Optimization of the ultrasound-assisted synthesis of lutein disuccinate using uniform design.

The ultrasound-assisted synthesis of lutein disuccinate from all-trans lutein (AL) and succinic anhydride (SA) was investigated in this study. Triethylamine was used as the catalyst. Based on the single-factor experiments, a 7-level-3-factor uniform design and response surface analysis were further employed to evaluate the effects of the selected variables including molar ratio of SA/AL, reaction time and ultrasonic power on the yield of lutein disuccinate. The results indicated that the data were adequately fitted into a second-order polynomial model; the molar ratio of SA/AL significantly affected the synthesis of lutein disuccinate, whereas reaction time and ultrasonic power did not. Based on ridge max analysis, the optimum condition for lutein disuccinate synthesis was predicted to be the molar ratio of SA/AL 265.3:1, ultrasonic power 300 W and reaction time 131.6 min with the lutein disuccinate yield of 80.53±0.18%, which give a 43.8% increase compared with the traditional method, and also significantly shorten the reaction time.

Evaluation of androgen receptor transcriptional activities of some pesticides in vitro.

Organophosphates and pyrethroids are among the most common pesticides currently in use worldwide. Several pesticides have been reported to possess hormonal activities, and thus are classified as endocrine disruptors. The present study was planned to evaluate potential androgenic and antiandrogenic activities of the pesticides. The selected chemicals are three organophosphate pesticides including dichlorvos, parathion and trichlorphon, and two pyrethroid pesticides including permethrin and cypermethrin. We evaluated the pesticides for androgen receptor (AR)-mediated mechanisms using a human AR reporter gene assay in African monkey kidney cell line CV-1 transiently transfected with the constructed reporter gene plasmid pMMTV-CAT and the hAR expression plasmid AR/pcDNA3.1. We demonstrated that parathion showed significant inhibitory effects on the transcriptional activity induced by 1 nM of DHT with IC(50) value of (2.01+/-0.42) x 10(-7) M, though trichlorphon and dichlorvos lacked this activity. The two pyrethroid pesticides permethrin and cypermethrin exhibited lower activity than parathion with IC(50) value of (5.68+/-2.20) x 10(-5) and (6.80+/-2.30) x 10(-5) M, respectively. On the other hand, we failed to find AR-mediated androgenic activities of the tested chemicals. It is suggested that parathion possesses the highest activity, and permethrin and cypermethrin acted as poor antiandrogens. The present study provides insight into the mechanism of the pesticides.