BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2020
·
IF 1.863
Yuanguo Xiong,Hao Lu,Hanlin Xu
Hepatic fibrosis (HF) is a common disease, with currently no available treatment. Galangin, a natural flavonoid extracted from Alpinia officinaruim Hance, has multiple effects demonstrated in previous studies. The aim of the present study was to explore the anti-fibrogenic effect of galangin in vitro, and research its potential molecular mechanisms. LX-2 cells were chosen as an in vitro HF model, and were treated with galangin in different concentrations. Cell viability was analyzed using Cell Counting Kit-8 (CCK-8) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cell apoptosis was measured using flow cytometry, and the anti-fibrogenic effect of galangin was determined using quantitative reverse transcription polymerase chain reaction (RT-qPCR), immunofluorescence, and western blotting. The results show that the proliferation of LX-2 cells was efficiently inhibited by galangin, and apoptosis was induced in a dose-dependent manner. Both the mRNA and protein expression of α-SMA and collagen I were markedly downregulated. Galangin also inhibited the PI3K/Akt and Wnt/β-catenin signaling pathways and increased the Bax/Bcl-2 ratio. The results of this study suggest that galangin has an anti-fibrogenic effect and may represent a promising agent in the treatment of hepatic fibrosis.
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
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肝病学
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产品关联
DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2016
·Vol. 14
·期 1
·904-910
·
IF 1.559
Liandi Xie,Yang Wu,Zongjing Fan,Yang Liu,Jixiang Zeng
In the present study, the mechanisms associated with the Astragalus polysaccharide (APS)-mediated protection of human cardiac microvascular endothelial cells (HCMEC) against hypoxia/reoxygenation (HR) injury were investigated. Pretreatment of HCMECs with APS at various concentrations was performed prior to Na2S2O4-induced HR injury. Subsequently, cell viability and apoptosis were measured by MTT and Hoechst assays, respectively. The viability of HCMECs was reduced by Na2S2O4 and apoptosis was enhanced; however, cell viability was observed to be increased by APS via inhibition of apoptosis. Additionally, intracellular reactive oxygen species (ROS), Ca2+, nitric oxide (NO), malondialdehyde (MDA), superoxide dismutase (SOD), phosphatidylinositol 3-kinase (PI3K)-protein kinase B (AKT), B‑cell lymphoma‑2 (Bcl‑2), Bcl‑2 associated X protein (Bax) and caspase‑3 were measured using detection kits or western blot analysis. In HCMECs with HR injury, the levels of ROS and Ca2+, MDA and Bax expression levels, and the activity of caspase‑3 were elevated. By contrast, the level of NO, the protein expression levels of SOD, Bcl‑2 and PI3K, and the phosphorylation of AKT were decreased. However, compared with the HR group, the effects of HR injury were significantly reduced by APS, with APS providing a protective effect on HCMECs, particularly at higher doses. The current study concluded that APS protects HCMECs from Na2S2O4‑induced HR injury by reducing the levels of ROS, Ca2+, MDA and Bax, inhibiting the activity of caspase‑3, and enhancing the levels of NO, SOD, Bcl‑2, PI3K and phosphorylated AKT. These results may provide an insight into the clinical application of APS and novel therapeutic strategies for HR injury.
