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Antidiabetic, anti-inflammatory, antioxidant, and cytotoxicity potentials of green-synthesized zinc oxide nanoparticles using the aqueous extract of Helichrysum cymosum. 利用腊菊水提取物绿色合成的氧化锌纳米颗粒的抗糖尿病、抗炎、抗氧化和细胞毒性潜力。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-12-01 Epub Date: 2024-11-04 DOI: 10.1007/s13205-024-04125-0
Achasih Q Nkemzi, Kunle Okaiyeto, Omolola Oyenihi, Chinyerum S Opuwari, Okobi E Ekpo, Oluwafemi O Oguntibeju

The current research involved the synthesis of zinc oxide nanoparticles (ZnO-NPs) using an aqueous extract of Helichrysum cymosum shoots, and subsequent characterization via different analytical methods, such as UV-Vis spectroscopy, Scanning electron microscope (SEM), Energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), Transmission electron microscope (TEM), and zeta potential. The biological effects of the ZnO-NPs were then tested against C3A hepatocyte cells and L6 myocyte cell lines via series of analysis, including cytotoxicity, antioxidant, anti-inflammatory, and antidiabetic effect via enzymatic inhibition. The UV-Vis analysis showed a maximum absorption spectrum at 360, and the TEM analysis reveals a spherical and hexagonal structures, with an average dimension of 28.05-58.3 nm, and the XRD reveals a crystalline hexagonal structure. The zeta potential evaluation indicated that the ZnO-NPs are relatively stable at - 20 mV, and the FTIR analysis identified some important functional group associated with phenolics, carboxylic acid, and amides that are responsible for reducing and stabilizing the ZnO-NPs. The synthesized ZnO-NPs demonstrated cytotoxic effects on the cell lines at higher concentrations (125 µg/mL and 250 µg/mL), complicating the interpretation of the results of the inflammatory and antioxidant assays. However, there was a significant (p < 0.05) increase in the inhibitions of pancreatic lipase, alpha-glucosidase, and alpha-amylase, indicating beneficial antidiabetic effects.

目前的研究涉及利用腊菊嫩枝的水提取物合成氧化锌纳米颗粒(ZnO-NPs),并随后通过不同的分析方法进行表征,如紫外可见光谱、扫描电子显微镜(SEM)、能量色散 X 射线光谱(EDX)、X 射线衍射(XRD)、透射电子显微镜(TEM)和 zeta 电位。然后,通过一系列分析,包括细胞毒性、抗氧化、抗炎和酶抑制抗糖尿病作用,测试了 ZnO-NPs 对 C3A 肝细胞和 L6 肌细胞的生物效应。紫外可见光谱分析显示,该化合物在 360 波长处有最大吸收光谱;TEM 分析显示,该化合物呈球形和六边形结构,平均尺寸为 28.05-58.3 nm;XRD 显示,该化合物呈结晶六边形结构。zeta电位评估表明,ZnO-NPs在- 20 mV下相对稳定,傅立叶变换红外光谱分析确定了一些与酚类、羧酸和酰胺相关的重要官能团,它们是还原和稳定ZnO-NPs的主要成分。合成的 ZnO-NPs 在较高浓度(125 微克/毫升和 250 微克/毫升)时对细胞系有细胞毒性作用,这使得炎症和抗氧化检测结果的解释变得复杂。然而,在较高浓度下(125 微克/毫升和 250 微克/毫升),锰氧化物对细胞株的细胞毒性作用明显(p
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引用次数: 0
Nanomaterial-enabled drug transport systems: a comprehensive exploration of current developments and future avenues in therapeutic delivery. 纳米材料药物传输系统:全面探索治疗传输的当前发展和未来途径。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-12-01 Epub Date: 2024-11-04 DOI: 10.1007/s13205-024-04135-y
Shatabdi Basu, Pragnya Biswas, Mariya Anto, Nandini Singh, Koel Mukherjee

