Synthesis and structure-activity relationship of tyrosinase inhibiting novel bi-heterocyclic acetamides: Mechanistic insights through enzyme inhibition,kinetics and computational studies

The present research was designed for the selective synthesis of novel bi-heterocyclic acetamides, 9a-n, and their tyrosinase inhibition to overwhelm the problem of melanogenesis. The structures of newly synthesized compounds were confirmed by spectral techniques such as ¹H NMR, ¹³C NMR, and EI-MS along with elemental analysis. The inhibitory effects of these bi-heterocyclic acetamides (9a-n) were evaluated against tyrosinase and all these molecules were recognized as potent inhibitors relative to the standard used. The Kinetics mechanism was analyzed by Lineweaver-Burk plots which explored that compound, 9h, inhibited tyrosinase competitively by forming an enzyme-inhibitor complex. The inhibition constants K_i calculated from Dixon plots for this compound was 0.0027 µM. The computational study was coherent with the experimental records and these ligands exhibited good binding energy values (kcal/mol). The hemolytic analysis revealed their mild cytotoxicity towards red blood cell membranes and hence, these molecules can be pondered as nontoxic medicinal scaffolds for skin pigmentation and related disorders.     

Ecotypic differentiation reveals seed colour‐related alkaloid content in a crop wild relative

• Crop wild relatives can be a useful source of genotypes that maximise crop survival and yield in specific habitats. Lupinus angustifolius is an annual forb with crop varieties derived from a narrow genetic basis but that are cultivated worldwide. Its seeds have high nutritional value, but they naturally contain alkaloids with anti‐nutritive factors. The study of its wild populations can be useful to find genotypes that contribute to higher climate resilience and greater yield under stressing environmental conditions.
• Using a common garden, we evaluated ecotypic differentiation in four natural populations from two contrasting latitudes in terms of plant biomass, seed mass and number, alkaloid content in seeds for the three main alkaloids present in the plant and seed colour, including its possible influence on post‐dispersal predation. Correlations among traits were also assessed.
• We found differences among populations for all traits except final biomass. Northern populations had lighter seeds and a tendency to yield more seeds when they produced white seeds, compared to southern populations and variegated seeds. Regardless of latitude, populations showed differences in alkaloid concentration, with all three alkaloids found generally in high or low concentrations in each population. Proportion of white seed morphs varied in each population. Seed colour did not influence predator preference. In addition, white seed colour was related to a low alkaloid content.
• Our results evidence the existence of natural ecotypic differentiation in L. angustifolius not only due to latitudinal range, but also to local environmental factors. White seed coat colour could be used as a visual clue for identification of low‐alkaloid genotypes, a priority trait in L. angustifolius breeding programmes.

     

Detecting a hierarchical genetic population structure: the case study of the Fire Salamander (Salamandra salamandra) in Northern Italy

The multistep method here applied in studying the genetic structure of a low dispersal and philopatric species, such as the Fire Salamander Salamandra salamandra, was proved to be effective in identifying the hierarchical structure of populations living in broad‐leaved forest ecosystems in Northern Italy. In this study, 477 salamander larvae, collected in 28 sampling populations (SPs) in the Prealpine and in the foothill areas of Northern Italy, were genotyped at 16 specie‐specific microsatellites. SPs showed a significant overall genetic variation (Global F_ST = 0.032, P < 0.001). The genetic population structure was assessed by using STRUCTURE 2.3.4. We found two main genetic groups, one represented by SPs inhabiting the Prealpine belt, which maintain connections with those of the Eastern foothill lowland (PEF), and a second group with the SPs of the Western foothill lowland (WF). The two groups were significantly distinct with a Global F_ST of 0.010 (P < 0.001). While the first group showed a moderate structure, with only one divergent SP (Global F_ST = 0.006, P < 0.001), the second group proved more structured being divided in four clusters (Global F_ST = 0.017, P = 0.058). This genetic population structure should be due to the large conurbations and main roads that separate the WF group from the Prealpine belt and the Eastern foothill lowland. The adopted methods allowed the analysis of the genetic population structure of Fire Salamander from wide to local scale, identifying different degrees of genetic divergence of their populations derived from forest fragmentation induced by urban and infrastructure sprawl.     

