Verbascoside isolated from Tectona grandis mediates gastric protection in rats via inhibiting proton pump activity

Evidences have suggested that Tectona grandis (TG) attenuates gastric mucosal injury; however its mechanism has not yet been established. The aim of present study was to evaluate the gastroprotective mechanism of ethanolic extract of TG (E-EtOH), butanolic fraction (Fr-Bu) and to identify its active constituents. Anti-ulcer activities were evaluated against cold restraint (CRU) and pyloric ligation (PL) induced gastric ulcer models and further confirmed through H⁺ K⁺-ATPase inhibitory activity. Cytoprotective activity was evaluated in alcohol (AL) induced gastric ulcer model and further through PGE₂ level. E-EtOH and Fr-Bu attenuated ulcer formation in CRU. Moreover E-EtOH and Fr-Bu displayed potent anti-secretory activity as evident through reduced free acidity and pepsin activity in PL, confirmed further by in vitro inhibition of H⁺ K⁺-ATPase activity. In addition cytoprotective potential of E-EtOH and Fr-Bu were apparent with protection in AL model, increased PGE₂ content and enhanced mucin level in PL. Phytochemical investigations of Fr-Bu yielded terpenoides and a phenolic glycoside, verbascoside. The anti-secretory mechanism of verbascoside mediated apparently through inhibition of H⁺ K⁺-ATPase with corresponding decrease in plasma gastrin level, is novel to our finding. Gastroprotection elicited by TG might be through proton pump inhibition and consequent augmentation of the defensive mechanism.     

短期NaCl胁迫对西伯利亚白刺幼苗Na~+、K~+分配和平衡的影响

[目的]为探究西伯利亚白刺盐适应机制。[方法]以1年生西伯利亚白刺水培幼苗为材料,研究不同浓度NaCl(0、200、300 mmol·L-1)胁迫24 h后根系Na~+、K~+离子流的动态变化(利用扫描离子选择微电极技术,SIET)及植株各器官中Na~+、K~+含量的静态变化(利用电感耦合等离子体光谱仪,ICP-OES)。[结果]表明:(1)短期NaCl胁迫显著提高了西伯利亚白刺根、茎、叶中Na~+含量,其中,叶中Na~+含量是根中的3倍以上;西伯利亚白刺根、茎、叶中K~+含量保持稳定或上升;(2)盐胁迫下,西伯利亚白刺根、茎、叶中K~+/Na~+呈下降趋势,其中,在200、300 mmol·L-1NaCl胁迫下,根中K~+/Na~+差异不显著;(3)离子流结果显示,NaCl胁迫显著提高了西伯利亚白刺根系Na~+的外流;对照和200 mmol·L-1NaCl胁迫下,K~+净流量分别为156、159 pmol·cm-2·s-1,差异不显著;300 mmol·L-1NaCl胁迫显著提高了K~+的内流,净流量为-370 pmol·cm-2·s-1。[结论]综合分析认为,西伯利亚白刺通过叶片对Na~+区隔,加强根系对Na~+的外排和K~+内流,进而维持植株根系K~+/Na~+的相对平衡,以此适应盐渍环境。     

重金属Pb2+和Cd2+对毛竹种子萌发及幼苗早期生长的影响

以毛竹种子为试材,研究不同浓度铅离子(Pb2+)、镉离子(Cd2+)对毛竹种子萌发和幼苗早期生长的影响。结果表明:随着Pb2+和Cd2+浓度的增加,毛竹种子的发芽率呈现出先升高后降低的趋势,发芽指数、活力指数均与浓度呈负相关关系;同时,Pb2+和Cd2+对幼苗根伸长、芽伸长及生物量积累等指标具有显著的抑制作用,并且这种抑制作用随着浓度的升高而增强,尤其是根部,根伸长抑制率最高分别达到96.20%和94.00%;幼苗地上部分与地下部分对Pb2+、Cd2+的积累随着胁迫强度的增加而升高,但地下部分的积累量要显著高于前者,相同浓度下最高差距分别达到地上部分的27.21、6.25倍。     

Mechanism-based CYP2D6 inactivation by acridone alkaloids of Indonesian medicinal plant Lunasia amara

Fourteen acridone alkaloids isolated from Lunasia amara Blanco were tested for their mechanism-based inhibition on human liver microsomal dextromethorphan O-demethylation activity, a prototype marker for cytochrome P450 2D6 (CYP2D6). Among the 14 compounds, 5-hydroxygraveroline (1), 8-methoxyifflaiamine (2), lunamarine (3), and lunine (12) increased their inhibitory activity with increasing preincubation time. Then, we further examined the possibility of mechanism-based inhibition on 5-hydroxygraveroline (1) and lunamarine (3), which showed the potent inhibition. Further investigations on 1 and 3 showed that the characteristic time- and concentration-dependent inhibition, which required a catalytic step with NADPH, was not protected by nucleophiles, and was decreased by the presence of a competitive inhibitor. Thus, 1 and 3 were concluded as mechanism-based inactivators of CYP2D6.     

Fire intensity effects on seed germination of native and invasive Eastern deciduous forest understory plants

Low-intensity fires were important for maintaining the structure of Eastern deciduous forests (EDFs) for thousands of years before European settlement of North America, though fire suppression became a standard management practice in the 1930s. More recently, prescribed fires have been reintroduced to EDF habitats to aid in the restoration of native plant diversity, but invasions of non-native species such as Microstegium vimineum (Japanese stiltgrass) may increase prescribed fire intensity and suppress colonization of native species. As fire becomes a more common management tool in these habitats, it is vital to predict fire temperature effects on the native and non-native species present in the system. In this study, we found that prescribed fires in areas invaded by Microstegium can be 250-300 °C hotter than fires in nearby native-dominated areas. We then compared the effects of fire on germination rates of six native and three non-native EDF understory species representing the range of functional groups common in this habitat. We manipulated both fire intensity (temperature and length of exposure) and type of fire effect (direct flame and indirect furnace heat) to generate germination curves and make predictions about potential prescribed fire effects on populations of these species. There were very different responses among species to both direct (flame) and indirect (furnace) heating. Germination of three native species, Lycopus americana (American water horehound), Verbesina alternifolia (wingstem), and Vernonia gigantea (tall ironweed), showed signs of being stimulated by heating at low temperatures, while germination of all non-native species (M. vimineum, Elaeagnus umbellata, and Schedonorus phoenix) were inhibited at these lower intensities. High fire intensity (temperatures above 300 °C) effectively killed most species, though one native species, Senna hebacarpa (American senna) and one non-native species, E. umbellata (autumn olive), were capable of tolerating 500 °C temperatures. We conclude that high-intensity prescribed fires in habitats invaded by Microstegium may reduce seed germination of some non-native species, but may also inhibit the regeneration of native understory species.