Shamon L A, Pezzuto J M, Graves J M, Mehta R R, Wangcharoentrakul S, Sangsuwan R, Chaichana S, Tuchinda P, Cleason P, Reutrakul V
Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 60612, USA.
Cancer Lett. 1997 Jan 15;112(1):113-7. doi: 10.1016/S0304-3835(96)04554-5.
Triptolide, a highly oxygenated diterpene isolated from Tripterygium wilfordii Hook f. (Celastraceae), has been shown to demonstrate potent antileukemic activity in rodent models at remarkably low treatment doses. A variety of other physiological responses are known to be mediated by this compound, including immunosuppressive and antifertility effects. We currently report that triptolide was not mutagenic toward Salmonella typhimurium strain TM677, either in the presence or absence of a metabolic activating system. Relatively potent but non-specific cytotoxicity was observed with a panel of cultured mammalian cell lines, and modest antitumor activity was observed when an i.p. dose of 25 microg was administered three times weekly to athymic mice carrying human breast tumors. Treatment regimens involving higher doses of triptolide (e.g. 50 microg/mouse three times weekly) were lethal.
雷公藤甲素是从卫矛科植物雷公藤中分离得到的一种高度氧化的二萜类化合物，已证明在啮齿动物模型中，极低的治疗剂量就能显示出强大的抗白血病活性。已知该化合物还介导多种其他生理反应，包括免疫抑制和抗生育作用。我们目前报告，无论有无代谢激活系统，雷公藤甲素对鼠伤寒沙门氏菌TM677菌株均无致突变性。在一组培养的哺乳动物细胞系中观察到相对较强但非特异性的细胞毒性，当对携带人乳腺肿瘤的无胸腺小鼠每周腹腔注射25微克，给药三次时，观察到适度的抗肿瘤活性。涉及更高剂量雷公藤甲素的治疗方案（如每周三次，每次50微克/小鼠）是致命的。
