Carbon Chain Length Determines Inhibitory Potency of Perfluoroalkyl Sulfonic Acids on Human Placental 3β-Hydroxysteroid Dehydrogenase 1: Screening, Structure-Activity Relationship, and In Silico Analysis / 生物医学与环境科学（英文）

OBJECTIVE@#This study aimed to compare 9 perfluoroalkyl sulfonic acids (PFSA) with carbon chain lengths (C4-C12) to inhibit human placental 3β-hydroxysteroid dehydrogenase 1 (3β-HSD1), aromatase, and rat 3β-HSD4 activities.@*METHODS@#Human and rat placental 3β-HSDs activities were determined by converting pregnenolone to progesterone and progesterone secretion in JEG-3 cells was determined using HPLC/MS-MS, and human aromatase activity was determined by radioimmunoassay.@*RESULTS@#PFSA inhibited human 3β-HSD1 structure-dependently in the order: perfluorooctanesulfonic acid (PFOS, half-maximum inhibitory concentration, IC 50: 9.03 ± 4.83 μmol/L) > perfluorodecanesulfonic acid (PFDS, 42.52 ± 8.99 μmol/L) > perfluoroheptanesulfonic acid (PFHpS, 112.6 ± 29.39 μmol/L) > perfluorobutanesulfonic acid (PFBS) = perfluoropentanesulfonic acid (PFPS) = perfluorohexanesulfonic acid (PFHxS) = perfluorododecanesulfonic acid (PFDoS) (ineffective at 100 μmol/L). 6:2FTS (1H, 1H, 2H, 2H-perfluorooctanesulfonic acid) and 8:2FTS (1H, 1H, 2H, 2H-perfluorodecanesulfonic acid) did not inhibit human 3β-HSD1. PFOS and PFHpS are mixed inhibitors, whereas PFDS is a competitive inhibitor. Moreover, 1-10 μmol/L PFOS and PFDS significantly reduced progesterone biosynthesis in JEG-3 cells. Docking analysis revealed that PFSA binds to the steroid-binding site of human 3β-HSD1 in a carbon chain length-dependent manner. All 100 μmol/L PFSA solutions did not affect rat 3β-HSD4 and human placental aromatase activity.@*CONCLUSION@#Carbon chain length determines inhibitory potency of PFSA on human placental 3β-HSD1 in a V-shaped transition at PFOS (C8), with inhibitory potency of PFOS > PFDS > PFHpS > PFBS = PFPS = PFHxS = PFDoS = 6:2FTS = 8:2FTS.

Effects of injection of Huangqi injectio into Zusanli (ST 36) on immune function in the patient of schizophrenia / 中国针灸

<p><b>OBJECTIVE</b>To study on effects of injection of Huangqi Injectio into Zusanli (ST 36) on the hospital infection and immune function in the patient of schizophrenia.</p><p><b>METHODS</b>Thirty inpatients of chronic schizophrenia were treated with injection of Huangqi Injectio into bilateral Zusanli (ST 36), 2 mL each point, thrice each week, for 8 weeks. Relative immune indexes and the hospital infection were investigated.</p><p><b>RESULTS</b>The hospital infection and the sub-infection were 4 cases (13.3%), 7 cases-times (23.3%) in the injection group; and 9 cases (15.0%), 19 cases-times (31.7%) in the control group, respectively, with no significant difference between the two groups (P>0.05). The drug-administration duration was 7.77 days/case and 11.87 days/case in the two groups, respectively (P<0.01). In the injection group, as compared with that of last 3 years the duration was 7.77 days/case and 14.08 days/case (P<0.01). IgG, IgA, IgM and T-cell subgroups did not have significant changes, but there was the most different value before and after injection in SIL-2R of the no-infection group, and the longer the drug administration duration, the smaller the different values.</p><p><b>CONCLUSION</b>Injection of Huangqi Injectio into Zusanli (ST 36) has definite effect for prevention of the hospital infection in inpatients of chronic schizophrenia, and SIL-2R is a valuable index for investigation of the hospital of infection.</p>