New Insights in Routine Procedure for Mathematical Evaluation of in vitro Cytotoxicity Data from Cancer Cell Lines

Zaharieva, Maya M.; Trochopoulos, Antonios; Dimitrova, Lyudmila; Berger, Martin R.; Najdenski, Hristo; Konstantinov, Spiro; Kroumov, Alexander Dimitrov

doi:10.7546/ijba.2018.22.2.87-106

Cited by 9 publications

(9 citation statements)

References 10 publications

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“…The median individual effects (median inhibitory concentrations, IC 50 ) of the WWs obtained from the four rose species were calculated by adapting an algorithm published elsewhere [98]. The theory of Chou and Talalay was applied, with some modifications [99].…”

Section: Mathematical Modelling Of Cytotoxic Effects and Redox-modulating Capacities Of Wastewatersmentioning

confidence: 99%

Redox-Modulating Capacity and Antineoplastic Activity of Wastewater Obtained from the Distillation of the Essential Oils of Four Bulgarian Oil-Bearing Roses

et al. 2021

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The wastewater from the distillation of rose oils is discharged directly into the soil because it has a limited potential for future applications. The aim of the present study was to determine in vitro the chromatographic profile, redox-modulating capacity, and antineoplastic activity of wastewater obtained by distillation of essential oils from the Bulgarian Rosa alba L., Rosa damascena Mill., Rosa gallica L., and Rosa centifolia L. We applied UHPLC-HRMS for chromatographic analysis of rose wastewaters, studied their metal-chelating and Fe(III)-reducing ability, and performed MTT assay for the evaluation of cytotoxic potential against three tumorigenic (HEPG2—hepatocellular adenocarcinoma, A-375—malignant melanoma, A-431—non-melanoma epidermoid squamous skin carcinoma) and one non-tumorigenic human cell lines (HaCaT—immortalized keratinocytes). The median inhibitory concentrations (IC50) were calculated with nonlinear modeling using the MAPLE® platform. The potential of the wastewaters to induce apoptosis was also examined. Mono-, di-, and acylated glycosides of quercetin and kaempferol, ellagic acid and its derivatives as main chemical components, and gallic acid and its derivatives—such as catechin and epicatechin—were identified. The redox-modulating capacity of the samples (TPTZ test) showed that all four wastewaters exhibited the properties of excellent heavy metal cleaners, but did not exert very strong cytotoxic effects. The lowest IC50 rate was provided in wastewater from R. centifolia (34–35 µg/mL of gallic acid equivalents after a 72 h period for all cell lines). At 24 and 48 hours, the most resistant cell line was HEPG2, followed by HaCaT. After 72 h of exposure, the IC50 values were similar for tumor and normal cells. Still, R. damascena had a selectivity index over 2.0 regarding A-431 non-melanoma skin cancer cells, showing a good toxicological safety profile in addition to moderate activity—IC50 of 35 µg/mL polyphenols. The obtained results related to wastewaters acquired after the distillation of essential oils from the Bulgarian R. alba, R. damascena, R. gallica, and R. centifolia direct our attention to further studies for in-depth elucidation of their application as detoxifying agents under oxidative damage conditions in other experimental datasets.

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Section: Mathematical Modelling Of Cytotoxic Effects and Redox-modulating Capacities Of Wastewatersmentioning

confidence: 99%

Redox-Modulating Capacity and Antineoplastic Activity of Wastewater Obtained from the Distillation of the Essential Oils of Four Bulgarian Oil-Bearing Roses

et al. 2021

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“…The calculation of the median inhibitory concentrations (IC 50 ) was performed as published before [81]. Briefly, a nonlinear regression procedure based on the weighted least squares statistical criterion as an objective function of the search was coded in the MAPLE ® software of symbolic mathematics.…”

Section: Calculation Of the Median Inhibitory Concentrations And Rsa Analysismentioning

confidence: 99%

Improvement of the Antimicrobial Activity of Oregano Oil by Encapsulation in Chitosan—Alginate Nanoparticles

