TS Science
Applications
Application
Found 707 Results / Page 3 of 48
-
Enantiomerically Pure Quinoline-Based k-Opioid Receptor Agonists: Chemoenzymatic Synthesis and Pharmacological Evaluation
2020 / ChemMedChemRacemic K‐opioid receptor (KOR) agonist 2‐(3,4‐dichlorophenyl)‐1‐[(4aRS ,8SR ,8aSR )‐8‐(pyrrolidin‐1‐yl)‐3,4,4a,5,6,7,8,8a‐octahydroquinolin‐1(2H )‐yl]ethan‐1‐one ((±)‐4 ) was prepared in a diastereoselective synthesis. The first key step of the synthesis was the diastereoselective hydrogenation of the silyl ether of 1,2,3,4‐tetrahydroquinoin‐8‐ol ((±...
Continue reading -
Peroxynitrous acid (ONOOH) modifies the structure of Anastellin and influences its capacity to polymerize fibronectin
2020 / Redox BiologyAnastellin (AN), a fragment of the first type III module in fibronectin (FN), initiates formation of superfibronectin, a polymer which resembles the native cell-derived fibrillar FN found in the extracellular matrix of many tissues, but which displays remarkably different functional properties. Here we demonstrate that exposure of AN to the biologically-important i...
Continue reading -
Triple-Negative Breast Cancer Cells Exhibit Differential Sensitivity to Cardenolides from Calotropis gigantea
2020 / Journal of Natural ProductsTriple-negative breast cancers (TNBC) are aggressive and heterogeneous cancers that lack targeted therapies. We implemented a screening program to identify new leads for subgroups of TNBC using diverse cell lines with different molecular drivers. Through this program, we identified an extract from Calotropis gigantea that caused selective cytotoxicity in BT-549 cel...
Continue reading -
Mechanistic Assessment of Functionalized Mesoporous Silica-Mediated Insulin Fibrillation
2020 / The Journal of Physical Chemistry BInsulin, which is a small protein hormone consisting of 51 amino acids, rapidly fibrillates under stressogenic conditions. This biotechnological/medical problematic reaction quickly accelerates in the presence of some particles, while there are several other particles that slow down the kinetic process. To address the unexplored demand of the particles that modulat...
Continue reading -
Highly oxygenated and rearranged limonoids from the stem barks of Entandrophragma utile
2020 / PhytochemistrySeventeen highly oxygenated and rearranged limonoids, including nine previously undescribed phragmalin-type limonoids with 1,8,9- and 8,9,30-orthesters (entanutilins C–K, 1–9), three undescribed limonoids with rare rearranged-6/6/7/5 skeleton (entanutilins L-N, 10–12), and 5 known limonoids, were isolated from the stem barks of Entandrophragma uti...
Continue reading -
Uncommon nornardosinane, seconeolemnane and related sesquiterpenoids from Xisha soft coral Litophyton nigrum
2020 / Bioorganic ChemistryThree new nardosinane-type sesquiterpenoids linardosinenes A–C (1–3) and four new neolemnane-type sesquiterpenoids lineolemnenes A–D (4–7), together with the related known compound 4-acetoxy-2,8-neolemnadien-5-one (8), were isolated from the Xisha soft coral Litophyton nigrum. The structures of these new compounds were elucidated by comprehe...
Continue reading -
Phospholipid-Dependent Functions of a Macrocyclic Analogue of the Ion-Channel-Forming Antibiotic Gramicidin A
2020 / Chemical and Pharmaceutical BulletinAn ion-channel-forming natural peptide, gramicidin A (1), exhibits potent antimicrobial activity against Gram-positive bacteria, although medical applications are limited to topical use due to its mammalian cytotoxicity. We recently reported that the artificial macrocyclic analogue 2 provides a promising starting point for developing new ion-channel-based systemic ...
