生物活性 | |||
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描述 | Balsalazide disodium (BSZ) is a colon-specific prodrug of the salicylate, 5-aminosalicylic acid[3]. It has a variety of biological activities including promoting apoptosis, anti‐inflammatory, and anti‐tumor effects[4]. ¬¬¬A preliminary mechanistic study in cultured human colon cancer cells showed that BSZ inhibited colon cancer cell proliferation in vitro[3]. In the murine azoxymethane (AOM)/dextran sodium sulfate (DSS) model, the number of F4/80-positive macrophages was significantly lower in the BSZ-treated groups compared with the CAC (colitis-associated carcinogenesis) group (P < 0.05). At the endpoint, the total numbers of tumors in the BSZ-treated groups were significantly low compared with the CAC group (P < 0.05), and the BSZ-treated groups had significantly lower F4/80-positive macrophages in the tumor stroma (P < 0.01). The protein production of macrophage inflammatory protein 1β, monocyte chemoattractant protein-1, interleukin (IL)-6, and IL-10 in the colon tissues decreased in concordance with the plasma concentrations of the cytokines (P < 0.05). The BSZ-treated groups revealed lower expression of p-STAT3 compared with the CAC group. These results revealed that BSZ have chemopreventive effects against CAC through IL-6/STAT3 suppression[4]. BSZ treatment of AOM-injected rats reduced ACF (aberrant crypt foci) formation in a dose-dependent manner by 60% with the greatest effect observed on ACF with 4 or more crypts. In B6-Min/+ mice, a dose-dependent reduction of intestinal tumor number was observed which reached 80% in the distal small intestine and colon[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.43mL 2.29mL 1.14mL |
22.87mL 4.57mL 2.29mL |
参考文献 |
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