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Toxicity of Oils Extracted From the Arils of Blighia sapida (K.D. Koenig) in Wistar Rats. 从 Blighia sapida (K.D. Koenig) 的果仁中提取的油对 Wistar 大鼠的毒性。
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-11-08 eCollection Date: 2024-01-01 DOI: 10.1155/2024/1998836
Aklesso Nabede, Haziz Sina, Mélila Mamatchi, Tiatou Souho, Batcha Ouadja, S M Ismaël Hoteyi, Hafiz A Salami, Adolphe Adjanohoun, Lamine Baba-Moussa, Kou'santa Amouzou

Blighia sapida oil, a substance with a rich history of use for its nutritional, therapeutic, traditional, and cosmetic benefits, was the focus of our study. We investigated the impact of consuming edible oil from B. sapida arils on Wistar rats. The crude oil from unripe arils was extracted using cold pressing and then administered to the rats. The toxicity was evaluated according to the OECD method. Notably, there were no signs of food poisoning or adverse effects on the weight and behavior of the rats treated with B. sapida oils. The LD50 of the oil was more significant than 5000 mg/kg of body weight, and hematological and biochemical parameters did not differ significantly from the control group. Rats fed with an oil-supplemented diet showed an increase in weight compared to the negative control group. No fatty deposits were found in vital organs, and consuming the oil did not affect the immune system or biochemical biomarkers. However, excessive intake of fat may have harmful effects on tissues. Our findings strongly suggest that B. sapida oil is safe for consumption within reasonable limits. The data we present here reveal that the oil derived from B. sapida is suitable for moderate consumption and may offer various health advantages, a potential that warrants further exploration.

无患子油是一种具有丰富营养、治疗、传统和美容功效的物质,是我们研究的重点。我们研究了食用无花果油对 Wistar 大鼠的影响。我们使用冷压法从未成熟的假种皮中提取粗油,然后给大鼠食用。根据经合组织的方法对其毒性进行了评估。值得注意的是,使用无患子油的大鼠没有出现食物中毒的迹象,体重和行为也没有受到不良影响。该油的半数致死剂量大于 5000 毫克/千克体重,血液学和生化指标与对照组没有明显差异。与阴性对照组相比,用油添加剂喂养的大鼠体重有所增加。在重要器官中没有发现脂肪沉积,食用油也没有影响免疫系统或生化生物标志物。然而,过量摄入脂肪可能会对组织产生有害影响。我们的研究结果有力地表明,在合理范围内食用无患子油是安全的。我们在此提供的数据显示,从无患子中提取的油适合适量食用,并可能提供各种健康优势,这一潜力值得进一步探索。
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引用次数: 0
Xylooligosaccharide Production From Lignocellulosic Biomass and Their Health Benefits as Prebiotics. 从木质纤维素生物质中生产低聚木糖及其作为益生元对健康的益处。
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-11-05 eCollection Date: 2024-01-01 DOI: 10.1155/2024/6179375
Kajal Kumari, Sushil Nagar, Sakshi Goyal, Sonu Maan, Vishal Chugh, Vinod Kumar, Neeraj Kharor

Lignocellulosic biomass (LCB) comprising of wheat bran, coconut husk, rice husk, cereals straw, and other hardwood and softwoods is a good source for the production of xylooligosaccharides (XOS) (prebiotic). XOS produced are nondigestible carbohydrates being stable under stomach pH and digestive enzymes so they can be easily delivered to the intestine in native form, thus stimulating the growth of probiotics. Here we review about the raw material, production, purification, and application of XOS with health benefits. Importance of XOS being valuable food ingredient is increasing as they perform a variety of functions, including reduction in cholesterol levels, gastrointestinal health maintenance, anticancer and antioxidant properties, and modulation of immune system. We also discuss the different characterization methods which are necessary to determine the degree of polymerization (DP) of XOS. Low DP (xylobiose and xylotriose) is usually preferred for the application of XOS in various sectors. This review emphasizes the growing significance of XOS as a prebiotic, serving as nourishment for probiotics.

