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Iron(III) Monoglycerolate: A Potential Hemostatic Agent for Topical Application 单甘酯酸铁(III):一种潜在的局部应用止血剂
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-09 DOI: 10.2174/0115734072295011240425080837
Tat’yana Khonina, Alexander Safronov, M. Bulatova, L. Larionov, Irina Antropova, M. Dobrinskaya, N. Izmozherova, D. Tishin, Semyon Alekseenko, E. Bogdanova, Maxim Karabanalov, O. Chupakhin
Glycerolates of biogenic elements are of interest because of their pharmacologicalactivity. Some of them are used as active substances in agents for topical applicationand as biocompatible precursors in sol-gel synthesis of bioactive materials.In this work, morphostructural feature, ability to hydrolyze, and the pharmacologicalactivity of previously synthesized iron(III) monoglycerate were studied.Analytical techniques, including SEM, TEM, XRD, TGA, IR spectroscopy, DLS andELS, were used. Hemostatic activity was studied in vivo, and primary toxicological studies werecarried out on experimental animals. Antimicrobial activity was studied using the agar diffusionmethod.When dispersed in glycerol, solid crystalline iron(III) monoglycerolate transforms intoan amorphous state, forming aggregates with an average particle size of 250 nm (according toDLS data). It slowly hydrolyzes in water at room temperature, while hydrolysis does not takeplace in an aqueous glycerol media. Iron(III) monoglycerolate is nontoxic and exhibits pronouncedhemostatic activity and low antibacterial activity (relative to the strain S. аureus).Iron(III) monoglycerolate can be considered a potential hemostatic agent, showingpromise for topical application in medical and veterinary practice, as well as a novel biocompatibleprecursor in the sol-gel synthesis of practically useful substances.
生物元素甘油酯因其药理活性而备受关注。本研究使用了扫描电镜、电子显微镜、XRD、TGA、红外光谱、DLS 和ELS 等分析技术,研究了先前合成的单(III)甘油酸铁的形态结构特征、水解能力和药理活性。对体内止血活性进行了研究,并对实验动物进行了初级毒理学研究。当分散在甘油中时,固体结晶单甘酯酸铁(III)会转变为无定形状态,形成平均粒径为 250 nm 的聚集体(根据 DLS 数据)。在室温下,它在水中会缓慢水解,而在甘油水介质中则不会水解。单甘油酸铁(III)无毒,具有明显的止血活性和较低的抗菌活性(相对于 S. аureus 菌株而言)。单甘油酸铁(III)可被视为一种潜在的止血剂,有望在医疗和兽医实践中得到局部应用,同时也是一种新型的生物相容性前体,可用于溶胶-凝胶合成实际有用的物质。
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引用次数: 0
Anticancer Activity and GC-MS Profiling of Bioactive Constituents in the Methanolic Extracts of Spatoglossum variabile and Gracilaria corticata Spatoglossum variabile 和 Gracilaria corticata 甲醇提取物的抗癌活性和生物活性成分的气相色谱-质谱分析
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-24 DOI: 10.2174/0115734072296835240409124751
S. Sruthi, Shahjahan A, Kumaran K, Dannie Macrin, Vijay Murali RM, K.N. Aruljothi
Marine algae stand out as repositories of bioactive metabolites, widelyharnessed in treating diverse diseases. Given the often-challenging side effects associated withconventional cancer treatments, researchers are increasingly turning their attention to marine algaeas a promising source for discovering novel and potent anticancer compounds. In this study,we meticulously explored the potential anticancer activity of Spatoglossum variabile andGracilaria corticata sourced from the Indian Ocean.Marine algae are rich in bioactive metabolites that are extensively used to treat various diseases. Researchers have considered marine algae for novel and promising anticancer compounds due to the adverse effects of standard cancer treatmentsThe secondary metabolites were extracted using methanol solvent accordingto the standard protocol. The extract was subjected to GC-MS analysis and evaluated forits short- and long-term cytotoxicity and anti-proliferative ability in the HCT116 cell line usingMTT, clonogenic, and trypan blue dye exclusion assays, respectively.The methanolic extract of Spatoglossum variabile contained 21 uniqueanticancer compounds, except for the other bioactive compounds. The results indicate that increasingthe concentration of algal extracts decreased the cell viability significantly, with an IC50of 51.49 μg/mL and 37.50 μg /mL in the HCT116 cell line. The results showed a significant reductionin colorectal cancer colony formation and a gradual reduction in cell proliferation. Theseresults underscore the potential for targeted, low-toxicity biomedicines due to their selective cytotoxicityagainst cancer cells.The extract was subjected to GC-MS analysis and evaluated for its short- and long-term cytotoxicity and anti-proliferative ability in HCT116 cell line using MTT, clonogenic, and trypan blue dye exclusion assays, respectively.Our findings show that Spatoglosuum variabile & Gracilaria corticata extracts containvarious bioactive compounds, display long-term and short-term cytotoxicity and antiproliferativeeffects, which indicates that their constituent compounds might be further refinedinto effective anti-colorectal cancer medications.The methanolic extract of Spatoglossum variabile contained 21 unique anti-cancer compounds, in addition to other bioactive compounds. The results indicate that increasing the concentration of algal extracts decreased the cell viability significantly, with an IC50 of 51.49 µg/mL and 37.50 µg /ml in the HCT116 cell line. The results showed a significant reduction in colony formation and a gradual reduction in cell proliferation
