Novel 4-azasteroidal N-glycoside analogues bearing sugar-like D ring: synthesis and anticancer activities

A series of novel N-glycoside analogues with 4-azasteroid moiety bearing sugar-like D ring were conveniently synthesized by constructing the core dihydropyran ring embedded in 4-azasteroidal skeleton which was prepared from 4-aza-5α-androst-3,17-dione 1 in four steps. The structure of 6b were unambiguously proved by the appropriate X-ray structural analysis. Anticancer activity was found for all of the analogues with purinyl moiety against breast cancer (MCF-7), human neuroblastoma (SK-N-SH), cervical cancer cell (HeLa) and prostatic cancer (PC-3), while the analogue 7 containing 1,2,4-triazole heterocycle as the nucleobase was inactive against all of the tested cancer cell lines. The biology results showed the purinyl moiety attached to the pyran ring of 6a-d, substituent at 6'-position of purine base and introduction of a halogen atom at 2'-position of 6'-chloropurine had obviously effect on the evaluated anticancer activity.     

北亚热带马尾松净生产力对气候变化的响应

掌握马尾松生产力与气候变化的关系,特别是在马尾松自然分布的北界研究生产力对气候变化的响应具有重要意义,以马尾松自然分布北界的河南鸡公山国家级自然保护区内的老龄马尾松林作为研究对象,根据河南信阳的马尾松生物量与树高胸径的关系,利用样地调查和年轮宽度推算出过去的30a中的生物量和生产力动态,并用当地的温度、湿度、降水、光照以及帕尔默干旱度指数5项气候因子与生产力做相关分析,在此基础上用多元逐步回归得到了气候因子与生产力的回归方程。结果显示:鸡公山马尾松林生物量从1980年的59.00 t/hm²逐步增加到2009年的254.75 t/hm²,30a中平均年净生产力为6.64 t/hm²;气候分析表明年净生产力与气候因子关系较为密切:上年8月降水、当年2月温度、3月湿度以及10月的光照和温度与生产力正相关,当年5月光照、10月的降水和湿度与生产力负相关,当年2月到9月的PDSI都与生产力正相关,并且在6月的相关系数最高。研究表明,北亚热带的马尾松生产力的年际变化主要是气候因素引起的,受当年生长季的长短和生长季的土壤水分可用性限制,在未来该地区升温增湿的条件下马尾松林的生产力可能会升高。     

Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand

The sigma-2 (σ2) receptor has been suggested to be a promising target for pharmacological interventions to curb tumor progression. Development of σ2-specific ligands, however, has been hindered by lack of understanding of molecular determinants that underlie selective ligand-σ2 interactions. Here we have explored effects of electron donating and withdrawing groups on ligand selectivity for the σ2 versus σ1 receptor using new benzamide-isoquinoline derivatives. The electron-donating methoxy group increased but the electron-withdrawing nitro group decreased σ2 affinity. In particular, an extra methoxy added to the para-position (5e) of the benzamide phenyl ring of 5f dramatically improved (631 fold) the σ2 selectivity relative to the σ1 receptor. This para-position provided a sensitive site for effective manipulation of the sigma receptor subtype selectivity using either the methoxy or nitro substituent. Our study provides a useful guide for further improving the σ2-over-σ1 selectivity of new ligands.     

Prenatal diagnosis in a mentally retarded woman with mosaic ring chromosome 18

We present a pregnant woman with mental retardation and mosaic for ring 18 referred for prenatal diagnosis. Major clinical features included short stature with clinodactyly in feet, foot deformity and club feet, hypotonia, kyphosis, and absence of breast development, low set ears, high arched palate, dental decay and speech disorder. Prenatal diagnosis was carried. Using amniocentesis. The fetus had a normal karyotype described as 46,XX. The fetus was evaluated for clinical features after delivery; she was healthy with no abnormal clinical characterizations.     

Fire history of a prairie/forest boundary: more than 250 years of frequent fire in a North American tallgrass prairie

Questions: Most modern fire‐prone landscapes have experienced disruptions of their historic fire regimes. Are the primary tallgrass prairies of the Flint Hills reflective of a history of continuous fire occurrence? Did fire frequency, severity, size and seasonality change in connection with changes in land use? Has fire occurrence been related to drought conditions? Location: Edges of Cross Timbers forest stands at the Tallgrass Prairie Preserve (TGPP) in the Flint Hills of Osage County, Oklahoma, USA. Methods: Cross‐sections of 76 Quercus stellata were collected from Cross Timbers stands at or near the grassland edge in the TGPP. Dendrochronological methods were used to identify years of formation for tree rings and fire scars. Superposed epoch analysis was used to evaluate the effect of drought conditions on fire occurrence. Results: Fires were recorded in 46.6% of the years between 1729 and 2005. In 41 cross‐sections at one site, the mean fire interval between 1759 and 2003 was 2.59 years, with fire interval decreasing from a mean fire interval of 3.76 years in the early part of the record to 2.13 years in modern times. No extended periods without fire were recorded in the study area. Drought conditions had no significant effect on fire occurrence. Conclusions: In contrast with many fire‐prone landscapes worldwide, the prairies of the Flint Hills have experienced no recent fire suppression or exclusion. Changes in fire frequency mark transitions in land use, primarily from being traditionally used by Native Americans to being managed for cattle production.     

