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Simultaneous quantification of duloxetine and 1-naphthol in pharmaceutical and biological matrices using a sensitive and eco-friendly synchronous fluorescence technique 利用灵敏环保的同步荧光技术同时定量药物和生物基质中的度洛西汀和1-萘酚
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-21 DOI: 10.1186/s43088-026-00826-y
Fatma F. Abdallah, Aly M. Waseem, Ali M. Yehia, Nehal F. Farid

Background

Duloxetine hydrochloride (DL) is a widely prescribed serotonin–norepinephrine reuptake inhibitor requiring stringent quality control due to the potential presence of 1-naphthol (NP), a genotoxic process-related impurity. DL and NP exhibit nearly identical native fluorescence spectra, posing a significant challenge for their simultaneous quantification by conventional fluorometric methods.

Objective

This study aimed to develop and validate a rapid, sensitive, and sustainable synchronous fluorescence spectroscopy (SFS) method with improved environmental profile for the simultaneous determination of DL and NP in pharmaceutical and biological matrices, without chromatographic separation or chemical derivatization.

Method

A dual-wavelength SFS approach was optimized using a fixed wavelength difference (Δλ = 125 nm), enabling selective detection at 356–362 nm for DL and 359–366 nm for NP in an 80% methanol–Britton–Robinson buffer system (pH 3.0). The method was fully validated by ICH Q2(R1) guidelines and rigorously evaluated for sustainability using four complementary greenness metrics: AGREE, ComplexMoGAPI, Analytical Eco-Scale, and Blue Applicability Grade Index (BAGI).

Results

Linear calibration curves (r² ≥ 0.9996) were obtained over 20–500 ng/mL for both analytes. The limits of detection were 6.19 ng/mL (DL) and 6.54 ng/mL (NP), with intra- and inter-day precision (%RSD < 1.5%) and mean recoveries of 100.26% (DL) and 99.89% (NP). The method showed excellent specificity in Cymbalta® capsules and spiked human plasma. Comprehensive greenness assessment confirmed high sustainability: AGREE score = 0.79, ComplexMoGAPI = 72.5/100, Analytical Eco-Scale = 81, and BAGI = 72.5/100, collectively classifying the method as “excellent green analysis” with strong practical applicability.

Conclusion

The proposed SFS method represents a chromatography-free, derivatization-free, and validated platform with enhanced sustainability features that successfully balance analytical performance, environmental responsibility, and laboratory feasibility. It offers a sustainable, cost-effective, and regulatory-compliant solution for routine quality control and bioanalytical monitoring of DL and its genotoxic impurity NP.

盐酸度洛西汀(DL)是一种广泛使用的5 -羟色胺-去甲肾上腺素再摄取抑制剂,由于可能存在1-萘酚(NP),一种与工艺相关的遗传毒性杂质,需要严格的质量控制。DL和NP表现出几乎相同的天然荧光光谱,这对传统荧光测定方法的同时定量提出了重大挑战。目的建立一种快速、灵敏、可持续的同步荧光光谱(SFS)方法,用于同时测定药物和生物基质中的DL和NP,无需色谱分离或化学衍生化。方法采用固定波长差(Δλ = 125 nm)优化双波长SFS方法,在80%甲醇- britton - robinson缓冲体系(pH 3.0)中,在356 ~ 362 nm选择性检测DL, 359 ~ 366 nm选择性检测NP。该方法通过ICH Q2(R1)指南进行了充分验证,并使用四个互补的绿色指标进行了严格的可持续性评估:AGREE, ComplexMoGAPI, Analytical Eco-Scale和蓝色适用性等级指数(BAGI)。结果在20 ~ 500 ng/mL范围内均获得r²≥0.9996的线性校准曲线。检出限分别为6.19 ng/mL (DL)和6.54 ng/mL (NP),日内、日间精密度(%RSD < 1.5%),平均加样回收率分别为100.26% (DL)和99.89% (NP)。该方法对欣百达®胶囊和加标人血浆具有良好的特异性。综合绿色度评价结果表明,该方法具有较高的可持续性:AGREE得分为0.79,ComplexMoGAPI为72.5/100,Analytical Eco-Scale为81,BAGI为72.5/100,整体评价该方法为“优秀绿色分析”,实用性强。结论提出的SFS方法代表了一个无色谱、无衍生化、经过验证的平台,具有增强的可持续性特征,成功地平衡了分析性能、环境责任和实验室可行性。它为DL及其遗传毒性杂质NP的常规质量控制和生物分析监测提供了一种可持续的、具有成本效益的、符合法规的解决方案。
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引用次数: 0
Dichamanetin attenuates hydrogen peroxide-induced cytotoxicity in retinoic acid (RA) -differentiated human neuroblastoma (SH-SY5Y) cells 双沙曼黄素减弱过氧化氢诱导的视黄酸(RA)分化的人神经母细胞瘤(SH-SY5Y)细胞的细胞毒性
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-21 DOI: 10.1186/s43088-026-00842-y
Muhammad-Safuan Zainuddin, Chee-Wei Ang, Saatheeyavaane Bhuvanendran, Adzzie-Shazleen Azman

Background

Alzheimer’s disease (AD) is a leading neurodegenerative disorder that imposes a significant global socioeconomic burden. It is characterised as progressive cognitive decline and a complex multifactorial pathology. Despite extensive research, current therapeutic options are limited. Emerging evidence suggests that oxidative stress is critical in the early pathological event preceding the classical hallmarks of AD. Targeting oxidative stress is a promising strategy for treating AD. Flavonoids are attractive due to their antioxidant, anti-inflammatory, and neuroprotective effects in AD. Dichamanetin (C29H24O6) is a rare C-benzylated flavanone that seldom occur in nature with reported antibacterial, and anti-malarial. Importantly, it has been suggested to possess anti-Alzheimer’s disease in-silico. However, neither its antioxidative nor neuroprotective potential has been explored in-vitro. Thus, this study aimed to address this gap by establishing an efficient method for the synthesis of dichamanetin and investigating its antioxidant properties and neuroprotective potential against hydrogen peroxide (H₂O₂)-induced cytotoxicity in-vitro.

Methods

In this study, we described the synthesis of dichamanetin using microwave irradiation and investigated its antioxidative activity using DPPPH and FRAP assay. Furthermore, we studied dichamanetin’s neuroprotective potential against hydrogen peroxide (H2O2)-insult as an in-vitro AD model using three treatment conditions include pre-treatment, co-treatment, and staggered co-treatment using CCK-8 cell viability assay.

Results

Dichamanetin was synthesised via microwave irradiation method, overcoming the limitations of isolation and purification from natural sources which often resulted in low yield. The improved synthesis method produced a good yield of 50% and purity of 95–97% determined via LC-MS and 1H NMR analyses. It shows that dichamanetin has low antioxidative activity as shown by FRAP ability. Importantly, it was non-cytotoxic to cholinergic neurons at concentrations below 3.125 µg/mL. It is shown to be a potent neuroprotectant in protecting the cholinergic neurons against H2O2-insult at 0.781 µg/mL, eliciting the highest neuroprotective effect in 6-hour staggered co-treatment comparable to quercetin and donepezil.

