Research on Reversal Effects in Cisplatin-resistant Human Lung Adenocarcinoma Cell Line A549/DDP by Standard Substances from Traditional Chinese Medicine / 世界科学技术-中医药现代化

Objective: To investigate the reversal effects in A549/DDP by standard substances (SS) from Traditional Chinese Medicine. Methods: Cell proliferation assays were performed to investigate the Resistant Index of A549/DDP and its tolerance to selected SS. The working concentrations of SS, IC5 calculated by nonlinear regressions, were applied as reversal doses to investigate the effects. Results: The resistant index of A549/DDP was 31.79. Tetramethylpyrazine and Matrine were well tolerated. Berberine hydrochloride, Dauricine, Oridomin exhibited dose-depend inhibitory effects on A549/DDP cell line. The working concentrations of them could effectively reverse the resistance of A549/DDP cell line to DDP. (P＜0.01) . Conclusion: The selected standard substances from Traditional Chinese Medicine were capable to reverse the resistance of A549/DDP cell line to DDP.

Interaction of mouse intestinal P-glycoprotein with oral antidiabetic drugs and its inhibitors.

Type 2 diabetes (T2DM) is a progressive insulin secretory defect accompanied by resistance to insulin, and thereby making glycemic control a major concern in the treatment of these patients. Oral drug administration, though a popular option for its non-invasiveness, suffer from poor bioavailability. It could be related to the efflux transport of intestinal P-glycoprotein (Pgp). In the present study, we explored the binding interactions of antidiabetic drugs i.e., sulfonylurea drugs (glimepiride, glipizide, glyburide) and rapid acting insulin secretagogues viz., nateglinide, repaglinide and rosiglitazone; and Pgp inhibitors i.e., Generation I (verapamil and tamoxifen), III (tetradrine and tariquidar), and natural inhibitors (fumagillin and piperine) in mouse Pgp model. Our results revealed that fumagillin piperine and verapamil possess maximum interaction energies with Pgp compared to antidiabetic drugs. These observations elucidate the role of fumagillin and piperine as potential natural compounds which could intervene in the efflux action of Pgp in extruding the antidiabetic drugs and may have implications for increasing efficacy of oral antidiabetic therapy.