Synthesis and Cytotoxic Studies of Undecenoic Acid-based Schiffs Base Derivatives Bearing 1,2,4-Triazole Moiety

Ethosomes® are one of the main deformable vesicles proposed to overcome the stratum corneum. They are composed of lecithin, ethanol and water, resulting in round vesicles characterized by a narrow size distribution and a negative surface charge. Taking into account their efficiency to deliver drugs into deeper skin layers, the current study was designed to evaluate the influence of different lipids on the physico-chemical features of traditional ethosomes in the attempt to influence their fate. Three lipids (DOPE, DSPE and DOTAP) were used for the study, but only DOTAP conferred a net positive charge to ethosomes, maintaining a narrow mean size lower than 300 nm and a good polydispersity index. Stability and in vitro cytotoxic studies have been performed using Turbiscan Lab analysis and MTT dye exclusion assay, respectively. Data recorded demonstrated the good stability of modified ethosomes and a reasonable absence of cell mortality when applied to human keratinocytes, NCTC 2544, which are used as a cell model. Finally, the best formulations were selected to evaluate their ability to encapsulate drugs, through the use of model compounds. Cationic ethosomes encapsulated oil red o and rhodamine b in amounts comparable to those recorded from conventional ethosomes (over 50%). Results recorded from this study are encouraging as cationic ethosomes may open new opportunities for skin delivery.

Download Full-text

Pulchinenosides from Pulsatilla Chinensis Increase P-Glycoprotein Activity and Induce P-Glycoprotein Expression

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2020/4861719 ◽

2020 ◽

Vol 2020 ◽

pp. 1-8

Author(s):

Yali Liu ◽

Ling Zhang ◽

Shaofeng Wei ◽

Jinyang Cai ◽

Zhenzhong Zang ◽

...

Keyword(s):

Membrane Vesicles ◽

Pcr Analysis ◽

Mrna Levels ◽

Intestinal Epithelial ◽

Glycoprotein P ◽

P Glycoprotein ◽

Human Intestinal Epithelial Cells ◽

Pulsatilla Chinensis ◽

Dependent Transport ◽

Cytotoxic Studies

Five pulchinenosides (pulchinenoside B3, pulchinenoside BD, pulchinenoside B7, pulchinenoside B10, and pulchinenoside B11) isolated from Pulsatilla chinensis (Bge) Regel saponins extract exhibited strong antitumor activities but poor gastrointestinal absorption properties. The enteric induction of P-glycoprotein (P-gp) is understood to restrict the oral bioavailability of some pharmaceutical compounds and lead to adverse drug reactions. Therefore, the present investigation was intended to delineate the impacts of pulchinenosides on cellular P-gp function and expression using Sf9 membrane vesicles and LS180 cells as a surrogate of human intestinal epithelial cells. Preliminary cytotoxic studies showed that 10 μM was an acceptable concentration for cytotoxicity and antiproliferation studies for all pulchinenosides using the alamarBlue assay. The cell cycle of LS180 cells detected by flow cytometry was not significantly influenced after 48 hours of coincubation with 10 μM of pulchinenosides. In the presence of pulchinenosides, the ATP-dependent transport of N-methyl-quinidine mediated by P-glycoprotein was stimulated significantly. The upregulation of P-glycoprotein and mRNA levels was found by Western blot and real-time PCR analysis in LS180 cells. Parallel changes indicate that all pulchinenosides are exposed to pulchinenosides-mediated transcriptional regulation. In conclusion, pulchinenosides could induce P-glycoprotein expression and directly increase its functional activity.

Download Full-text

Preparation and Characterization of a Novel Terbium Complex Coordinated with 10-Undecenoic Acid for UV-Cured Coatings

International Journal of Polymer Science ◽

10.1155/2020/2175259 ◽

2020 ◽

Vol 2020 ◽

pp. 1-8

Author(s):

Chenjie Jiao ◽

Rong Zhong ◽

Yanfang Zhou ◽

Hongfei Zhang

Keyword(s):

Rare Earth ◽

Green Light ◽

Precipitation Method ◽

Rare Earth Complex ◽

Terbium Complex ◽

Uv Curable ◽

Good Thermal Stability ◽

Potential Applications ◽

Undecenoic Acid ◽

The Rare Earth

A UV-cured composite containing a rare earth complex was prepared for this study. First, the photoluminescent terbium complex was synthesized with a long-chain unsaturated fatty acid (10-Undecenoic acid) by a solution precipitation method, resulting in the 10-UA-Tb(III) complex. Its structure was proven by FTIR, elemental analysis, XRD, and TGA. The results indicated that the organic acid ligand successfully coordinated with the Tb3+ ion and that the complex had a chelate bidentate structure. The emission spectrum of the 10-UA-Tb(III) complex indicated that the complex can emit a bright green light with the unique luminescence of the Tb3+ ion. Furthermore, the luminescence properties of complexes with different ratios of Tb3+ and ligand were studied, and the ratio of Tb3+ and the ligand had an obvious impact on the luminescence intensity of the 10-UA-Tb(III) complex. Subsequently, the prepared rare earth complex was doped into a UV-cured coating in different proportions to obtain a UV-cured composite. The morphology of the rare earth UV-cured composite was observed by SEM. The images showed that the rare earth complex was dispersed uniformly in the polymer matrix. Moreover, the composites could emit fluorescence. Additionally, it has good thermal stability and compatibility with the resin. Therefore, these composites should have potential applications in UV curable materials, such as luminescence coatings.

Download Full-text