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Bioresources and Bioprocessing · 2025 ·Vol. 12 ·期 1 ·1-13 · IF 5.1

Tea leaf exosome-like nanoparticles (TELNs) improve oleic acid-induced lipid metabolism by regulating miRNAs in HepG-2 cells

Lei Xuanhao,Li Haonan,Chen Sibei,Li Bing,Xia Huili,Li Jun,Guan Feng,Ge Jian

Tea is a widely consumed beverage globally, but the tea industry faces a significant waste management challenge. In this study, we developed tea leaf exosome-like nanoparticles (TELNs) with an average size of 274 ± 24.7 nm and a zeta potential of -20.6 ± 0.78 mV, using polyethylene glycol (PEG) 6000 precipitation followed by ultracentrifugation. Structural analysis confirmed that TELNs are composed of lipids, proteins, and RNAs. In vitro assays on HepG-2 cells revealed that TELNs are non-toxic at concentrations up to 300 µg/mL and can be efficiently internalized. TELNs exhibited significant antioxidant capacity and were able to significantly ameliorate H 2 O 2 -induced oxidative stress, increase the viability and reduce the accumulation of ROS in Hepg-2 cells. Notably, TELNs significantly alleviated OA-induced lipid metabolic disorders and hepatocellular injury. Further molecular analysis revealed that TELNs downregulated the expression of miR-21-5p, miR-17-3p, and miR-107, leading to the upregulation of their target genes PPARα, CYP7A1, and CPT-1A, which contributed to the improvement of lipid metabolism. This study is the first to demonstrate the lipid metabolism regulation potential of TELNs, providing new insights into their underlying mechanisms and helping to develop new therapeutic strategies for lipid metabolism-related diseases. Furthermore, it expands the scope of tea use and helps to reuse tea residues. Graphical

CAS / MDL: 112-80-1 7722-84-1
研究领域: 食品科学 · 分子生物学 · 营养学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2021 · IF 6.953

Isolation, characterization and HepG-2 inhibition of a novel proteoglycan from Flammulina velutipes

Hui Xu,Ye Hu,Qiuhui Hu,Jianhui Liu,Anxiang Su,Minhao Xie,Gaoxing Ma,Fei Pei,Alfred Mugambi Mariga,Wenjian Yang

Flammulina velutipes has anti-inflammatory, immunomodulatory, antioxidant and many bioactive properties with high contents of carbohydrate, proteins and fibers. In this study, a novel proteoglycan with polysaccharide complexes and protein chain, named PGD1-1, was isolated from F. velutipes . The structural characteristics of PGD1-1 were then determined, and its anti-proliferation and pro-apoptotic activities against HepG-2 cells were demonstrated in vitro. Results proved that the average molecular weight of PGD1-1 was 32.71 kDa, and the carbohydrate and protein contents were 93.35 and 2.33%, respectively. The protein moiety was bonded to a polysaccharide chain via O-glycosidic linkage. The monosaccharides consisted of d -glucose, D-galactose and D-xylose in a molar ratio of 21.90:2.84:1.00. PGD1-1 significantly inhibited the proliferation of HepG-2 cells by affecting cell lipid peroxidation and nitric oxide production. In addition, PGD1-1 promoted the apoptosis of HepG-2 cells, especially the early apoptosis. These findings proved that PGD1-1 was a novel potent ingredient against the proliferation of HepG-2, which will provide a theoretical basis for the development and utilization of the functional ingredients of the F. velutipes .

