Bergapten

具有多种生物活性的呋喃香豆素衍生物；以浓度依赖性方式降低DLD-1和LoVo结肠直肠癌细胞的活力，将细胞周期停止在G0/G1和亚G1期，并在50μM时诱导细胞凋亡；具有光敏活性；增加豚鼠皮肤在UVA辐射下的晒伤细胞数量；在10mg/kg剂量下，在长春新碱诱发的神经性疼痛大鼠模型中，增加机械、冷和热异常性疼痛以及机械性痛觉过敏测定中的痛阈值；抑制长春新碱诱发的大鼠血浆TNF-α和IL-1β水平升高以及脊髓和坐骨神经中GSH水平降低；抑制人肝微粒体中的CYP3A4（IC50=~25μM）。A furanocoumarin derivative with diverse biological activities; decreases the viability of DLD-1 and LoVo colorectal cancer cells in a concentration-dependent manner, halts the cell cycle at the G0/G1 and sub-G1 phases, and induces apoptosis at 50 μM; has photosensitizing activity; increases the number of sunburn cells in guinea pig skin in response to UVA radiation; increases the pain threshold in assays for mechanical, cold, and hot allodynia, as well as mechanical hyperalgesia, in a rat model of vincristine-induced neuropathic pain at 10 mg/kg; inhibits vincristine-induced increases in plasma TNF-α and IL-1β levels and decreases in GSH levels in the spinal cord and sciatic nerve in rats; inhibits CYP3A4 (IC50 = ~25 μM) in human liver microsomes.