Dahuang Lingxian Prescription Regulates Effect of TAK1 and TRAF6 Interaction and Co-localization on Inflammatory Response of Bile Duct Cells / 中国实验方剂学杂志

ObjectiveTo observe the repair effect of Dahuanglingxian prescription （DHLX） on bile duct epithelial cells of rats. To explore whether its mechanism of action is to adjust the mutual binding of transforming growth factor -β （TGF-β） activated kinase 1（TAK1） and tumor necrosis factor receptor-associated factor 6 （TRAF6）， and regulate the activation of the nuclear transcription factor -κB （NF-κB）/mitogen-activated protein kinase （MAPK） signaling pathway. MethodThe 20 SD rats were randomly divided into normal group and DHLX group， 10 rats in each group， were given saline and DHLX （320 mg·kg-1·d-1） for 8 days， to prepare normal serum and DHLX serum. Biliary epithelial cells were extracted from normal SD rats and divided into 9 groups： Normal group， model group （20 mg·L-1）， LPS+DHLX group （20 mg·L-1+10% DHLX）， LPS+PDTC group （20 mg·L-1+200 μmol·L-1）， LPS+SB203580 group （20 mg·L-1+0.5 μmol·L-1）， LPS+PDTC+SB203580 group （20 mg·L-1+200 μmol·L-1+0.5 μmol·L-1）， LPS+PDTC+DHLX group （20 mg·L-1+200 μmol·L-1+10% DHLX serum）， LPS+SB203580+DHLX group （20 mg·L-1+0.5 μmol·L-1+10% DHLX serum）， LPS+PDTC+SB203580 +DHLX group （20 mg·L-1+200 μmol·L-1+0.5 μmol·L-1+10% DHLX serum）. The microscopic observation of morphological changes in each group of cells after drug intervention. Enzyme-linked immunosorbent assay（ELISA） was used to detect the expression of （IL）-1β and IL-6 in each group of cells. Western blot detected the expression levels of TAK1 and TRAF6 proteins in each group of cells， Co-IP detected the interaction between TAK1 and TRAF6， and further observed the distribution and co-localization of TAK1 and TRAF6 using Laser confocal microscope. ResultAfter the action of LPS， the cell synapses are reduced， the cell body becomes significantly rounded and smaller， but the cell morphology of each group tends to be normal after medication. Compared with normal group， the expression levels of IL-1β and IL-6 in model group were significantly increased （P<0.05）， while the expression level of TAK1 was decreased while the expression level of TRAF6 was increased （P<0.05）. The content of TAK1-TRAF6 protein complex showed a decreasing trend， and the two proteins co-located in the cytoplasm. Compared with model group， the expression levels of IL-1β and IL-6 in LPS+DHLX group were significantly decreased （P<0.05）， the expression level of TAK1 was increased and the expression level of TRAF6 was decreased （P<0.05）， the content of TAK1-TRAF6 protein complex was significantly increased （P<0.01）， and the two proteins were significantly co-located in cytoplasm. Compared with LPS+DHLX group， the expression levels of IL-1β and IL-6 in other groups were significantly decreased （P<0.05，P<0.01）. TAK1-TRAF6 protein complex content in each group was significantly decreased after pathway blocker intervention （P<0.05）， while TAK1-TRAF6 protein complex content in each group was significantly increased after pathway blocker combined with DHLX intervention （P<0.05）. Co-localization of the TAK1-TRAF6 in cytoplasm was not obvious. ConclusionIn the LPS-induced inflammatory response of bile duct cells， the binding of TAK1 and TRAF6 showed a weakening trend， but DHLX could reverse the phenomenon， we think the mechanism of action may be related to promoting the mutual binding of TAK1 and TARF6 to inhibit the activation of the NF-κB/MAPK signaling pathway.

