Effect of Lycium barbarum polysaccharides on the retinal ultrastructure of streptozocin-induced diabetic rats / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To study the retinal ultrastructure of streptozocin (STZ)-induced diabetic rats and the intervention effect of Lycium Barbarum Polysaccharides (LBP).</p><p><b>METHODS</b>The STZ-induced diabetic SD rat model was established. LBP was given to those in the treatment group by gastrogavage. Changes of body weight, blood glucose, and retinal ultrastructure at 24-week were observed.</p><p><b>RESULTS</b>Early retinal changes covered mitochondrion changes, cell degeneration and apoptosis of retinal neurons and neuroglia cells in the diabetic rats. No change of body weight or blood glucose was observed between the LBP group and the diabetic model group (P > 0.05). The ultrastructural changes were obviously relieved by LBP, and limited to the inner nuclear layer.</p><p><b>CONCLUSIONS</b>LBP could obviously relieve pathological changes of mitochondrion, hinder neural cell apoptosis. Its effect might not be achieved by lowering blood glucose. It was expected to be used in preventing and treating early diabetic retinal neuropathy.</p>

Synthesis and central none-opioid analgesic activity of SIPI5047 / 药学学报

Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.

Design and synthesis of aralkyl-ketone piperazine derivatives and their antalgic activities / 药学学报

To synthesize aralkyl-ketone piperazine derivatives as analgesic agents, the N atom of the one side of piperazine ring is protected by formyl group firstly, then the unprotected N atom is alkylated to prepare aralkyl-ketone piperazine derivatives. Their analgesic biological activities were well studied by mice writhing model, rat hot plate model and rat tail flick model. Sixty four compounds were synthesized and pharmacological tests in vivo revealed these compounds have potent analgesic activities, especially compound I12, I14, I14 I21 and I37. These four compounds are more worthy for further research.

Influence of polysaccharide from Aloe vera on the proliferation of the human epithelial cells cultured in vitro / 中华烧伤杂志

<p><b>OBJECTIVE</b>To investigate the influence of polysaccharide from Aloe Vera (AP) on the proliferation of the human epithelial cells cultured in vitro.</p><p><b>METHODS</b>The human epithelial cells undergoing 3 to 4 passages of confluence culture were randomly divided into control and 25, 50, 100, 200 and 400 mg/L AP groups according to different dosage of the polysaccharide (AP) added into the culture medium. In the control group (C), equal volume of DK-SFM medium was added to the culturing cells. The conjugation time of epithelial cells, the changes in the cell morphology and ultrastructure were observed under inverted phase contrast microscope and transmission electron microscope, respectively. The cell proliferation was measured by MTT, cell count analysis and [(3)H]-TdR incorporation. Flow cytometry analysis was employed to detect the cell cycle. The leakage rate of lactate dehydrogenase (LDH) was assayed for the evaluation of the epithelial cell injury.</p><p><b>RESULTS</b>There was no significant difference in the morphology of the epithelial cells among the groups under inverted phase contrast microscope. But under the transmission electron microscope (TEM), the cells in 100 to 400 mg/L AP groups were seen to have proliferated actively, with euchromatin dominant in the nuclei, while heterochromatin was dominant in the cellular nucleus in control and 25 mg/L AP groups. The confluence time of epithelial cells in 50, 100, 200, 400 mg/L AP groups (154 +/- 12, 141 +/- 20, 130 +/- 19, 124 +/- 13) h preceded noticeably than that in control group (182 +/- 8) h, (P < 0.01). The cell proliferation in 100, 200, 400 mg/L groups reached the peak on the 5th day after AP treatment, while that in control and other groups was delayed by 1 to 2 days. The survival rate of the cells in 25 to 400 mg/L AP groups increased dramatically compared with that in control group, with its [(3)H]-TdR incorporation levels significantly increased in a dose dependent manner. The leakage rate of LDH in 200 and 400 mg/L AP groups was lower than that in control group (P < 0.01). The flow cytometric analysis of the cell cycle distribution revealed that the percentage of cell cycle from phase G0/G1 to G2/M and S in 25 to 400 mg/L AP groups increased significantly in a dose dependent manner compared with that in control group (P < 0.01).</p><p><b>CONCLUSION</b>AP might be beneficial to the protection of epithelial cells by promoting cell proliferation through inducing the progression of epidermal cells from phase G0/G1 into G2/M and S phases.</p>

Effect of Aloe coarse polysaccharide on cytokine secretion of keratinocytes in vitro / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effects of Aloe coarse polysaccharide on the levels of growth factors (EGF, TGF-alpha, TGF-beta1) and interleukins (IL-1beta, IL-6, IL-8) and tumor necrosis factor (TNF) in cultured keratinocytes.</p><p><b>METHOD</b>The cultured keratinocytes were treated with Aloe coarse polysaccharide at concentrations of 75, 150, 300, 600, 1 200 mg x L(-1) land the equal volume of media as control group. The levels of EGF, TGF-alpha, TGF-beta1, IL-1beta, IL-6, IL-8 and TNF in the supernatants of cultured keratinocytes were assayed by enzyme-linked immunosorbent assay (ELISA) and radioimmunoassay (RIA).</p><p><b>RESULT</b>Compared with the control group, the levels of EGF, TGF-alpha, IL-1beta, IL-6 and IL-8 were significantly increased by treatment with Aloe coarse polysaccharide (P < 0.05, P < 0.01) and in a dose dependent manner, and the levels of TGF-beta1 and TNF were also increased but no statistical significance.</p><p><b>CONCLUSION</b>Aloe coarse polysaccharide may promote keratinocytes to secrete EGF, TGF-alpha, IL-1beta, IL-6 and IL-8.</p>