In vitro chemotherapeutic and antiangiogenic properties of cardenolides from Acokanthera oblongifolia (Hochst.) Codd

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Maha M. Soltan ◽  
Howaida I. Abd-Alla ◽  
Amal Z. Hassan ◽  
Atef G. Hanna
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Enzyme Inactivation ◽  
Enzyme Linked Immunosorbent Assay ◽  
Anticancer Properties ◽  
Mechanistic Investigation ◽  
G2m Phase

Abstract Acovenoside A and acobioside A were isolated from Acokanthera oblongifolia. Their anticancer properties were explored regarding, antiproliferative and antiangiogenic activities. The study included screening phase against six cancer cell lines followed by mechanistic investigation against HepG2 cancer cell line. The sulforhodamine-B (SRB) was used to determine their growth inhibitory power. In the other hand, flow cytometry techniques were recorded the cell death type and cell cycle analysis. The clonogenic (colony formation) and wound healing assays, enzyme-linked immunosorbent assay (ELISA) and molecular docking, were performed to evaluate the antiangiogenesis capability. Both compounds were strongly, inhibited four cancer cell lines at GI50 less than 100 nM. The in vitro mechanistic investigation against HepG2 resulted in cell accumulations at G2M phase and induction of apoptosis upon treating cells separately, with 400 nM Acov-A and 200 nM Acob-A. Interestingly, the same concentrations were able to activate caspase-3 by 7.2 and 4.8-fold, respectively. Suppressing the clonogenic capacity of HepG2 cells (20 and 40 nM) and inhibiting the migration of the colon Caco-2 cancer cells were provoke the results of vascular endothelial growth factor receptor2 (VEGFR2) kinase enzyme inactivation. The docked study was highly supportive, to the antiangiogenic approach of both cardenolides. The isolated cardenolides could orchestrate pivotal events in fighting cancer.

Design, Synthesis, Molecular Docking, and Anticancer Evaluation of Pyrazole Linked Pyrazoline Derivatives with Carbothioamide Tail as EGFR Kinase Inhibitors

2020 ◽  
Vol 21 (1) ◽  
pp. 42-60
Author(s):  
Farah Nawaz ◽  
Ozair Alam ◽  
Ahmad Perwez ◽  
Moshahid A. Rizvi ◽  
Mohd. Javed Naim ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Kinase Assay ◽  
Cervix Uteri ◽  
Egfr Kinase

Background: The Epidermal Growth Factor Receptor (known as EGFR) induces cell differentiation and proliferation upon activation through the binding of its ligands. Since EGFR is thought to be involved in the development of cancer, the identification of new target inhibitors is the most viable approach, which recently gained momentum as a potential anticancer therapy. Objective: To assess various pyrazole linked pyrazoline derivatives with carbothioamide for EGFR kinase inhibitory as well as anti-proliferative activity against human cancer cell lines viz. A549 (non-small cell lung tumor), MCF-7 (breast cancer cell line), SiHa (cancerous tissues of the cervix uteri), and HCT-116 (colon cancer cell line). Methods: In vitro EGFR kinase assay, in vitro MTT assay, Lactate dehydrogenase release, nuclear staining (DAPI), and flow cytometry cell analysis. Results: Compounds 6h and 6j inhibited EGFR kinase at concentrations of 1.66μM and 1.9μM, respectively. Furthermore, compounds 6h and 6j showed the most potent anti-proliferative results against the A549 KRAS mutation cell line (IC50 = 9.3 & 10.2μM). Through DAPI staining and phase contrast microscopy, it was established that compounds 6h and 6j also induced apoptotic activity in A549 cells. This activity was further confirmed by FACS using Annexin-V-FITC and Propidium Iodide (PI) labeling. Molecular docking studies performed on 6h and 6j suggested that the compounds can bind to the hinge region of ATP binding site of EGFR tyrosine kinase in a similar pose as that of the standard drug gefitinib. Conclusion: The potential anticancer activity of compounds 6h and 6j was confirmed and need further exploration in cancer cell lines of different tissue origin and signaling pathways, as well as in animal models of cancer development.

