EUROPEAN JOURNAL OF PHARMACOLOGY
·
2017
·
IF 2.896
Jun Wang,Qiuwen Li,Xiaojuan Li,Weiqi Yuan,Sichao Huang,Shaohui Cai,Jun Xu
Fibroblast activation protein-α (FAPα) is a serine protease of the post-prolyl peptidase family that is specifically expressed in the majority of human epithelial tumors , but not in normal tissues. In this study, we demonstrated the anti-tumor activity of a novel targeting drug formed by conjugating epirubicin (EPI) with an FAPα-specific dipeptide (Z-Gly-Pro) and named it Z-GP-EPI. Consistent with this tumor-targeting delivery strategy, the results illustrated that Z-GP-EPI could release EPI efficiently after incubating with FAPα and could exhibit similar antitumor effects as EPI in vitro in FAPα over-expressed tumor cells (4T1/FAPα + ). Furthermore, the evaluation of antitumor activity of Z-GP-EPI in vivo was implemented in a 4T1/FAPα + tumor-bearing mice xenograft model. Our results illustrated that Z-GP-EPI had similar antitumor effects in 4T1/FAPα + tumor-bearing mice and showed no visible cardiotoxicity side effects compared with free EPI. Thus, our study indicated that this FAPα-activated prodrug targeting strategy may provide a new mechanism for the targeted delivery of antitumor agents and improve their safety levels.
研究领域:
肿瘤学
·
药理学
·
生物化学
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DOI
PubMed
高影响因子
Pharmaceutics
·
2019
·Vol. 11
·期 3
·123
·
IF 4.773
Jun Ding,Guilin Chen,Guofang Chen,Mingquan Guo
Epirubicin-capped silver nanoparticles (NPs) were synthesized through a one-pot method by using epirubicin as both the functional drug and the reducing agent of Ag+to Ag0. The preparation process was accomplished in 1 h. In addition, the obtained epirubicin-capped silver nanoparticle was characterized by transmission electron microscopy (TEM), energy-dispersive X-ray spectroscopy (EDX), and infrared spectroscopy. The results showed that a layer of polymer epirubicin had formed around the silver nanoparticle, which was 30-40 nm in diameter. We further investigated the antitumor activity of the prepared epirubicin-capped silver nanoparticle, and the half maximal inhibitory concentration (IC50) against Hep G2 cells was 1.92 μg/mL, indicating a good antitumor property of the nanoparticle at low dosage.Keywords:epirubicin;one-pot synthesis;silver nanoparticle;antitumor
研究领域:
药学
·
纳米医学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CANCER LETTERS
·
2012
·
IF 4.238
Ying-Zheng Zhao,Dan-Dan Dai,Cui-Tao Lu,Li-Juan Chen,Min Lin,Xiao-Tong Shen,Xiao-Kun Li,Ming Zhang,Xi Jiang,Rong-Rong Jin,Xing Li,Hai-Feng Lv,Lu Cai,Pin-Tong Huang
Multidrug resistance (MDR) is one of the major reasons for the failure of cancer chemotherapy. A newly reported liposome carrier, propylene glycol liposomes (EPI-PG-liposomes) were made to load epirubicin (EPI) which enhanced EPI absorption in MDR tumor cells to overcome the drug resistance. MDA-MB 435 and their mutant resistant (MDA-MB 435/ADR) cells were used to examine the cellular uptake and P-gp function in vitro for EPI-PG-liposomes by fluorescence microscopy and FCM, respectively. Mammary tumor model was also established to investigate the tumor growth inhibition and pharmacodynamics of EPI-PG-liposomes in vivo . Morphology evaluation showed that EPI-PG-liposomes had a homogeneous spherical shape with an average diameter of 182 nm. Based on cell viability assay, fluorescent microscopy examination, and EPI uptake assay, EPI-PG-liposomes exhibited an effective growth inhibition not only in MDA-MB-435 cells, but also in MDA-MB 435/ADR cells. EPI-PG-liposomes have high permeability not only on tumor cell membrane, but also on cell nucleus membrane. P-gp function assay showed that the anticancer action of EPI-PG-liposomes was not related to P-gp efflux pump, suggesting that PG-liposomes would not affect the normal physiological functions of membrane proteins. EPI-PG-liposomes also showed a better antitumor efficacy compared to EPI solution alone. With high entrapment efficiency, spherical morphology and effective inhibition on MDR cancer cells, EPI-PG-liposomes may represent a better chemotherapeutic vectors for cancer targeted therapy.
