Effects of N,N-heterocyclic ligands on the in vitro cytotoxicity and DNA interactions of copper(ii) chloride complexes from amidino-O-methylurea ligands

2016 ◽  
Vol 40 (7) ◽  
pp. 5861-5876 ◽  
Author(s):  
Atittaya Meenongwa ◽  
Rosa F. Brissos ◽  
Chaiyaporn Soikum ◽  
Prapansak Chaveerach ◽  
Patrick Gamez ◽  
...  
Keyword(s):  
Biological Activities ◽  
In Vitro Cytotoxicity ◽  
Dna Interactions ◽  
Heterocyclic Ligands ◽  
Chloride Complexes ◽  
Guanidine Derivatives

Four novel copper(ii) complexes based on guanidine derivatives have been synthesized by addition of N,N-heterocyclic ligands, and their interesting biological activities have been evaluated.

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Mannich Bases ◽  
In Vitro Cytotoxicity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

scholarly journals Multifaceted Studies of the DNA Interactions and In Vitro Cytotoxicity of Anticancer Polyaromatic Platinum(II) Complexes

2016 ◽  
Vol 22 (26) ◽  
pp. 8943-8954 ◽  
Author(s):  
Benjamin J. Pages ◽  
Jennette Sakoff ◽  
Jayne Gilbert ◽  
Alison Rodger ◽  
Nikola P. Chmel ◽  
...  
Keyword(s):  
In Vitro Cytotoxicity ◽  
Dna Interactions

Antibacterial activity and in vitro cytotoxicity evaluation of alginate-AgNP fibers

2016 ◽  
Vol 87 (11) ◽  
pp. 1377-1386 ◽  
Author(s):  
Xihui Zhao ◽  
Qun Li ◽  
Xiaowen Li ◽  
Yanzhi Xia ◽  
Bing Wang ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Treatment Time ◽  
Biological Activities ◽  
In Vitro Cytotoxicity ◽  
Cell Counting ◽  
Logarithmic Phase ◽  
E Coli ◽  
Alginate Fibers ◽  
And Staphylococcus Aureus

Biopolymer nanocomposites containing metal nanoparticles have attracted much attention due to their excellent properties and broad applications. In this work, alginate fibers embedded with silver nanoparticles (AgNPs) were prepared. The as-obtained alginate-AgNP fibers exhibited antibacterial activity against both Gram microorganisms of model microbes Escherichia coli (Gram-negative) and Staphylococcus aureus (Gram-positive). A growth kinetic study with S. aureus and E. coli displayed the inhibition of bacterial growth at the logarithmic phase. The cytotoxic effect of the fibers in human cervical cancer (HeLa) cells was assessed by cell counting kit-8 (CCK-8) assay and flow cytometry. The as-prepared alginate-AgNP fibers, particularly with high amount and long treatment time, showed high cell-killing efficiency. These findings emphasize that such alginate-AgNP fibers with multifaceted biological activities are a promising material for applications in the textile or biomedical fields.

Aminoacid-derivatized Cu (II) complexes: Synthesis, DNA interactions and in vitro cytotoxicity

2017 ◽  
Vol 849-850 ◽  
pp. 157-169 ◽  
Author(s):  
Rinky Singh ◽  
P. Rama Devi ◽  
Sharmita S. Jana ◽  
Ranjitsinh V. Devkar ◽  
Debjani Chakraborty
Keyword(s):  
In Vitro Cytotoxicity ◽  
Dna Interactions

Synthesis, structures and in vitro cytotoxicity studies of platinum(IV) complexes with N,S and S,S heterocyclic ligands

Polyhedron ◽  
2009 ◽  
Vol 28 (17) ◽  
pp. 3699-3706 ◽  
Author(s):  
Cornelia Vetter ◽  
Goran N. Kaluđerović ◽  
Reinhard Paschke ◽  
Santiago Gómez-Ruiz ◽  
Dirk Steinborn
Keyword(s):  
In Vitro Cytotoxicity ◽  
Heterocyclic Ligands ◽  
Cytotoxicity Studies

