Abstract
Abstract
Objectives
Cancer is a leading global health issue with complex causes. Conventional treatments often face challenges like drug resistance and toxicity. Plant-derived compounds such as artemisinin have gained interest due to their diverse anticancer mechanisms, including ROS generation and apoptosis induction. In this study, the biological activities of ART-FB, a hybrid compound combining benzothiophene and artemisinin, were systematically investigated for the first time.
Methods
ART-FB’s cytotoxicity was tested on various human cancer cell lines (Caco-2, LNCaP, HeLa, A549) and HUVEC via MTT assay. Colony formation, scratch-wound, and Annexin V/PI assays were used to assess proliferation, migration, and apoptosis. Apoptotic gene expression was analyzed by qPCR. Anti-inflammatory effects were studied in LPS-stimulated RAW264.7 cells via Griess assay and qPCR.
Results
ART-FB showed selective cytotoxicity in Caco-2, LNCaP, HeLa, and A549 cancer cell lines, with lower toxicity in non-cancerous HUVEC cells. It effectively suppressed proliferation, colony formation, and migration, especially in LNCaP and A549 cells, suggesting potential anti-metastatic activity. Annexin V/PI staining and gene expression analysis confirmed that ART-FB induces apoptosis via both intrinsic and extrinsic pathways, with the strongest effects in LNCaP and Caco-2 cells. In LPS-stimulated RAW264.7 macrophages, ART-FB significantly reduced nitric oxide levels and downregulated
iNOS
,
COX-2
,
TNF-α
, and
IL-6
, while upregulating
IL-10
, suggesting dual anticancer and anti-inflammatory action.
Conclusions
ART-FB exhibits both anticancer and anti-inflammatory properties, targeting key pathways involved in tumor growth and immune response. These findings indicate that ART-FB is a promising candidate for further preclinical development as a multifunctional therapeutic agent.