Papamuri

I whakauruhia a Thalidomide hei rongoa whakamarumaru, he kaihoko immunomodulatory me te tirotirohia mo te rongoa i nga tohu o nga mate pukupuku maha. Ka aukati a Thalidomide i te E3 ubiquitin ligase，he matatini CRBN-DDB1-Cul4A.

Whakaahuatanga

Ko te Thalidomide i te tuatahi ka whakatairangahia hei whakamarumaru, ka aukati i te cereblon (CRBN), he waahanga o te cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, me te Kd o∼250 nM, a he immunomodulatory, anti-inflammatory me te mate pukupuku anti-angiogenic.

In Vitro

Ko te Thalidomide i te tuatahi ka whakatairangahia hei whakamarumaru, he immunomodulatory, anti-inflammatory me te anti-angiogenic mate pukupuku, me te whai i te cereblon (CRBN), he waahanga o te cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, me te Kd o∼250 nM[1].Thalidomide (50μg/mL) e whakakaha ana i te mahi anti-tumor o te icotinib ki te whakararu o te PC9 me te A549 pūtau e rua, a ka honoa tenei paanga ki te apoptosis me te heke o te pūtau.I tua atu, ka whakakorehia e Thalidomide me te icotinib nga huarahi EGFR me VEGF-R2 i roto i nga kamera PC9 [3].

Ko te Thalidomide (100 mg/kg, po) ka aukati i te whakaheke o te collagen, ka whakaheke i te taumata whakaputanga mRNA oα-SMA me te collagen I, me te tino whakaiti i nga cytokines pro-inflammatory i roto i nga kiore RILF.Ka whakaitihia e Thalidomide te RILF ma te whakakore i te ROS me te whakaheke i te ture o TGF-βKo te ara Smad e whakawhirinaki ana ki te mana Nrf2[2].Ko te Thalidomide (200 mg / kg, po) me te icotinib e whakaatu ana i nga paanga anti-tumor synergistic i roto i nga kiore tahanga e mau ana i nga kamera PC9, te whakakore i te tipu o te pukupuku me te whakatairanga i te mate pukupuku[3].