研究领域:
肿瘤学
·
药理学
·
生物医学工程
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DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2021
·Vol. 45
·期 15
·6880-6888
·
IF 3.591
Tao Gong,Rina Cheng,Xiaoyu Wang,Jing Li,Wenting Liang,Zhihong Wei,Shaomin Shuang,Yuyao Wang,Rui Guo
Herein, triformyl cholic acid-modified Fe3O4 magnetic nanoparticles (TCA-MNPs) were first constructed and developed as a novel drug carrier, possessing a uniform size of 12 ± 2 nm, superparamagnetic response, and good stability. Doxorubicin hydrochloride (DOX) and epirubicin hydrochloride (EPI) could effectively aggregate on the surface of TCA-MNPs via triformyl cholic acid regulatory hydrogen-bonding interaction and the π–π stacking-induced self-assembly of drug molecules. The loading capacity of DOX and EPI reached up to 1363.6 mg g−1 and 1293.5 mg g−1, respectively. Moreover, the release of loaded drugs could be achieved by adjusting the acidic microenvironment of cancer cells. Significantly, the drug-loaded nanocomposite (TCA-MNPs/DOX) showed the functions of triformyl cholic acid-mediated hepatocyte recognition and magnetic-guided targeting for the synergistic targeted therapy of hepatoma cells in vitro and in vivo. These findings demonstrate that the as-prepared drug nanocarriers have potential practical application values for the diagnosis and treatment of hepatocellular carcinoma.
研究领域:
药剂学
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肿瘤学
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纳米医学
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产品关联
DOI
高影响因子
Journal of Materials Chemistry B
·
2013
·Vol. 1
·期 33
·4099-4109
·
IF 0
Pierre Dramou,Pengli Zuo,Hua He,Lien Ai Pham-Huy,Wenyue Zou,Deli Xiao,Chuong Pham-Huy,Theophilus Ndorbor
The preparation, characterization and application of novel anticancer “epirubicin” (EPI) water-compatible magnetic molecularly imprinted polymers (M-MIPs) like artificial antibodies by computational design and chemical synthesis as a carrier for drug delivery is described herein. Two monomers: methacrylic acid (MAA) and methacrylamide (MAM) were selected by computational simulation from the four chemicals used. Covalent and non-covalent bonds were evaluated by this technique based on the interaction mode and energy with template or solvent. Non-covalent bonding was predominant in all cases and major energy interaction was observed. The nanomaterials were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRD), and a vibrating sample magnetometer (VSM). The loading and controlled release studies performed showed a slight advantage for the M-MIP obtained from MAA than that from MAM at ambient temperature. However, the drug release in vitro was slightly better for the second M-MIP when the temperature increased to 50 °C. The water-compatible nanomaterial showed good pH-sensitive drug release profiles in vitro. Briefly, due to its magnetic property, amphiphilicity, good biomimetic recognition of EPI, high adsorption capacity and controlled release, the epirubicin M-MIPs synthesized in this study are suitable to be applied to a magnetic targeted drug delivery system.
研究领域:
药学
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材料科学
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生物医学工程
✓ 已验证
DOI
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Minglong Huang,Xin Wang,Jialin Xing,Bowen Zhang,Lurong Zhang,Yaqiao Li,Hongying Xiao,Qing Wang,Jun Yuan,Yafan Xiao,Zhenzhen Zhao,Zhonggui He,Lingxiao Li,Bingjun Sun
Human serum albumin (HSA) is regarded as an ideal carrier for chemo-drug delivery due to its superior advantages. However, for drugs like Epirubicin (EPI), which exhibit poor binding affinity to HSA, efficient delivery remains challenging. Herein, we proposed a fatty acid modification strategy to improve the binding affinity of EPI to HSA for efficient cancer therapy. Briefly, fatty acids (FAs) with varying chain lengths (C 14 , C 18 , and C 22 ) were connected to EPI via pH-sensitive hydrazone bond to create EPI prodrugs (EPI-FAs). These EPI-FAs were then co-assembled with HSA at different mass ratios to screen the optimal formulations. We found that the chain length significantly impacted the binding affinity and assembly performance of EPI-FAs with HSA, as well as the subsequent in vivo fate and anti-tumor efficacy. Notably, EPI-C 18 exhibited high binding affinity and superior assembly performance with HSA, resulting in improved pharmacokinetic behavior with an AUC 0 – 24 h of 38.72 times higher than the EPI Solution. Moreover, the nanocomplex of EPI-C 18 and HSA showed potent anti-tumor activity with minimal toxicity (even at a high dose of 10 mg/kg equal to EPI). This work would offer innovative insights and theoretical basis for the design of albumin-based nano-formulation.