研究领域:
心血管研究
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Shaojie Zhang,Renjie Gao,Baocong Ding,Junhao Li,Tanggan Wang,Jiaheng Chen,Chong Li,Yukun Jiao,Lijun Song
Combining selenium nanoparticles (SeNPs) with bioactive polysaccharides is one of the effective ways to overcome the shortcomings of SeNPs and polysaccharide and obtain novel antitumor drug candidates. In this study, a heteropolysaccharide (MTP70) with moderate antihepatoma activity was isolated from the stems of Marsdenia tenacissima (Roxb.) Wight et Arn. To further improve the antihepatoma activity of MTP70 and the application of SeNPs, a novel stable nanoparticle (MTP-SeNP) was designed and fabricated. MTP-SeNPs (Se content of 8.25 %) were characterized as monodisperse spherical nanoparticles (50 nm) with MTP70 wrapped on the surface of the SeNPs by the formation of C O⋯Se bonds and possessed high stability and good dispersion in water for almost a month. In addition, MTP-SeNPs showed higher inhibitory effect compared with MTP70. MTP-SeNPs could effectively inhibit the proliferation, invasion, and metastasis of HePG2 cells by inducing apoptosis and arresting the cell cycle at the S phase, which were closely related to the activation of the Bax/Bcl-2/Caspases and p-21/Akt/Cyclin A2 signaling pathways. Our results provide a theoretical basis for further development and application of M. tenacissima polysaccharide, and show that MTP-SeNPs could be explored as a promising anti-hepatoma agent in the pharmaceutical and biomedical industries.
研究领域:
药理学
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纳米技术
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肿瘤学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
NUTRITION AND CANCER-AN INTERNATIONAL JOURNAL
·
2021
·
IF 2.9
Yonglu Li,Yaxuan Wang,Xin Yu,Ting Yu,Xiaodong Zheng,Qiang Chu
Lung cancer with high mortality is regarded as a challenging global problem with unsatisfied curative effects. Clinically, the chemotherapy drugs are often faced with side-effects and tumor resistance. Radix Tetrastigma (RT) is a traditional Chinese herb and now regarded as a kind of functional food. In this study, A549-bearing nude mice control was adopted to evaluate the anti-tumor capacity of RT. Results demonstrated that RT showed excellent anti-tumor ability with no side-effect on mice compared to chemotherapy drug (5-Fu).Further studies proved that RT down-regulated the proliferation-related proteins (PCNA, Ki67) and vascular endothelial growth factor (VEGF). Additionally, RT up-regulated the ratio of Bax/Bcl-2, which caused the over-expression of Caspase-9, leading to the activation of downstream protein caspase-3, eventually resulting in apoptosis of A549 in solid tumor. These results together suggest that RT inhibits the non-small cell lung cancer (NSCLC) via Bax/Bcl2/Caspase-9/Caspase-3 pathway. Furthermore, the anti-A549 abilities of the main flavonoid components from RT were compared, and kaempferol-3-O-rutinoside would play a role in RT’s outstanding anti-NSCLC ability.
研究领域:
肿瘤学
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药理学
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中药学
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分子生物学
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DOI
PubMed
高影响因子
Foods
·
2025
·Vol. 14
·期 6
·1026
·
IF 5.1
Qiuyan Li,Lu Jiang,Ni Chen,Xingzhi Wang,Jiajun Yao,Zhien Su,Suqing Zhao
Melanoma is one of the most lethal cancers originating from melanocytes. Its incidence and mortality have been rising rapidly for several decades and have posed a serious threat to human health. Current melanoma treatments are hindered by the scope of application, low efficiency, high cost, and toxic side effects. Due to their affordability and minimal side effects, natural bioactive compounds derived from plants are promising candidates for melanoma treatment. This study aims to delve into the isolation, purification, and characterization of potato proteins and to explore their potential in melanoma treatment. Two potato proteins, patatin PP-1 and aspartate protease inhibitor PP-2, were isolated and purified by a newly developed method in this work, and their physicochemical properties were systematically characterized. Both potato proteins showed great antiproliferative activities and migration inhibition effects on melanoma cells. Meanwhile, Western blotting results illustrated that they could induce endogenous cell apoptosis by regulating the Bax/Bcl-2 pathway. Notably, aspartate protease inhibitor PP-2 demonstrated the best performance in inhibiting the growth and migration of melanoma cells, which might be attributed to the combined effect of its significant antioxidative activity and the inhibition effect of certain necessary protease activities in melanoma. This study provides valuable insights for developing nutraceuticals and therapeutic strategies against melanoma, which can lead to breakthroughs in melanoma treatment.