Conclusions

Dichamanetin attenuated H₂O₂-induced cytotoxicity in RA-differentiated SH-SY5Y cells, supporting its potential as a neuroprotective candidate against oxidative stress. Further studies are warranted to elucidate the underlying mechanisms and validate its efficacy, pharmacokinetics, safety, and therapeutic potential in relevant in vivo models of Alzheimer’s disease.

Graphical Abstract

阿尔茨海默病(AD)是一种主要的神经退行性疾病,造成了重大的全球社会经济负担。它的特点是进行性认知能力下降和复杂的多因素病理。尽管进行了广泛的研究,但目前的治疗选择仍然有限。新出现的证据表明,氧化应激在阿尔茨海默病经典特征出现之前的早期病理事件中起着关键作用。靶向氧化应激是治疗AD的一种很有前途的策略。黄酮类化合物因其抗氧化、抗炎和神经保护作用而受到关注。Dichamanetin (C29H24O6)是一种罕见的c -苄基黄酮,在自然界中很少出现,有抗菌和抗疟疾的报道。重要的是,它已经被认为拥有抗阿尔茨海默病的芯片。然而,其抗氧化和神经保护潜能尚未在体外探索。因此,本研究旨在通过建立一种有效的合成方法来解决这一空白,并研究其抗氧化性能和抗过氧化氢(h2o2)诱导的体外细胞毒性的神经保护潜力。方法采用微波辐照法合成双沙曼黄素,并采用DPPPH法和FRAP法研究其抗氧化活性。此外,我们通过CCK-8细胞活力测定,研究了双沙曼黄素作为体外AD模型对过氧化氢(H2O2)损伤的神经保护潜力,采用预处理、共处理和交错共处理三种处理条件。结果采用微波辐照法合成了地沙马黄素,克服了从天然来源分离纯化的限制。改进后的合成方法产率为50%,经LC-MS和1H NMR分析纯度为95-97%。结果表明,双沙曼黄素具有较低的抗氧化活性。重要的是,当浓度低于3.125µg/mL时,它对胆碱能神经元无细胞毒性。研究表明,在0.781µg/mL浓度下,它是一种有效的神经保护剂,可以保护胆碱能神经元免受h2o2的损伤,在6小时的交错共处理中,其神经保护效果最高,可与槲皮素和多奈哌齐媲美。结论双沙曼黄素可减轻h2o2诱导的ra分化SH-SY5Y细胞的细胞毒性,支持其作为抗氧化应激的神经保护候选物质的潜力。需要进一步的研究来阐明其潜在的机制,并验证其在阿尔茨海默病相关体内模型中的有效性、药代动力学、安全性和治疗潜力。图形抽象
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引用次数: 0
From cultivation to clinical translation: a critical review of ginger phytochemistry, antimicrobial mechanisms, bioavailability, and standardization 从栽培到临床转化:生姜植物化学、抗菌机制、生物利用度和标准化的重要综述
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-21 DOI: 10.1186/s43088-026-00844-w
Chris Izaak Jones, Haema Thevanayagam, Yee Mon Htet, Goh Bey Hing, Mohmad Farooq Shaikh, Kavitha Rajendran

Ginger (Zingiber officinale Roscoe) is simultaneously a food, traditional medicine, and source of chemically diverse phenolic and volatile constituents. Its antimicrobial promise is supported by numerous in vitro studies, yet translation remains constrained by inconsistent botanical identification, extraction-dependent composition, non-comparable susceptibility assays, limited pharmacokinetic–pharmacodynamic integration, and a scarcity of controlled clinical evidence. This critical narrative review integrates botanical identity, genotype–environment and post-harvest effects, chemistry, analytical standardization, antimicrobial mechanisms, pathogen-specific evidence, human disposition, and formulation science. Rather than ranking cultivars on isolated measurements, the review treats cultivar, environment, maturity, processing, extraction, and analytical platform as interacting determinants of the final chemical phenotype. Evidence is organized mechanistically—membrane perturbation, biofilm and quorum-sensing interference, metabolic and enzymatic inhibition, oxidative stress, host-directed effects, and antimicrobial synergy—and then appraised by pathogen class. Gingerols and shogaols are rapidly transformed and extensively conjugated; therefore, nominal extract dose cannot be equated with systemic exposure to free parent compounds. HPTLC, HPLC/UPLC, LC–MS/MS, GC–MS, chemometrics, and validated reference materials are positioned as prerequisites for reproducible biological claims. Nanoformulations and ginger-derived vesicles may improve stability, localization, and exposure, but their safety, scalability, compositional definition, and comparative advantage require rigorous evaluation. Overall, ginger is best regarded as a platform for standardized antimicrobial adjuncts and food- or material-based applications, not as a clinically validated replacement for conventional anti-infective therapy. Future progress requires authenticated multicenter sample sets, harmonized assays, exposure-linked mechanistic studies, resistance-aware designs, and appropriately powered clinical trials.

生姜(Zingiber officinale Roscoe)既是一种食物,也是一种传统药物,也是化学上多种酚类和挥发性成分的来源。其抗菌前景得到了许多体外研究的支持,但翻译仍然受到不一致的植物鉴定、提取物依赖成分、不可比较的敏感性测定、有限的药代动力学-药效学整合以及缺乏对照临床证据的限制。这篇批判性的叙述性综述整合了植物特性、基因型-环境和收获后效应、化学、分析标准化、抗菌机制、病原体特异性证据、人类倾向和配方科学。这篇综述将品种、环境、成熟度、加工、提取和分析平台视为最终化学表型的相互作用决定因素,而不是根据孤立的测量结果对品种进行排序。证据被机械地组织起来——膜扰动、生物膜和群体感应干扰、代谢和酶抑制、氧化应激、宿主定向效应和抗菌协同作用——然后按病原体类别进行评价。姜辣素和姜辣素迅速转化并广泛结合;因此,名义提取物剂量不能等同于全身暴露于游离母体化合物。HPTLC, HPLC/UPLC, LC-MS /MS, GC-MS,化学计量学和验证的标准物质被定位为可重复性生物声明的先决条件。纳米配方和生姜衍生的囊泡可以改善稳定性、定位和暴露,但它们的安全性、可扩展性、成分定义和比较优势需要严格的评估。总的来说,生姜最好被视为标准化抗菌辅助剂和基于食品或材料的应用的平台,而不是作为常规抗感染治疗的临床验证替代品。未来的进展需要经过认证的多中心样本集、统一的测定方法、暴露相关的机制研究、耐药性感知设计和适当的临床试验。
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引用次数: 0
Current trends, knowledge structure, and evidence landscape of phosphorylation-related research in organoid models: a bibliometric analysis 类器官模型中磷酸化相关研究的当前趋势、知识结构和证据景观:文献计量学分析
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-16 DOI: 10.1186/s43088-026-00849-5
Rui Guo, Jing Jia, Chaojun Wei

Background

Research on phosphorylation in organoid models has experienced rapid expansion; however, the knowledge structure, academic impact, and depth of evidence in this field remain inadequately characterized.

