JOURNAL OF INORGANIC BIOCHEMISTRY
·
2016
·
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
·
毒理学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 24
·13103-13111
·
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
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
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
·
肿瘤学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2022
·
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
·
纳米技术
·
药学
·
癌症研究
✓ 已验证
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
·
肿瘤学
·
分子生物学
·
中医药
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2024
·Vol. 57
·期 8
·1174-1178
·
IF 0.8
Zheng Qing-Xuan,Wang Rui,Li Hui-Jing,Dehaen Wim,Huai Qi-Yong
Oleanolic acid (OA) is a natural product with certain antitumor activity. In order to enhance its cytotoxicity, a total of five derivatives of OA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells), A549 cells (human nonsmall cell lung cancer cells) and BEAS-2B cells (human cervical cancer cells) were evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results indicated that these target compounds have a wide molar activity range and some of them showed better activity than the commercial drug, doxorubicin. Compound 2a induces apoptosis of 14, 27, and 56% of MDA-MB-231 cells at 2, 4, and 8 mM respectively, and shows a linear correlation of concentration.
研究领域:
肿瘤学
·
药物化学
·
分子药理学
·
天然产物化学
·
转化医学
✓ 已验证
DOI
高影响因子
Frontiers in Cell and Developmental Biology
·
2020
·
IF 5.186
Jiang Ying,Song Hanbing,Jiang Ling,Qiao Yu,Yang Dan,Wang Donghua,Li Ji
Background: Silybin was known to exert inhibition in prostate cancer, but the underlying mechanism remained largely unknown. This study was designed to find out the potential target of Silybin on prostate cancer and explore the relative mechanisms.Methods: Firstly, we screened the possible targets of Silybin through the PubChem database and Subpathway – GM. Then DU145 cells were transferred to investigate the correction about related targets, magnetic bead sorting and flow cytometry were used to sort and identify the cells. Proliferation, migration and invasion ability of DU145 cells were detected by MTT assay, Transwell assay, plate clonality and sphere formation assay. BALB/c nude mice were constructed models with implanted sarcoma and measured the tumor volume every 5 days as wells tumor weight. The levels of proteins were detected by Western blot and immunocytochemistry. RT-PCR was selected to test the expression of protein’s mRNA.Results: It was screened out the ALDH1A1 was highly correlated with subpathways of the Silybin risk metabolic pathway. And ALDH1A1 expression was positively correlated RARα with Ets1 by interfering with the ALDH1A1 gene. Importantly, ALDH1A1(+) cells showed proliferation, migration and invasion ability. In addition, it showed that Silybin exerted the inhibition on prostate cells by suppressed the proliferation, migration and invasion ability of cells in vitro experiment. Silybin also reduced the tumor volume and weight. And Silybin displayed obviously reduced the proteins and mRNA of ALDH1A1, RARα, Ets1 and MMP9 expressions.Conclusion: Our results indicated that Silybin showed inhibition of prostate cancer and the mechanism was involving with downregulating ALDH1A1 expression, thereby inhibiting the activation of RARα and preventing the activation of Ets1 to inhibit the growth and invasion of prostate cancer.
研究领域:
肿瘤学
·
药理学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Results in Chemistry
·
2023
·
IF 2.3
Jianhua Deng,Daosheng Li,Rui Chen,Xiangsheng Zeng,Yu Liu
The possibility of fabricating metal nanoparticles using plant extracts has already been explored in phytomedicines. Nanobiotechnology has a wide range of potential applications, including the cosmetics industry, packaging, coatings, biomedicine, and the enhancement of biological activity. Nickel oxide (NiO) was fabricated in a waste-free, low-cost method and then used to adorn Marsdenia tenacissima extract (MTE), a crucial plant leaf. After forming the nanoparticles, MTE@NiO-NPs were also tested for their optical and biological qualities. The morphological characteristics of NiO-NPs are rhombohedra and slightly agglomerated, and the particle size of the biosynthesized NiO-NPs is observed in the range of ∼ 15 nm. The in vitro cytotoxicity of Marsdenia tenacissima extract (MTE) and nanoparticles on lung cancer cells (A549 and H1299) by MTT assay. The in vitro cytotoxicity assay results revealed that the newly fabricated nanoparticles effectively kill cancer cells with low minimal inhibitory concentration. The various biochemical staining assays assessed the cell death and morphological investigation. Furthermore, the mode of cell death was evaluated by mitochondrial membrane potential (Δψm) and reactive oxygen species (ROS). Therefore, the study concludes that the plant leaves extract of Marsdenia tenacissima is a powerful reducing/capping agent in fabricating MTE@NiO-NPs, demonstrating useful biological features.
研究领域:
纳米技术
·
药理学
·
癌症研究
·
生物技术
✓ 已验证
产品关联
DOI
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2025
·
IF 2.5
Yun Liu,Xuefang Shang,Ashraf H. Abadi,Mingpan Cheng
To address the challenge of antibiotic resistance and enhance the functionality of pharmaceutical materials, aldehyde chitosan-based dynamic polymers (ACs) incorporating amikacin and cefotaxime, denoted as ACs-amikacin and ACs-cefotaxime, respectively, were synthesized. These polymer's chemical structure was characterized using 1H-NMR and FT-IR analysis. Subsequently, methylthiazolyldiphenyl-tetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays were employed to evaluate their safety. Furthermore, it was demonstrated that these polymers retained the antibacterial activity of the antibiotics. This study introduces a novel strategy for dynamic natural materials capable of exerting a synergistic effect in pharmaceutical applications through the conjugation of natural materials with active pharmaceutical agents.
