Shimomura K, Mullinix M G, Kakunaga T, Fujiki H, Sugimura T
Science. 1983 Dec 16;222(4629):1242-4. doi: 10.1126/science.6316505.
Aplysiatoxin and debromoaplysiatoxin, which are isolated from the seaweed, Lyngbya gracilis, differ in their chemical structure only by the presence or absence of a bromine residue in the hydrophilic region. The function and the structure-activity relation of the hydrophilic region are not known. Aplysiatoxin increased malignant transformation, stimulated DNA synthesis, and inhibited the binding of phorbol-12,13-dibutyrate and epidermal growth factor to cell receptors. Debromoaplysiatoxin inhibited the binding of these two substances as strongly as aplysiatoxin but did not increase malignant transformation or stimulate DNA synthesis. These results indicate that a slight change in the chemical structure of the hydrophilic region of aplysiatoxin affects its abilities to increase cell transformation and stimulate DNA synthesis and that the abilities of the tumor promoters to inhibit the binding of phorbol-12,13-dibutyrate and epidermal growth factor are dissociable from their abilities to increase cell transformation and stimulate DNA synthesis under some circumstances.
从海藻纤细席藻（Lyngbya gracilis）中分离出的海兔毒素和去溴海兔毒素，其化学结构仅在亲水区是否存在溴残基方面有所不同。亲水区的功能及其构效关系尚不清楚。海兔毒素可增加恶性转化、刺激DNA合成，并抑制佛波醇-12,13-二丁酸酯和表皮生长因子与细胞受体的结合。去溴海兔毒素对这两种物质结合的抑制作用与海兔毒素一样强，但不会增加恶性转化或刺激DNA合成。这些结果表明，海兔毒素亲水区化学结构的微小变化会影响其增加细胞转化和刺激DNA合成的能力，并且在某些情况下，肿瘤促进剂抑制佛波醇-12,13-二丁酸酯和表皮生长因子结合的能力与其增加细胞转化和刺激DNA合成的能力是可分离的。
