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... Environmental toxicant- and oxidant-induced [e.g., cigarette smoke (CS)] respiratory oxidative stress and inflammatory response play a vital role in the onset and progression of COPD. The nuclear factor erythroid 2-related factor 2 (Nrf2) represents an important mechanism for regulating intracellular oxidative stress and inflammatory response and is a promising target for developing agents against ...
... Wnt signaling regulates various processes such as cell proliferation, differentiation, and embryo development. However, numerous diseases have been attributed to the aberrant transduction of Wnt signaling. We screened a plant extract library targeting TCF/β-catenin transcriptional modulating activity with a cell-based luciferase assay. Activity-guided fractionation of the MeOH extract of the E. lo ...
Agaricus bisporus; Danio rerio; adults; bone formation; bone morphogenetic proteins; cartilage; cell walls; chitin; dose response; fins; fish; glucosamine; hydrochloric acid; hydrolysis; larvae; models; osteoporosis; skeletal development
Abstract:
... Glucosamine hydrochloride (GAH), one of the most basic and important derivatives of chitin, is obtained by hydrolysis of chitin in concentrated hydrochloric acid. At present, little is known about how GAH functions in skeletal development. In this report, we demonstrate that GAH, extracted from the cell wall of Agaricus bisporus, acts in a dose-dependent manner to promote not only cartilage and bo ...
Khadidja Aya Beladjila; Djemaa Berrehal; Zahia Kabouche; Maria Paola Germanò; Valeria D’Angelo; Nunziatina De Tommasi; Felicia D’Andrea; Alessandra Braca; Marinella De Leo
... Ten new iridoid glycosides (1–10) and two new monoterpenoids (11 and 12), together with nine known compounds (13–21), were isolated from the n-butanol extract of the aerial parts of Anarrhinum pedatum. The structural characterization of all compounds was performed by spectroscopic analysis, including 1D and 2D NMR and HRESIMS experiments. The isolates were assayed for their antiangiogenic activity ...
... Bioactivity-guided fractionation of the ethyl acetate extract of the leaves of Poupartia borbonica led to the isolation of three new alkyl cyclohexenone derivatives 1–3, and named Poupartone A–C. The structures of the new compounds were elucidated by 1D and 2D NMR spectroscopic data analysis and MS, whereas calculated and experimental ECD spectra were used to define the absolute configurations. Th ...
... Six new C₂₁ steroidal glycosides, cynotophyllosides A–F (1–6), together with 16 known compounds, were isolated from the roots of Cynanchum otophyllum. The structures of the new compounds were elucidated by spectroscopic analysis and chemical methods. The three major components, otophylloside F (15), otophylloside B (17), and rostratamine 3-O-β-d-oleandropyranosyl-(1→4)-β-d-cymaropyranosyl-(1→4)-β- ...
... Toads produce potent toxins, named bufadienolides, to defend against their predators. Pharmacological research has revealed that bufadienolides are potential anticancer drugs. In this research, we reported nine bufadienolides from the eggs of the toad Bufo bufo gargarizans, including two new compounds (1 and 3). The chemical structures of 1 and 3, as well as of one previously reported semisynthesi ...
Gerardo D. Anaya-Eugenio; Ermias Mekuria Addo; Nathan Ezzone; Joshua M. Henkin; Tran Ngoc Ninh; Yulin Ren; Djaja D. Soejarto; A. Douglas Kinghorn; Esperanza J. Carcache de Blanco
... Corchorusoside C (1), isolated from Streptocaulon juventas collected in Vietnam, was found to be nontoxic in a zebrafish (Danio rerio) model and to induce cytotoxicity in several cancer cell lines with notable selective activity against prostate DU-145 cancer cells (IC₅₀ 0.08 μM). Moreover, corchorusoside C induced DU-145 cell shrinkage and cell detachment. In CCD-112CoN colon normal cells, 1 show ...
Wentao Dai; Imelda T. Sandoval; Shengxin Cai; Kaylee A. Smith; Richard Glenn C. Delacruz; Kevin A. Boyd; Jessica J. Mills; David A. Jones; Robert H. Cichewicz
... Phenotype-based screening of a fungal extract library yielded an active sample from a Penicillium sp. isolate that impaired zebrafish motility. Bioassay-guided purification led to the identification of 14 meroterpenoids including six new metabolites, arisugacins L–Q (4, 5, 8, and 12–14), seven known arisugacins (1–3, 6, 7, 9, and 10), and one known terreulactone (11). Their structures were determi ...