Over the years, nanotechnology has gained popularity as a viable solution to address gene and drug delivery challenges over conventional methods. Extensive research has been conducted on nanosystems that consist of organic/inorganic materials, drugs, and its biocompatibility become the primary goal of improving drug delivery. Various surface modification methods help focus targeted and controlled drug release, further enabling multidrug delivery also. This newer technology ensures the stability of drugs that can unravel the mechanisms involved in cellular processes of disease development and its management. Tailored medication delivery provides benefits such as therapy, controlled release, and reduced adverse effects, which are especially important for controlling illnesses like cancer. However, multifunctional nanocarriers that possess high viscoelasticity, extended circulation half-life, biocompatibility, and biodegradability face some challenges and limitations too in human bodies. To produce a consistent therapeutic platform based on complex three-dimensional nanoparticles, careful design and engineering, thorough orthogonal analysis methods, and reproducible scale-up and manufacturing processes will be required in the future. Safety and effectiveness of nano-based drug delivery should be thoroughly investigated in preclinical and clinical trials, especially when considering biodistribution, targeting specific areas, and potential immunological toxicities. Overall, the current review article explores the advancements in nanotechnology, specific to nanomaterial-enabled drug delivery systems, carrier fabrication techniques and modifications, disease management, clinical research, applications, limitations, and future challenges. The work portrays how nanomedicine distribution affects healthcare with an emphasis on the developments in drug delivery techniques.

多年来,与传统方法相比,纳米技术作为解决基因和药物递送难题的一种可行方案,已逐渐受到人们的青睐。人们对由有机/无机材料、药物及其生物相容性组成的纳米系统进行了广泛的研究,并将其作为改善药物输送的首要目标。各种表面改性方法有助于有针对性地控制药物释放,进一步实现多药给药。这种更新的技术可确保药物的稳定性,从而揭示疾病发生和治疗的细胞过程所涉及的机制。量身定制的给药方式具有治疗、控制释放和减少不良反应等优点,这对于控制癌症等疾病尤为重要。然而,具有高粘弹性、延长循环半衰期、生物相容性和生物降解性的多功能纳米载体在人体中也面临着一些挑战和限制。要生产出基于复杂三维纳米颗粒的稳定治疗平台,未来需要精心设计和工程设计、全面的正交分析方法以及可重复的放大和制造工艺。应在临床前和临床试验中对纳米给药的安全性和有效性进行彻底研究,尤其是在考虑生物分布、靶向特定区域和潜在免疫毒性时。总之,本综述文章探讨了纳米技术的发展,特别是纳米材料给药系统、载体制造技术和改性、疾病管理、临床研究、应用、局限性和未来挑战。文章以给药技术的发展为重点,描绘了纳米医学的分布如何影响医疗保健。
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引用次数: 0
Bioinformatics analysis and experimental validation of the oncogenic role of COL11A1 in pan-cancer. COL11A1在泛癌症中致癌作用的生物信息学分析和实验验证。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-12-01 Epub Date: 2024-11-04 DOI: 10.1007/s13205-024-04133-0
Xiaofeng Wan, Qingmei Deng, Anling Chen, Xinhui Zhang, Wulin Yang

The intricate expression patterns and oncogenic attributes of COL11A1 across different cancer types remain largely elusive. This study used several public databases (TCGA, GTEx, and CCLE) to investigate the pan-cancer landscape of COL11A1 expression, its prognostic implications, interplay with the immune microenvironment, and enriched signaling cascades. Concurrently, western blot analyses were performed to verify COL11A1 expression in lung adenocarcinoma (LUAD) cell lines and clinical samples. In addition, COL11A1 knockout cell lines were generated to scrutinize the functional consequences of COL11AI expression on cancer cell behavior by use MTT, colony formation, and scratch wound healing assays. A comprehensive database investigation revealed that COL11A1 was upregulated in a majority of tumor tissues and its expression was highly correlated with a patient's prognosis. Notably, genetic alterations in COL11A1 predominantly occurred as mutations, while its DNA methylation status inversely mirrored gene expression levels across multiple promoter regions. Our findings suggest that COL11A1 helps to modulate the tumor immune landscape and potentially acts through the epithelial-mesenchymal transition (EMT) pathway to exert its oncogenic function. Western blot analyses further substantiated the specific upregulation of COL11A1 in LUAD cell lines and tissues, suggesting a close association with the EMT process. Ablation of COL11A1 in cancer cells significantly reduced their proliferative, clonogenic, and migratory abilities, underscoring the functional significance of COL11A1 in tumor cell behavior. Collectively, this research revealed the prevalent overexpression of COL11A1 in pan-cancer tissues, its profound prognostic and microenvironmental correlations, and the mechanistic underpinnings of its tumor-promoting effects as mediated via EMT signaling. Our findings suggest that COL11A1 could serve as a prognostic and diagnostic biomarker and therapeutic target for cancer.