研究领域:
肿瘤学
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药理学
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植物化学
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产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2020
·
IF 2.87
Yan Xu,Xiangmei Jin,Jun Zhang,Kun Wang,Xiaoyan Jin,Dongyuan Xu,Xizhe Tian,Lan Liu
In this study, we designed, formulated, and investigated the potential antitumor activity of a folate receptor (FR)-mediated double-targeted drug delivery system. The system comprised of the FR ligand folic acid (FA), glycine-phenylalanine-leucine-glycine (Gly-Phe-Leu-Gly, GFLG), which can be specifically cleaved by cathepsin B, and the anticancer drug mitomycin C (MMC). The antitumor effect of FA-GFLG-MMC was compared to that of MMC. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay revealed that FA-GFLG-MMC has a significantly higher inhibitory effect on HeLa, SiHa, and PC9 cells (high FR expression) than that on 16HBE and A549 cells (low FR expression). Furthermore, FA-GFLG-MMC inhibited cancer cell proliferation in a dose-dependent manner. Free MMC was toxic to both cancer and normal cells. Apoptosis of the HeLa, SiHa, and PC9 cells was higher than that of the A549 cells; however, the apoptotic effect on 16HBE cells was minimal. Proapoptotic protein bcl-2-associated X-protein (BAX) and antiapoptotic protein BCL-2 play critical roles in cellular defense and apoptotic signal transduction. BAX/BCL-2 ratio is used to determine the intensity of an apoptotic signal and assess whether a cell will survive or undergo apoptosis. BAX and BCL-2 expression in cells treated with 5 μM FA-GFLG-MMC was studied by Western blotting. FA-GFLG-MMC increased the BAX/BCL-2 ratio in HeLa, SiHa, and PC9 cells. The results show that FA-GFLG-MMC can effectively inhibit tumor cell proliferation by inducing apoptosis. Therefore, the system developed can enhance the delivery of anticancer drugs to cancer cells and thereby reduce their toxic effects on normal cells.
研究领域:
药理学
·
肿瘤学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2018
·Vol. 23
·期 7
·1578
·
IF 3.098
Wenrui Wang,Tiantian Chen,Henan Xu,Baihui Ren,Xiaodan Cheng,Rongrong Qi,Haibo Liu,Yueyue Wang,Lei Yan,Sulian Chen,Qingling Yang,Changjie Chen
Curcumin (Cur) has been widely used in medicine, due to its antibacterial, anti-inflammatory, antioxidant, and antitumor effects. However, its clinic application is limited by its instability and poor solubility. In the present wok, curcumin was loaded into solid lipid nanoparticles (SLNs), in order to improve the therapeutic efficacy for breast cancer. The results measured using transmission electron microscopy (TEM) indicated that Cur-SLNs have a well-defined spherical shape; the size was about 40 nm with a negative surface charge. The drug loading and encapsulation efficiency in SLNs reached 23.38% and 72.47%, respectively. The Cur-SLNs showed a stronger cytotoxicity against SKBR3 cells. In vitro cellular uptake study demonstrated a high uptake efficiency of the Cur-SLNs by SKBR3 cells. Moreover, Cur-SLNs induced higher apoptosis in SKBR3 cells, compared to cells treated by free drug. In addition, Western blot analysis revealed that Cur-SLNs could promote the ratio ofBax/Bcl-2, but decreased the expression ofcyclin D1andCDK4. These results suggested that Cur-SLNs could be a potential useful chemotherapeutic formulation for breast cancer therapy.Keywords:solid lipid nanoparticle;curcumin;breast cancer;cyclin D1
研究领域:
药学
