Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3. Chloropyramine hydrochloride may be useful in the treatment of invasive breast cancer.
BT474 cells demonstrate a high sensitivity to Chloropyramine hydrochloride (compound 1), with a 1 µM concentration leading to a 40% reduction in cell viability after 48 hours. At the same 1 µM concentration, the viability of MCF7-pcDNA3 cells remains significantly higher compared to MCF7-VEGFR-3 cells (P<0.01), and at a 10 µM concentration, the viability difference doubles (P<0.001). Additionally, a concentration-dependent decrease in cell proliferation is observed in BT474 cells treated with Chloropyramine hydrochloride. A continued 48-hour treatment at higher doses leads to apoptosis in breast cancer cells overexpressing VEGFR-3, with a 10 µM dose inducing apoptosis in over 60% of these cells. In comparative treatments, MCF7-pcDNA3 and MCF7-VEGFR-3 cells treated with 10 µM Chloropyramine hydrochloride for 48 hours show a fourfold increase in apoptotic cell death in the VEGFR-3 overexpressed line (18% vs. 76% respectively)[1].
Chloropyramine HCl/氯吡胺盐酸盐 动物研究
Animal study
Chloropyramine hydrochloride significantly reduces tumor growth in both model systems, with tumor sizes in treated groups being about 20% of those in vehicle control groups. Doxorubicin, administered at 3 mg/kg, results in a 60% reduction in tumor growth, though it shows no effect at 0, 3 mg/kg doses. Conversely, Chloropyramine hydrochloride alone reduces tumor growth by 50%. A low-dose combination of Chloropyramine hydrochloride and doxorubicin prolongs the anti-tumor effect, achieving an 85% reduction in tumor growth, which surpasses the effect of either drug alone[1].
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