COL11A1在不同癌症类型中错综复杂的表达模式和致癌属性在很大程度上仍然难以捉摸。本研究利用几个公共数据库(TCGA、GTEx 和 CCLE)研究了 COL11A1 的泛癌症表达、其预后影响、与免疫微环境的相互作用以及丰富的信号级联。同时,还进行了 Western 印迹分析,以验证 COL11A1 在肺腺癌(LUAD)细胞系和临床样本中的表达。此外,研究人员还生成了 COL11A1 基因敲除细胞系,通过 MTT、菌落形成和划痕伤口愈合试验来研究 COL11AI 表达对癌细胞行为的功能性影响。一项全面的数据库调查显示,COL11A1在大多数肿瘤组织中上调,其表达与患者的预后高度相关。值得注意的是,COL11A1的基因改变主要表现为突变,而其DNA甲基化状态与多个启动子区域的基因表达水平成反比。我们的研究结果表明,COL11A1有助于调节肿瘤免疫格局,并可能通过上皮-间质转化(EMT)途径发挥其致癌功能。Western印迹分析进一步证实了COL11A1在LUAD细胞系和组织中的特异性上调,表明它与EMT过程密切相关。在癌细胞中消减 COL11A1 能明显降低其增殖、克隆和迁移能力,凸显了 COL11A1 在肿瘤细胞行为中的功能意义。总之,这项研究揭示了 COL11A1 在泛癌症组织中的普遍过表达、其与预后和微环境的密切关系,以及其通过 EMT 信号介导的肿瘤促进作用的机理基础。我们的研究结果表明,COL11A1 可作为癌症的预后和诊断生物标志物及治疗靶点。
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引用次数: 0
Recent advances in the synthesis of antidepressant derivatives: pharmacologic insights for mood disorders. 抗抑郁衍生物合成的最新进展:情绪障碍的药理学启示。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-05 DOI: 10.1007/s13205-024-04104-5
Jeetendra Kumar Gupta, Kuldeep Singh, Alok Bhatt, Prateek Porwal, Rekha Rani, Anubhav Dubey, Divya Jain, Sachchida Nand Rai

Mood disorders, including depression, remain a significant global health concern, necessitating continuous efforts to develop novel and more effective antidepressant therapies. Although there have been significant advancements in comprehending the biology of Major Depressive Disorder (MDD), a considerable number of people suffering from depression do not exhibit positive responses to the pharmacologic treatments now available. This study specifically examines emerging targets and potential future approaches for pharmaceutical interventions in the treatment of MDD. The discussion revolves around novel therapeutic agents and their effectiveness in treating depression. The focus is on the specific pathophysiological pathways targeted by these agents and the amount of evidence supporting their use. While conventional antidepressants are anticipated to continue being the primary treatment for MDD in the foreseeable future, there is currently extensive research being conducted on numerous new compounds to determine their effectiveness in treating MDD. Many of these compounds have shown encouraging results. This review highlighted the recent advances in the synthesis of antidepressant derivatives and explores their pharmacologic insights for the treatment of mood disorders.

包括抑郁症在内的情绪障碍仍然是全球关注的重大健康问题,因此有必要不断努力开发新的、更有效的抗抑郁疗法。尽管在理解重度抑郁症(MDD)的生物学特性方面取得了重大进展,但仍有相当多的抑郁症患者对现有的药物治疗没有表现出积极的反应。本研究特别探讨了治疗 MDD 的药物干预的新目标和未来潜在方法。讨论围绕新型治疗药物及其治疗抑郁症的有效性展开。重点在于这些药物所针对的特定病理生理途径以及支持其使用的证据数量。虽然在可预见的未来,传统抗抑郁药仍将是治疗 MDD 的主要药物,但目前正在对大量新化合物进行广泛研究,以确定它们对治疗 MDD 的有效性。其中许多化合物都取得了令人鼓舞的成果。本综述重点介绍了抗抑郁衍生物合成方面的最新进展,并探讨了它们在治疗情绪障碍方面的药理作用。
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引用次数: 0
Advancing epigenetic profiling in cervical cancer: machine learning techniques for classifying DNA methylation patterns. 推进宫颈癌的表观遗传学分析:对 DNA 甲基化模式进行分类的机器学习技术。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-09 DOI: 10.1007/s13205-024-04107-2
Apoorva, Vikas Handa, Shalini Batra, Vinay Arora