Comparison of tranexamic acid pharmacokinetics after intra-articular and intravenous administration in rabbits

Tranexamic Acid [TXA] is commonly administered in total knee arthroplasty for reducing blood loss. There has been a growing interest in the topical use of TXA except intravenous use for prevention of bleeding in TKA. The aim of this study was to develop and validate a HPLC-MS method to detect TXA and apply to compare the pharmacokinetic profile of TXA after intravenous [IV] and topical intra-articular [IA] application of TXA at a dose of 20 mg/kg in rabbits. In order to prove intra-articular administration is better than that of intravenous administration from the point of rabbit pharmacokinetic. Two groups of rabbits [n=6/group] respectively received TXA intra-articularly or intravenously. Blood samples were collected at scheduled time. The concentration of TXA in plasma was determined by a validated HPLC-MS method. Excellent linearity was found between 0.015 and 70.0microg/ml with a lower limit of quantitation [LLOQ]of 0.015microg/ml [r>0.99]; moreover, all the validation data including accuracy and precision [intra- and inter-day] were all within the required limits. The pharmacokinetic parameters in IA and IV group were: C[max]: 30.65+/-3.31 VS 54.05+/- 6.21 fig/ml [p<0.0l]; t[1/2]: 1.26+/-0.05 VS 0.68+/-0.13h [p<0.05]; AUC[0-t]: 42.98+/-7.73 VS 23.39+/-4.14microg/ml- h [p<0.0l], time above the minimum effective concentration [%T > MEC]: 1.5-2.2 VS 0.7-1.2h [p<0.05]. HPLC-MS method is suitable for TXA pharmacokinetic studies. The results demonstrated that topical intra-articular application of TXA showed a reduced peak plasma concentration and prolonged therapeutic drug level compared with intravenous TXA from the point of rabbit pharmacokinetic

Dynamic changes of the epididymal size after vasectomy: An ultrasonographic observation / 中华男科学杂志

<p><b>OBJECTIVE</b>To investigate the dynamic changes of the epididymal size 1 year after vasectomy.</p><p><b>METHODS</b>Fifty male volunteers received vasoligation. Before and at 1, 2, 3, 6, and 12 months after operation, we measured the size and detected the internal echoes of the epididymis using color Doppler ultrasonography.</p><p><b>RESULTS</b>The bilateral epididymides were both thickened post-operatively in all the 50 cases, with statistically significant differences between the baseline and the 1st month, the 1st and the 2nd month, the 2nd and the 3rd month, or the 3rd and the 6th month after surgery (all P < 0.01), but not between the 6th and the 12th month (P > 0.05).</p><p><b>CONCLUSION</b>Within 6 months after vasectomy, the bilateral epididymides manifested a progressive thickening, but basically restored their balance of secretion-absorption after 6 months.</p>

Triterpenoids and steroids from Excoecaria agallocha / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Excoecaria agallocha L.</p><p><b>METHOD</b>The constituents were isolated and purified by repeated column chromatography and their structures were elucidated by spectroscopic analysis.</p><p><b>RESULT</b>Six triterpenoids including taraxerone (1), beta-amyrin acetate (2), 3beta-[(2E,4E)-6-oxo-decadienoyloxy]-olean-12-ene (3), taraxerol (4), acetylaleuritolic acid (5), and cycloart-22-ene-3beta, 25-diol (6), and three steroids including beta-sitostenone (7), (24R)-24-ethylcholesta-4,22-dien-3-one (8), and beta-sitosterol (9) were isolated and identified from the stems and twigs of the mangrove plant E. agallocha.</p><p><b>CONCLUSION</b>Compounds 5-8 were isolated from E. agallocha for the first time.</p>

Chemical constituents from herb of Gueldenstaedtia stenophylla / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Gueldenstaedtia stenophylla.</p><p><b>METHOD</b>Various chromatographic techniques were used to separate and purify the constituents and structure determination was mainly based on the analysis of the spectroscopic data.</p><p><b>RESULT</b>Seven compounds, including 2', 4, 7-trihydroxy-4'-methoxyisoflavans (1), genkwanin (2), quercetin (3), rutin(4), 12-oleanen-3beta, 22beta, 24-triol (5), betulinic acid (6), and 3, 4-dihydroxybenzoic acid (7) were isolated and identified.</p><p><b>CONCLUSION</b>All these compounds were isolated from the genus Gueldenstaedtia for the first time.</p>