Nakao Y, Matsuda S, Kimoto H, Matsui T, Kobayashi N, Kishihara M, Fujita T, Watanabe S, Ueda K, Ito Y
Int J Cancer. 1982 Dec 15;30(6):687-95. doi: 10.1002/ijc.2910300603.
Three different diterpen polyols and the teleocidin have antileukemic effects on the human thymic leukemia cell line HPB-ALL by inducing phenotypic differentiation. We tested TPA (phorbol esters), mezerein (daphnane), milliamin (ingenol ester) and teleocidin B (teleocidins) as representative of the chemical structure of each principle and found that these agents have the similar biological activity of inducing phenotypic differentiation in HPB-ALL cells. Moreover, competitive binding of [3H]PDB to cell-surface receptors was significantly inhibited by these agents; n-butyrate and phorbol per se did not inhibit the binding of [3H]PDB. Despite differences in the structure of the principles, these agents may have similarly acting side-chain structures.
三种不同的二萜多元醇和杀鱼菌素通过诱导表型分化对人胸腺白血病细胞系HPB - ALL具有抗白血病作用。我们测试了作为每种主要成分化学结构代表的佛波酯（TPA）、瑞香毒素（二萜类）、大戟醇酯（千金二萜醇酯）和杀鱼菌素B（杀鱼菌素），发现这些药物在HPB - ALL细胞中具有相似的诱导表型分化的生物学活性。此外，这些药物显著抑制了[3H]佛波醇-12,13-二丁酸酯（[3H]PDB）与细胞表面受体的竞争性结合；正丁酸盐和佛波醇本身并不抑制[3H]PDB的结合。尽管主要成分的结构存在差异，但这些药物可能具有相似作用的侧链结构。