木质纤维素生物质(LCB)包括麦麸、椰子壳、稻壳、谷物秸秆以及其他硬木和软木,是生产木寡糖(XOS)(益生元)的良好来源。生产的 XOS 是不可消化的碳水化合物,在胃的 pH 值和消化酶的作用下非常稳定,因此很容易以原生态的形式输送到肠道,从而刺激益生菌的生长。在此,我们将对具有健康益处的 XOS 的原料、生产、提纯和应用进行综述。XOS 具有多种功能,包括降低胆固醇水平、维护胃肠道健康、抗癌和抗氧化特性以及调节免疫系统,因此作为有价值的食品配料,其重要性与日俱增。我们还讨论了确定 XOS 聚合度(DP)所需的不同表征方法。低聚合度(木糖和木三糖)通常是将 XOS 应用于各个领域的首选。本综述强调,作为益生菌的营养品,木糖醇作为益生元的重要性与日俱增。
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引用次数: 0
Hypoglycemic Assessment of Aqueous Leaf Extract of Moringa oleifera on Diabetic Wistar Rats. 辣木叶水提取物对糖尿病 Wistar 大鼠的降血糖作用评估
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-10-23 eCollection Date: 2024-01-01 DOI: 10.1155/2024/9779021
Egbujo Ejike Amina, James O Adisa, Solomon Matthias Gamde, Etinosa Beauty Omoruyi, Habauka M Kwaambwa, Lamech M Mwapagha

Background: Moringa oleifera leaf is used for diabetes due to its pharmacologic effects. Patients with hyperglycemia experience beta cell destruction. However, no research on risk awareness has been done to ascertain its safety. The present study describes the antidiabetic effect of Moringa oleifera leaf, such as the protection of pancreatic beta cells and the induction of glycogen synthesis, before addressing the secondary effects of diabetes, such as hepatic and renal toxicity. Methods: Forty-five Wistar rats weighed 160 ± 10 g were divided into nine groups. All animal operations complied with the National Institute of Health (NIH) guidelines for the care and use of laboratory animals as approved by the Animal Ethical Committee, University of Jos. Group I was normal control and Group II was diabetic animals induced with alloxan. Insulin and extract doses of 200, 400, and 800 mg/kg were given to diabetic Groups III-VI. Normal animals in Groups VII-IX were given extract at doses of 200, 400, and 800 mg/kg for 28 days. Tissues were retrieved for biochemical and histological investigations using standard techniques. Results: There was decrease relative body weight of diabetic animals (95.50 ± 5.50) when compared to normal control (142.75 ± 20.08) with increased levels of urea (control 6.13 ± 0.523 and diabetes 29.23 ± 1.267) and creatinine (control 0.70 ± 0.057 and diabetes 2.13 ± 0.185). Histology of the liver and pancreas also points to organ damage due to hyperglycemia. However, oral administration of extract showed antidiabetic effect with protection of pancreatic beta cells and the induction of glycogen synthesis, no glycogen was deposited in the liver, addressing the secondary effects of diabetes, such as hepatic and renal toxicity. Further discovery revealed that extract elevated antioxidant enzyme expression. Conclusion: Leaf extract from Moringa oleifera reduces blood sugar and lessens the damage caused by hyperglycemia in the pancreas and liver.

背景:油辣木叶因其药理作用被用于治疗糖尿病。高血糖患者的β细胞会遭到破坏。然而,尚未开展风险意识研究以确定其安全性。本研究介绍了油辣木叶的抗糖尿病作用,如保护胰岛β细胞和诱导糖原合成,然后探讨了糖尿病的副作用,如肝毒性和肾毒性。研究方法45 只体重为 160±10 克的 Wistar 大鼠分为 9 组。I 组为正常对照组,II 组为用阿脲诱导的糖尿病动物。胰岛素和提取物剂量分别为 200、400 和 800 毫克/千克,用于糖尿病组 III-VI。给第七至第九组的正常动物服用提取物,剂量分别为 200、400 和 800 毫克/千克,持续 28 天。采用标准技术提取组织进行生化和组织学研究。结果与正常对照组(142.75 ± 20.08)相比,糖尿病动物的相对体重下降(95.50 ± 5.50),尿素(对照组为 6.13 ± 0.523,糖尿病组为 29.23 ± 1.267)和肌酐(对照组为 0.70 ± 0.057,糖尿病组为 2.13 ± 0.185)水平升高。肝脏和胰腺的组织学检查也表明,高血糖会导致器官损伤。然而,口服提取物具有抗糖尿病作用,可保护胰腺β细胞并诱导糖原合成,肝脏中没有糖原沉积,从而解决了糖尿病的继发性影响,如肝毒性和肾毒性。进一步研究发现,提取物能提高抗氧化酶的表达。结论油辣木叶提取物能降低血糖,减轻高血糖对胰腺和肝脏造成的损害。
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引用次数: 0
Comparative Analysis of Phytochemicals and Antioxidant Characterization Among Different Parts of Catharanthus roseus: In Vitro and In Silico Investigation. 蔷薇科植物不同部位的植物化学成分和抗氧化特性比较分析:体外和体内研究
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-10-18 eCollection Date: 2024-01-01 DOI: 10.1155/2024/1904029
Farjana Akter Hira, Ashekul Islam, Kanika Mitra, Ummey Hafsa Bithi, Khondoker Shahin Ahmed, Sanzida Islam, Shaike Mohammad Abdullah, Md Nazim Uddin