Temperature‐growth divergence in white spruce forests of Old Crow Flats,Yukon Territory,and adjacent regions of northwestern North America

We present a new 23‐site network of white spruce ring‐width chronologies near boreal treeline in Old Crow Flats, Yukon Territory, Canada. Most chronologies span the last 300 years and some reach the mid‐16th century. The chronologies exhibit coherent growth patterns before the 1930s. However, since the 1930s, they diverge in trend and exhibit one of two contrasting, but well‐replicated patterns we call Group 1 and Group 2. Over the instrumental period (1930–2007) Group 1 sites were inversely correlated with previous‐year July temperatures while Group 2 sites were positively correlated with growth‐year June temperatures. At the broader northwestern North America (NWNA) scale, we find that the Group 1 and Group 2 patterns are common to a number of white spruce chronologies, which we call NWNA 1 and NWNA 2 chronologies. The NWNA 1 and NWNA 2 chronologies also share a single coherent growth pattern prior to their divergence (ca. 1950s). Comparison of the NWNA 1/NWNA 2 chronologies against gridded 20th‐century temperatures for NWNA and reconstructed northern hemisphere summer temperatures (ad 1300–2000) indicates that all sites responded positively to temperature prior to the mid‐20th century (at least back to ad 1300), but that some changed to a negative response (NWNA 1) while others maintained a positive response (NWNA 2). The spatial extent of divergence implies a large‐scale forcing. As the divergence appears to be restricted to the 20th century, we suggest that the temperature response shift represents a moisture stress caused by an anomalously warm, dry 20th‐century climate in NWNA, as indicated by paleoclimatic records. However, because some sites do not diverge and are located within a few kilometres of divergent sites, we speculate that site‐level factors have been important in determining the susceptibility of sites to the large‐scale drivers of divergence.     

胃印戒细胞癌与非印戒细胞癌临床病理分析

目的：通过比较胃印戒细胞癌与非印戒细胞癌的临床特征与病理资料,探讨胃印戒细胞癌的临床特征,病理特点及预后。方法：回顾性分析2005年1月至2007年1月在哈尔滨医科大学附属第三医院住院治疗的1138例胃癌患者临床资料,根据组织学类型分为胃印戒细胞癌组和非印戒细胞癌扣对两组的性别、年龄、家族史、肿瘤发生部位、浸润深度、淋巴结转移、远处转移及根治术后中位进展时间、1年生存率和3年生存率进行统计分析比较。结果：胃印戒细胞癌好发于女性（P〈0．05）;年龄≤55岁的患者发病率高于非印戒细胞癌（P〈0．05）,≥56岁的患者发病率低于非印戒细胞癌（P〈0．05）;肿块生长部位以胃中下部为主（P〈0．05）,侵犯胃上部者明显少于非印戒细胞癌（P〈0．05）;胃印戒细胞癌多数在胃壁组织内呈弥漫浸润性生长,垂直浸润能力较弱,突破浆膜层者明显少于非印戒细胞癌（P〈0．05）;根治术后中位进展时间胃印戒细胞癌（10个月）较非印戒细胞癌（12个月）提前2个月,进展风险增加（P〈0．05）;胃印戒细胞癌在家族史、淋巴结转移、远处转移及根治术后1年和3年生存率方面与非印戒细胞癌比较无差异。结论：胃印戒细胞癌多发于中青年女性;好发年龄小于56岁;发病部位以胃中下部为主;多呈弥漫性浸润性生长,且较少突破浆膜层;中位进展时间短,进展风险高。     

Potato Cell Plasma Membrane Receptors to Ring Rot Pathogen Extracellular Polysaccharides

The interaction of extracellular polysaccharides (EPS) of the potato ring rot bacterial pathogen Clavibacter michiganensis ssp. sepedonicus (Spieck. et Kott.) Skaptason et Burkh. (Cms) with protoplasts isolated both from leaf cells of plants grown in vitro and microsomal membrane fractions obtained from cell suspension cultures of two potato (Solanum tuberosum L.) cultivars contrasted by their resistance to this pathogen was studied. The EPS intensively bind to protoplast surfaces and microsomal membranes of the susceptible cultivar but not to those of the resistant cultivar. Treatment with protease, excess of unlabelled EPS, and with dextran, did not lead to the binding of fluorochrome‐labelled EPS to protoplasts and microsomal membranes (from both cultivars). It is proposed that (a) a great number of receptors to EPS Cms are present in the plasma membranes of potato cells of susceptible cultivars, (b) these receptors contain proteinaceous sites exposed on the external side of the plasma membrane which participate in EPS binding, and (c) the plasma membranes of cells of resistant cultivars contain a small but sufficient quantity of receptors to EPS able to induce defensive responses in plants.     

Neue,chlorsubstituierte thiophenacetylenverbindungen mit ungewöhnlicher struktur aus Helichrysum-arten

The investigation of two further Helichryswn species afforded in addition to known constituents three new thiophene compounds with unusual structures. A biogenetic scheme of aromatic ring formation for this new type of chlorine containing compounds is proposed. Most probably, the pyran ring of the chloroenol ether is transformed to an aromatic ring by dehydrogenation, hydrolysis and intramolecular aldol condensation.