Oxiconazole (Ro 13-8996) 是一种广谱抗真菌剂,能抑制念珠菌 (Candida)、曲霉属真菌 (Aspergillus) 和毛癣菌属真菌 (Trichophyton) 的生长。Oxiconazole 也是一种高效的CYP3A4反式激活剂,可与利福平 (Rifampicin; HY-B0272) 竞争性拮抗。Oxiconazole 通过过氧化物酶 2 (PRDX2) 介导的细胞自噬 (autophagy) 停滞来发挥抗结直肠癌的作用。
生物活性 | Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungalagent which can inhibit the growth ofCandida,AspergillusandTrichophyton. Oxiconazole is also a highly efficacious activator ofCYP3A4transactivation, which could be antagonized byRifampicin(HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectalcancer(CRC) via peroxiredoxin-2 (PRDX2)-mediatedautophagyarrest[1][2][3]. |
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体外研究 (In Vitro) | Oxiconazole (24 h; 0-40 μM) inhibits CRC cell growth[3]. Oxiconazole has antifungal activity againstCandida,AspergillusandTrichophyton[1]. Antifungal Activities of Oxiconazole[1].
| Candidaalbicans | Candidaglabrata | Candidaparapsilosis | Aspergillusfumigatus | Aspergillusflavus | Trichophytonmentagrophytes | Trichophytonrubrum | Oxiconazole | 0.03 μg/mL | 0.01 μg/mL | 0.008 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL |
Cell Proliferation Assay[3] Cell Line: | HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 | Concentration: | 0-40 μM | Incubation Time: | 24 h | Result: | Exhibited inhibitory activity against HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 with IC50s of 25.86 μM, 27.34 μM, 21.01 μM, 25.56 μM, 21.75 μM, 24.87 μM and 126.4 μM. |
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体内研究 (In Vivo) | Oxiconazole (50 mg/kg/day; IP; for 12 days) significantly restrains CRC cell growth[3].
Animal Model: | BALB/c nude mice (injected subcutaneously with HCT116 cells (1×107/mouse)[3] | Dosage: | 50 mg/kg/day | Administration: | IP; for 12 days | Result: | Significantly restrained CRC cell growth and showed no obvious side effects. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |