ent-Pimarane Diterpenes from the Aerial Parts of Siegesbeckia pubescens

Five new ent-pimarane diterpenes ( 1 – 5 ) and five known analogs ( 6 – 10 ) were isolated from the aerial parts of Siegesbeckia pubescens. Their structures, including absolute configurations, were determined by comprehensive spectroscopic methods especially 1D and 2D NMR and quantum chemical electronic circular dichroism calculations. All the isolated compounds were evaluated for their cytotoxicity against human BT549, A549 and H157 cancer cell lines. Among them, compounds 1 and 2 showed mild cytotoxicity against lung cancer cell lines H157 with IC₅₀ values of 16.35±2.59 and 18.86±4.83 μM, respectively.     

中国汉族人群间-α-胰蛋白酶抑制因子(ITI)的遗传多态性

我们建立了测定间-α-胰蛋白酶抑制因子遗传表型的聚丙烯酰胺凝胶等电聚焦免疫固定技术,应用这种方法对居住在成都地区的汉族群体进行了群体研究和家系调查,结果表明中国汉族人群间-α-胰蛋白酶抑制因子具有遗传多态性,它有希望成为法医血液遗传学新的遗传标记。     

Development of acute thermotolerance in L929 cells: lack of HSP28 synthesis and phosphorylation.

We investigated the correlation between the development of acute thermotolerance and the phosphorylation, synthesis, and expression of the HSP28 family in murine L929 cells. Following heating at 43 degrees C for 30 min, thermotolerance developed rapidly in exponential-phase cells and reached its maximum 4-9 h after heat shock. Maximal thermal resistance was maintained for 24 h and then gradually decayed. However, heat-induced phosphorylation of HSP28 was not detected. Furthermore, HSP28 synthesis during incubation at 37 degrees C for 12 h following heat shock was not detected by [3H]-leucine labeling followed by two-dimensional polyacrylamide gel electrophoresis. In addition, Northern blots failed to demonstrate expression of the HSP28 gene. Unlike HSP28, the expression of constitutive and inducible HSP70 genes, along with the synthesis of their proteins, was observed during incubation at 37 degrees C after heat shock. These results demonstrate that HSP28 synthesis and its phosphorylation are not required to develop acute thermotolerance in L929 cells.     

Dasymaschalon tibetense (Annonaceae): a new species from China

A new species, Dasymaschalon tibetense, has been described from South Tibet, China. The species is related to D. rostratum, but can be easily distinguished by its rounded apex of fruitlets and its 7.7–9.5 cm long petals.     

硒对培养人胚肝细胞Ⅲ型前胶原,羟脯氨酸合成的影响

原代培养人胚肝细胞经１．１５６×１０￣(－７）ｍｏｌ／Ｌ硒预处理４ｈ,加入２０ｍｍｏｌ／Ｌ四氟化碳作用２０ｈ,观察硒对其Ⅲ型前胶原（ＰＣⅢ）和羟脯氨酸（Ｈｙｐ）生成的影响。结果培养液中ＰＣⅢ水平、细胞内Ｈｙｐ含量及细胞内外丙二醛（ＭＤＡ）水平均降低,与未加硒对照组比较差别有显著性（Ｐ＜０．０１）。而硒谷腕甘肽过氧化物酶（Ｓｅ－ＧＳＨ－ＰＸ）活性则较对照组显著增高（Ｐ＜０．００１）,且ＰＣⅢ水平与Ｓｅ－ＧＳＨ－Ｐ＿Ｘ／ＭＤＡ比值呈负相关（ｒ＝－０．９１５６,Ｐ＜０．０１）。提示硒可提高Ｓｅ－ＧＳＨ－Ｐ＿Ｘ／ＭＤＡ比值,抑制脂质过氧化激发的肝细胞胶原合成。     

