Journal of Experimental Pharmacology最新文献

{"title":"Gingerols and Shogaols of <i>Zingiber officinale var. sunti Valeton</i> as Potential Allosteric Agonists of Human GABA_A Receptor by in silico Pharmacology Approach.","authors":"Faisal Kuswandani, Gofarana Wilar, Indah Suasani Wahyuni, Sandra Megantara, Dian Ayu Eka Pitaloka, Jutti Levita, Supat Jiranusornkul","doi":"10.2147/JEP.S524890","DOIUrl":"10.2147/JEP.S524890","url":null,"abstract":"<p><strong>Background: </strong>Gingerols and shogaols are the main active constituents in <i>Zingiber officinale</i> var. <i>sunti</i> Valeton has been reported for its anti-anxiety activity. Anti-anxiety drugs, such as benzodiazepines, alleviate anxiety disorders by enhancing the activity of gamma-aminobutyric acid type A (GABA_A) receptors through positive allosteric regulation at the α1/γ2 interface extracellular domain.</p><p><strong>Purpose: </strong>To elucidate the binding energy and stability of gingerols and shogaols toward human GABA_A receptor (hGABA_AR), compared to their known allosteric agonist (diazepam), and further phytochemical analysis in the ethanol extract of <i>Z. officinale</i> var. <i>sunti</i> Valeton rhizome (EEZO).</p><p><strong>Methods: </strong>The ligands, namely gingerols (6-, 8-, and 10-gingerol) and shogaols (6-, 8-, and 10-shogaol), were evaluated by pre-ADMET screening tools and molecular docking simulation towards hGABA_AR α1/γ2 subtype (PDB ID: 6X3X). Compounds with the best pre-ADMET profile and affinity were subjected to a 200 ns molecular dynamics (MD) simulation. The UPLC analysis was performed to detect and quantify gingerol and shogaol in EEZO.</p><p><strong>Results: </strong>The best pre-ADMET prediction was shown by 6-gingerol, whereas the molecular docking simulations revealed that the best binding affinity and stability were shown by 6-gingerol (-7.41 kcal/mol) and 10-shogaol (-8.24 kcal/mol), which are comparable to that of diazepam. They build hydrogen bonds with α1 Ser206 and pi interaction with γ2 Phe77. The MD simulation confirmed that the stability of the 10-shogaol/hGABA_AR and 6-gingerol/hGABA_AR complexes is equal to that of diazepam/hGABA_AR. The UPLC analysis resulted in a level of 44.98 µg/mL for 6-gingerol and 2.52 µg/mL for 10-shogaol.</p><p><strong>Conclusion: </strong>6-Gingerol and 10-shogaol of EEZO may have the potential to be developed as novel allosteric agonists of human GABA_A receptors, thus explaining their anti-anxiety activity. However, the activity towards the human GABA_A receptor is lower than diazepam, its known allosteric agonist.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"359-374"},"PeriodicalIF":0.0,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12182062/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144475516","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>Etlingera Elatior</i> Inflorescence Extract Mitigates Acute Gastric Ulcers by Suppressing the Expression of Inducible Nitric Oxide Synthase in Ethanol-Induced Wistar Rats.","authors":"Deshanda Kurniawan Prayoga, Diah Lia Aulifa, Arif Budiman, Jutti Levita, Supat Jiranusornkul","doi":"10.2147/JEP.S524517","DOIUrl":"10.2147/JEP.S524517","url":null,"abstract":"<p><strong>Background: </strong>Ethanol consumption by oral route can induce gastric cell necrosis and vascular damage due to excessive reactive oxygen species (ROS) production. ROS activates the translocation of NF-κB to the nucleus and increases iNOS expression, an enzyme that catalyzes nitric oxide (NO) production, eventually disrupting gastric protective mechanisms and contributing to ulcer formation. <i>Etlingera elatior</i> inflorescence, which has been traditionally used to alleviate stomach discomfort, was reported to possess anti-inflammatory activity. However, such a study on the downregulation of the iNOS expression is lacking.</p><p><strong>Purpose: </strong>To confirm the gastro-protective and anti-ulcer effects of the <i>E. elatior</i> inflorescence (EEIE) extract via downregulation of iNOS expression in ethanol-induced gastric ulcer rats.</p><p><strong>Methods: </strong>The fresh inflorescence petals were collected from West Java, Indonesia, and were extracted using 70% ethanol. The effects of 5 days of oral administration of EEIE were studied in ethanol-induced adult male Wistar rats by examining the weight gain percentage, feed residue, stomach ratio index, and microscopic and macroscopic evaluation of gastric mucosal damage. Subsequently, the iNOS expression in the rats' stomach was Western blotted by employing β-actin as the loading control.