海藻是生物活性代谢物的宝库,被广泛用于治疗各种疾病。鉴于传统的癌症治疗方法往往会产生令人头疼的副作用,研究人员正越来越多地把目光转向海洋藻类,认为它们是发现新型强效抗癌化合物的大有希望的来源。在这项研究中,我们对来自印度洋的 Spatoglossum variabile 和 Gracilaria corticata 的潜在抗癌活性进行了细致的探索。由于标准癌症治疗方法的不良影响,研究人员已将海洋藻类视为新型和有前景的抗癌化合物。Spatoglossum variabile 的甲醇提取物含有 21 种独特的抗癌化合物,其他生物活性化合物除外。结果表明,藻类提取物浓度的增加会显著降低细胞的活力,对 HCT116 细胞株的 IC50 为 51.49 μg /mL,对 HCT116 细胞株的 IC50 为 37.50 μg /mL。结果显示,结直肠癌细胞集落形成明显减少,细胞增殖逐渐降低。对提取物进行了 GC-MS 分析,并使用 MTT、克隆生成和胰蓝染料排除法分别评估了其在 HCT116 细胞系中的短期和长期细胞毒性及抗增殖能力。我们的研究结果表明,Spatoglossuum variabile 和 Gracilaria corticata 提取物含有多种生物活性化合物,具有长期和短期的细胞毒性和抗增殖作用,这表明它们的组成化合物有可能被进一步提炼成有效的抗结直肠癌药物。结果表明,藻类提取物浓度的增加会显著降低细胞的活力,在 HCT116 细胞系中的 IC50 为 51.49 µg/mL 和 37.50 µg /ml。结果表明,细胞集落形成明显减少,细胞增殖也逐渐减少。
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引用次数: 0
Xanthone Derivatives: A Pharmacological Panorama of Versatility 氧杂蒽酮衍生物:多用途药理学全景图
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-18 DOI: 10.2174/0115734072278162240406123303
Anuradha Mehra, Rekha Sangwan, Emmanuel Owusu
Xanthones are a class of naturally occurring compounds found in various plantsources. Over the years, studies have revealed therapeutic impending xanthones in treating andmanaging several ailments, including cancer, inflammation, and microbial infections. Xanthonesexert their therapeutic effects through various mechanisms, such as anti-inflammatory, antioxidant,and anti-proliferative activities. It has also been found that xanthones induce apoptosis, inhibitcell proliferation, and arrest cell cycles by modulating several signaling pathways. This reviewobjective is to deliver an inclusive overview of the therapeutic essence of xanthones andtheir potential use as a natural remedy for managing and treating various diseases.
氧杂蒽酮是一类存在于各种植物资源中的天然化合物。多年来的研究表明,氧杂蒽酮可治疗和控制多种疾病,包括癌症、炎症和微生物感染。氧杂蒽酮通过各种机制发挥治疗作用,如抗炎、抗氧化和抗增殖活性。研究还发现,氧杂蒽酮可通过调节多种信号通路诱导细胞凋亡、抑制细胞增殖和阻滞细胞周期。这篇综述旨在全面概述氧杂蒽酮的治疗本质,以及其作为天然疗法管理和治疗各种疾病的潜力。
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引用次数: 0
GCMS Analysis of Bioactive Compounds and Evaluation of Anti-parkinsonActivity of Leaf Extract of Curculigo orchioides in Experimental Animals 莪术叶提取物生物活性化合物的 GCMS 分析及对实验动物抗帕金森活性的评价
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-18 DOI: 10.2174/0115734072285993240403110533
U. D'Souza, Chandrashekar K.S., Shruthi R, Vasudev Pai
Curculigo orchioides Gaertn, a plant belonging to the Hypoxidaceaefamily, is well-known for its traditional uses of all plant parts. This plant is commonly knownas golden eye grass, black musli, Kali musli, or Kali Musali. Parkinson's disease is a neurodegenerative disorder that is commonly observed in older adults. It is caused by a variety of mechanisms, including neuroinflammation, which results in the loss of dopamine release when triggeredand causes motor symptoms.Ethanolic extract was prepared by shade-drying the leaves, making them into a coarsepowder, and the extract was prepared by maceration technique with the help of ethanol. GCMSanalysis and Haloperidol-induced Parkinsonism study were carried out to evaluate the antiParkinson activity in albino Wistar rats. Ethanolic extract of Curculigo orchioides was subjectedto GCMS analysis. The National Institute of Standards and Technology database was used to interpret the mass spectrum of the GC-MS. The screening models were catalepsy, rotarod and a fewin vitro models, namely the estimation of catalase acetylcholinesterase levels. The animals weredivided into 6 groups, namely control, disease, standard (levodopa), low dose (100 mg/kg p.o.),medium dose (200 mg/kg p.o.), high dose (400 mg/kg p.o.) groups having 6 animals each wereused for rotarod and catalepsy models for 14 daysThe results obtained showed a dose-dependent increase in the anti-Parkinson activity.The evaluation of neuromuscular movements of the ethanolic leaf extract of Curculigo orchioidesshowed that the pre-treatment with different ranges of dose (100 mg/ml, 200 mg/kg, and 400mg/kg) suggested a dose-dependent significant increase in fall-off time when compared with bothstandard and disease groups GCMS analysis revealed the presence of flavonoids, Vitamin andfatty acid esters.The anti-Parkinson activity of Flavonoids has been reported previously. Hence, theactivity may be attributed to kaempferol-3-O-glucuronide.
