| Apicidin Attenuates MRSA Virulence through Quorum-Sensing Inhibition and Enhanced Host Defense |
2019 |
457 |
Recurrent epidemics of drug-resistant Staphylococcus aureus illustrate the rapid lapse of antibiotic efficacy following clinical implementation. Over the last decade, community-associated methicillin-resistant S. aureus (MRSA) has emerged as a domina... |
| Benzoquinones and Terphenyl Compounds As Phosphodiesterase-4B Inhibitors from a Fungus of the Order Chaetothyriales (MSX 47445) |
2013 |
1760 |
Three bioactive compounds were isolated from an organic extract of an ascomycete fungus of the order Chaetothyriales (MSX 47445) using bioactivity-directed fractionation as part of a search for anticancer leads from filamentous fungi. Of these, two w... |
| Biosynthesis of Fluorinated Peptaibols Using a Site-Directed Building Block Incorporation Approach |
2017 |
1002 |
Synthetic biological approaches, such as site-directed biosynthesis, have contributed to the expansion of the chemical space of natural products, making possible the biosynthesis of unnatural metabolites that otherwise would be difficult to access. S... |
| Biosynthetically Distinct Cytotoxic Polyketides from Setophoma terrestris |
2015 |
551 |
Sixteen polyketides belonging to diverse structural classes, including monomeric/dimeric tetrahydroxanthones and resorcylic acid lactones, were isolated from an organic extract of a fungal culture Setophoma terrestris (MSX45109) by bioactivity-direct... |
| Chemoinformatic Expedition of the Chemical Space of Fungal Products |
2016 |
526 |
Aim: Fungi are valuable resources for bioactive secondary metabolites. However, the chemical space of fungal secondary metabolites has been studied only on a limited basis. Herein, we report a comprehensive chemoinformatic analysis of a unique set of... |
| Chemoselective fluorination and chemoinformatic analysis of griseofulvin: Natural vs fluorinated fungal metabolites |
2017 |
1044 |
[2017-2018 UNCG University Libraries Open Access Publishing Fund Grant Winner.] Griseofulvin is a fungal metabolite and antifungal drug used for the treatment of dermatophytosis in both humans and animals. Recently, griseofulvin and its analogues hav... |
| Contrasting Roles of H3K4me3 and H3K9me3 in Regulation of Apoptosis and Gemcitabine Resistance in Human Pancreatic Cancer Cells |
2018 |
352 |
Background: Pancreas ductal adenocarcinoma (PDAC) has the most dismal prognosis among all human cancers since it is highly resistant to chemotherapy, radiotherapy and immunotherapy. The anticipated consequence of all therapies is induction of tumor a... |
| Cyclodepsipeptides, Sesquiterpenoids, and Other Cytotoxic Metabolites from the Filamentous Fungus Trichothecium sp. (MSX 51320) |
2011 |
1737 |
Two new cyclodepsipeptides (1 and 2), two new sesquiterpenoids (3 and 4), and the known compounds guangomide A (5), roseotoxin S, and three simple trichothecenes were isolated from the cytotoxic organic extract of a terrestrial filamentous fungus, Tr... |
| Cytotoxic and antimicrobial drimane meroterpenoids from a fungus of the Stictidaceae (Ostropales, Ascomycota) |
2021 |
425 |
As part of our ongoing research on bioactive fungal metabolites, two new metabolites were isolated from a fungus of the Stictidaceae (strain MSX62440), dasyscyphins F and G (1 and 3), along with the known dasyscyphin C (2). Compound 1 was characteriz... |
| Cytotoxic epipolythiodioxopiperazine alkaloids from filamentous fungi of the Bionectriaceae |
2012 |
2140 |
Bioactivity-directed fractionation of the organic extracts of two filamentous fungi of the Bionectriaceae, strains MSX 64546 and MSX 59553 from the Mycosynthetix library, led to the isolation of a new dimeric epipolythiodioxopiperazine alkaloid, vert... |
| Cytotoxic Xanthone-Anthraquinone Heterodimers from an Unidentified Fungus of the Order Hypocreales (MSX 17022) |
2011 |
2012 |
Two new xanthone-anthraquinone heterodimers, acremoxanthone C (5) and acremoxanthone D (2), have been isolated from an extract of an unidentified fungus of the Order Hypocreales (MSX 17022) by bioactivity-directed fractionation as part of a search fo... |
