Journal of Macromolecular Science Part B-Physics
·
2024
·
IF 1.2
Mengmei Yin,Kangrui Yuan,Zhengqi Lv,Yiwen Yuan,Xichen Feng,Qinghua Wu
Lanthanide luminescent materials have rapidly emerged as potential candidates in the fields of drug delivery and bioimaging. In this study a spherical composite material theory with uniform particle size, good biocompatibility, fluorescence emission performance and an efficient targeted drug delivery system was proposed. To achieve this, a facile ultrasonic atomization approach to synthesize sodium alginate-lanthanum (SA-La) cross-linked microspheres at room temperature was developed, and then they were loaded with doxorubicin (DOX), yielding DOX@SA-La for targeted liver cancer cell treatment. Fluorescence studies indicated that the SA-La microspheres exhibited excellent fluorescence properties with intense blue fluorescence emitted. Moreover, the ability of drug release in-vitro of the SA-La and Calcium alginate (SA-Ca) microspheres were proved by UV-visible spectrophotometry, and the drug release values of these two drug carriers were considerable. In addition, cytotoxicity tests via the CCK-8 assay revealed that the DOX@SA-La delivery system considerably inhibited hepatocellular carcinoma cells growth. Conclusively, the SA-La fluorescent microsphere drug carriers enables real-time anti-cancer efficacy observations and analyses, having promise as a potent therapeutic and diagnostic tool for liver cancer treatments and drug tracing in the tumors.
研究领域:
药学
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材料科学
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生物医学工程
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肿瘤学
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生物化学
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DOI
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 6
·817
·
IF 4.8
Luqi Qin,Yixia Zhou,Bei Fan,Jiahuan Zheng,Rao Diao,Jiameng Liu,Fengzhong Wang
Background/Objectives: Endophytes can produce bioactive metabolites similar to their host plants. CM-YJ44 ( Pseudomonas protegens CHA0, 99.24% similarity), an endophyte from Dendrobium officinale , has not yet validated hypoglycemic potential. This study aimed to evaluate its anti-insulin resistance (IR) activity and metabolite profile. Methods: The fermentation broth of CM-YJ44 was separated into three fractions (CM-YJ44-1, -2, and -3) using semi-preparative high-performance liquid chromatography (pre-HPLC). An IR HepG2 cell model was constructed to evaluate their glucose uptake capacity. CM-YJ44-3 was further tested for oxidative stress, inflammatory, and insulin signaling pathway activation. Metabolites in CM-YJ44-3 were preliminarily identified using the Q Exactive Focus LC-MS system (QE), and the dendrobine content was quantified by ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS). Molecular docking was performed to predict the binding affinities between dendrobine and target proteins. Results: Among the three fractions, CM-YJ44-3 significantly reduced nitric oxide (NO) and reactive oxygen species (ROS) levels in IR cells, enhanced glycogen synthesis, upregulated the activities of pyruvate kinase (PK) and hexokinase (HK), and suppressed the expression of inflammatory factors. Its mechanism of action was mainly through activation of the IRS1/PI3K/Akt/GSK3β/GLUT4 signaling pathway. QE analysis preliminarily identified 24 metabolites in CM-YJ44-3. Quantitative analysis by UPLC-MS/MS showed that the dendrobine content was 78.73 ± 4.29 ng/mL. Molecular docking results indicated that dendrobine exhibited binding energies below −5 kcal/mol with multiple target proteins involved in this signaling pathway, suggesting it may be a key bioactive component responsible for the anti-IR effect. Conclusions: This study provides the first evidence of hypoglycemic bioactive metabolite production by strain CM-YJ44, indicating its potential as a novel microbial candidate for alleviating IR.
