Method for Obtaining Daedaleopsis confragosa K-1326 Extracts with Antitumor Activity

A method for extraction and fractionation of proteins and polysaccharides from the biomass of the basidial fungus Daedaleopsis confragosa K-1326, having antitumor activity, shown on the epidermoid carcinoma cell line A431 and the cells of melanoma В16, has been developed. This method allows for reproducible production of series of preparations and can be used to obtain preparations from other basidiomycetes. The results obtained in this work show the promising prospects for the development and use of drugs from basidiomycetes for treatment of cancer. Basidiomycetes, Daedaleopsis confragosa, antitumor activity, fractionation, extraction The work was performed under the State Assignment «Development of preventive and therapeutic drugs based on basidiomycetes for the prevention and treatment of influenza with pandemic potential».

UV Light Stimulated Activation of Camkii in Human Epidermoid Carcinoma A431 Cells

Summary The Ca2+/calmodulin dependent kinase II (CaMKII) represents a family of serine/threonine kinases with diverse functions, implicated in various signalling pathways in the cell, especially in those controlling cellular proliferation and cellular death. The human epidermoid carcinoma cell line A431 is an established model for the study of the cell cycle and cancer-associated signalling, in which the role of CaMKII is not so well elucidated. Therefore, the present study aimed to investigate the role of CaMKII in the induction of apoptosis in the cell line A431 following ultraviolet (UV) irradiation and to determine the downstream events with a focus on the caspase cascade. For the latter purpose, we employed a method initially developed for the simultaneous determination of the activity of 10 different caspase enzymes. Following exposure to UV light, we observed activation of the activator caspase-8 followed by activation of the effector caspase-3, triggering apoptosis in the epidermoid carcinoma cell line A431. The results supported a pivotal role of caspases and demonstrated that a protein kinase cascade involving caspases-8 and -3 is the main pathway driven in UV-induced apoptosis in the human carcinoma cell line A431, and apoptotic stimuli triggering this pathway passed through activation of the kinase CaMKII.

Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR

A series of novel quinazoline glycoside derivatives were designed, synthesized, and evaluated for their inhibition activities against EGFR-WT, EGFR/L858R/T790M, and skin epidermoid carcinoma cell line (A431).

Antiviral Furanosesquiterpenes from Commiphora erythraea

The crude methanolic extract obtained from C. erythraea resin was chromatographed on silica gel with solvent of increasing polarity. The extract and fractions were evaluated for cytotoxicity and antiviral activity [parainfluenza type 3 virus (PIV3)] by plaque forming units (PFU) reduction assay using HEp-2 cells (human larynx epidermoid carcinoma cell line). From the active fraction, five compounds were isolated and tested. Only two of these showed anti-PIV3 activity with a selectivity index (SI) of 66.6 and 17.5, respectively. Both the compounds are furanosesquiterpenoids.