Methods

Publications indexed in the Web of Science Core Collection (SCI-EXPANDED) from 2005 to 2025 were retrieved on April 2, 2026. Following document-type restriction, deduplication, and manual screening, a total of 236 studies were included. CiteSpace was employed to analyze publication trends, collaboration patterns, co-citation structures, highly cited studies, keyword evolution, and citation-based impact. The included studies were further classified according to evidence type.

Results

Publication output experienced a significant increase after 2017, with the United States and China emerging as the primary contributors. However, the levels of productivity did not consistently correlate with citation impact or collaborative centrality. Co-citation analysis indicated that the field predominantly focuses on the establishment of stem cell-derived organoids, translational oncology, cerebral organoid disease models, and the signaling pathways that regulate organoid growth and differentiation. The most highly cited studies primarily centered on mechanistic phospho-signaling research, while more recent influential works have expanded into disease modeling and phosphoproteomics. Notably, 184 out of 236 studies (77.97%) were classified as providing signaling evidence, whereas only 24 studies (10.27%) offered direct evidence of phosphorylation. Furthermore, intestinal and brain organoids comprised the majority of the studies included, highlighting a pronounced tissue bias within the research.

Conclusions

Research on phosphorylation within organoid models is a rapidly expanding yet heterogeneous field, predominantly characterized by studies focused on signaling pathways, while direct evidence of phosphorylation remains scarce. These findings underscore significant disparities in impact, model utilization, and the depth of evidence, which should guide future mechanistic and translational research endeavors.

在类器官模型中磷酸化的研究迅速扩大;然而,这一领域的知识结构、学术影响和证据深度仍然不够充分。方法于2026年4月2日检索Web of Science Core Collection (SCI-EXPANDED) 2005 ~ 2025年收录的出版物。经过文档类型限制、重复数据删除和手动筛选,总共纳入了236项研究。使用CiteSpace分析出版物趋势、合作模式、共被引结构、高被引研究、关键词演变和基于引用的影响。根据证据类型对纳入的研究进行进一步分类。结果2017年之后,中国和美国的论文发表量显著增加,成为主要贡献者。然而,生产力水平并不总是与引文影响或协作中心性相关。共引分析表明,该领域主要集中于干细胞衍生类器官的建立、转化肿瘤学、脑类器官疾病模型以及调节类器官生长和分化的信号通路。被引用最多的研究主要集中在机制磷酸化信号研究上,而最近更有影响力的工作已经扩展到疾病建模和磷酸化蛋白质组学。值得注意的是,236项研究中有184项(77.97%)被归类为提供信号证据,而只有24项研究(10.27%)提供了磷酸化的直接证据。此外,肠道和大脑类器官构成了所纳入研究的大部分,突出了研究中明显的组织偏见。类器官模型中磷酸化的研究是一个快速发展但异质性的领域,主要集中在信号通路的研究上,而磷酸化的直接证据仍然很少。这些发现强调了在影响、模型利用和证据深度方面的显著差异,这些差异应该指导未来的机制和转化研究工作。
{"title":"Current trends, knowledge structure, and evidence landscape of phosphorylation-related research in organoid models: a bibliometric analysis","authors":"Rui Guo,&nbsp;Jing Jia,&nbsp;Chaojun Wei","doi":"10.1186/s43088-026-00849-5","DOIUrl":"10.1186/s43088-026-00849-5","url":null,"abstract":"<div><h3>Background</h3><p>Research on phosphorylation in organoid models has experienced rapid expansion; however, the knowledge structure, academic impact, and depth of evidence in this field remain inadequately characterized.</p><h3>Methods</h3><p>Publications indexed in the Web of Science Core Collection (SCI-EXPANDED) from 2005 to 2025 were retrieved on April 2, 2026. Following document-type restriction, deduplication, and manual screening, a total of 236 studies were included. CiteSpace was employed to analyze publication trends, collaboration patterns, co-citation structures, highly cited studies, keyword evolution, and citation-based impact. The included studies were further classified according to evidence type.</p><h3>Results</h3><p>Publication output experienced a significant increase after 2017, with the United States and China emerging as the primary contributors. However, the levels of productivity did not consistently correlate with citation impact or collaborative centrality. Co-citation analysis indicated that the field predominantly focuses on the establishment of stem cell-derived organoids, translational oncology, cerebral organoid disease models, and the signaling pathways that regulate organoid growth and differentiation. The most highly cited studies primarily centered on mechanistic phospho-signaling research, while more recent influential works have expanded into disease modeling and phosphoproteomics. Notably, 184 out of 236 studies (77.97%) were classified as providing signaling evidence, whereas only 24 studies (10.27%) offered direct evidence of phosphorylation. Furthermore, intestinal and brain organoids comprised the majority of the studies included, highlighting a pronounced tissue bias within the research.</p><h3>Conclusions</h3><p>Research on phosphorylation within organoid models is a rapidly expanding yet heterogeneous field, predominantly characterized by studies focused on signaling pathways, while direct evidence of phosphorylation remains scarce. These findings underscore significant disparities in impact, model utilization, and the depth of evidence, which should guide future mechanistic and translational research endeavors.</p></div>","PeriodicalId":481,"journal":{"name":"Beni-Suef University Journal of Basic and Applied Sciences","volume":"15 1","pages":""},"PeriodicalIF":3.1,"publicationDate":"2026-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1186/s43088-026-00849-5.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149189491","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}
引用次数: 0
Integrated experimental and computational evaluation of a Marsilea minuta-loaded hydrogel for enhanced wound-healing 综合实验和计算评估的Marsilea分钟负载水凝胶促进伤口愈合
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-06 DOI: 10.1186/s43088-026-00845-9
Satyapriya Mahapatra, Ghanshyam Panigrahi, Sandesh Kumar Pattanaik, Lorie Dehury, Ashutosh Prasad Ghadei, Diptirani Rath

Background

Marsilea minuta L., a medicinal aquatic fern is of ethnopharmacological importance as per various traditional systems of medicine. It is used to treat skin disorders like wound in India.This study aims to explore the effect of the methanolic extract of M. minuta by using both in silico and in-vivo techniques in the treatment of wounds.