研究领域: 分子生物学 · 肿瘤学 · 药理学
✓ 已验证 DOI PubMed 高影响因子
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MOLECULES · 2023 ·Vol. 28 ·期 19 ·6843 · IF 4.6

Ni/Mn-Complex-Tethered Tetranuclear Polyoxovanadates: Crystal Structure and Inhibitory Activity on Human Hepatocellular Carcinoma (HepG-2)

Fumei Shi,Yilan Chen,Chuanheng Dong,Jiajia Wang,Chunman Song,Yalin Zhang,Zhen Li,Xianqiang Huang

Polyoxometalates (POMs) exhibit unique structural characteristics and excellent physical and chemical properties, which have attracted significant attention from scholars in the fields of anticancer research and chemotherapy. Herein, we successfully synthesized and structurally characterized two novel polyoxovanadates (POVs), denoted as POVs-1and POVs-2, where [M(1-vIM)4]2[VV4O12]·H2O (M: NiIIand MnII, 1-vinylimidazole abbreviated as 1-vIM) serve as ligands. The two POVs are isomeric and consist of fundamental structural units, each comprising one [V4O12]4−cluster, two [M(1-vIM)4]2+cations, and one water molecule. Subsequently, we evaluated the cell viability of human hepatocellular carcinoma (HepG-2) cells treated with the synthesized POVs using the MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazoliumbromide) assay. And the changes in cell nucleus morphology, mitochondrial membrane potential (Δψm), and reactive oxygen species levels in HepG-2 exposed to POVs were monitored using specific fluorescent staining techniques. Both hybrid POVs showed potent inhibitory activities, induing apoptosis in HepG-2 cells along with significant mitochondria dysfunction and a burst of reactive oxygen species. Notably, the inhibitory effects of POVs-2were more pronounced than those of POVs-1, which is primarily attributed to the different transition metal ions present. These findings underscore the intricate relationship between the metal components, structural characteristics, and the observed antitumor activities in HepG-2 cells.Keywords:polyoxovanadates;imidazole ligands;human hepatocellular carcinomas;anticancer;apoptosis

研究领域: 生物化学 · 肿瘤学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2022 ·Vol. 27 ·期 1 ·281 · IF 4.927

Dual-Responsive Alginate Hydrogel Constructed by Sulfhdryl Dendrimer as an Intelligent System for Drug Delivery

Li Li,Dongyu Lei,Jiaojiao Zhang,Lu Xu,Jiashan Li,Lu Jin,Le Pan

Intelligent stimulus-triggered release and high drug-loading capacity are crucial requirements for drug delivery systems in cancer treatment. Based on the excessive intracellular GSH expression and pH conditions in tumor cells, a novel glutathione (GSH) and pH dual-responsive hydrogel was designed and synthesized by conjugates of glutamic acid-cysteine dendrimer with alginate (Glu-Cys-SA) through click reaction, and then cross-linked with polyethylene glycol (PEG) through hydrogen bonds to form a 3D-net structure. The hydrogel, self-assembled by the inner disulfide bonds of the dendrimer, is designed to respond to the GSH heterogeneity in tumors, with a remarkably high drug loading capacity. The Dox-loadedGlu-Cys-SAhydrogel showed controlled drug release behavior, significantly with a release rate of over 76% in response to GSH. The cytotoxicity investigation indicated that the prepared DOX-loaded hydrogel exhibited comparable anti-tumor activity against HepG-2 cells with positive control. These biocompatible hydrogels are expected to be well-designed GSH and pH dual-sensitive conjugates or polymers for efficient anticancer drug delivery.

研究领域: 药学 · 生物医学工程 · 材料科学 · 肿瘤学
✓ 已验证 DOI 高影响因子
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CHINESE JOURNAL OF CHEMISTRY · 2016 ·Vol. 34 ·期 6 ·609-616 · IF 1.872

Improvement of Stability and Anticancer Activity of Chlorambucil-Tetrapeptide Conjugate Vesicles

Wei Zhang,Wenjun Zhu,Ruiyu He,Shuo Fang,Yemin Zhang,Chen Yao,Muhammad Ismail,Xinsong Li