研究领域:
药剂学
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生物化学
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肿瘤学
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产品关联
DOI
高影响因子
Discover Oncology
·
2025
·Vol. 16
·期 1
·1-13
·
IF 2.9
Huang Hai-yi,Lin Lisa Zong Yong,Lu Xin-yi,Jiang Ying
Triple negative breast cancer (TNBC) refers to a molecular subtype of breast cancers (BC) with high rate of distant metastases and poor prognosis. Epirubicin (EPI) is widely used for the therapy of TNBC but it’s limited in clinical use due to cardiotoxicity and chemotherapy resistance. We previously identified F-α-DDB-derivative, a novel synthetic of bifendate, as a potential agent to improve the therapeutic efficacy of TNBC in combination with EPI since F-α-DDB-derivative inhibited MDA-MB-468, but not as much as EPI. In this study, we investigated the antitumor activity of F-α-DDB-derivative in combination with EPI against TNBC in vitro and in vivo and whether co-treatment would induce additional cardiotoxicity. In human TNBC MDA-MB-468 cells, application of F-α-DDB-derivative (11.5, 23.0, 46.0 μg/ml) in combination with EPI (1.5, 3.0, 6.0 μg/ml) exhibited great inhibition on cell viability and cell proliferation. Additionally, F-α-DDB-derivative (5.75, 11.5, 23.0, 46.0 μg/ml) interacted with EPI (0.75, 1.5, 3.0, 6.0 μg/ml) synergistically to induce apoptosis in MDA-MB-468 cells. This suggests that F-α-DDB-derivative may be more sensitive to apoptotic pathways. Furthermore, we revealed that co-administration of EPI and F-α-DDB-derivative (ip, once every other day for 14 days) significantly increased the therapeutic efficacy of EPI (2.0 mg/kg) or F-α-DDB-derivative (20.0 mg/kg) in mice harboring MDA-MB-468 cell xenografts without additional cardiotoxicity compared to that in EPI monotherapy group. These results implicate that co-treatment of EPI and F-α-DDB-derivative may be a potential therapeutic approach for the treatment of TNBC.
研究领域:
肿瘤学
·
药理学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2014
·
IF 3.84
Yuting Wang,Jianmei Xie,Li Tao,Hui Tian,Shi Wang,Hong Ding
A novel nano-Au/MWNTs-ZnO modified screen printed electrode (SPE) was fabricated for directly simultaneous determination of epirubicin (EPI) and methotrexate (MTX) in whole blood samples. Electrochemical performances of the modified electrode were greatly enhanced due to the presence of nano-Au/MWNTs-ZnO nanocomposites. The optimum experimental conditions for the detection were explored, and the currents of EPI and MTX measured by SWV presented a good linear property with the increasing of the concentrations. Under optimized conditions, the linear ranges of EPI and MTX were determined to be 0.005–0.200 μM and 0.02–1.00 μM, with the detection limits of 2.5 nM and 10 nM, respectively. Furthermore, the nano-Au/MWNTs-ZnO SPE was applied for simultaneous determination of EPI and MTX in pharmaceutical injections and diluted human blood samples with wonderful satisfactory results.
研究领域:
分析化学
·
医学检验
·
纳米材料科学
✓ 已验证
产品关联
DOI
高影响因子
MATERIALS & DESIGN
·
2021
·
IF 7.991
Kunyu Zhang,Zhong Wan,Huabo Jiang,Xiufeng Xiao,Qian Feng,Yanchun Meng,Yongsheng Yu
Breast cancer is one of the leading causes of cancer-related deaths in women. Chemotherapy remains one of the main clinical treatments for breast cancer. However, this therapy has appreciable side effects. Nanoscale carriers, such as metal nanoparticles and liposomes, are being widely utilized as drug delivery vehicles to achieve precise targeting of tumor cells. In this study, we designed a novel upconversion nanocarriers (UCNCs) host-guest complexation system based on a photolabile capping-like molecule. UCNCs containing epirubicin (EPI) were grafted with a dimer-targeting peptide via cyclodextrin-adamantine host-guest complexation. After entering breast tumor cells with the guidance of the dimer-targeting peptide, the core of the UCNCs upconverted near-infrared light to ultraviolet light which subsequently triggered the intracellular on-demand release of epirubicin. The precise and efficient delivery and release of epirubicin inside breast cancer cells significantly inhibited cancer cells proliferation, migration, and invasion in vitro and decreased the tumor size in vivo . We believe that this UCNCs system is a promising platform for the precise and controllable delivery of various chemotherapy drugs for clinical cancer treatments.
