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目的测定桦木醇及2个新合成的桦木醇一氧化氮(NO)供体衍生物在正辛醇-水中的表观油水分配系数,进一步为体内吸收研究提供参考。方法采用摇瓶法和高效液相法测定桦木醇及其NO供体衍生物在正辛醇-水中的表观油水分配系数,并进行比较。结果桦木醇、3-2’-硝氧丙酰氧桦木醇及3-羰基-28-2’-硝氧乙酰氧桦木醇的表观油水分配系数的对数值(lg P)分别为-0.259,0.570,0.337,表明桦木醇NO供体衍生物在体内透生物膜能力较好,可被较好地吸收。结论桦木醇及其衍生物结构与油水分配系数之间有密切的关系,合理的修饰有利于提高桦木醇的生物利用度。
Aim To determine the apparent oil-water partition coefficients of betulin and two newly synthesized derivatives of betulin as nitric oxide (NO) donor in n-octanol-water, and to provide references for the in vivo absorption studies. Methods The apparent oil-water partition coefficients of betulin and NO donor derivatives in n-octanol-water were determined by shake flask method and high performance liquid phase method and compared. Results The logarithm value (lg P) of the apparent oil-water partition coefficients of betulin, 3-2’-nitroxypropionate betulin and 3-carbonyl-28-2’-nitrooxyacetoxy betulin were -0.259, 0.570,0.337, indicating that betulin alcohol NO donor derivatives have better biofilm permeability in vivo and can be well absorbed. Conclusion There is a close relationship between the structure of betulin and its derivatives and oil-water partition coefficient. Reasonable modification is helpful to improve the bioavailability of betulin.