Cytotoxic effects of a novel maleimide derivative on epithelial and tumor cells

Ali, Bakat; Kupa, Léonard de Vinci Kanda; Heluany, Cíntia Scucuglia; Drewes, Carine Cristiane; Vasconcelos, Stanley N. S.; Farsky, Sandra Helena Poliselli; Stefani, Hélio A.

doi:10.1016/j.bioorg.2017.04.013

Cited by 18 publications

(12 citation statements)

References 33 publications

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“…According to the results, there was no statistical difference among the absorbance values between with and without centrifugation application (Figure 3, Step 6). Although centrifugation was recommended in many studies [17,18], we could not achieved statistically significant results for centrifugation.…”

Section: Optimization Of the Other Parameters (Step 4-9)contrasting

confidence: 58%

“…Various organic solvents such as dioxane, cyclohexane, tetrahydrofuran, dimethylformamide were also used for the assay [15,16]. In some previous reports, a centrifugation step was performed to precipitate formazan salts before solvent addition and medium removal to dissolve formazan salts [17,18]. Although the MTT test is one of the effective and reliable method to measure cell viability, this analytical techniques used various kind of studies [19,20] and it is necessary to optimize its accuracy and minimize the factors that affect MTT activity for specific cell lines.…”

Section: Introductionmentioning

confidence: 99%

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Optimization of some parametric values of MTT for the determination of human melanoma (SK-Mel-30) cell viability

Babacan

Kaba

Akçakale

et al. 2022

International Journal of Life Sciences and Biotechnology

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3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyltetrazoliumbromide (MTT) assay is a widely used assessment method for the determination of anticancerogenic effects of active compounds including plant secondary metabolites. Recently, some important plant active ingredients have been widely investigated for anticancerogenic properties on melanoma cancer lines which are the most lethal type of skin cancer. Although some methods including DNA assay, 3H-thymidine incorporation and flow cytometry have been recommended for counting cells in the culture, MTT is one of the most frequent method and therefore, MTT assay needs to be optimized for melanoma cell lines. In this study, the MTT analytical procedure for determination of cell viability of human melanoma cell line (SK-Mel-30) was divided into nine steps and various parameters in each step (reagent amount, incubation time, centrifugation, solvent type, waiting time before spectrophotometric analysis and spectrophotometric parameters) were optimized. Optimum amount of MTT reagent and incubation time after MTT addition were determined as 10 µL and 4 h for 96 well plate, respectively. Various solvents were evaluated for solubility effectiveness of the formed crystals and DMSO was found to be the best solvent to dissolve the crystals. Waiting time before spectrophotometric reading and Uv-vis spectrums were also evaluated. At the end of the study a flowchart, presented the best analytical conditions, was constructed. Obtained findings can be used for the determination of anticancerogenic properties of plant ingredients.

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Section: Optimization Of the Other Parameters (Step 4-9)contrasting

confidence: 58%

Section: Introductionmentioning

confidence: 99%

Optimization of some parametric values of MTT for the determination of human melanoma (SK-Mel-30) cell viability

Babacan

Kaba

Akçakale

et al. 2022

International Journal of Life Sciences and Biotechnology

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“…At 48 h viability values were even higher than 100%, which can particularly be due to the nonconjugated sites of the maleimide with G2. The low percentage of MR of G2 in the polymer m-PEG-PLGA in comparison to the other CPPs indicate that the accessible sites of unreacted maleimide may cause an increase in the cellular metabolism and therefore a greater MTT response [44]. Supplementary Figure 4 shows that the formulation without conjugated CPP (FMT-m-PEG-PLGA-NPs) with all the sites of unconjugated maleimide had greater MTT values than G2 (p < 0.01) and the other formulations (p < 0.0001) when assayed in HCE-2 cells at a concentration of 50 μg•ml −1 for 48 h.…”