... Eight prenylated xanthones including four new analogues were extracted and purified from the leaves of Garcinia xipshuanbannaensis. Multiple techniques including UV, 1D and 2D NMR, and HRESIMS were used to determine the structures of the isolated xanthones. These xanthones were evaluated for their cytotoxicity toward human cancer cells, and compound 4 exhibited activity against HeLa cells. A cytot ...
... Eight new dammarane-type triterpenoids (1–8), together with a related known analogue (9), were isolated from the roots of Rhus chinensis, a traditional Chinese medicine for treating coronary artery heart disease, guided by LC-MS analysis. Their structures were elucidated based on extensive spectroscopic analysis and quantum chemical calculations. Notably, compounds 1–7 and 9 possess an unusual 17α ...
Gabriel D. Bosse; Cristoval Urcino; Maren Watkins; Paula Flórez Salcedo; Sabrina Kozel; Kevin Chase; April Cabang; Samuel S. Espino; Helena Safavi-Hemami; Shrinivasan Raghuraman; Baldomero M. Olivera; Randall T. Peterson; Joanna Gajewiak
... Natural products such as conotoxins have tremendous potential as tools for biomedical research and for the treatment of different human diseases. Conotoxins are peptides present in the venoms of predatory cone snails that have a rich diversity of pharmacological functions. One of the major bottlenecks in natural products research is the rapid identification and evaluation of bioactive molecules. T ...
Danio rerio; anti-inflammatory activity; corals; diterpenoids; probability; South China Sea
Abstract:
... Five new dolabellane diterpenes, clavularinlides A–E (1–5), and four new racemic elemane alkaloids, clavulacylides A–D (7–10), together with one known compound (6), were isolated from the soft coral Clavularia inflata collected in the South China Sea. Their structures were elucidated by 1D and 2D NMR, HRESIMS, calculated ECD, and DP4+ probability analyses. Compounds 1–7 showed anti-inflammatory ac ...
... Fermentation of Acremonium tubakii W. Gams isolated from a soil sample collected from the University of Utah led to the isolation and characterization of six new linear pentadecapeptides, emerimicins V–X (1–6). Peptaibols containing 15-residues are quite rare, with only 22 reported. Genome mining and bioinformatic analysis were used to identify the emerimicin 60 kbp eme biosynthetic cluster harbor ...
Christina A. Lydon; Logesh Mathivathanan; Juanita Sanchez; Larissa A. H. dos Santos; Thomas Sauvage; Sarath P. Gunasekera; Valerie J. Paul; John P. Berry
... A new, cyclic carbonate eudesmane-type sesquiterpene, eudesmacarbonate (1), was isolated from marine filamentous cyanobacterial mats associated with apparent ingestion-related intoxications of captive bottlenose dolphins in the Florida Keys. Sequencing of 16S rDNA revealed that mats were composed of closely related Oscillatoriacean species including a previously undocumented species of Neolyngbya. ...
Sanchez Laura M.; Knudsen Giselle M.; Helbig Claudia; De Muylder Geraldine; Mascuch Samantha M.; Mackey Zachary B.; Gerwick Lena; Clayton Christine; McKerrow James H.; Linington Roger G.
... Almiramide C is a marine natural product with low micromolar activity against Leishmania donovani, the causative agent of leishmaniasis. We have now shown that almiramide C is also active against the related parasite Trypanosoma brucei, the causative agent of human African trypanosomiasis. A series of activity-based probes have been synthesized to explore both the molecular target of this compound ...
... Gamma-aminobutyric acid type A (GABAA) receptors are major inhibitory neurotransmitter receptors in the central nervous system and a target for numerous clinically important drugs used to treat anxiety, insomnia, and epilepsy. A series of allosteric GABAA receptor agonists was identified previously with the aid of HPLC-based activity profiling, whereby activity was tracked with an electrophysiolog ...
... Transcriptome analysis is shown to be an effective strategy to understand the potential function of natural products. Here, it is reported that 11 previously undescribed hydroanthraquinones [nigroquinones A–K (1–11)], along with eight known congeners, were isolated from Nigrospora sphaerica. Their structures were elucidated by interpreting spectroscopic and spectrometric data including high-resolu ...
... Epilepsy is a chronic neurological disorder, characterized by recurrent, spontaneous, and transient seizures, and affects more than 70 million people worldwide. Although two dozen antiepileptic drugs (AEDs) are approved and available in the market, seizures remain poorly controlled in one-third of epileptic patients who are suffering from drug resistance or various adverse effects. Recently, the x ...