| Delivery of eupenifeldin via polymer-coated surgical buttresses prevents local lung cancer recurrence |
2021 |
517 |
Lung cancer is the leading cause of cancer deaths worldwide. Unfortunately, high recurrence rates and poor survival remain despite surgical resection and conventional chemotherapy. Local drug delivery systems are a promising intervention for lung can... |
| Dereplicating and Spatial Mapping of Secondary Metabolites from Fungal Cultures in Situ |
2015 |
1575 |
Ambient ionization mass spectrometry techniques have recently become prevalent in natural product research due to their ability to examine secondary metabolites in situ. These techniques retain invaluable spatial and temporal details that are lost th... |
| Development and Utilization of a Palladium-Catalyzed Dehydration of Primary Amides To Form Nitriles |
2018 |
1021 |
A palladium(II) catalyst, in the presence of Selectfluor, enables the efficient and chemoselective transformation of primary amides into nitriles. The amides can be attached to aromatic rings, heteroaromatic rings, or aliphatic side chains, and the r... |
| Discovery of Anticancer Agents of Diverse Natural Origin |
2016 |
481 |
Recent progress is described in an ongoing collaborative multidisciplinary research project directed towards the purification, structural characterization, chemical modification, and biological evaluation of new potential natural product anticancer a... |
| Effects of (5z)-7-Oxozeaenol on MDA-MB-231 Breast Cancer Cells |
2012 |
467 |
Aim: (5Z)-7-Oxozeaenol was studied to reveal the path through which it exerts its effects on triple-negative MDA-MB-231 breast cancer cells. Materials and Methods: The apoptotic effect of (5Z)-7-oxozeaenol on MDA-MB-231 cancer cells was analyzed by c... |
| Effects of (5z)-7-Oxozeaenol on the Oxidative Pathway of Cancer Cells |
2012 |
352 |
Aim: As part of an on going investigation of novel anticancer agents from natural origin, the biological and cellular effects of (5Z)-7-oxozeaenol on cancer cells were investigated. Materials and Methods: The expression of nuclear factor kappa B (NF-... |
| Enhanced Dereplication of Fungal Cultures Via Use of Mass Defect Filtering |
2017 |
995 |
Effective and rapid dereplication is a hallmark of present-day drug discovery from natural sources. This project strove to both decrease the time and expand the structural diversity associated with dereplication methodologies. A 5?min liquid chromato... |
| Epigenetic Manipulation of a Filamentous Fungus by the Proteasome-Inhibitor Bortezomib Induces the Production of an Additional Secondary Metabolite |
2014 |
967 |
The use of epigenetic modifiers, such as histone deacetylase inhibitors and DNA methyltransferase inhibitors, has been explored increasingly as a technique to induce the production of additional microbial secondary metabolites. The application of suc... |
| Fungal Identification Using Molecular Tools: A Primer for the Natural Products Research Community |
2017 |
2171 |
Fungi are morphologically, ecologically, metabolically, and phylogenetically diverse. They are known to produce numerous bioactive molecules, which makes them very useful for natural products researchers in their pursuit of discovering new chemical d... |
| High-Resolution MS, MS/MS, and UV Database of Fungal Secondary Metabolites as a Dereplication Protocol for Bioactive Natural Products |
2013 |
1108 |
A major problem in the discovery of new biologically active compounds from natural products is the reisolation of known compounds. Such reisolations waste time and resources, distracting chemists from more promising leads. To address this problem, de... |
| In Situ Mass Spectrometry Monitoring of Fungal Cultures Led to the Identification of Four Peptaibols with a Rare Threonine Residue |
2017 |
969 |
Peptaibols are an intriguing class of fungal metabolites due both to their wide range of reported bioactivities and to the structural variability that can be generated by the exchange of variable amino acid building blocks. In an effort to streamline... |
| Isolation, Semisynthesis, Covalent Docking and Transforming Growth Factor Beta-Activated Kinase 1 (TAK1)-Inhibitory Activities of (5Z)-7-Oxozeaenol Analogues |
