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JOURNAL OF CLUSTER SCIENCE · 2023 · IF 2.8

Synthesis, Crystal Structure and Anticancer Studies of Cubane-Type Ni(II) Complex Derived from 5-bromosalicylaldehyde-2-aminophenol Schiff Base

Luo Yun,Hou Min,Yan Yu,Li Wen Ge,Tong Jing

The Schiff base ligand (5-bromosalicylaldehyde)-2-aminophenol (H 2 L) and its complex were synthesized and characterized. The crystal structure was established by single-crystal X-ray diffraction, which showed that the monomer [Ni 4 L 4 (CH 3 CH 2 OH) 4 ]·1.46(CH 3 CH 2 OH) (the Ni(II) complex) crystallized in the tetragonal structure with space group I 4 1 / a . IR, elemental analysis, and thermogravimetric analysis were used to further confirm the structure of the Ni(II) complex. Its independent unit consists of four Ni(II) atoms, four L 2− Schiff base ligands, and four coordinated ethanol molecules. In vitro anticancer activities against the four human cell lines, A-549, MDA-MB-231, SMMC-7721, and CNE-2Z, revealed that the Ni(II) complex exhibited significant anticancer activity. Furthermore, the anticancer activities of the Ni(II) complex on SMMC-7721 and CNE-2Z cells were much better than that of cisplatin. In addition, migration and the Transwell assay illustrated that the Ni(II) complex could inhibit the invasion and cell migration of tumor cells CNE-2Z and SMMC-7721.

研究领域: 化学 · 材料科学 · 药理学 · 肿瘤学
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Frontiers in Bioengineering and Biotechnology · 2025 · IF 4.8

Selenium-modified hydroxyapatite titanium coating: enhancing osteogenesis and inhibiting cancer in bone invasion by head and neck squamous cell carcinoma

Xutao Wen,Qin Zhou,Sihan Lin,Huaming Mai,Ling Zhang

Introduction Head and neck squamous cell carcinoma (HNSCC) frequently invades the jaw, and surgical treatment often leads to bone defects requiring reconstruction with titanium plates. To enhance the anti-tumor and bone regeneration properties of titanium, a selenium-modified hydroxyapatite coating was developed on titanium surfaces. Methods Selenium-modified hydroxyapatite coatings was fabricated using micro-arc oxidation (MAO). The coating properties were characterized by SEM, XPS, AFM, Contacting angle test and ICP-OES. Cell proliferation assays were performed using rBMSCs and Cal27 cells. The osteogenic potential of the materials was assessed via ALP and OCN immunofluorescence staining and quantitative polymerase chain reaction (qPCR). Apoptosis in Cal27 cells was analyzed through flow cytometry, and ROS levels in rBMSCs and Cal27 cells were measured using ROS fluorescent probes. Results A coating was successfully formed on the surface of titanium with a porous structure via MAO. The atomic percentages of calcium, phosphorus and selenium on the coating surface were 42.47%, 45.43% and 12.3%, respectively, and the ion components could be released steadily and slowly. In vitro , 0.2 µg/mL selenium had toxic effects on Cal27 and promoted osteogenic differentiation of rBMSCs. PCR showed that selenium increased the expression of genes related to osteogenic differentiation of rBMSCs by 3–5 times. ROS detection found differences in intracellular ROS content between Cal27 and rBMSCs. Discussion By incorporating selenium-modified coatings, titanium implant materials can simultaneously promote osteogenesis and inhibit tumor growth, offering a promising strategy for postoperative functional recovery in HNSCC patients.

研究领域: 生物材料学 · 肿瘤学 · 再生医学
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RSC Advances · 2017 ·Vol. 7 ·期 43 ·26625-26632 · IF 3.108

Microwave-assisted synthesis of polypyridyl ruthenium(II) complexes as potential tumor-targeting inhibitors against the migration and invasion of Hela cells through G2/M phase arrest

Jieqiong Cao,Qiong Wu,Wenjie Zheng,Li Li,Wenjie Mei

A series of polypyridyl ruthenium(II) complexes coordinated by phenanthroimidazole derivatives [Ru(phen)2(R)](ClO4)2 (where 1 R = IP, 2 R = PIP, 3 R = p-HPIP, 4 R = p-OCH3PIP) was synthesized with an average yield of >85% under microwave irradiation at 140 °C for 30 min. The inhibitory effect of these complexes against various tumour cells were evaluated by MTT assay, and the results showed that these polypyridyl ruthenium(II) complexes exhibited acceptable inhibition against different tumour cells, especially 4, with an IC50 of 18.4 μM for Hela cells. The results showed that 4 inhibited the growth of cervical cancer Hela cells by inducing G2/M phase arrest, which was followed by slight apoptosis. Further studies showed that 4 displayed better inhibition against the invasion and metastasis of Hela cells than NAMI-A. Studies on the in vivo distribution and metabolism indicated that 4 was rapidly distributed in the entire body, absorbed by the tumour tissue and had only a small accumulation of toxicity in the body. These results demonstrated that this type of ruthenium(II) complex can block the growth of Hela cells and inhibit their migration and invasion through G2/M phase arrest, which suggests the complex could act as a potential tumour-targeting inhibitor in future clinical applications.