Continue reading -
The Stability Maintenance of Protein Drugs in Organic Coatings Based on Nanogels
2020 / PharmaceuticsProtein drugs are often loaded on scaffolds with organic coatings to realize a spatiotemporal controlled release. The stability or activity of protein drugs, however, is largely affected by the organic coating, particularly with organic solvents, which can dramatically reduce their delivery efficiency and limit their application scope. In spite of this, little atte...
Continue reading -
Monarubins A–C from the Marine Shellfish-Associated Fungus Monascus ruber BB5
2020 / Marine DrugsThree new compounds, monarubins A–C (1, 6 and 13), together with ten known compounds, including four alkaloids (2–5), two isocoumarins (7 and 8) and four polyketides (9–12), were isolated from marine shellfish-associated fungus Monascus ruber BB5. The structures were determined on the basis of the 1D and 2D NMR, MS, UV and IR data. The absolute co...
Continue reading -
Two new flavonoids from Dracaena usambarensis Engl.
2020 / Phytochemistry LettersInvestigations of the root extract of Dracaena usambarensis Engl. for anticancer principles led to the characterization of one new homoisoflavonoid, (3S)-3,4ʹ,5,6-tetrahydroxy-7-methoxyhomoisoflavanone (1) and a new retrodihydrochalcone, 4ʹ,4-dihydroxy-2,3-dimethoxydihydrochalcone (2) along with six previously reported compounds, including two homoisoflavonoids, 7-...
Continue reading -
Absolute Configuration and Corrected NMR Assignment of 17-Hydroxycyclooctatin, a Fused 5–8–5 Tricyclic Diterpene
2020 / Journal of Natural ProductsThe absolute configuration and corrected NMR assignment of 17-hydroxycyclooctatin isolated from Streptomyces sp. M56 recovered from a nest of South African Macrotermes natalensis termites are reported. 17-Hydroxycyclooctatin is a unique tricyclic diterpene (C20) consisting of a fused 5–8–5 ring system, and in this study, its structure was unambiguously ...
Continue reading -
Cytotoxic alkaloids from the marine shellfish-associated fungus Aspergillus sp. XBB-4 induced by an amino acid-directed strategy
2020 / RSC AdvancesEight different culture media were used to culture shellfish Panopea abbreviate associated fungus Aspergillus sp. XBB-4. In a glucose-peptone-yeast (GPY) culture medium supplied with amino acids, this fungus can produce chemodiversity metabolites. Four new alkaloids including three β-carboline alkaloids, aspercarbolines A–C (1–3) and one piperazine...
Continue reading -
A simple injectable peptide-based hydrogel of tanshinone ⅡA for antioxidant and anticoagulation
2020 / Journal of Drug Delivery Science and TechnologyIn this study, the hydrophobic drug Tanshinone ⅡA (Tan ⅡA) as a therapeutic drug was loaded into naphthalene acetic acid-phenylalanine-phenylalanine-glycine hydrogel (Nap-FFG) to construct the supramolecular hydrogels. Nap-FFG hydrogel fibers crosslinked into a network-like structure by self-assembly of polypeptides and then achieved drug loading. The rheological a...
Continue reading -
Self-Assembly of Exendin-4-Derived Dual Peptide Agonists is Mediated by Acylation and Correlated to the Length of Conjugated Fatty Acyl Chains
2020 / molecular pharmaceuticsDual glucagon-like peptide-1/glucagon receptor agonists have emerged as promising candidates for the treatment of diabetes and obesity. Issues of degradation sensitivity and rapid renal clearance are addressed, for example, by the conjugation of peptides to fatty acid chains, promoting reversible albumin binding. We use combined dynamic and static light scattering ...
Continue reading -
Peptide-Based Soft Hydrogels Modified with Gadolinium Complexes as MRI Contrast Agents
2020 / PharmaceuticsPoly-aromatic peptide sequences are able to self-assemble into a variety of supramolecular aggregates such as fibers, hydrogels, and tree-like multi-branched nanostructures. Due to their biocompatible nature, these peptide nanostructures have been proposed for several applications in biology and nanomedicine (tissue engineering, drug delivery, bioimaging, and fabri...
Continue reading
약관
약관내용