Rational combinations of indirubin and arylidene derivatives exhibit synergism in human non‐small cell lung carcinoma cells

Abstract

Rational combination of natural and synthetic derivatives to treat lung cancer has advantages of both efficacy and safety. Herein, the combination of indirubin‐3‐monoxime (I3M), a chemical derived from Chinese herbal medicine and FXY‐1, a synthetic arylidene derivative, was tested for combined activity in lung cancer cells. A dose‐dependent synergistic reduction in cell viability was recorded with the combinations in A549 and NCI‐H460 cells. Combination treatments of I3M and FXY‐1 showed antimetastatic effects in both cells. Cell cycle analysis revealed G1 growth phase reduction with subsequent accumulation of sub G0 contents. Annexin V assay revealed higher apoptotic cells with combinations compared to individual treatments. I3M + FXY‐1 combination significantly decreased the antiapoptotic Bcl‐2 protein and increased pro‐apoptotic Bax protein levels. These results demonstrate efficacy of I3M + FXY‐1 in lung cancer cells and suggest further preclinical research in animal models to develop it into a new form combination chemotherapeutic against lung cancer. Practical applications Current investigation will open new options in rational combinations of natural and synthetic compounds to treat cancer. The observed efficacy and safety of the combinations will add to the advantage of higher therapeutic window in formulating treatment regimens. The antimetastatic effects by the combinations provides promising efficacy in controlling the lung cancer progression. A detailed in vivo investigation is recommended to transform the combinations to novel chemotherapeutic options against lung cancer.

A Combined Chemical, Computational, and In Vitro Approach Identifies SBL-105 as Novel DHODH Inhibitor in Acute Myeloid Leukemia Cells

“…Cell proliferations were assessed using MTT assay as described elsewhere 16 . AML cells (5 × 10 3 cells/well) were grown in a 96-well tissue culture plate in regular growth medium.…”

Anticancer efficacy of 3-(4-isopropyl) benzylidene-8-ethoxy, 6-methyl, chroman-4-one (SBL-060), a novel, dual, estrogen receptor-Akt kinase inhibitor in acute myeloid leukemia cells

“…ELISA was performed according to the manufacturer's instructions. Cell proliferation was assessed using the MTT assay, as described previously [8]. Briefly, THP-1 and HL-60 cells at a concentration of 5 × 10 3 cells/well were grown in 96-well tissue culture plates in regular growth medium.…”

“…Therefore, targeting ERs in AML cells could afford a reasonable target to combat disease progression. Tumor progression and hence is regarded as a valid target to control rapidly proliferating cancer cells [8]. Although AML is not directly linked to sex hormones, the relationship between estrogen, ERs, and AML has been documented [2].…”

Thymoquinone inhibits IL‐7‐induced tumor progression and metastatic invasion in prostate cancer cells by attenuating matrix metalloproteinase activity and Akt/NF‐κB signaling

“…This component has been documented for its therapeutic properties, such as antioxidant [9] and anti‐inflammatory [10]. It also effectuates against various forms of cancers, including colon [11], lung [12], kidney [10], and leukemia [13]. Some studies reported that Tq controls proliferating cancer cells through various signaling pathways, such as PIP3/Akt/NF‐κB [14], MAPK [15], and STAT‐3 [16].…”