Curculigo orchioides Gaertn 是一种隶属于 Hypoxidaceaefamily 的植物,以其所有植物部分的传统用途而闻名。这种植物通常被称为金眼草、黑麝香、Kali musli 或 Kali Musali。帕金森病是一种神经退行性疾病,常见于老年人。帕金森病是一种神经退行性疾病,常见于中老年人,由多种机制引起,包括神经炎症,在触发时导致多巴胺释放丧失,引起运动症状。对白化 Wistar 大鼠进行了气相色谱分析和氟哌啶醇诱导的帕金森氏症研究,以评估其抗帕金森氏症活性。对 Curculigo orchioides 的乙醇提取物进行了 GCMS 分析。使用美国国家标准与技术研究所的数据库来解释 GC-MS 的质谱。筛选模型包括催眠、旋转木马和一些体外模型,即估算过氧化氢酶乙酰胆碱酯酶水平。将动物分为 6 组,即对照组、疾病组、标准组(左旋多巴)、低剂量组(100 毫克/千克口服)、中剂量组(200 毫克/千克口服)、高剂量组(400 毫克/千克口服),每组 6 只动物,分别进行为期 14 天的转体和催眠模型试验。对 Curculigo orchioidess 乙醇叶提取物的神经肌肉运动的评估表明,与标准组和疾病组相比,不同剂量范围(100 毫克/毫升、200 毫克/千克和 400 毫克/千克)的预处理可显著增加脱落时间。因此,这种活性可能归因于山奈酚-3-O-葡萄糖醛酸。
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引用次数: 0
Antifungal Activity of Chitosan Nanocomposites against Candida albicans:A Systematic Review 壳聚糖纳米复合材料对白色念珠菌的抗真菌活性:系统综述
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-16 DOI: 10.2174/0115734072297928240404074703
P. Shakib, Shirzad Fallahi, G. Goudarzi, Shahram Ahmadi Somaghian, Sana Amiri, Sirus Nemati Delfan, Kourosh Cheraghipour
This investigation aims to explore the potential anti-Candida albicanseffects of Chitosan nanocomposites.Researchers searched several databases, including Scopus, PubMed, Science Direct,Cochrane, and Ovid, for articles published between 2000 and 2023 using specific keywords.Of the 5,600 studies that were first searched in the databases, after removing duplicates(700 cases) and applying inclusion and exclusion criteria, 43 studies were selected for evaluationafter duplicate removal.According to studies, the anti-Candida albicans properties of chitosan nanocompositesare more than routine antifungals such as nystatin; therefore, it can be concluded that Chitosannanocomposites can be used to deal with Candida albicans.
研究人员使用特定关键词检索了 Scopus、PubMed、Science Direct、Cochrane 和 Ovid 等多个数据库中 2000 年至 2023 年间发表的文章。根据研究结果,壳聚糖纳米复合材料的抗白色念珠菌性能超过了常规抗真菌药(如奈替丁),因此可以认为壳聚糖纳米复合材料可用于治疗白色念珠菌。
{"title":"Antifungal Activity of Chitosan Nanocomposites against Candida albicans:\u0000A Systematic Review","authors":"P. Shakib, Shirzad Fallahi, G. Goudarzi, Shahram Ahmadi Somaghian, Sana Amiri, Sirus Nemati Delfan, Kourosh Cheraghipour","doi":"10.2174/0115734072297928240404074703","DOIUrl":"https://doi.org/10.2174/0115734072297928240404074703","url":null,"abstract":"\u0000\u0000This investigation aims to explore the potential anti-Candida albicans\u0000effects of Chitosan nanocomposites.\u0000\u0000\u0000\u0000Researchers searched several databases, including Scopus, PubMed, Science Direct,\u0000Cochrane, and Ovid, for articles published between 2000 and 2023 using specific keywords.\u0000\u0000\u0000\u0000Of the 5,600 studies that were first searched in the databases, after removing duplicates\u0000(700 cases) and applying inclusion and exclusion criteria, 43 studies were selected for evaluation\u0000after duplicate removal.\u0000\u0000\u0000\u0000According to studies, the anti-Candida albicans properties of chitosan nanocomposites\u0000are more than routine antifungals such as nystatin; therefore, it can be concluded that Chitosan\u0000nanocomposites can be used to deal with Candida albicans.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140695453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, Characterization, Docking Studies, and In-vitro CytotoxicActivity of Some Novel 2, 3 Disubstituted Naphthalene 1,4 DioneDerivatives 一些新型 2, 3 二取代萘 1,4 二酮衍生物的合成、表征、对接研究和体外细胞毒性活性
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-16 DOI: 10.2174/0115734072298465240403084903
Dilipkumar S, Karthik V, Gowramma B, Magesh M, Kaviarasan L
Many quinone derivatives as of now utilized for anticancer medications.Especially, 1,4-naphthoquinones are dynamic derivatives, and it was broadly utilized in unrefinedsubstances in the drugs and agrochemicals industry.In this work, we planned and combined five different moieties into 2, 3disubstituted naphthalene-1,4-dione molecules. Various spectral studies distinguished the syntheticdesigns of the produced compounds. The naphthoquinone derivatives were exposed to the primarymolecular descriptor by Molinspiration programming, and all the descriptor values are withinthe specified value.In this work, we planned and combined five different moieties into 2, 3disubstituted naphthalene-1,4-dione molecules. Various spectral studies distinguished the syntheticdesigns of the produced compounds. The naphthoquinone derivatives were exposed to the primarymolecular descriptor by Molinspiration programming, and all the descriptor values are withinthe specified value.Each of the five naphthoquinone derivatives was docked against theTopoisomerase II utilizing Auto Dock program 4.2.5. (PDB: 3L4K). The docking tells us that thestudied compounds possess significant to moderate inhibition toward the targeted enzymes.Among the studied compounds, compound L3 showed the most elevated binding score (-10.66kcal/mol with one H-bond) than the adriamycin (-9.58 kcal/mol with two H-bonds) and compoundL2 (- 9.86 kcal/mol with two H-bonds). The derivatives were tried for in-vitro cytotoxicitystudies against MCF - 7 by the SRB method. Among them, compounds L2 (28.42±3.1 μg/mL)and L3 (29.38±3.2 μg/mL) were the most significant ones when contrasted with the control Adriamycin(15.28±3.4 μg/mL).The current research indicates that the tested compounds show anticancer actionagainst the MCF-7 breast cancer cell line. Thus, the study is an attempt to advance toward theidentification of innovative anticancer drugs.
