BODIPY-peptide conjugate: Synthesis, photo-physical and cell viability studies

The synthesis and biological studies of BODIPY-GPR peptide conjugate (BD-2) are reported. As compared to the parent BODIPY (BD-1), the peptide linked BD-2showed blue shifted absorption and emission with excellent Stokes shift of 201 nm. Molecular docking studies on EGFR protein kinase indicated very efficient binding affinity of BD-2 as compared to the standard drug (Erlotinib). The cell viability experiments of BD-2on normal (HEK293T) and lung cancer (A549) cell lines indicated 85–95% viability. Bioimaging studies showed that, BD-2was able to penetrate the lung cancer cell line.

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Synthesis and in vitro Evaluation of Dihydrobenzimidazole Thiopyranooxazinone Derivatives as a Potent Biological Agents

Asian Journal of Organic & Medicinal Chemistry ◽

10.14233/ajomc.2020.ajomc-p251 ◽

2020 ◽

Vol 5 (2) ◽

pp. 164-170

Author(s):

Deepak P. Kardile ◽

Mrunal K. Shirsat

Keyword(s):

Lung Cancer ◽

Human Lung ◽

Cancer Cell Line ◽

Docking Studies ◽

Lung Cancer Cell Line ◽

Human Lung Cancer ◽

Lung Cancer Cell ◽

Anticancer Activities ◽

In Silico Molecular Docking

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.

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Cytotoxicity effect of ethanolic extract of Mikania glomerata against A549 human lung cancer cell line

International Journal of Advances in Scientific Research ◽

10.7439/ijasr.v2i7.3512 ◽

2016 ◽

Vol 2 (7) ◽

pp. 139 ◽

Cited By ~ 2

Author(s):

S. Sarojini ◽

V. Ramesh ◽

P. Senthilkumaar

Keyword(s):

Lung Cancer ◽

Cell Viability ◽

Cell Line ◽

Cancer Cell ◽

Human Lung ◽

Cancer Cell Line ◽

Lung Cancer Cell Line ◽

Human Lung Cancer ◽

Lung Cancer Cell ◽

Mikania Glomerata

The genus Mikania is the largest of its kind in the family Eupatorieae (Asteraceae), with more than 430 species concentrated mainly in the tropical regions, among which, Mikania glomerata is a most common herb generally employed in the treatment of respiratory disorders. The Milania glomerata plant leaf extracts were used for anticancer study against A549 human lung cancer cell line. The solid liquid extraction method has been employed to prepare the ethanol extract of Mikania glomerata through soxhelt apparatus method. To check the anti-proliferative effect of this extract, the extract chosen was tested for cell viability on the lung cancer cells A549 in different concentrations. Cell viability was evaluated by MTT assay for 24 hour and 48 hours. The LD50 value was calculated for the level of cell death and its effectiveness. The dose-dependent manner plays an important role in the treatment of lung cancer cell lines. The present study suggests that Mikania glomerata may be used as an alternative anticancer agent and further research is needed to improve the effectiveness.

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