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Total 1090 results found since Jan 2013.

Molecules, Vol. 23, Pages 1586: The Mechanism for siRNA Transmembrane Assisted by PMAL
nnan Lu The capacity of silencing genes makes small interfering RNA (siRNA) appealing for curing fatal diseases. However, the naked siRNA is vulnerable to and degraded by endogenous enzymes and is too large and too negatively charged to cross cellular membranes. An effective siRNA carrier, PMAL (poly(maleic anhydride-alt-1-decene) substituted with 3-(dimethylamino) propylamine), has been demonstrated to be able to assist siRNA transmembrane by both experiments and molecular simulation. In the present work, the mechanism of siRNA transmembrane assisted by PMAL was studied using steered molecular dynamics simulations bas...
Source: Molecules - June 29, 2018 Category: Chemistry Authors: Yanfei Lu Jipeng Li Nan Su Diannan Lu Tags: Article Source Type: research

Molecules, Vol. 27, Pages 1936: A Comprehensive Computational Investigation into the Conserved Virulent Proteins of Shigella species Unveils Potential Small-Interfering RNA Candidates as a New Therapeutic Strategy against Shigellosis
In this study, we analyzed 264 conserved sequences from 15 different conserved virulence genes of Shigella sp., through extensive rational validation using a plethora of first-generation and second-generation computational algorithms for siRNA designing. Fifty-eight siRNA candidates were obtained by using the first-generation algorithms, out of which only 38 siRNA candidates complied with the second-generation rules of siRNA designing. Further computational validation showed that 16 siRNA candidates were found to have a substantial functional efficiency, out of which 11 siRNA candidates were found to be non-immunogenic. Fi...
Source: Molecules - March 17, 2022 Category: Chemistry Authors: Parag Palit Farhana Tasnim Chowdhury Namrata Baruah Bonoshree Sarkar Sadia Noor Mou Mehnaz Kamal Towfida Jahan Siddiqua Zannatun Noor Tahmeed Ahmed Tags: Article Source Type: research

Molecules, Vol. 28, Pages 2191: Potential of siRNA-Bearing Subtilosomes in the Treatment of Diethylnitrosamine-Induced Hepatocellular Carcinoma
grawal Mohammad Owais Therapeutics, based on small interfering RNA (siRNA), have demonstrated tremendous potential for treating cancer. However, issues such as non-specific targeting, premature degradation, and the intrinsic toxicity of the siRNA, have to be solved before they are ready for use in translational medicines. To address these challenges, nanotechnology-based tools might help to shield siRNA and ensure its specific delivery to the target site. Besides playing a crucial role in prostaglandin synthesis, the cyclo-oxygenase-2 (COX-2) enzyme has been reported to mediate carcinogenesis in various types of canc...
Source: Molecules - February 27, 2023 Category: Chemistry Authors: Fauzia Jamal Ghufran Ahmed Mohammad Farazuddin Ishrat Altaf Saba Farheen Qamar Zia Asim Azhar Hira Ahmad Aijaz Ahmed Khan Satyanarayana Somavarapu Anshu Agrawal Mohammad Owais Tags: Article Source Type: research

Molecules, Vol. 21, Pages 1279: Development of an Innovative Intradermal siRNA Delivery System Using a Combination of a Functional Stearylated Cytoplasm-Responsive Peptide and a Tight Junction-Opening Peptide
In this study, we examined intradermal siRNA permeability in the tape-stripped (20 times) back skin of mice or AD-like skin of auricles treated with 6-carboxyfluorescein-aminohexyl phosphoramidite (F AM)-labeled siRNA, the tight junction modulator AT1002, and the functional cytoplasm-responsive stearylated peptide STR-CH2R4H2C by using confocal laser microscopy. We found that strong fluorescence was observed deep and wide in the epidermis and dermis of back skin and AD-like ears after siRNA with STR-CH2R4H2C and AT1002 treatment. After 10 h from administration, brightness of FAM-siRNA was significantly higher for STR-CH2R4...
Source: Molecules - September 23, 2016 Category: Chemistry Authors: Hisako Ibaraki Takanori Kanazawa Yuuki Takashima Hiroaki Okada Yasuo Seta Tags: Article Source Type: research

