BIOMEDICINE & PHARMACOTHERAPY
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2016
·
IF 2.326
Qin Tang,Fangling Ji,Jianli Guo,Jingyun Wang,Yachen Li,Yongming Bao
Chrysin , one of natural flavonoid compounds, has recently been found to possess anti-inflammatory, antiallergic and anticancer properties. To increase its anticancer effects, 5 chrysin derivates were synthesized on the base of DNA intercalator structure. The inhibiting effects of chrysin and its derivatives on cancer cells Hela, BGC823, MCF-7, HepG2, and normal cells HEK-293, were evaluated by MTT assays . 5-(2′-amino) phenyl-7-cyclohexanemethylchrysin (Ch-1), a unique chrysin derivate, killed all the cancer cells but kept above 60% survival rate in normal cells HEK-293 at 62.5 μM. Treated with chrysin from 250 μM to 500 μM, those cells were still maintained above 60% survival rate. The result of circular dichroism spectra showed that Ch-1 could intercalate DNA while chrysin had no effects on DNA. Interestingly, Hela cells survival rates were 95% and 10%, after treated with 20 μM and 30 μM of Ch-1, respectively. Both intrinsic and extrinsic apoptotic pathway were identified in regulating the cell death caused by Ch-1 in Hela cells. p53, the upstream regulator of apoptotic pathway were extremely significantly up-regulated in Hela cells treated with 25 μM Ch-1. Moreover, the inhibiting effects and apoptotic related proteins responses to Ch-1 on Hela cells were abolished after pre-treated with Pifithrin-α (Pft-α), a p53 inhibitor. So, p53-depedent apoptosis is the crucial factor governing the inhibiting effects of Ch-1 in Hela cells. Amazingly, Ch-1 at non-toxic concentration (2.5–10 μM) enhanced significantly anti-cancer effect of 10-hydroxy camptothecin (HCPT) on Hela, BGC823, and MCF-7 cells.
研究领域:
癌症研究
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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
PubMed
高影响因子
Materials Today Communications
·
2024
·
IF 3.7
Yao Yue,Peng Deng,Zhou Wang,Chen Ling,Ziye Zhu,Yongjin Li,Xiajun Zhang
Currently, ferrite magnetic nanoparticles are widely utilized in the biomedical domain, encompassing antibacterial, catalytic, imaging, and drug delivery among other fields. In this study, Cu 0.5 Zn 0.5 Fe 2 O 4 nanoparticles were synthesized via the rapid combustion-calcination process. By incorporating inorganic metal elements with specific functionalities, the limitations of iron oxide could be overcome, enabling targeted roles in various applications. The morphology, phase composition, and magnetic properties were characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and vibrating sample magnetometry (VSM). The impact of anhydrous ethanol quantity, calcination temperature, and duration on the magnetic properties and grain size of the nanomaterials was investigated. Cu 0.5 Zn 0.5 Fe 2 O 4 nanoparticles were evaluated for their inhibitory effects on human gastric cancer cells (SGC-7901 and HGC-27) under different preparation conditions. The results of the MTT assay revealed a concentration - and time-dependent inhibition of tumor cell proliferation by Cu 0.5 Zn 0.5 Fe 2 O 4 nanoparticles. Nanoparticles exhibiting a magnetic energy of 20.23 emu/g and an average particle size of 51.6 nm, synthesized using 20 mL of anhydrous ethanol, calcination temperature of 400 °C, and a calcination duration of 2.0 h, displayed significant inhibitory effects on tumor cells. Furthermore, The nanoparticles not only showed low toxicity to human normal stomach cells GES-1, but also enhanced the inhibitory effect on tumor cells under the action of an external magnetic field.
研究领域:
纳米技术
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生物医学工程
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材料科学
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肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 54
·31201-31212
·
IF 2.936
Xiaokang Long,Yao-Fu Zeng,Yunmei Liu,Ying Liu,Tangluo Li,Lanqing Liao,Yu Guo
Genistein amino acid derivatives 4a–4d were synthesized and evaluated for their cytotoxic activities against MCF-7, Hela, MGC-803 and HCT-116 cell lines by MTT assays in vitro. The results revealed that compounds 4a–4d showed better activity than the parent compound genistein. Particularly, compound 4b displayed the most significant anticancer activity against MGC-803 with an IC50 value of 12.08 μM. In addition, the mechanisms of interaction between genistein, compounds 4a–4d and BSA were investigated via multi-spectroscopic techniques such as ultraviolet (UV) spectroscopy, fluorescence, circular dichroism (CD), and molecular docking under physiological conditions. The results suggested that endogenous fluorescence of BSA could be quenched by genistein and compounds 4a–4d via forming BSA-compound complex, which meant a static quenching mechanism was involved. The negative values of enthalpy (ΔH) and entropy (ΔS) indicated that interactions between BSA and the ligands were spontaneous, and hydrogen bonding and van der Waals interactions were involved in the BSA-compound complexion formation. The UV, synchronous and 3D fluorescence results revealed that the micro-environment of tryptophan and conformation of BSA were changed after binding to ligands. CD analysis demonstrated the variation in the secondary structure and that the α-helix content of BSA decreased. Eventually, molecular docking was executed to forecast the binding forces and binding sites between BSA and compounds 4a–4d.
研究领域:
药理学
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生物化学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Natural Product Communications
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2020
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IF 0.468
Ling-Li Zheng,Guan Wen,Yun-Xin Yao,Xiao-Huan Li,Feng Gao
Based on the strong activity dependence of paclitaxel (PTX; Taxol) or docetaxel (Taxotere) on the C-13 side chain, a small library of dehydroepiandrosterone, cholesterol, vitamin D2, and alkaloids talatisamine and songorine-PTX hybrids have been synthesized and evaluated for in vitro anticancer activity by MTT assay against human breast (MCF-7), colon (HCT116), lung carcinoma (A549), and renal adenocarcinoma (786-0) cancer cell lines. Most hybrids (11b, 12b, 13b, 15b, and 18b) reduced the growth of MCF-7 and 786-0 cells with low PTX sensitivity in vitro. Among the synthesized compounds, hybrid 11b was better in inhibiting the growth of the 4 cells than PTX. A relatively low IC50 value of compound 11b (8.16 ± 0.04 μM) was also examined after exposure for 48 hours. Hybrid 11b showed a proapoptotic effect in HCT116 cells evaluated by Annexin V/propidium iodide binding assay. The level of hybrid 11b leading to protective cell death in HCT116 cells was detected using western blot and not easily observed in our basic examinations.
研究领域:
药理学
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肿瘤学
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药物化学
·
细胞生物学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）