INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2020
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IF 5.162
Jing-Yu Liu,Xiao-Xiao Hou,Zhuo-Yu Li,Shu-Hua Shan,Ming-Chang Chang,Cui-Ping Feng,Yin Wei
The fruiting body of Hericium erinaceus has been used to treat digestive system disorder-related diseases for over 2000 years in China. A novel polysaccharide, HEFP-2b, was obtained from H. erinaceus fruiting bodies. Physical and chemical analysis showed that HEFP-2b consisted of fucose, galactose, glucose, and mannose in molar ratio of 11.81:22.82:44.28:21.09, and that its molecular weight was 3.252 × 10 4 Da. The backbone of HEFP-2b consisted of →6)-linked-α-D-Glc p -(1→ and →4)-β-D-Gal p -(1→ and →3,6) -α-D-Man p linkage, with two side-branching units of (1→ and →6)-β-D-Gal p and (1→ and →4)-α-D-Man p , terminated by Glc and Fuc. The results of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and cell cycle arrest experiments revealed that HEFP-2b considerably inhibited the growth of colon cancer cells (HCT-116) in vitro . The growth inhibitory effects of HEFP-2b correlated with their ability to arrest the cell cycle at the S -phase. Our results will provide valuable information for future studies on HEFP-2b as a novel health-promoting functional food ingredient that can be used for treating colon cancer.
研究领域:
药理学
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肿瘤学
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生物化学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Inorganics
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2022
·Vol. 10
·期 11
·202
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IF 3.149
Liang Qin,Fenglan Liang,Yan Li,Jiana Wu,Shiyuan Guan,Meiyin Wu,Shiling Xie,Manshi Luo,Deyun Ma
A hydrostable 2D Zn-based MOF, {[Zn(5-PIA)(imbm)]·2H2O}n(1) (5-H2PIA = 5-propoxy-isophthalic acid, imbm = 1,4-di(1H-imidazol-1-yl)benzene), was synthesized and structurally characterized. Complex1shows good water and thermal stability based on the TGA and PXRD analyses and displays a 2D framework with 1D channels of 4.8 × 13.8 and 10.0 × 8.3 Å2along theaaxis. The 5-fluorouracil (5-FU) payload in activated complex1(complex1a) is 19.3 wt%, and the cumulative release value of 5-FU at 120 h was about 70.04% in PBS (pH 7.4) at 310 K. In vitro MTT assays did not reveal any cytotoxic effect of NIH-3T3 and HEK-293 cells when the concentration of1was below 500 μg/mL and 5 μg/mL, respectively. No morphological abnormalities were observed on zebrafish exposed to complex1.Keywords:zinc-organic framework;drug delivery;5-fluorouracil;MTT assays;zebrafish toxicity
研究领域:
材料科学与工程
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医学
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药理学
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产品关联
DOI
高影响因子
PLoS One
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2017
·Vol. 12
·期 8
·e0183941
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IF 2.806
Wen Che,Yun Bao,Feng Tang
Background
Resistance to human epidermal growth factor receptor-2 (HER2)-targeted therapies is common, and results in treatment failure and new tumor progression. C35 is over-expressed in many invasive breast cancer endogenously, and functions as an oncogene in breast cancer cell lines.
Methods
The current study aims to investigate effects of C35 on cell viability and migration of HER2-positive breast tumor cells and explore possible mechanisms. The protein expression of C35 in BT-474 breast ductal carcinoma cells was interfered by siRNAs. MTT assay was utilized to detect the viability of BT474 breast ductal carcinoma cells after transfection. The migration of BT474 breast ductal carcinoma cells was examined by cell wound scratch assay.