Chlorambucil is a classic nitrogen mustard drug that has been used in the treatment of cancers. It may induce neutropenia, thrombocytopenia and other side effects because of its short lifetime and off-target effect. In this report, chlorambucil-tetrapeptide (AAAK, A 3 K) conjugate vesicles were developed to improve the stability and bioactivity of chlorambucil. First of all, chlorambucil-A 3 K conjugate was synthesized by solid phase synthesis strategy. Secondly, the chlorambucil-A 3 K conjugate was assembled and characterized by critical aggregation concentration, circular dichroism, dynamic light scattering and transmission electron microscopy. The results indicated that the chlorambucil-A 3 K conjugate can be assembled to form spherical vesicles with an average diameter of 390.5 nm, and high drug loading about 47.1% is reached. Surprisingly, the preliminary biological evaluation of the chlorambucil-A 3 K conjugate vesicles revealed the best in vitro anticancer activity against HeLa, HepG-2 and MCF-7 cell lines compared with chlorambucil and chlorambucil-A 3 K conjugate free drugs. Furthermore, conjugate vesicles showed excellent in vivo antitumoral activity. It can be partly attributed to their vesicular structure which isolates chlorambucil active moiety from aqueous solution to retard degradation before killing cancer cells. Therefore, chlorambucil-peptide (A 3 K) conjugate vesicles may be an alternative delivery system of chlorambucil.

CAS / MDL: 1122-58-3 540-63-6
研究领域: 药学 · 癌症研究 · 纳米技术 · 药物递送系统
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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2017 ·Vol. 52 ·期 5 ·1176-1184 · IF 1.64

Carboxymethylation of corn bran polysaccharide and its bioactive property

Jing Li,Wenting Shang,Xu Si,Dandan Bu,Padraig Strappe,Zhongkai Zhou,Chris Blanchard

Summary Corn bran polysaccharides were extracted using an ultrasonic-assisted method with a yield of 33.50% and then carboxymethylated. The occurrence of modification was confirmed using Fourier transform infrared spectral analysis. The surface of polysaccharide particles became loosened following the carboxymethylation. The effect of sodium hydroxide concentration, reaction temperature, and the reaction time on the degree of substitution was investigated, and the relationship among the substitution degree, total phenolic content and antioxidant activity were studied. With sodium hydroxide concentration of 6.0 mol L −1 , keeping the reaction temperature of 60 °C and reaction time of 5.0 h, the modified polysaccharides possessed the highest degree of substitution and antioxidant activity. Cell culture model indicated that the carboxymethylated polysaccharide significantly inhibited the proliferation of A549 and HepG-2 cells, and these antitumour characteristics may be associated with the elevated expression of CASP3 , CASP8 , CASP9 , and p53 , as well as the significantly decreased expression of Bcl-2 and iNOS genes. The excellent antioxidant capacity and strong antitumour activity of these polysaccharides might provide a potential application as a naturally functional ingredient.

研究领域: 食品科学 · 生物化学 · 药理学 · 分子生物学
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CHEMISTRY & BIODIVERSITY · 2020 ·Vol. 17 ·期 9 ·e2000066 · IF 2.039

Design, Synthesis and in Vitro Evaluation of Tylophorine Derivatives as Possible Antitumor Agents

Zhiguo Mang,Shuai Zhang,Jing Bai,Meijuan Li,Hao Li

Structural simplification and modification of natural products are always very important resources to antitumor drugs. By introducing various aminomethyl groups and amide groups into the phenanthrene ring of tylophorine, a novel series of tylophorine derivatives have been designed and synthesized, and their antiproliferative activities against MCF-7, A549 and HepG-2 cells have been evaluated, too. The results indicated that most of the prepared compounds exhibited good antitumor activities. Especially, one compound with an {ethyl[2-(morpholin-4-yl)ethyl]amino}methyl group at the side chain exhibited the most significant cytotoxic effects.

