Five New Guaiane Sesquiterpenes from the Endophytic Fungus Xylaria sp. YM 311647 of Azadirachta indica

Five new guaiane sesquiterpenes, 1 – 5 , were isolated from the culture broth of the endophytic fungus Xylaria sp. YM 311647, isolated from Azadirachta indica A. Juss . The structures of these compounds were elucidated on the basis of spectroscopic analyses, and their inhibitory activities against five pathogenic fungi were evaluated. All guaiane sesquiterpenes showed moderate or weak antifungal activities in a broth microdilution assay.     

Atherosclerosis,Oxidation and Endometriosis

Endometriosis affects younger women of childbearing age. Atherosclerosis is considered as a disease of the old and increases with the ageing process. Both diseases are characterized by the increased presence of activated macrophages and associated increases in growth promoting activity and the production of inflammatory cytokines. In this review, we propose that oxidative stress and the presence of forms of oxidized low-density lipoprotein (LDL) might contribute to both Atherosclerosis and Endometriosis.     

Asymmetric reduction of prochiral ketones to chiral alcohols catalyzed by plants tissue

As an important organic compound, chiral alcohols are the key chiral building blocks to many single enantiomer pharmaceuticals. Asymmetric reduction of the corresponding prochiral ketones to produce the chiral alcohols by biocatalysis is one of the most promising routes. Asymmetric reduction of different kinds of non-natural prochiral ketones catalyzed by various plants tissue was studied in this work. Acetophenone, 4'-chloroacetophenone and ethyl 4-chloroacetoacetate were chosen as the model substrates for simple ketone, halogen-containing aromatic ketone and beta-ketoesters, respectively. Apple (Malus pumila), carrot (Daucus carota), cucumber (Cucumis sativus), onion (Allium cepa), potato (Soanum tuberosum), radish (Raphanus sativus) and sweet potato (Ipomoea batatas) were chosen as the biocatalysts. It was found that these kinds of prochiral ketoness could be reduced by these plants tissue with high enantioselectivity. Both R- and S-form configuration chiral alcohols could be obtained. The e.e. and chemical yield could reach about 98 and 80% respectively for acetophenone and 4'-chloroacetophenone reduction reaction with favorable plant tissue. And the e.e. and yield for ethyl 4-chloroacetoacetate reduction reaction was about 91 and 45% respectively.     

Combination of newly developed high quality <Emphasis Type="Italic">Fuqu</Emphasis> with traditional <Emphasis Type="Italic">Daqu</Emphasis> for <Emphasis Type="Italic">Luzhou-flavor</Emphasis> liquor brewing

Application of a compound starter composed of traditional Daqu, high quality Fuqu developed previously in our lab, and alcohol-producing and aroma-producing yeasts in the brewing of Luzhou-flavor liquor was investigated. Compared with traditional Daqu, the compound starter demonstrated apparently higher starch utilization and alcohol productivity both in flasks and in pits. Flavor ingredient analyses showed that the flavor ingredient compositions of liquors produced with the compound starter were similar to those obtained with the traditional process. With appropriate after treatments, the compound starter may be applied in distilleries for elevating the productivity of traditional liquor or producing high quality new-style distilled liquor. As starch utilization can be increased significantly, using this compound starter in liquor brewing is especially meaningful for lessening environmental pollution. These findings may also be helpful for further understanding the mechanisms of Chinese liquor brewing.     

Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents

Based on a shared structural core of diarylamine in several known anticancer drugs as well as a new cytotoxic hit 6-chloro-2-(4-cyanophenyl)amino-3-nitropyridine (7), 30 diarylamines and diarylethers were designed, synthesized, and evaluated for cytotoxic activity against A549, KB, KB-vin, and DU145 human tumor cell lines (HTCL). Four new leads 11e, 12, 13a, and 13b were discovered with GI(50) values ranging from 0.33 to 3.45μM. Preliminary SAR results revealed that a diarylamine or diarylether could serve as an active structural core, meta-chloro and ortho-nitro groups on the A-ring (either pyridine or phenyl ring) were necessary and crucial for cytotoxic activity, and the para-substituents on the other phenyl ring (B-ring) were related to inhibitory selectivity for different tumor cells. In an investigation of potential biological targets of the new leads, high thoughput kinase screening discovered that new leads 11e, 12 and 13b especially inhibit Mer tyrosine kinase, a proto-oncogene associated with munerous tumor types, with IC(50) values of 2.2-3.0μM. Therefore, these findings provide a good starting point to optimize a new class of compounds as potential anticancer agents, particularly targeting Mer tyrosine kinase.     

不同光强对吴茱萸生长动态和光合日变化的影响

报道了不同生长光强(透光率分别为15%、30%、50%、100%)对吴茱萸的生长和光合日变化的影响。结果表明:生长环境光强对吴茱萸苗期株高、地径和冠面积的影响较大,100%RI下的株高、地径和冠面积明显小于各遮荫处理,其中30%RI下吴茱萸的株高、地径和冠面积最大,这表明苗期强光不利于吴茱萸的生长。随着光强的减弱,吴茱萸增大冠面积与株高有利于截获更多光能。10月下旬,100%RI下吴茱萸净光合速率(Pn)日变化曲线呈"双峰型",11:30～14:30,吴茱萸的Pn、胞间二氧化碳浓度与气孔导度均下降,表明此时的光合午休现象是由气孔部分关闭造成的。各遮荫处理下,吴茱萸的Pn日变化均呈"单峰型",并无第二峰的出现,可能与遮荫条件下,下午光强较弱,环境温度较高,空气相对湿度较低有关。     

Natural Killer Cells Are Characterized by the Concomitantly Increased Interferon-γ and Cytotoxicity in Acute Resolved Hepatitis B Patients

Natural killer (NK) cells are abundant in the liver and have been implicated in inducing hepatocellular damage in patients with chronic hepatitis B virus (HBV) infection. However, the role of NK cells in acute HBV infection remains to be elucidated. We comprehensively characterized NK cells and investigated their roles in HBV clearance and liver pathology in 19 chronic hepatitis B (CHB) patients and 21 acute hepatitis B (AHB) patients as well as 16 healthy subjects. It was found that NKp46⁺ NK cells were enriched in the livers of AHB and CHB patients. We further found that peripheral NK cells from AHB patients expressed higher levels of activation receptors and lower levels of inhibitory receptors than those from CHB patients and HC subjects, thus displaying the increased cytolytic activity and interferon-γ production. NK cell activation levels were also correlated positively with serum alanine aminotransferase levels and negatively with plasma HBV DNA levels in AHB patients, which is further confirmed by the longitudinal follow-up of AHB patients. Serum pro-inflammatory cytokine and chemokine levels were also increased in AHB patients as compared with CHB and HC subjects. Thus, the concomitantly increased interferon-γ and cytotoxicity of NK cells were associated with liver injury and viral clearance in AHB patients.