目前,许多醌类衍生物已被用于抗癌药物,尤其是 1,4-萘醌类衍生物具有很强的生命力,在药物和农用化学品行业中被广泛应用于未精制物质。各种光谱研究区分了所制化合物的合成设计。通过 Molinspiration 程序对萘醌衍生物进行了主分子描述符分析,所有描述符值均在规定值范围内。各种光谱研究区分了所生成化合物的合成设计。利用 Molinspiration 程序对萘醌衍生物进行了主分子描述,所有描述值均在指定值范围内。(PDB:3L4K)与拓扑异构酶 II 进行对接。在所研究的化合物中,化合物 L3 的结合得分最高(-10.66kcal/mol,一个 H 键),高于阿霉素(-9.58 kcal/mol,两个 H 键)和化合物 L2(-9.86 kcal/mol,两个 H 键)。采用 SRB 法对这些衍生物进行了针对 MCF - 7 的体外细胞毒性研究。与对照组阿霉素(15.28±3.4 μg/mL)相比,其中化合物 L2(28.42±3.1 μg/mL)和 L3(29.38±3.2 μg/mL)的细胞毒性最为显著。本研究表明,测试化合物对 MCF-7 乳腺癌细胞株具有抗癌作用。
{"title":"Synthesis, Characterization, Docking Studies, and In-vitro Cytotoxic\u0000Activity of Some Novel 2, 3 Disubstituted Naphthalene 1,4 Dione\u0000Derivatives","authors":"Dilipkumar S, Karthik V, Gowramma B, Magesh M, Kaviarasan L","doi":"10.2174/0115734072298465240403084903","DOIUrl":"https://doi.org/10.2174/0115734072298465240403084903","url":null,"abstract":"\u0000\u0000Many quinone derivatives as of now utilized for anticancer medications.\u0000Especially, 1,4-naphthoquinones are dynamic derivatives, and it was broadly utilized in unrefined\u0000substances in the drugs and agrochemicals industry.\u0000\u0000\u0000\u0000In this work, we planned and combined five different moieties into 2, 3\u0000disubstituted naphthalene-1,4-dione molecules. Various spectral studies distinguished the synthetic\u0000designs of the produced compounds. The naphthoquinone derivatives were exposed to the primary\u0000molecular descriptor by Molinspiration programming, and all the descriptor values are within\u0000the specified value.\u0000\u0000\u0000\u0000In this work, we planned and combined five different moieties into 2, 3\u0000disubstituted naphthalene-1,4-dione molecules. Various spectral studies distinguished the synthetic\u0000designs of the produced compounds. The naphthoquinone derivatives were exposed to the primary\u0000molecular descriptor by Molinspiration programming, and all the descriptor values are within\u0000the specified value.\u0000\u0000\u0000\u0000Each of the five naphthoquinone derivatives was docked against the\u0000Topoisomerase II utilizing Auto Dock program 4.2.5. (PDB: 3L4K). The docking tells us that the\u0000studied compounds possess significant to moderate inhibition toward the targeted enzymes.\u0000Among the studied compounds, compound L3 showed the most elevated binding score (-10.66\u0000kcal/mol with one H-bond) than the adriamycin (-9.58 kcal/mol with two H-bonds) and compound\u0000L2 (- 9.86 kcal/mol with two H-bonds). The derivatives were tried for in-vitro cytotoxicity\u0000studies against MCF - 7 by the SRB method. Among them, compounds L2 (28.42±3.1 μg/mL)\u0000and L3 (29.38±3.2 μg/mL) were the most significant ones when contrasted with the control Adriamycin\u0000(15.28±3.4 μg/mL).\u0000\u0000\u0000\u0000The current research indicates that the tested compounds show anticancer action\u0000against the MCF-7 breast cancer cell line. Thus, the study is an attempt to advance toward the\u0000identification of innovative anticancer drugs.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140697708","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antioxidant Properties of Brassica Rapa L. Seeds and Immunostimulant Effect on Immunity Broilers Cells (Gallus Gallus Domesticus) 芸苔子的抗氧化特性及对肉鸡细胞免疫刺激的影响
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-09 DOI: 10.2174/0115734072282302240402043805
Soukaina Laaraj, Ibtisaam Ouahidi, Nada Al Moudani, A. Boukir, Samira Jaouhar, Safae Er Raouan, L. Aarab
In the past few decades, researchers have focused on finding the benefitsof natural substances derived from plants.This study aimed to evaluate the use of Brassica rapa seeds in poultry feed as an antioxidantand immunostimulant of host defenses.We prepared three extracts using ethanol, Ethyl Acetate, and water. Spectrophotometricmethods determined the total phenolic and flavonoid content in the three extracts. Antioxidantactivity was assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing/antioxidantpower (FRAP), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS)radicals and β-Carotene bleaching methods. An assessment of their immunostimulant activities invitro was performed on chicken immunity cell proliferation (splenocytes, thymocytes, and Bursacells) and IgY production.We prepared three different extracts using ethanol, Ethyl Acetate, and water. The total phenolic and flavonoid content in the three extracts was determined by spectrophotometric methods.Antioxidant activity has been assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing/antioxidant power (FRAP), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radicals and β-Carotene bleaching methods. Assessment of their immunostimulant activities in vitro was tested on chicken immunity cell proliferation (splenocytes, thymocytes, and Bursa cells) and IgY productionThe total phenolic contents ranged from 