Synthesis, Characterization and Biological Evaluation of Novel Triazolyl - Acridine Derivatives as Cytotoxic Agents

Author(s):  
Mandeep Singh ◽  
D. N Prasad ◽  
Supriya Agnihotri

Acridine and Triazols both are biologically active heterocyclic rings with cytotoxic potential. Triazolyl- acridine adduct attract the attention in the field of medicinal chemistry. Here we synthesized a series of triazolyl- acridine compounds by the appropriate procedures. Structure of all synthesized compounds was confirmed by the various spectroscopic methods e.g. FT-IR, proton NMR and Mass spectrograms. All synthesized triazolyl-acirdines compounds were assayed in-vitro for cytotoxic activity against MCF-7 (human breast adenocarcinoma cell line) and HT-29 (human colon adenocarcinoma cell line) cells by MTT- assay. All target compounds shows increasing activity in dose dependent manner. However MPSP-9 was sensitive against MCF-7 but compound MPSP-1 was most sensitive with minimum inhibitory concentration (IC50 value) against MCF-7 and HT-29 both cell lines.

2011 ◽  
Vol 43 (08) ◽  
pp. 519-523 ◽  
Author(s):  
J.-A. Teng ◽  
R.-L. Hou ◽  
D.-L. Li ◽  
R.-P. Yang ◽  
J. Qin

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2262 ◽  
Author(s):  
Ewa Kochan ◽  
Adriana Nowak ◽  
Małgorzata Zakłos-Szyda ◽  
Daria Szczuka ◽  
Grażyna Szymańska ◽  
...  

American ginseng, Panax quinquefolium (L.), is traditionally used in folk medicine. It exhibits a range of anti-inflammatory, hepatoprotective, anti-diabetic, anti-obesity, anti-hyperlipidemic and anti-carcinogenic effects. Its main components are ginsenosides, also known as panaxosides or triterpene saponins. In order to obtain high yields of ginsenosides, different methods of controlled production are involved, i.e., with hairy root cultures. However, they are still employed under in vitro conditions. Our studies revealed that hairy root cultures subjected to an elicitation process can be considered as a potent source of ginsenosides. The present study examines the biological activity of ginseng hairy root cultures against the Caco-2 human adenocarcinoma cell line. Among our six different clones of P. quinquefolium hairy roots, extracts B and Be (treated with elicitor) were the strongest inhibitors of the cellular metabolic activity. While all extracts induced DNA damage, B and Be also generated reactive oxygen species (ROS) in a concentration-dependent manner, which was correlated with the depletion of the mitochondrial membrane potential and induction of apoptosis. These findings indicate that further research concerning P. quinquefolium hairy root cultures should focus on the activity of rare ginsenosides and other biologically active compound profiles (i.e., phenolic compounds).


2002 ◽  
Vol 173 (1) ◽  
pp. 161-167 ◽  
Author(s):  
C Gil-Puig ◽  
M Blanco ◽  
T Garcia-Caballero ◽  
C Segura ◽  
R Perez-Fernandez

GH expression in mammary tumors has been related to the increase and spreading of cell proliferation. Using the MCF-7 human breast adenocarcinoma cell line, it has been demonstrated that autocrine GH-stimulated mammary carcinoma cell proliferation decreased the apoptosis rate and enhanced cell spreading. Surprisingly, no data are available about the presence of Pit-1 (the main pituitary regulator of GH) or GH expression in this cell line. Using RT-PCR, Western blot and immunohistochemistry, we have demonstrated the presence of both mRNA coding Pit-1 and GH as well as Pit-1 and GH protein in the MCF-7 cell line. These data could imply that Pit-1 may be an adequate target to inhibit breast cell proliferation.


2013 ◽  
Vol 68 (3-4) ◽  
pp. 108-112 ◽  
Author(s):  
Maryam Hamzeloo Moghadam ◽  
Farzaneh Naghibi ◽  
Azadeh Atoofi ◽  
Mitra Asgharian Rezaie ◽  
Mahboobeh Irani ◽  
...  

Cytotoxic activity of gaillardin, a sesquiterpene lactone isolated from Inula oculus-christi L. (Asteraceae), was assessed in the human breast adenocarcinoma cell line MCF-7, human hepatocellular carcinoma cell line HepG-2, human non-small cell lung carcinoma cell line A-549, and human colon adenocarcinoma cell line HT-29, resulting in IC50 values of 6.37, 6.20, 4.76, and 1.81 μg/mL, respectively, in the microculture tetrazolium-formazan MTT assay. In vitro apoptosis-inducing properties of gaillardin were also evaluated in MCF-7 cells with the terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nickend labeling (TUNEL) assay. The results suggest gaillardin as a candidate for further studies in cancer therapy


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