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肿瘤学
·
纳米技术
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产品关联
DOI
PubMed
高影响因子
ACS Applied Bio Materials
·
2026
·
IF 5.6
Wenjing Zhang,Xiaoyang Chen,Ziyi Lin,Shangyang Pan,Zufa sabeel,Wenxin Li,Heyun Shen,Zhao Yang
Breast cancer (BC) remains the most prevalent and deadly malignancy among women worldwide. While photothermal therapy (PTT) and chemodynamic therapy (CDT) offer tumor-specific and minimally invasive advantages, their standalone efficacy is limited. Ligustilide (LIG) can exert antitumor effects by generating •O2–, but its bioavailability is poor, thus necessitating improved delivery strategies. Here, we reported a multifunctional nanoplatform (FeD@LIG) integrating PTT, CDT, and chemotherapy for the simultaneous elimination of breast cancer stem cells (BCSCs) and non-BCSCs. FeD@LIG was synthesized via one-step oxidative polymerization of dopamine, co-loading Fe3+ and LIG. The nanospheres exhibited excellent photothermal conversion efficiency (52.8%) and pH/GSH-responsive drug release. Upon near-infrared (NIR) irradiation, FeD@LIG triggered ROS generation via Fenton-like reactions and elevated local temperature, leading to enhanced oxidative stress, apoptosis, and LIG release. In vitro, FeD@LIG reduced cell viabilities of MCF-7 and MDA-MB-231 cells to 12.5 and 7.9%, respectively, and significantly inhibited BCSCs’ self-renewal. In vivo, FeD@LIG achieved a tumor inhibition rate of 92.8% with minimal toxicity. Mechanistic studies revealed activation of the BAX/BCL-2/Caspase-3 pathway and suppression of Hedgehog signaling. Overall, FeD@LIG represents a promising nanotherapeutic strategy for overcoming drug resistance and recurrence by inhibiting both BCSCs and non-BCSCs through multimodal synergistic therapy.
✓ 已验证
DOI
PubMed
高影响因子
Evidence-based Complementary and Alternative Medicine
·
2020
·
IF 1.813
Yuan-Yuan Li,Nan-Qu Huang,Fei Feng,Ying Li,Xiu-Mei Luo,Lin Tu,Jing-Qiu Qu,Yi-Man Xie,Yong Luo
Icaritin (ICT) is the main component in the traditional Chinese herb Epimedium, and it has been shown to have anti-Alzheimer’s disease (AD) effects, but its neuroprotective effects and the pharmacological mechanisms are unclear. In the present study, senescence-accelerated mouse prone 8 (SAMP8) mice were randomly divided into a model group and an ICT-treated group. Learning and memory abilities were detected by the Morris water maze assay, and the expression of amyloid beta protein (Aβ) and β-site APP cleavage enzyme 1 (BACE1) was determined by Western blotting and polymerase chain reaction (PCR). Histological changes in CA1 and CA3 were detected by hematoxylin-eosin staining (H&E staining), and the immunohistochemical analysis was used to detect the expression and localization of Bax and Bcl-2. The results showed that compared with the SAMP8 mice, the ICT-treated SAMP8 mice showed improvements in spatial learning and memory retention. In addition, the number of necrotic cells and the morphological changes in CA1 and CA3 areas were significantly alleviated in the group of ICT-treated SAMP8 mice, and the expression of BACE1, Aβ1-42 levels, and the Bax/Bcl-2 ratio in the hippocampus was obviously decreased in the ICT-treated group compared with the control group. The results demonstrated that ICT reduced BACE-1 levels, the contents of Aβ1-42, and the Bax/Bcl-2 ratio, suggesting that ICT might have potential therapeutic benefits by delaying or modifying the progression of AD.