Background: The study investigates the antioxidant properties of Catharanthus roseus, focusing on identifying its antioxidant compounds and chemical constituents. We compare antioxidant activities across its root, stem, flower, and leaf and examine the inhibition of reactive oxygen species (ROS)-generating enzymes by the plant's phytocompounds. Methods: We conducted a comprehensive analysis that included proximate analysis, mineral content assessment, and in vitro antioxidant characterization of various plant parts-root, stem, flower, and leaf. The levels of bioactive phytochemicals in both ethanol and mixed-solvent extracts of Catharanthus roseus were quantified using high-performance liquid chromatography with a diode array detector (HPLC-DAD). Additionally, we performed molecular docking studies to explore the interactions of quantified phytocompounds. Results: HPLC-DAD analysis quantified catechin hydrate, catechol, (-) epicatechin, rutin hydrate, trans-cinnamic acid, quercetin, vanillic acid, kaempferol, and trans-ferulic acid in Catharanthus roseus. Despite the ethanol extract having higher total antioxidant properties and flavonoid content, the mixed-solvent extract exhibited higher EC50 for reducing power and lower IC50 for ABTS, 2,2-diphenyl-1-picrylhydrazyl (DPPH), and metal chelating activities. Molecular docking studies indicated that compounds such as catechin, rutin, epicatechin, quercetin, and kaempferol significantly inhibit the ROS-generating enzyme microsomal prostaglandin E synthase 1 (mPGES-1). Conclusions: The mixed-solvent extract had higher levels of catechin hydrate, rutin hydrate, trans-ferulic acid, and vanillic acid, whereas the ethanol extract contained more (-) epicatechin, catechol, kaempferol, quercetin, and trans-cinnamic acid. While the extracts displayed antioxidant activity, the phytoconstituents also inhibited ROS-generating mPGES-1. These results identify key compounds with potential for developing new chemotherapeutic agents against ROS.

背景:本研究调查了长春花的抗氧化特性,重点是确定其抗氧化化合物和化学成分。我们比较了其根、茎、花和叶的抗氧化活性,并研究了该植物的植物化合物对活性氧(ROS)生成酶的抑制作用。研究方法我们对植物的各个部分(根、茎、花和叶)进行了全面分析,包括近似分析、矿物质含量评估和体外抗氧化特性鉴定。我们使用带二极管阵列检测器的高效液相色谱法(HPLC-DAD)对石竹的乙醇提取物和混合溶剂提取物中生物活性植物化学物质的含量进行了定量分析。此外,我们还进行了分子对接研究,以探索定量植物化合物之间的相互作用。结果HPLC-DAD 分析定量了儿茶素水合物、儿茶酚、(-) 表儿茶素、芦丁水合物、反式肉桂酸、槲皮素、香草酸、山柰酚和反式阿魏酸。尽管乙醇提取物的总抗氧化性和类黄酮含量较高,但混合溶剂提取物的还原力 EC50 值较高,ABTS、2,2-二苯基-1-苦基肼(DPPH)和金属螯合活性的 IC50 值较低。分子对接研究表明,儿茶素、芦丁、表儿茶素、槲皮素和山柰醇等化合物能显著抑制 ROS 生成酶微粒体前列腺素 E 合酶 1(mPGES-1)。结论混合溶剂提取物中的儿茶素水合物、芦丁水合物、反式阿魏酸和香草酸含量较高,而乙醇提取物中的(-)表儿茶素、儿茶酚、山奈儿茶酚、槲皮素和反式肉桂酸含量较高。在提取物显示出抗氧化活性的同时,植物成分还抑制了产生 ROS 的 mPGES-1。这些结果确定了一些关键化合物,它们具有开发新的抗 ROS 化疗药物的潜力。
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引用次数: 0
Green Synthesis and Anti-Inflammatory Activity of Silver Nanoparticles Based on Leaves Extract of Aphania senegalensis. 基于 Aphania senegalensis 叶提取物的银纳米粒子的绿色合成和抗炎活性。
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-09-19 eCollection Date: 2024-01-01 DOI: 10.1155/2024/3468868
Fatemata Diallo, Insa Seck, Samba Fama Ndoye, Tamsir Niang, Sidy Mouhamed Dieng, Fatou Thiam, Moussa Ndao, El Hadji Mamour Sakho, Alioune Fall, Madièye Séne, Matar Seck