462.5 to 794.8 mg /g of extract, the order ofTPC was as follows: EtOAc > EtOH >Water. Flavonoid contents were, 63.7 mg in EtOH extract,81.2 mg in EtOAc extract, and 108.7 mg/g Extract in aqueous extract. By DPPH, the IC50s ofEtOH, EtOAc, and water, were 1.8μg/ml, 2.4μg/ml, and 1.5μg/ml, respectively. Using the Ferric-Reducing Antioxidant Power (FRAP), we remarked that the EtOH and EtOAc extracts have importantantioxidant powers. The ABTS assay indicated that EtOH and water had the highest activitieswith IC50s of 0.19 and 0.07, respectively. Finally, by the β-carotene bleaching test, we observedthat the IC50 of the EtOH, EtOAc, and water were 62.1 μg/mL; 72.7 μg/mL, and 45.8μg/mL, respectively. The results obtained indicate that Brassica aqueous extract stimulates humoralimmunity by stimulating splenocyte (B and T-lymphocytes) and Bursa cell (B-lymphocyte)proliferation by more than 200% of response vs control. In addition, the aqueous extract highlystimulated the function of bursa cells by 208% of the reaction. In the same conditions, we recordeda stimulation of cellular immunity mediated by thymocytes by an increase in cell proliferation(352.7% of response) implicated in virus protection. These extracts also possessed an antimicrobialeffect against diverse microorganisms such as coliforms and Staphylococcus. The FT-IRspectrum indicated that the hydroxyl group (phenol), hydroxybenzoic acid family, carbohydratemolecules such as glucopyranose, a carbonyl ester group, hydrocar
本研究旨在评估芸苔属植物种子在家禽饲料中作为抗氧化剂和宿主防御免疫刺激剂的用途。我们用乙醇、乙酸乙酯和水制备了三种提取物,并用分光光度法测定了三种提取物中的总酚和类黄酮含量。抗氧化活性采用 1,1-二苯基-2-苦基肼(DPPH)、铁还原/抗氧化力(FRAP)、2,2'-偶氮双(3-乙基苯并噻唑啉-6-磺酸)二铵盐(ABTS)自由基和 β-胡萝卜素漂白法进行评估。我们用乙醇、乙酸乙酯和水制备了三种不同的提取物。抗氧化活性采用 1,1-二苯基-2-苦基肼(DPPH)、铁还原/抗氧化力(FRAP)、2,2'-偶氮双(3-乙基苯并噻唑啉-6-磺酸)二铵盐(ABTS)自由基和β-胡萝卜素漂白法进行评估。总酚含量范围为 462.5 至 794.8 毫克/克提取物,总酚含量的顺序如下:EtOAc > EtOH > EtOAc > EtOH > EtOAc > EtOH > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAc > EtOAcEtOAc>EtOH>水。类黄酮含量分别为:乙醇提取物 63.7 毫克/克,乙酸提取物 81.2 毫克/克,水提取物 108.7 毫克/克。在 DPPH 作用下,EtOH、EtOAc 和水提取物的 IC50 分别为 1.8μg/ml、2.4μg/ml 和 1.5μg/ml。利用铁还原抗氧化能力(FRAP),我们发现 EtOH 和 EtOAc 提取物具有重要的抗氧化能力。ABTS 试验表明,EtOH 和水的活性最高,IC50 分别为 0.19 和 0.07。最后,通过β-胡萝卜素漂白试验,我们发现EtOH、EtOAc和水的IC50分别为62.1 μg/mL、72.7 μg/mL和45.8 μg/mL。研究结果表明,芸苔素水提取物通过刺激脾细胞(B 淋巴细胞和 T 淋巴细胞)和法氏囊细胞(B 淋巴细胞)的增殖来刺激体液免疫,其反应量是对照组的 200% 以上。此外,水提取物还能高度刺激法氏囊细胞的功能,其反应为对照组的 208%。在相同条件下,我们记录到胸腺细胞通过增加细胞增殖(反应的 352.7%)对细胞免疫功能的刺激,这与病毒防护有关。这些提取物还对大肠菌群和葡萄球菌等多种微生物具有抗菌作用。傅立叶变换红外光谱(FT-IRspectrum)表明,这些提取物中含有羟基(苯酚)、羟基苯甲酸家族、碳水化合物分子(如吡喃葡萄糖)、羰基酯基、碳氢链(烷基):总酚含量范围为 462.5 至 794.8 毫克/克提取物,TPC 顺序如下:EtOAc > EtOH > 水。类黄酮含量分别为:乙醇提取物 63.7 毫克/克,乙酸提取物 81.2 毫克/克,水提取物 108.7 毫克/克。利用铁还原抗氧化能力(FRAP),我们发现 EtOH 和 EtOAc 提取物具有重要的抗氧化能力。ABTS 试验表明,EtOH 和水的活性最高,IC50 分别为 0.19 和 0.07。最后,通过β-胡萝卜素漂白试验,我们发现EtOH、EtOAc和水的IC50分别为62.1 µg/mL、72.7 µg/mL和45.8 µg/mL。研究结果表明,芸苔素水提取物可刺激脾细胞(B 淋巴细胞和 T 淋巴细胞)和法氏囊细胞(B 淋巴细胞)增殖,从而刺激体液免疫,其反应量是对照组的 200% 以上。此外,水提取物对法氏囊细胞功能的刺激也很高,是对照组的 208%。在同样的条件下,我们记录到胸腺细胞通过增加细胞增殖(反应的 352.7%)来刺激细胞免疫,从而起到保护病毒的作用。这些提取物还对大肠菌群和葡萄球菌等多种微生物具有抗菌作用。傅立叶变换红外光谱显示,存在羟基(苯酚)、羟基苯甲酸家族、碳水化合物分子(如葡萄糖苷)、羰基酯基、碳氢链(烷基)。
{"title":"Antioxidant Properties of Brassica Rapa L. Seeds and Immunostimulant Effect on Immunity Broilers Cells (Gallus Gallus Domesticus)","authors":"Soukaina Laaraj, Ibtisaam Ouahidi, Nada Al Moudani, A. Boukir, Samira Jaouhar, Safae Er Raouan, L. Aarab","doi":"10.2174/0115734072282302240402043805","DOIUrl":"https://doi.org/10.2174/0115734072282302240402043805","url":null,"abstract":"\u0000\u0000In the past few decades, researchers have focused on finding the benefits\u0000of natural substances derived from plants.\u0000\u0000\u0000\u0000This study aimed to evaluate the use of Brassica rapa seeds in poultry feed as an antioxidant\u0000and immunostimulant of host defenses.\u0000\u0000\u0000\u0000We prepared three extracts using ethanol, Ethyl Acetate, and water. Spectrophotometric\u0000methods determined the total phenolic and flavonoid content in the three extracts. Antioxidant\u0000activity was assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing/antioxidant\u0000power (FRAP), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS)\u0000radicals and β-Carotene bleaching methods. An assessment of their immunostimulant activities in\u0000vitro was performed on chicken immunity cell proliferation (splenocytes, thymocytes, and Bursa\u0000cells) and IgY production.