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Condition: Cholesterol

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Total 572 results found since Jan 2013.

Cholesterol Grafted Cationic Lipopolymers: Potential siRNA Carriers for Selective Chronic Myeloid Leukemia (CML) Therapy.
This article is protected by copyright. All rights reserved. PMID: 31714657 [PubMed - as supplied by publisher]
Source: Biomed Res - November 11, 2019 Category: Research Authors: Remant KC, Thapa B, Valencia-Serna J, Domun SS, Dimitroff C, Jiang X, Uludağ H Tags: J Biomed Mater Res A Source Type: research

siRNA Delivery into Tumor Cells by Cationic Cholesterol Derivative-Based Nanoparticles and Liposomes.
In this study, we synthesized new diamine-type cationic cholesteryl carbamate (OH-C-Chol, cholesteryl (2-((2-hydroxyethyl)amino)ethyl)carbamate) and triamine-type carbamate (OH-NC-Chol, cholesteryl (2-((2-((2-hydroxyethyl)amino)ethyl)amino)ethyl)carbamate), and prepared cationic nanoparticles composed of OH-C-Chol or OH-NC-Chol with Tween 80 (NP-C and NP-NC, respectively), as well as cationic liposomes composed of OH-C-Chol or OH-NC-Chol with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (LP-C and LP-NC, respectively) for evaluation of their possible use as siRNA delivery vectors. LP-C and LP-NC/siRNA complexes (lip...
Source: Biological and Pharmaceutical Bulletin - March 8, 2015 Category: Drugs & Pharmacology Authors: Hattori Y, Hara E, Shingu Y, Minamiguchi D, Nakamura A, Arai S, Ohno H, Kawano K, Fujii N, Yonemochi E Tags: Biol Pharm Bull Source Type: research

siRNA-Loaded Polyion Complex Micelle Decorated with Charge-Conversional Polymer Tuned to Undergo Stepwise Response to Intra-Tumoral and Intra-Endosomal pHs for Exerting Enhanced RNAi Efficacy.
This study aimed to develop an siRNA-loaded polyion complex (PIC) micelle equipped with a smart polymeric shell featuring tumor-targetability and endosome-escapability for enhanced RNAi activity in cancer cells. To this end, an acidic pH-responsive polypeptide was designed to exert a stepwise change in its charged state from negative to modestly positive and highly positive in response to slightly acidic environment of tumor (pH ~6.7) and further lowered-pH condition of late endosomal compartments (pH ~5.0), respectively, for selective binding to cancer cell surface and subsequent endosome disruption. This polypeptide, ter...
Source: Biomacromolecules - November 30, 2015 Category: Biochemistry Authors: Tangsangasaksri M, Takemoto H, Naito M, Maeda Y, Sueyoshi D, Kim HJ, Miura Y, Ahn J, Azuma R, Nishiyama N, Miyata K, Kataoka K Tags: Biomacromolecules Source Type: research

Mono-arginine Cholesterol-based Small Lipid Nanoparticles as a Systemic siRNA Delivery Platform for Effective Cancer Therapy
This study describes the development of neutral, small lipid nanoparticles (SLNPs) made of a nontoxic cationic cholesterol derivative, as a suitable carrier of systemic siRNA to treat cancers. The cationic cholesterol derivative, mono arginine-cholesterol (MA-Chol), was synthesized by directly attaching an arginine moiety to cholesterol via a cleavable ester bond. siRNA-loaded SLNPs (siRNA@SLNPs) were prepared using MA-Chol and a neutral helper lipid, dioleoyl phosphatidylethanolamine (DOPE), as major components and a small amount of PEGylated phospholipid mixed with siRNA. The resulting nanoparticles were less than ~...
Source: Theranostics - June 5, 2016 Category: Molecular Biology Authors: Jinju Lee, Phei Er Saw, Vipul Gujrati, Yonghyun Lee, Hyungjun Kim, Sukmo Kang, Minsuk Choi, Jae-Il Kim, Sangyong Jon Tags: Research Paper Source Type: research