CAS / MDL: 67-68-5
研究领域: 肿瘤学 · 药物化学 · 天然产物研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMOMETRICS AND INTELLIGENT LABORATORY SYSTEMS · 2022 · IF 4.175

Quantification of miRNAs by mass spectrometry based on DNase I-assisted amplification with the aid of a chemometric model

Qing Liu,Xin Fang,Zeng-Ping Chen,Cai-Xia Shi,Ru-Qin Yu

Herein, the hydrolysis patterns of DNase I against a DNA probe in both single-strand form and DNA/miRNA heteroduplex were experimentally investigated in detail by mass spectrometric technique. Based on the knowledge obtained in the experiments, DNase I-assisted signal amplification strategy was proposed and used to design a mass spectrometric platform for miRNA detection. As a proof of concept, the performance of the proposed platform was evaluated for the detection of miRNA-122 in cell lysate samples. An advanced calibration model was explicitly derived to model the relationships between the concentration of miRNA-122 and the mass spectral signals of mass spectrometrically detected fragments of the DNA probe produced in the DNase I-assisted signal amplification process. With the aid of the advanced calibration model, the proposed mass spectrometric platform achieved quite accurate quantification results for miRNA-122 in cell lysate samples of Huh-7 and HepG-2 ​cell lines with recovery rates ranging from 98% to 104%. It is noteworthy that the proposed mass spectrometric platform can differentiate the target miRNA from other non-target ones based on their mass spectral response patterns instead of mass spectral intensities, and hence possesses high specificity for the target miRNA. It is reasonable to expect that the combination of mass spectrometry based on DNase I-assisted signal amplification with the advanced chemometric model provides a competitive alternative for designing cost-effective and label-free miRNA detection methods.

CAS / MDL: 1609-47-8
研究领域: 生物化学 · 分子生物学 · 分析化学
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Journal of Biobased Materials and Bioenergy · 2022 ·Vol. 16 ·期 1 ·117-126 · IF 0.687

Liquid Chromatography-Mass Spectrometry Characterized Hydrolysate Fractions Possess Anticancer Activity In Vitro

Feng Nianjie,She Shaowen,Hu Chuanqin,Wu Qian

To find new plant-derived antitumor drugs, hydrolysate and fractions of poplar were analyzed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for their inhibitory effect against liver cancer HepG-2 cells. Strong cytotoxicity of hydrolysate was revealed at processing temperature of 180 °C or above. The hydrolysate formed at 180 °C was sequentially extracted using organic solvent to obtain five fractions, and only the diethyl ether-soluble fraction (F De) showed specific cytotoxicity. The eluted fraction of acetone/n-hexane (F 1) was further isolated by column chromatography separation from the F De fraction at a yield of 70%, and could severely decrease cell viability. LC-MS chromatography indicated that 5-hydroxymethyl furfural, ρ-hydroxybenzoic acid and syringaldehyde were the main compounds in the F 1 fraction. Furthermore, the results of flow cytometry, Western blotting, and polymerase chain reaction indicated that syringaldehyde could tightly control the growth and metabolism of HepG-2 cells. The findings could move forward the value-added applications of lignocellulosic hydrolysate on traditional medicines.

研究领域: 植物学 · 遗传学 · 肿瘤学 · 药理学 · 分析化学
✓ 已验证 DOI 高影响因子
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RSC Advances · 2017 ·Vol. 7 ·期 67 ·42159-42167 · IF 3.108

Folic acid-conjugated carbon dots as green fluorescent probes based on cellular targeting imaging for recognizing cancer cells

