Isolation and Structure Elucidation of New Metabolites from the Mariana-Trench-Associated Fungus sp. SY2601.

Fungi are important resource for the discovery of novel bioactive natural products. This study investigated the metabolites produced by Mariana-Trench-associated fungus sp. SY2601 in EY liquid and rice solid media, resulting in the isolation and structure determination of 28 metabolites, including five new compounds, asperindopiperazines A-C (-), 5-methoxy-8,9-dihydroxy-8,9-deoxyaspyrone (), and 12-aspertetranone D ().

New Hygrocins K-U and Streptophenylpropanamide A and Bioactive Compounds from the Marine-Associated sp. ZZ1956.

Marine-derived actinomycetes are one of the most important sources for the discovery of novel bioactive natural products. This study characterized the isolation, structural elucidation and biological activity evaluation of thirty compounds, including twelve previously undescribed compounds, namely hygrocins K-U (-, and ) and streptophenylpropanamide A (), from the marine-associated actinomycete sp. ZZ1956.

Cytotoxic metabolites from the marine-associated Streptomyces sp. ZZ1944.

Marine-derived actinomycetes from the genus Streptomycete have a huge potential for the production of metabolites with structural and bioactive uniqueness and diversity. This study described the isolation and structural elucidation of twenty metabolites, including seven previously unreported compounds galbonolide H, galbonolide I, streptophenylpropionic acid A, treptophenylpropyl ester A, streptophenvaleramide A, seco-geldanamycin A and streptorapamycin A, from the marine-associated Streptomycete sp. ZZ1944.

Talaromydien a and talaroisocoumarin A, new metabolites from the marine-sourced fungus sp. ZZ1616.

New talaromydien A and talaroisocoumarin A (), together with nine known compounds (-), were isolated from a culture of the marine-derived sp. ZZ1616 in potato dextrose broth medium. Structures of the new compounds were elucidated based on their HRESIMS data, NMR spectroscopic analyses, the modified Mosher's method, ECD, C NMR and optical rotation calculations.

Multitask CapsNet: An Imbalanced Data Deep Learning Method for Predicting Toxicants.

Drug development has a high failure rate, with safety properties constituting a considerable challenge. To reduce risk, in silico tools, including various machine learning methods, have been applied for toxicity prediction. However, these approaches often confront a serious problem: the training data sets are usually biased (imbalanced positive and negative samples), which would result in model training difficulty and unsatisfactory prediction accuracy.

Streptonaphthyridine A, a new naphthyridine analogue with antiproliferative activity against human glioma cells from mariana trench-associated actinomycete sp. SY2111.

A new naphthyridine analogue, named streptonaphthyridine A (), together with eight previously reported compounds (-), were isolated from a Mariana Trench sediment-associated actinomycete sp. SY2111. Planar structure of streptonaphthyridine A was established by analyses of its HRESIMS data and extensive NMR spectra and its absolute configuration was determined by a combination of single crystal X-ray diffraction analysis and optical rotation calculations.

Evaluation of the antiproliferative activity of 106 marine microbial metabolites against human lung cancer cells and potential antiproliferative mechanism of purpuride G.

A total of 106 marine microbial metabolites were evaluated for their antiproliferative activity against human lung cancer cells. Results showed that 23 compounds exhibited activity in inhibiting the proliferation of A549 and H157 cells with IC values ranging from 1.5 to 48.

A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors.

Residual disease is the major cause for colorectal cancer (CRC) relapse. Herein, we explore whether and how a natural molecule CADPE killed heterogenic populations in a panel of CRC cell lines with KRAS/BRAF mutations that are natively resistant to EGFR- or VEGFR-targeted therapy, without sparing persistent cells, a reservoir of the disease relapse. Results showed that CADPE killed the tumor bulk and residual cells in the panel of CRC cell lines, rapidly inactivated c-Myc, STAT3, and NF-κB, and then decreased the protein levels of key signaling molecules for CRC, such as β-catenin, Notch1, and the nodes of mTOR pathways; eukaryotic translation initiation factors (eIF4F); anti-apoptotic proteins (Bcl-xl, Mcl-1, and survivin); and stemness-supporting molecules (CD133, Bim-1, and VEGF).