Cytotoxic and Genotoxic Activities of Alkaloids from the Bulbs of Griffinia gardneriana and Habranthus itaobinus (Amaryllidaceae)

2019 ◽  
Vol 19 (5) ◽  
pp. 707-717 ◽  
Author(s):  
Eduardo R. Cole ◽  
Jean P. de Andrade ◽  
João F. Allochio Filho ◽  
Elisângela F. P. Schmitt ◽  
Anderson Alves-Araújo ◽  
...  
Keyword(s):  
Cell Lines ◽  
Caspase 3 ◽  
Biological Activities ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Isolation And Identification ◽  
Wide Range

Background: Amaryllidaceae plants are known to be a great source of alkaloids, which are considered an extensive group of compounds encompassing a wide range of biological activities. The remarkable cytotoxic activities observed in most of the Amaryllidaceae alkaloids derivatives have prompt the chemical and biological investigations in unexplored species from Brazil. Objective: To evaluate the cytotoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator. Methods: Methanolic crude extracts of Griffinia gardneriana and Habranthus itaobinus bulbs were submitted to acid-base extraction to obtain alkaloid-enriched fractions. The obtained fractions were fractionated using chromatographic techniques leading to isolation and identification of some alkaloids accomplished via HPLC and 1H-NMR, respectively. Molecular docking studies assessed the amount of free binding energy between the isolated alkaloids with the caspase-3 protein and also calculated the theoretical value of Ki. Studies have also been developed to evaluate in vitro cytotoxicity and genotoxicity in such alkaloids and apoptosis activation via the caspase pathway using both tumor and normal cell lines. Results: Seven alkaloids were isolated and identified. Among these, 11-hydroxyvittatine and 2-α-7- dimethoxyhomolycorine were not cytotoxic, whereas tazettine, trisphaeridine, and sanguinine only showed activity against the fibroblast lineage. Lycorine and pretazettine were 10 to 30 folds more cytotoxic than the other alkaloids, including cancerous lines, and were genotoxic and capable of promoting apoptosis via the caspase-3 pathway. This result supports data obtained in docking studies wherein these two compounds exhibited the highest free energy values. Conclusion: The cytotoxicity assay revealed that, among the seven alkaloids isolated, only lycorine and pretazettine were active against different cell lines, exhibiting concentration- and time-dependent cytotoxic actions alongside genotoxic action and the ability to induce apoptosis by caspase-3, a result consistent with those obtained in docking studies.

scholarly journals Phytochemical Profile, Antioxidant Activity, and Cytotoxicity Assessment of Tagetes erecta L. Flowers

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1201
Author(s):  
Ana Flavia Burlec ◽  
Łukasz Pecio ◽  
Solomiia Kozachok ◽  
Cornelia Mircea ◽  
Andreia Corciovă ◽  
...  
Keyword(s):  
Biological Activities ◽  
In Vitro Cytotoxicity ◽  
In Vitro Assays ◽  
Tagetes Erecta ◽  
Phytochemical Analysis ◽  
Total Extract ◽  
Tagetes Erecta L ◽  
Cytotoxicity Assessment

Tagetes erecta L. is a popular ornamental plant of the Asteraceae family, which is widely cultivated not only for its decorative use, but also for the extraction of lutein. Besides carotenoid representatives, which have been extensively studied, other important classes of secondary metabolites present in the plant, such as polyphenols, could exhibit important biological activities. The phytochemical analysis of a methanolic extract obtained from T. erecta inflorescences was achieved using liquid chromatography–mass spectrometry (LC-MS) techniques. The extract was further subjected to a multistep purification process, which allowed the separation of different fractions. The total extract and its fractions contain several polyphenolic compounds, such as hydroxybenzoic and hydroxycinnamic acid derivatives, flavonols (especially quercetagetin glycosides), and several aglycons (e.g., quercetin, patuletin). One of the fractions, containing mostly quercetagitrin, was subjected to two different antioxidant assays (metal chelating activity and lipoxygenase inhibition) and to in vitro cytotoxicity assessment. Generally, the biological assays showed promising results for the investigated fraction compared to the initial extract. Given the encouraging outcome of the in vitro assays, further purification and structural analysis of compounds from T. erecta extracts, as well as further in vivo investigations are justified.

