Comparative sensitivity of tumor and non-tumor cell lines as a reliable approach for in vitro cytotoxicity screening of lysine-based surfactants with potential pharmaceutical applications

Nogueira, Daniele Rubert; Mitjans, Montserrat; Infante, M. R.; Vinardell, M. Pilar

doi:10.1016/j.ijpharm.2011.08.020

Cited by 51 publications

(39 citation statements)

References 41 publications

(55 reference statements)

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“…The choice of 77KS as a bioactive excipient in the NP formulation was based on our previous studies, which showed its pH-sensitive membrane-disruptive activity, together with improved kinetics in the endosomal pH range and low cytotoxic potential (Nogueira et al 2011a(Nogueira et al , 2011b. 77KS was incorporated into the NPs at a concentration below its CMC, thereby indicating that this surfactant is presented in the formulation in its monomer form.…”

Section: Resultsmentioning

confidence: 99%

“…We chose the in vitro model systems to perform this study, as they provide a rapid and effective means to assess NPs for a number of toxicological endpoints and mechanism-driven responses. Primarly, we evaluated if the unloaded-CS-NPs have any cytotoxic effect, which can be attributed especially to the presence of surfactant (Nogueira et al 2011b). Fig.…”

Section: In Vitro Assessments Of Antitumor Activitymentioning

confidence: 99%

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Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

et al. 2015

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The encapsulation of antitumor drugs in nanosized systems with pH-sensitive behavior is a promissing approach that may enhance the success of chemotherapy in many cancers. The nanocarrier dependence on pH might trigger an efficient delivery of the encapsulated drug both in the acidic extracellular environment of tumors and, especially, in the intracellular compartments through disruption of endosomal membrane. In this context, here we reported the preparation of chitosan-based nanoparticles encapsulating methotrexate as a model drug (MTX-CS-NPs), which comprises the incorporation of an amino acid-based amphiphile with pHresponsive properties (77KS) on the ionotropic complexation process. The presence of 77KS clearly gives a pH-sensitive behavior to NPs, which allowed accelerated release of MTX with decreasing pH as well as pH-dependent membrane-lytic activity. This latter performance demonstrates the potential of these NPs to facilitate cytosolic delivery of endocytosed materials.Outstandingly, the cytotoxicity of MTX-loaded CS-NPs was higher than free drug to MCF-7 tumor cells and, to a lesser extent, to HeLa cells. Based on the overall results, MTX-CS-NPs modified with the pH-senstive surfactant 77KS could be potentially useful as a carrier system for intracellular drug delivery and, thus, a promising targeting anticancer chemotherapeutic agent.

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Section: Resultsmentioning

confidence: 99%

Section: In Vitro Assessments Of Antitumor Activitymentioning

confidence: 99%

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

et al. 2015

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“…Naringenin (5) Luteolin (6) Quercetin (7) Vitexin (R= glucose) (8) Quercetin 3-O-β-glucoside (R=glucose) (9) Rutin (10) (Sardari et al, 2009), some of them from the Moraceae family. It is already reported that the cytotoxicity potential of compounds varies with the type of cell line and the method employed to evaluate it (Nogueira et al 2011), also with the type of substance which is investigated and its time of exposition (Van de Sandt, 1992). The screening of anti-HSV-1 activity of the extract was carried on at the highest non-toxic concentration (119 µg/mL) in Vero cells, because being the viruses intracellular parasites, the death of the cells could lead to a false antiviral effect.…”

Section: Antibacterial Assaymentioning

confidence: 99%

Evaluation of cytotoxicity, anti-herpes simplex virus type 1 (HSV-1) and antibacterial activities of Ficus vasta and phytoconstituents

