Cytotoxicity In Vitro, Apoptosis, Cellular Uptake, Cell Cycle Distribution, Mitochondrial Membrane Potential Detection, DNA Binding, and Photocleavage of Ruthenium(II) Complexes

2013 ◽  
Vol 66 (5) ◽  
pp. 555 ◽  
Author(s):  
Gan-Jian Lin ◽  
Zheng-Zheng Li ◽  
Jun-Hua Yao ◽  
Hong-Liang Huang ◽  
Yang-Yin Xie ◽  
...  

Four new ruthenium(ii) complexes [Ru(bpy)2(NHPIP)](ClO4)2 (Ru-1), [Ru(phen)2(NHPIP)](ClO4)2 (Ru-2), [Ru(bpy)2(AHPIP)](ClO4)2 (Ru-3), and [Ru(phen)2(AHPIP)](ClO4)2 (Ru-4) (bpy = 2,2′-bipyridine; phen = 1,10-phenanthroline; NHPIP = 2-(3-nitro-4-hydroxylphenyl)imidazo[4,5-f][1,10]phenanthroline; AHPIP = 2-(3-amino-4-hydroxylphenyl)imidazo[4,5-f][1,10]phenanthroline) were synthesized and characterized by elemental analysis, electrospray mass spectrometry, and 1H NMR spectroscopy. The cytotoxicity in vitro of these complexes against BEL-7402, HeLa, MG-63, and MCF-7 cells was evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. Ru-4 shows the highest cytotoxic activity towards the selected cell lines among the four complexes. The morphological apoptosis was assayed by an acridine orange/ethidium bromide staining method, and the percentages of necrotic and apoptotic cells were determined by flow cytometry. The cellular uptake and the cell cycle arrest in BEL-7402 cell was investigated. The results showed these complexes inhibit the proliferation of BEL-7402 cells at G0/G1 phase arrest. The detection of mitochondrial membrane potentials using the fluorescence probe JC-1 (5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethylbenzimidazolcarbocyanine iodide) exhibited that the mitochondrial membrane potentials decrease. Upon irradiation, these complexes can effectively cleave pBR322 DNA.

2014 ◽  
Vol 38 (6) ◽  
pp. 2554-2563 ◽  
Author(s):  
Guang-Bin Jiang ◽  
Jun-Hua Yao ◽  
Ji Wang ◽  
Wei Li ◽  
Bing-Jie Han ◽  
...  

The in vitro cytotoxicity, apoptosis, cellular uptake, cell cycle arrest, ROS, mitochondrial membrane potential, western blot analysis and DNA-binding induced by Ru1 were investigated.


2019 ◽  
Vol 43 (22) ◽  
pp. 8566-8579 ◽  
Author(s):  
Miao He ◽  
Qiao-Yan Yi ◽  
Wen-Yao Zhang ◽  
Lan Bai ◽  
Fan Du ◽  
...  

Three new iridium(iii) polypyridyl complexes were synthesized. The cytotoxic activity in vitro and in vivo, apoptosis, cell cycle arrest, mitochondrial membrane potential, ROS and the expression of Bcl-2 family proteins were investigated.


2021 ◽  
Vol 11 ◽  
Author(s):  
Lixia Cao ◽  
Shaorong Zhao ◽  
Qianxi Yang ◽  
Zhendong Shi ◽  
Jingjing Liu ◽  
...  

The multidrug-resistant (MDR) phenotype is usually accompanied by an abnormal expression of histone deacetylase (HDAC). Given that HDAC is vital in chromatin remodeling and epigenetics, inhibiting the role of HDAC has become an important approach for tumor treatment. However, the effect of HDAC inhibitors on MDR breast cancer has not been elucidated. This study aim to demonstrate the potential of chidamide (CHI) combined with the chemotherapy drug doxorubicin (DOX) to overcome chemotherapeutic resistance of breast cancer in vitro and in vivo, laying the experimental foundation for the next clinical application. The results showed that, CHI combined with DOX showed significant cytotoxicity to MDR breast cancer cells in vitro and in vivo compared with the CHI monotherapy. The cell cycle distribution results showed that CHI caused G0/G1 cell cycle arrest and inhibited cell growth regardless of the addition of DOX. At the same time, annexin V staining and TUNEL staining results showed that CHI enhanced the number of cell apoptosis in drug-resistant cells. The western blot analysis found that p53 was activated in the CHI-treated group and combined treatment group, and then the activated p53 up-regulated p21, apoptosis regulator recombinant protein (Puma), and pro-apoptotic protein Bax, down-regulated the apoptotic proteins Bcl-xL and Bcl-2, and activated the caspase cascade to induce apoptosis.


RSC Advances ◽  
2015 ◽  
Vol 5 (31) ◽  
pp. 24534-24543 ◽  
Author(s):  
Wei Li ◽  
Bing-Jie Han ◽  
Jun-Hua Yao ◽  
Guang-Bin Jiang ◽  
Yun-Jun Liu

Four Ru(ii) complexes [Ru(N–N)2(DHBT)](ClO4)2 were synthesized and characterized. The cytotoxicity in vitro, apoptosis, comet assay, cell migration, ROS, mitochondrial membrane potential, cell cycle arrest and expression of proteins were investigated.


RSC Advances ◽  
2014 ◽  
Vol 4 (77) ◽  
pp. 40899-40906 ◽  
Author(s):  
Bing-Jie Han ◽  
Guang-Bin Jiang ◽  
Ji Wang ◽  
Wei Li ◽  
Hong-Liang Huang ◽  
...  

Three complexes were synthesized and characterized. The cytotoxicity, apoptosis, cellular uptake, reactive oxygen species, mitochondrial membrane potential, cell cycle arrest and western blot analysis were investigated.


2019 ◽  
Vol 19 (9) ◽  
pp. 1103-1113 ◽  
Author(s):  
Islam El-Garawani ◽  
Sobhy Hassab El Nabi ◽  
Ebtesam Nafie ◽  
Samar Almeldin

Background: Fennel (Foeniculum vulgare) and rose geranium (Pelargonium graveolens) oils are known for their various biological effects including anticancer properties. Objective: This study aimed to evaluate the anticancer mechanism of fennel and geranium oils combined treatment on MCF-7 cells. Methods: The GC-MS method for essential oil characterization as well as the in vitro cytotoxicity, morphological changes, real-time PCR and immunocytochemical investigation for apoptosis-related markers, in addition, to flow cytometric cell cycle distribution analysis were done. Results: The major constituents of both essential oils were anethole (55.33 %) and estragole (11.57 %) for fennel essential oil. However, cintronellol (34.40 %) and geraniol (8.67 %) were identified in geranium oil. The results revealed an IC50 of 220±5.7 and 60±2.1µg/ml for fennel and geranium oils, respectively. The mechanistic anticancer properties were investigated throughout the 70, 50, and 25µg/ml of oils mixture. The marked apoptotic morphology and the flow cytometric cell cycle distribution analysis in addition to the levels of apoptosisrelated makers such as p53, caspase-3, mir-21, mir-92a, Bcl-2, and ki-67 confirmed that fennel and geranium oils combination induced cell cycle arrest and apoptosis in MCF-7 cells. Moreover, the oils mixture did not exert any significant (P<0.01) toxicity on normal human peripheral blood lymphocytes in vitro. Conclusion: The findings showed that the mixture of oils exerted selective cytotoxicity towards MCF-7 cells through induction of cell cycle arrest and apoptosis which may be triggered by the synergistic effect between the active ingredients of fennel and geranium oils.


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