Section: Discussionmentioning

confidence: 97%

“…In contrast, pAntp-NPs promoted greater TNF-α secretion than positive control (LPS-stimulated cells). This effect could probably be related with the mechanism used for cellular internalization of pAntp [43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58] . Particularly, the most accepted cellular internalization mechanism for the pAntp 43-58 is translocation, which would generate excessive destabilization of the cell membrane in HCE-2 cells, activating the inflammatory cascade that lead to increased secretion of certain cytokines.…”

Section: Discussionmentioning

confidence: 99%

“…This allows a greater pharmacological effect of the encapsulated component than NPs without CPPs on their surface [17]. CPPs such as Penetratin (pAntp [43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58] ) and the transcriptional activator peptide sequence (TAT 49-57 ) of HIV-1 have been shown to be effective for the cellular internalization of polypeptides and the transfection of nucleic acids. Besides, many of the CPPs share characteristics with antimicrobial peptides, such as cationic sequences with multiple Arg residues [18][19][20].…”

mentioning

confidence: 99%

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Ocular Penetration of fluorometholone-loaded PEG-PLGA Nanoparticles Functionalized With cell-penetrating Peptides

González-Pizarro

Parrotta

Vera

et al. 2019

Nanomedicine (Lond.)

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Aim: Development of fluorometholone-loaded PEG-PLGA nanoparticles (NPs) functionalized with cell-penetrating peptides (CPPs) for the treatment of ocular inflammatory disorders. Materials & methods: Synthesized polymers and peptides were used for elaboration of functionalized NPs, which were characterized physicochemically. Cytotoxicity and ability to modulate the expression of proinflammatory cytokines were evaluated in vitro using human corneal epithelial cells (HCE-2). NPs uptake was assayed in both in vitro and in vivo models. Results: NPs showed physicochemical characteristics suitable for ocular administration without evidence of cytotoxicity. TAT-NPs and G2-NPs were internalized and displayed anti-inflammatory activity in both HCE-2 cells and mouse eye. Conclusion: TAT-NPs and G2-NPs could be considered a novel strategy for the treatment of ocular inflammatory diseases of the anterior and posterior segment.

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Impairing Tumor Metabolic Plasticity via a Stable Metal‐Phenolic‐Based Polymeric Nanomedicine to Suppress Colorectal Cancer

Duan

Rothenberg

et al. 2023

Advanced Materials

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Targeting metabolic vulnerability of tumor cells is a promising anticancer strategy. However, the therapeutic efficacy of existing metabolism‐regulating agents is often compromised due to tolerance resulting from tumor metabolic plasticity, as well as their poor bioavailability and tumor‐targetability. Inspired by the inhibitive effect of N‐ethylmaleimide on the mitochondrial function, a dendronized‐polymer‐functionalized metal‐phenolic nanomedicine (pOEG‐b‐D‐SH@NP) encapsulating maleimide‐modified doxorubicin (Mal‐DOX) is developed to enable improvement in the overall delivery efficiency and inhibition of the tumor metabolism via multiple pathways. It is observed that Mal‐DOX and its derived nanomedicine induces energy depletion of CT26 colorectal cancer cells more efficiently than doxorubicin, and shifts the balance of programmed cell death from apoptosis toward necroptosis. Notably, pOEG‐b‐D‐SH@NP simultaneously inhibits cellular oxidative phosphorylation and glycolysis, thus potently suppressing cancer growth and peritoneal intestinal metastasis in mouse models. Overall, the study provides a promising dendronized‐polymer‐derived nanoplatform for the treatment of cancers through impairing metabolic plasticity.

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Cytotoxic effects of a novel maleimide derivative on epithelial and tumor cells

Cited by 18 publications

References 33 publications

Optimization of some parametric values of MTT for the determination of human melanoma (SK-Mel-30) cell viability

Optimization of some parametric values of MTT for the determination of human melanoma (SK-Mel-30) cell viability

Ocular Penetration of fluorometholone-loaded PEG-PLGA Nanoparticles Functionalized With cell-penetrating Peptides

Impairing Tumor Metabolic Plasticity via a Stable Metal‐Phenolic‐Based Polymeric Nanomedicine to Suppress Colorectal Cancer

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