Xuewei Zhao,Junli Zhang,Lihong Shi,Ming Xian,Chuan Dong,Shaomin Shuang

Implementing visual detection of cancer cells has the potential to contribute greatly to basic biological research; early diagnosis of cancer is still a challenging issue. In this work, we designed and fabricated folic acid-conjugated fluorescent carbon dots (FA-CDs) for targeted imaging of cancer cells. The green fluorescent CDs were prepared by a facile hydrothermal treatment of dandelion as the carbon source and ethanediamine (EDA). The surfaces of the CDs possessed active amino groups for further covalent conjugation with FA. The uptake of FA-CDs into HepG-2 cells occurs via receptor-mediated endocytosis; this was confirmed by a comparative experiment using FR-negative (FR−) PC-12 cells as revealed by confocal laser scanning microscopy. Intracellular experiments demonstrated that the FA-CDs could accurately recognize positive FR (FR++/FR+) cancer cells in different cell mixtures of MCF-7/HepG-2 cells and HepG-2/PC-12 cells and could distinctly indicate the expression level of FR on the membranes of the cancer cells. The FA-CDs show excellent biocompatibility and low toxicity and may have great potential as an effective tool for accurately differentiating cancer cells from normal cells, in addition to cancer detection, prognosis, and individualized treatment.

研究领域: 生物医学工程 · 癌症生物学 · 材料科学 · 细胞生物学 · 纳米技术
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RSC Advances · 2014 ·Vol. 5 ·期 10 ·7773-7780 · IF 3.708

Surface charge effect on the cellular interaction and cytotoxicity of NaYF4:Yb3+, Er3+@SiO2 nanoparticles

Junping Zhang,Fuyao Liu,Tao Li,Xiuxia He,Zhenxin Wang

Taking advantage of the unique optical properties of upconversion nanoparticles (NP) and the feasibly modified nature of SiO2, NaYF4:Yb3+, Er3+@SiO2 core@shell (UCNP@SiO2) NPs with excellent morphology have been synthesized to investigate the surface charge effect on the interactions of NPs with cells. The cellular uptake behaviors, cytotoxicities and intracellular metal ion release of the as-prepared NPs have been investigated in two cell lines (HeLa and HepG-2) by fluorescence microscopy, MTT assay and inductively coupled plasma mass spectrometry (ICP-MS), respectively. It is found that the UCNP@SiO2 NPs with positive surface charge have much higher cell internalization ability and cytotoxicity than those with negative surface charge. The experimental results also demonstrate that the cytotoxicity of UCNP@SiO2 NP is closely related to the increase of intracellular reactive oxygen species (ROS) and metal ion release of internalized NPs.

研究领域: 纳米技术 · 细胞生物学 · 材料科学 · 毒理学
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Sensing and Bio-Sensing Research · 2015 · IF 0

Cy5 labeled single-stranded DNA-polydopamine nanoparticle conjugate-based FRET assay for reactive oxygen species detection

Lina Ma,Zhen Lei,Fuyao Liu,Zhenxin Wang

This work reports on a simple and feasible fluorescence resonance energy transfer (FRET) assay for detecting reactive oxygen species (ROS) both in solution and living cell using polydopamine nanoparticle (PDA NP) as energy acceptor and Cy5 labeled single-stranded DNA (Cy5-ssDNA) as energy donor. The Cy5-ssDNA and PDA NPs form self-assembled conjugates (Cy5-ssDNA-PDA NP conjugates) via π-stacking interactions. In the presence of ROS, the PDA NP adsorbed Cy5-ssDNAs can be effectively cleaved, resulting in the release of Cy5 molecules into solution and recovery of fluorescence emission of Cy5. In order to obtain ROS solution, the glucose oxidase-catalyzed oxidation reaction of glucose with O 2 is employed to generate hydrogen peroxide for Fenton-like reaction. The formation of ROS in Fenton-like reaction can be detected as low as glucose oxidase-catalyzed oxidation of 100   pM glucose by the Cy5-ssDNA-PDA NP conjugate-based FRET assay. The recovery ratio of Cy5 fluorescence intensity is increased linearly with logarithm of glucose concentration from 100   pM to 1   μM, demonstrating that the FRET assay has wide dynamic range. In particular, intracellular ROS has been successfully detected in chemical stimulated HepG-2 cells by the Cy5-ssDNA-PDA NP conjugate-based FRET assay with a fluorescence microscopy, indicating that this approach has great potential to monitor ROS in living cells.

研究领域: 分析化学 · 生物化学 · 分子生物学 · 纳米技术
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