Methods

The plant material Marsilea minuta L., (MEMM) was defatted first with petroleum ether to remove the fat and then extracted with solvent methanol in a Soxhlet apparatus. GC-MS analysis was used to identify the compound annotations tentatively in the methanolic extract. The methanolic extract was prepared into a hydrogel for the investigation of wound-healing activity using the excision model in rats. The animals were divided into four groups i.e. a standard group (STD) that treated with Silver nitrate gel, a normal control group (NC) treated with Gel base, and two groups treated with the MEMM-loaded hydrogel formulations (MEMM 5 % w/v and MEMM 10 % w/v), containing six animals per group. The primary end point was wound contraction area, and additionally % of wound-healing and histopathological examination were adopted. Additionally, in-silico molecular docking was conducted against the target proteins to support our findings. One-way ANOVA was used to examine group differences, followed by Tukey's post hoc test for multiple comparisions.

Results

The experimental evidence shows that the 10 % w/v hydrogel group exhibits effective wound-healing activity as compared to that of the standard group. Histopathological examination confirms collagen formations, which accelerated re-epithelialization and remodelling of the wound. Further, the in-silico investigations support our findings, as the tentatively identified compounds showed moderate to strong binding affinities for wound-healing targets such as VEGFR-2, COX-2, and MMP-9.

Conclusion

This study concludes that M. minuta contains a diverse array of tentatively identified compounds that support the plant’s wound-healing activity. Overall, this investigation of scientific evidence supports the ethnopharmacological claim and highlights it as a promising, adjunctive natural therapeutic candidate for wound-healing.

marsilea minuta L.是一种药用水生蕨类植物,在各种传统医学体系中具有重要的民族药理学意义。在印度,它被用来治疗皮肤疾病,比如伤口。本研究旨在通过体外和体内两种技术,探讨米努塔甲醇提取物在伤口治疗中的作用。方法先用石油醚脱脂,然后在索氏装置中用溶剂甲醇萃取。采用气相色谱-质谱法对甲醇提取物中的化合物进行初步鉴定。将甲醇提取物制备成水凝胶,用于大鼠切除模型伤口愈合活性的研究。将实验动物分为四组,即标准组(STD)用硝酸银凝胶处理,正常对照组(NC)用凝胶碱处理,两组用MEMM负载水凝胶配方(MEMM 5% w/v和MEMM 10% w/v)处理,每组6只动物。以创面收缩面积为主要终点,并采用%创面愈合率和组织病理学检查。此外,针对目标蛋白进行了硅分子对接以支持我们的发现。组间差异采用单因素方差分析,多组比较采用Tukey事后检验。结果实验结果表明,10% w/v水凝胶组较标准组具有较好的创面愈合活性。组织病理学检查证实胶原形成,加速了伤口的再上皮化和重塑。此外,计算机研究支持我们的发现,因为初步鉴定的化合物对创面愈合靶点(如VEGFR-2、COX-2和MMP-9)具有中等到强的结合亲和力。本研究得出结论,龙葵含有多种初步鉴定的支持该植物伤口愈合活性的化合物。总的来说,这项科学证据的调查支持民族药理学的说法,并强调它是一个有前途的,辅助的自然治疗候选人的伤口愈合。
{"title":"Integrated experimental and computational evaluation of a Marsilea minuta-loaded hydrogel for enhanced wound-healing","authors":"Satyapriya Mahapatra,&nbsp;Ghanshyam Panigrahi,&nbsp;Sandesh Kumar Pattanaik,&nbsp;Lorie Dehury,&nbsp;Ashutosh Prasad Ghadei,&nbsp;Diptirani Rath","doi":"10.1186/s43088-026-00845-9","DOIUrl":"10.1186/s43088-026-00845-9","url":null,"abstract":"<div><h3>Background</h3><p><i>Marsilea minuta</i> L., a medicinal aquatic fern is of ethnopharmacological importance as per various traditional systems of medicine. It is used to treat skin disorders like wound in India.This study aims to explore the effect of the methanolic extract <i>of M. minuta</i> by using both in silico and in-vivo techniques in the treatment of wounds.</p><h3>Methods</h3><p>The plant material <i>Marsilea minuta</i> L., (MEMM) was defatted first with petroleum ether to remove the fat and then extracted with solvent methanol in a Soxhlet apparatus. GC-MS analysis was used to identify the compound annotations tentatively in the methanolic extract. The methanolic extract was prepared into a hydrogel for the investigation of wound-healing activity using the excision model in rats. The animals were divided into four groups i.e. a standard group (STD) that treated with Silver nitrate gel, a normal control group (NC) treated with Gel base, and two groups treated with the MEMM-loaded hydrogel formulations (MEMM 5 % w/v and MEMM 10 % w/v), containing six animals per group. The primary end point was wound contraction area, and additionally % of wound-healing and histopathological examination were adopted. Additionally, in-silico molecular docking was conducted against the target proteins to support our findings. One-way ANOVA was used to examine group differences, followed by Tukey's post hoc test for multiple comparisions.</p><h3>Results</h3><p>The experimental evidence shows that the 10 % w/v hydrogel group exhibits effective wound-healing activity as compared to that of the standard group. Histopathological examination confirms collagen formations, which accelerated re-epithelialization and remodelling of the wound. Further, the in-silico investigations support our findings, as the tentatively identified compounds showed moderate to strong binding affinities for wound-healing targets such as VEGFR-2, COX-2, and MMP-9.</p><h3>Conclusion</h3><p>This study concludes that <i>M. minuta</i> contains a diverse array of tentatively identified compounds that support the plant’s wound-healing activity. Overall, this investigation of scientific evidence supports the ethnopharmacological claim and highlights it as a promising, adjunctive natural therapeutic candidate for wound-healing.</p></div>","PeriodicalId":481,"journal":{"name":"Beni-Suef University Journal of Basic and Applied Sciences","volume":"15 1","pages":""},"PeriodicalIF":3.1,"publicationDate":"2026-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1186/s43088-026-00845-9.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149132429","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}
引用次数: 0
The efficacy of the crude Origanum genus (Lamiaceae) essential oils on experimentally infected mice with Blastocystis spp. 牛头草属(Lamiaceae)粗精油对实验性囊虫感染小鼠的作用。
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-05 DOI: 10.1186/s43088-026-00838-8
Ekhlas H. Abdel-Hafeez, Mohamed M. Abdel-Fatah, Manar M. Sanadeki, Manar M. S. A. Nasr, Shaimaa M. Hafez, Reham A. M. Abd Rabou

Background

Blastocystis spp. is a common intestinal protozoan with a controversial role in gastrointestinal disease, and the variable efficacy of conventional therapies has prompted the search for alternative treatment options. This study evaluated the therapeutic effects of crude Origanum essential oil in experimentally infected mice compared with nitazoxanide (NTZ).

Methods

Forty male Swiss albino mice were allocated into four groups: negative control, infected untreated, NTZ-treated ((:100text{:mg/kg/day})), and crude Origanum oil-treated ((:0.5text{:mL/kg/day})). The essential oil was evaluated in its crude form without chemical characterization (e.g., GC-MS). Mice were orally infected with (:1times:{10}^{5}text{:Blastocystis}) cysts and treated for seven days. Treatment efficacy was assessed by fecal cyst counts, intestinal nitric oxide (NO) and malondialdehyde (MDA) levels, and histopathological examination of intestinal tissues. Data was analyzed using one-way ANOVA.