研究领域:
微生物学
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药理学
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植物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2021
·
IF 7.514
Yue-ming Hu,Su-zhen Lu,Ya-si Li,Hui Wang,Yan Shi,Lu Zhang,Zong-cai Tu
The protective effect of antioxidant peptides from grass carp scale gelatin on hydrogen peroxide (H 2 O 2 ) - mediated oxidative injured HepG2 cells was investigated, and the protective mechanism as well as peptide structure were studied. Pretreated with grass carp scale gelatin hydrolysates (GSGH) for 24 h significantly increased the survival rates and decreased the apoptosis rates of H 2 O 2 - mediated oxidative injured HepG2 cells. The increase in SOD, CAT and GPX activities, reduce in ROS level and MDA content, and weaken in damage on cell membrane and DNA could be responsible for the protective effect of GSGH on H 2 O 2 -mediated oxidative injured HepG2 cells. Peptide sequences of GSGH were analyzed by LC-ESI-Q-Orbitrap-MS/MS, and results showed that most of them were low molecular weight peptide at 358–986 Da. Synergistic effect existed among antioxidant peptides and contributed to the strong antioxidant activities of GSGH.
研究领域:
生物化学
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细胞生物学
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食品科学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2018
·Vol. 19
·期 10
·3184
·
IF 3.687
Zhiwen Qi,Chengzhang Wang,Jianxin Jiang,Caie Wu
A series of novel C15 urushiol derivatives were designed by introducing a pechmann structure and F-, Cl-, and Br-nitro substituents with different electronic properties into its alkyl side chain, as well as a triazolyl functional group in its aromatic oxide. Their chemical structures were determined based on the analysis of the NMR (nuclear magnetic resonance) spectroscopic and mass spectrometric data. The results showed that compound4exhibited a strong inhibition of the HepG2 cell proliferation (half maximal inhibitory concentration (IC50): 2.833 μM to human hepatocellular carcinoma (HepG2), and 80.905 μM to human normal hepatocytes (LO2)). Furthermore, it had an excellent synergistic effect with levopimaric acid. The nitrogen atom of the triazole ring formed a hydrogen-bonding interaction with Gly103, Gly154, and Tyr308, which made compound4bind to histone deacetylase (HDAC)2 more tightly. One triazole ring and His33 formed a π–π stacking effect; the other, whose branches were deep into the pocket, further enhanced the interaction with HDAC2. Meanwhile, compound4involved a hydrophobic interaction with the residues Phe210 and Leu276. The hydrophobic interaction and π–π stacking provided powerful van der Waals forces for the compounds.Keywords:urushiol;triazole;diels-alder;pechmann;anti-tumor;HDAC2
研究领域:
药理学
·
肿瘤学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Nutrition
·
2022
·
IF 6.59
Tao Liang,Gu Fan,Liu Yan,Yang Min,Wu Xing-Zhong,Sheng Jun,Tian Yang
Moringa oleifera leaves are a kind of new food raw materials, rich in functional factors, M. oleifera leaves aqueous extract have antioxidant activity and M. oleifera leave protein is an important active ingredient in the aqueous extract. Numerous studies have shown that peptides have strong antioxidant activity. To reveal the antioxidant effects of M. oleifera (MO) leaves peptides, MO leave antioxidant peptides were isolated and prepared to clarify their antioxidant activity. MLPH1 (<1 kDa), MLPH3 (1~3 kDa), MLPH5 (3~5 kDa), and MLPH10 (5~10 kDa) fractions were obtained by the membrane ultrafiltration classification of MO leaves proteolytic hydrolysate (MLPH). MLPH1 was further separated by centrifugal filters, and the fraction separated by <1 kDa (MLPH1-1) was identified and analyzed by LC–MS/MS. The purpose of this study was to investigate the effect of MO leaves antioxidant peptide pretreatment on H2O2-treated HepG2 cells and to refine the antioxidant activity. The results showed that MLPH1 had the strongest antioxidant activity, and three MO leaves antioxidant peptides (LALPVYN, LHIAALVFQ, and FHEEDDAKLF) were obtained. The peptide with the sequence LALPVYN and a molecular weight of 788.44 Da had the strongest antioxidant activity. After 24 h of LALPVYN pretreatment, the cell viability and the CAT, GSH-Px, and SOD enzyme activity were significantly increased, and the MDA, ROS, and apoptosis rates were significantly decreased. These results provide a theoretical basis for further research on the antioxidant mechanism of MO leaves peptides.
