二氢青蒿素与青蒿琥酯的抗孕作用

CONTRAGESTATIONAL EFFECTS OF DIHYDKOARTEMISININ AND ARTESUNATE

研究表明，二氢青蒿素与青蒿琥酯对小鼠、金黄地鼠、豚鼠及兔均有抗孕作用。在金黄地鼠和豚鼠表现为引致流产，在小鼠和兔表现为使胚胎吸收。小鼠妊娠ｄ７、金黄地鼠妊娠ｄ５单次ｓｃ二氢青蒿素的抗孕ＥＤ＿（５０）（９５％可信限）分别为３２．８（２７．７～３８．９）及６．１（５．６～６．７）ｍｇ·ｋｇ￣（－１），豚鼠妊娠ｄ１８单次ｉｍ二氢青蒿素的抗孕ＥＤ＿（５０）为１８．３（１３．９～２４．２）ｍｇ·ｋｇ￣（－１），。金黄地鼠妊娠ｄ５单次ｓｃ青蒿琥酯的抗孕ＥＤ＿（５０）为１２．２（１０．３～１４．４）ｍｇ．ｋｇ￣（－１）．以金黄地鼠进行的观察表明二氢青蒿素对胚胎有较高的选择性作用，引起胚胎坏死的剂量对于母体子宫、卵巢和一般健康状况无明显损害。

In experiments carried out in mice,hamsters,guinea pigs and rabbits bothdihvdroartemisinin and artesunate showed contragestational effect.In mice and rabbits they causedembryo absorption whereas in hamsters and guinea pigs they induced abortion. The contragestationalED50 of dihydroartemisinin given sc on d 7 of pregnancy in mice and d 5 of pregnancy in hamsters were32.8(27.7～38.9)mg.kg-1 and 6.1(5.6～6.7)mg·kg-1 respectively.The ED50 of this drug givenim on d 18 of pregnancy in guinea pigs was 18.3(13.9～24. 2) mg·kg-1. Dihydroartemisinin alsoshowed mid-pregnancy terminating effect in hamsters. The contragestational ED50 of artesunate givensc on d 5 of pregnancy in hamsters and the ED50 of sodium artesunate given sc on d 5～8 of pregnancyin hamsters were 12. 2(10.3～14.4)mg.kg-1 and 1.0(0.9～1.2)mg·kg-1 daily respectively。Results of light microscopic examination revealed that dihydroartemisinin was selectively toxic toembrvo sac,At dose levels sufficient to induce embryo sac necrosis,dihydroartemisinin did not injurethe uterus and ovarv of the maternal animals.On the ground of the foregoing observations we considerthat dihvdroartemisinin,artesunate and their analogous drugs should not be used to treat malaria inpregnant women and there is the possibility to exploit intent ional abortion agents from artemisininderivatives。