Heteroleptic Pd(II) dithiocarbamates: synthesis, characterization, packing and in vitro anticancer activity against HeLa cell line

2015 ◽  
Vol 68 (14) ◽  
pp. 2539-2551 ◽  
Author(s):  
Shahan zeb Khan ◽  
Muhammad Kashif Amir ◽  
Muhammad Moazzam Naseer ◽  
Rashda Abbasi ◽  
Kehkashan Mazhar ◽  
...  
Author(s):  
Nevin Çankaya ◽  
Mehmetcan İzdal ◽  
Serap Yalçin Azarkan

Background: In recent years, discovery and development of new drugs play a critical role in cancer therapy. Objective: In this study, the effect of MPAEA and p-acetamide on cellular toxicity and on silico in HeLa cancer cells have been investigated. Methods: In this study, 2-choloro-N-(4-methoxyphenyl)acetamide (p-acetamide) and 2-(4-methoxyphenylamino)-2- oxoethyl acrylate (MPAEA) have been synthesized and characterized by FTIR, 1H, and 13C-NMR. Cytotoxicity of pacetamide and MPAEA have been investigated by XTT cell proliferation assay on the HeLa cell line. IC50 values of pacetamide and MPAEA have been identified on the HeLa cell line. Further, molecular docking study was carried out by Autodock Vina using BCL-2 (PDB ID: 4MAN), BCL-W (PDB ID: 2Y6W), MCl-1 (PDB ID: 5FDO) AKT (PDB ID: 4GV1) and BRAF (PDB ID: 5VAM) as a possible apoptotic target for anticancer activity. Results: According to the obtained results, MPAEA and p-acetamide were successfully synthesized and characterized. The interactions between ligands and anti-apoptotic proteins were evaluated by molecular docking and their free energy of binding were calculated and used as descriptor. Conclusion: In vitro and in silico the results demonstrated that MPAEA had potent anticancer activity on HeLa cell line.


2019 ◽  
Vol 6 (1) ◽  
pp. 30-32
Author(s):  
Poonkodi K ◽  
Mini R ◽  
Vimaladevi K ◽  
Prabhu V ◽  
Anusuya M ◽  
...  

The present investigation is carried out to study the invitro cytotoxicity of ethanol extract of Syzygium samarangense leaves on HeLa cell line by using MTT assay. Ethanol extract of S. samarangense showed concentration dependent activity on HeLa cell line with IC50 value of 40.5 μg/ml which shows that ethanol extract of S. samarangense posses significant cytoxicity.Moreover the preliminary phytochemical screening showed the presence of fatty acids, alkaloids, flavonoids, terphenoids, saponins, tannins and steroids which are responsible for its cytotoxicity. There are only a few reports are available for cytotoxicity of ethanol extract of S. samarangense.


2020 ◽  
pp. 4-7
Author(s):  
M. R. Kamala Priya ◽  
Priya R. Iyer

Doxorubicin is the most common chemotherapy drug used in cancer therapy. Its usage is associated with various side-effects. In order to overcome the challenges in Doxorubicin administration, the present study has focussed on synthesizing a drug conjugate with biosynthesized gold nanoparticles and doxorubicin. The gold nanoparticles were biosynthesized using green extracts of medicinal plants with potential anticancer activities. The nanoparticle that possesses anticancer activity was conjugated with the drug for a combinatorial effect of the nanoparticles and the drug. The in vitro cytotoxicity was checked in Vero cell line through MTT assay. The in vitro anti proliferative effects were screened against cervical cancer in HeLa cell line. Fluorescence activated cell sorting analysis was carried out to detect the difference between live and dead cell populations. The preliminary confirmation was carried out in UV-VIS spectrophotometer. The morphological characterization was carried out by SEM and stability by Zeta potential. The IC50 of the nanocompounds demonstrated anti-proliferative activity against cervical cancer similar to the chemotherapeutic drug, Doxorubicin; additionally in a much lesser concentration of the drug. The in vitro cytotoxicity exhibited high viability of cells in Vero cell line with minimum viability of 80% in all the tested concentrations. There was a synergistic effect of the nanoparticles along with the drug; thereby an enhanced therapeutic efficiency was achieved. FACS analysis showed 36% of cell death in Dox treated HeLa cells whereas 96% of cell death in Nano-Dox treated HeLa cells. Nano-Dox conjugate has demonstrated high anticancer effects than drug alone Doxorubicin. Further biosynthesized nanomaterials based drug formulation can be developed as a potential strategy in cancer therapy.


2019 ◽  
Vol 99 (8) ◽  
pp. 4167-4173 ◽  
Author(s):  
Edwin E Martínez‐Leo ◽  
Armando M Martín‐Ortega ◽  
Juan J Acevedo‐Fernández ◽  
Rosa Moo‐Puc ◽  
Maira R Segura‐Campos

2020 ◽  
Vol 47 (8) ◽  
pp. 6135-6142
Author(s):  
Jalal Hassanshahi ◽  
Afsaneh Mirzahosseini-pourranjbar ◽  
Zahra Hajializadeh ◽  
Ayat Kaeidi

Background: Cancer is still one of the most serious problems that affect human health. Despite the intense efforts to develop treatments, effective agents are still not available. In some cases, conventional therapy could be harmful or fail because of emerging drug resistance. Therefore, the development of novel therapies against cancer is of utmost importance. Assessment of anticancer effects of bacterial metabolites on cancer cells may help in the process of finding new cheap, reliable, contentious and safe cancer therapy. Objective: To determine the anticancer effect of the extracellular metabolites of eight bacterial species on HeLa cell line. Methodology: Extracellular metabolites were prepared by isolating and culturing eight bacterial species (Escherichia coli, Staphylococcus aureus, Micrococcus, Pseudomonas aeruginosa, Lactic acid bacteria, Klebsiella, Proteus and E. coli with its phage) in liquid media. Tubes were incubated overnight and centrifuged. Supernatant was filtered and concentrated using Infra-Red concentrator. Different concentrations were prepared and their anticancer effect were evaluated using MTT cell proliferation assay. Results: Results showed variation among the eight bacteria concerning proliferation inhibition against HeLa cells in a time and concentration dependent manner. Pseudomonas and E. coli with its phage revealed considerable anticancer activity with 63% and 86% inhibitory effects (both at 1000 µg\ml) and IC50 of 301 and 1395 µg/dl at 24h respectively. While Proteus and Micrococcus showed low inhibitory effects and S. aureus enhanced the proliferation of HeLa cells at low concentrations. Conclusion: Among the tested bacteria, Pseudomonas and E. coli and its phage gave the best anticancer inhibitory effects against HeLa cells. Further studies using purified components of effective bacteria are recommended.


2019 ◽  
Vol 44 (1-2) ◽  
pp. 42-49
Author(s):  
Tiantian Guo ◽  
Yiming Song ◽  
Yinghui Lu ◽  
Guolin Li ◽  
Tian Liu ◽  
...  

The first synthesis of a natural triterpenoid saponin bearing N-acetylglucosamine, albidoside A, which is isolated from the roots of Acacia albida, is concisely achieved in a convergent strategy. Preliminary pharmacological research shows anticancer activity against HL-60, MCF-7, MDA-MB-231, Hep-2, and Hela cell lines. In particular, it exhibited good selectivity, which is five times more cytotoxic toward Hep-2 cells (IC50 = 8.91 μM) than the Hela cell line.


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