>Background: </strong>Seeds of plant <i>Scaphium affine</i> are traditionally used by the healers of \"India\" for the treatment of piles.</p><p><strong>Objectives: </strong>The primary objective of the study was to assess the anti-hemorrhoidal potential of the ethanolic seed extract of <i>Scaphium affine</i>.</p><p><strong>Methods: </strong>After the soxhlet extraction method, the seed extract from<i> Scaphium affine</i> was first submitted to phytochemical standardization and then GC-MS analysis. Rats were given Croton oil and Jatropha oil to develop hemorrhoids, and <i>Scaphium affine</i> seed extract (ESA) was administered orally for 5 days and 3 days, respectively, at doses of 1000 and 500 mg/kg. The Rectoanal coefficient (RAC) was calculated as an inflammatory marker. The hemorrhoidal tissues were also subjected to cytokine profiling, biochemical estimation and histopathology.</p><p><strong>Results: </strong>ESA demonstrated the presence of flavonoids, saponins, phytosterols, phenols, and tannins. GCMS analysis elucidated the presence of hexadecanoic acid 2 hydroxy -1,3 propane diyl ester,9 Octadecanoic acid ethyl ester, Cyclohexane 1,4 di methyl cis, Farnesol isomer,1, E-11, Z-13 octa decatriene, Stigmasterol, N-(5 ethyl -1,3,4-thiadiazol-yl) benzamide, N, N Dinitro 1,3,5,7 tetraza bicyclo 93,3,1) as major phytoconstituents. The results depicted more potent anti-hemorrhoidal activity of ESA at 1000 mg/kg, p.o., which was evident through a decrease in RAC. A significant decline in the levels of IL-1β, IL-6, and TNF-α expression was observed, along with the restoration of altered antioxidants and enzymes. Histopathological analysis confirmed the tissue recovery as it revealed minimal inflammation and decreased dilated blood vessels in treated animals.</p><p><strong>Conclusion: </strong>Based on the results it can be concluded that seeds of <i>Scaphium affine</i> showed significant anti-hemorrhoid agents which may be attributed to their anti-inflammatory and anti-oxidant potential due to the presence of certain phytoconstituents in it. The study also supports the traditional use of seeds of <i>Scaphium affine</i> for the first time in the treatment of hemorrhoids.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"118-128"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139736987","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}
Arun K Mishra, Kamal Y Thajudeen, Mhaveer Singh, Gulam Rasool, Arvind Kumar, Harpreet Singh, Kalicharan Sharma, Amrita Mishra
{"title":"<i>In-silico</i> based Designing of benzo<i>[d]</i>thiazol-2-amine Derivatives as Analgesic and Anti-inflammatory Agents.","authors":"Arun K Mishra, Kamal Y Thajudeen, Mhaveer Singh, Gulam Rasool, Arvind Kumar, Harpreet Singh, Kalicharan Sharma, Amrita Mishra","doi":"10.2174/0118715230296273240725065839","DOIUrl":"10.2174/0118715230296273240725065839","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Aims: </strong>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.</p><p><strong>Materials and methods: </strong>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.</p><p><strong>Results: </strong>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. <i>In vitro</i> evaluation of the COX-1 and COX-2 enzyme inhibitory activities was performed for synthesized compounds.</p><p><strong>Discussion: </strong>Compounds G10 and G11 exhibited significant COX-1 and COX-2 enzyme inhibitory action with an IC<sub>50</sub> 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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"230-260"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142006215","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}
{"title":"Corrigendum to: Anti- SARS-CoV-2 IgG and IgM Levels in Iraqi General Population.","authors":"Amina Hamed Alobaidi, Hussein Inam Mustafa, Ahmed Mutar Salih, Abdulghani Mohamed Alsamarai","doi":"10.2174/1871523023999240522153411","DOIUrl":"https://doi.org/10.2174/1871523023999240522153411","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"23 2","pages":"148"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142006216","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}
Gajala Deethamvali Ghouse Peer, Anjali Priyadarshini, Archana Gupta, Arpana Vibhuti, Vethakkani Samuel Raj, Chung-Ming Chang, Ramendra Pati Pandey