</p><p><strong>Results: </strong>EEIE reduced weight gain percentage but did not show a significant difference in feed residue. EEIE increased the stomach ratio index, and at a dose of 625 mg/kg BW, significantly reduced the ulcer index, providing 100% protection (p < 0.05) to rats while decreasing inflammatory cell infiltration. EEIE inhibited the expression of iNOS in both cleaved and full-length forms at this dose.</p><p><strong>Conclusion: </strong><i>Etlingera elatior</i> inflorescence may have the potential to mitigate acute gastric ulcers by downregulating the expression of iNOS in ethanol-induced Wistar rats. However, further studies are needed to confirm its role in alleviating chronic ulcer models.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"343-357"},"PeriodicalIF":0.0,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12182249/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144475515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Zingerone Attenuates Cadmium-Induced Neuroinflammation, Oxidative Stress and Cognitive Deficit on the Prefrontal Cortex of Adult Wistar Rats.","authors":"Augustine Oviosun, Ezinne Chidinma Oviosun, Nto Johnson Nto, Adejoke Elizabeth Memudu, Emeka Godson Anyanwu","doi":"10.2147/JEP.S519571","DOIUrl":"10.2147/JEP.S519571","url":null,"abstract":"<p><strong>Introduction/background: </strong>Exposure to heavy metals like cadmium can adversely affect our brain function and cognitive abilities. Scientific evidence has strongly linked cadmium exposure to neurotoxicity, including oxidative damage and neuroinflammation. This study investigated the therapeutic role of <i>Zingerone</i> on cadmium-induced inflammation, oxidative stress and cognitive decline in the prefrontal cortex.</p><p><strong>Methodology: </strong>Thirty adult male Wistar rats were randomly assigned to six groups of five rats each. Group A (Control group), Group B (5mg/kg of cadmium induction), Group C (100mg/kg of <i>Zingerone</i> only), Group D-F (Treatment groups: 5mg/kg of cadmium+50mg/kg,100mg/kg, 200mg/kg of Zingerone respectively). To determine the cognitive abilities, we used a novel object recognition test (NORT), the whole treatment lasted for 21 days. We used blood samples and brain tissue for histological, biochemical and immunohistochemical evaluations. Data from this study was analysed using GraphPad Prism 10, and statistical difference between groups was determined using one-way ANOVA followed by Tukey's post hoc test (p <0.05).</p><p><strong>Result and discussion: </strong>There was significant reduction in superoxide dismutase (SOD), catalase (CAT) and significant increase malondialdehyde (MDA) in the cadmium-only group; however, this effect was mitigated in Groups C-F that received zingerone treatment. Cadmium exposure resulted in elevated levels of inflammatory cytokine Interleukin-6 (IL-6) and Tumor Necrosis Factor-alpha (TNF-α), these increases were significantly reduced in all <i>Zingerone-treated</i> groups. <i>Zingerone</i> considerably improved cognitive function, as seen by significant improvements in the discrimination index and novel object recognition time. Also, <i>Zingerone</i> significantly mitigated the over-expressivity of astrocytes in the prefrontal cortex and improved the histoarchitecture of the prefrontal cortex.</p><p><strong>Conclusion: </strong>This study shows that z<i>ingerone</i> demonstrated anti-oxidative and anti-inflammatory abilities and enhanced cognitive performance. These results indicate that zingerone might be a useful therapeutic agent that can mitigate neuroinflammation, oxidative damage, and cognitive decline.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"323-341"},"PeriodicalIF":0.0,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12174926/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325944","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Morin Mitigates Methamphetamine-Induced Neurotoxicity: Effects on Motor and Cognitive Function.","authors":"Godson E Anyanwu, Amarachukwu Vivian Umeano, Vivian O Ojiakor, Amechi U Katchy, Chinyere N Anyanwu, Sodiq Fakorede","doi":"10.2147/JEP.S498984","DOIUrl":"10.2147/JEP.S498984","url":null,"abstract":"<p><strong>Introduction: </strong>Neurodegenerative diseases are a major public health concern, often associated with motor and cognitive deficits. Methamphetamine (METH) exposure induces lasting neurological impairment and neuronal loss. This study evaluated Morin's potential to reverse these effects, focusing on motor and cognitive dysfunction in METH-induced neurotoxicity.