Paclitaxel-octreotide conjugates inhibit growth of human non-small cell lung cancer cells / 中国肿瘤生物治疗杂志

ABSTRACT

Objective: To evaluate the cytotoxicity and targeting ability of self-developed paclitaxel-octreotide (PTX-OCT) conjugates on A549 non-small cell lung cancer (NSCLC) cells and Calu-6 NSCLC cells. Methods: Conjugates PTX-OCT and 2PTX-OCT were synthesized by our school. Reverse transcription-polymerase chain reaction was used to detect mRNA of human somatostatin receptor subtypes (SSTRs) using specific primers. The cells were treated with different concentrations (1, 100 nmol/L and 1 ?mol/L) of paclitaxel and the conjugates for different time periods (24-72 h); we also set up a control group. MTT assay was used to evaluate the cell viability after treatment; cell cycle perturbations were determined by FAC Scan flow cytometer 24 h after treatment with 1 ?mol/L paclitaxel, PTX-OCT, and 2PTX-OCT. Results: Both A549 cell and Calu-6 cell expressed the mRNA of SSTR2 and SSTR5; no SSTR mRNA was detected in the fibroblasts. The conjugates had a similar cytotoxicity to paclitaxel; they both effectively inhibited the growth of A549 cells and Calu-6 cells in a concentration-and time-dependent manner. After 72 h treatment with 1 ?mol/L paclitaxel, PTX-OCT and 2PTX-OCT, the survival rates of A549 cells were (26.9?7.3)%, (26.6?9.2)% and (35.7?4.3)%, respectively; the survival rates of Calu-6 cells were (29.5?5.0)%, (28.2?9.7)% and (26.5?4.9)%, respectively. The survival rate A549 cells at 72 h after treatment was lower than that at 24 h after treatment(P