Results
In addition, the protein expression of C35, HER2, AKT and p-AKT in breast ductal carcinoma cells were detected by Western Blot. The protein expression of C35 was weaker in siRNA1 and siRNA2 groups compared with the control group. The relative expression ratio of C35 to β-actin decreased significantly in siRNA2 and siRNA1 groups. When C35 expression was interfered by siRNA1 and siRNA2 for 48 h, the viability of BT474 breast ductal carcinoma cells decreased compared with the control group. In addition, the migration of breast ductal carcinoma cells decreased when C35 expression was interfered by siRNA1 for 24 h, and interfered by siRNA1 and siRNA2 for 48 h.
研究领域:
肿瘤学
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分子生物学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
Cancer Biomarkers
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2019
·Vol. 24
·期 4
·469-475
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IF 2.859
Qin Yujing,Li Wenxue,Long Yingli,Zhan Zhijia
OBJECTIVE: This study aims to determine the correlation between p-cofilin expression and cisplatin resistance in patients with ovarian cancer, and also to investigate the role of p-cofilin in prognosis. PATIENTS AND METHODS: The ovarian cancer cell line A2780/DDP resistant to cisplatin was prepared. The cell resistance to cisplatin was measured via MTT assay. The cell invasion capacity was identified via Transwell assay. The mRNA expression and protein level was evaluated via semi-quantitative PCR and Western blot, respectively. The tumor tissues of patients with cisplatin-resistant ovarian cancer were collected. The relationship between prognosis and p-cofilin expression was analyzed. RESULTS: The growth rate of A2780 was similar to that of A2780/DDP. The sensitivity of A2780 to cisplatin was significantly higher than that of A2780/DDP (p< 0.01). The migration capacity of A2780/DDP was significantly increased compared to that of A2780 (p< 0.01), indicating that the cisplatin-resistant cell lines were successfully constructed. Both CFL1 mRNA level and p-cofilin level in A2780/DDP was significantly higher than that in A2780 (p< 0.01). The p-cofilin level in cancer tissues in patients with cisplatin-resistant ovarian cancer was significantly higher than that in patients with cisplatin-sensitive ovarian cancer (p< 0.01). The cisplatin resistance was positively correlated with the p-cofilin expression level (r= 0.802, p= 0.023). The survival time of patients with normal or low level of p-cofilin was significantly longer than that of patients with high expression. CONCLUSION: The cisplatin resistance of ovarian cancer is closely related to the expression level of p-cofilin, which affects the prognosis of patients with ovarian cancer.
研究领域:
肿瘤学
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分子生物学
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癌症研究
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产品关联
DOI
PubMed
高影响因子
NATURAL PRODUCT RESEARCH
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2021
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IF 2.862
Meitao Duan,Ahmed Mahal,Ban Mohammed,Yongyan Zhu,Huaming Tao,Shaoyu Mai,Maysoon Al-Haideri,Quanhong Zhu
Three new derivatives of tetrahydrocurcumin 6, 7 and 9 have been prepared as potent antitumor agents using copper(II)-catalyzed ‘click chemistry’. Their structures were identified using 1H-NMR, 13C-NMR and HRMS techniques. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay has been carried out to investigate the in vitro cytotoxicity against human cervical carcinoma (HeLa), human lung adenocarcinoma (A549), human hepatoma carcinoma (HepG2) and human colon carcinoma (HCT-116). Compound 6 has showed significant inhibitory activity against HCT-116 cell line with an IC50 value of 17.86 μM compared to tetrahydrocurcumin (50.96 μM) and positive control etoposide (19.48 μM) while showed no inhibitory activity against NCM460 cell line. Compounds 7 showed moderate inhibitory activity compared to tetrahydrocurcumin and etoposide while compound 9 showed no obvious inhibitory activity. The results suggested further structure modifications of tetrahydrocurcumin to improve its anticancer activity.