</p><p><strong>Methods: </strong>Adult rats were randomly assigned into seven groups, including control, Morin-only, METH-only, METH plus fluoxetine, and three groups receiving METH followed by varying doses of Morin. Following METH induction, Morin, a natural flavonoid with antioxidant properties, was administered to rats. Neurobehavioral tests evaluated motor and cognitive function; serum levels of oxidative stress markers, inflammatory cytokines, dopamine, and acetylcholine were measured. Histological and immunohistochemical analyses of the basal ganglia were performed to evaluate neuronal integrity.</p><p><strong>Results: </strong>METH exposure significantly elevated oxidative stress and inflammatory markers, altered neurotransmitter levels, and impaired both motor and cognitive performance, coinciding with neuronal loss in the basal ganglia. Treatment with Morin ameliorated these effects in a dose-dependent manner. Neuronal degenerative features noted in the METH-only group were significantly ameliorated in the Morin-treated groups.</p><p><strong>Conclusion: </strong>These findings indicate that Morin mitigates METH-induced neurotoxicity by reducing oxidative stress, and suppressing inflammation. This study demonstrates Morin's potential as a treatment option for the neurological effects of methamphetamine misuse.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"307-321"},"PeriodicalIF":0.0,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12168913/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144309981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Anti-Tyrosinase and Radical Scavenging Activities of Selected Cassipourea Plants and Isolated 7-Methoxygeranin A: Traditional Use as Skin Lighteners.","authors":"Nomakhosi Mpofana, Michael Paulse, Masande Yalo, Ncoza Cordelia Dlova, Ahmed Hussein, Adedayo Ayodeji Lanrewaju, Halimat Yusuf Lukman, Jamiu Olaseni Aribisala, Fanie Rautenbach, Jeanine L Marnewick, Saheed Sabiu","doi":"10.2147/JEP.S504759","DOIUrl":"10.2147/JEP.S504759","url":null,"abstract":"<p><strong>Background: </strong>In rural areas of KwaZulu-Natal and Eastern Cape Provinces, South Africa, women have traditionally used bark extracts from <i>Cassipourea flanaganii, C. malosana</i>, and <i>C. gummiflua</i> for skin lightening and sun protection. This study investigates the anti-tyrosinase and antioxidant activities of methanolic bark extracts from these species, aiming to validate their traditional use and identify potential lead compounds for the treatment of skin hyperpigmentation.</p><p><strong>Methods: </strong>Anti-tyrosinase activity was evaluated using half-maximal inhibitory concentration (IC₅₀) values, and antioxidant capacity was measured through FRAP, DPPH, and TEAC assays. Polyphenol and flavanol contents were quantified using Folin-Ciocalteu method. Potential lead compounds were identified through molecular docking, pharmacokinetic analysis, and molecular dynamics (MD) simulations. Statistical analyses, including ANOVA and post-hoc tests, compared extract activities.</p><p><strong>Results: </strong><i>C. flanaganii</i> exhibited the most potent anti-tyrosinase activity (IC₅₀: 37.10 µg/mL), though statistical differences among species were non-significant. <i>C. gummiflua</i> showed the highest polyphenol (143.68 mg GAE/g) and flavanol (14.67 mg QE/g) content, correlating with superior antioxidant activity (FRAP: 526.07 µmol AAE/g; DPPH: 390.26 µmol TE/g; TEAC: 596.98 µmol TE/g). The isolated compound 7-methoxygeranin A demonstrated lower anti-tyrosinase activity (IC₅₀: 45.16 µg/mL) compared to <i>C. flanaganii</i> extract, suggesting the presence of more potent metabolites. Molecular docking and MD simulations identified emodin 6,8-dimethyl ether as a thermodynamically stable lead compound (binding free energy: -39.88 kcal/mol), interacting with key catalytic residues over 150 ns. The compound demonstrated prolonged residence at the active site of tyrosinase, indicating strong-binding stability.