This study focuses on the synthesis of silver nanoparticles (AgNPs) using the extract of Aphania senegalensis leaves. The extraction was done using maceration at room temperature in water for 48 h. The synthesized nanoparticles were characterized by IR, XRD, TEM, and SEM. The thermal stability of these nanoparticles was studied by TGA. The zeta potential was used to define the size, charge distribution, and stability of the nanoparticles. Optimization reactions were carried out based on reaction time, pH, and temperature. The nanoparticles obtained from optimal conditions were evaluated on induced inflammation. The determination of the average diameters and geometry of nanoparticles was carried out by XRD by calculating the lattice constants, and they are between 18.11 and 50 nm. The evaluation of anti-inflammatory activity showed that the nanoparticles are 10 times more active than the extract of Aphania senegalensis leaves. Minimum doses of 10 mg/kg orally and 3 mg/kg were obtained for the plant extract, respectively. These results are promising for the possibility of AgNPs to be used for the treatment of inflammation.

本研究的重点是利用 Aphania senegalensis 叶子的提取物合成银纳米粒子 (AgNPs)。合成的纳米粒子通过红外光谱、XRD、TEM 和 SEM 进行了表征。热重分析法研究了这些纳米颗粒的热稳定性。zeta 电位用于确定纳米颗粒的尺寸、电荷分布和稳定性。根据反应时间、pH 值和温度进行了优化反应。对在最佳条件下获得的纳米颗粒进行了诱导炎症评估。通过 XRD 计算晶格常数,确定了纳米粒子的平均直径和几何形状,它们介于 18.11 纳米和 50 纳米之间。抗炎活性评估结果表明,纳米颗粒的活性比 Aphania senegalensis 叶子提取物高 10 倍。植物提取物的最小口服剂量分别为 10 毫克/千克和 3 毫克/千克。这些结果为 AgNPs 用于治疗炎症带来了希望。
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引用次数: 0
Proteomics and Bioinformatics Investigations Link Overexpression of FGF8 and Associated Hub Genes to the Progression of Ovarian Cancer and Poor Prognosis. 蛋白质组学和生物信息学研究发现,FGF8 和相关枢纽基因的过表达与卵巢癌的进展和预后不良有关。
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-09-13 eCollection Date: 2024-01-01 DOI: 10.1155/2024/4288753
Vikrant Kumar, Anil Kumar Tomar, Ayushi Thapliyal, Savita Yadav

Ovarian cancer's asymptomatic nature, high recurrence rate, and resistance to platinum-based chemotherapy highlight the need to find and characterize new diagnostic and therapeutic targets. While prior studies have linked aberrant expression of fibroblast growth factor 8 (FGF8) to various cancer types, its precise role has remained elusive. Recently, we observed that FGF8 silencing reduces the cancer-promoting properties of ovarian cancer cells, and thus, this study aimed to understand how FGF8 regulates the development of ovarian cancer. LC-MS/MS-based quantitative proteomics analysis identified 418 DEPs, and most of them were downregulated in FGF8-silenced ovarian cancer cells. Many of these DEPs are associated with cancer progression and unfavorable prognosis. To decipher the biological significance of DEPs, bioinformatics analyses encompassing gene ontology, pathway analysis, protein-protein interaction networks, and expression analysis of hub genes were carried out. Hub genes identified in the FGF8 protein network were upregulated in ovarian cancer compared to controls and were linked to poor prognosis. Subsequently, the expression of hub genes was correlated with patient survival and regulation of the tumor microenvironment. Conclusively, FGF8 and associated hub genes help in the progression of ovarian cancer, and their overexpression may lead to higher immune infiltration, poor prognosis, and poor survival.

