Paeonol regulates phenotypic conversion of macrophages via estrogen receptor-a / 中国药理学通报

Aim To study the effect of paeonol on macrophage phenotvpe conversion based on estrogen receptora (ERa).Methods The macrophage Ml polarization model was established by 100 jjig • L"' LPS and 20 pug • L_1 I FN-7.ELISA was used to examine the effects of paeonol on tumor necrosis factor-a ( TNF-cx ) , interleukin-1 £ ( 1L-1 £ ) , interleukin-10 (IL-10), superoxide dismutase (SOD) , and malondi- aldehyde ( MDA).Western blot was used to detect the expression of M1 phenotvpe markers iNOS, CD86 and M2 phenotvpe markers Arg-1 and CD 163 in macrophages.Further, the methods of blockers and shRNA interference were used to verify whether the effect of paeonol was mediated by ERa.Results ELISA results shower] that paeonol reduced the content of TNF-a, IL- lp and MDA, and increased the content of IL-10 and SOD.Western blot results showed that paeonol reduced the expression of iNOS and CD86 proteins in model group, and increased the expression of Arg-1 and CD163 proteins.Both ERa selective blocker MPP and ERa shRNA reduced the efficacy of paeonol, while ERp selective blocker PHTPP had no significant effect on paeonol.Conclusion Paeonol can induce the transformation of macrophages into M2 type by ERa and alleviate the progression of atherosclerosis.

Sangtongjian Mixture ameliorates glucose and lipid metabolism in type 2 diabetic rats / 中成药

AIM To observe the effects of Sangtongjian Mixture (STJ) on glucose and lipid metabolism,insulin resistance and fat cytokines in type 2 diabetic rats,and their mechanisms of action.METHODS One hundred and forty rats fed on the combination of STZ and high fat diet were established as the type 2 diabetic models.Fasting blood glucose (FBG) level reached more than 16.7 mmol/L and then the rats were randomly divided into model group,metformin (180 mg/kg) group,STJ (73.5,147 and 294 mg/kg) groups.Ten rats were set as the blank group.Each treatment group was intragastrically given the corresponding agents for twelve weeks.The fasting blood glucose levels of rats were measured once every two weeks after the administration.After a 12-week administration period,glycosylated serum protein (GSP),glycosylated hemoglobin (GHb) and lipid profile indices (TC,TG,HDL-C and LDL-C) were determined.The serum insulin level was measured by radioimmunoassay,and homeostasis model assessment of insulin resistance (HOMA-IR) and insulin sensitivity index (ISI) were calculated.The levels of serum adiponectin and leptin were detected by ELISA.RESULTS STJ remarkably decreased the levels of FBG,GSP,GHb,TC,TG,LDL-C,leptin and HOMR-IR in type 2 diabetic rats.Furthermore,STJ also significantly increased the levels of HDL-C,adiponectin and ISI.CONCLUSION STJ can improve glucose and lipid metabolism in type 2 diabetic rats by ameliorating insulin resistance and regulating fat cytokine levels.

Toxic effects of strychnine and strychnine N-oxide on zebrafish embryos / 中国天然药物

AIM@#The application of strychnine (S) is limited due to its toxicity; strychnine N-oxide (SNO) is a derivative of strychnine. The aim was to employ zebrafish embryos to investigate and compare the developmental toxicity induced by S and SNO.@*METHODS@#The toxicity of S and SNO was examined through the hatching rate and survival rate. Morphological changes of the zebrafish were observed with a dissecting microscope. Apoptosis was detected through acridine orange (AO) staining and flow cytometry. Apoptotic genes were measured by RT-PCR.@*RESULTS@#Embryo malformation was observed in the embryos exposed to S at 200 μmol·L(-1). When SNO concentration was increased to 1 mmol·L(-1), scoliolosis, and pericardial edema could be seen in some embryos. Results from fluorescence microscopy and flow cytometry analysis showed that S at 200 μmol·L(-1) induced apoptosis, whereas the apoptotic rate in the SNO-treated group (200 μmol·L(-1)) was much lower than that in the S group. RT-PCR analysis showed that p53 mRNA expression and the ratio of Bax/Bcl-2 in the S group were significantly altered compared with the control group (*P < 0.05). Moreover, Bax mRNA expression in both S and SNO group were significantly different from that in the control group (**P < 0.01).@*CONCLUSION@#These results lead to the conclusion that SNO has significantly lower toxicity than S in zebrafish embryos.

Study of effect of tongsaimai tablets on experimental diabetic foot model rats / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the effect of Tongsaimai (TSM) tablets in treating foot trauma of diabetic foot (DF) model rats, and discuss its potential mechanism.</p><p><b>METHOD</b>Male SD rats were selected to duplicate the diabetic foot ulcer model and randomly divided into the blank control group, the model group, the metformin treatment group, and TSM 12.44, 6.22, 3.11 g x kg(-1) groups (n = 10). The healing of ulcer wounds were observed on day 1, 4, 8, 13 and 18. After 18 days, a histopathologic examination was conducted for ulcer tissues. The contents of superoxide dismutase (SOD) and malondialdehyde (MDA) were detected by hydroxylamine and TBA methods. The content of interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-alpha) were determined with the radioimmunoassay. The immunohistochemical method was used to observe the expression of vascular endothelial growth factor (VEGF) in ulcer tissues and the number of capillary vessels.</p><p><b>RESULT</b>TSM could alleviate the pathological changes of diabetic foot rats, accelerate the ulcer healing on 4, 8, 13, 18 d, reduce MDA, IL-6, TNF-alpha, VEGF content in rat serum at 18 d (after the rehabilitation period), and enhance the SOD content. Specifically, the TSM 12.44 g x kg(-1) group showed significant differences compared with the model group (P < 0.05, P < 0.01). At 18 d after the treatment (the late rehabilitation period), the VEGF expression of TSM 12.44, 6.22 g x kg(-1) groups and the number of blood capillaries of the TSM 12.44 g x kg(-1) group were significantly lower than that of the model group (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>TSM could promote the foot wound healing of DF model rats, reduce MDA, IL-6 and TNF-alpha levels in serum, increase the SOD content and decrease the VEGF expression and the number of blood capillaries in the late rehabilitation period. Its action mechanism may be related to the inhibition of oxidative stress injury and the inflammatory cell infiltration.</p>