Results

Infected untreated mice exhibited reduced activity and soft stools. Clinical improvement was observed in both treatment groups within 5–7 days, and no mortality occurred during the study. The infected untreated group showed the highest cyst burden ((:6.2times:{10}^{5}pm:0.4times:{10}^{5}text{:cysts/g:stool})), whereas NTZ and crude Origanum oil treatment significantly reduced cyst shedding by (:85.6%) and (:91.3%), respectively, compared with infected controls ((:p<0.001)). No cysts were detected in the non-infected control group. Infection was associated with significant increases in intestinal NO and MDA levels, indicating oxidative stress and inflammation. Both treatments significantly reduced these markers ((:p<0.001)), with values in the Origanum-treated group approaching those of the negative control group. Histopathological examination revealed villous atrophy, epithelial desquamation, and inflammatory cell infiltration in infected untreated mice. NTZ treatment resulted in partial improvement of these lesions, whereas crude Origanum oil treatment was associated with marked restoration of villous architecture and minimal inflammatory changes.

Conclusions

Under this experimental model, crude Origanum vulgare essential oil improved parasitological, biochemical, and histopathological parameters in Blastocystis-infected mice. Because chemical profiling was not performed, these effects reflect the biological activity of the crude extract as a whole. Further studies incorporating GC-MS characterization are needed to identify active constituents, optimize dosing, and confirm these findings in other models and clinical settings.