研究领域:
肿瘤学
·
药剂学
·
纳米医学
✓ 已验证
DOI
高影响因子
ANALYST
·
2014
·Vol. 139
·期 19
·4940-4946
·
IF 3.906
Han-Peng Jiang,Jiu-Xia Zhu,Chunyan Peng,Jiajia Gao,Fang Zheng,Yu-Xiu Xiao,Yu-Qi Feng,Bi-Feng Yuan
In the current study, we developed a facile strategy for the one-pot synthesis of an aptamer-based organic–silica hybrid monolithic capillary column. A 5′-SH-modified aptamer, specifically targeting doxorubicin, was covalently modified in the hybrid silica monolithic column by a sol–gel method combined with “thiol–ene” click reaction. The prepared monolithic column had good stability and permeability, large specific surface, and showed excellent selectivity towards chemotherapeutic anthracyclines of doxorubicin and epirubicin. In addition, the enantiomers of doxorubicin and epirubicin can be easily separated by aptamer-based affinity monolithic capillary liquid chromatography. Furthermore, doxorubicin and epirubicin spiked in serum and urine were also successfully determined, which suggested that the complex biological matrix had a negligible effect on the detection of doxorubicin and epirubicin. Finally, we quantified the concentration of epirubicin in the serum of breast cancer patients treated with epirubicin by intravenous injection. The developed analytical method is cost-effective and rapid, and biological samples can be directly analyzed without any tedious sample pretreatment, which is extremely useful for monitoring medicines in serum and urine for pharmacokinetic studies.
研究领域:
分析化学
·
药物分析
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
OncoTargets and Therapy
·
2021
·
IF 4.147
Jiuzhou Liu,Shasha Ren,Xiangyu Zhang,Yun Feng,Zhenglun Qiu,Li Ma,Jingwen Huang
Background Breast cancer (BC) is the most common type of cancer among women worldwide, and about 30% of males will have recurrent disease.Methods In order to treat recurrent BC, we designed a type of silica nanodelivery system loaded with epirubicin and curcumin (composite nanoparticles, CNPs). To promote CNPs clinical application, the stability, the blood, immune and cell compatibility, skin stimulation experiments, anti-tumor activity in vivo and in vitro were studied.Results In our study, the CNPs had a particle size of 73.9 nm and a uniform size and morphology; moreover, they maintained physical and chemical stability in the blood protein environment. Additionally, results showed that nanoparticles had good blood and immune compatibility, and they did not affect intracellular superoxide dismutase (SOD) and intracellular catalase (CAT). Skin stimulation experiments showed that CNPs did not cause any obvious irritative damage to the intact skin of rabbits. In the cytotoxicity study, CNPs showed strongest antitumor activity. The results of cell cycle and apoptosis studies showed that CNPs could mainly induce apoptosis of S and G2/M phase cells. In vivo, CNPs showed strongest aggregation in the tumor after 6 h of tail vein administration, and a large amount of CNPs continued to accumulate in the blood after 12 h of administration, indicating that CNPs had long circulation ability. The in vivo antitumor activities showed that CNPs had the strongest antitumor activity and tumor targeting ability, and hematoxylin-eosin staining of internal organs showed no obvious difference between treatment groups and negative control.Conclusion CNPs have an ideal biosafety and therapeutic effect for recurrent BC, and they have potential clinical application value.
研究领域:
药学
·
肿瘤学
·
纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LIFE SCIENCES
·
2021
·
IF 5.037
Dawei Yang,Xiaoyu Tian,Yuchen Ye,Yin Liang,Jie Zhao,Tao Wu,Na Lu
Senescent cancer cells contribute to tumor refractoriness. The removal of senescent cells after chemotherapy prevents or delays cancer relapse. Our study showed that GL-V9 (5-hydroxy-8-methoxy-2-phenyl-7-(4-(pyrrolidin-1-yl) butoxy)-4-H-chromen-4-one), a potential anticancer drug, eliminated senescent MEFs (Mouse embryonic fibroblasts) and drug-induced senescent breast cancer cells. GL-V9 induced apoptosis in senescent MDA-MB-231 cells. Mechanistically, it alkalized lysosomes and increased the abundance of mitochondria as well as ROS (Reactive oxygen species). The senolytic effect of GL-V9 was also observed in epirubicin-treated mammary tumors in MMTV-PyMT mice. Our data thus indicated that GL-V9 is a promising senolytic drug which could be used to improve the outcome of cancer chemotherapy.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
✓ 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）