Study of anti-atherosclerosis effect and potential mechanisms of piperine in ApoE / 中国药理学通报

Aim To investigate the therapeutic effects of piperine (PIP) on atherosclerosis in ApoE mice fed with high fat diet and the potential mechanisms. Methods After PIP was administered for 20 weeks, aorta was stained by oil red O with the area of aortic plaque analyzed. The levels of blood lipids and serum inflammatory factors were detected. Hepatic expressions of oxidative stress related factors were determined. Human umbilical vein endothelial cells (HUVECs) were cultured and treated with a series of concentrations of PIP after LPS induction. The levels of NO and oxidative lipids were detected and factors of PI3K/Akt/eNOS pathway were analyzed. Results Serum levels of TG, LDL-C, TNF-α and CRP were significantly reduced by PIP in ApoE

Synthesis and antifatigue activities of new benzamide derivatives / 药学学报

To explore novel antifatigue agents targeting with AMPA receptor, 10 compounds were synthesized and their structures were confirmed by 1H NMR, ESI-MS and elemental analysis. 1-BCP was treated as the leading compound. The antifatigue activities were evaluated by weight-loaded forced swimming test, and the AMPA receptor binding affinities were tested with radioligand receptor binding assays. The results unveiled that 5b appeared to possess potent antifatigue activities and high affinity with AMPA receptor, which deserved further studies.

Effects of naringin on proliferation, differentiation and maturation of rat calvarial osteoblasts in vitro / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the effects of naringin on the proliferation, differention and maturaion of rat calvarial osteoblasts (ROB).</p><p><b>METHOD</b>Segregated neonatal SD rat skull, enzyme digestion to obtain ROB. The culture medium was replaced every three days. Serial subcultivation proceeded when cells covered with 80% culture dish. Naringin supplemented into the culture at 1 x 10(-4), 1 x 10(-5), 1 x 10(-6), 1 x 10(-7) mol x L(-1) respectively. MTT method was adopted in proliferation analysis and the activity of ALP was examined after induced 9 days. Search the best concentration and supplemented into the medium, then the osteogenic differentiation markers including the secretion amount of osteocalcin, osteopontin and bone morphogenetic protein-2 were compared between the naringin-supplemented group and the control. Total RNA was isolated and the mRNA level of bFGF, IGF-1, Runx-2, Osterix, ERa and ERbeta was investigated by Real time RT-PCR. Total protein also was isolated and the expression ERa, ERbeta and collagen I was examined by Western blot. After the addition of ICI 182.780, an inhibitor of the estrogen signal pathway, these index also was examined and the changes were compared.</p><p><b>RESULT</b>The ROB proliferation was motivated by naringin dose-dependently. And it evidently leads to osteogenic process and maturation. 1 x 10(-5) mol x L(-1) is the best concentration. Naringin improved the secretion of osteocalcin, osteopontin, bone morphogenetic protein-2 and collagen I significantly. Besides, it can also enhanced the mRNA level of bFGF, IGF-1, Runx-2, Osterix, ERalpha and ERbeta. While all these effects can be restrained by ICI 182.780.</p><p><b>CONCLUSION</b>The naringin with final concentration of 1 x 10(-5) mol x L(-1) enhances the osteogenic differentiation and maturation of ROB significantly, while the promoting effects vanished after the addition of ICI 182.780. These results suggesting that naringin is one of the phytoestrogens and have the activity of bone formation may via estrogen signal pathway, it can be developed into a new drug for osteoporosis therapy.</p>