研究领域: 药理学 · 肿瘤学 · 生物化学
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Materials Express · 2023 ·Vol. 13 ·期 1 ·81-84 · IF 0.7

Evaluation of the therapeutic effect of mitomycin-loaded hydrogel in inhibiting tumor-cell proliferation and invasion in pancreatic cancer

Wang Wen-Wen,Yang Li-Jie,Guo Jun-Feng

Pancreatic cancer is a common tumor of the digestive system with a high degree of malignancy and poor prognosis. Its incidence has significantly increased worldwide in recent years. Currently, approximately 90% of patients cannot be treated surgically. Thus, drug therapy plays an important role in pancreatic cancer treatment. In this study, hydrogels loaded with mitomycin were prepared from hyaluronic acid and carboxymethyl chitosan, which have excellent biocompatibility. SEM results showed that the hydrogels had a three-dimensional interoperable porous structure, and CCK-8 results showed that hydrogels loaded with mitomycin significantly reduced cancer-cell proliferation. The hydrogels also reduced the migration of cancer cells in a dose-dependent manner, indicating their potential use as a drug-carrier material for pancreatic cancer treatment.

研究领域: 肿瘤学 · 药剂学
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JOURNAL OF MEDICINAL CHEMISTRY · 2019 · IF 6.054

Fuplatin: An Efficient and Low-Toxic Dual-Prodrug

Ran Zhang,Xue-Qing Song,Rui-Ping Liu,Zhong-Ying Ma,Jing-Yuan Xu

As FDA-approved chemotherapeutic agents, cisplatin, oxaliplatin, and 5-fluorouracil are widely used in clinic but limited by severe side-effects. To ameliorate their respective defects, a series of “dual-prodrug” by linking oxoplatin and 5-FU were designed and synthesized. The assembled compounds 10–17, named Fuplatin, exhibited much higher cytotoxicity against the tested cancer cells while lower cytotoxicity toward the human normal lung cells than free drugs or their combinations. Among them, 14 enhanced cellular accumulation with 62- and 825-fold amount of oxaliplatin and 8 at 9 h, respectively, significantly induced DNA damage and cell apoptosis, and inhibited migration and invasion in HCT-116 cells. Compound 14 arrested the cell cycle at S and G2 phases and up-regulated thymidylate synthase and p53, consistent with the results of the combination, suggesting 14 adopted a collaborative mode of 5-FU and oxaliplatin to kill cancer cells. In vivo, compound 14 showed high antitumor effect and no observable toxicity in NOD/SCID mice bearing HCT-116 tumors.

研究领域: 肿瘤学 · 药理学 · 化疗
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Asian Journal of Pharmaceutical Sciences · 2024 · IF 10.7

Porous PLGA microspheres for the inhalation delivery of icariin and miR-23b in the treatment of metastatic lung cancer

Boyu Xiong,Xinxin Shao,Guangxu Fang,Mengmeng Dong,Haobo Han,Quanshun Li

Herein, porous poly(lactic-co-glycolic acid) (PLGA) microspheres were prepared to load icariin and miR-23b for the treatment of metastatic lung cancer. The microspheres exhibited desirable aerodynamic diameter, high drug loading and encapsulation efficiency, as well as a favorable drug release profile, which was beneficial for the deposition and exposure of drugs in the lung tissues. The release solution from microspheres exhibited a favorable anti-proliferative effect by inducting cell apoptosis and arresting the cell cycle at G1 phase, and meanwhile inhibited the migration and invasion of cancer cells. More importantly, the microspheres could be effectively inhaled and accumulated in the lung tissues to trigger the in situ apoptosis of tumor cells and suppress metastasis, using mice bearing melanoma-metastatic lung cancer as a model. Furthermore, inhalation of the microspheres showed good favorable biocompatibility, barely causing tissue damage. Overall, porous PLGA microspheres provide a promising platform for the inhalable co-delivery of drugs and genes to obtain ideal therapeutic efficacy in lung cancer and other pulmonary diseases.

CAS / MDL: 38215-36-0
研究领域: 药学 · 肿瘤学 · 生物技术 · 肺科学
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