Bioactive Alkaloids from the Actinomycete sp. ZZ1866.

The new alkaloids marinacarbolines E-Q (-, -), caerulomycin N (), and actinoallonaphthyridine A (), together with the known marinacarboline C () and cyanogramide (), were isolated from the actinomycete sp. ZZ1866. The structures of the isolated compounds were elucidated based on their HRESIMS data, extensive NMR spectroscopic analyses, Mosher's method, ECD calculations, single-crystal X-ray diffraction analysis, and chemical degradation studies.

New Antifungal Metabolites from the Mariana Trench Sediment-Associated Actinomycete sp. SY1965.

New streptothiazolidine A (), streptodiketopiperazines A () and B (), and ()-1-(3-ethylphenyl)-1,2-ethanediol (), together with eight known compounds (-), were isolated from the Mariana Trench sediment-associated actinomycete sp. SY1965. The racemic mixtures of (±)-streptodiketopiperazine ( and ) and (±)-1-(3-ethylphenyl)-1,2-ethanediol ( and ) were separated on a chiral high-performance liquid chromatography (HPLC) column.

Bioactive Metabolites from the Mariana Trench Sediment-Derived Fungus sp. SY2107.

Mariana Trench sediments are enriched in microorganisms, however, the structures and bioactivities of their secondary metabolites are not very known. In this study, a fungus sp. SY2107 was isolated from a sample of Mariana Trench sediment collected at a depth of 11000 m and an extract prepared from the culture of this fungus in rice medium showed antimicrobial activities.

A rare diketopiperazine glycoside from marine-sourced sp. ZZ446.

Two diketopiperazines were isolated from a culture of the marine-derived actinomycete sp. ZZ446. Their structures were elucidated as maculosin () and maculosin---L-rhamnopyranoside () based on their NMR and HRESIMS data, specific rotation, and chemical degradation.

Novel cyclohexene and benzamide derivatives from marine-associated sp. ZZ502.

Three new compounds and the known benzamides of 2-acetamido-3-hydroxybenzamide, 2-amino-3-hydroxybenzamide, and 2-aminobenzamide were isolated from the culture of a marine actinomycete sp. ZZ502. Structures of the new compounds were determined as 3-amino-2-carboxamine-6()-chloro-4(),5()-dihydroxy-cyclohex-2-en-1-one, 3-amino-2-carboxamine-4(),6()-dihydroxy-cyclohex-2-en-1-one, and 3-hydroxy-2-propionamidobenzamide based on extensive NMR spectroscopical analysis, HRESIMS data, ECD calculation, and X-ray diffraction analysis.

Bioactive Penicipyrrodiether A, an Adduct of GKK1032 Analogue and Phenol A Derivative, from a Marine-Sourced Fungus Penicillium sp. ZZ380.

Penicipyrrodiether A, an adduct of GKK1032 analogue and phenol A derivative, was isolated from a culture of marine-associated fungus Penicillium sp. ZZ380 and represents the first example of this type of fungal metabolite. Its structure was elucidated by extensive spectroscopic analyses, including 1D- and 2D-NMR, HRESIMS, MS/MS, and electronic circular dichroism calculation as well as single-crystal X-ray diffraction.

Peniciphenalenins A-F from the culture of a marine-associated fungus Penicillium sp. ZZ901.

Marine-derived fungi of the genus Penicillium represent a huge potential for synthesizing the secondary metabolites with structural and bioactive uniqueness and diversity. In this study, six previously undescribed compounds peniciphenalenins A-F and four known compounds (+)-sclerodin, (+)-scleroderolide, (+)-sclerodione, and physcion were isolated from the culture of a marine-derived fungus Penicillium sp. ZZ901.

Anti-glioma Efficacy and Mechanism of Action of Tripolinolate A from Tripolium pannonicum.

Tripolinolate A as a new bioactive phenolic ester was previously isolated from a halophyte of . However, the and anti-glioma effects and mechanism of tripolinolate A have not been investigated. This study has demonstrated that (1) tripolinolate A inhibited the proliferation of different glioma cells with IC values of 7.