Molecules, Vol. 21, Pages 1334: Targeted Delivery of siRNA to Transferrin Receptor Overexpressing Tumor Cells via Peptide Modified Polyethylenimine
In conclusion, the HAI peptide may be useful to target TfR overexpressing tumors in targeted gene and siRNA delivery approaches.
Source: Molecules - October 9, 2016 Category: Chemistry Authors: Yuran Xie Bryan Killinger Anna Moszczynska Olivia Merkel Tags: Article Source Type: research

Molecules, Vol. 22, Pages 231: Construction and Biological Evaluation of a Novel Integrin ανβ3-Specific Carrier for Targeted siRNA Delivery In Vitro
Conclusion: The chimeric peptide of c(RGD)2-9R can be developed as an effective siRNA delivery carrier and shows potential as a new strategy for RNAi-based gene therapy.
Source: Molecules - February 3, 2017 Category: Chemistry Authors: Xueqi Chen Meng Liu Rongfu Wang Ping Yan Chunli Zhang Chao Ma Lei Yin Tags: Article Source Type: research

Molecules, Vol. 24, Pages 2211: Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
i Studies on siRNA delivery have seen intense growth in the past decades since siRNA has emerged as a new class of gene therapeutics for the treatment of various diseases. siRNA bioconjugate, as one of the major delivery strategies, offers the potential to enhance and broaden pharmacological properties of siRNA, while minimizing the heterogeneity and stability-correlated toxicology. This review summarizes the recent developments of siRNA bioconjugate, including the conjugation with antibody, peptide, aptamer, small chemical, lipidoid, cell-penetrating peptide polymer, and nanoparticle. These siRNA bioconjugate, either ...
Source: Molecules - June 12, 2019 Category: Chemistry Authors: Wanyi Tai Tags: Review Source Type: research

Molecules, Vol. 28, Pages 1618: A Novel Hybridization LC-MS/MS Methodology for Quantification of siRNA in Plasma, CSF and Tissue Samples
sian Therapeutic oligonucleotides, such as antisense oligonucleotide (ASO) and small interfering RNA (siRNA), are a new class of therapeutics rapidly growing in drug discovery and development. A sensitive and reliable method to quantify oligonucleotides in biological samples is critical to study their pharmacokinetic and pharmacodynamic properties. Hybridization LC-MS/MS was recently established as a highly sensitive and specific methodology for the quantification of single-stranded oligonucleotides, e.g., ASOs, in various biological matrices. However, there is no report of this methodology for the bioanalysis of doubl...
Source: Molecules - February 8, 2023 Category: Chemistry Authors: Long Yuan Jean-Fran çois Dupuis Kevork Mekhssian Tags: Article Source Type: research

Molecules, Vol. 27, Pages 1302: Selenocystine-Derived Label-Free Fluorescent Schiff Base Nanocomplex for siRNA Delivery Synergistically Kills Cancer Cells
In this study, we developed a nanocarrier for siRNA based on a selenocystine analog engineered polyetherimide and achieved traceable siRNA delivery and the synergic killing of tumor cells. Notably, we applied the label-free Schiff base fluorescence mechanism, which enabled us to trace the siRNA delivery and to monitor the selenocystine analogs’ local performance. A novel selenocystine-derived fluorescent Schiff base linker was used to crosslink the polyetherimide, thereby generating a traceable siRNA delivery vehicle with green fluorescence. Moreover, we found that this compound induced tumor cells to undergo...
Source: Molecules - February 15, 2022 Category: Chemistry Authors: Yang Liu Haoying Yang Qian Liu Mingming Pan Danli Wang Shiyuan Pan Weiran Zhang Jinfeng Wei Xiaowei Zhao Junfeng Ji Tags: Article Source Type: research

Molecules, Vol. 25, Pages 2692: Lipid and Polymer-Based Nanoparticle siRNA Delivery Systems for Cancer Therapy
les RNA interference (RNAi) uses small interfering RNAs (siRNAs) to mediate gene-silencing in cells and represents an emerging strategy for cancer therapy. Successful RNAi-mediated gene silencing requires overcoming multiple physiological barriers to achieve efficient delivery of siRNAs into cells in vivo, including into tumor and/or host cells in the tumor micro-environment (TME). Consequently, lipid and polymer-based nanoparticle siRNA delivery systems have been developed to surmount these physiological barriers. In this article, we review the strategies that have been developed to facilitate siRNA survival in the ci...
Source: Molecules - June 9, 2020 Category: Chemistry Authors: Francesco Mainini Michael R. Eccles Tags: Review Source Type: research