研究领域:
生物化学
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药理学
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细胞生物学
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食品科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOSENSORS & BIOELECTRONICS
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2017
·
IF 7.78
Xuan Cai,Libo Shi,Wenqian Sun,Hongli Zhao,Hong Li,Haiyan He,Minbo Lan
Quantification of superoxide anions (O 2 •− ) is significant in the monitoring of many serious diseases and the design of enzyme-mimic catalysts plays the main role in the development of non-enzymatic O 2 •− sensors. Herein, we proposed a facile self-assembly process to synthesize manganese phosphate modified carbon networks using three kinds of widely-used carbon materials (MWCNTs, NGS and GO) as pillar connectors. Characterizations demonstrate that manganese phosphate is widely dispersed inside and on the surface of carbon networks without visible morphology. Meanwhile, all three kinds of synthesized catalysts were successfully immobilized on the screen-printed carbon electrodes to evaluate the electrochemical performance of fabricated sensors. The results indicate that sensors based on Mn x (PO 4 ) y modified MWCNTs exhibit high sensitivity with an extremely low detection limit of 0.127 μM (S/N = 3) and a wide liner range of 0–1.817 mM (R 2 = 0.998). We further employed the recommended sensors in the real-time monitoring of HepG2 cells released O 2 •− under the stimulating of Zymosan (20 mg/mL). Noticeably, the proposed sensors exhibit not only sensitive response but also stable current steps upon different addition of Zymosan. The calculated concentrations of cell-released O 2 •− vary from 6.772 to 24.652 pM cell −1 for the Zymosan amount used in this work. The established novel sensors display low background current and signal noises, thus holding unique advantages in the trace analysis of O 2 •− in biological samples and in vivo environment.
研究领域:
生物化学
·
医学诊断
✓ 已验证
DOI
PubMed
高影响因子
Evidence-based Complementary and Alternative Medicine
·
2021
·
IF 2.63
Jian Zhao,Hewei Li,Wanying Li,Zixian Wang,Zhewen Dong,Huan Lan,Chengqiang Wang,Jia-Le Song
Sinapic acid (Sa) is a small-molecule phenolic acid compound predominant in fruits, vegetables, and grains. This study investigated the antitumor effects of cisplatin (DDP) combined with Sa (Sa/DDP) on the hepatic cancer cells (HCC), HepG2 and SMMC-7721. The HepG2 and SMMC-7721 cells were treated with Sa or Sa/DDP, and the cell proliferation and cell cycle were detected using the MTT assay. The cell migration was detected using the transwell and scratch assays, while apoptosis and autophagy were detected using Hoechst, MDC, and Annexin V-FITC/PI staining. The protein expression was quantitated using the western blot. Sa/DDP was found to not only inhibit cancer cell proliferation and migration but also induce cell apoptosis. Simultaneously, the Sa/DDP combination was found to activate autophagy, and the HCQ autophagy inhibitor enhanced the apoptosis in the Sa/DDP-induced liver cancer cells. The combined use of Sa and DDP makes it an attractive adjuvant therapy strategy for tumors, establishing the prospect of phenolic acid compounds for the adjuvant treatment of hepatocellular carcinoma.
研究领域:
肿瘤学
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药理学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2017
·Vol. 7
·期 66
·41779-41786
·
IF 3.108
Zhou Yang,Fan Wu,Hongjie Yang,Ping Zhou
A novel protein tyrosine phosphatase 1B (PTP1B) inhibitor, FYGL, extracted from Ganoderma lucidum, was first reported to have an efficient hypoglycemic effect and high safety in vivo in our previous study. However, the underlying mechanism of the anti-diabetes activity was still unclear. The dominant effective component of FYGL was demonstrated to be a neutral hyperbranched proteoglycan macromolecule. Therefore, it is necessary to first elucidate how the biomacromolecule works at the cellular level, in order to understand its possible functional mechanism in vivo. Herein, we focused on demonstrating the cell internalization and endocytosis mechanism of FYGL in HepG2 cells. A series of cellular uptake pathways was explored, including clathrin-mediated endocytosis, caveolae/lipid-mediated endocytosis, and macropinocytosis. Confocal laser scanning microscopy and flow cytometry were used to demonstrate the absorption of FYGL by HepG2 cells. Furthermore, pharmacologically selective inhibitors and Western blot methods were used to demonstrate that macropinocytosis mediated by c-Src/PI3K cascades was the preferred route for the uptake of FYGL in cells. Our study provided the basis of uptake of FYGL for an efficient hypoglycemic effect. The functional mechanism of the signaling pathway in vivo will be reported in the future.