This study investigates the ability to predict DNA methylation patterns in cervical cancer cells using decision-tree-based ensemble approaches and neural network-based models. The research findings suggest that a model based on random forest achieves a significant prediction accuracy of 91.35%. This projection was derived from comprehensive experimentation and a meticulous performance evaluation of the random forest model, employing a range of measures including Accuracy, Sensitivity, Specificity, Matthews Correlation Coefficient, F1-score, Recall, and Precision. The results indicate that the random forest model exhibits superior performance compared to other tree-based models such as the Simple Decision Tree and XGBoost, as well as neural network-based models including Convolutional Neural Networks, Feed Forward Networks, and Wavelet Neural Networks. The findings indicate that using random forest-based techniques has great potential for future study and might be highly valuable in clinical applications, especially in improving diagnostic and treatment strategies based on epigenetic profiles.

本研究调查了使用基于决策树的集合方法和基于神经网络的模型预测宫颈癌细胞中 DNA 甲基化模式的能力。研究结果表明,基于随机森林的模型的预测准确率高达 91.35%。这一预测结果来自对随机森林模型的全面实验和细致的性能评估,采用了一系列衡量标准,包括准确度、灵敏度、特异度、马修斯相关系数、F1-分数、召回率和精确度。结果表明,与其他基于树的模型(如简单决策树和 XGBoost)以及基于神经网络的模型(包括卷积神经网络、前馈网络和小波神经网络)相比,随机森林模型表现出更优越的性能。研究结果表明,使用基于随机森林的技术具有巨大的研究潜力,在临床应用中可能极具价值,特别是在改进基于表观遗传特征的诊断和治疗策略方面。
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引用次数: 0
Biohydrogen production from co-substrates through dark fermentation by bacterial consortium. 细菌联合体通过暗发酵从共底物中生产生物氢。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-25 DOI: 10.1007/s13205-024-04106-3
Chelladurai Mumtha, Pambayan Ulagan Mahalingam

Hydrogen is a clean energy carrier that can be used as fuel for fuel cells. Dark fermentative biohydrogen production with other waste biomass needs to be explored as an alternative for sustainable biohydrogen production in future. In this study, lab-scale bioreactor were carried out to produce biohydrogen from co-substrates using bacterial consortium at 37 ℃. For the experimental setup, a 1-L-working-volume reactor was used for biohydrogen production by bacterial monocultures and consortium on co-substrates. A batch experiment was performed at 37 °C with an initial pH of 7.0 and a mixing ratio of 600:300 between dairy whey and sugarcane bagasse. Total solids (TS), volatile solids (VS), total chemical oxygen demand (TCOD), soluble chemical oxygen demand (SCOD), and hydrogen production rate (HPR) were determined from co-substrates during the dark fermentation process. Morphologic changes of biohydrogen producing bacteria binds on co-substrates after the fermentation process were determined using SEM imaging. The bacteria can degrade the substrate when they attach to it causing hole formation and cracked the surface area. The level of biohydrogen production by bacterial consortium was observed and the results revealed a hydrogen production rate of 35.9 mL H2/L/h. In fermentative H2 production, it is quite similar to that of most H2-producing bacteria previously studied, especially that of the bacterial consortium, and this indicates that the attempt to find an outstanding bacterial strain for fermentative H2 production might be very difficult if not impossible.

