Lipid metabolism and mechanism research of piperine on glucose metabolism of model rats with insulin resistance syndrome / 中国药理学通报

Aim To investigate the effect of piperine (PIP)on triglycerides(TG),free fatty acid(FFA), tumor necrosis factor-α(TNF-α)and leptin of model rats with insulin resistance syndrome(IRS).Methods By feeding rats with high-fat,high-glucose and high-salt diet,IRS model rats were established.Triglycer-ides(TG)was observed dynamically every 4 weeks, treating on the 4th weeks and 8 weeks continuously. TG (method of GOD-POD),FFA (method of colori-metric),TNF-αand leptin (method of ELISA)were measured.Results After 8 weeks treatment,the level of TG,FFA,TNF-αand leptin in PIP group decreased obviously,while it increased in model group signifi-cantly.Conclusions PIP could reduce TG and FFA and improve abnormal lipid metabolism of model rats with IRS significantly.Perhaps the mechanism is relat-ed with the down-regulation of cytokine TNF-αand leptin.

One pot synthesis of diarylfurans from aryl esters and PhI(OAc)2 via palladium-associated iodonium ylides.

The example of palladium-catalyzed intermolecular cyclization for the synthesis of various diarylfurans in which one of the aromatic rings originates from the phenolic part of the starting ester and the other one from PhI(OAc)2 has been reported. The reaction is carried out through two steps: the rearrangement of palladium-associated iodonium ylides to form o-iodo diaryl ether and then palladium catalyzed intramolecular direct arylation. This reaction can tolerate a variety of functional groups and is alternative or complementary to the previous methods for the synthesis of diarylfurans.

Energy-efficient green catalysis: supported gold nanoparticle-catalyzed aminolysis of esters with inert tertiary amines by C-O and C-N bond activations.

Catalyzed by supported gold nanoparticles, an aminolysis reaction between various aryl esters and inert tertiary amines by C-O and C-N bond activations has been developed for the selective synthesis of tertiary amides. Comparison studies indicated that the gold nanoparticles could perform energy-efficient green catalysis at room temperature, whereas Pd(OAc)2 could not.

Aminolysis of aryl ester using tertiary amine as amino donor via C-O and C-N bond activations.

An aminolysis reaction between various aryl esters and inert tertiary amines by C-O and C-N bond activations has been developed for the selective synthesis of a broad scope of tertiary amides under neutral and mild conditions. The mechanism may undergo the two key steps of oxidative addition of acyl C-O bond in parent ester and C-N bond cleavage of tertiary amine via an iminium-type intermediate.

Advances in studies of renal adverse reactions of Leonurus heterophyllus / 中国中药杂志

Motherwort (Herb of Leonurus heterophyllus) was a traditional Chinese medicine used for the treatment of various kinds of gynaecological diseases, which was considered as non-toxic medicine since ancient times. However, adverse effects such as kidney damage, uterus damage, allergy and diarrhea were frequently reported recently. This paper reviews the possible target site, toxic dosage, chemical substance and other related factors of these kidney damage caused by motherwort from both the clinic and animal experiment view.

[Study on performance of Ni3 V2O8 catalyst and analysis of X-ray photoelectron spectroscopy].

