7459-33-8Relevant academic research and scientific papers
Linoleic acid esters of hydroxy linoleic acids are anti-inflammatory lipids found in plants and mammals
Kolar, Matthew J.,Konduri, Srihari,Chang, Tina,Wang, Huijing,McNerlin, Clare,Ohlsson, Lena,H?rr?d, Magnus,Siegel, Dionicio,Saghatelian, Alan
, p. 10698 - 10707 (2019)
Fatty acid esters of hydroxy fatty acids (FAHFAs) are a recently discovered class of biologically active lipids. Here we identify the linoleic acid ester of 13-hydroxy linoleic acid (13-LAHLA) as an anti-inflammatory lipid. An oat oil fraction and FAHFA-enriched extract from this fraction showed anti-inflammatory activity in a lipopolysaccharide-induced cytokine secretion assay. Structural studies identified three LAHLA isomers (15-, 13-, and 9-LAHLA) as being the most abundant FAHFAs in the oat oil fraction. Of these LAHLAs, 13-LAHLA is the most abundant LAHLA isomer in human serum after ingestion of liposomes made of fractionated oat oil, and it is also the most abundant endogenous LAHLA in mouse and human adipose tissue. As a result, we chemically synthesized 13-LAHLA for biological assays. 13-LAHLA suppresses lipopolysaccharide-stimulated secretion of cytokines and expression of pro-inflammatory genes. These studies identify LAHLAs as an evolutionarily conserved lipid with anti-inflammatory activity in mammalian cells.
CATIONIC LIPIDS AND USES THEREOF
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Page/Page column 152-153, (2021/01/23)
The present invention relates to novel cationic lipids of formula I, and more specifically formula IV. These are used, for example, in liposomes for the delivery of nucleic acids to cells.
GLYCEROL DERIVATIVE, PREPARATION METHOD THEREFOR, AND IMMUNOMODULATOR COMPRISING SAME AS EFFECTIVE INGREDIENT
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Paragraph 0076-0077, (2021/07/02)
Disclosed are a glycerol derivative that is useful for improving, preventing or treating inflammation-related diseases by inhibiting overexpression of various inflammatory cytokines such as IL-4, IL-6 and so on, or chemokine CXCL8 and reducing migration of HL-60 cell lines, preparation method therefor, and an immunomodulator containing the same as active ingredient. It includes a glycerol derivative represented by Chemical formula 2 or 3 in the specification.
Pharmacological and structure-activity relationship studies of oleoyl-lysophosphatidylinositol synthetic mimetics
Falasca, Marco,Keating, Damien J.,Kizilkaya, Hüsün Sheyma,Kokh, Elena,Mancera, Ricardo L.,Massi, Massimiliano,Paternoster, Silvano,Rosenkilde, Mette Marie,Simpson, Peter V.
, (2021/08/30)
Metabolic diseases, such as obesity and type 2 diabetes, are relentlessly spreading worldwide. The beginning of the 21st century has seen the introduction of mechanistically novel types of drugs, aimed primarily at keeping these pathologies under control. In particular, an important family of therapeutics exploits the beneficial physiology of the gut-derived glucagon-like peptide-1 (GLP-1), with important clinical benefits, from glycaemic control to cardioprotection. Nonetheless, these protein-based drugs act systemically as exogenous GLP-1 mimetics and are not exempt from side effects. The food-derived lipid oleoyl-lysophosphatidylinositol (LPI) is a potent GPR119-dependent GLP-1 secreting agent. Here we present a structure-activity relationship (SAR) study of a synthetic library of oleoyl-LPI mimetics capable to induce the physiological release of GLP-1 from gastrointestinal enteroendocrine cells (EECs). The best lead compounds have shown potent and efficient release of GLP-1 in vitro from human and murine cells, and in vivo in diabetic db/db mice. We have also generated a molecular model of oleoyl-LPI, as well as its best performing analogues, interacting with the orthosteric site of GPR119, laying foundational evidence for their pharmacological activity.
3-PYRROLIDINE-INDOLE DERIVATIVES AS SEROTONERGIC PSYCHEDELIC AGENTS FOR THE TREATMENT OF CNS DISORDERS
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Paragraph 00286, (2021/08/14)
The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions. Formula (I)
COMPOSITION AND METHODS FOR TREATMENT OF PRIMARY CILIARY DYSKINESIA
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Paragraph 0321, (2021/11/13)
The present invention provides, among other things, methods and compositions for treating primary ciliary dyskinesia (PCD) based on mRNA therapy. The compositions used in treatment of PCD comprise an mRNA comprising a dynein axonemal intermediate chain 1 (DNAI1) coding sequence and are administered at an effective dose and an administration interval such that at least one symptom or feature of PCD is reduced in intensity, severity, or frequency or has a delayed onset. mRNAs with optimized DNAI1 coding sequences are provided that can be administered without the need for modifying the nucleotides of the mRNA to achieve sustained in vivo function.
