维生素K2(20)的两相合成工艺及其营养剂量对增加骨密度的研究

 在以BF₃·OEt₂作催化剂及45~47℃的反应条件下,将大过量的2-甲基-1,4萘二酚循环与香叶基香叶醇(每次保持摩尔比为10:1)在CH₃NO₂-正己烷两相反应体系中进行Friedel-Crafts烷基化反应合成维生素K₂(20)的氢醌,再在催化量的FeCl₃·6H₂O作用下经空气氧化,以满意的收率及较高的化学选择性合成了维生素K₂(20) . 同时,利用去卵巢致大鼠骨质疏松模型,参考维生素K₂人体低端推荐摄入量(50μg/d)进行了动物实验剂量设计并进行了维生素K₂(20)增加骨密度的营养剂量的量效关系研究,结果表明:每天给药 25~100μg/(kg·d),均能防止去势大鼠的骨流失,使股骨中点及远心端骨密度明显增加(P<0.05),并呈现出相应的量效关系.研究为维生素K₂(20)的工业生产提供了可能的工艺,也为提高骨密度以预防骨质疏松的人体营养补充剂量(50~100μg/d)提供了可行性依据.

The two-phase synthesis of menatetrenone and its dose-effect relationship of anti-osteoporosis activity in ovariectomized rats

With the two-phase reactive system of CH₃NO₂/n-hexane,the hydroquinone of menatetrenone was prepared at 45—47℃ by BF₃·Et₂O catalyzed Friedel-Crafts alkylation of 2-methyl-1,4-naphthohydroquinone and gernaylgeraniol.Then menatetrenone was synthesized in good yield and high selectivity by treating the hydroquinone with the catalytic amount of FeCl₃·6H₂O and the oxygen of air.The dose-effect relationship of anti-osteoporosis activity of menatetrenone in ovariectomized rats was investigated.Our results suggest that low-dose menatetrenone could prevent the bone loss in ovariectomized young rats,thus nutritional dose of menatetrenone may be beneficial in the prevention of osteoporosis in the elderly.