</p><p><strong>Conclusion: </strong>While <i>C. flanaganii</i> demonstrated the strongest anti-tyrosinase activity, C. gummiflua showed the highest antioxidant potential. Emodin 6,8-dimethyl ether emerged as a promising candidate for skin-lightening applications, warranting further in vitro and in vivo validation. These findings support the traditional use of <i>Cassipourea</i> species and highlight their potential for developing natural skin health products. Further studies are needed to explore the pharmacokinetics, safety, and efficacy of these compounds in clinical settings.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"287-306"},"PeriodicalIF":0.0,"publicationDate":"2025-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12136075/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144225676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biocompatibility and Effectiveness of Amphotericin B-Loaded Metal-Organic Structures (AmB-ZIF-8) as Dermal Drug Transporters in Experimental Cutaneous Leishmaniasis.","authors":"Heider Carreño, Jorge Osorio, Enrique Mejía-Ospino, Patricia Escobar","doi":"10.2147/JEP.S511808","DOIUrl":"10.2147/JEP.S511808","url":null,"abstract":"<p><strong>Purpose: </strong>Information on metal-organic frameworks (MOFs) as topical drug delivery systems (DDS) for antileishmanial drugs is limited. This study outlines our strategies for developing MOF-drug conjugate as a topical treatment for cutaneous leishmaniasis (CL) in mice infected with <i>Leishmania (L). amazonensis</i>.</p><p><strong>Methods: </strong>We selected conjugates from two commercial MOFs (ZIF-8 and Fe-BTC) and seven antileishmanial compounds. Amphotericin B (AmB) and zeolitic imidazolate framework-8 (AmB@ZIF-8) were chosen and prepared at an AmB: ZIF-8 ratio of 1.5:1.0 using the impregnation method. Conjugates were characterised using dynamic light scattering, UV-Vis, FTIR, and SEM. Hydrogels were prepared and evaluated for toxicity and efficacy in CL-BALB/c mice.</p><p><strong>Results: </strong>AmB@ZIF-8 exhibited a 59.6% loading capacity, 6.67% encapsulation efficiency, and 2% in vitro drug release (IVR). The particle size of AmB@ZIF-8 was smaller and more polydisperse than ZIF-8 (1370 nm vs 2537 nm). The conjugation of AmB to ZIF-8 was demonstrated. AmB@ZIF-8 exhibited similar antileishmanial activity to AmB against promastigotes. Topical 0.5% AmB@ZIF-8 and 0.5% AmB hydrogels, administered for 30 days, were unable to decrease lesion sizes or parasite loads. Initially, there was stabilisation of the lesion size; however, the lesions subsequently increased considerably during the 30-day follow-up period. The MOF-hydrogel treatment was non-irritating.</p><p><strong>Conclusion: </strong>There were very low EE% and AmB IVR. AmB@ZIF-8 and AmB hydrogels were found to be safe but ineffective against CL-infected mice. Several factors may explain these negative results, including the large size of the commercial ZIF-8, the aggregation of AmB in solution, the excess AmB used for impregnation, and the conditions of the IVR assay. We suggest continuing to use ZIF-8 as a DDS due to its sensitivity to acidic pH levels; however, we recommend reducing the particle size and lowering the drug-to-ZIF-8 ratio. Other alternatives are discussed in the present paper. We also advocate investigating alternative antileishmanial drugs as cargo, such as miltefosine or pentamidine.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"269-286"},"PeriodicalIF":0.0,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12133161/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144216036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Small Interfering RNA (siRNA) in Dyslipidemia: A Systematic Review on Safety and Efficacy of siRNA.","authors":"Sai Santhosha Mrudula Alla, Dhruv Jayeshkumar Shah, Shourya Meyur, Pahel Agarwal, Deekshitha Alla, Sai Lokesh Moraboina, Gayatri Vijay Ghadvaje, Ruth Getaneh Bayeh, Aparna Malireddi, Tess Shajan, Bodipudi Vineetha, Thalvayapati Sai Prudhvi, Patrick Biziyaremye","doi":"10.2147/JEP.S521579","DOIUrl":"10.2147/JEP.S521579","url":null,"abstract":"<p><strong>Introduction: </strong>RNA interference (RNAi) therapy represents an evolving advancement in the management of dyslipidemia. One prominent form of RNAi therapy is small interfering RNA (siRNA), which has emerged as a promising therapeutic strategy. This study aims to critically analyze the efficacy and safety of siRNA in the treatment of dyslipidemia.