Design, synthesis and pharmacological evaluation of novel Artemisinin-Thymol

Abstract

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.

Computational and experimental insights on the interaction of artemisinin, dihydroartemisinin and chloroquine with SARS-CoV-2 spike protein receptor-binding domain (RBD)

“…Nevertheless, it can block the binding of SARS-CoV-2 to ACE2 in vitro (Wang et al 2020). On similar basis, other antimalarial agents such as artemisinins demonstrated in vitro inhibition of SARS-CoV-2 (Krishna et al 2021;Kavak et al 2021). Extracts from the sweet woodworm Artemisia annua have been used for centuries in Chinese traditional medicine for treating the symptoms of febrile diseases, tidal fever and summer heat stroke (Brown 2010).…”

Advances of antitumor drug discovery in traditional Chinese medicine and natural active products by using multi‐active components combination

“…To splice thymol and artemisinin to synthesize a new artemisinin thymol conjugate and tested the cytotoxic activity of the compound on different cancer cell lines in vitro (Figure 2). The results showed that the new compound had inhibitory effects on HepG2 cells, LNCaP cells, Caco‐2 cells, HeLa cells, and HEK293 cells, especially on human colorectal adenocarcinoma Caco‐2 22 . Dihydroartemisinin (DHA) is obtained by reducing artemisinin with sodium borohydride.…”

Anticancer and apoptotic effects of a polysaccharide extract isolated from Lactarius chrysorrheus Fr. in HepG2 and PANC-1 cell lines

“…The relative gene expression levels were normalized to glyceraldehyde 3-phosphate dehydrogenase (GAPDH). For the determination of mRNA levels, the 2 −ΔΔCt method was used as described previously [26]. Primer sequences for all genes were acquired from the NCBI database (Supplementary Table S1) and were synthesized by Sentebiolab (Sentegen, Turkey).…”