研究领域:
药理学
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细胞生物学
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分子生物学
✓ 已验证
产品关联
DOI
高影响因子
AAPS PHARMSCITECH
·
2018
·Vol. 19
·期 5
·2048-2057
·
IF 2.666
Zhai Qingqing,Li Hailong,Song Yanlin,Wu Ruijiao,Tang Chuanfang,Ma Xiaodong,Liu Zhihao,Peng Jinyong,Zhang Jianbin,Tang Zeyao
This work aimed to develop and optimize several lipid nanocapsule formulations (LNCs) to encapsulate cisplatin (CDDP) for treatment of hepatocellular carcinoma. By comparing the effect of oil/surfactant ratio, lecithin content, and oil/surfactant type on LNC characteristics, two LNCs were selected as optimal formulations: HS15-LNC (Solutol HS 15/MCT/lecithin, 54.5:42.5:3%, w / w ) and EL-LNC (Cremophor EL/MCT/lecithin, 54.5:42.5:3%, w / w ). Both LNCs could effectively encapsulate CDDP with the encapsulation efficiency of 73.48 and 78.84%. In vitro release study showed that both LNCs could sustain the release CDDP. Moreover, cellular uptake study showed that C6-labeled LNCs could be effectively internalized by HepG2 cells. Cellular cytotoxicity study revealed that both LNCs showed negligible cellular toxicity when their concentrations were below 313 μg/mL. Importantly, CDDP-loaded LNCs exhibited much stronger cell killing potency than free CDDP, with the IC50 values decreased from 17.93 to 3.53 and 5.16 μM after 72-h incubation. In addition, flow cytometric analysis showed that the percentage of apoptotic cells was significantly increased after treatment with LNCs. Therefore, the prepared LNC formulations exhibited promising anti-hepatocarcinoma effect, which could be beneficial to hepatocellular carcinoma therapy.
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Food & Function
·
2025
·
IF 5.4
Qi Gu,Litao Wang,Mingyue Xu,Wan-Mei Zhou,Guosheng Liu,Haiting Tian,Thomas Efferth,Chenlu Wang,Yujie Fu
Phloretin is a natural dihydrochalcone with a variety of biological activities. Its potential in modulating lipid metabolism in vitro and in vivo with HepG2 and C. elegans was investigated in this study. Phloretin significantly diminished lipid accumulation and ROS levels, mitigated the degree of lipid peroxidation, and ameliorated mitochondrial dysfunction in HepG2 cells. The expression levels of lipid synthesis genes (SREBP and FASN) were downregulated, while PI3K-AKT related genes (AKT, FOXO, MTOR) were upregulated. Furthermore, phloretin significantly alleviated the detrimental effects of lipid accumulation on growth indices and locomotor ability in C. elegans. It also reduced lipofuscin, ROS level as well as glucose and triglyceride contents, significantly affected amino acid and lipid metabolism pathways based on metabolomics profiles and analysis. Gene expression levels of sbp-1, mdt-15, fat-5, fat-6, and fat-7 were markedly down-regulated following treatment with phloretin, while daf-16, age-1 and skn-1were significantly up-regulated. Tests with mutant C. elegans strains of daf-16, age-1, sbp-1 and nhr-49 further confirmed that the phloretin-induced decrease in lipid accumulation was attributed to the inhibition of lipid biosynthesis pathway by IIS and sbp-1/SREBP. Our study indicated that phloretin exerted hypolipidemic effects in vitro and in vivo, providing a basic foundation for considering phloretin as a phytochemical candidate for regulating lipid metabolism and preventing hyperlipidemia.
