一种新型异黄酮7-羟基-4′-甲基异黄酮的合成及其生物活性的初步研究

Synthesis of and Preliminary Studies on the Bioactivities of 7-Hydroxy-4'-methyl-isoflavone

利用间苯二酚和对甲基苯乙酸在三氟化硼/乙醚催化作用下的缩合反应,通过一锅法,制备了一种新型异黄酮体-羟基-4′-甲基异黄酮,并设计合成了I1和(I2～I6)五种新的衍生物。在此基础上,采用家兔颅盖骨骨髓成骨细胞,就其对该成骨细胞DNA,胶原蛋白的合成和碱性磷酸酶的活性等因素的影响进行了初步试验。研究表明:所合成的六种化合物对上述因素均有不同程度的促进作用。

A novel isoflavone 7hydroxy4'methylisoflavone (I1) was synthesized from the unprotected resorcinol and pmethylphenylacetic acid by an onepot method using boronetherate as catalyst, and five new derivatives (I2～I6)were also obtained through the corresponding reactions. Preliminary pharmacological tests of the effects on collagen synthesis and alkaline phosphatase activity of rabbit osteoblasts in vitro showed that all of these compounds could promote the growth of the osteoblasts to a certain degree..