Co-delivery of paclitaxel and anti-survivin siRNA via redox-sensitive oligopeptide liposomes for the synergistic treatment of breast cancer and metastasis
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Xinyan Chen, Yidi Zhang, Chunming Tang, Chunli Tian, Qiong Sun, Zhigui Su, Lingjing Xue, Yifan Yin, Caoyun Ju, Can Zhang The overexpression of survivin in breast cancer cells is an important factor of paclitaxel (PTX) resistance in breast cancer. To overcome PTX resistance and improve the antitumor effect of PTX, we developed a novel liposome-based nanosystem (PTX/siRNA/SS-L), composed of a redox-sensitive cationic oligopeptide lipid (LHSSG2C14) with a proton sponge effect, natural soybean phosphatidylcholin...
Source: International Journal of Pharmaceutics - June 29, 2017 Category: Drugs & Pharmacology Source Type: research

Development and characterization of a novel cationic PEGylated niosome-encapsulated forms of doxorubicin, quercetin and siRNA for the treatment of cancer by using combination therapy.
Authors: Hemati M, Haghiralsadat F, Yazdian F, Jafari F, Moradi A, Malekpour-Dehkordi Z Abstract The aim of this study was to optimize the cationic PEGylated niosome-containing anti-cancer drugs and siRNA to enhance the therapeutic response. Therefore, various surfactant-based (tween-60) vesicles of doxorubicin (DOX; a chemotherapeutic drug) and quercetin (QC; a chemosensitizer) were prepared. To load siRNA on niosomes, 1, 2-dioleoyl-3-trimethylammonium-propane (DOTAP) was used as a cationic lipid. The optimum formulation containing tween-60:cholesterol:DPPC:DOTAP:DSPE-PEG2000 at 49.5:5.5:15:25:5 demonstrated that ...
Source: Artificial Cells, Nanomedicine and Biotechnology - July 24, 2018 Category: Biotechnology Tags: Artif Cells Nanomed Biotechnol Source Type: research

REGULATION OF OVULATORY GENES IN BOVINE GRANULOSA CELLS: LESSONS FROM siRNA SILENCING OF PTGS2.
Abstract Prostaglandin endoperoxide synthase 2 (PTGS2), tumor necrosis factor-alpha-induced protein-6 (TNFAIP6), pentraxin-3 (PTX3), epidermal growth factor like factors: amphiregulin (AREG) and epiregulin (EREG) are essential for successful ovulation. We compared here the induction of these ovulatory genes in bovine granulosa cells (GCs) in vivo (after LH surge) and in vitro (forskolin treatment). These genes were markedly stimulated in GCs isolated from cows 21hr after LH- surge. In isolated GCs, forskolin induced a distinct temporal profile for each gene. Generally, there was a good agreement between the in viv...
Source: Reproduction - October 16, 2014 Category: Reproduction Medicine Authors: Shrestha K, Lukasik K, Baufeld A, Vanselow J, Moallem U, Meidan R Tags: Reproduction Source Type: research

Identification of metabolically stable 5'-phosphate analogs that support single-stranded siRNA activity
In this report we used crystal structure of the 5'-phosphate binding pocket of Ago-2 bound with guide strand to design and synthesize ss-siRNAs containing various 5'-phosphate analogs. Our results indicate that the electronic and spatial orientation of the 5'-phosphate analog was critical for ss-siRNA activity. Chemically modified ss-siRNA targeting human apoC III mRNA demonstrated good potency for inhibiting ApoC III mRNA and protein in transgenic mice. Moreover, ApoC III ss-siRNAs were able to reduce the triglyceride and LDL cholesterol in transgenic mice demonstrating pharmacological effect of ss-siRNA. Our study provid...
Source: Nucleic Acids Research - March 31, 2015 Category: Research Authors: Prakash, T. P., Lima, W. F., Murray, H. M., Li, W., Kinberger, G. A., Chappell, A. E., Gaus, H., Seth, P. P., Bhat, B., Crooke, S. T., Swayze, E. E. Tags: Chemical Biology and Nucleic Acid Chemistry Source Type: research

