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.

Tissue specific delivery of estrone-conjugated siRNAs.

An estrone phosphoramidite, synthesized in a single step, was directly incorporated at the 5' ends of small interfering RNAs (siRNAs). The resulting estrone-conjugated siRNAs readily pass through cellular membranes and down-regulate the target protein, and show specific distributions in vivo.

Identification and Analysis of the Chloroplast rpoC1 Gene Differentially Expressed in Wild Ginseng.

Panax ginseng is a well-known herbal medicine in traditional Asian medicine, and wild ginseng is widely accepted to be more active than cultivated ginseng in chemoprevention. However, little has actually been reported on the difference between wild ginseng and cultivated ginseng. Thus, to identify and analyze those differences, we used suppressive subtraction hybridization (SSH) sequences with microarrays, realtime polymerase chain reaction (PCR), and reverse transcription PCRs (RT-PCRs).

Complexation and conjugation approaches to evaluate siRNA delivery using cationic, hydrophobic and amphiphilic peptides.

In this study, we used solid phase synthesis to prepare three kinds of peptides and then formulated their peptide-siRNA complexes and peptide-siRNA conjugates. Both the complexation and conjugation systems were nontoxic and allowed the delivery of siRNA into the cytoplasm without the need for any transfection agents and with subsequent inhibition of gene expression.

Evaluation of physicochemical properties, skin permeation and accumulation profiles of salicylic acid amide prodrugs as sunscreen agent.

Various amide prodrugs of salicylic acid were synthesised, and their physicochemical properties including lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skin permeation and accumulation profiles were also evaluated using a combination of common permeation enhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain.

Evaluation of salicylic acid fatty ester prodrugs for UV protection.

The purpose of this study was to investigate the physicochemical properties and in vitro evaluation of fatty ester prodrugs of salicylic acid for ultraviolet (UV) protection. The physicochemical properties such as lipophilicity, chemical stability and enzymatic hydrolysis were investigated with the following fatty ester prodrugs of salicylic acid: octanoyl (C8SA), nonanoyl (C9SA), decanoyl (C10SA), lauroyl (C12SA), myristoyl (C14SA) and palmitoyl oxysalicylate (C16SA). Furthermore, their skin permeation and accumulation were evaluated using a combination of common permeation enhancing techniques such as the use of a lipophilic receptor solution, removal of stratum corneum and delipidization of skin.

Cationic nucleolipids as efficient siRNA carriers.

We synthesized five novel uridine-based cationic nucleolipids, introducing basic amino acid residues at the 5' position of uridine, through 1,3-dipolar cycloaddition, and hydrophobic alkyl moieties at the 2' and 3' positions, through carbamate linkages. Their lipoplexes delivered siRNAs efficiently to cells, in vitro, without any severe toxicity.

Hemin inhibits hypertensive rat vascular smooth muscle cell proliferation through regulation of cyclin D and p21.

We tested the hypothesis that HO-1 (heme oxygenase-1) activity varied between vascular smooth muscle cells (VSMC) in spontaneously hypertensive (SHR) and normotensive Wistar-Kyoto (WKY) rats. HO-1 levels were measured under baseline and hemin-stimulated conditions and cell proliferation was monitored. Basal HO-1 levels in untreated cells were lower in SHR compared to WKY rats.