Triptolide-d3 (PG490-d3) 是氘标记的雷公藤内酯。雷公藤内酯是从雷公藤根中提取的二萜类三环氧化物，具有免疫抑制、抗炎、抗增殖和抗肿瘤作用。雷公藤内酯是一种 NF-κB 活化抑制剂。
Triptolide-d3 is intended for use as an internal standard for the quantification of triptolide by GC- or LC-MS. Triptolide is a diterpenoid triepoxide that has been found in T. wilfordii and has diverse biological activities.1,2,3,4 It inhibits dCTP pyrophosphatase 1 (Ki = 168 µM), an enzyme that prevents halogenated nucleotides from entering DNA synthesis.1 It reduces viability of A549, H1299, NCI H520, NCI H1650, and H1975 human non-small cell lung cancer (NSCLC) cells when used at a concentration of 50 nM.2 Intranasal administration of liposomes containing triptolide (0.4 mg/kg) reduces tumor growth in a rat orthotopic model of lung cancer. Triptolide (0.2 mg/kg) reduces intestinal inflammation and prevents colon shortening in a mouse model of ulcerative colitis induced by dextran sulfate .3 It also inhibits skin allograft rejection and increases graft survival time in mice when administered at a dose of 0.1 mg/kg per day post-transplantation.4
1.Corson, T.W., Cavga, H., Aberle, N., et al.Triptolide directly inhibits dCTP pyrophosphataseChemBioChem12(11)1767-1773(2011) 2.Song, J.M., Molla, K., Anandharaj, A., et al.Triptolide suppresses the in vitro and in vivo growth of lung cancer cells by targeting hyaluronan-CD44/RHAMM signalingOncotarget.8(16)26927-26940(2017) 3.Tang, B., Zhu, J., Zhang, B., et al.Therapeutic potential of triptolide as an anti-inflammatory agent in dextran sulfate sodium-induced murine experimental colitisFront. Immunol.11592084(2020) 4.Yang, S.-X., Gao, H.-L., Xie, S.-S., et al.Immunosuppression of triptolide and its effect on skin allograft survivalInt. J. Immunopharmacol.14(6)963-969(1992)
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