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A molecular hybridization of natural products is a new concept in drug discovery and having critical roles to design new molecules with improved biological properties. Hybrid molecules display higher biological activities when compared to the parent drugs. Moreover, they create new biological properties. In the present study, two natural products (thymol and artemisinin (ART)) are used for the synthesis of new hybrid thymol-artemisinin molecule. After characterization, the cytotoxic activity of ART-thymol is tested against different cancer cell lines and non-cancerous human cell lines. ART-Thymol show the cytotoxic effect with EC 50 values 70,96μM for HepG2, 97,31μM for LnCap, 6,03μM for Caco-2, 77,98μM for HeLa and 62,28μM for HEK293 cells, respectively. Moreover, ART-Thymol was checked for druglikeness, and the kinase inhibitory activity of ART-Thymol is investigated by using molecular docking in the present study. These results improved that thymol-artemisinin may be new candidates as an anticancer agents.

Mushrooms are widely used in many cultures for nutritional and health benefits. The Lactarius species is found in the Aegean region of Turkey. Lactarius chrysorrheus Fr. is a wild mushroom that contains a milky juice. In this study, we investigated the in vitro cytotoxic potential and apoptotic effect of the polysaccharide extract prepared from L. chrysorrheus by water extraction and alcohol precipitation using the tetrazolium MTT dye assay, annexin V staining, wound healing and colony formation, and qRT-PCR. The molecular weights of three peaks observed in HPLC chromatograms were calculated as 1869.9, 3043.92 and 16821.47 Da. The extract exhibited cytotoxic activity at 72 h, with an IC50 value of 296.42 ?g/mL in HepG2 and 444.43 ?g/mL in PANC-1 cells; the extract that was tested on the normal HEK293 cell line exhibited no cytotoxicity. Further, L. chrysorrheus upregulated the expression of CASPASE 3 and CASPASE 9 while downregulating B-cell lymphoma 2 (BCL-2) and B-cell lymphoma-extra large (Bcl-xL) genes, and inhibited cell migration and colony formation in HepG2 and PANC-1 cells. This study provides new insight into the use of the polysaccharide from L. chrysorrheus in the development of novel anticancer agents.

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Heteroaromatic indoles play a leading role in the development of pharmaceutical, medical, chemical and agricultural fields due to their structural properties. In this study, it was first time that biological properties of (antioxidant, antimicrobial, cytotoxic and apoptotis-induced anticancer) 3-(5-bromothiophen-2-yl)-1ethyl-2-phenyl-1H-indole 4 and 3-([2,2'-bithiophen]-5-yl)-1ethyl-2-phenyl-1H-indole 5 were described. According to the overall results, while 4 did not show any significant cytotoxic, antioxidant and antimicrobial activities, 5 showed high reduc-ing activity and very strong antibacterial activity against Enterococcus faecalis. Furthermore, 5 showed dose-dependent cytotoxic effect in all tested cell lines. The EC 50 values of the 5 were found to be 16 μM for CaCo-2, 29 μM for LnCaP, 14 μM for MDA-MB231, 21 μM for HepG2 and 87 μM for HEK293 cells, respectively. 5 also caused induction of apoptosis and promising glutathione S-transferase (GST) enzyme inhibition in HepG2 cells. Consequently, 5 could be also considered as a promising medical agent in cancer treatment.[a] Dr. M.