Cancer-specific gene silencing through therapeutic siRNA delivery with B vitamin-based nanoassembled low-molecular-weight hydrogelators.

This paper describes the synthesis, characterization, and in vitro and in vivo siRNA transfection ability of B vitamin-based cationic clickable bolaamphiphiles (VBs). Our VBs derived from vitamins B₂, B₃, B₅, B₆, and B₇ formed nanoassembled low-molecular-weight hydrogelators (LMWGs, vitagels). The vitagels VB2, VB6, and VB7 (derived from vitamins B₂, B₆, and B₇, respectively) facilitated delivery of small interfering RNAs (siRNA), efficiently silencing gene expression specifically into cancer cell lines; in addition, the LMWGs derived from vitamins B₃, B₅, and B₆ were biocompatible.

Electrochemical discrimination of phthalic acid among three phthalic acid isomers based on an N-butylaminomethyl-ferrocene derivative.

A chemosensor compound (1) consisting of a central ferrocene with two butylaminomethyl arms showed unexpected facile electrochemical oxidation of the secondary amines in proximity to the ferrocene, which was utilized for electrochemical discrimination of phthalic acid selectively over two other isomers, isophthalic acid and terephthalic acid.

N-cholesteryl amino acid conjugates and their antimicrobial activities.

A series of N-cholesteryl amino acid conjugates have been synthesized using a reductive amination protocol in good yield and purity. All the synthesized conjugates were evaluated for their in vitro antimicrobial activities against Gram positive and Gram negative bacteria. Among the conjugates tested, N-cholesteryl GABA 12 showed the highest potency toward the methicillin-resistant Staphylococcus aureus with the lowest MIC value of 2 μg/mL.

Synthesis and antimicrobial activity of imidazole and pyridine appended cholestane-based conjugates.

A series of 3α-amino-5α-cholestane and 3α,7α-diamino-5α-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3α,7α-Di(pyridylmethyl)amino-5α-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 μg/mL.