雾灵山国家自然保护区森林群落物种多样性研究

在样方法获取全面资料并用数量方法确定森林群落类型的基础上,对雾灵山国家自然保护区各森林群落的物种多样性(D)、生态优势度(C)、群落均匀度(J)等指标进行了计测;并着重对物种多样性进行评价,分析了物种多样性变化的时空规律,就物种多样性的保护与持续利用进行探讨。分析结果表明：雾灵山国家自然保护区森林群落物种多样性比较丰富,其D值在2.37～4.17之间;在特定高度范围内,随海拔增高D值增大,C值变小;多数森林群落灌木层的D值高于乔木层,C值低于乔木层;地带性群落的D值大于非地带性群落,C值相反。     

Contaminant sources, distribution and fate in the Athabasca, Peace and Slave River Basins, Canada

Northern river ecosystems worldwide are under increasing environmental stress from degrading developments that influence water quality and associated ecological integrity. In particular, contaminant-related threats to these systems are rising from enhanced industrial and municipal effluent discharges along with elevated non-point source inputs related to land-use activities such as forestry, agriculture, mining and long-range atmospheric transport. In this regard, the contaminants program of the Northern River Basins Study (NRBS) in western Canada identified key contaminant sources to the Athabasca, Slave and Peace river basins (particularly related to pulp-mill developments) and assessed their environmental fate and distribution in water and sediments. The study also developed and employed new analytical approaches and generated improved models to predict contaminant transport and fate in the aquatic environment and related food webs. Consequently the study focused on those contaminant families identified in characterization studies as arising from key point- and non-point sources within the basins or as being of greatest toxicological significance. These included resin acids, polychlorinated dioxins and furans, polychlorinated biphenyls, chlorinated phenolics, polyaromatic hydrocarbons and selected heavy metals such as mercury. Low or non-detectable concentrations of a number of contaminant groups were found in the ambient water phase including chlorinated phenolics, some chlorinated dioxins and furans and some resin acids. For both suspended and depositional sediments, significant declines were observed over the study period for the major chlorinated contaminant groups tested, correlating directly with the implementation of improved effluent treatment in many of the pulp mills located in the basins. In general, the environmental levels of chlorinated organic and metal contaminants in water or sediments were low and within Canadian health or environmental guidelines. It is hoped that the approaches used and lessons learned from the NRBS will be of use to others assessing contaminant and multiple stressor issues in other large river ecosystems.     

光、暗处理对蚕豆茎内皮层形成的影响 Ⅱ.与栓化作用有关的酶及抗氧化剂的关系

以蚕豆（ＶｉｃｉａｆａｂａＬ．）幼苗为材料,结合不同的光强及黑暗对茎中内皮层形成的影响,对参与栓化作用有关的酶活性及内源抗氧化物质的含量进行了测定,并讨论了光对内皮层形成的调节机制。实验结果表明,高光强抑制茎中内皮层形成,而低光强和黑暗诱导茎中形成内皮层。在低光强和暗中,脂肪氧化酶在内皮层栓化前期活性显著增加,可能与栓化作用的启动有关,而高光强下ＬＯＸ始终处在较低水平。ＰＡＬ活性为光所诱导,与内皮层的栓化没有直接的相关性。在高光强条件下生长的幼苗茎中抗坏血酸和谷胱甘肽含量比低光强和暗中的高。外源施用抗坏血酸,可抑制低光强下茎内皮层的栓化,而对暗中茎内皮层的栓化无影响。推测高强度光对栓化作用的抑制原因可能是高光强下植物体内有高含量的抗氧化物质,并具备更有利的活性氧清除途径,从而抑制了栓化作用的进行     