研究领域:
代谢生物学
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分子生物学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF HAZARDOUS MATERIALS
·
2020
·
IF 9.038
Qiang Chu,Wen Chen,Ruoyi Jia,Xiang Ye,Yonglu Li,Yangyang Liu,Yong Jiang,Xiaodong Zheng
Acrylamide (ACR), as a raw material of polyacrylamide that used in water purification, was verified to possess various toxicity. Tetrastigma hemsleyanum (TH) is a medicinal plant widely used to anti-inflammation and anti-tumor in Chinese folks. However, more researches focused on the biological activities in tubers and the leaves were ignored. Thus, the protective effect of Tetrastigma hemsleyanum leaves extract (THLE) against ACR-induced toxicity in HepG2 cells and Caenorhabditis elegans ( C. elegans ) was explored in this study. In vitro , we observed that THLE attenuated ACR-induced toxicity in HepG2 cell via regulating Akt/mTOR/FOXO1/MAPK signaling pathway. Further research proved that 5-caffeoylquinic acid (5-CA) plays a major role in THLE’s amelioration effect of ACR toxicity. In vivo , it was found that THLE possesses the same protective effect in ACR-treated wild-type N2 C. elegans and daf-2 (-) (deficit in DAF-2) mutants. However, the anti-ACR toxicity effect of THLE in daf-16 (-) mutants (deficit in DAF-16 that homologous to FOXO family in human) was weakened. Our results indicated that THLE exhibited protective effects against ACR-induced toxicity both in HepG2 cells and C. elegans , while DAF-16/FOXO gene is involved in THLE’ protective effect via regulating the expression levels of downstream antioxidant genes.
研究领域:
药理学
·
毒理学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2024
·
IF 2.5
Mengyun Dong,Tianliang Zhang,Xueli Liang,Xinyi Cheng,Fuyan Shi,Hang Yuan,Fengxiang Zhang,Qiqi Jiang,Xia Wang
Sesamin, a special compound present in sesame and sesame oil, has been reported a role in regulating lipid metabolism, while the underlying mechanisms remain unclear. Autophagy has been reported associated with lipid metabolism and regarded as a key modulator in liver steatosis. The present work aimed to investigate whether sesamin could exert its protective effects against lipid accumulation via modulating autophagy in HepG2 cells stimulated with oleic acid (OA). Cell viability was evaluated using the CCK-8 method, and triglycerides (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein, cholesterol (LDL-C), alanine aminotransferase (ALT), along with aspartate aminotransferase (AST) were assessed by oil red O staining, transmission electron microscopy (TEM), and biochemical kits to investigate the lipid-lowering effects of sesamin. Differentially expressed genes were screened by RNA sequencing and validated using real-time quantitative PCR and Western blot. Autophagy and mitophagy related molecules were analyzed employing TEM, Western blot, and immunofluorescence. The data shows that in HepG2 cells stimulated by OA, sesamin reduces levels of TG, TC, LDL-C, ALT, and AST while elevating HDL-C, alleviates the lipid accumulation and improves fatty acid metabolism through modulating the levels of fat metabolism related genes including PCSK9, FABP1, CD36, and SOX4. Sesamin restores the suppressed autophagy in HepG2 cells caused by OA, which could be blocked by autophagy inhibitors. This indicates that sesamin improves fatty acid metabolism by enhancing autophagy levels, thereby mitigating the intracellular lipid accumulation. Furthermore, sesamin significantly enhances the mitophagy and improves mitochondrial homeostasis via activating the PINK/Parkin pathway. These data suggest that sesamin alleviates the excessive lipid accumulation in HepG2 caused by OA by restoring the impaired mitophagy via the PINK1/Parkin pathway, probably playing a preventive or therapeutic role in hepatic steatosis.
研究领域:
药理学
·
细胞生物学
·
分子生物学
·
代谢
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）