氢是一种清洁能源载体,可用作燃料电池的燃料。需要探索利用其他废弃生物质进行暗发酵生物制氢,作为未来可持续生物制氢的替代方法。本研究采用实验室规模的生物反应器,利用细菌群在 37 ℃ 下从共基质中生产生物氢。在实验设置中,使用了一个工作容积为 1 升的反应器,通过细菌单培养基和联合培养基生产生物氢。批量实验在 37 °C、初始 pH 值为 7.0、乳清和甘蔗渣的混合比例为 600:300 的条件下进行。在暗发酵过程中测定了共底物的总固体(TS)、挥发性固体(VS)、总化学需氧量(TCOD)、可溶性化学需氧量(SCOD)和产氢率(HPR)。利用扫描电镜成像技术测定了发酵过程后结合在共底物上的生物产氢菌的形态变化。当细菌附着在基质上时,会导致基质降解,形成孔洞并使表面积开裂。观察了细菌群的生物制氢水平,结果显示制氢率为 35.9 mL H2/L/h。在发酵产氢方面,它与之前研究的大多数产氢细菌(尤其是细菌联合体)的产氢率十分相似,这表明要找到一种优秀的发酵产氢细菌菌株可能非常困难,甚至不可能。
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引用次数: 0
Correction: Genome-wide identification and characterization of glutathione S-transferase gene family in quinoa (Chenopodium quinoa Willd.). 更正:藜麦(Chenopodium quinoa Willd.)
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-12 DOI: 10.1007/s13205-024-04076-6
Shivani Tiwari, Swati Vaish, Nootan Singh, Mahesh Basantani, Atul Bhargava

[This corrects the article DOI: 10.1007/s13205-023-03659-z.].

[此处更正了文章 DOI:10.1007/s13205-023-03659-z]。
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引用次数: 0
Pharmacokinetic predictions of ROS-mediated targets and genotoxin combinations via multiple ligand simultaneous docking and ROS evaluation in vitro using HepG2 cell lines. 利用 HepG2 细胞系,通过多配体同时对接和 ROS 体外评估,对 ROS 介导的靶标和基因毒素组合进行药代动力学预测。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-14 DOI: 10.1007/s13205-024-04109-0
C P Sri Snehaa, Praveen Kumar Issac, Palanisamy Rajaguru, Velan Pugalenthi

Although combination therapy is known for its high efficacy, reduced side effects and drug resistance, toxicity remains a major drawback. Some of the genes are likely to induce hepatotoxicity through ROS-mediated mechanisms when a drug is metabolized alone or in combination in the liver. To address this, we have developed a scientific approach to predict the toxicity of different genotoxin combinations and validate their interactions with various targets. The current study is an extensive study of our previous set of in vivo rat liver microarray data processed using R studio for their functional analysis. About five combinations of genotoxins such as CPT/ETP, CPT/CPL, ETP/CPL, CP/CPT and EES/CP along with their differential gene expression targeting Chemical carcinogenesis-ROS are chosen for this study. We aim to examine the binding affinity of different genotoxin combinations using in silico multiple ligand simultaneous docking (MLSD) and are then bio-evaluated for cytotoxicity in vitro using human hepatocellular carcinoma cell lines (HepG2) with the MTT assay. As a result, dose-response cytotoxicity with its strength of interactions and a significant variance in ROS levels in the treated cells is observed compared to their IC50 values. Out of 5 combinations such as CPT/CPL, ETP/CPL and EES/CP are found not only to be significantly cytotoxic but also induce oxidative stress specifically above their IC50 values with good and moderate binding interactions ensuring their toxicity. On the contrary, the safe combinations are found to be CTP/ETP and CP/CPT possibly with no and tolerable adverse effects standing as preliminary information for researchers in drug design and development.

