Research Information System
CHEMISTRYSELECT, vol.10, no.28, 2025 (SCI-Expanded)
Natural products are essential sources for the discovery and development of new anticancer drugs due to their biological activities and minimal side effects. Artemisinin is the best natural product with anti-malarial agent, and it has a variety of biological activities. Moreover, benzothiophene is a heteroaromatic compound known for its diverse biological activities. In this study, the cytotoxic, apoptotic, and anti-inflammatory activities of benzothiophene-artemisinin hybrids (BTPART and BTFART) were investigated. The MTT assay confirmed that these hybrids exhibited dose-dependent cytotoxic effects on Caco-2, HepG2, LNCaP, MDA-MB-231, MCF-7, HeLa, and Ishikawa cell lines. These hybrids also significantly reduced colony formation and demonstrated antimetastatic properties in Caco-2, HepG2, LNCaP, and MDA-MB-231 cell lines. The apoptotic effects of the hybrids were analyzed by using flow cytometry and qPCR by evaluating apoptosis-related genes (Bcl-2, Bax, Casp-3, Casp-8, Casp-9, and P53). The results indicated that both hybrids effectively induced apoptosis. In addition, both molecules display anti-inflammatory properties by reducing nitric oxide (NO) production and suppressing key inflammatory markers, including COX2, iNOS, IL-6, and TNF-alpha, while increasing IL-10 expression. As a result, benzothiophene-artemisinin hybrids have potential as therapeutic candidates for cancer treatment, particularly in liver and prostate cancers, and may also be beneficial in managing inflammatory diseases.