Hall I H, Liou Y F, Lee K H
J Pharm Sci. 1982 Jun;71(6):687-90. doi: 10.1002/jps.2600710620.
Molephantinin, a germacranolide, has previously been shown to possess antineoplastic activity in rodents. The principle effect of molephantinin on Ehrlich ascites carcinoma cells was to depress DNA and protein synthesis both in vivo and in vitro. DNA synthesis was inhibited at the following sites: DNA polymerase, purine synthesis specifically at inosinic acid dehydrogenase and to a lesser degree at dihydrofolate reductase, pyrimidine synthesis at orotidine monophosphate decarboxylase, thymidine kinase, histone phosphorylation, and oxidative phosphorylation processes. The protein synthesis inhibition pattern resembled more an initiation inhibitor as opposed to an elongation inhibitor.
莫勒法宁是一种吉马烷型倍半萜内酯,此前已证明它在啮齿动物中具有抗肿瘤活性。莫勒法宁对艾氏腹水癌细胞的主要作用是在体内和体外均抑制DNA和蛋白质合成。DNA合成在以下位点受到抑制:DNA聚合酶、嘌呤合成(特别是次黄嘌呤核苷酸脱氢酶,二氢叶酸还原酶的抑制程度较小)、嘧啶合成(在乳清苷酸脱羧酶、胸苷激酶、组蛋白磷酸化以及氧化磷酸化过程中)。蛋白质合成抑制模式更类似于起始抑制剂,而非延伸抑制剂。