2015 |
1243 |
(5Z)-7-Oxozeanol and related analogues were isolated and screened to explore their activity as TAK1 inhibitors. Seven analogues were synthesized and more than a score of natural products isolated that examined the role that different areas of the mol... |
| Meroterpenoids from Neosetophoma sp.: A Dioxa[4.3.3]propellane Ring System, Potent Cytotoxicity, and Prolific Expression |
2019 |
1076 |
Six fungal metabolites, of which five were new, including one (1) with a dioxa[4.3.3]propellane ring system, were discovered, identified, and structurally elucidated from Neosetophoma sp. (strain MSX50044); these compounds are similar to the bis-trop... |
| The MLL1-H3K4me3 Axis-Mediated PD-L1 Expression and Pancreatic Cancer Immune Evasion |
2017 |
474 |
Background: Pancreatic cancer is one of the cancers where anti-PD-L1/PD-1 immunotherapy has been unsuccessful. What confers pancreatic cancer resistance to checkpoint immunotherapy is unknown. The aim of this study is to elucidate the underlying mech... |
| Nanoparticle Drug-Delivery Systems for Peritoneal Cancers: A Case Study of the Design, Characterization and Development of the Expansile Nanoparticle |
2017 |
378 |
Nanoparticle (NP)-based drug-delivery systems are frequently employed to improve the intravenous administration of chemotherapy; however, few reports explore their application as an intraperitoneal therapy. We developed a pH-responsive expansile nano... |
| New Diketopiperazine Dimer from a Filamentous Fungal Isolate of Aspergillus sydowii |
2015 |
930 |
Prior investigations of filamentous fungi in our group have resulted in the isolation of several new and biologically active natural products.[1-3] Continuing these investigations, we have now analyzed the metabolites from a fungal isolate of Aspergi... |
| Obionin B: an o-pyranonaphthoquinone decaketide from an unidentified fungus (MSX 63619) from the order Pleosporales |
2011 |
1409 |
A fungal extract (MSX 63619), from the Mycosynthetix library of over 50,000 fungi, displayed promising cytotoxicity against a human tumor cell panel. Bioactivity-directed fractionation led to the isolation of an o-pyranonaphthoquinone decaketide, whi... |
| Optimizing Production and Evaluating Biosynthesis in Situ of a Herbicidal Compound, Mevalocidin, from Coniolariella Sp. |
2016 |
1312 |
Mevalocidin is a fungal secondary metabolite produced by Coniolariella sp. It is a unique phytotoxin that demonstrates broad spectrum post-emergent herbicidal properties. With limited options for weed control, the commercialization of a natural produ... |
| Peptaibols from Two Unidentified Fungi of the Order Hypocreales with Cytotoxic, Antibiotic, and Anthelmintic Activities |
2012 |
1084 |
As part of an ongoing investigation of filamentous fungi for anticancer leads, an active culture was identified from the Mycosynthetix library (MSX 70741, of the order Hypocreales, Ascomycota). The fungal extract exhibited cytotoxic activity against ... |
| Peptaibols, Tetramic Acid Derivatives, Isocoumarins, and Sesquiterpenes from a Bionectria sp. (MSX 47401) |
2013 |
1452 |
An extract of the filamentous fungus Bionectria sp. (MSX 47401) showed both promising cytotoxic activity (>90% inhibition of H460 cell growth at 20 µg/mL) and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). A bioact... |
| Plasma Pharmacokinetics and Bioavailability of Verticillin A Following Different Routes of Administration in Mice Using Liquid Chromatography Tandem Mass Spectrometry |
2017 |
249 |
Verticillin A is a natural product isolated from fungal cultures and has displayed potent antibiotic, antiviral, nematocidal, and anticancer properties in vitro. While in vivo studies have been limited due to sparse supply, the in vivo efficacy data ... |
| Prealamethicin F50 and Related Peptaibols from Trichoderma arundinaceum: Validation of their Authenticity via in situ Chemical Analysis |
2017 |
1029 |
In the field of natural products chemistry, a common question pertains to the authenticity of an isolated compound, i.e. are the interesting side chains biosynthesized naturally or an artefact of the isolation/purification processes? The droplet-liqu... |