囊虫是一种常见的肠道原生动物,在胃肠道疾病中起着有争议的作用,传统治疗方法的不同疗效促使人们寻找替代治疗方案。本研究比较了土一枝精油对实验性感染小鼠的治疗作用,并与硝唑肼(nitazoxanide, NTZ)进行了比较。方法雄性瑞士白化病小鼠40只,随机分为阴性对照组、感染未处理组、ntz处理组((:100text{:mg/kg/day}))和牛头草粗油处理组((:0.5text{:mL/kg/day}))。精油以其原始形式进行评估,不进行化学表征(例如GC-MS)。小鼠口服感染(:1times:{10}^{5}text{:Blastocystis})囊肿并治疗7天。通过粪便囊肿计数、肠道一氧化氮(NO)、丙二醛(MDA)水平及肠道组织病理学检查评价治疗效果。数据分析采用单因素方差分析。结果感染未处理小鼠表现出活性降低和软便。两组患者均在5-7天内临床改善,研究期间无死亡发生。感染未处理组的囊肿负荷最高((:6.2times:{10}^{5}pm:0.4times:{10}^{5}text{:cysts/g:stool})),而与感染对照组((:p<0.001))相比,NTZ和牛头草粗油处理分别显著减少了(:85.6%)和(:91.3%)的囊肿脱落。未感染对照组未检出囊肿。感染与肠道NO和MDA水平显著升高相关,提示氧化应激和炎症。两种处理都显著降低了这些标记物((:p<0.001)),处理组的数值接近阴性对照组。组织病理学检查显示,感染未治疗的小鼠绒毛萎缩,上皮脱屑,炎症细胞浸润。NTZ治疗导致了这些病变的部分改善,而粗Origanum油治疗与绒毛结构的显著恢复和最小的炎症变化相关。结论在该实验模型下,土茯苓粗精油可改善囊胚感染小鼠的寄生虫学、生化和组织病理学指标。由于没有进行化学分析,这些影响反映了粗提取物作为一个整体的生物活性。需要进一步的研究结合GC-MS表征来确定有效成分,优化剂量,并在其他模型和临床环境中证实这些发现。
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引用次数: 0
Computational elucidation of the potential mechanisms of Warburgia ugandensis against colorectal cancer 乌干达沃布贾抗结直肠癌潜在机制的计算阐明
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-01 DOI: 10.1186/s43088-026-00840-0
Yohana Amos, Bienvenu Nsengimaana, Mercy Bisola Faleyimu, Peter Olorundunsin Adeniyi, Aishat Adebola Lawal, Orace Mathieu Kenou, Darius Riziki Martin, Ashita Jawali, Olaitan I. Awe
<div><h3>Background</h3><p>Colorectal cancer remains a major global health challenge due to its high incidence, mortality, therapeutic resistance, and treatment-related adverse effects. <i>Warburgia ugandensis</i> is a medicinal plant that has demonstrated anti-colorectal cancer; however, the specific bioactive compounds responsible and their underlying molecular mechanisms remain underexplored. This study investigated the anti-colorectal cancer potential and molecular mechanisms of <i>W. ugandensis</i> phytochemicals using an integrated computational approach.</p><h3>Methods</h3><p>Phytochemicals were retrieved from published literature and the Collection of Open Natural Products database, standardized, and screened for drug-likeness and oral bioavailability. Potential protein targets were predicted and intersected with colorectal cancer-associated genes, followed by network pharmacology and functional enrichment analyses. Molecular docking, 100 ns molecular dynamics simulations, molecular mechanics Poisson-Boltzmann surface area binding energy calculations, and absorption, distribution, metabolism, excretion, and toxicity (ADMET) analyses were performed to evaluate compound-target interactions, complex stability, and pharmacological properties.</p><h3>Results</h3><p>Among 242 identified phytochemicals, 21 compounds satisfied drug-likeness and oral bioavailability criteria. Target prediction identified 435 potential protein targets of the screened phytochemicals, of which 411 overlapped with colorectal cancer-associated genes. Network analysis of the overlapping targets identified PIK3CA, PIK3CD, GNAI1, GNAI3, and SRC as key hub genes. Functional enrichment analysis suggested that these targets are involved in cancer-relevant signaling pathways, including the phosphatidylinositol 3-kinase-protein kinase B, insulin receptor, and relaxin signaling pathways. Molecular docking identified quercetin, kaempferol, and bemadienolide as leading candidates, with strong binding affinities toward GNAI1 (-9.8 kcal/mol), GNAI3 (-9.6 kcal/mol), and PIK3CD (-8.7 kcal/mol), respectively. Molecular dynamics simulations demonstrated stable protein-ligand complexes with reduced structural fluctuations over 100 ns. Binding free energy analysis revealed favorable interactions, with quercetin-GNAI1 showing the strongest predicted binding stability (-86.2 ± 3.3 kcal/mol). Pharmacokinetic and toxicity predictions indicated high gastrointestinal absorption and generally low predicted toxicity profiles.</p><h3>Conclusion</h3><p>This study provides computational, hypothesis-generating evidence that <i>Warburgia ugandensis</i> phytochemicals may modulate multiple molecular targets and signaling pathways involved in colorectal cancer. Quercetin, kaempferol, and bemadienolide represent promising candidates for further experimental investigation. Nevertheless, these predictive findings require validation through in-vitro and in-vivo studies to establish their therapeutic releva
结直肠癌由于其高发病率、死亡率、治疗耐药性和治疗相关的不良反应,仍然是一个主要的全球健康挑战。乌干达Warburgia ugandensis是一种具有抗结直肠癌作用的药用植物;然而,具体的生物活性化合物及其潜在的分子机制仍未得到充分研究。本研究采用综合计算方法研究了乌干达白檀植物化学物质的抗结直肠癌潜能和分子机制。方法从已发表文献和开放天然产物数据库中检索植物化学物质,进行标准化、药物相似性和口服生物利用度筛选。预测潜在的蛋白靶点并与结直肠癌相关基因交叉,随后进行网络药理学和功能富集分析。通过分子对接、100 ns分子动力学模拟、分子力学泊松-玻尔兹曼表面积结合能计算、吸收、分布、代谢、排泄和毒性(ADMET)分析来评估化合物与靶标的相互作用、复合物的稳定性和药理学性质。结果鉴定的242种植物化学物质中,有21种化合物符合药物相似度和口服生物利用度标准。靶标预测确定了筛选的植物化学物质的435个潜在蛋白靶点,其中411个与结直肠癌相关基因重叠。重叠靶点的网络分析鉴定出PIK3CA、PIK3CD、GNAI1、GNAI3和SRC是关键枢纽基因。功能富集分析表明,这些靶点与癌症相关的信号通路有关,包括磷脂酰肌醇3-激酶-蛋白激酶B、胰岛素受体和松弛素信号通路。分子对接鉴定槲皮素、山奈酚和贝马二烯内酯为主要候选化合物,分别与GNAI1 (-9.8 kcal/mol)、GNAI3 (-9.6 kcal/mol)和PIK3CD (-8.7 kcal/mol)具有较强的结合亲和力。分子动力学模拟表明,稳定的蛋白质配体复合物在100 ns内结构波动减小。结合自由能分析显示出良好的相互作用,槲皮素- gnai1表现出最强的结合稳定性(-86.2±3.3 kcal/mol)。药代动力学和毒性预测表明,胃肠道吸收高,毒性预测一般较低。结论本研究提供了计算性的、可产生假设的证据,表明乌干达Warburgia uandensis植物化学物质可能调节与结直肠癌相关的多个分子靶点和信号通路。槲皮素、山奈酚和贝马二烯内酯是进一步实验研究的有希望的候选者。然而,这些预测结果需要通过体外和体内研究验证,以确定其治疗相关性。临床试验编号不适用。
{"title":"Computational elucidation of the potential mechanisms of Warburgia ugandensis against colorectal cancer","authors":"Yohana Amos,&nbsp;Bienvenu Nsengimaana,&nbsp;Mercy Bisola Faleyimu,&nbsp;Peter Olorundunsin Adeniyi,&nbsp;Aishat Adebola Lawal,&nbsp;Orace Mathieu Kenou,&nbsp;Darius Riziki Martin,&nbsp;Ashita Jawali,&nbsp;Olaitan I. Awe","doi":"10.1186/s43088-026-00840-0","DOIUrl":"10.1186/s43088-026-00840-0","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Background&lt;/h3&gt;&lt;p&gt;Colorectal cancer remains a major global health challenge due to its high incidence, mortality, therapeutic resistance, and treatment-related adverse effects. &lt;i&gt;Warburgia ugandensis&lt;/i&gt; is a medicinal plant that has demonstrated anti-colorectal cancer; however, the specific bioactive compounds responsible and their underlying molecular mechanisms remain underexplored. This study investigated the anti-colorectal cancer potential and molecular mechanisms of &lt;i&gt;W. ugandensis&lt;/i&gt; phytochemicals using an integrated computational approach.&lt;/p&gt;&lt;h3&gt;Methods&lt;/h3&gt;&lt;p&gt;Phytochemicals were retrieved from published literature and the Collection of Open Natural Products database, standardized, and screened for drug-likeness and oral bioavailability. Potential protein targets were predicted and intersected with colorectal cancer-associated genes, followed by network pharmacology and functional enrichment analyses. Molecular docking, 100 ns molecular dynamics simulations, molecular mechanics Poisson-Boltzmann surface area binding energy calculations, and absorption, distribution, metabolism, excretion, and toxicity (ADMET) analyses were performed to evaluate compound-target interactions, complex stability, and pharmacological properties.&lt;/p&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;p&gt;Among 242 identified phytochemicals, 21 compounds satisfied drug-likeness and oral bioavailability criteria. Target prediction identified 435 potential protein targets of the screened phytochemicals, of which 411 overlapped with colorectal cancer-associated genes. Network analysis of the overlapping targets identified PIK3CA, PIK3CD, GNAI1, GNAI3, and SRC as key hub genes. Functional enrichment analysis suggested that these targets are involved in cancer-relevant signaling pathways, including the phosphatidylinositol 3-kinase-protein kinase B, insulin receptor, and relaxin signaling pathways. Molecular docking identified quercetin, kaempferol, and bemadienolide as leading candidates, with strong binding affinities toward GNAI1 (-9.8 kcal/mol), GNAI3 (-9.6 kcal/mol), and PIK3CD (-8.7 kcal/mol), respectively. Molecular dynamics simulations demonstrated stable protein-ligand complexes with reduced structural fluctuations over 100 ns. Binding free energy analysis revealed favorable interactions, with quercetin-GNAI1 showing the strongest predicted binding stability (-86.2 ± 3.3 kcal/mol). Pharmacokinetic and toxicity predictions indicated high gastrointestinal absorption and generally low predicted toxicity profiles.&lt;/p&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;p&gt;This study provides computational, hypothesis-generating evidence that &lt;i&gt;Warburgia ugandensis&lt;/i&gt; phytochemicals may modulate multiple molecular targets and signaling pathways involved in colorectal cancer. Quercetin, kaempferol, and bemadienolide represent promising candidates for further experimental investigation. Nevertheless, these predictive findings require validation through in-vitro and in-vivo studies to establish their therapeutic releva","PeriodicalId":481,"journal":{"name":"Beni-Suef University Journal of Basic and Applied Sciences","volume":"15 1","pages":""},"PeriodicalIF":3.1,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1186/s43088-026-00840-0.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149132243","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}
引用次数: 0
In silico identification and design of 2-(3-methoxyphenoxy)-N-methylacetamide analogs as anti-tuberculosis transcriptional regulator (EthR) inhibitors via E-pharmacophore modeling, QSAR, docking, MMGBSA, ADMET, and molecular dynamics 2-(3-甲氧基苯氧基)- n -甲基乙酰胺类似物作为抗结核转录调节因子(EthR)抑制剂,通过e -药效团模型、QSAR、对接、MMGBSA、ADMET和分子动力学在硅上鉴定和设计
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-10-01 DOI: 10.1186/s43088-026-00827-x
Anne Jibrin, Adamu Uzairu, Imran Mohd, Gideon Adamu Shallangwa, Stephen Eyije Abechi, Abdullahi Bello Umar

Background

Tuberculosis (TB) remains a leading cause of infectious mortality worldwide, exacerbated by the emergence of multidrug-resistant strains and the dose-limiting toxicity of existing chemotherapeutics. Targeting regulatory mechanisms that potentiate current drugs offers a promising alternative strategy. EthR, a TetR-family transcriptional repressor that downregulates ethA and thereby limits ethionamide activation, has emerged as an attractive molecular target. Inhibiting EthR can enhance ethionamide efficacy while potentially reducing required dosage. Although 2-(3-methoxyphenoxy)-N-methylacetamide derivatives have been reported as EthR binders, their pharmacophoric features, structure–activity relationships, and dynamic interaction profiles remain insufficiently characterized.