研究领域:
化学
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药理学
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
Food Science & Nutrition
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2024
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IF 3.5
Peiyu Xue,Hongmei Zhao,Xinyong You,Weiming Yue
Lactoferrin and polyphenols are common natural functional compounds. Their interactions and the consequential alterations in functional activity have received widespread attention. The work aimed to investigate the interaction between lactoferrin and kaempferol, as well as evaluate the in vitro anticancer properties of the lactoferrin–kaempferol complex. The results of the spectra experiments revealed that lactoferrin and kaempferol are capable of forming complexes to quench the endogenous fluorescence of lactoferrin. Further insight into the binding mechanism was gained through molecular docking and molecular dynamics simulations. These analyses suggest that both hydrophobic interactions and hydrogen bonding are essential factors in the interaction between lactoferrin and kaempferol. Furthermore, the MTT assay and apoptosis by flow cytometry were conducted, revealing a synergistic effect of kaempferol and lactoferrin on the inhibition of HeLa cell proliferation. The findings from this investigation could improve our understanding of lactoferrin's interaction with polyphenols and the role of the lactoferrin–kaempferol complex in inhibiting cancer cell proliferation.
研究领域:
药理学
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癌症研究
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分子生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
Oncology Letters
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2018
·Vol. 15
·期 4
·5739-5743
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IF 1.664
Hua Zhang,Yumei Cao,Yuru Chen,Guangxi Li,Hanshu Yu
The present study investigated the inhibitory effects of apatinib on the proliferation of the SMMC-7721 hepatocellular carcinoma cell line to explore the possible mechanism. The MTT assay was used to detect the inhibitory effects of the different concentrations of apatinib on the proliferation of SMMC-7721 cells. Annexin V/PI double staining was performed to investigate the effects of apatinib on the apoptosis of SMMC‑7721 cells. Expression of the apoptosis-related genes Bcl-2, Bax and caspase-9 after apatinib treatment was detected by reverse transcription‑quantitative PCR (RT-qPCR) and western blot analysis. Expression of the PI3K, p-PI3K, Akt and p-Akt proteins after apatinib treatment was detected using western blot analysis. The MTT results showed that apatinib inhibited the in vitro proliferation of SMMC-7721 cells. Annexin V/PI double staining showed that apatinib induced the apoptosis of SMMC‑7721 cells in a concentration-dependent manner. Results of RT-qPCR and western blot analysis showed that apatinib was able to induce the expression of pro-apoptotic genes Bax and caspase-9 and inhibited the expression of anti-apoptotic gene Bcl-2. In addition, the western blot analysis revealed that p-PI3K and p-Akt was significantly decreased following apatinib treatment, while no significant differences were found in the total protein levels of PI3K and Akt. The results of the present show that apatinib is capable of promoting the apoptosis of SMMC-7721 cells by inhibiting the PI3K/Akt signal transduction pathway, upregulating the expression of pro-apoptotic genes Bax and caspase-9, and downregulating the expression level of the anti-apoptotic gene Bcl-2.
研究领域:
肿瘤学
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分子生物学
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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
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2018
·Vol. 8
·期 24
·13103-13111
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IF 2.936
Jing Zhang,Di Zhang,Xu Hu,Ruiling Liu,Zhonghao Li,Yuxia Luan
Because of the drawbacks of cytarabine (Ara-C) such as poor lipid solubility, deamination inactivation and low oral bioavailability limiting its application by oral administration, herein we propose a novel amphiphilic low molecular weight cytarabine prodrug (PA-Ara) by conjugating palmitic acid (PA) to Ara-C, making it possible to avoid the deamination inactivation by protecting the active 4-amino, as well as improving lipid solubility. Thanks to the rational design, the oil/water partition coefficient (P) of PA-Ara was improved tremendously compared with Ara-C, and the PA-Ara conjugation was stable enough in artificial digestive juice, ensuring that most molecules could be absorbed in the form of the prodrug. Results from an MTT assay conducted to measure the cytotoxicity of Ara-C and PA-Ara to HL60 (acute myeloblastic leukemia cell line) and K562 cells (chronic granulocytic leukemia cell line) showed that PA-Ara had significantly stronger antiproliferation activities than Ara-C. Significantly, we firstly compared the bioavailability of the oral fatty acid chain modified cytarabine prodrug preparation with injection and the relative bioavailability was up to 61.77% for our PA-Ara, which was much superior to that of oral Ara-C solution (3.23%). Overall, these findings make it clear that the PA-Ara suspension has the potential to be a promising new cytarabine oral preparation for leukemia therapy.