Anti-glioma Natural Products Downregulating Tumor Glycolytic Enzymes from Marine Actinomycete Streptomyces sp. ZZ406.

Marine natural products are important resources for discovering novel anticancer drugs. In this study, an extract prepared from the culture of a sea anemone-derived actinomycete Streptomyces sp. ZZ406 in soluble starch and casein-related liquid medium was found to have activity in inhibiting the proliferation of glioma cells and reducing the production of lactate in glioma cells.

Anti-colorectal cancer effects of tripolinolate A from Tripolium vulgare.

Tripolinolate A (TLA) is recently identified as a new compound from a halophyte plant Tripolium vulgare and has been shown to have significant in vitro activity against the proliferation of colorectal cancer and glioma cells. This study was designed to further investigate the effects of TLA on the proliferation of human normal cells, and the apoptosis and cell cycle in colorectal cancer cells, and the growth of tumors in the colorectal cancer-bearing animals. The data obtained from this study demonstrated that: 1) TLA had much less cytotoxicity in the human normal cells than the colorectal cancer cells; 2) TLA remarkably induced apoptosis in the human colorectal cancer cells and blocked cell cycle at G/M phase, and 3) TLA had significant anti-colorectal cancer activity in the tumor-bearing animals.

A unique indolizinium alkaloid streptopertusacin A and bioactive bafilomycins from marine-derived Streptomyces sp. HZP-2216E.

Streptopertusacin A, a unique indolizinium alkaloid existing as a zwitterion, and six bafilomycins including two previously undescribed ones of 21,22-en-bafilomycin D and 21,22-en-9-hydroxybafilomycin D were isolated from a culture of the seaweed-derived Streptomyces sp. HZP-2216E. Structures of these isolated compounds were determined based on extensive NMR spectroscopic analyses, HRESIMS and MS-MS data.

Antiglioma pseurotin A from marine Bacillus sp. FS8D regulating tumour metabolic enzymes.

Pseurotin A was isolated from a culture of marine Bacillus sp. FS8D and showed to be active against the proliferation of four different glioma cells with IC values of 0.51-29.

Bioactive Bafilomycins and a New N-Arylpyrazinone Derivative from Marine-derived Streptomyces sp. HZP-2216E.

A MeOH extract prepared from culture of an actinomycete sp. HZP-2216E isolated from marine green algae was found to significantly inhibit proliferation of human glioma cells. Two different media were applied to culture this marine actinomycete, which produced two new compounds of 23--butyrylbafilomycin D and streptoarylpyrazinone A, together with known bafilomycin D, 9-hydroxybafilomycin D, and bafilomycin A.

Cytotoxic Bagremycins from Mangrove-Derived Streptomyces sp. Q22.

New bagremycins C-E (3-5) and bagrelactone A (6), together with known bagremycins A (1) and B (2), 4-hydroxystyrene (7), and 4-hydroxystyrene 4-O-α-d-galactopyranoside (8), were isolated from a mangrove-derived actinomycete, Streptomyces sp. Q22. Structures of these new compounds were elucidated based on their NMR and HRESIMS spectroscopic data as well as chemical degradation.

Rare Polyene-polyol Macrolides from Mangrove-derived Streptomyces sp. ZQ4BG.

Bioactive natural products from mangrove-derived actinomycetes are important sources for discovery of drug lead compounds. In this study, an extract prepared from culture of an actinomycete Streptomyces sp. ZQ4BG isolated from mangrove soils was found to have activity in inhibiting proliferation of glioma cells.

Antiproliferative cyclodepsipeptides from the marine actinomycete Streptomyces sp. P11-23B downregulating the tumor metabolic enzymes of glycolysis, glutaminolysis, and lipogenesis.

Two cyclodepsipeptides and a known cyclodepsipeptide valinomycin were isolated from a culture of the marine actinomycete Streptomyces sp. P11-23B. Their structures were established based on NMR, HRESIMS, and MS-MS spectroscopic interpretation as well as by chemical degradation.