尽管联合疗法以疗效高、副作用小和耐药性低而著称,但毒性仍然是其主要缺点。当药物在肝脏中单独或联合代谢时,其中一些基因很可能通过 ROS 介导的机制诱发肝毒性。为此,我们开发了一种科学方法来预测不同基因毒素组合的毒性,并验证它们与各种靶点的相互作用。目前的研究是对我们之前使用 R studio 处理的一组体内大鼠肝脏微阵列数据进行功能分析的广泛研究。本研究选择了五种基因毒素组合,如 CPT/ETP、CPT/CPL、ETP/CPL、CP/CPT 和 EES/CP,以及它们针对化学癌变-ROS 的不同基因表达。我们的目的是利用硅学多配体同时对接(MLSD)技术研究不同基因毒素组合的结合亲和力,然后使用 MTT 法对人肝癌细胞株(HepG2)进行体外细胞毒性生物评估。结果,观察到剂量-反应细胞毒性及其相互作用的强度,以及与它们的 IC50 值相比,处理细胞中 ROS 水平的显著差异。在 CPT/CPL、ETP/CPL 和 EES/CP 等 5 种组合中,发现它们不仅具有显著的细胞毒性,而且还能诱导氧化应激,其毒性明显高于其 IC50 值,其良好和适度的结合相互作用确保了它们的毒性。相反,CTP/ETP 和 CP/CPT 被认为是安全的组合,它们可能不会产生任何不良影响,而且是可以承受的,这为研究人员进行药物设计和开发提供了初步信息。
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引用次数: 0
Editorial Expression of Concern: Two species of Ulva inhibits the progression of cervical cancer cells SiHa by means of autophagic cell death induction. 社论表达关注:两种莼菜通过诱导自噬细胞死亡抑制宫颈癌细胞SiHa的进展。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-24 DOI: 10.1007/s13205-024-04115-2
Asmita Pal, Preeti Verma, Subhabrata Paul, Indira Majumder, Rita Kundu
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引用次数: 0
Enhancing glioblastoma cytotoxicity through encapsulating O6-benzylguanine and temozolomide in PEGylated liposomal nanocarrier: an in vitro study. 通过在 PEG 化脂质体纳米载体中封装 O6-苄基鸟嘌呤和替莫唑胺来增强胶质母细胞瘤的细胞毒性:一项体外研究。
IF 2.6 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Pub Date : 2024-11-01 Epub Date: 2024-10-23 DOI: 10.1007/s13205-024-04123-2
Manasa Manjunath Hegde, Pranoti Palkar, Sadhana P Mutalik, Srinivas Mutalik, Jayant Sastri Goda, B S Satish Rao

Glioblastoma (GBM) (grade IV glioma) is the most fatal brain tumor, with a median survival of just 14 months despite current treatments. Temozolomide (TMZ), an alkylating agent used with radiation, faces challenges such as systemic toxicity, poor absorption, and drug resistance. To enhance TMZ effectiveness, we developed poly(ethylene glycol) (PEG) liposomes co-loaded with TMZ and O6-benzylguanine (O6-BG) for targeted glioma therapy. These liposomes, prepared using the thin-layer hydration method, had an average size of 146.33 ± 6.75 nm and a negative zeta potential (-49.6 ± 3.1 mV). Drug release was slower at physiological pH, with 66.84 ± 4.62% of TMZ and 69.70 ± 2.88% of O6-BG released, indicating stability at physiological conditions. The liposomes showed significantly higher cellular uptake (p < 0.05) than the free dye. The dual drug-loaded liposomes exhibited superior cytotoxicity against U87 glioma cells, with a lower IC50 value (3.99µg/mL) than the free drug combination, demonstrating enhanced anticancer efficacy. The liposome formulation induced higher apoptosis (19.42 ± 3.5%) by causing sub-G0/G1 cell cycle arrest. The novelty of our study lies in co-encapsulating TMZ and O6-BG within PEGylated liposomes, effectively overcoming drug resistance and improving targeted delivery for glioma treatment.

Supplementary information: The online version contains supplementary material available at 10.1007/s13205-024-04123-2.

胶质母细胞瘤(GBM)(IV 级胶质瘤)是最致命的脑肿瘤,尽管目前有多种治疗方法,但中位生存期仅为 14 个月。替莫唑胺(TMZ)是一种与放射线配合使用的烷化剂,它面临着全身毒性、吸收不良和耐药性等挑战。为了提高TMZ的疗效,我们开发了共载TMZ和O6-苄基鸟嘌呤(O6-BG)的聚乙二醇(PEG)脂质体,用于胶质瘤的靶向治疗。这些脂质体采用薄层水合法制备,平均尺寸为 146.33 ± 6.75 nm,Zeta 电位为负(-49.6 ± 3.1 mV)。在生理 pH 值下,药物释放速度较慢,TMZ 和 O6-BG 的释放量分别为 66.84 ± 4.62% 和 69.70 ± 2.88%,这表明脂质体在生理条件下是稳定的。脂质体的细胞吸收率(p 50 值(3.99µg/mL))明显高于游离药物组合,表明抗癌功效增强。脂质体制剂通过引起亚 G0/G1 细胞周期停滞,诱导更多细胞凋亡(19.42 ± 3.5%)。我们研究的新颖之处在于将TMZ和O6-BG共同包裹在PEG化脂质体中,有效克服了耐药性,提高了胶质瘤治疗的靶向给药效果:在线版本包含补充材料,可查阅 10.1007/s13205-024-04123-2。
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引用次数: 0
期刊
3 Biotech
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