Modulated cellular delivery of anti-VEGF siRNA (bevasiranib) by incorporating supramolecular assemblies of hydrophobically modified polyamidoamine dendrimer in stealth liposomes
Publication date: 20 August 2016 Source:International Journal of Pharmaceutics, Volume 510, Issue 1 Author(s): Nasim Golkar, Soliman Mohammadi Samani, Ali Mohammad Tamaddon A novel lipopolymer based system was designed and characterized for cellular delivery of anti-VEGF siRNA in SKBR-3 breast tumor cell line. Polyamidoamine (PAMAM) dendrimers of low generations (G1, G2 and G3) were incorporated into polyethylene glycol (PEG)-stabilized liposomes by following the consecutive steps: (a) synthesis of the cholesterol conjugates (40% molar ratio of cholesterol to primary amines of PAMAM), (b) incorporation of the conjugat...
Source: International Journal of Pharmaceutics - June 17, 2016 Category: Drugs & Pharmacology Source Type: research

Complexation of Chol-DsiRNA in place of Chol-siRNA greatly increases the duration of mRNA suppression by polyplexes of PLL(30)-PEG(5K) in primary murine syngeneic breast tumors after i.v. administration
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Vishakha V. Ambardekar, Rajesh R. Wakaskar, Zhen Ye, Stephen M. Curran, Timothy R. McGuire, Don W. Coulter, Rakesh K. Singh, Joseph A. Vetro RNA interference has tremendous potential for cancer therapy but is limited by the insufficient potency of RNAi molecules after i.v. administration. We previously found that complexation with PLL(30)-PEG(5K) greatly increases the potency of 3′-cholesterol-modified siRNA [Chol-siRNA] in primary murine syngeneic 4T1 breast tumors after i.v. administration but mRNA suppress...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

The growth of siRNA-based therapeutics: updated clinical studies.
Abstract More than two decades after the natural gene-silencing mechanism of RNA interference was elucidated, small interfering RNA (siRNA)-based therapeutics have finally broken into the pharmaceutical market. With three agents already approved and many others in advanced stages of the drug development pipeline, siRNA drugs are on their way to becoming a standard modality of pharmacotherapy. The majority of late-stage candidates are indicated for rare or orphan diseases, whose patients have an urgent need for novel and effective therapies. Additionally, there are agents that have the potential to meet the need of...
Source: Biochemical Pharmacology - January 26, 2021 Category: Drugs & Pharmacology Authors: Zhang MM, Bahal R, Rasmussen TP, Manautou JE, Zhong XB Tags: Biochem Pharmacol Source Type: research

Effects of sterol derivatives in cationic liposomes on  biodistribution and gene-knockdown in the lungs of mice systemically injected with siRNA lipoplexes
Mol Med Rep. 2021 Aug;24(2):598. doi: 10.3892/mmr.2021.12237. Epub 2021 Jun 24.ABSTRACTCationic liposomes can be intravenously injected to deliver short interfering (si)RNAs into the lungs. The present study investigated the effects of sterol derivatives in systemically injected siRNA/cationic liposome complexes (siRNA lipoplexes) on gene‑knockdown in the lungs of mice. Cationic liposomes composed of 1,2‑dioleoyl‑3‑trimethylammonium‑propane or dimethyldioctadecylammonium bromide (DDAB) were prepared as a cationic lipid, with sterol derivatives such as cholesterol (Chol), β‑sitosterol, ergosterol (Ergo) or stig...
Source: Molecular Medicine - June 24, 2021 Category: Molecular Biology Authors: Yoshiyuki Hattori Hiromu Saito Teruaki Oku Kei-Ichi Ozaki Source Type: research