真菌诱导子对悬浮培养西洋参细胞的生理效应

报道了不同真菌诱导子对悬浮培养的西洋参（Ｐａｎａｘｑｕｉｎｑｕｅｆｏｌｉｕｍ）细胞生长、皂甙和多糖合成,以及细胞内和培养液中过氧化物酶活性的生理效应。悬浮培养的西洋参细胞经刺盘孢菌（Ｃｏｌｌｅｔｏｔｒｉｃｈｕｍｎｉｃｏｌｔｉａｎａｅ）丝体诱导子处理后,总皂甙产率可由对照的２９６ｍｇ／Ｌ增加到６７９ｍｇ／Ｌ（约占细胞干重的（１６．３％）,比对照提高约１．３倍,而且总皂甙的８５％排放在培养液中;经黑曲霉（Ａｓｐｅｒｇｉｌｌｕｓｎｉｇｒａｎ）诱导子处理后,细胞多糖含量可达到１１．７９％（细胞干重）,比对照增加１倍多。初步纯化的刺盘孢菌丝体诱导子和尖孢镰刀菌（Ｆｕｓｕｒｉｕｍｏｘｙｓｐｏｒｕｍ）滤液诱导子在诱导处理前期能明显促进西洋参细胞生长,同时细胞内及培养液中过氧化物酶活性显著增加;随时间延长,细胞生长和酶活性逐步受到抑制。     

黄芪有效成分对氧自由基清除作用的ESR研究

用电子自旋共振技术研究了黄芪总黄酮(TFA)、黄芪总皂甙(TSA)和黄芪总多糖(TPA)对次黄嘌呤／黄嘌呤氧化酶体系产生的超氧阴离子自由基和H₂O₂－Fe²⁺体系产生的羟自由基的清除作用．结果表明,这3种成分均有清除氧自由基的作用;对超氧阴离子自由基的清除效能大于对羟自由基的清除作用;其作用强度依次为TFA＞TSA＞TPA．结果提示清除氧自由基可能是黄芪抗衰老的主要机理之一,TFA和TSA是黄芪抗氧化作用的主要药理活性成分．     

The design and pharmacology of novel selective muscarinic agonists and antagonists

The muscarinic pharmacology of C1-methyl-substituted chiral compounds related to McN-A-343 and of (R)- and (S)-dimethindene has been studied. Among the McN-A-343 analogues, the (S)-enantiomers were more potent and had higher affinity than the (R)-isomers. The quaternary compound (S)-BN 228 was found to be the most potent M1-selective agonist known today (pEC50: M1/rabbit vas deferens = 7.83; M2/guinea-pig atria = 6.35; M3/guinea-pig ileum = 6.29). In both the atria and ileum the tertiary carbamate, (S)-4-F-MePyMcN, was a competitive antagonist (pA2 value = 7.39 and 6.82, respectively). In contrast, in rabbit vas deferens (S)-4-F-MePyMcN was a potent partial agonist (pEC50 = 7.22; apparent efficacy = 0.83). These results indicate that (S)-4-F-MePyMcN might be a useful tool to study M1 receptor-mediated effects involved in central cholinergic function. (S)-Dimethindene was a potent M2-selective antagonist (pA2 = 7.86/atria; pKi = 7.8/rat heart) with lower affinities for the M1 (pA2 = 6.36/rat duodenum; pKi = 7.1/NB-OK 1 cells), M3 (pA2 = 6.92/guinea-pig ileum; pKi = 6.7/rat pancreas) and M4 receptors (pKi = 7.0/rat striatum). It was more potent (up to 41-fold) than the (R)-isomer. In contrast, the stereoselectivity was inverse at ileal H1 receptors (pA2: (R)-isomer = 9.42; (S)-isomer = 7.48). Thus, (S)-dimethindene could be a valuable agent to test the hypothesis that M2 antagonists show beneficial effects in the treatment of cognitive disorders. It might also become the starting point for the development of diagnostic tools for quantifying M2 receptors in the CNS with PET imaging.