卵巢癌无症状、复发率高、对铂类化疗具有抗药性,这些特点凸显了寻找新的诊断和治疗靶点并确定其特性的必要性。虽然先前的研究已将成纤维细胞生长因子 8(FGF8)的异常表达与各种癌症类型联系起来,但其确切作用仍难以捉摸。最近,我们观察到 FGF8 的沉默降低了卵巢癌细胞的促癌特性,因此,本研究旨在了解 FGF8 如何调控卵巢癌的发展。基于LC-MS/MS的定量蛋白质组学分析发现了418个DEPs,其中大部分在FGF8沉默的卵巢癌细胞中被下调。其中许多 DEPs 与癌症进展和不良预后有关。为了解读DEPs的生物学意义,研究人员进行了生物信息学分析,包括基因本体、通路分析、蛋白-蛋白相互作用网络和枢纽基因的表达分析。与对照组相比,在FGF8蛋白网络中发现的枢纽基因在卵巢癌中上调,并且与不良预后有关。随后,中心基因的表达与患者的生存和肿瘤微环境的调节相关。结论是,FGF8和相关的枢纽基因有助于卵巢癌的进展,它们的过度表达可能导致更高的免疫浸润、预后不良和生存率低下。
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引用次数: 0
Effects of Low Concentration of Glyphosate-Based Herbicide on Genotoxic, Oxidative, Inflammatory, and Behavioral Meters in Danio rerio (Teleostei and Cyprinidae). 低浓度草甘膦除草剂对鲤科鱼类基因毒性、氧化、炎症和行为指标的影响
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-09-10 eCollection Date: 2024-01-01 DOI: 10.1155/2024/1542152
Eduardo Bortolon Ribas, Gustavo Colombo Dal-Pont, Ariana Centa, Marcos Otávio Bueno, Ricardo Cervini, Rosana Claudio Silva Ogoshi, Claudriana Locatelli

The glyphosate herbicide is a pesticide widely used in the world and can contaminate soil, air, and water. The objective of this work was to evaluate the toxicity of a glyphosate-based herbicide (GBH) in zebrafish (Danio rerio). Fish were exposed to different concentrations of GBH (0, 50, 250, and 500 µg/L) for 96 hours. Brain, liver, and blood were collected for biochemical and genotoxicity analyses, and behavioral tests were performed. The results showed that there was a reduction in the activity of the antioxidant enzymes of catalase (CAT) and glutathione-S-transferase (GST) in the liver at all concentrations and at the highest concentration in the brain. There was also a reduction in lipid peroxidation in the liver at all concentrations of glyphosate. There was an increase in micronuclei in the blood at the 500 µg/L concentration. However, the count of nuclear abnormalities showed no differences from the control. Interleukin-1beta (IL-1β) generation was inhibited at all concentrations in the liver and at the highest concentration in the brain. No significant differences were found in the behavioral test compared to the control. The results showed that acute exposure to GBH promoted an inflammatory event, which reduced the efficiency of antioxidants, thus producing a disturbance in tissues, mainly in the liver, causing immunosuppression and generating genotoxicity.

草甘膦除草剂是世界上广泛使用的一种杀虫剂,会污染土壤、空气和水。这项研究旨在评估草甘膦除草剂(GBH)对斑马鱼(Danio rerio)的毒性。将斑马鱼暴露于不同浓度的 GBH(0、50、250 和 500 µg/L)中 96 小时。收集脑、肝和血液进行生化和遗传毒性分析,并进行行为测试。结果表明,在所有浓度下,肝脏中过氧化氢酶(CAT)和谷胱甘肽-S-转移酶(GST)的活性都有所降低,脑中的浓度最高。在所有草甘膦浓度下,肝脏中的脂质过氧化反应也有所减少。浓度为 500 微克/升时,血液中的微核有所增加。不过,核异常计数与对照组相比没有差异。在所有浓度下,肝脏中白细胞介素-1β(IL-1β)的生成都受到抑制,在最高浓度下,脑中的白细胞介素-1β的生成也受到抑制。行为测试结果与对照组相比没有发现明显差异。结果表明,急性接触 GBH 会引发炎症事件,降低抗氧化剂的效率,从而造成组织(主要是肝脏)紊乱,导致免疫抑制并产生遗传毒性。
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引用次数: 0
In Vitro Antibacterial and Antioxidant Activities, Pharmacokinetics, and In Silico Molecular Docking Study of Phytochemicals from the Roots of Ziziphus spina-christi. 紫花地丁根中植物化学物质的体外抗菌和抗氧化活性、药效学和硅学分子对接研究
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-08-09 eCollection Date: 2024-01-01 DOI: 10.1155/2024/7551813
Hadush Gebrehiwot, Urgessa Ensermu, Aman Dekebo, Milkyas Endale, Tariku Nefo Duke