{"title":"Exploration of Antileishmanial Compounds Derived from Natural Sources.","authors":"Gajala Deethamvali Ghouse Peer, Anjali Priyadarshini, Archana Gupta, Arpana Vibhuti, Vethakkani Samuel Raj, Chung-Ming Chang, Ramendra Pati Pandey","doi":"10.2174/0118715230270724231214112636","DOIUrl":"10.2174/0118715230270724231214112636","url":null,"abstract":"<p><strong>Aims: </strong>Leishmaniasis is a deadly tropical disease that is neglected in many countries. World Health Organization, along with a few other countries, has been working together to protect against these parasites. Many novel drugs from the past few years have been discovered and subjected against leishmaniasis, which have been effective but they are quite expensive for lower-class people. Some drugs showed no effect on the patients, and the longer use of these medicines has made resistance against these deadly parasites. Researchers have been working for better medication by using natural products from medicinal plants (oils, secondary metabolites, plant extracts) and other alternatives to find active compounds as an alternative to the current synthetic drugs.</p><p><strong>Materials and methods: </strong>To find more potential natural products to treat Leishmania spp, a study has been conducted and reported many plant metabolites and other natural alternatives from plants and their extracts. Selected research papers with few term words such as natural products, plant metabolites, Leishmaniasis, <i>in vivo</i>, <i>in vitro</i>, and treatment against leishmaniasis; in the Google Scholar, PubMed, and Science Direct databases with selected research papers published between 2015 and 2021 have been chosen for further analysis has been included in this report which has examined either <i>in vivo</i> or <i>in vitro</i> analysis.</p><p><strong>Results: </strong>This paper reported more than 20 novel natural compounds in 20 research papers that have been identified which report a leishmanicidal activity and shows an action against promastigote, axenic, and intracellular amastigote forms.</p><p><strong>Conclusion: </strong>Medicinal plants, along with a few plant parts and extracts, have been reported as a possible novel anti-leishmanial medication. These medicinal plants are considered nontoxic to Host cells. Leishmaniasis treatments will draw on the isolated compounds as a source further and these compounds compete with those already offered in clinics.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"1-13"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139567424","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}
Nadim Siddique, Akash Ved, Karuna Shanker Shukla, Amit Kumar Nigam
{"title":"Standardization and Pharmacological Evaluation of <i>Ziziphus mauritiana</i> Extract for Sedative and Anticonvulsant Activity in Mice and Rat.","authors":"Nadim Siddique, Akash Ved, Karuna Shanker Shukla, Amit Kumar Nigam","doi":"10.2174/0118715230276586231215045816","DOIUrl":"10.2174/0118715230276586231215045816","url":null,"abstract":"<p><strong>Introduction: </strong><i>Ziziphus mauritiana</i>, sometimes called Indian jujube or Ber, belongs to the Rhamnaceae group of plants. The aqueous and ethanolic Ziziphus mauritiana formulations were shown to have analgesic, antipyretic, potent analgesic, anti-inflammatory, and anti-emetic properties.</p><p><strong>Aims & objectives: </strong>The aim of this study is to investigate the sedative and anticonvulsant activities of <i>Ziziphus mauritiana</i> extract by governing 200 and 400 mg/kg body weight orally.</p><p><strong>Materials and methods: </strong>The leaves are extracted with ethanol and lukewarm water with a soxhlet apparatus for 72 hours. After that acute extract toxicity study was performed and then locomotor activity, pentobarbital induced sleeping time and anticonvulsant activity were performed with the extract.</p><p><strong>Results: </strong>Oral administration of extract at dosages of 200 & 400 mg/kg was employed after an immediate toxicity test. At a dosage of 400 mg/kg, the number of locomotions was reduced significantly lengthened the period of time spent sleeping and there was showed a dosage-dependent reduction in all phases of an epileptic episode.</p><p><strong>Conclusion: </strong>In this study, the extract reduced locomotor activity, however, it had a superior profile for an antiepileptic action than phenytoin since it decreased locomotor activity to a lesser level. The considerable increase in pentobarbitone sleep hours with the extracts at a higher dose supported the sedative action of <i>Z. mauritiana</i>.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"31-38"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139567426","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}