研究领域:
药学
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药物递送系统
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药理学
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肿瘤学
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DOI
PubMed
高影响因子
JOURNAL OF INORGANIC BIOCHEMISTRY
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2016
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IF 3.205
Bin Liu,Yanfei Liu,Jie Chai,Xiangquan Hu,Duoming Wu,Binsheng Yang
As a man-made additive, chromium picolinate Cr(pic) 3 has become a popular dietary supplement worldwide. In this paper Cr(pic) 3 and its new derivatives Cr(6-CH 3 -pic) 3 ( 1 ), [Cr(6-NH 2 -pic) 2 (H 2 O) 2 ]NO 3 ( 2 ) and Cr(3-NH 2 -pic) 3 ( 3 ) were synthesized, and complexes 1 and 2 were characterized by X-ray crystal structure (where pic = 2-carboxypyridine). The relationship between the chemical properties and biotoxicity of these complexes was fully discussed: (1) The dynamics stability of chromium picolinate complexes mainly depends on the Cr N bonds length. (2) There is a positive correlation between the dynamics stability, electrochemical potentials and generation of reactive oxygen species through Fenton-like reaction. (3) However, no biological toxicity was observed through MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and sub-chronic oral toxicity study for these chromium picolinate compounds. Together, our findings establish a framework for understanding the structure-property-toxicity relationships of the chromium picolinate complexes.
研究领域:
化学
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毒理学
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材料科学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2018
·
IF 3.909
Lizeng Cheng,Liang Chen,Qiongqiong Yang,Yuanfeng Wang,Xinlin Wei
Selenium (Se)-containing polysaccharide, a Se-conjugate macromolecule, generally exhibited higher antitumor activity than its regular polysaccharide. Previously, we extracted Se-containing tea polysaccharides (Se-TPS) from Se-enriched tea, and explored its structure and antioxidant activity. In this study, we investigated antitumor activity of Se-TPS on sarcoma 180 (S-180), and compared with its regular polysaccharides TPS and dietary supplement Se-yeast. In vitro antitumor activity of Se-TPS was evaluated by MTT and LDH assays, and the results indicated that Se-TPS can significantly inhibit the proliferation of S-180 in dose-dependent manner (R 2 = 0.97, p < 0.0001). In S-180 cancer xenograft model in Kunming mice, Se-TPS oral administration at three doses of 50, 100 and 200 mg/kg body weight daily for 13 days resulted in significant tumor regression. At the same dose, Se-TPS exhibited significantly higher antitumor activity than TPS and Se-yeast. Importantly, Se-TPS can significantly increase the spleen and thymus indices of tumor-bearing mice, suggesting the safety and immunomodulatory activity of Se-TPS. Therefore, Se-TPS may be a desirable antitumor agent for therapeutic and immunomodulatory applications.
