Cytotoxic and anticancer properties of new ruthenium polypyridyl complexes with different lipophilicities

Tikum, Anjong Florence; Jeon, Yu Jeong; Lee, Ju Hyun; Park, Min Hee; Bae, In Yeong; Kim, Sang Heon; Lee, Hye Jin; Kim, Jinheung

doi:10.1016/j.jinorgbio.2018.01.003

Cited by 15 publications

(1 citation statement)

References 25 publications

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“…The alkyl groups within a molecule contribute to its overall lipophilic character. An increase in the lipophilic character usually imparts better cytotoxic properties by improving the penetration of the drug across the cellular membranes [34]. Addition of alkyl groups or increasing the alkyl chain length has resulted into an improved cytotoxic potential of the drugs [35,36].…”

Section: Pharmacological Evaluationmentioning

confidence: 99%

Cytotoxic and Pro-Apoptotic Properties of Ethyl-p-Methoxycinnamate and Its Hydrophilic Derivative Potassium-p-Methoxycinnamate

et al. 2018

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Purpose The present study was designed to investigate the underlying mechanism of cytotoxic and pro-apoptotic potential of ethyl-p-methoxycinnamate (EPMC) and its hydrophilic derivative potassium-p-methoxycinnamate (KPMC). Methods EPMC was isolated from Kaempferia galanga extract and its ethyl chain was replaced with potassium by KOH reflux to synthesize KPMC. The anti-proliferative effect of EPMC and KPMC was evaluated in six cancer cell lines and two normal cell lines by MTT assay. The inhibitory effects of the test compounds on colony formation, cell migration, chromatin condensation and mitochondrial membrane potential was further investigated in HCT-116 cells whereas their effect on caspase 3, 7, 8 and 9 activities was studied in HCT-116 and PC-3 cells. Results EPMC exhibited significant antiproliferative effect in all six cancer cell lines with maximum cytotoxicity against HCT-116 cells (selectivity index > 6). Our results showed significant inhibition of cell migration and colony formation in EPMC-treated colorectal carcinoma cells (HCT-116) when compared to the normal colon fibroblasts (CCD-18co). It exhibited dose dependent chromatin condensation and loss of mitochondrial membrane potential with subsequent induction of caspase 3/7 activity. KPMC did not inhibit the proliferation of either cell lines in MTT assay. Moreover, the cell migration, colony formation and caspase induction in KPMC-treated cells was comparable with the negative control. Conclusion The replacement of alkyl chain in EPMC by potassium resulted into the loss of cytotoxic and pro-apoptotic effects of EPMC.

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Section: Pharmacological Evaluationmentioning

confidence: 99%

Cytotoxic and Pro-Apoptotic Properties of Ethyl-p-Methoxycinnamate and Its Hydrophilic Derivative Potassium-p-Methoxycinnamate

et al. 2018

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Synthesis and antibacterial against Staphylococcus aureus of new ruthenium (II) polypyridine complexes containing pyrene groups

Wei

Wang

et al. 2022

Applied Organom Chemis

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As the treatment of Staphylococcus aureus infection becomes more and more difficult, it is particularly important to develop new antibacterial agents against S. aureus infection. Herein, three ruthenium (II) complexes containing pyrene groups, [Ru (bpy)2(PYIP)](PF6)2 (Ru‐1), [Ru (dtbpy)2(PYIP)](PF6)2 (Ru‐2), and [Ru (ttbpy)2(PYIP)](PF6)2 (Ru‐3) (PYIP = 2‐(pyren‐1‐yl‐1H‐imidazo[4,5‐f][1,10]phenanthroline, bpy = 2,2′‐bipyridine, dtbpy = 4,4′‐dimethyl‐2,2′‐bipyridine and ttbpy = 4,4′‐di‐tert‐butyl‐2,2′‐bipyridine) were designed and synthesized. The antibacterial activities of them against S. aureus were evaluated by determining the minimum inhibitory concentration and minimum bactericidal concentration. The results showed that three ruthenium complexes had excellent antibacterial activities against S. aureus. Among them, Ru‐2 exhibited the best bacteriostatic concentration and bactericidal activities, which was selected for the further antibacterial mechanism exploring. Ru‐2 can obviously inhibit the growth of bacterial biofilm, and the drug resistance results showed that Ru‐2 can effectively prevent the development of bacterial resistance. Moreover, the in vivo antibacterial activity of Ru‐2 was evaluated by establishing mouse infection model with the results that Ru‐2 could effectively inhibit the growth of bacteria and make mouse wounds heal faster.

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Lysosome-targeted ruthenium(II) complex encapsulated with pluronic® F-127 induces oncosis in A549 cells

Pan,

Zhang,

Huang

et al. 2024

J Biol Inorg Chem

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Cytotoxic and anticancer properties of new ruthenium polypyridyl complexes with different lipophilicities

Cited by 15 publications

References 25 publications

Cytotoxic and Pro-Apoptotic Properties of Ethyl-p-Methoxycinnamate and Its Hydrophilic Derivative Potassium-p-Methoxycinnamate

Cytotoxic and Pro-Apoptotic Properties of Ethyl-p-Methoxycinnamate and Its Hydrophilic Derivative Potassium-p-Methoxycinnamate

Synthesis and antibacterial against Staphylococcus aureus of new ruthenium (II) polypyridine complexes containing pyrene groups

Lysosome-targeted ruthenium(II) complex encapsulated with pluronic® F-127 induces oncosis in A549 cells

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