In vitro evaluation of anticancer properties of exopolysaccharides from Lactobacillus acidophilus in colon cancer cell lines

2015 ◽  
Vol 52 (2) ◽  
pp. 163-173 ◽  
Author(s):  
Venkataraman Deepak ◽  
Sharavan Ramachandran ◽  
Reham Mohammed Balahmar ◽  
Sureshbabu Ram Kumar Pandian ◽  
Shiva D. Sivasubramaniam ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Lactobacillus Acidophilus ◽  
Cancer Cell Lines ◽  
Colon Cancer Cell ◽  
In Vitro Evaluation ◽  
Anticancer Properties ◽  
Colon Cancer Cell Lines

scholarly journals Synthesis, Characterization, and In Vitro Cancer Cell Growth Inhibition Evaluation of Novel Phosphatidylcholines with Anisic and Veratric Acids

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2022 ◽  
Author(s):  
Marta Czarnecka ◽  
Marta Świtalska ◽  
Joanna Wietrzyk ◽  
Gabriela Maciejewska ◽  
Anna Gliszczyńska
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Human Organism ◽  
Cancer Cell Growth ◽  
Anticancer Properties ◽  
Health Promoting ◽  
Phenolcarboxylic Acids ◽  
Mcf 7

Phenolic acids and its methoxy derivatives are known to induce caspase-mediated apoptosis activity and exhibit cytotoxic effect towards various cancer cell lines. However, their low stability and poor bioavailability in the human organism extensively restrict the utility of this group of compounds as anticancer and health-promoting agents. In this report, a series of eight novel phosphatidylcholines (3a-b, 5a-b, 7a-b, 8a-b) containing anisic or veratric acids (1a-b) at sn-1 and/or sn-2 positions were synthesized. The phenoylated phospholipids were obtained in good yields 28–66%. The structures of novel compounds were determined by their spectroscopic data. All synthesized compounds were evaluated for their antiproliferative activity towards six cancer cell lines and normal cell line Balb/3T3. Lipophilization of phenolcarboxylic acids significantly increased their anticancer properties. The asymmetrically substituted phenoylated phosphatidylcholines exhibited higher antiproliferative effect than free acids. Lysophosphatidylcholine (7b) effectively inhibited the proliferation of human leukaemia (MV4-11), breast (MCF-7), and colon (LoVo) cancer cell lines at concentrations of 9.5–20.7 µm and was from 19 to 38-fold more active than corresponding free veratric acid. The conjugation of anisic/veratric acids with the phosphatidylcholine have proved the anticancer potential of these phenolcarboxylic acids and showed that this type of lipophilization is an effective method for the production of active biomolecules.

scholarly journals Synthesis, Characterization and In Vitro Evaluation of Novel 5-Ene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-ones as Possible Anticancer Agents

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1162
Author(s):  
Serhii Holota ◽  
Sergiy Komykhov ◽  
Stepan Sysak ◽  
Andrzej Gzella ◽  
Andriy Cherkas ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines ◽  
Hek293 Cells ◽  
In Vitro Evaluation ◽  
Anticancer Properties ◽  
Sar Study

The present paper is devoted to the search for drug-like molecules with anticancer properties using the thiazolo[3,2-b][1,2,4]triazole-6-one scaffold. A series of 24 novel thiazolo-[3,2-b][1,2,4]triazole-6-ones with 5-aryl(heteryl)idene- and 5-aminomethylidene-moieties has been synthesized employing three-component and three-stage synthetic protocols. A mixture of Z/E-isomers was obtained in solution for the synthesized 5-aminomethylidene-thiazolo[3,2-b]-[1,2,4]triazole-6-ones. The compounds have been studied for their antitumor activity in the NCI 60 lines screen. Some compounds present excellent anticancer properties at 10 μM. Derivatives 2h and 2i were the most active against cancer cell lines without causing toxicity to normal somatic (HEK293) cells. A preliminary SAR study had been performed for the synthesized compounds.

Parallel Solid-Phase Synthesis using a New Diethylsilylacetylenic Linker and Leading to Mestranol Derivatives with Potent Antiproliferative Activities on Multiple Cancer Cell Lines

2019 ◽  
Vol 18 (10) ◽  
pp. 1469-1481 ◽  
Author(s):  
Raphaël Dutour ◽  
René Maltais ◽  
Martin Perreault ◽  
Jenny Roy ◽  
Donald Poirier
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Solid Phase ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Multiple Cancer ◽  
Anticancer Properties ◽  
Antiproliferative Agent