\u0000\u0000\u0000\u0000We prepared three different extracts using ethanol, Ethyl Acetate, and water. The total phenolic and flavonoid content in the three extracts was determined by spectrophotometric methods.Antioxidant activity has been assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing/antioxidant power (FRAP), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radicals and β-Carotene bleaching methods. Assessment of their immunostimulant activities in vitro was tested on chicken immunity cell proliferation (splenocytes, thymocytes, and Bursa cells) and IgY production\u0000\u0000\u0000\u0000The total phenolic contents ranged from 462.5 to 794.8 mg /g of extract, the order of\u0000TPC was as follows: EtOAc > EtOH >Water. Flavonoid contents were, 63.7 mg in EtOH extract,\u000081.2 mg in EtOAc extract, and 108.7 mg/g Extract in aqueous extract. By DPPH, the IC50s of\u0000EtOH, EtOAc, and water, were 1.8μg/ml, 2.4μg/ml, and 1.5μg/ml, respectively. Using the Ferric-\u0000Reducing Antioxidant Power (FRAP), we remarked that the EtOH and EtOAc extracts have important\u0000antioxidant powers. The ABTS assay indicated that EtOH and water had the highest activities\u0000with IC50s of 0.19 and 0.07, respectively. Finally, by the β-carotene bleaching test, we observed\u0000that the IC50 of the EtOH, EtOAc, and water were 62.1 μg/mL; 72.7 μg/mL, and 45.8\u0000μg/mL, respectively. The results obtained indicate that Brassica aqueous extract stimulates humoral\u0000immunity by stimulating splenocyte (B and T-lymphocytes) and Bursa cell (B-lymphocyte)\u0000proliferation by more than 200% of response vs control. In addition, the aqueous extract highly\u0000stimulated the function of bursa cells by 208% of the reaction. In the same conditions, we recorded\u0000a stimulation of cellular immunity mediated by thymocytes by an increase in cell proliferation\u0000(352.7% of response) implicated in virus protection. These extracts also possessed an antimicrobial\u0000effect against diverse microorganisms such as coliforms and Staphylococcus. The FT-IR\u0000spectrum indicated that the hydroxyl group (phenol), hydroxybenzoic acid family, carbohydrate\u0000molecules such as glucopyranose, a carbonyl ester group, hydrocar","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140721616","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic Potential, Pharmacological Activities and Analytical Aspectsof Liriodendrin in Medicine: Novel and Potential Therapy Options for theTreatment of Human Disorders and Associated Complications 利奥碘德林在医学中的治疗潜力、药理活性和分析方面:治疗人类疾病及相关并发症的新的和潜在的治疗方案
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-09 DOI: 10.2174/0115734072286081240326082701
K. Patel, D. Patel
Natural products and their derived secondary metabolites play an important role inmedicine and other allied health sectors. Liriodendrin is one of the main lignans of Boerhaaviadiffusa roots. Liriodendrin is a lignin class phytochemical having numerous health beneficialproperties in medicine, including anti-myocardial ischemia, anti-arrhythmic, anti-oxidant and anti-inflammatory potential. This present review aims to analyze the reported ethnomedicinal properties,pharmacological activities and analytical aspects of liriodendrin and identify the remaininggaps in medicinal fields for their future investigations. The pharmacological properties of liriodendrinhave been described in the present paper in order to describe its better utilization in naturalmedicine in the future. Biological poptential and pharmacological activities of liriodendrinhave been described in the present work with their analytical development in the scientific fields.In the present work, scientific data on liriodendrin were collected from different scientific databasessuch as PubMed, Springer, Google, Science Direct, and Google Scholar. They describedtheir biological potential on the basis of the available scientific literature. Further, research andreview articles from peer-reviewed journals were also searched during data collection. The presentpaper's scientific data signified the biological importance of liriodendrin in medicine, whichhas been isolated from Boerhaavia diffusa and other medicinal plants. Liriodendrin has biologicalpotential against myocardial infarction, arrhythmias, lung injury, hepatic injury, antiinflammatory,ulcerative colitis, gastric injury, SARS-CoV-2 protease and intestinal inflammation.Further, its effectiveness in medicine was also due to its anti-convulsant activity, nitric oxideinhibitory potential, cytotoxicity, cytoprotective nature, anti-oxidant, and anti-microbial potential.The present paper's scientific data also described the metabolism and analytical development fortheir isolation, separation and identification in different samples. Detailed pharmacological activitiesof liriodendrin have been described here in the present work and highlighted its importantpharmacological properties and analytical aspects. Liriodendrin is a valuable phytochemical ofBoerhaavia diffusa, which has numerous biological applications in medicine. Further, this studycan also validate the traditional and ethnobotanical use of the Boerhaavia diffusa and other plantmaterial, which contain a significant amount of liriodendrin as an active phytochemical. Liriodendrinhave huge biological potential far beyond its traditional uses in human complications.