Methods

In this study, a comprehensive in silico workflow was employed to design and evaluate novel 2-(3-methoxyphenoxy)-N-methylacetamide analogs as EthR inhibitors. An energetically optimized e-pharmacophore model was developed and used to virtually screen a curated compound library. Quantitative structure–activity relationship (QSAR) modeling was performed to elucidate key molecular descriptors governing inhibitory activity. High-ranking compounds were subjected to molecular docking, MM-GBSA binding free-energy calculations, ADMET prediction, and 100 ns molecular dynamics (MD) simulations to assess binding stability and drug-likeness.

Results

The generated e-pharmacophore hypothesis effectively captured essential steric and electronic features required for EthR inhibition. The QSAR model demonstrated robust predictive performance (R² = 0.8289; Q² = 0.6383), revealing a strong correlation between functional-group distribution and bioactivity. Docking studies identified several analogs with high affinity for the hydrophobic regulatory pocket of EthR, stabilized by persistent hydrogen-bond interactions with key residues including Trp103, Asn179, and Phe184. MMGBSA analysis confirmed favorable binding free energies ranging from − 71.43 to − 96.28 kcal/mol. The selected hits exhibited acceptable pharmacokinetic properties and low predicted toxicity. MD simulations further demonstrated conformational stability of the protein-ligand complexes, with low RMSD fluctuations and sustained intermolecular interactions throughout the simulation period.

Conclusions

This integrative computational investigation identifies 2-(3-methoxyphenoxy)-N-methylacetamide analogs as promising EthR inhibitors with favorable binding energetics, stability, and drug-like characteristics. By elucidating their pharmacophoric requirements and dynamic binding behavior, the study provides a mechanistically informed framework for the rational development of EthR-targeted adjunct therapies, offering a viable pathway toward improved anti-tuberculosis treatment strategies.

结核病(TB)仍然是世界范围内传染性死亡的主要原因,多药耐药菌株的出现和现有化疗药物的剂量限制性毒性加剧了结核病。靶向调节机制,增强现有药物提供了一个有希望的替代策略。EthR是一种ter家族转录抑制因子,可下调乙烷,从而限制乙酰胺的激活,已成为一个有吸引力的分子靶标。抑制乙醚可以增强乙酰胺的功效,同时可能减少所需的剂量。虽然2-(3-甲氧基苯氧基)- n -甲基乙酰胺衍生物已被报道作为乙醚粘合剂,但其药效特征、构效关系和动态相互作用谱仍未得到充分的表征。方法在本研究中,采用一个综合的计算机工作流来设计和评估新的2-(3-甲氧基苯氧基)- n -甲基乙酰胺类似物作为乙醚抑制剂。开发了一个能量优化的电子药效团模型,并用于虚拟筛选一个精心筛选的化合物库。通过定量构效关系(QSAR)建模来阐明控制抑制活性的关键分子描述子。高阶化合物进行分子对接、MM-GBSA结合自由能计算、ADMET预测和100 ns分子动力学(MD)模拟,以评估结合稳定性和药物相似性。结果生成的e-药效团假说有效地捕获了抑制乙醚受体所需的基本空间和电子特征。QSAR模型显示出稳健的预测性能(R²= 0.8289;Q²= 0.6383),表明功能基团分布与生物活性之间存在很强的相关性。对接研究发现了几种对EthR疏水调控口袋具有高亲和力的类似物,这些类似物通过与Trp103、Asn179和Phe184等关键残基的持续氢键相互作用来稳定。MMGBSA分析证实了有利的结合自由能范围为- 71.43 ~ - 96.28 kcal/mol。选定的命中表现出可接受的药代动力学性质和低预测毒性。MD模拟进一步证明了蛋白质-配体复合物的构象稳定性,在整个模拟期间具有低RMSD波动和持续的分子间相互作用。这项综合计算研究确定了2-(3-甲氧基苯氧基)- n -甲基乙酰胺类似物是有前途的乙醚抑制剂,具有良好的结合能量学、稳定性和药物样特性。通过阐明它们的药效需求和动态结合行为,本研究为合理开发靶向ethrr的辅助疗法提供了机制信息框架,为改进抗结核治疗策略提供了可行途径。
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引用次数: 0
Existence and Hyers-Ulam stability of a coupled fractional differential system involving the ({rm{Psi }})-Caputo derivative and mixed boundary conditions 含有({rm{Psi }}) -Caputo导数和混合边界条件的耦合分数阶微分系统的存在性和Hyers-Ulam稳定性
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-09-30 DOI: 10.1186/s43088-026-00828-w
Ouarda Saifia, Adel Lachouri, Mohammad Esmael Samei

In this study, the Banach contraction principle and Schaefer’s fixed point theorem are employed to establish, respectively, the uniqueness and existence of solutions for a coupled fractional differential system subject to mixed boundary conditions. These conditions consist of Dirichlet conditions and nonlocal fractional integral conditions involving the (Psi)-Riemann-Liouville fractional integral evaluated at the interior point (gamma). Furthermore, the Hyers-Ulam stability of the proposed system is examined. Finally, an illustrative example is provided to support the theoretical findings.

本文利用Banach收缩原理和Schaefer不动点定理分别建立了一类耦合分数阶微分系统在混合边界条件下解的唯一性和存在性。这些条件由Dirichlet条件和非局部分数积分条件组成,涉及(Psi) -Riemann-Liouville分数积分在内部点(gamma)处求值。进一步,对所提系统的Hyers-Ulam稳定性进行了检验。最后,给出了一个实例来支持理论发现。
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引用次数: 0
Lycopene partially ameliorates alcohol-induced sperm dysfunction and testicular toxicity in male Wistar rats 番茄红素部分改善雄性Wistar大鼠酒精诱导的精子功能障碍和睾丸毒性
IF 3.1 Q2 MULTIDISCIPLINARY SCIENCES Pub Date : 2026-09-29 DOI: 10.1186/s43088-026-00843-x
Oore-oluwapo Ololade Daramola, Adekunle Wahab Oyeyemi, Adeniran O. Akinola, Miracle Deborah Adeniyi, Ayomikun Joyce Tomomewo, Divine Ndako, Jesutofunmi Oguntimehin, Babatunde Oguntimehin, Dayo Rotimi Omotoso

Background

Alcohol consumption predisposes one to various hazards like reproductive toxicity. Lycopene, a carotenoid with antioxidant capacity credited with the ability to decrease oxidative stress has been reportedly used to ameliorate reproductive damage in experimental animals. This research investigated the mitigating abilities of lycopene administration on reproductive toxicity caused by alcohol in male Wistar rats.

