Functionalized Sulfur-Containing Heterocyclic Analogs Induce Sub-G1 Arrest and Apoptotic Cell Death of Laryngeal Carcinoma In Vitro

Abstract

In this study, we speculate that the hydroxyl-containing benzo[b]thiophene analogs, 1-(3-hydroxybenzo[b]thiophen-2-yl) ethanone (BP) and 1-(3-hydroxybenzo[b]thiophen-2-yl) propan-1-one hydrate (EP), might possess antiproliferative activity against cancer cells. Hydroxyl-containing BP and EP show selectivity towards laryngeal cancer cells (HEp2), with IC50 values of 27.02 ± 1.23 and 35.26 ± 2.15 µM, respectively. The hydroxyl group present in the third position is responsible for the anticancer activity and is completely abrogated when the hydroxyl group is masked. BP and EP enhance the antioxidant enzyme activity and reduce the ROS production, which are correlated with the antiproliferative effect in HEp-2 cells. An increase in the BAX/BCL-2 ratio occurs during the BP and EP treatment and activates the caspase cascade, resulting in apoptosis stimulation. It also arrests the cells in the Sub-G1 phase, indicating the induction of apoptosis. The molecular docking and simulation studies predicted a strong interaction between BP and the CYP1A2 protein, which could aid in combinational therapy by enhancing the bioavailability of the drugs. BP and EP possess an antioxidant property with low antiproliferative effects (~5.18 µg/mL and ~7.8 µg/mL) as a standalone drug, therefore, they can be combined with other drugs for effective chemotherapy that might trigger the effect of pro-oxidant drug on healthy cells.

Cell-free fat extract regulates oxidative stress and alleviates Th2-mediated inflammation in atopic dermatitis

“…As extracellular ROS can induce apoptosis (Zhang et al, 2015), the degree of apoptosis reflects ROS-induced cytotoxicity. The fluorescence results shown by the apoptosis kit observed a decrease in the number of green + cells after FE intervention (Figure 2E), and for more accurate quantification, flow cytometry analyzed the Sub-G1 peaks, which reflected the proportion of apoptotic cells (Haridevamuthu et al, 2023). The results showed that L-, H-and M-FE all reduced apoptosis caused by high ROS (Figure 2F).…”

From Plants to Wound Dressing and Transdermal Delivery of Bioactive Compounds

“…Sulfur-containing compounds can also be isolated from plants, and used for their diverse biological activities, such as anti-inflammatory, antioxidant, and anticancer activities [ 202 , 203 , 204 , 205 , 206 , 207 , 208 ].…”