Ziziphus spina-christi (Rhamnaceae family) is a medicinal plant traditionally used to treat dandruff, wounds, hair loss, diarrhea, mastitis, abdominal pain, and gastrointestinal complications. To support this, the present work aims to study the in vitro antibacterial and antioxidant activities of compound isolates from the roots of Ziziphus spina-christi along with their in silico computational analyses. Compounds were isolated on silica gel column chromatography and an agar disc diffusion and DPPH radical scavenging assays were employed to study the antibacterial and antioxidant activities, respectively. The ADME and toxicity properties of the compounds were evaluated using SwissADME and ProTox-II online Web tools, respectively. Conversely, the in silico molecular docking studies were attained via a Biovia Discovery Studio Visualizer 2021 in combination with the AutoDock Vina software. The silica gel chromatographic separation of the combined CH2Cl2 : CH3OH (1 : 1) and CH3OH root extracts afforded trimethyl trilinolein (1), stearic acid (2), 13-hydroxyoctadeca-9, 11-dienoic acid (3), β-sitosteryl-3β-glucopyranoside-6'-O-palmitate (4), and stigmasterol (5). Notably, the in vitro antibacterial study revealed the extract and β-sitosteryl-3β-glucopyranoside-6'-O-palmitate (4) with the highest inhibitory activities (15.25 ± 0.35 and 14.25 ± 0.35 mm, respectively) against E. coli compared to ciprofloxacin (21.00 ± 0.35 mm) at 2 mg/mL. The CH2Cl2 : CH3OH (1 : 1) extract (IC50 : 1.51 µg/mL) and β-sitosteryl-3β-glucopyranoside-6'-O-palmitate (4) (IC50 : 5.41 µg/mL) also exhibited auspicious DPPH scavenging activities, followed by stigmasterol (5) (IC50 : 6.88 µg/mL) compared to the ascorbic acid standard (IC50 : 0.46 µg/mL). The molecular docking analyses unveiled the highest binding affinity by β-sitosteryl-3β-glucopyranoside-6'-O-palmitate (4) (-8.0 kcal/mol) against P. aeruginosa PqsA relative to the ciprofloxacin standard (-8.2 kcal/mol). Furthermore, the organ toxicity predictions showed that all the compounds exhibit no hepatotoxicity and cytotoxicity effects and stigmasterol (5) affords drug-likeness protocols. Overall, the combined experimental and computational investigations of this study support the traditional uses of Ziziphus spina-christi for antibacterial and natural antioxidant applications.

辣根(鼠李科)是一种药用植物,传统上用于治疗头皮屑、伤口、脱发、腹泻、乳腺炎、腹痛和胃肠道并发症。为支持这一研究,本研究旨在研究从辣木根分离出的化合物的体外抗菌和抗氧化活性,并对其进行硅学计算分析。化合物经硅胶柱层析分离,并采用琼脂盘扩散法和 DPPH 自由基清除法分别研究其抗菌和抗氧化活性。利用 SwissADME 和 ProTox-II 在线网络工具分别评估了化合物的 ADME 和毒性特性。而硅学分子对接研究则是通过 Biovia Discovery Studio Visualizer 2021 与 AutoDock Vina 软件相结合实现的。硅胶色谱分离了 CH2Cl2 :CH3OH(1 : 1)和 CH3OH 的根提取物可得到三甲基三羟基甲苯(1)、硬脂酸(2)、13-羟基十八碳-9,11-二烯酸(3)、β-谷甾醇-3β-吡喃葡萄糖苷-6'-O-棕榈酸酯(4)和豆甾醇(5)。值得注意的是,体外抗菌研究显示,与 2 mg/mL 环丙沙星(21.00 ± 0.35 mm)相比,提取物和 β-谷甾醇基-3β-吡喃葡萄糖苷-6'-O-棕榈酸酯(4)对大肠杆菌的抑制活性最高(分别为 15.25 ± 0.35 mm 和 14.25 ± 0.35 mm)。CH2Cl2 :CH3OH (1 : 1) 提取物(IC50:1.51 µg/mL)和 β-谷甾醇基-3β-吡喃葡萄糖苷-6'-O-棕榈酸酯 (4)(IC50:5.41 µg/mL)也表现出良好的 DPPH 清除活性,其次是豆甾醇 (5)(IC50:6.88 µg/mL),而抗坏血酸标准品(IC50:0.46 µg/mL)的 IC50 为 0.46 µg/mL。分子对接分析表明,β-谷甾醇-3β-吡喃葡萄糖苷-6'-O-棕榈酸酯(4)(-8.0 千卡/摩尔)与铜绿假单胞菌 PqsA 的结合亲和力最高,而环丙沙星的标准结合亲和力为-8.2 千卡/摩尔。此外,器官毒性预测表明,所有化合物都没有肝毒性和细胞毒性效应,而且豆固醇(5)具有药物相似性协议。总之,本研究的实验和计算综合研究支持了辣木籽在抗菌和天然抗氧化方面的传统用途。
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引用次数: 0
MIP-4 is Induced by Bleomycin and Stimulates Cell Migration Partially via Nir-1 Receptor. 博莱霉素诱导 MIP-4 并部分通过 Nir-1 受体刺激细胞迁移
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-08-02 eCollection Date: 2024-01-01 DOI: 10.1155/2024/5527895
M Pacurari, I Cox, A N Bible, S Davern

Background: CC-chemokine ligand 18 also known as MIP-4 is a chemokine with roles in inflammation and immune responses. It has been shown that MIP-4 is involved in the development of several diseases including lung fibrosis and cancer. How exactly MIP-4 is regulated and exerts its role in lung fibrosis remains unclear. Therefore, in the present study, we examined how MIP-4 is regulated and whether it acts via its potential receptor Nir-1.