Unsaturation and Polar Head Effect on Gelation, Bioactive Release, and Cr/Cu Removal Ability of Glycolipids
Bojja, Sreedhar,Holey, Snehal Ashokrao,Nayak, Rati Ranjan,Sekhar, Kanaparedu P. C.,Swain, Deepak Kumar
, p. 3080 - 3088 (2020/08/06)
Designing of multifunctional soft and smart materials from natural sources is a useful strategy for producing safer chemicals having potential applications in biomedical research and pharmaceutical industries. Herein, eight glycolipids with variation in unsaturation of hydrophobic tail and polar headgroup size were designed. The effect of unsaturation in the tail group and headgroup size on gelation ability, and mechanical and thermal stability of glycolipid hydro/organogels was studied to understand structure and property relationship. Glycolipids are functional amphiphilic molecules having potential applications in the field of drug delivery and metal removal. The encapsulation capacity and kinetic release behavior of hydrophobic/hydrophilic bioactives like curcumin/riboflavin from the hydrophobic/hydrophilic pockets of glycolipids hydro/organogels was examined. A significant observation was that the glucamine moiety of the glycolipid headgroup plays a vital role in removal of Cr and Cu from oil/water biphasic systems. Typical functions of the glycolipid hydrogels are metal chelation and enzyme-triggered release behavior, enabled them as promising material for Cr, Cu removal from edible oils and controlled release of water soluble/insoluble bioactives.
2, 4-dinitrophenol derivative and application thereof
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Paragraph 0128-0130, (2020/08/18)
The present invention relates to a 2, 4-dinitrophenol derivative represented by a general formula (I) or a pharmaceutically acceptable salt thereof, in which L and R are as described in the text, anda composition comprising an effective dose of a compound of general formula (I) or a pharmaceutically acceptable salt thereof. The compound with the general formula (I) or the pharmaceutical salt thereof is used for treating the non-alcoholic fatty liver disease. The invention also discloses application of the traditional Chinese medicine composition in medicines for treating non-alcoholic steatohepatitis, hepatic steatosis, type 2 diabetes mellitus, acquired dyslipidemia, dyslipidemia, local dyslipidemia, hypertriglyceridemia, obesity, metabolic syndrome, Rette's syndrome, aging-related metabolic syndrome or insulin resistance and the like.
Synthesis, characterization and corrosion inhibition studies of polyunsaturated fatty acid derivatives on the acidic corrosion of mild steel: Experimental and computational studies
Abdulazeez, Ismail,Abubshait, Haya A.,Abubshait, Samar A.,Elsharif, Asma M.
, (2020/09/17)
In an effort to make an efficient and benign CI for the purpose of acidizing, a novel range of new derivatives of polyunsaturated fatty acids (PUFA) were prepared from a group of amines and Z-9,12-octadecadienoic acid with Excellent yields. Elemental analysis, FTIR, 13C NMR and 1H NMR was employed to realize a description for the newly manufactured compound. The inhibitive action of synthesized amides was examined by means of potentiodynamic polarization techniques and weight loss measurements in 1.00 M HCl. Derivatives of Z-9,12-octadecadienoic acid amides (DA) were found to obey the Langmuir adsorption model. The hydrophobic nature of mild steel (MS) was revealed by measurement of the contact angle in the presence of CI. The experimental findings were found to be supported by quantum chemical calculations. Inhibition efficiencies were computed for various DA concentrations for inhibition against the wear of MS in 100.00 ml of 1.00 M HCl, with exposure for four days at temperatures ranging from 298 to 333 K. For a DA concentration of 100 ppm, every inhibitor molecule showed outstanding percentage inhibition efficiencies in 1.00 M HCl. Compounds 2, 3, 4, 5, 6, 7, 8 and 9 offered a robust percentage inhibition efficiency of 92.90, 86.6, 49.8, 82.7, 85.9, 96.70, 94.30 and 91.30, correspondingly, at 100 ppm. The interaction of the p-electrons in compounds with low-energy, empty Fe d-orbitals helped the inhibitive molecules (IMs) to experience adsorption and inhibit the process of anodic dissolution. When Tafel plots were employed for the compounds used in the electrochemical method, similar findings were obtained for the percentage inhibition efficiencies. Compound adsorption on the MS surface was discovered to obey Arrhenius and Transition state plots in 1.00 M HCl.
Antiproliferative 3-deoxysphingomyelin analogs: Design, synthesis, biological evaluation and molecular docking of pyrrolidine-based 3-deoxysphingomyelin analogs as anticancer agents
Hassan, Ahmed H.E.,Park, Hye Rim,Yoon, Yoon Mi,Kim, Hye In,Yoo, Sung Yeun,Lee, Kun Won,Lee, Yong Sup
, p. 444 - 455 (2019/01/03)
Sphingomyelins and glycerophospholipids are structurally related phospholipids. Nevertheless, glycerophospholipids analogs are known as antitumor agents while sphingomyelin analogs were reported as cytoprotective agents. Herein, we have addressed the development of 3-deoxysphingomyelin analogs as cytotoxic agents possessing modified sphingobases. Thus, pyrrolidine-based 3-deoxysphingomyelin analogs were synthesized and evaluated against a panel of cell lines representing four major types of cancers. Compounds 3d, 4d and 6d elicited better GI50 values than the FDA approved drug miltefosine. Investigation of their impact on Akt phosphorylation as a possible mechanism for the antiproliferative activity of this class of compounds revealed that these compounds might elicit a concentration-dependent mechanism via inhibition of Akt phosphorylation at the lower concentration. Molecular docking predicted their binding modes to Akt to involve polar head binding to the Pleckstrin homology domain and hydrophobic tail extension into a hydrophobic pocket connecting the Pleckstrin homology domain and the kinase domain. As a whole, the described work suggests compounds 3d, 4d and 6d as promising pyrrolidine-based 3-deoxysphingomyelin analogs for development of novel cancer therapies.