Rashed

Ono²

2013

Int Curr Pharm J

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This study deals with the evaluation of in vitro cytotoxicity of the methanol 80% extract of Ficus vasta aerial parts in Vero cells, anti-HSV-1 and antibacterial activities and the determination of the phytochemical content of the F. vasta methanol extract. The extract was tested for its cytotoxicity in Vero cells and for anti-HSV-1 and against bacterial strains as S. aureus, S. epidermidis, E. coli and P. aeruginosa and also phytochemical constituents were detected. The results showed that this extract presented a CC50 value of 389 µg/mL, an intermediate value taking into account other researchers reported for some Moraceae species. Regarding the other biological activities, antiviral effect was not demonstrated by a HSV-1 challenge dilution of 100x tissue culture infective dose 50% (TCID50) and also by the disk-diffusion method at the higher non-toxic concentration of the extract (119 µg/mL). Phytochemical analysis of the methanol extract proved the presence of carbohydrates, tannins, flavonoids, coumarins, alkaloids and triterpenes. Chromatographic separation of the methanol extract resulted in the isolation and identification of ?-sitosterol, stigmasterol, lupeol, ursolic acid, naringenin, luteolin, quercetin, vitexin, quercetin 3-O-?-glucoside and rutin. The results indicated that F. vasta aerial parts methanol extract is potential candidate for experiments of biological activity screening that are not anti-HSV-1 or antibacterial against the strains evaluated in this study, to be carried on in the future.DOI: http://dx.doi.org/10.3329/icpj.v3i1.17295 International Current Pharmaceutical Journal, December 2013, 3(1): 211-218

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“…Specific responses related to the cell line tested are described in the literature with different materials. 31 It is possible to infer that for CCD 1059sk cells derived from skin fibroblasts, latex C-serum was not cytotoxic at the concentrations tested. Although more studies of pre-clinical and clinical toxicity are needed, this results can be an indicative of possible therapeutic application of latex C-serum as a treatment for skin diseases related to reactive species or even preventive skin pharmacological formulations.…”

Section: Discussionmentioning

confidence: 92%

“…11,12 Nogueira et al (2011) 31 recommend that different cell lines from different origins must be used to screen the toxicological effects of new products with potential biomedical applications. For initial screening of latex C-serum potential toxicity, two human cell lines were chosen: MRC-5, derived from lung fibroblasts, and CCD 1059sk, derived from skin fibroblasts.MRC-5 cell line that were exposed to latex C-serum up to the concentration of 50 µg/mL showed no reduction of the cell viability, when compared to the control group.…”

Section: Discussionmentioning

confidence: 99%

Free-radical Scavenging properties and Cytotoxic Activity Evaluation of Latex C-serum from Hevea brasiliensis RRIM 600

Kerche

Cavalcante

Danna

et al. 2016

FRA

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Background: There are few studies exploring the antioxidant properties of the latex C-serum of the Hevea brasiliensis latex and their possible use for therapeutic application. Objective: This study investigated the in vitro antioxidant activity of the latex C-serum of H. brasiliensis and assessed the cytotoxicity of this fraction in two human cell lines derived from normal tissue (MRC-5 and CCD 1059sk. Chemical characterization was also assessed. Methods: Latex from H. brasiliensis was centrifuged and the C-serum phase was tested for in vitro free radical scavenging assays, such as hydroxyl and nitric oxide radicals, hydrogen peroxide and total antioxidant capacity by the phosphomolibdate method. Latex C-serum was also investigated for cytotoxic properties by the MTT test. Latex C-serum was chemical characterized by Infrared Spectroscopy Fourier Transform (FTIR). Results: Latex C-serum effectively scavenged hydroxyl and nitric oxide radicals and hydrogen peroxide and presented potent antioxidant activity. The results were compared to ascorbic acid, a standard antioxidant. The cytotoxicity evaluation of latex C-serum demonstrated cell line dependency and for CCD 1059sk cells derived from skin fibroblasts, latex C-serum was not cytotoxic. FTIR showed the presence of proteins in latex C-serum. Conclusion: Latex C-serum from Hevea brasiliensis presented strong antioxidant potential and these results openthe possibility of further studies aiming the use of latex C-serum as treatment for skin diseases related to reactive oxygenspecies or skin preventive pharmacological formulations.

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Comparative sensitivity of tumor and non-tumor cell lines as a reliable approach for in vitro cytotoxicity screening of lysine-based surfactants with potential pharmaceutical applications

Cited by 51 publications

References 41 publications

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

Evaluation of cytotoxicity, anti-herpes simplex virus type 1 (HSV-1) and antibacterial activities of Ficus vasta and phytoconstituents

Free-radical Scavenging properties and Cytotoxic Activity Evaluation of Latex C-serum from Hevea brasiliensis RRIM 600

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