研究领域:
药用材料
·
高分子化学
·
抗菌研究
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
ANTI-CANCER DRUGS
·
2021
·Vol. 33
·期 1
·19
·
IF 2.248
Liu Shengli,Liu Honglian,Sun Hao,Deng Shengming,Yue Ling,Weng Zhen,Yang Jianfeng,Zuo Bin,He Yang,Zhang Bin
Albendazole (ABZ), a clinical antiparasitic drug, has shown potential antitumor effects in various tumors. Herein, we prepared dimeric cRGD [(cRGD) 2 ] modified human serum albumin (HSA) nanosystem to co-delivery of albendazole (ABZ) and iodine-131 ( 131 I) for chemoradiotherapy of triple-negative breast cancer (TNBC). [email protected] NPs were synthesized by the self-assembly method. 131 I-(cRGD) 2 / [email protected] NPs were fabricated through covalently binding [email protected] NPs with (cRGD) 2 peptides, followed by chloramine T direct labeling with 131 I. In vitro therapeutic effects on TNBC (MDA-MB-231 and 4T1 cells) were determined using MTT assay, crystal violet assay, wound-healing assay and western blotting analysis. In vivo treatment was performed using 4T1-bearing mice, and the tumor-targeting efficacy was assessed by gamma imaging. The distribution of NPs was quantitatively analyzed by detecting the gamma counts in tumor and main organs. The nanoparticles possessed negative charge, moderate size and good polydispersity index. Dual responding to pH and redox, the in vitro release rate of ABZ was more than 80% in 72 h. In vitro, NPs inhibited the proliferation of TNBC cells in a concentration-dependent manner and decreased cell migration. Western blotting analysis showed that the NPs, as well as free ABZ, cell-dependently induced autophagy and apoptosis by restraining or promoting the expression of p-p38 and p-JNK MAPK. In vivo, gamma imaging exhibited an earlier and denser radioactivity accumulation in tumor of 131 I-(cRGD) 2 / [email protected] NPs compared to NPs free of (cRGD) 2 conjugating. Furthermore, 131 I-(cRGD) 2 / [email protected] NPs significantly suppressed tumor growth by restraining proliferation and promoting apoptosis in vivo. Our study suggested that the nanoparticles we developed enhanced tumor-targeting of ABZ and increased antitumor effects by combination of chemotherapy and radiotherapy.
研究领域:
肿瘤学
·
药学
·
纳米技术
·
癌症治疗
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2024
·Vol. 29
·期 2
·483
·
IF 4.2
Linlin Cui,Li Zhao,Guanghuan Shen,Dahai Yu,Tian Yuan,Yingyu Zhang,Bo Yang
Cordycepin has good antitumor activity, but its clinical application is limited due to the easy deamination of N6 in structure. In this study, a large lipolysis group was introduced at the cordycepin N6 to improve the problem, cordycepin derivatives (3a–4c) were synthesized, and biological evaluation of compounds was studied. In this study, the vitro antitumor activity of the compounds against MCF7 cells, HepG2 cells and SGC-7901 cells was evaluated by MTT assay. In the results, compound4ashowed the most obvious inhibitory effect on MCF7 cells with an IC50value of 27.57 ± 0.52 μM, which was much lower than cordycepin. Compound4ashowed high selectivity between MCF7 and normal MCF-10A cells. Further biological evaluation showed that compound4apromoted apoptosis and blocked the cell cycle in the G0/G1 phase. Then, Western Blot was used to detect related apoptotic proteins. It was found that Compound4acould down-regulate the expression of Bcl-2 protein and up-regulate the expression of p53, Bax, Caspase-3 and Caspase-9 proteins. The mitochondrial membrane potential decreased continuously and the positive expression rate decreased. It was speculated that compound4ainduced the apoptosis of MCF7 cells through the mitochondrial pathway.Keywords:cordycepin derivatives;antitumor;structural modification
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
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2020
·
IF 4.192
Niu Zhang,Jun-Peng Zeng,Yan-Ping Wu,Meng Wei,Hong Zhang,Liufeng Zheng,Ze-Yuan Deng,Jing Li
The digestion and absorption of different structural lipids in human milk may be different. Hence, by simulating in vitro infant digestion and Caco-2 cells to explore the effects of 1-oleoyl-2-palmitoyl-3-linoleoylglycerol (OPL)/1,3-dilinoleoyl-2-palmitoylglycerol (LPL)/1,3-dioleoyl-2-palmitoylglycerol (OPO) and their mixtures (M) (OPL/LPL/OPO in M1, M2, and M3 were 1.5/0.5/1, 1.2/1.2/1, and 0.5/0.2/1, respectively) on digestion and absorption. The digestibility of the OPO group was higher than those of the OPL and LPL groups, and the M3 group was higher than the M1 and M2 groups. The synthesis and transport of triglycerides in Caco-2 cells in OPL and LPL groups were higher than the OPO group, and the M1 group was significantly higher than that of M3. The expression of FABP1, PPARα, and MTT protein in OPL and M1 groups was significantly higher than OPO and M3, respectively. There are differences in the digestion and absorption of differently structured lipids from this study.
研究领域:
营养学
·
生物化学
·
儿科
✓ 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）