Recent approaches for reducing hemolytic activity of chemotherapeutic agents

Jeswani, Gunjan; Alexander, Amit; Saraf, Shailendra; Saraf, Swarnlata; Qureshi, Azra; AJAZUDDIN, .

doi:10.1016/j.jconrel.2015.06.001

Cited by 52 publications

(38 citation statements)

References 53 publications

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“…The amphipathic balance between the hydrophobic benzene nucleus and hydrophilic elements is an important parameter which determines the ability of acids to change the osmotic stability of RBCs . While the non‐polar part of the detergent dissolves in the lipid phase, the polar part remains in the aqueous medium, and as a result, the lipid part of the cell membrane is drawn to the aqueous phase causing cell lysis …”

Section: Resultsmentioning

confidence: 99%

“…[37] While the non-polar part of the detergent dissolves in the lipid phase, the polar part remains in the aqueous medium, and as a result, the lipid part of the cell membrane is drawn to the aqueous phase causing cell lysis. [39] A further study of the MP activity (MPA) of all compounds based on RBCs was carried out at a concentration of 1 μM, as it is known that reduction of concentration or substitution of the hydrogen atom in the carboxy fragment allows to minimize hemolytic efficiency. [20,24,25] An evaluation of MPA demonstrated that almost all compounds exhibited a statistically significant increase of cell survival under H 2 O 2 -oxidative stress conditions during the entire incubation period ( Figure 3).…”

Section: Resultsmentioning

confidence: 99%

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Synthesis and Antioxidant Ability of Novel Derivatives Based on para‐Coumaric Acid Containing Isobornyl Groups

Буравлев

Dvornikova

Schevchenko

et al. 2019

Chemistry & Biodiversity

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A series of novel esters and amides was synthesized on the basis of para‐coumaric acid containing isobornyl groups in ortho‐positions relative to the phenolic hydroxy group. Antioxidant properties of the obtained compounds were evaluated and compared on in vitro models: radical‐scavenging ability, antioxidant activity on a substrate containing the lipids of animal brain, cytotoxicity of red blood cells, antioxidant and membrane‐protective properties on the model of oxidative red blood cells hemolysis. Statistically significant relationship was established between the antioxidant activity of the studied compounds in model system containing animal lipids and the parameters reflecting their antioxidant properties on the model of H2O2‐induced hemolysis of red blood cells. It was determined that an amide with a morpholine fragment has the highest antioxidant activity. The specified derivative significantly surpassed the reference substances (parent acid, BHT) and was not inferior to the effective antioxidant 2,6‐diisobornyl‐4‐methylphenol in terms of its properties.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Synthesis and Antioxidant Ability of Novel Derivatives Based on para‐Coumaric Acid Containing Isobornyl Groups

Буравлев

Dvornikova

Schevchenko

et al. 2019

Chemistry & Biodiversity

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“…In order to reduce the hemolytic activity and improve the efficacy of chemotherapeutic drugs, polymer based drug delivery carriers and co-administration of drugs with phytochemicals have been practised 18 . Many phytochemicals demonstrated their efficacy either alone or in combination with chemo-drugs.…”

Section: Introductionmentioning

confidence: 99%

Size Dependent Uptake and Hemolytic Effect of Zinc Oxide Nanoparticles on Erythrocytes and Biomedical Potential of ZnO-Ferulic acid Conjugates

Babu

Subastri

Arumugam

et al. 2017

Sci Rep

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Despite zinc oxide nanoparticles (ZnONPs) being increasingly used as carriers in biomedical fields due to their multifaceted properties and therapeutic importance, better understanding of the mechanisms and cellular consequences resulting from their interaction with cells and cellular components has been warranted. In the present study, we investigate the size-dependent interaction of ZnONPs on RBCs, and its impact on cell viability, DNA damage, ROS generation and morphological changes, employing cellular and analytical methods. Size, charge, stability and solubility were confirmed by DLS, zeta potential, ICP-AES and TEM analysis. Further ICP-AES, TEM, spectroscopic observations and cell based assays showed that ZnONPs exhibited a size dependent impact on RBCs and haemoglobin (Hb), particularly size <50 nm. Conversely, ferulic acid (FA) conjugates and serum albumin significantly reduced the adverse effects exhibited by ZnONPs. The extent of DNA damage and ROS generation is comparatively low in ZnONPs-FA than in ZnONPs alone treated cells. Thus our study documents a novel conceptualization delineating the influence of size on the material properties and therapeutic potential of nanoparticle.

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“…All compounds were tested on human red blood cells (RBCs) to evaluate the toxicity of each compound to induce irreversible damages in the membrane of erythrocytes by the release of hemoglobin and intracellular components. [ 57,58 ] Results show that compounds 3 , 5a–d , 5f–g , 6a–c , 6e–g , 7a–b , 7d–g , 8c–g , and 9a–g lead to 100% hemolysis at a concentration of ≥ 200 μM, indicating that these compounds would be nontoxic. Compounds 5e , 6d , 7c , and 8a–b were considered moderately toxic.…”

Section: Resultsmentioning

confidence: 99%

New thiazolyl‐pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents

Cuartas

Robledo

Vélez

et al. 2020

Archiv der Pharmazie

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A new series of N-substituted pyrazoline derivatives 6a-g, 7a-g, 8a-g, and 9a-g was synthetized by reaction of hydrazine derivatives and chalcone-thiazole hybrids bearing nitrogen mustard 5a-g. The chalcones 5a-g were obtained by Claisen-Schmidt condensation of thiazole-2-nitrogen mustard 3 and selected acetophenones 4a-g. These new compounds 6/7/8/9a-g were screened for their antifungal activity against Cryptococcus neoformans, with IC 50 values of 3.9-7.8 µg/ml for the N-3, 5-dichlorophenyl pyrazolines 9e-g. Interestingly, those compounds show low cytotoxic effects toward erythrocytes (RBC). In addition, N-acetyl (6a,b) and N-formyl pyrazolines (7a, 7b, 7c, and 7g) showed inhibitory activity against methicillinsusceptible Staphylococcus aureus, methicillin-resistant S. aureus, and vancomycinintermediate S. aureus, with the most important minimum inhibitory concentration values ranging from 31.25 to 125 µg/ml. Regarding the antiprotozoal activity, thiazolyl-pyrazolines 9g, 8f, and 7c display high activity against Plasmodium falciparum, Leishmania (V) panamensis, and Trypanosoma cruzi, with EC 50 values of 11.80, 6.46, and 4.98 μM, respectively, and with 7c being approximately 2.6-fold more potent than benznidazole with a selectivity index of 1.61 on U-937 human cells, showing promising potential as a novel antitrypanosomal agent. K E Y W O R D S antibacterial activity, antifungal activity, antiprotozoal activity, chalcone, pyrazoline

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Recent approaches for reducing hemolytic activity of chemotherapeutic agents

Cited by 52 publications

References 53 publications

Synthesis and Antioxidant Ability of Novel Derivatives Based on para‐Coumaric Acid Containing Isobornyl Groups

Synthesis and Antioxidant Ability of Novel Derivatives Based on para‐Coumaric Acid Containing Isobornyl Groups

Size Dependent Uptake and Hemolytic Effect of Zinc Oxide Nanoparticles on Erythrocytes and Biomedical Potential of ZnO-Ferulic acid Conjugates

New thiazolyl‐pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents

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