12 Feb

Aryl Phosphate Derivatives of Bromo-Methoxy-Azidothymidine: RESULTS(4)


Kinetics of Sperm Immobilization

The comparative concentration-dependent effects of AZT, three analogues of AZT, and four aryl phosphate derivatives of AZT on sperm motility were analyzed by CASA (Fig. 3A). At a concentration > 25 ^M, WHI-07 abrogated the motility of > 95% of the treated sperm, whereas AZT and its derivatives, WHI-02, WHI-08, and WHI-09 without the 5-bromo 6-methoxy functional groups, were inactive even at 300 ^M. Also, the kinetics of sperm immobilization was fast with spermicidal AZT derivatives when compared to that with N-9 at 100 ^M (Fig. 3B). buy flovent inhaler

There was a linear relationship between incubation time and progressive sperm motility by CASA. Regression analysis of progressive motility against duration of incubation time for WHI-05 and WHI-07 showed positive correlation coefficients of 0.88 (p < 0.005) and 0.84 (p < 0.003). The corresponding times required for 50% motility loss of progressively motile sperm exposed to WHI-05 and WHI-07 (at 100 ^M concentration) were 17 min (95% confidence interval: 12-26 min) and 6 min (95% confidence interval: 4-11 min), respectively. Complete sperm immobilization was achieved after 120 min of exposure to N-9, 60 min exposure to WHI-05, and 30 min of exposure to WHI-07. By comparison, the sperm motility in control samples remained stable (96 ± 2.5% compared to baseline) during the 150-min monitoring period.

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