Materials and methods: A549 cells were grown and maintained in DMEM : F12 (1 : 1) and supplemented with 10% FBS and 1000 U of penicillin/streptomycin and maintained as recommended by the manufacturer (ATCC). Cell migration and invasion, immunohistochemistry (IHC), Western blot, qPCR, and siRNA Nir-1 were used to determine MIP-4 regulation and its role in cell migration.

Results: Cell migration was increased following stimulation of cells with recombinant (r) MIP-4 and bleomycin (BLM), whereas quenching rMIP-4 with its antibody (Ab) or addition of the Ab to BLM or H2O2 diminished rMIP-4-induced cell migration. Along with cell migration, rMIP-4, BLM, and H2O2 induced the formation of actin filaments dynamic structures whereas costimulation with MIP-4 Ab limited BLM- and H2O2-induced effects. MIP-4 mRNA and protein were increased by BLM and H2O2, and the addition of its Ab significantly reduced treatments effect. Experiments with siRNA investigating whether Nir-1 is a potential MIR-4 receptor indicated that the inhibition of Nir-1 decreased cell migration/invasion but did not totally inhibit rMIP-4-induced cell migration.

Conclusion: Therefore, our data indicate that MIP-4 is regulated by BLM and H2O2 and costimulation with its Ab limits the effects on MIP-4 and that the Nir-1 receptor partially mediates MIP-4's effects on increased cell migration. These data also evidenced that MIP-4 is regulated by fibrotic and oxidative stimuli and that quenching MIP-4 with its Ab or therapeutically targeting the Nir-1 receptor may partially limit MIP-4 effects under fibrotic or oxidative stimulation.

背景:CC-趋化因子配体 18 又称 MIP-4,是一种在炎症和免疫反应中发挥作用的趋化因子。研究表明,MIP-4 与肺纤维化和癌症等多种疾病的发生发展有关。MIP-4在肺纤维化中究竟是如何调节和发挥作用的,目前仍不清楚。因此,在本研究中,我们研究了 MIP-4 是如何被调控的,以及它是否通过其潜在受体 Nir-1 起作用:A549 细胞在 DMEM :F12 (1 : 1),并添加 10% FBS 和 1000 U 青霉素/链霉素,按照生产商(ATCC)的建议进行培养和保存。采用细胞迁移和侵袭、免疫组织化学(IHC)、Western blot、qPCR 和 siRNA Nir-1 等方法确定 MIP-4 的调控及其在细胞迁移中的作用:结果:用重组(r)MIP-4和博莱霉素(BLM)刺激细胞后,细胞迁移增加,而用其抗体(Ab)淬灭rMIP-4或在BLM或H2O2中加入Ab会减少rMIP-4诱导的细胞迁移。在细胞迁移的同时,rMIP-4、BLM 和 H2O2 诱导了肌动蛋白丝动态结构的形成,而 MIP-4 抗体的成本刺激则限制了 BLM 和 H2O2 诱导的效应。MIP-4 mRNA 和蛋白在 BLM 和 H2O2 的作用下会增加,而加入 MIP-4 Ab 则会明显降低处理效果。用 siRNA 研究 Nir-1 是否是潜在的 MIR-4 受体的实验表明,抑制 Nir-1 可减少细胞迁移/侵袭,但不能完全抑制 rMIP-4 诱导的细胞迁移:因此,我们的数据表明,MIP-4受BLM和H2O2调控,其Ab的成本刺激限制了对MIP-4的影响,Nir-1受体部分介导了MIP-4对细胞迁移增加的影响。这些数据还证明,MIP-4受纤维化和氧化刺激的调控,用MIP-4的Ab淬灭MIP-4或治疗性靶向Nir-1受体可能会部分限制MIP-4在纤维化或氧化刺激下的作用。
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引用次数: 0
In Vitro Antibacterial, Antioxidant, Cytotoxicity Activity, and In Silico Molecular Modelling of Compounds Isolated from Roots of Hydnora johannis. 从 Hydnora johannis 根部分离的化合物的体外抗菌、抗氧化、细胞毒性活性和硅学分子模型。
IF 3.4 Q2 BIOCHEMICAL RESEARCH METHODS Pub Date : 2024-06-21 eCollection Date: 2024-01-01 DOI: 10.1155/2024/3713620
Teshome Degfie, Milkyas Endale, Muhdin Aliye, Rajalakshmanan Eswaramoorthy, Tariku Nefo Duke, Aman Dekebo