</p><p><strong>Methods: </strong>PubMed, Scopus, and Web of Science servers were used to conduct a systematic search in compliance with the PRISMA guidelines.</p><p><strong>Results: </strong>A total of 20 studies with 6651 participants were included in the analysis. The drugs used in the studies were. Inclisiran led to a notable 44.09% reduction in LDL and 37.5% in apolipoprotein levels among individuals with hypercholesterolemia. In hyperlipoproteinemia(a), therapies like Lepodisiran and Olpasiran achieved a 75.69% drop in apolipoproteins and 16.25% in LDL. For hypertriglyceridemia, agents such as ARO-APOC3 and Plozasiran showed over 50% reductions in both VLDL and triglycerides. In mixed hyperlipidemia and chylomicronemia, Plozasiran significantly reduced triglycerides by up to 79% and apolipoproteins by 87.5%. The 5 most common adverse effects reported were nasopharyngitis, diabetes mellitus (including new-onset diabetes mellitus and worsening diabetes mellitus), injection site adverse effects, back pain, and hypertension.</p><p><strong>Conclusion: </strong>In conclusion, the benefits of siRNA therapy in dyslipidemia management appear to outweigh its potential drawbacks, demonstrating promising efficacy and safety profiles. However, further research is necessary to fully understand its long-term effects and optimize its therapeutic potential.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"249-267"},"PeriodicalIF":0.0,"publicationDate":"2025-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12126973/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144199346","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Aaptamine Alters Vimentin Expression and Migration Capability of Triple-Negative Breast Cancer Cells.","authors":"Astrid Feinisa Khairani, Widad Aghnia Shalannandia, Muhammad Hasan Bashari, Nur Atik","doi":"10.2147/JEP.S512099","DOIUrl":"10.2147/JEP.S512099","url":null,"abstract":"<p><strong>Purpose: </strong>This study aimed to explore the effect of Aaptamine, an alkaloid derived from marine sponges, on the vimentin expression in both mRNA and protein levels and the migration capacity of breast cancer cells.</p><p><strong>Methods: </strong>The triple-negative breast cancer cell line MDA-MB-231 was used for in vitro experiments. Low-cytotoxicity concentrations of Aaptamine (12.5 to 50 μM) were given to MDA-MB-231 cells. The vimentin mRNA and protein expression were evaluated using RT-qPCR and immunofluorescence, respectively, 72 h after Aaptamine treatment. The migration scratch assay was conducted for 48 hours.</p><p><strong>Results: </strong>Aaptamine treatment in three different doses did not affect the expression of vimentin at the mRNA level while significantly lowering vimentin protein expression at the concentration of 12.5 µM. In addition, Aaptamine significantly inhibited breast cancer cell migration in a dose-dependent manner.</p><p><strong>Conclusion: </strong>Aaptamine inhibits vimentin protein expression and demonstrates anti-migration activity in the sub-cytotoxic dose.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"239-247"},"PeriodicalIF":0.0,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12105642/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144150691","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antidiabetic Effect of Hydro-Ethanolic Leaf Extract of <i>Sclerocarya Birrea</i> (A. Rich.) Hochst in Wistar Rats.","authors":"Abdul Gafar Victoir Coulidiaty, Estelle Noëla Hoho Youl, Téné Marceline Yaméogo, Farouk Adedeji Oladoja, Tolulope Anuoluwapo Odejobi, Raogo Ouedraogo, Olufunsho Awodele","doi":"10.2147/JEP.S523697","DOIUrl":"10.2147/JEP.S523697","url":null,"abstract":"<p><strong>Introduction: </strong>Diabetes mellitus, characterized by chronic hyperglycaemia, remains a major global health burden. Limitations of conventional therapies have led to growing interest in medicinal plants like <i>Sclerocarya birrea</i> (A. Rich.) Hochst. widely used in African ethnomedicine. Though prior research has focused more on the stem bark, studies on the leaves, considered more sustainable and traditionally relevant, are still lacking in vivo data. This study assessed the antidiabetic potential of a hydroethanolic leaf extract of <i>Sclerocarya birrea</i> in Wistar rats.