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Molecules, Vol. 26, Pages 4626: Cholesterol Sequestration from Caveolae/Lipid Rafts Enhances Cationic Liposome-Mediated Nucleic Acid Delivery into Endothelial Cells
In this study, we demonstrated that the transient modulation of caveolae/lipid rafts mediated endocytosis with the cholesterol-sequestrating agents, nystatin, filipin III, and siRNA against Cav-1, which significantly increased the transfection properties of cationic lipid-(2-hydroxy-N-methyl-N,N-bis(2-tetradecanamidoethyl)ethanaminium chloride), namely, amide liposomes in combination with 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (AD Liposomes) in liver sinusoidal endothelial cells (SK-Hep1). In particular, nystatin was found to be highly effective with 2–3-fold enhanced transfection efficacy when compared wit...
Source: Molecules - July 30, 2021 Category: Chemistry Authors: Santhosh Chandar Maddila Chandrashekhar Voshavar Porkizhi Arjunan Rashmi Prakash Chowath Hari Krishna Reddy Rachamalla Balaji Balakrishnan Poonkuzhali Balasubramanian Rajkumar Banerjee Srujan Marepally Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2119: A Versatile Solid-Phase Approach to the Synthesis of Oligonucleotide Conjugates with Biodegradable Hydrazone Linker
aminova One of the ways to efficiently deliver various drugs, including therapeutic nucleic acids, into the cells is conjugating them with different transport ligands via labile or stable bonds. A convenient solid-phase approach for the synthesis of 5′-conjugates of oligonucleotides with biodegradable pH-sensitive hydrazone covalent bonds is proposed in this article. The approach relies on introducing a hydrazide of the ligand under aqueous/organic media to a fully protected support-bound oligonucleotide containing aldehyde function at the 5′-end. We demonstrated the proof-of-principle of this approach by synthesiz...
Source: Molecules - April 7, 2021 Category: Chemistry Authors: Mariya I. Meschaninova Nina S. Entelis Elena L. Chernolovskaya Alya G. Venyaminova Tags: Article Source Type: research

Molecules, Vol. 25, Pages 1877: Trimeric Small Interfering RNAs and Their Cholesterol-Containing Conjugates Exhibit Improved Accumulation in Tumors, but Dramatically Reduced Silencing Activity
ernolovskaya Cholesterol derivatives of nuclease-resistant, anti-MDR1 small-interfering RNAs were designed to contain a 2’-OMe-modified 21-bp siRNA and a 63-bp TsiRNA in order to investigate their accumulation and silencing activity in vitro and in vivo. The results showed that increasing the length of the RNA duplex in such a conjugate increases its biological activity when delivered using a transfection agent. However, the efficiency of accumulation in human drug-resistant KB-8-5 cells during delivery in vitro in a carrier-free mode was reduced as well as efficiency of target gene silencing. TsiRNAs dem...
Source: Molecules - April 17, 2020 Category: Chemistry Authors: Ivan V. Chernikov Daniil V. Gladkikh Ulyana A. Karelina Mariya I. Meschaninova Alya G. Ven ’yaminova Valentin V. Vlassov Elena L. Chernolovskaya Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3413: Design of Peptidomimetic Functionalized Cholesterol Based Lipid Nanoparticles for Efficient Delivery of Therapeutic Nucleic Acids
a Baigude Lipid nanoparticles (LNP) are the most potent carriers for the delivery of nucleic acid-based therapeutics. The first FDA approved a short interfering RNA (siRNA) drug that uses a cationic LNP system for the delivery of siRNA against human transthyretin (hTTR). However, preparation of such LNP involves tedious multi-step synthesis with relatively low yields. In the present study, we synthesized cationic peptidomimetic functionalized cholesterol (denote Chorn) in straightforward chemical approaches with high yield. When formulated with helper lipids, Chorn LNPs complexed with siRNA to form nanoparticles with a...
Source: Molecules - September 18, 2019 Category: Chemistry Authors: Ehexige Ehexige Tsogzolmaa Ganbold Xiang Yu Shuqin Han Huricha Baigude Tags: Article Source Type: research