天然产品及其衍生的次级代谢物在医药和其他相关保健领域发挥着重要作用。鹅掌楸木质素是鹅掌楸根中的主要木质素之一。鹅掌楸木质素是一种木质素类植物化学物质,在医学上具有多种有益健康的特性,包括抗心肌缺血、抗心律失常、抗氧化和抗炎潜力。本综述旨在分析所报道的鹅掌楸碱的民族药用特性、药理活性和分析方面,并找出在药用领域尚存在的空白,以便今后进行研究。本文阐述了鹅掌楸的药理特性,以便今后在天然药物中更好地利用它。本研究从 PubMed、Springer、Google、Science Direct 和 Google Scholar 等不同的科学数据库中收集了有关鹅掌楸的科学数据。在本研究中,我们从不同的科学数据库(如 PubMer、Springer、Google、Science Direct 和 Google Scholar)中收集了有关鹅掌楸碱的科学数据,并根据现有的科学文献对其生物潜力进行了描述。此外,在数据收集过程中还搜索了同行评审期刊上的研究和评论文章。本文的科学数据表明,从白花蛇舌草和其他药用植物中分离出的鹅掌楸碱在医学上具有重要的生物学意义。鹅掌楸碱具有防治心肌梗塞、心律失常、肺损伤、肝损伤、抗炎、溃疡性结肠炎、胃损伤、SARS-CoV-2 蛋白酶和肠道炎症的生物学潜力。本文的科学数据还描述了它们在不同样品中的代谢和分析发展,以分离、分离和鉴定它们。本研究还详细描述了鹅掌楸碱的药理活性,并着重介绍了其重要的药理特性和分析方法。鹅掌楸中的鹅掌楸碱是一种珍贵的植物化学物质,在医学上有广泛的生物学应用。此外,这项研究还验证了传统和民族植物学中对白花蛇舌草和其他植物材料的使用,这些材料中含有大量的活性植物化学物质--鹅掌楸碱。鹅掌楸具有巨大的生物潜力,远远超出了其在人类并发症中的传统用途。
{"title":"Therapeutic Potential, Pharmacological Activities and Analytical Aspects\u0000of Liriodendrin in Medicine: Novel and Potential Therapy Options for the\u0000Treatment of Human Disorders and Associated Complications","authors":"K. Patel, D. Patel","doi":"10.2174/0115734072286081240326082701","DOIUrl":"https://doi.org/10.2174/0115734072286081240326082701","url":null,"abstract":"\u0000\u0000Natural products and their derived secondary metabolites play an important role in\u0000medicine and other allied health sectors. Liriodendrin is one of the main lignans of Boerhaavia\u0000diffusa roots. Liriodendrin is a lignin class phytochemical having numerous health beneficial\u0000properties in medicine, including anti-myocardial ischemia, anti-arrhythmic, anti-oxidant and anti-\u0000inflammatory potential. This present review aims to analyze the reported ethnomedicinal properties,\u0000pharmacological activities and analytical aspects of liriodendrin and identify the remaining\u0000gaps in medicinal fields for their future investigations. The pharmacological properties of liriodendrin\u0000have been described in the present paper in order to describe its better utilization in natural\u0000medicine in the future. Biological poptential and pharmacological activities of liriodendrin\u0000have been described in the present work with their analytical development in the scientific fields.\u0000In the present work, scientific data on liriodendrin were collected from different scientific databases\u0000such as PubMed, Springer, Google, Science Direct, and Google Scholar. They described\u0000their biological potential on the basis of the available scientific literature. Further, research and\u0000review articles from peer-reviewed journals were also searched during data collection. The present\u0000paper's scientific data signified the biological importance of liriodendrin in medicine, which\u0000has been isolated from Boerhaavia diffusa and other medicinal plants. Liriodendrin has biological\u0000potential against myocardial infarction, arrhythmias, lung injury, hepatic injury, antiinflammatory,\u0000ulcerative colitis, gastric injury, SARS-CoV-2 protease and intestinal inflammation.\u0000Further, its effectiveness in medicine was also due to its anti-convulsant activity, nitric oxide\u0000inhibitory potential, cytotoxicity, cytoprotective nature, anti-oxidant, and anti-microbial potential.\u0000The present paper's scientific data also described the metabolism and analytical development for\u0000their isolation, separation and identification in different samples. Detailed pharmacological activities\u0000of liriodendrin have been described here in the present work and highlighted its important\u0000pharmacological properties and analytical aspects. Liriodendrin is a valuable phytochemical of\u0000Boerhaavia diffusa, which has numerous biological applications in medicine. Further, this study\u0000can also validate the traditional and ethnobotanical use of the Boerhaavia diffusa and other plant\u0000material, which contain a significant amount of liriodendrin as an active phytochemical. Liriodendrin\u0000have huge biological potential far beyond its traditional uses in human complications.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140720662","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Eucalyptus globulus Labill. Essential Oil Effect on the Attachment of OralBacteria to Hydroxyapatite and Biofilm Formation 蓝桉精油对口腔细菌附着羟基磷灰石和生物膜形成的影响精油对口腔细菌附着羟基磷灰石和生物膜形成的影响
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-02 DOI: 10.2174/0115734072296932240319060406
Kahina Hardou-Belhoucine, F. Brahmi, Daniel Grenier, Khokha Mouhoubi, K. Madani, L. Boulekbache‐Makhlouf
