Mbiri

Thalidomide idayambitsidwa ngati mankhwala oziziritsa, immunomodulatory agent komanso amafufuzidwa pochiza zizindikiro za khansa zambiri. Thalidomide imalepheretsa E3 ubiquitin ligase,chomwe ndi chovuta cha CRBN-DDB1-Cul4A.

Kufotokozera

Thalidomide poyamba imalimbikitsidwa ngati sedative, inhibits cereblon (CRBN), gawo la cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ndi Kd ya∼250 nM, ndipo ali ndi immunomodulatory, anti-yotupa komanso anti-angiogenic khansa.

Mu Vitro

Thalidomide poyamba imalimbikitsidwa ngati sedative, imakhala ndi immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, ndipo imalimbana ndi cereblon (CRBN), gawo la cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ndi Kd ya∼250 nM[1]. Thalidomide (50μg/mL) imathandizira ntchito yolimbana ndi chotupa ya icotinib motsutsana ndi kuchuluka kwa ma PC9 ndi ma cell a A549, ndipo izi zimagwirizana ndi apoptosis ndi kusamuka kwa ma cell. Kuphatikiza apo, Thalidomide ndi icotinib zimalepheretsa njira za EGFR ndi VEGF-R2 m'maselo a PC9 [3].

Thalidomide (100 mg/kg, po) imalepheretsa kuyika kwa collagen, kutsitsa-kuwongolera kuchuluka kwa mawu a mRNA.α-SMA ndi collagen I, ndipo amachepetsa kwambiri ma cytokines oyambitsa kutupa mu mbewa za RILF. Thalidomide imachepetsa RILF kudzera mu kupondereza kwa ROS komanso kutsika kwa TGF-β/Smad njira yodalira mawonekedwe a Nrf2[2]. Thalidomide (200 mg/kg, po) yophatikizidwa ndi icotinib imawonetsa zotsatira zotsutsana ndi chotupa mu mbewa zamaliseche zokhala ndi ma cell a PC9, kupondereza kukula kwa chotupa ndi kulimbikitsa kufa kwa chotupa[3].