Molecules, Vol. 25, Pages 2714: Conjugation of Doxorubicin to siRNA Through Disulfide-based Self-immolative Linkers
Debart Co-delivery systems of siRNA and chemotherapeutic drugs have been developed as an attractive strategy to optimize the efficacy of chemotherapy towards cancer cells with multidrug resistance. In these typical systems, siRNAs are usually associated to drugs within a carrier but without covalent interactions with the risk of a premature release and degradation of the drugs inside the cells. To address this issue, we propose a covalent approach to co-deliver a siRNA-drug conjugate with a redox-responsive self-immolative linker prone to intracellular glutathione-mediated disulfide cleavage. Herein, we report the use...
Source: Molecules - June 10, 2020 Category: Chemistry Authors: Florian Gauthier Jean-R émi Bertrand Jean-Jacques Vasseur Christelle Dupouy Fran çoise Debart Tags: Article Source Type: research

Molecules, Vol. 26, Pages 3238: Size- and Surface- Dual Engineered Small Polyplexes for Efficiently Targeting Delivery of siRNA
This study provides a promising strategy to engineer the size and surface of polyplexes, allowing long blood circulation and targeted delivery of siRNA.
Source: Molecules - May 27, 2021 Category: Chemistry Authors: Shuang Liu Shaohui Deng Xiaoxia Li Du Cheng Tags: Article Source Type: research

Molecules, Vol. 27, Pages 1170: Effect of Cationic Lipid Nanoparticle Loaded siRNA with Stearylamine against Chikungunya Virus
In this study, nanodelivery systems (hybrid polymeric/solid lipid nanoparticles) using cationic lipids (stearylamine, C9 lipid, and dioctadecylamine) and polymers (branched PEI-g-PEG -PEG) were prepared, characterized, and complexed with siRNA. The four developed delivery systems (F1,F2,F3, and F4) were assessed for stability and potential toxicities against CHIKV. In comparison to the other nanodelivery systems, F4 containing stearylamine (Octadecylamine; ODA), with an induced optimum cationic charge of 45.7 mV in the range of 152.1 nm, allowed maximum siRNA complexation, better stability, and higher transfection, with st...
Source: Molecules - February 9, 2022 Category: Chemistry Authors: Manish Kumar Jeengar Mallesh Kurakula Poonam Patil Ashwini More Ramakrishna Sistla Deepti Parashar Tags: Article Source Type: research

Molecules, Vol. 27, Pages 4377: Tetrazine-Induced Bioorthogonal Activation of Vitamin E-Modified siRNA for Gene Silencing
Xinjing Tang The temporal activation of siRNA provides a valuable strategy for the regulation of siRNA activity and conditional gene silencing. The bioorthogonal bond-cleavage reaction of benzonorbonadiene and tetrazine is a promising trigger in siRNA temporal activation. Here, we developed a new method for the bio-orthogonal chemical activation of siRNA based on the tetrazine-induced bond-cleavage reaction. Small-molecule activatable caged siRNAs were developed with the 5′-vitamin E-benzonobonadiene-modified antisense strand targeting the green fluorescent protein (GFP) gene and the mitotic kinesin-5 ...
Source: Molecules - July 8, 2022 Category: Chemistry Authors: Xueli Zhang Amu Gubu Jianfei Xu Ning Yan Wenbo Su Di Feng Qian Wang Xinjing Tang Tags: Article Source Type: research

Molecules, Vol. 22, Pages 86: Novel PEI/Poly-γ-Gutamic Acid Nanoparticles for High Efficient siRNA and Plasmid DNA Co-Delivery
In this study, we created a very high efficient DNA/siRNA co-delivery system by incorporating a negatively-charged poly- γ-glutamic acid (γ-PGA) into PEI/nucleic acid complexes. Spherical nanoparticles with about 200 nm diameter were formed by mixing PEI/plasmid DNA/siRNA/γ-PGA (dual delivery nanoparticles; DDNPs) with specific ratio (N/P/C ratio) and the particles present positive surface charge under all manufact uring conditions. The gel retardation assay shows both nucleic acids were effectively condensed by PEI, even at low N/P ratios. The PEI-based DDNPs reveal excellent DNA/siRNA transfection efficiency in the hu...
Source: Molecules - January 3, 2017 Category: Chemistry Authors: Shu-Fen Peng Hung-Kun Hsu Chun-Cheng Lin Ya-Ming Cheng Kuang-Hsing Hsu Tags: Article Source Type: research