The plant Hydnora johannis has been utilized in folk medicine. Analyzing phytochemical composition of dichloromethane/methanol (1 : 1) root part of Hydnora johannis gave oleic acid (1), caffeic acid-2-hydroxynonylester (2), catechin (3), and a pregnane derivative (4). NMR spectroscopy was used to characterize compounds 1-3, while compound 4 was identified through GC-MS analysis and literature comparison. The cytotoxicity of extracts from roots of H. johannis was conducted against MCF-7 cell lines (human breast cancer) by MTT assay. According to the cytotoxicity study, n-hexane extract exhibited a high level of toxicity with 28.9 ± 5.6% cell viability. Antibacterial activity was tested against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pyogen. The highest bacterial growth mean inhibition zone was measured for catechin (3) (13.72 ± 0.05 mm)) against P. aeruginosa at 0.25 mg/mL and acceptable related to standard. Antioxidant activity was studied by the DPPH assay. Based on the data from the antioxidant study, DCM/MeOH extract (70.32%) and catechin (3) showed good antioxidant activity (65.61%) (IC50 0.25 μg/mL) relative to that of the positive control (78.21%, IC50 0.014 μg/mL) at 12.5 μg/mL. In each docking pose, catechin (3) scored higher binding affinity of -7.9, -7.2, and -6.4 kcal/mol towards PqsA, DNA gyraseB, and S. aureus PK, respectively, compared to amoxicillin (-8.1, -6.1, and -6.4 kcal/mol). All five Lipinski rules were obeyed by compounds 1-3, which showed an acceptable drug resemblance. The lipophilicity was computed as less than five (1.47-4.01) indicating a lipophilic property. Catechin (3) obeys Veber's rule implying its good oral bioavailability. Binding affinity scores of catechin (3)-protein interactions are in line with those from in vitro tests, indicating its potential antibacterial effect. The obtained cytotoxicity and antibacterial activity results support the utilization of H. johannis in folk medicine.

植物 Hydnora johannis 一直被用于民间医药。通过分析 Hydnora johannis 根部二氯甲烷/甲醇(1:1)中的植物化学成分,得出了油酸(1)、咖啡酸-2-羟基壬酯(2)、儿茶素(3)和一种孕烷衍生物(4)。利用核磁共振光谱鉴定了化合物 1-3 的特征,而化合物 4 则是通过气相色谱-质谱分析和文献比较确定的。通过 MTT 试验,研究了约翰尼根提取物对 MCF-7 细胞系(人类乳腺癌)的细胞毒性。细胞毒性研究显示,正己烷提取物的毒性较高,细胞存活率为 28.9 ± 5.6%。对大肠杆菌、绿脓杆菌、金黄色葡萄球菌和化脓性链球菌进行了抗菌活性测试。在 0.25 毫克/毫升的浓度下,儿茶素(3)对铜绿假单胞菌的细菌生长平均抑制区最大(13.72 ± 0.05 毫米),与标准值相比是可以接受的。抗氧化活性采用 DPPH 法进行研究。根据抗氧化研究的数据,DCM/MeOH 提取物(70.32%)和儿茶素(3)显示出良好的抗氧化活性(65.61%)(IC50 0.25 μg/mL),而阳性对照(78.21%,IC50 0.014 μg/mL)的抗氧化活性为 12.5 μg/mL。与阿莫西林(-8.1、-6.1和-6.4 kcal/mol)相比,儿茶素(3)在每个对接姿势中与PqsA、DNA gyraseB和金黄色葡萄球菌PK的结合亲和力分别为-7.9、-7.2和-6.4 kcal/mol。化合物 1-3 遵守了所有五条 Lipinski 规则,显示了可接受的药物相似性。计算得出的亲脂性小于 5(1.47-4.01),表明化合物具有亲脂性。儿茶素(3)符合 Veber 规则,这意味着它具有良好的口服生物利用度。儿茶素(3)与蛋白质相互作用的结合亲和力得分与体外测试结果一致,表明其具有潜在的抗菌作用。所获得的细胞毒性和抗菌活性结果支持在民间医药中使用约翰内斯草。
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引用次数: 0
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Biochemistry Research International
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