We describe a novel two-step method, starting from bulk silicon wafers, to construct DNA conjugated silicon nanoparticles (SiNPs). This method first utilizes reactive high-energy ball milling (RHEBM) to obtain alkene grafted SiNPs. The alkene moieties are subsequently reacted with commercially available thiol-functionalized DNA via thiol–ene click chemistry to produce SiNP DNA conjugates wherein the DNA is attached through a covalent thioether bond. Further, to show the utility of this synthetic strategy, we illustrate how these SiNP ODN conjugates can detect cancer-associated miR-21 via a fluorescence ON strategy. Given that an array of biological molecules can be prepared with thiol termini and that SiNPs are biocompatible and biodegradable, we envision that this synthetic protocol will find utility in salient SiNP systems for potential therapeutic and diagnostic applications.

A napthalimide based fluorescenct sensor displaying a significant increase in emission upon binding CB[7] with excellent pH stability was developed and utilized in a surface-bound displacement assay for the rapid detection of CB[7] encapsulation of therapeutically relevant drug classes. Previously unknown binders with moderate to strong affinities were discovered.

CD437 (6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid) is a novel synthetic retinoic acid derivative that has been shown to selectively induce apoptosis in human lung cancer cells. This compound, however, is limited in its application due to its low solubility in aqueous solutions. One technique for increasing the solubility and bioavailability of a cytotoxic agent is the formation of inclusion complexes with cyclodextrins. Herein, we report the formation and characterization of a 2:1 complex between β-cyclodextrin (β-CD) and CD437. It is shown that CD437 is a tight binder of β-CD with an overall association constant of 2.6 ± 0.6 ×10 7 M −2 . In addition, we demonstrate (a) that β-CD-derived complexation enhances the aqueous solubility of CD437, and (b) that a significant increase in the toxicity of CD437 against a human lung adenocarcinoma cell line can be achieved by co-treatment with β-CD. Keywordscyclodextrin; inclusion complex formation; supramolecular chemistry; anticancer agent CD437 (6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid) is a synthetic retinoic acid (RA) derivative which is known to have antineoplastic properties across a variety of cancer cell lines, including lung, 1 prostate, 2 ovarian, 3-4 cervical, 5 and head and neck. 6 Typically, the molecular action of retinoids depends on the binding to and activation of a subset of the nuclear hormone receptor superfamily which contains both retinoic acid receptors (RARs) and retinoid X receptors (RXRs), each of which is encoded by three genes, α, β, and γ. CD437, like RA, can bind directly to a heterodimer formed between retinoic acid receptor γ (RARγ) and a retinoid X receptor (RXR). Growth arrest and cell differentiation then occur when the activated RARγ/RXR dimer binds to a RA response element on DNA. 7 In contrast to RA, however, CD437 also displays strong apoptotic properties. In addition to the RARγ-dependent pathway, CD437 is also able to exert its * Corresponding Author: J. Jayawickramarajah, Tel.: +01-504-862-3580, Fax: +01-504-865-5596, jananj@tulane.edu. † Department of Medicine ‡ Department of Chemistry Supplementary data Supplementary data associated with this article can be found, in the online version, at xxx Publisher's Disclaimer: This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final citable form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. NIH Public Access NIH-PA Author ManuscriptNIH-PA Author Manuscript NIH-PA Author Manuscript apoptotic effects through an RARγ-independent pathway. 8 Thus CD437 has been shown to induce apoptosis in both RA-resistant cell lines [8][9] and RARγ-negative cell lines. 8,10 Despite the significant anti...