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Noonindoles G–L: Indole Diterpene Glycosides from the Australian Marine-Derived Fungus Aspergillus noonimiae CMB-M0339
2023 / Journal of Natural ProductsFungal indole diterpenes (IDTs) occupy a valuable region of bioactive natural product chemical space, displaying potent and selective inhibition of therapeutically important ion channels and with potential application in the treatment of glaucoma, cancer, and neurodegenerative diseases, as well as insecticides and antivirals. We have employed an integrated workflow...
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Budesonide-loaded bilosomes as a targeted delivery therapeutic approach against acute lung injury in rats
2022 / Journal of Pharmaceutical SciencesBudesonide (BUD), a glucocorticoids drug, inhibits all steps in the inflammatory response. It can reduce and treat inflammation and other symptoms associated with acute lung injury such as COVID-19. Loading BUD into bilosomes could boost its therapeutic activity, and lessen its frequent administration and side effects. Different bilosomal formulations were prepared...
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Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D3
2022 / journal of medicinal chemistryThe toxic calcemic effects of the natural hormone 1α,25-dihydroxyvitamin D3 (1,25D3, 1,25-dihydroxycholecalciferol) in the treatment of hyperproliferative diseases demand the development of highly active and noncalcemic vitamin D analogues. We report the development of two highly active and noncalcemic analogues of 1,25D3 that lack the C-ring and possess an m...
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Cryptic Epoxytiglianes from the Kernels of the Blushwood Tree (Fontainea picrosperma)
2022 / journal of natural productsThe kernels of the Australian blushwood tree (Fontainea picrosperma) are the source of the veterinary anticancer drug tigilanol tiglate (2a, Stelfonta) and contain a concentration of phorboids significantly higher than croton oil, the only abundant source of these compounds previously known. The oily matrix of the blushwood kernels is composed of free fatty acids a...
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Antiviral Profiling of C-18- or C-19-Functionalized Semisynthetic Abietane Diterpenoids
2022 / journal of natural productsViral infections affect several million patients annually. Although hundreds of viruses are known to be pathogenic, only a few can be treated in the clinic with available antiviral drugs. Naturally based pharmacotherapy may be a proper alternative for treating viral diseases. Several natural and semisynthetic abietane-type diterpenoids have shown important antivira...
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RNA FORMULATIONS SUITABLE FOR THERAPY
2022 / PatentThe present invention relates to compositions comprising RNA, preferably messenger RNA (mRNA), more preferably self-amplifying RNA (saRNA), and polymers, in particular cationic polymers, such as polyethylenimine (PEI), poly-L-Lysin (PEL), polyvinylamine (PVA) or polyallylamine (PAA), where individual RNA molecules are present in solution. In the formulations, the R...
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(+)-Usnic acid and its salts, inhibitors of SARS‐CoV‐2, identified by using in silico methods and in vitro assay
2022 / Scientific ReportsThe pandemic caused by severe acute respiratory Coronavirus-2 (SARS-CoV-2) has been ongoing for over two years, and treatment for COVID-19, other than monoclonal antibodies, is urgently required. Accordingly, we have investigated the inhibitors of SARS-CoV-2 protein targets by high-throughput virtual screening using a marine natural products database. Considering...
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A Biopharmaceutical Perspective on Higher-Order Structure and Thermal Stability of mRNA Vaccines
2022 / Molecular pharmaceuticsPreservation of the integrity of macromolecular higher-order structure is a tenet central to achieving biologic drug and vaccine product stability toward manufacturing, distribution, storage, handling, and administration. Given that mRNA lipid nanoparticles (mRNA-LNPs) are held together by an intricate ensemble of weak forces, there are some intriguing parallels to...
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(±)-Neonardochinone A, a pair of enantiomeric neoligans from Nardostachys chinensis with their anti-Alzheimer’s disease activities
2020 / Phytochemistry LettersA pair of new enantiomeric neoligans, (±)-neonardochinone A (1) were isolated from Nardostachys chinensis. The structure of 1 was determined by extensive spectroscopic analysis, containing IR, HRESIMS, NMR spectra and single crystal X-ray diffraction. The enantiomeric separation was finished by HPLC on a chiral column. The absolute configurations were assign...
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New antifungal tetrahydrofuran derivatives from a marine sponge-associated fungus Aspergillus sp. LS78
2020 / FitoterapiaTwo new tetrahydrofuran derivatives named aspericacids A and B (1 and 2) were isolated from the metabolites produced by the sponge-associated Aspergillus sp. LS78. They represented an unusual type of tetrahydrofuran derivatives, possessing 2,5-disubstituted tetrahydrofuran ring coupled with a chain unsaturated fatty acid. The planar structures of 1 and 2 were deter...
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Effects of Secondary Structure on Solid-State Hydrogen-Deuterium Exchange in Model α-Helix and β-Sheet Peptides
2020 / molecular pharmaceuticsThe effects of peptide secondary structure on the rate and extent of deuterium incorporation in solid-state hydrogen-deuterium exchange mass spectrometry (ssHDX-MS) were assessed. Unstructured PDLA peptides, an α-helical model peptide (Peptide A) and a β-sheet model peptide (Peptide B) were co-lyophilized with various excipients. Peptide structures were ...
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Polyprenylated acylphloroglucinols as deubiquitinating protease USP7 inhibitors from Hypericum hookerianum
2020 / FitoterapiaHookerianones A – E (1–5), five new polyprenylated acylphloroglucinols (PPAPs), along with six known ones, were isolated from the aerial parts of Hypericum hookerianum. Their structures were elucidated by analyses of MS, NMR, chiroptical properties, biogenetic pathway, and/or single crystal X-ray diffraction. A ubiquitin-rhodamine 110 assay showed that ...
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21-Epi-taichunamide D and (±)-versicaline A, three unusual alkaloids from the endophytic Aspergillus versicolor F210
2020 / Tetrahedron LettersThree new alkaloids, 21-epi-taichunamide D (1) and (±)-versicalin A ((±)-6), along with four known analogues (2–5) were isolated from the endophytic Aspergillus versicolor F210, which harbored in the bulbs of Lycoris radiata. Structurally, compound 1 is the third natural indole alkaloid with a rare methylsulfonyl unit, and (±)-6 existing ...
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Effect of N-methylated and fatty acid conjugation on analogs of antimicrobial peptide Anoplin
2020 / European Journal of Pharmaceutical SciencesWith the increment of drug-resistant bacteria and the slow development of novel antibiotics, antimicrobial peptides have gained increasing attention as a potential antibiotic alternative. They not only displayed a broad-spectrum antimicrobial activity but also were difficult to induce resistance development because of their unique membrane-lytic activity. Herein, t...
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Simple and non-charged long-lived fluorescent intracellular organelle trackers
2020 / Dyes and PigmentsIn this work the preferential accumulation of long-lived acridone derivatives in mitochondria were evaluated, based on a new concept of non-protonable and non-charged group carriers. In this sense, the thiophene ring has been proved to act, for the first time, as mitochondria targeting group. Moreover, the unique long lifetime of the dyes has allowed the determinat...
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