scholarly journals Evaluation of Antiproliferative Palladium(II) Complexes of Synthetic Bisdemethoxycurcumin towards In Vitro Cytotoxicity and Molecular Docking on DNA Sequence

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4369
Author(s):  
Natalia Miklášová ◽  
Peter Herich ◽  
Juan Carlos Dávila-Becerril ◽  
Joaquín Barroso-Flores ◽  
Eva Fischer-Fodor ◽  
...  
Keyword(s):  
Biological Activity ◽  
Colorectal Carcinoma ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Large Family ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Colorectal Carcinoma

Metallodrugs form a large family of therapeutic agents against cancer, among which is cisplatin, a paradigmatic member. Therapeutic resistance and undesired side effects to Pt(II) related drugs, prompts research on different metal–ligand combinations with potentially enhanced biological activity. We present the synthesis and biological tests of novel palladium(II) complexes containing bisdemethoxycurcumin (BDMC) 1 and 2. Complexes were fully characterized and their structures were determined by X-ray diffraction. Their biological activity was assessed for several selected human tumor cell lines: Jurkat (human leukaemic T-cell lymphoma), HCT-116 (human colorectal carcinoma), HeLa (human cervix epitheloid carcinoma), MCF-7 (human breast adenocarcinoma), MDA-MB-231 (human mammary gland adenocarcinoma), A549 (human alveolar adenocarcinoma), Caco-2 (human colorectal carcinoma), and for non-cancerous 3T3 cells (murine fibroblasts). The cytotoxicity of 1 is comparable to that of cisplatin, and superior to that of 2 in all cell lines. It is a correlation between IC50 values of 1 and 2 in the eight studied cell types, promising a potential use as anti-proliferative drugs. Moreover, for Jurkat cell line, complexes 1 and 2, show an enhanced activity. DFT and docking calculations on the NF-κB protein, Human Serum Albumin (HSA), and DNA were performed for 1 and 2 to correlate with their biological activities.

Synthesis and biological evaluation of 4-aminoantipyrine analogues

2020 ◽  
Vol 16 ◽  
Author(s):  
Houwei Ren ◽  
Premnath Dhanaraj ◽  
Israel V M V Enoch ◽  
Mosae Selvakumar Paulraj ◽  
Indiraleka M
Keyword(s):  
Cervical Cancer ◽  
Dna Cleavage ◽  
Anticonvulsant Activity ◽  
Biological Activities ◽  
Biological Evaluation ◽  
In Vitro Cytotoxicity ◽  
Dilution Method ◽  
Maximal Electroshock ◽  
Protein Receptors

Objectives: The aim of the present study is to carry out a simple synthesis of aminoantipyrine analogues and exploration of their antibacterial, cytotoxic, and anticonvulsant potential. Methods: The compounds were characterized employing multi-spectroscopic methods. The in vitro pharmacological response of a series of bacteria were screened employing serial dilution method. The derivatives were screened against maximal electro-shock for their anticonvulsant activity. Molecular docking was carried out to optimize the interaction of the compounds with HPV16-E7 receptors. Further, the in vitro cytotoxicity was tested against human cervical cancer (SiHa) cell lines. Results: The compounds show protection against maximal electroshock, esp. 3-nirto- and 4-methyl-3-nitrobenzamido derivatives. In addition, they reveal appreciable DNA cleavage activities and interactions with HPV16-E7 protein receptors, esp. 3,5-dinitro- and 4-methyl-3-nitrobenzamido derivatives. Furthermore, they show potent activity against cervical cancer cells (LD50 value up to 1200 in the case of 4-methyl-3-nitrobenzamido derivative and an inhibition of a maximum of 97% of cells). Conclusions: The simply synthesized aminoantipyrine derivatives show a variety of biological activities like antibacterial and anticancer effects. In addition, this is the first study demonstrating that 4-aminoantipyrine derivatives shows an anticonvulsant activity.

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