... Four new jatropholane-type diterpenes (1–4), named sikkimenoids A–D, were isolated from the aerial parts of Euphorbia sikkimensis. The structural elucidations of 1–4 were accomplished by extensive NMR analyses, and their absolute configurations were established by ECD calculations. Compound 2 exhibited weak antiangiogenic activity with an IC₅₀ value of 43.0 μM when evaluated using a zebrafish mode ...
Danio rerio; Porifera; X-ray diffraction; alkaloids; circular dichroism spectroscopy; hepatoprotective effect; models; probability; spectral analysis; South China Sea
Abstract:
... Four new indole-C-mannopyranoside alkaloids, neopetrosins A–D (1–4), together with one new diamine alkaloid, haliclorensin D (6), were isolated from the marine sponge Neopetrosia chaliniformis collected off Xisha Island in the South China Sea. Their structures and absolute configurations were determined by spectroscopic analysis, single-crystal X-ray diffraction, calculated electronic circular dic ...
... Twenty-one dihydro-β-agarofuran derivatives were purified from the seeds of Euonymus maackii, and eight compounds (1–8) were identified as new natural products. Their structures were deduced by extensive spectroscopic analysis, X-ray diffraction studies, and comparison of observed and reported NMR data. Compounds 10, 12, 17, and 18 significantly increased the cell viability of Aβ₂₅–₃₅-treated SH-S ...
... Three new phenolic biphenyl derivatives (1–3) and one new lignan glycoside (4) were isolated from the leaves and twigs of Osteomeles schwerinae. The structures of the new compounds were established by spectroscopic data interpretation. The inhibitory effects of 1–4 on rat lens aldose reductase in vitro were examined, and compounds 1–3 markedly inhibited the enzyme with IC₅₀ values of 3.8 to 13.8 μ ...
... Chemicals targeting the liver stage (LS) of the malaria parasite are useful for causal prophylaxis of malaria. In this study, four lichen metabolites, evernic acid (1), vulpic acid (2), psoromic acid (3), and (+)-usnic acid (4), were evaluated against LS parasites of Plasmodium berghei. Inhibition of P. falciparum blood stage (BS) parasites was also assessed to determine stage specificity. Compoun ...
Danio rerio; advanced glycation end products; chemical structure; glucose; inhibitory concentration 50; larvae; proanthocyanidins; spectroscopy
Abstract:
... Three new A-type proanthocyanidins (1–3), ent-epiafzelechin-(2α→O→7,4α→8)-ent-afzelechin 3′-O-β-d-glycopyranoside (1), ent-epiafzelechin-(2α→O→7,4α→8)-ent-epiafzelechin-(2α→O→7,4α→8)-ent-afzelechin (2), and ent-epiafzelechin-(2α→O→7,4α→8)-ent-epicatechin-(2α→O→7,4α→8)-ent-afzelechin (3), and three known compounds (4–6) were isolated from the whole plant of Spenceria ramalana. The structures of the ...
... Spirocitromycetin, an antiosteoporotic polyketide bearing a unique spirocycle, was characterized from a human mucus sputum-derived Penicillium velutinum. Its structure and absolute configuration were elucidated spectrally, with its biosynthetic pathway likely mediated via polivione, a reported heptaketide. Spirocitromycetin was shown to be antiosteoporotic at 0.1 μM in the prednisolone-induced ost ...
... This project was focused on the discovery of novel compounds that promote endogenous β-cell regeneration. Screening of extracts identified the fungus Stachybotrys chartarum as a promising candidate. After fermentation and extraction of S. chartarum, we isolated five new prenylated xanthones, namely, staprexanthones A–E (1–5), with staprexanthone A (1) being the first natural xanthone bearing a rar ...
Danio rerio; Gonyaulax; biomass; hydroxylation; liquid chromatography; mass spectrometry; nuclear magnetic resonance spectroscopy; solvents; toxicity; yessotoxin
Abstract:
... Liquid chromatography–high-resolution mass spectrometry (LC-HRMS) analysis of a Namibian strain of Gonyaulax spinifera showed the presence of a number of yessotoxins (YTXs). Principal among these were YTX (1), homoYTX (2), and a tentative hydroxylated analogue that did not correspond to any previously confirmed YTX structures. Culturing the G. spinifera strain afforded sufficient biomass for purif ...
... Bakuchiol, a prenylated phenolic monoterpene derived from the fruit of Psoralen corylifolia L. (Buguzhi), is widely used to treat tumors, viruses, inflammation, and bacterial infections. In this study, we designed and synthesized 30 bakuchiol derivatives to identify new anti-inflammatory drugs. The anti-inflammatory activities of the derivatives were screened using lipopolysaccharide-induced RAW26 ...