Lactate esters are widely used as food additives, perfume materials, medicine additives, and personal care products. The objective
of this work was to investigate the effect of a series of lactate esters as penetration enhancers on the in vitro skin permeation of four drugs with different physicochemical properties, including ibuprofen, salicylic acid, dexamethasone
and 5-fluorouracil. The saturated donor solutions of the evaluated drugs in propylene glycol were used in order to keep a
constant driving force with maximum thermodynamic activity. The permeability coefficient (Kp), skin concentration of drugs (SC), and lag time (T), as well as the enhancement ratios for Kp and SC were recorded. All results indicated that lactate esters can exert a significant influence on the transdermal delivery
of the model drugs and there is a structure-activity relationship between the tested lactate esters and their enhancement
effects. The results also suggested that the lactate esters with the chain length of fatty alcohol moieties of 10–12 are more
effective enhancers. Furthermore, the enhancement effect of lactate esters increases with a decrease of the drug lipophilicity,
which suggests that they may be more efficient at enhancing the penetration of hydrophilic drugs than lipophilic drugs. The
influence of the concentration of lactate esters was evaluated and the optimal concentration is in the range of 5∼10 wt.%.
In sum, lactate esters as a penetration enhancer for some drugs are of interest for transdermal administration when the safety
of penetration enhancers is a prime consideration. 相似文献
During community assembly, plant functional traits are under selective pressure from processes operating at multiple spatial scales. However, in fragmented landscapes, there is little understanding of the relative importance of local-, patch- and landscape-scale processes in shaping trait distributions. Here, we investigate cross-scale influences of landscape change on traits that dictate plant life history strategies in re-assembling plant communities in a fragmented landscape in eastern China. Using forest dynamics plots (FDPs) on 29 land-bridge islands in which all woody plants have been georeferenced and identified to species, we characterized and derived two composite measures of trait variation, representing variation across the leaf economics spectrum and plant size. We then tested for trait shifts in response to local-, patch- and landscape-scale factors, and their potential cross-scale interactions. We found substantial community-wide trait changes along local-scale gradients (i.e. forest edge to interior): more acquisitive leaf economic traits and larger sized species occurred at edges, with a significant increase in trait means and trait range. Moreover, there were significant cross-scale interaction effects of patch and landscape variables on local-scale edge effects. Altered spatial arrangement of habitat in the surrounding landscape (i.e. declining habitat amount and increasing patch density), as well as decreasing area at the patch level, exacerbated edge effects on traits distributions. We suggest that synergistic interactions of landscape- and patch-scale processes, such as dispersal limitation, on local-scale environmental filtering at edges, together shape the spatial distributions of plant life history strategies in fragmented plant communities. 相似文献
Winter low temperature disturbance in the southern subtropics has important effects on the weed community structure, but the role of uniquely low temperatures in biological invasions is unclear. Here, we examined the competitive effects of an invasive plant, Bidens pilosa L., and its native congener, Bidens biternata (Lour.) Merr. et Sherff, during high and low temperature seasons to determine whether low temperatures promote the competitiveness of B. pilosa in the southern subtropics of China. The growth and physiological responses of the two Bidens species to low (10/5 °C) and optimum (30/25 °C) temperatures were examined to determine how the invasive B. pilosa responds to low temperature stress. Our results showed that the competitive balance index values of B. pilosa in low temperature seasons were significantly higher than those in high temperature seasons, which implied that low temperatures may be more beneficial to the competitiveness of B. pilosa than high temperatures in the southern subtropics. The smaller decline in the relative growth rate and the photosynthetic ability of B. pilosa compared with B. biternata under low temperature stress indicated that the former was less negatively affected by low temperature than the latter. A higher DPPH· (1.1-diphenyl-2-picrylhy-drazyl) scavenging rate and greater heat-stable protein content in B. pilosa under low temperatures might help the invasive plant to maintain more effective physiological functions and thus a higher growth rate. Overall, the uniquely low temperature in the southern subtropics of China is expected to promote the invasiveness of the exotic B. pilosa.
Designing protein sequences that fold to a given three-dimensional (3D) structure has long been a challenging problem in computational structural biology with significant theoretical and practical implications. In this study, we first formulated this problem as predicting the residue type given the 3D structural environment around the Cα atom of a residue, which is repeated for each residue of a protein. We designed a nine-layer 3D deep convolutional neural network (CNN) that takes as input a gridded box with the atomic coordinates and types around a residue. Several CNN layers were designed to capture structure information at different scales, such as bond lengths, bond angles, torsion angles, and secondary structures. Trained on a very large number of protein structures, the method, called ProDCoNN (protein design with CNN), achieved state-of-the-art performance when tested on large numbers of test proteins and benchmark datasets. 相似文献