Non-P-glycoprotein mediated mechanism for multidrug resistance precedes P-glycoprotein expression during in vitro selection for doxorubicin resistance in a human lung cancer cell line

Lung Cancer ◽  
1991 ◽  
Vol 7 (3) ◽  
pp. 207-208
2020 ◽  
Vol 5 (2) ◽  
pp. 164-170
Author(s):  
Deepak P. Kardile ◽  
Mrunal K. Shirsat

In the present study, dihydrobenzimidazole thiopyranooxazinone derivatives were efficiently synthesized, which were further characterized and authenticated by means of TLC and different spectral analysis such as IR and 1H NMR. The synthesized compounds DPK2d2 to DPK2d8 were screened for their in vitro antimicrobial, antitubercular and anticancer activities. The results showed that the titled compounds DPK3d1, DPK3d2 and DPK3d4 exhibited potent antimicrobial activity, shows a broadspectrum activity against Bacillus subtilis, Escherichia coli (antibacterial) and Aspergillus niger (antifungal) as compared to ciprofloxacin and fluconazole, respectively. Compounds DPK3d1, DPK3d3 and DPK3d5 exhibited potent antitubercular activities against Mycobacterium tuberculosis as compared to pyrazinamide, ciprofloxacin and streptomycin. Compounds DPK3d3, DPK3d4 and DPK3d5 showed highly potent cytotoxic activity against human lung cancer cell line (A549) as compared to adriamycin. In silico molecular docking studies shown that all the ligands highest binding affinity range -6.7 to -8.7 for selected 1CB4 PDB of superoxide dismutase, which recognized that ligands having antioxidant activity.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 986
Author(s):  
Brigitta Kis ◽  
Ioana Zinuca Pavel ◽  
Daniela Haidu ◽  
Mariana Nela Ștefănuț ◽  
Zorița Diaconeasa ◽  
...  

Populus nigra L. is a plant from Salicaceae family, native in Europe. Many parts of this tree can be used as active ingredients, but the most valuable are the buds. In recent years, a growing number of studies reported their activity in the development of a wide range of pharmacological activities including diabetes, cardiovascular diseases, and cancer. The aim of this study was to determine the phytochemical composition and to evaluate the inorganic elements’ concentration as well as the in vitro antiproliferative and pro-apoptotic potential of a Populus nigra L. buds extract collected from Timișoara (Romania) against A549 human lung cancer cell line. Populus nigra L. bud extract was found to contain twelve different phenolic compounds. The inorganic elements concentrations were below the limit of detection for Co, Pb, and As, whereas Cu = 6.66 µg/g; Cr = 0.79 µg/g; Ni = 3.28 µg/g; Fe = 39.00 µg/g; Zn = 14.84 µg/g; Mn = 0.59 µg/g; Al = 2109.87 µg/g; and Cd = 0.019 µg/g. The extract was tested for the in vitro antiproliferative and pro-apoptotic potential on A549 human lung cancer cell line using different concentrations, namely 10, 25, 50, 75, 100, and 150 μg/mL. Results have shown that poplar bud extract induced a significant decrease of tumor cell viability in a dose-dependent manner with an IC50 = 72.49 μg/mL and blocked the cells in the G0/G1 phase of the cell cycle. Phenomena of early apoptosis (from 1.34 ± 0.33% control cells to 2.68 ± 0.62% at 150 µg/mL) and late apoptosis (from 1.43 ± 0.14% control cells to 5.15 ± 1.02% at 150 µg/mL) were detected by Annexin V-PI double staining. Poplar bud extract can be regarded as a promising candidate for future studies involving lung cancer.


3 Biotech ◽  
2021 ◽  
Vol 11 (6) ◽  
Author(s):  
Prateek Kumar ◽  
Anjali Chauhan ◽  
Munendra Kumar ◽  
Bijoy K. Kuanr ◽  
Aditi Kundu ◽  
...  

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