scholarly journals Comparative Analyses of Metabolomic Fingerprints and Cytotoxic Activities of Soft Corals from the Colombian Caribbean

Marine Drugs ◽  
2019 ◽  
Vol 17 (1) ◽  
pp. 37 ◽  
Author(s):  
Liliana Santacruz ◽  
Olivier Thomas ◽  
Carmenza Duque ◽  
Mónica Puyana ◽  
Edisson Tello
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
High Resolution Mass Spectrometry ◽  
Biological Activities ◽  
Analytical Techniques ◽  
Living Organism ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Soft Corals

Soft corals (Cnidaria, Anthozoa, Octocorallia) are a diverse group of marine invertebrates that inhabit various marine environments in tropical and subtropical areas. Several species are recognized as prolific sources of compounds with a wide array of biological activities. Recent advances in analytical techniques, supported by robust statistical analyses, have allowed the analysis and characterization of the metabolome present in a single living organism. In this study, a liquid chromatography-high resolution mass spectrometry metabolomic approach was applied to analyze the metabolite composition of 28 soft corals present in the Caribbean coast of Colombia. Multivariate data analysis was used to correlate the chemical fingerprints of soft corals with their cytotoxic activity against tumor cell lines for anticancer purpose. Some diterpenoids were identified as specific markers to discriminate between cytotoxic and non-cytotoxic crude extracts of soft corals against tumor cell lines. In the models generated from the comparative analysis of PLS-DA for tumor lines, A549 and SiHa, the diterpene 13-keto-1,11-dolabell-3(E),7(E),12(18)-triene yielded a high score in the variable importance in projection. These results highlight the potential of metabolomic approaches towards the identification of cytotoxic agents against cancer of marine origin. This workflow can be useful in several studies, mainly those that are time consuming, such as traditional bioprospecting of marine natural products.

Cytotoxic Activities of Red Algae Collected from Jeju Island Against Four Tumor Cell Lines

2006 ◽  
Vol 11 (3) ◽  
pp. 177-183 ◽  
Author(s):  
Kil-Nam Kim ◽  
Ki-Wan Lee ◽  
Choon-Bok Song ◽  
Chang-Bum Ahn ◽  
You-Jin Jeon
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Red Algae ◽  
Jeju Island ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines

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.

New Spirocyclic Hydroxamic Acids as Effective Antiproliferative Agents

2020 ◽  
Vol 20 ◽  
Author(s):  
Margarita E. Neganova ◽  
Sergey G. Klochkov ◽  
Yulia R. Aleksandrova ◽  
Vladimir N. Osipov ◽  
Dmitry V. Avdeev ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Histone Deacetylase ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antioxidant Activities ◽  
Hydroxamic Acids ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Hek 293 ◽  
Underlying Mechanisms

Aims: The main goal of this work where is to synthesize new original spirocyclic hydroxamic acids, investigate their cytotoxicity against to the panel of tumor cell lines and possible mechanism of action of these active compounds. Background: Hydroxamic acids are one of the promising classes of chemical compounds with proven has anticancer potential properties. This is manifested in the presence of metal chelating and antioxidant activities, the ability to inhibit histone deacetylase enzymes and a chemosensitizing effect against well known cytostatics. Objective: Original spirocyclic hydroxamic acids were synthesized and spectrums of their antiproliferative activities were investigated. Methods: The cytotoxic activities on different tumor lines (SH-SY5Y, HeLa and healthy cells HEK-293) were investigated and determined possible underlying mechanisms of their activity. Result: New original spirocyclic hydroxamic acids were synthesized. These compounds exhibit antiproliferative properties against of the various tumor cultures cells and also exhibits antioxidant activity, a depolarizing effect on the mitochondrial membrane, inhibit the activity of the histone deacetylase enzyme, and also decrease of basal glycolysis and glycolytic capacity reserve of HeLa and SH-SY5Y tumor cell lines. Conclusion: The most promising are compounds 5j-l containing two chlorine atoms as substituents in the quinazoline part of the molecule and hydroxamate function. Therefore, these compounds can be considered as hit compounds for the development on their basis multi-target anticancer agents.

Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines

2010 ◽  
Vol 65 (10) ◽  
pp. 1271-1278 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Jorge Manzur ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Myelogenous Leukemia ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

With the ligands 4-phenyl-1-(furan-2-carbaldehyde)thiosemicarbazone, HTSC1, (1), 4-phenyl-1- (5´-phenyl-furan-2-carbaldehyde)thiosemicarbazone, HTSC2 (2), o-methoxy-benzaldehydethiosemicarbazone, HTSC3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC4 (4), the corresponding palladium(II) complexes, Pd(TSC1)2 (5), Pd(TSC2)2 (6), Pd(TSC3)2 (7), and Pd(TSC4)2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structure of Pd(TSC3)2 (7) was determined by single-crystal X-ray diffraction. Complex 7 shows a squareplanar geometry, where two deprotonated ligands are coordinated to the PdII center through the nitrogen and sulfur atoms in a trans arrangement. In vitro antitumor studies against different human tumor cell lines have revealed that the palladium(II) complexes 5- 8 are more cytotoxic (IC50 values in the range of 0.21 - 3.79 μM) than their corresponding ligands (1 - 4) (> 60 μM). These results indicate that the antiproliferative activity is enhanced when thiosemicarbazone ligands are coordinated to the metal. Among the studied palladium(II) complexes, 8 exhibits high antitumor activity on K562 chronic myelogenous leukemia cells with a low value of the inhibitory concentration (IC50 = 0.21 μM).

scholarly journals Cytotoxic Polyketides from a Deep-Sea Sediment Derived Fungus Diaporthe phaseolorum FS431

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3062 ◽  
Author(s):  
Zheng Niu ◽  
Yuchan Chen ◽  
Heng Guo ◽  
Sai-Ni Li ◽  
Hao-Hua Li ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Deep Sea ◽  
Human Tumor ◽  
Electron Capture Detection ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Deep Sea Sediment ◽  
Diaporthe Phaseolorum

Two new chromone-derived polyketides phaseolorins, G and H (1 and 2), and one new anthraquinone derivative, phaseolorin I (3), together with three known compounds (4–6), were isolated from the deep-sea sediment-derived fungus Diaporthe phaseolorum FS431. The structures of the new compounds were determined by comprehensive analysis of their spectroscopic data, and the absolute configuration of 1 was established by quantum chemical calculations of electron capture detection (ECD). All the isolated compounds (1–6) were tested for their in vitro cytotoxic activities against four human tumor cell lines, of which compound 4 exhibited significant effect against MCF-7, HepG-2, and A549 tumor cell lines with IC50 values of 2.60, 2.55, and 4.64 µM, respectively.

Synthesis and Biological Evaluation of New Piperazine Substituted 3, 5-Diarylisoxazolines

2019 ◽  
Vol 16 (2) ◽  
pp. 294-302 ◽  
Author(s):  
Hui Gao ◽  
Bei Liu ◽  
Ping Zhu ◽  
Li-Jun Zhang ◽  
Chun-Ping Wan ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Aim and Objective: Isoxazolines are an important class of nitrogen and oxygen-containing heterocycles, which have gained much importance as the potential biological agents. In order to study structureactivity relationships of isoxazolines, this work has been conducted. Materials and Methods: A series of new piperazine substituted 3, 5-diarylisoxazoline derivatives (6-31) were designed and synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anticancer effect against a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. Results: The substituents of the NH group of piperazine ring had an obvious influence on biological activities. Especially, compounds 5, 7, 8, 10, 11, 13 and 27-showed good inhibitory effect on the generation of NO compared to dexamethasone. Furthermore, derivatives 5, 6, 7, 8, 9, 13 and 26 were found to be potential selectively anticancer activity on human tumor cell lines, which displayed better cytotoxic activity to positive control 5- FU. Conclusion: Piperazine substituted 3, 5-diarylisoxazoline derivatives could be considered as new antiinflammatory and anticancer agents.

Gold Nanorods are Selective Cytotoxic Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Mohamed El Gendy ◽  
Michael Weinfeld ◽  
Ahmed Abdoon
Keyword(s):  
Tumor Cell ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Human Tumor ◽  
Cytotoxic Agents ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Hepatoma Hepg2

