Ford W C, Harrison A, Waites G M
J Reprod Fertil. 1981 Sep;63(1):67-73. doi: 10.1530/jrf.0.0630067.
6-Chloro-6-deoxyfructose or 6-chloro-6-deoxyglucitol (greater than 90 mumol/kg/day), 6-chloro-6-deoxyglucose or 6-chloro-6-deoxymannose (greater than 120 mumol/kg/day) and 6-chloro-6-deoxygalactose (greater than 300 mumol/kg/day) all had an antifertility action in the male rat when given by mouth. Spermatozoa from the infertile rats were unable to oxidize glucose. This effect was always produced by a lower dose than the antifertility effect and the threshold dose for the 2 effects varied in a parallel fashion between the different 6-chloro-6-deoxysugars. Glucose oxidation appeared to be inhibited at the triose phosphate isomerase or glyceraldehyde 3-phosphate dehydrogenase reaction. These effects of 6-chloro-6-deoxysugars are similar to those of alpha-chlorohydrin. The activities of the glycolytic enzymes were greatly in excess of the observed flux through the pathway and high concentrations of glucose 6-phosphate and triose phosphate accumulated in rat spermatozoa incubated with 2 mM-D-glucose.
6-氯-6-脱氧果糖或6-氯-6-脱氧葡糖醇(大于90微摩尔/千克/天)、6-氯-6-脱氧葡萄糖或6-氯-6-脱氧甘露糖(大于120微摩尔/千克/天)以及6-氯-6-脱氧半乳糖(大于300微摩尔/千克/天)经口给予雄性大鼠时均具有抗生育作用。不育大鼠的精子无法氧化葡萄糖。这种作用总是由低于抗生育作用的剂量产生,并且这两种作用的阈剂量在不同的6-氯-6-脱氧糖之间以平行方式变化。葡萄糖氧化似乎在磷酸丙糖异构酶或3-磷酸甘油醛脱氢酶反应处受到抑制。6-氯-6-脱氧糖的这些作用与α-氯醇的作用相似。糖酵解酶的活性大大超过通过该途径观察到的通量,并且在与2 mM-D-葡萄糖一起孵育的大鼠精子中积累了高浓度的6-磷酸葡萄糖和磷酸丙糖。