et al. 2021

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Oregano oil (OrO) possesses well-pronounced antimicrobial properties but its application is limited due to low water solubility and possible instability. The aim of this study was to evaluate the possibility to incorporate OrO in an aqueous dispersion of chitosan—alginate nanoparticles and how this will affect its antimicrobial activity. The encapsulation of OrO was performed by emulsification and consequent electrostatic gelation of both polysaccharides. OrO-loaded nanoparticles (OrO-NP) have small size (320 nm) and negative charge (−25 mV). The data from FTIR spectroscopy and XRD analyses reveal successful encapsulation of the oil into the nanoparticles. The results of thermogravimetry suggest improved thermal stability of the encapsulated oil. The minimal inhibitory concentrations of OrO-NP determined on a panel of Gram-positive and Gram-negative pathogens (ISO 20776-1:2006) are 4–32-fold lower than those of OrO. OrO-NP inhibit the respiratory activity of the bacteria (MTT assay) to a lower extent than OrO; however, the minimal bactericidal concentrations still remain significantly lower. OrO-NP exhibit significantly lower in vitro cytotoxicity than pure OrO on the HaCaT cell line as determined by ISO 10993-5:2009. The irritation test (ISO 10993-10) shows no signs of irritation or edema on the application site. In conclusion, the nanodelivery system of oregano oil possesses strong antimicrobial activity and is promising for development of food additives.

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“…In contrast to MLT, which forms micellar aqueous solutions and cannot be applied intravenously due to hemolytic properties, ERF forms lamellar aqueous solutions, and is suitable for intravenous administration [4,5,33]. ERF exerts remarkably strong antineoplastic activity in vitro against various types of neoplasias related to bacterial infections, such as oral squamous cell carcinoma [30,34,35] and cutaneous T-cell lymphoma [36,37]. Bacterial infections may compromise the anticancer therapy outcome due to inflammation in the tissue microenvironment and accelerated carcinogenesis [38][39][40][41][42].…”

Section: Introductionmentioning

confidence: 99%

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

Zaharieva

Kroumov

Dimitrova

et al. 2019

Biotechnology & Biotechnological Equipment

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2019) Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenic Staphyloccocusaureus strains, Biotechnology & Biotechnological Equipment, 33:1,[38][39][40][41][42][43][44][45][46][47][48][49][50][51][52][53] ABSTRACT In the light of the emerging bacterial resistance to broad-spectrum antibiotics, the search for new antibacterial therapeutics and drug combinations is one of the most challenging topics nowadays. In the present study, we investigated for the first time the antibacterial and biofilm inhibitory effects of the third generation anticancer alkylphosphocholine (APC) erufosine against pathogenic Staphylococcus aureus strains in comparison to the prototype of this pharmacological class of drugs, miltefosine. We also searched for synergistic antibacterial combinations between both APCs and curcumin incorporated in copolymeric micelles based on PluronicV R P123 or a mixture of Pluronic V R P123 and Pluronic V R F127 (P123/F127). The obtained quantitative redoxactivity experimental data and drug-drug interactions were evaluated by using mathematical models in the MAPLE software. Similar to miltefosine, erufosine showed a moderate bacteriostatic effect in clinically relevant concentrations (50 Ä 60 lmol/L) and inhibited the redox activity of the treated bacteria up to 90% at minimal inhibitory concentrations. The effect of both APCs towards methicillin resistant staphylococci was enhanced by combinations with P123/F127 micellar CRM at a ratio of 1:1. Erufosine showed a stronger median biofilm inhibition at lower concentrations (MBIC 50 ¼ 1.87 lmol/L) than miltefosine (MBIC 50 ¼ 6.0 lmol/L) and curcumin (MBIC 50 ¼ 24.84 lmol/L) as demonstrated by quantification of biofilm-bound bacteria. In conclusion, the estimated antibacterial activity of erufosine widens the spectrum of its useful pharmacological effects, which is important for its clinical development. The established synergistic and additive drug combinations could be beneficial for the application of both APCs in cancer therapy, since numerous malignancies are accompanied by bacterial infections. ARTICLE HISTORY

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New Insights in Routine Procedure for Mathematical Evaluation of in vitro Cytotoxicity Data from Cancer Cell Lines

Cited by 9 publications

References 10 publications

Redox-Modulating Capacity and Antineoplastic Activity of Wastewater Obtained from the Distillation of the Essential Oils of Four Bulgarian Oil-Bearing Roses

Redox-Modulating Capacity and Antineoplastic Activity of Wastewater Obtained from the Distillation of the Essential Oils of Four Bulgarian Oil-Bearing Roses

Improvement of the Antimicrobial Activity of Oregano Oil by Encapsulation in Chitosan—Alginate Nanoparticles

Micellar curcumin improves the antibacterial activity of the alkylphosphocholines erufosine and miltefosine against pathogenicStaphyloccocus aureusstrains

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