Expression of aquaporin 8 and its relationship with melanosis coli / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>The relationship between melanosis coli (MC) and aquaporin 8 (AQP8) has not yet been elucidated. The aim of this research was to investigate the relationship between the expression of AQP8 and the pathological mechanism of MC.</p><p><b>METHODS</b>Expression of AQP8 was detected by immunohistochemistry and reverse transcription-polymerase chain reaction (RT-PCR) in 37 MC colon tissues and 13 control colon tissues. Global gene expression analysis was also used to identify differently expressed genes. Its relationship with MC was analyzed by SPSS 11.5 statistical software.</p><p><b>RESULTS</b>The positive rate of AQP8 expression detected by immunohistochemistry in the MC group was 24.3% (9/37), significantly lower than the 69.2% (9/13) in the control group (P < 0.05). The relative expression level of AQP8 in MC group was 0.639 ± 0.160, lower than 0.921 ± 0.148 of controls (P < 0.05). Global gene expression analysis showed that AQP8 mRNA expression was downregulated in MC patients.</p><p><b>CONCLUSIONS</b>The decreased AQP8 expression in MC patients indicates that chronic use of laxatives containing anthraquinone may cause reduced water absorption. The expression of AQP8 may be related to MC.</p>

Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines and their anti-HIV reverse transcriptase activity / 药学学报

<p><b>AIM</b>Synthesis of 1-(3-phthalimido-2-oxobutyl)-4-substituted- phenylpiperazines (5-15).</p><p><b>METHODS</b>The starting material nitrogen mustard hydrochloride (16), reacted with the corresponding substituted anilines to afford piperazine hydrochlorides (17-27), which were then coupled with 1-bromo-3-phthalimidobutan-2-one (4) to give the target compounds.</p><p><b>RESULTS</b>Eleven target compounds (5-15) were synthesized, which were characterized by 1HNMR, IR and elemental analysis.</p><p><b>CONCLUSION</b>Anti-HIV-1 RT using HIV reverse transcriptase P-66 protein test showed that compounds 11, 14, 10 and 13 possessed inhibitory effects against HIV-1 reverse transcriptase (RT), with IC50 29.80, 35.20, 43.77 and 63.76 mumol.L-1, respectively.</p>