Methods

Twenty male Wistar rats (150–180 g) were grouped as follows: 1 (control; 3 mL/kg 1% tween 80), 2 (Alcohol; Alc 3.2 g/kg of 30% v/v), 3 (lycopene; Lyc10 mg/kg) and 4 (Alc + Lyc). They were orally treated for 35 days and anaesthetized on day 36. Spermatozoa were profiled microscopically. 8-hydroxydeoxyguanosine, Caspase-3 activities, BcL-2 and interleukin-1β (IL-1β) were evaluated using Enzyme Linked Immunosorbent Assay (ELISA) technique. Malondialdehyde (MDA) concentrations, superoxide dismutase (SOD) and catalase were spectrophotometrically determined and testicular histopathology was assessed. Data derived was statistically analysed, expressed as Mean ± standard error of mean (Mean ± SEM) and compared using one way analysis of variance followed by Waller-Duncan’s post-hoc test.

Result

Alcohol caused an increase in abnormal morphology of spermatozoa. It also caused an increase in MDA concentration, Caspase-3 and IL-1β expression while a decrease in SOD, catalase activities and zinc level were observed. In addition, alcohol exposure caused histopathological changes within the testicular tissue. However, lycopene administration ameliorated all the observed deleterious changes induced by alcohol exposure.

Conclusion

Lycopene improved sperm morphology, testicular catalase activity and zinc level, lowered MDA level, Caspase 3 and interleukin 1 expression and reversed testicular histopathology in rats subjected to damages caused by alcohol.

Clinical trial number

Not applicable.

饮酒会使人容易受到生殖毒性等各种危害。番茄红素是一种具有抗氧化能力的类胡萝卜素,被认为具有降低氧化应激的能力,据报道,它已被用于改善实验动物的生殖损伤。本研究探讨番茄红素对酒精致雄性Wistar大鼠生殖毒性的缓解作用。方法雄性Wistar大鼠20只(150 ~ 180 g),随机分为:1(对照组;80 ~ 80 % 1% 3 mL/kg), 2(酒精;Alc 3.2 g/kg 30% v/v), 3(番茄红素;Lyc10 mg/kg), 4 (Alc + Lyc)。口服治疗35 d, 36 d麻醉。显微镜下观察精子。采用酶联免疫吸附法(ELISA)检测8-羟基脱氧鸟苷、Caspase-3活性、BcL-2和白细胞介素-1β (IL-1β)。分光光度法测定丙二醛(MDA)浓度、超氧化物歧化酶(SOD)和过氧化氢酶(过氧化氢酶),并评估睾丸组织病理学。对所得数据进行统计学分析,以均数±标准差(Mean±SEM)表示,并采用单向方差分析和沃勒-邓肯事后检验进行比较。结果酒精引起精子形态异常增加。MDA浓度、Caspase-3和IL-1β表达升高,SOD、过氧化氢酶活性和锌水平降低。此外,酒精暴露引起睾丸组织内的组织病理学改变。然而,番茄红素改善了所有观察到的由酒精暴露引起的有害变化。结论番茄红素能改善酒精损伤大鼠精子形态、睾丸过氧化氢酶活性和锌水平,降低丙二醛(MDA)水平、Caspase 3和白细胞介素1 (interleukin 1)表达,逆转睾丸组织病理学。临床试验编号不适用。
{"title":"Lycopene partially ameliorates alcohol-induced sperm dysfunction and testicular toxicity in male Wistar rats","authors":"Oore-oluwapo Ololade Daramola,&nbsp;Adekunle Wahab Oyeyemi,&nbsp;Adeniran O. Akinola,&nbsp;Miracle Deborah Adeniyi,&nbsp;Ayomikun Joyce Tomomewo,&nbsp;Divine Ndako,&nbsp;Jesutofunmi Oguntimehin,&nbsp;Babatunde Oguntimehin,&nbsp;Dayo Rotimi Omotoso","doi":"10.1186/s43088-026-00843-x","DOIUrl":"10.1186/s43088-026-00843-x","url":null,"abstract":"<div><h3>Background</h3><p>Alcohol consumption predisposes one to various hazards like reproductive toxicity. Lycopene, a carotenoid with antioxidant capacity credited with the ability to decrease oxidative stress has been reportedly used to ameliorate reproductive damage in experimental animals. This research investigated the mitigating abilities of lycopene administration on reproductive toxicity caused by alcohol in male Wistar rats.</p><h3>Methods</h3><p>Twenty male Wistar rats (150–180 g) were grouped as follows: 1 (control; 3 mL/kg 1% tween 80), 2 (Alcohol; Alc 3.2 g/kg of 30% v/v), 3 (lycopene; Lyc10 mg/kg) and 4 (Alc + Lyc). They were orally treated for 35 days and anaesthetized on day 36. Spermatozoa were profiled microscopically. 8-hydroxydeoxyguanosine, Caspase-3 activities, <i>BcL-2</i> and interleukin-1β (IL-1β) were evaluated using Enzyme Linked Immunosorbent Assay (ELISA) technique. Malondialdehyde (MDA) concentrations, superoxide dismutase (SOD) and catalase were spectrophotometrically determined and testicular histopathology was assessed. Data derived was statistically analysed, expressed as Mean ± standard error of mean (Mean ± SEM) and compared using one way analysis of variance followed by Waller-Duncan’s post-hoc test.</p><h3>Result</h3><p>Alcohol caused an increase in abnormal morphology of spermatozoa. It also caused an increase in MDA concentration, Caspase-3 and IL-1β expression while a decrease in SOD, catalase activities and zinc level were observed. In addition, alcohol exposure caused histopathological changes within the testicular tissue. However, lycopene administration ameliorated all the observed deleterious changes induced by alcohol exposure.</p><h3>Conclusion</h3><p>Lycopene improved sperm morphology, testicular catalase activity and zinc level, lowered MDA level, Caspase 3 and interleukin 1 expression and reversed testicular histopathology in rats subjected to damages caused by alcohol.</p><h3>Clinical trial number</h3><p>Not applicable.</p></div>","PeriodicalId":481,"journal":{"name":"Beni-Suef University Journal of Basic and Applied Sciences","volume":"15 1","pages":""},"PeriodicalIF":3.1,"publicationDate":"2026-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1186/s43088-026-00843-x.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149133137","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}
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Beni-Suef University Journal of Basic and Applied Sciences
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