</p><p><strong>Methods: </strong>The extract was tested at 25-200 mg/kg in an oral glucose tolerance test (OGTT), and at 100-400 mg/kg in normoglycemic and high fructose-fed, streptozotocin (STZ)-induced type 2 diabetic rats over 21 and 28 days, respectively. Fasting blood glucose, insulin, glycated haemoglobin (HbA1c), glucose transporter type 4 (GLUT4), haematological and biochemical parameters, and histopathological changes in key organs were evaluated.</p><p><strong>Results: </strong>In the OGTT, the extract significantly reduced postprandial blood glucose at 100 and 200 mg/kg starting from 60 minutes post-glucose load (p < 0.05). In normoglycemic rats, repeated administration over 21 days led to a dose-dependent and statistically significant reduction in fasting blood glucose beginning on day 14 and sustained through day 21 (p < 0.01). In diabetic rats, fasting blood glucose levels were significantly reduced from day 7 onward, with 400 mg/kg producing effects comparable to glibenclamide by day 28 (p < 0.01). Insulin, GLUT4, and HbA1c levels were not significantly altered (p > 0.05). Haematological and biochemical parameters remained within normal ranges, and histopathological examination showed preservation of pancreatic and renal tissues in treated groups.</p><p><strong>Conclusion: </strong><i>Sclerocarya birrea</i> leaf extract significantly lowers blood glucose in both normoglycemic and diabetic rats without adverse effects, supporting its potential as a safe plant-based option for diabetes management. Further research is warranted to clarify its mechanisms and long-term impact.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"223-237"},"PeriodicalIF":0.0,"publicationDate":"2025-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12094824/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144119832","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Effects of the Ethanol Extract of <i>Allium Ascalonicum</i> L. in High-Fat-High-Fructose-Induced Insulin Resistance Swiss-Webster Male Mice.","authors":"Rani Yulifah Elkanawati, Sri Adi Sumiwi, Jutti Levita","doi":"10.2147/JEP.S513301","DOIUrl":"10.2147/JEP.S513301","url":null,"abstract":"<p><strong>Background: </strong>Insulin resistance (IR) is a condition where the body cannot respond properly to insulin, leading to elevated blood glucose and the development of type 2 diabetes mellitus (T2DM). The first-line anti-T2DM drug is metformin, however, it has shown adverse effects, challenging the search for alternative natural drugs. Plant flavonoids stimulate cellular glucose uptake, decrease hyperglycemia, and regulate key signaling pathways in glucose metabolism. Brebes shallots (<i>Allium ascalonicum</i> L.) are known to contain flavonoids and thus may have the potential to inhibit IR.</p><p><strong>Purpose: </strong>To evaluate the effects of the ethanol extract of Brebes shallots in improving IR conditions.</p><p><strong>Methods: </strong>Brebes shallots were collected from West Java, Indonesia. 500 g of the shallots were oven-dried and extracted using 70% ethanol for 3×24 h, the solvent was evaporated to a thick consistency, and the extract was abbreviated as EAA. The effects of EAA were studied in high-fat-high-fructose (HFHF)-induced Swiss-Webster male mice by performing the insulin tolerance test (ITT) and oral glucose tolerance test (OGTT), and the liver and pancreas index. The nutritional composition and quercetin levels in the extract were also determined.</p><p><strong>Results: </strong>The extraction process yielded a 28.1% EAA. EAA reduces % weight gain, blood glucose levels in OGTT, and liver and pancreas index. EAA significantly improved insulin tolerance in the HFHF-induced mice (<i>p <</i> 0.05). Proximate analysis resulted in 3.92% ash, 0.12% fat, 13.45% protein, and 60.69% carbohydrate, while quercetin was at 0.0065%.</p><p><strong>Conclusion: </strong><i>Allium ascalonicum</i> L. extract may improve IR conditions as confirmed by its ability to increase the ITT value and reduce blood glucose levels. However, further studies are needed to confirm its role in alleviating metabolic disorders.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"17 ","pages":"207-221"},"PeriodicalIF":0.0,"publicationDate":"2025-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12091064/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144110877","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}