Background: RM-133 belongs to a new family of aminosteroid derivatives demonstrating interesting anticancer properties, as confirmed in vivo in four mouse cancer xenograft models. However, the metabolic stability of RM-133 needs to be improved. After investigation, the replacement of its androstane scaffold by a more stable estrane scaffold led to the development of the mestranol derivative RM-581. Methods: Using solid-phase strategy involving five steps, we quickly synthesized a series of RM-581 analogs using the recently-developed diethylsilylacetylenic linker. To establish structure-activity relationships, we then investigated their antiproliferative potency on a panel of cancer cell lines from various cancers (breast, prostate, ovarian and pancreatic). Results: Some of the mestranol derivatives have shown in vitro anticancer activities that are close to, or better than, those observed for RM-581. Compound 23, a mestranol derivative having a ((3,5-dimethylbenzoyl)- L-prolyl)piperazine side chain at position C2, was found to be active as an antiproliferative agent (IC50 = 0.38 ± 0.34 to 3.17 ± 0.10 µM) and to be twice as active as RM-581 on LNCaP, PC-3, MCF-7, PANC-1 and OVCAR-3 cancer cells (IC50 = 0.56 ± 0.30, 0.89 ± 0.63, 1.36 ± 0.31, 2.47 ± 0.91 and 3.17 ± 0.10 µM, respectively). Conclusion: Easily synthesized in good yields by both solid-phase organic synthesis and classic solution-phase chemistry, promising compound 23 could be used as an antiproliferative agent on a variety of cancers, notably pancreatic and ovarian cancers, both having very bad prognoses.

scholarly journals Synthesis and Cytotoxic Evaluation of Novel Ester Derivatives of Betulin with AZT, d4T, and 3TC

2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200
Author(s):  
Dang Thi Tuyet Anh ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Dinh Thi Cuc ◽  
Nguyen Ha Thanh ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Antitumor Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Derivatives Of

Novel ester derivatives of betulin with AZT, d4T, and 3TC were synthesized and assessed for antitumor activities against the KB and HepG2 human cancer cell lines in vitro by MTT assay. Some derivatives displayed high anticancer properties, with IC50 values between 1 and 21 μM on the two cancer cell lines.

scholarly journals CELLector: Genomics Guided Selection of Cancer in vitro Models

2018 ◽  
Author(s):  
Hanna Najgebauer ◽  
Mi Yang ◽  
Hayley E Francies ◽  
Clare Pacini ◽  
Euan A Stronach ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
R Package ◽  
Cancer Cell Lines ◽  
In Vitro Models ◽  
Computational Method ◽  
R Shiny ◽  
Selection Of

The selection of appropriate cancer models is a key prerequisite for maximising translational potential and clinical relevance of in vitro oncology studies. We developed CELLector: a computational method (implemented in an open source R Shiny application and R package) allowing researchers to select the most relevant cancer cell lines in a patient-genomic guided fashion. CELLector leverages tumour genomics data to identify recurrent sub-types with associated genomic signatures. It then evaluates these signatures in cancer cell lines to rank them and prioritise their selection. This enables users to choose appropriate models for inclusion/exclusion in retrospective analyses and future studies. Moreover, this allows bridging data from cancer cell line screens to precisely defined sub-cohorts of primary tumours. Here, we demonstrate usefulness and applicability of our method through example use cases, showing how it can be used to prioritise the development of new in vitro models and to effectively unveil patient-derived multivariate prognostic and therapeutic markers.

scholarly journals Design, Synthesis and Anticancer activity of novel Triazole substituted Quinazoline Hybrids

2020 ◽  
Vol 11 (3) ◽  
pp. 3569-3579
Author(s):  
Paduri Karunakar ◽  
Swetha Gujjewar ◽  
Somesh Sharma ◽  
Srinivasu Pothukanuri ◽  
Krubakaran Muthusamy ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Liver Carcinoma ◽  
Synthetic Approach

Quinazolines and 1,2,4-triazoles are important class of nitrogen containing heterocyclic compounds having immense biological importance. From the literature review, pharmacokinetic properties of a drug can be modified or enhanced by building a triazole moiety into a compound like quinazoline. Therefore, the study of new hybrid systems which combines triazole system with quinazoline is still seemed warranted. In the present study, a sequence of novel 1,2,4-triazole derivatives containing quinazolinyl moiety were designed, synthesized and screened for their in vitro anticancer activity. Thirteen new hybrids are synthesized from readily accessible 5-bromoanthranilic acid. All the hybrid compounds were well explicated by IR, 1H, 13C NMR, and mass spectral data. Out of 13, some of the compounds manifested moderate to good antiproliferative activity against two cancer cell lines (HepG2 and MCF7). Remarkably, compounds 8A, 16H and 16K displayed potent activity (14- 49 µM) on both HepG2 (liver carcinoma) and MCF-7 (breast cancer) cell lines whereas compounds 8B, 8F, 16L, and 15 displayed substantial activity against HepG2 cancer cell line (34-65 µM). Synthetic approach described here is very simple and can be used for the syntheses of related compounds library which is useful for the exploration of further biological activities and is currently underway in our laboratory

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