51154-39-3Relevant academic research and scientific papers
Enantiomeric synthesis of natural alkylglycerols and their antibacterial and antibiofilm activities
Fernández Montoya, Deicy J.,Contreras Jordan, Luis A.,Moreno-Murillo, Bárbara,Silva-Gómez, Edelberto,Mayorga-Wandurraga, Humberto
, p. 2544 - 2550 (2019/11/13)
Alkylglycerols (AKGs) are bioactive natural compounds that vary by alkyl chain length and degree of unsaturation, and their absolute configuration is 2S. Three AKGs (5l–5n) were synthesised in enantiomerically pure form, and were characterised for the first time together with 12 other known and naturally occurring AKGs (5a–5k, 5o). Their structures were established using 1H and 13C APT NMR with 2D-NMR, ESI-MS or HRESI-MS and optical rotation data, and they were tested for their antibacterial and antibiofilm activities. AKGs 5a–5m and 5o showed activity against five clinical isolates and P. aeruginosa ATCC 15442, with MIC values in the range of 15–125 μg/mL. In addition, at half of the MIC, most of the AKGs reduced S. aureus biofilm formation in the range of 23%–99% and P. aeruginosa ATCC 15442 biofilm formation in the range of 14%–64%. The antibiofilm activity of the AKGs assessed in this work had not previously been studied.
Lipid nanoparticle formulations of non-viral capsid-free DNA vectors
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Paragraph 0403; 0405-0407, (2020/09/26)
Provided herein are lipid nanoparticle formulations that comprise an ionizable lipid and non-viral, capsid-free DNA vectors with covalently-closed ends.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
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Paragraph 00724, (2019/01/08)
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
3 - (1 - Piperazine - 4 - yl uncle ding yangtang acid radical) propionic acid amphiphilic derivatives and use thereof (by machine translation)
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Paragraph 0050; 0070; 0075; 0076; 0077, (2018/07/30)
The invention relates to an amphiphilic derivative of 3-(1-tert-butoxycarbonylpiperazin-4-yl)propionic acid, and a use thereof, and also relates to a liposome prepared from the amphiphilic derivative. The use is the use of the liposome as a drug carrier delivery system. The liposome prepared from the amphiphilic derivative can be compounded with gene drug siRNA to form a compound with small particle size and uniform particle size distribution. The amphiphilic derivative is electrically neutral in environment with the pH value of 7.4, increases the in vivo stability of the lipid compound and reduces cytotoxicity caused by too many positive charges. The liposome can specifically inhibit gene expression in human non-small cell lung cancer H1299-Pg13 cells in vitro, and can specifically transship fluorescence gene drugs into normal mouse liver cells in vivo.
OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF
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Paragraph 001405, (2017/04/23)
Among other things, the present disclosure relates to designed oligonucleotides, compositions, and methods thereof. In some embodiments, provided oligonucleotide compositions provide altered splicing of a transcript. In some embodiments, provided oligonucleotide compositions have low toxicity. In some embodiments, provided oligonucleotide compositions provide improved protein binding profiles. In some embodiments, provided oligonucleotide compositions have improved delivery. In some embodiments, provided oligonucleotide compositions have improved uptake. In some embodiments, the present disclosure provides methods for treatment of diseases using provided oligonucleotide compositions.
LIPID MEMBRANE STRUCTURE FOR siRNA INTRACELLULAR DELIVERY
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Paragraph 0089-0091, (2017/10/10)
A lipid membrane structure encapsulating an siRNA inside thereof and containing a lipid compound of the formula (I) as a lipid component (R1 and R2 represent CH3—(CH2)n—CH═CH—CH2—CH═CH—(CH2)m—, n represents an integer of 3 to 5, m represents an integer of 6 to 10, p represents an integer of 2 to 7, and R3 and R4 represent a C1-4 alkyl group or a C2-4 alkenyl group.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
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Paragraph 00656; 00867, (2017/07/14)
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
Compositions for nucleic acid delivery
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Page/Page column 114; 115, (2017/07/14)
The present invention is based, in part, upon the discovery of charged lipids that provide advantages when used in lipid particles for the in vivo delivery of a therapeutic agent. As such, described herein are compounds useful for delivering a nucleic acid to a cell.
Di-aliphatic substituted pegylated lipids
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Page/Page column 103, (2017/08/08)
The disclosure relates to di-aliphatic substituted PEGylated lipids and to methods of their preparation. The disclosure also relates to lipid conjugates containing di-aliphatic substituted PEGylated lipids, and to the use of di-aliphatic substituted PEGylated-lipid conjugates in drug delivery.
OLIGONUCLEOTIDES, COMPOSITIONS AND METHODS THEREOF
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Paragraph 001646, (2018/01/17)
The present disclosure pertains to the recognition that immune responses mediated by CpG oligonucleotides can be affected by the stereochemistry of modified internucleotidic linkages such as phosphorothioates. In some embodiments, the present disclosure relates to chirally controlled CpG oligonucleotide compositions comprising CpG oligonucleotides comprising multiple modified internucleotidic linkages such as phosphorothioate linkages, wherein the oligonucleotides comprise one or more CpG region motifs having defined stereochemistry patterns of chiral internucleotidic linkages. In some embodiments, CpG oligonucleotides comprising one or more CpG region motifs are capable of agonizing an immune response. In some embodiments, CpG oligonucleotides comprising one or more CpG region motifs are antagonistic. Methods for making and using chirally controlled CpG oligonucleotide compositions are also described. In some embodiments, no immune modulation is desired, and the present disclosure provides methods of identifying chirally controlled oligonucleotide compositions which have decreased immune modulation.