Periodontal disease and dental caries are two oral illnesses that are significantlyinfluenced by microorganisms, hence the usefulness of finding natural substances toinhibit them.This study aimed to assess the Eucalyptus globulus Labill. leaf and fruit essential oilseffect against Streptococcus mutans, Streptococcus sobrinus, Aggregatibacter actinomycetemcomitans,Porphyromonas gingivalis, Fusobacterium nucleatum, and Candida albicans to studytheir anticariogenic and antiperiodonto pathogenic activities.these activities were evaluated according to the determination of minimum inhibitoryconcentration (MIC) and minimum bactericidal concentration (MBC), anti-biofilm effects, andthe impact on the adhesion to hydroxyapatite, a main component of the tooth.both leaf and fruit essential oils showed strong antibacterial activity against anaerobicbacteria: F. nucleatum (MIC of 0.012 %) and P. gingivalis (MIC of 0.025 %). Anticarcinogenicactivity also showed MIC values of 0.06 % against S. mutans and, 0.5 % against S. sobrinus, andappropriate antifungal activity against C. albicans. It is interesting to note that both oils showed asignificant inhibitory property to biofilm formation by the different studied species and significantlyreduced the adhesion capacity of S. mutans and S. sobrinus to the hydroxyapatite surface atvery low concentrations of 0.12 and 0.5 % for S. mutans and S. sobrinus, respectively.These results highlight the strong potential of E. globulus essential oils as antimicrobialand antibiofilm agents, as well as their ability to inhibit bacterial adhesion, which is promisingfor the prevention of dental caries and plaque. This implies that E. globulus may be a newalternative source of substances of medicinal interest that can be used in the pharmaceutical industryto produce antimicrobial agents against dental caries and oral infectious diseases
牙周病和龋齿是两种受微生物严重影响的口腔疾病,因此寻找天然物质来抑制它们非常有用。本研究旨在评估球叶桉树精油和果实精油对变异链球菌、苏布雷链球菌、放线菌、牙龈卟啉单胞菌、核酸化脓杆菌和白色念珠菌的抗龋齿和抗牙周病致病活性。这些活性是通过测定最低抑菌浓度(MIC)和最低杀菌浓度(MBC)、抗生物膜效应以及对牙齿主要成分羟基磷灰石粘附性的影响来评估的:叶片和果实精油对厌氧菌有很强的抗菌活性:核酸酵母菌(MIC 为 0.012 %)和牙龈球菌(MIC 为 0.025 %)。抗癌活性还显示,对突变酵母菌的 MIC 值为 0.06 %,对索氏酵母菌的 MIC 值为 0.5 %,对白癣菌也有适当的抗真菌活性。值得注意的是,这两种精油对所研究的不同物种形成生物膜都有显著的抑制作用,而且在 0.12% 和 0.5% 的极低浓度下,就能显著降低变异杆菌和索布林杆菌对羟基磷灰石表面的粘附能力。这些结果凸显了球果香精油作为抗菌剂和抗生物膜剂的强大潜力,以及其抑制细菌粘附的能力,这对于预防龋齿和牙菌斑很有前景。这意味着球果香精油可能是一种新的药用物质替代来源,可用于制药业生产抗龋齿和口腔传染病的抗菌剂。
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引用次数: 0
Individual and Dual Cytotoxicity of the Combination of Passiflora Caerulea Leaf Extract and Titanium Oxide Nanoparticles against A549, U937, andHela Cells 西番莲叶提取物和纳米氧化钛组合对 A549、U937 和 Hela 细胞的单独和双重细胞毒性
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.2174/0115734072294581240311064402
L. Sindhura, Mohd. Nazneen Bobby, K. Srikanth, Helan Soundra Rani Michael, Abu Md Ashif Ikbal, Sabu Thomas, H. Kargarzadeh, Partha Palit
The study addresses the underexplored realm of cytotoxicity evaluationinvolving binary mixtures of Passiflora caerulea leaf extracts and Titanium nanoparticles(TiO2NPs). The focus lies on understanding the combined effects of these components on cancercells (A549, U937, and HeLa).In vitro cytotoxicity assessments were employed to evaluate the toxicity of P. caerulealeaf extracts, TiO2NPs, and their combination. The study utilized MTT, NRU, and LDH assays tomeasure cellular viability. Additionally, reactive oxygen species (ROS) and glutathione levelswere assessed alongside the aforementioned assays.The toxicity percentage exhibited dose-dependent behavior for P. caerulea leaf extracts,TiO2NPs, and their combination. Interestingly, when P. caerulea leaf extract and TiO2NPs werecombined, the reduction in cell viability was noticeably more than when the exposures were madeseparately. Moreover, the production of ROS was higher in the combined toxicity scenario, and amore pronounced decrease in glutathione levels was observed compared to individual exposures.The findings suggest that the combined effects of P. caerulea leaf extract andTiO2NPs induce greater cytotoxicity compared to their impacts. This underscores the potential forsynergistic cytotoxicity in combined exposure scenarios, warranting further exploration of combinedeffects in future studies.
该研究涉及西番莲叶提取物和钛纳米粒子(TiO2NPs)二元混合物的细胞毒性评估这一尚未充分开发的领域。研究重点在于了解这些成分对癌症细胞(A549、U937 和 HeLa)的综合影响。体外细胞毒性评估用于评价西番莲叶提取物、TiO2NPs 及其组合的毒性。该研究利用 MTT、NRU 和 LDH 检测法测量细胞活力。对于 P. caerulea 叶提取物、TiO2NPs 和它们的组合,毒性百分比表现出剂量依赖性。有趣的是,当 P. caerulea 叶提取物和 TiO2NPs 混合使用时,细胞活力的降低幅度明显高于单独使用时。此外,与单独接触相比,在联合毒性情况下产生的 ROS 更高,谷胱甘肽水平的下降也更明显。这强调了在联合暴露情况下产生协同细胞毒性的可能性,值得在今后的研究中进一步探讨联合效应。
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引用次数: 0
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Current Bioactive Compounds
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