Paclitaxel-octreotide conjugates inhibit growth of human non-small cell lung cancer cells in vitro.

AIM:To evaluate the effects of paclitaxel-octreotide conjugates on the growth of cultured non-small cell lung cancer cells. METHODS:RT-PCR was performed to detect mRNA for the subtypes of the human somatostatin receptor (SSTR) using specific primers. MTT-based cytotoxicity assay was used to evaluate the cell viability after treatment with paclitaxel and the conjugates. Cell cycle perturbations were determined using a Fluorescence-Activated Cell Sorter. RESULTS:Non-small cell lung cancer A549 and Calu-6 cells expressed mRNA for SSTR2 and SSTR5. Paclitaxel and the conjugates effectively inhibited the growth of A549 and Calu-6 cells in a concentration- and time-dependent manner. In SSTR-negative fibroblasts, the conjugates were less cytotoxic than paclitaxel. The conjugates and paclitaxel could induce the increase of G(2)/M phase ratio in A549 cells. CONCLUSION:The paclitaxel-octreotide conjugates can be used as selective-targeted chemotherapeutic agents for treating non-small cell lung cancer.