Ni3V2O8 catalyst was prepared by oxalate co-precipitation method with microwave heating in this paper. In order to study the relationship between the catalytic performance and the surface species, the catalyst was characterized by XRD, BET, H2-TPR, XPS, TEM and conductivity measurement. The surface property of Ni3V2O8 was studied by XPS and the catalytic performance of the oxidative dehydrogenation of propane to propylene was also investigated. The results of XRD showedthat pure Ni3V2O8 with nice structure was obtained. TEM experiments results demonstrated that the prepared Ni3V2O8 catalyst at 700 degrees C calcination showed uniform particle with the mean particle size of 30 nm. The surface area of the catalyst was 8.623 m2 x g(-1). The diagram of the relationship between electrical conductivity and oxygen partial pressure of Ni3V2O8 showed dsigma/dPO2, >0, implying that Ni3V2O8 catalyst was a p-type semiconductor. H2-TPR results showed that only one unsymmetrical reduction peak appeared at 663.5 degreesC within 300-900 degrees C region over Ni3V2O8 catalyst and no obvious shoulder peak was observed. It could also be found that the ratio of non complete reduction oxygen species was about 33.59% (O(-) 27.55%, O2(2-) 6.04%) from the O(1s) XPS result and more V4+ species existed on the Ni3V2O8 catalyst surface. The TPR and XPS results illustrated that the transformation of the lattice oxygen to non-complete reduction oxygen in NiV2O8 catalyst might promote the oxidation-reduction reaction between different valence vanadium and promoted the oxygen vacancy formation. This then led to abundant non-complete reduction oxygen O(-) and V4+ species formation on the surface of Ni3V2O8 catalyst. The active result of oxidative dehydrogenation of propane to propylene showed that the 60.02% propylene selectivity could be reached at 18.60% propane conversion. Compared with the reported results over the coexistent NiO and Ni3V2O8 system from the literature, pure Ni3V2O8 catalyst system in this present paper showed higher propylene selectivity than the coexistent NiO and Ni3V2O8 system under the same propane conversion condition, suggesting that the performance of propane to propene is correlated to the oxidation-reduction of V4+ / V5+ couple and non complete reduction oxygen species (O(-) or O2(2-)). This result further illustrated that NiV2O8 was active phase for oxidative dehydrogenation of propane to propylene. Combining the active and characterization results, it was found that catalytic activity was correlated to the surface non-complete reduction O(-) and V4+ species, which was beneficial to improving the propylene selectivity.

The effect of three steroidal saponins from Yin-tonic herbal medicince on muscarinic cholinergic receptors of cultured rat myocardiac cells / 中国药理学通报

Aim To observe the effect of three steroidal saponins on the M-cholinoceptor density of cultured rat myocardiac cells. Methods The time course of M-cholinoceptor density was observed and diosgenin (DIO),timosaponin aglycone (ZMS,S-configuration) and XMS,a stereoisomeric compound of ZMS in C-25 methyl group,R-configuration) were added to the culture medium from the 12th day of culture at three final concentration of 10~(-7),10~(-6) and 10~(-5) mol?L~(-1),and the M-cholinoceptor density was measured on the 16th day with radioligand binding assay. Results The density of M-cholinoceptor increased gradually at the beginning of culture,reached a plateau at 4～10 days,and then dropped gradually. On the 16th day of culture,the M-cholinoceptor density was about 60% of the plateau value.The up-regulation effect of ZMS on the density of cultured rat myocardiac cells on the 16 th day was only significant at a final concentration of 10~(-5) mol?L~(-1). On the contrary,XMS was effective even when its final concentration was as low as 10~(-7) mol?L~(-1). DIO showed no effect on the M-cholinoceptor density at any of its three concentration. Conclusion The above results indicate that XMS with lower concentration showed similar effect on the M-cholinoceptor density of cultured mylcardiac cells as that of ZMS with more higher concentration.

EFFECTS OF OIL OF PIPER LONGUM UNSAPONIFIABLE MATTER ON CHOLESTEROL METABOLISM IN EXPERIMENTAL HYPERCHO-LESTEROLEMIC MICE / 中国药理学通报

Exogenous hypercholesterolemia in mice was induced by feeding with diets containing 2% cholesterol. It was found that Oil of Piper Longum Unsaponifiable Matter ( OPUM ) at 40mg/kg?d-1 ig for 20d could reduce the levels of total cholesterol (TC). ( LDL + VLDL) - c and the hepatic cholesterol content, increase that of biliary cholesterol in exogenous hypercholesterolemic mice. The hypocholesterolemic effect of OPUM is in a dose-dependent manner over the range of 20~40mg/kg. OPUM at 40mg/kg ig could elevate Lecithin - Cholesterol Acyltransferase ( LCAT ) activity inhibited by treating with ip of yolk. It was suggested that the hypochole-sterol effect of OPUM could be concerned with protectiong cholesterol esterification and be of great advantage to protection from arteriosclerosis arteriosclerosis in mice.