研究领域:
药理学
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肿瘤学
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免疫学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
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2022
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IF 3.682
Juan Wu,Xi Wang,Binglong Zhu,Qinting He,Yaheng Zhang,Wei Jiang
As one of the well-known anticancer drugs, methotrexate (MTX) has been limited in clinical application due to its side effects on normal tissues. This study focused on the one-step hydrothermal synthesis and in vitro evaluation of Fe3O4/RGO-PEI as MTX carriers for targeted anticancer therapy. In which, the Fe3O4 provided magnetic response properties; RGO acted as a stage for Fe3O4 loading and improved the dispersion of Fe3O4; polyethylenimine (PEI) was used as a surface modifier and a storehouse for MTX. The prepared Fe3O4/RGO-PEI nanocomposites exhibited a suitable size, good stability and magnetic responsibility. And the MTX loading content and loading efficiency were calculated to be 26.6% and 90.5%, respectively. What’s more, due to the diffusion and dissolution of PEI, the Fe3O4/RGO-PEI-MTX exhibited excellent pH-sensitivity, the values of MTX release rate (%) within 48 h at pH 5.8 and 4.0 were 64.3% and 87.4%, respectively. Furthermore, MTT assays in cancer cells (HepG2) and normal cells (HUVEC) demonstrated that Fe3O4/RGO-PEI-MTX exhibited high anticancer activity while low toxicity to normal cells, and also the Fe3O4/RGO-PEI composites were practically non-toxic. Thus, our results revealed that Fe3O4/RGO-PEI-MTX would be a competitive candidate for targeted delivery and controlled release of MTX.
研究领域:
材料科学
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纳米技术
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药学
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癌症研究
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2023
·
IF 7.9
Jingya Ruan,Huimin Li,Mengqi Lu,Mimi Hao,Fan Sun,Haiyang Yu,Yi Zhang,Tao Wang
Background Jujube, a popular fruit from the Rhamnaceae family, relieves colorectal inflammation caused by spleen deficiency and has been used in many formulas in clinical for decades to treat colorectal cancer (CRC). As of yet, the therapeutic substances and mechanism of their action are unknown. Purpose The purpose of this study is to define the therapeutic substances of jujube and its mechanism of action in treating CRC . Methods The pharmacological effects of jujube extract and its fractions were evaluated in vivo using a CRC mouse model induced by AOM/DSS. The DAI value, colon length, mortality, tumor burden, and histological tumor size of the treated animals were compared. To explore the potential therapeutic substances, LC-MS analysis was conducted to characterize the serum migration components. A network pharmacology experiment was carried out for potential molecular targets. To verify the therapeutic substances as well as the molecular mechanism of jujube intervening CRC, cellular MTT assay of the serum migration components, Western blot and IHC tests were conducted. Results The in vivo pharmacological studies showed that compared to AOM/DSS treated mice, the mortality and DAI value, tumor burden, and histological tumor size of jujube extract and its fat-soluble fraction (mainly contained triterpenes) treated mice were significantly reduced, and their colon lengths were obviously longer than AOM/DSS treated mice. The targeted-LC/MS analysis supposed triterpenes 3, 7, 9, 11, 12, 14, 17 – 21, and 25 – 28 to be the serum migration components, which might be the potential therapeutic substances. In the network pharmacology experiment, the GO annotation and enrichment analysis of the KEGG pathway indicated that PI3K-Akt pathway and inflammatory reaction were important factors for jujube inhibiting CRC. Cellular MTT assay of serum migration components indicated that the potential effective substances from fat-soluble fraction to be triterpenes 3, 7, 17, 19, 20, and 25. The Western blot and IHC assays implied that the jujube extract, its fat-soluble fraction, and triterpenes 7, 17, and 20 showed inhibition on the expression of PI3K/Akt/NF-κB signaling pathway-related proteins. Additionally, it was noted in the pharmacodynamic experiment that ZJL's effectiveness was more apparent than ZJH and SQL in tumor burden rate, colon length, and spleen weight, which indicated that the efficacy of ZJ is contributed from CD and SQ, and they may have a synergistic effect on anti-CRC. Conclusion These results for the first time provide evidence that jujube triterpenes possess an anti-CRC effect, their mechanism was involving the control of the PI3K/Akt/NF-κB signaling pathway. What's more, the potential synergistic effect of the fat-soluble and water-soluble components found in this study provided a solid foundation for our deep understanding of how jujube can ameliorate CRC.
研究领域:
药理学
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肿瘤学
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分子生物学
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中医药
✓ 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）