| qNMR for Profiling the Production of Fungal Secondary Metabolites |
2017 |
1008 |
Analysis of complex mixtures is a common challenge in natural products research. Quantitative nuclear magnetic resonance spectroscopy offers analysis of complex mixtures at early stages and with benefits that are orthogonal to more common methods of ... |
| Resorcylic Acid Lactones with Cytotoxic and NF-KB Inhibitory Activities and Their Structure–Activity Relationships |
2011 |
1777 |
As part of our ongoing investigation of filamentous fungi for anticancer leads, an active fungal extract was identified from the Mycosynthetix library (MSX 63935; related to Phoma sp.). The initial extract exhibited cytotoxic activity against the H46... |
| Revisiting the Enniatins: A Review of Their Isolation, Biosynthesis, Structure Determination and Biological Activities |
2012 |
1127 |
Enniatins are cyclohexadepsipeptides isolated largely from Fusariumspecies of fungi, although they have been isolated from other genera, such as Verticillium and Halosarpheia. They were first described over 60 years ago, and their range of biological... |
| Romidepsin (Istodax, NSC 630176, FR901228, FK228, Depsipeptide): A Natural Product Recently Approved for Cutaneous T-Cell Lymphoma |
2011 |
1280 |
Romidepsin (Istodax), a selective inhibitor of histone deacetylases (HDACs), was approved for the treatment of cutaneous T-cell lymphoma in November 2009 by the US Food and Drug Administration. This unique natural product was discovered from cultures... |
| Scaffold Diversity of Fungal Metabolites |
2017 |
424 |
Many drug discovery projects rely on commercial compounds to discover active leads. However, current commercial libraries, with mostly synthetic compounds, access a small fraction of the possible chemical diversity. Natural products, in contrast, pos... |
| Sorbicillinoid Analogs with Cytotoxic and Selective Anti-Aspergillus Activities from Scytalidium album |
2014 |
976 |
As part of an ongoing project to explore filamentous fungi for anticancer and antibiotic leads, 11 compounds were isolated and identified from an organic extract of the fungus Scytalidium album (MSX51631) using bioactivity-directed fractionation agai... |
| Spiroscytalin, a New Tetramic Acid and Other Metabolites of Mixed Biogenesis from Scytalidium cuboideum |
2015 |
1232 |
Spiroscytalin (1), a new tetramic acid that possesses an uncommon spiro-ring fusion between a polyketide-derived octalin ring system and a 2,4-pyrrolidinedione, along with two known compounds, leporin B (2) and purpactin A (3), were isolated from a s... |
| Thielavin B Methyl Ester: A Cytotoxic Benzoate Trimer from an Unidentified Fungus (MSX 55526) from the Order Sordariales |
2011 |
1100 |
As part of our ongoing investigation of filamentous fungi for anticancer leads, an active fungal extract was identified from the Mycosynthetix library (MSX 55526; from the Order Sordariales). Bioactivity-directed fractionation yielded the known ergos... |
| Use of the Hollow Fiber Assay for the Discovery of Novel Anticancer Agents from Fungi |
2012 |
1143 |
The hollow fiber assay (HFA) is a drug discovery tool to aid investigators in the prioritization of lead compounds identified by in vitro testing for further development in animal models of disease. In the HFA, cells are cultured in hollow fibers con... |
| Verticillin A Inhibits Leiomyosarcoma and Malignant Peripheral Nerve Sheath Tumor Growth Via Induction of Apoptosis |
2016 |
1086 |
Objective: The heterogeneity of soft tissue sarcoma (STS) represents a major challenge for the development of effective therapeutics. Comprised of over 50 different histology subtypes of various etiologies, STS subsets are further characterized as ei... |
| Waol A, trans-dihydrowaol A, and cis-dihydrowaol A: polyketide-derived (gamma)-lactones from a Volutella species |
2013 |
1123 |
An organic extract of a filamentous fungus (MSX 58801), identified as a Volutella sp. (Hypocreales, Ascomycota), displayed moderate cytotoxic activity against NCI-H460 human large cell lung carcinoma. Bioactivity-directed fractionation led to the iso... |