Kāpae

Ua hoʻokomo ʻia ʻo Thalidomide ma ke ʻano he lāʻau sedative, immunomodulatory agent a ua noiʻi ʻia no ka mālama ʻana i nā hōʻailona o nā maʻi maʻi he nui.，ʻo ia kahi paʻakikī CRBN-DDB1-Cul4A.

wehewehe

Hoʻolaha mua ʻia ʻo Thalidomide ma ke ʻano he sedative, inhibits cereblon (CRBN), kahi ʻāpana o ka cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, me kahi Kd o∼250 nM, a he immunomodulatory, anti-inflammatory a me anti-angiogenic maʻi 'aʻai waiwai.

In Vitro

Hoʻolaha mua ʻia ʻo Thalidomide ma ke ʻano he sedative, he immunomodulatory, anti-inflammatory a me anti-angiogenic cancer properties, a me nā pahuhopu cereblon (CRBN), kahi ʻāpana o ka cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, me kahi Kd o∼250 nM[1]. Thalidomide (50μg / mL) hoʻoikaika i ka hana anti-tumor o ka icotinib e kū'ē i ka hoʻonuiʻana o nā pūnaewele PC9 a me A549, a ua pili kēia hopena me ka apoptosis a me ka neʻeʻana o nā pūnaewele. Eia kekahi, ʻo Thalidomide a me icotinib ke kāohi i nā ala EGFR a me VEGF-R2 i nā pūnaewele PC9 [3].

ʻO Thalidomide (100 mg/kg, po) kaohi i ka waiho ʻana o ka collagen, hoʻoponopono i ka pae hōʻike mRNA oα-SMA a me ka collagen I, a hoʻemi nui i nā cytokines pro-inflammatory i nā ʻiole RILF. Hoʻopau ʻo Thalidomide i ka RILF ma o ka hoʻopau ʻana i ka ROS a me ka hoʻoponopono iho o TGF-β/ Smad ala e pili ana i ke kūlana Nrf2 [2]. ʻO Thalidomide (200 mg / kg, po) i hui pū ʻia me ka icotinib e hōʻike ana i nā hopena anti-tumor synergistic i nā ʻiole nude e lawe ana i nā cell PC9, ke kāohi nei i ka ulu ʻana o ka maʻi tumora a me ka hoʻolaha ʻana i ka make maʻi tumor [3].