Background: Gold nanorods (GNRs) are very promising agents that have multiple applications in medicine and biology. However, the cytotoxic effects of GNRs have not been fully explored. Objective: Therefore, the main objective of this study was to determine the selective cytotoxic effect of GNRs towards several human tumor cell lines. Methods: To address this issue, three sizes of GNRs (10-nm, 25-nm, and 50-nm) were tested against two human tumor cell lines, namely, human hepatoma HepG2 and human prostate PC3 cancer cells. As GNRs are usually stored in soft tissues inside living bodies, we also tested the effect of GNRs on murine splenocyte viability. To determine if the GNRs displayed selectivity cytotoxicity towards cancer cells, active GNRs with the size showing the least cytotoxicity to splenocytes were then tested against a panel of 11 human tumor cell lines and two human non-tumor cell lines. Results: Our results showed that the most cytotoxic size of GNRs is 10-nm, followed by the 25-nm GNRs, while the 50-nm GNRs did not show a significant effect. In addition, the 25-nm GNRs were the least cytotoxic to splenocytes when tested for 24 and 48 h. These GNRs showed a selective cytotoxic effect to prostate cancer PC3 cells with median inhibitory concentration (IC50) = 8.3 + 0.37 µM, myeloblastic leukemia HL60 cells (IC50 = 19.7 + 0.89 µM), cervical cancer HeLa cells (IC50 = 24.6 + 0.37 µM), renal adenocarcinoma 786.0 cells (IC50 = 27.34 + 0.6 µM), and hepatoma HepG2 cells (IC50 = 27.79 + 0.03 µM) when compared to the effect on the non-tumor human cells; skin fibroblast BJ cell line (IC50 = 40.13 + 0.7 µM) or epithelial breast MCF10A cells (IC50 = 33.2 + 0.89 µM). A high selectivity indices (SI) were observed in GNRs-treated PC3 and HL60 cells with values ranging from 1.69 to 4.83, whereas moderate SIs were observed in GNRs-treated HeLa, 786.0, and HepG2 cells with values ranging from 1.19 to 1.63. Other cells did not show a similar selective effect, including human laryngeal HEp2 cells, colon HCT116, metastatic renal adenocarcinoma ACHN cells, and human breast cancer cells (MCF7, MDA-MB-231, and MDA-MB-468 cells). The effect of GNRs was confirmed using the colony formation assay and the effect was found to be cell cycle specific. Finally, it was shown that laser treatment can potentiate the cytotoxic effect of the 25-nm GNRs. Conclusion: GNRs are selective cytotoxic agents and they have the potential to act as candidate anticancer agents.

scholarly journals Preparation of Sesquiterpene Lactone Derivatives: Cytotoxic Activity and Selectivity of Action

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1113 ◽  
Author(s):  
María F. Beer ◽  
Augusto E. Bivona ◽  
Andrés Sánchez Alberti ◽  
Natacha Cerny ◽  
Guillermo F. Reta ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Chemotherapeutic Agents ◽  
Colon Tumor ◽  
Tumor Cell Lines ◽  
Diverse Range ◽  
Colon Tumor Cell

Cancer is one of the most important causes of death worldwide. Solid tumors represent the great majority of cancers (>90%) and the chemotherapeutic agents used for their treatment are still characterized by variable efficacy and toxicity. Sesquiterpene lactones are a group of naturally occurring compounds that have displayed a diverse range of biological activities including cytotoxic activity. A series of oxygenated and oxy-nitrogenated derivatives (4–15) from the sesquiterpene lactones cumanin (1), helenalin (2), and hymenin (3) were synthesized. The silylated derivatives of helenalin, compounds 13 and 14, were found to be the most active against tumor cell lines, with GI50 values ranging from 0.15 to 0.59 μM. The ditriazolyl cumanin derivative (11) proved to be more active and selective than cumanin in the tested breast, cervix, lung, and colon tumor cell lines. This compound was the least toxic against splenocytes (CC50 = 524.1 µM) and exhibited the greatest selectivity on tumor cell lines. This compound showed a GI50 of 2.3 µM and a SI of 227.9 on WiDr human colon tumor cell lines. Thus, compound 11 can be considered for further studies and is a candidate for the development of new antitumor agents.

scholarly journals Synthesis andIn VitroCytotoxic Activity of 2-Amino-7-(dimethylamino)-4-[(trifluoromethyl)phenyl]-4H-chromenes

2011 ◽  
Vol 8 (2) ◽  
pp. 598-602 ◽  
Author(s):  
M. Mahdavi ◽  
A. Asadipour ◽  
S. Rajabalian ◽  
M. Vosooghi ◽  
L. Firoozpour ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Mass Spectral Data ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Mass Spectral ◽  
H Nmr

Three 2-amino-4-(trifluoromethylphenyl)-3-cyano-7-(dimethylamino) -4H-chromene derivatives were synthesized and their cytotoxic activities were determined against six human tumor cell lines using MTT assay. Condensation of 3-(dimethylamino)phenol, trifluoromethybenzaldehydes and malonitrile in ethanol containing piperidine afforded corresponding chromenes(4a-c). The structure of the synthesized compound was confirmed by1H NMR, IR and Mass spectral data. Among compounds tested, 3-trifluoromethyl analogue(3b)was the most active against all human tumor cell lines (IC50=12-45 nM).

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