研究领域:
神经科学
·
药理学
·
老年学
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DOI
PubMed
高影响因子
MOLECULES
·
2017
·Vol. 22
·期 11
·1814
·
IF 2.861
Wenrui Wang,Lingyu Zhang,Tiantian Chen,Wen Guo,Xunxia Bao,Dandan Wang,Baihui Ren,Haifeng Wang,Yu Li,Yueyue Wang,Sulian Chen,Baoding Tang,Qingling Yang,Changjie Chen
In this study, resveratrol-loaded solid lipid nanoparticles (Res-SLNs) were successfully designed to treat MDA-MB-231 cells. The Res-SLNs were prepared using emulsification and low-temperature solidification method. The Res-SLNs were spherical, with small size, negative charge, and narrow size distribution. Compared with free resveratrol, the Res-SLNs displayed a superior ability in inhibiting the proliferation of MDA-MB-231 cells. In addition, Res-SLNs exhibited much stronger inhibitory effects on the invasion and migration of MDA-MB-231 cells. Western blot analysis revealed that Res-SLNs could promote the ratio of Bax/Bcl-2 but decreased the expression of cyclinD1 and c-Myc. These results indicate that the Res-SLN may have great potential for breast cancer treatment.Keywords:solid lipid nanoparticle;resveratrol;breast cancer;cyclinD1
研究领域:
药理学
·
肿瘤学
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Chemistry
·
2025
·
IF 4.2
Zhihong Hu,Xixi Hou,Yongjing Ren,Ziyuan Wu,Dong Yan,Hong Chen,Lan Wang
Cervical cancer ranks as the fourth most common cancer among women. However, the current treatments have significant side effects and limited therapeutic effects on advanced diseases, so it is necessary to discover better treatments for cervical cancer. The current study investigated the potential anticancer effects of a series of gefitinib-1,2,3-triazole derivative on Hela cells. Among the investigated, the target compound c13 showed good anticancer activity against Hela cells (IC50 = 5.66 ± 0.35 μM) compared with gefitinib (IC50 = 14.18 ± 3.19 μM). Moreover, compound c13 significantly inhibited the colony formation ability of Hela cells in a dose-dependent manner, accompanied by morphological changes in HeLa cells. Further investigations demonstrated that compound c13 triggered cell apoptosis and arrested the cell cycle at the G2/M phase in Hela cells. In addition, western blot analysis revealed that compound c13 upregulated the Bax/Bcl-2 ratio, and increased the levels of active caspase 3 and PARP1 cleavage, which suggested the involvement of the mitochondrial pathway in compound c13-induced apoptosis. In brief, these results indicated that compound c13 is a promising compound for the treatment of cervical cancer.
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
JOURNAL OF MOLECULAR STRUCTURE
·
2024
·
IF 4
Wei Tian,Mingyu Ji,Tingting Yang,Wen Zhong,Yanping Li,Mei Yang,Peilin Yang,Xing Long
Two new rhein-organotin complexes Ph 3 Sn(O 2 CC 14 H 7 O 4 ) ( RS01 ) and Cy 3 Sn(O 2 CC 14 H 7 O 4 ) ( RS02 ) were synthesized and characterized by elemental analysis, IR, 1 H NMR, 13 C NMR, 119 Sn NMR, X-ray crystallography and thermo-gravimetric analysis. Both complexes has a triclinic crystal system P -1 space group and one-dimensional supramolecular chain structure. The MTT results demonstrated that rhein's anticancer activity was effectively increased by introducing organotin, RS01 and RS02 exhibited excellent anticancer activity in vitro, significantly superior to cisplatin and mitoxantrone. Interestingly, despite the fact that RS01 and mitoxantrone share the same 9,10-anthraquinone scaffold structure, RS01 not only showed high anticancer activity but also much lower nephrotoxicity than mitoxantrone. Flow cytometry showed that RS01 could significantly induce cell apoptosis and arrest cell cycle in G2 phase. Molecular docking and UV–Vis absorption spectra suggested that RS01 may be intercalation with DNA. Furthermore, western blot results showed that RS01 activated the DNA damage critical protein γ -H 2 AX and regulated the expression level of the mitochondrial apoptotic pathway critical protein (Bax/Bcl-2). Thus, RS01 induced cell death may be mediated through DNA damage and mitochondrial pathways. As a result, RS01 has significant development and application potential as an anticancer agent.
研究领域:
无机化学
·
金属有机化学
·
癌症研究
·
药学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）