宗教文化对鼎湖山森林资源保护的影响

根据现有的文献史料和保护区内历代留存的碑刻,探讨了不同历史时期内鼎湖山宗教文化的兴衰,历代僧侣对鼎湖山森林实行禁伐保护的管理措施,以及对森林资源保护和森林群落演替的影响。从而提出,仅就文字记载来看,鼎湖山代表性植被——南亚热带季风常绿阔叶林群落受禁伐保护始于1633年,迄今已有366年的保护历史,其中庆云寺僧人实行禁伐保护的历史长达319年。宗教文化是鼎湖山森林群落及生物多样性保存完好的重要原因之一。     

青冈常绿阔叶林主要植物种叶片的光合特性及其群落学意义

 青冈(Quercus glauca)林乔木层主要树种叶片的净光合速率日进程在春夏季晴天均有明显午休。常绿树种的光合速率在秋季最高,大量换叶期最低,冬季仍有一定的净光合量。落叶树种的光合速率和光合产量低于常绿树种,随着群落的发育其地位将降低。青冈和石栎(Lithocarpus glaber)的光合速率接近,但青冈能够利用较弱的光,因而其高叶量的树冠具有较高的光合总量,以保持其在群落中的优势种地位;石栎主要利用较强的光,其较低叶量的树冠可以维持较高的光合总量,以保证其次优势种地位。灌木、草本层种类光合日进程均为单峰型。灌木种类对光的需求较高。蕨类植物耐荫强,因而在林中能占有稳定的伴生地位。     

浙江天童常绿阔叶林地被层的研究

 对天童常绿阔叶林地被层植物种类组成及群落学作用进行了初步研究。研究表明：组成地被层计有维管植物44科78属114种。蕨类植物优势度最大,里白占绝对优势。39种草木植物,以世界分布科和地面芽植物为主,常绿种类占84.6％,未见亚洲和北美洲间断分布的地理成分。乔灌木幼苗51种,80%的苗量集中于4～6个种中,优势种突出。藤本植物24种,草质藤本占25％,落叶种类42％。地面苔藓植物(22种)与枯枝落叶构成镶嵌分布,发育较成熟的群落中苔藓种类多,盖度大。里白及其枯死物形成层层交错重叠的地被层,阻碍凋落物进入地表,减弱光照,使近地表光照长期低于幼苗光补偿点,抑制了乔灌木优势种的更新。凋落物阻碍种子下移至半分解层,栲树种子下移率为17％至22.3％,冬季种子的动物损耗率平均为98.2％,凋落物中种子的平均腐烂率为28.2％,表层保存下来的栲树种子因缺水萌发速度慢且成活率低,下层萌发速度虽快,但腐烂率高,栲树天然更新幼苗主要来源于草窗。     

鼎湖山季风常绿阔叶林黄果厚壳桂群落植物元素含量特征

研究鼎湖山南亚热带季风常绿阔叶林黄果厚壳桂群落元素含量特征 ,分析了其中 9个种不同器官的 6种元素含量 ,结果表明 :1 )群落中植物不同器官的元素含量大小为 ,N:叶 >皮 >根 >枝 >茎 ,P:叶 >枝、皮 >根 >茎 ,K:叶 >皮 >枝 >根 >茎 ,Ca:皮 >叶 >枝 >根 >,Mg:叶 >皮 >根 >枝 >茎。 2 )椎栗、黄果厚壳桂、鼎湖钓樟和双盖蕨是群落中含 N量较高的种 ;椎栗、云南银柴和双盖蕨含 P量较高 ;各个种的含 K量相似。 3)养分含量表现出一定的层次性差异 ,上层种叶子含 P量高于下层种 ,但含 K量区别不显著。上层种茎 N、P、K含量显著低于下层种。黄果厚壳桂种群 ,其不同层次个体养分含量没有统计上的显著差异 ,但下层个体茎养分高 ,上层个体茎养分低。 4)群落不同元素间具有许多显著相关的元素对 ,其中 N与其它元素的相关性最大 ,其次是 Mg、P,再次是 K,而 Na不与其它任何元素相关 ,Ca相关性很少。从器官角度看 ,茎所含相关元素对最多 ,而枝、皮最少。