Six new highly oxygenated chloroazaphilone derivatives, isochromophilones A–F (1–6), were obtained from the mangrove-derived fungus Diaporthe sp. SCSIO 41011, together with six known analogues (7–12). The structures of 1–6 including absolute configurations determined by detailed NMR, MS spectroscopic analyses, and electronic circular dichroism spectra. Compounds 1 2 represent first reported azaphilones lacking a carbonyl group at C-6. Compound 8 exhibited cytotoxic activities against three...

To discover novel osteoclast-targeting antiosteoporosis leads from natural products, we identified 40 tanzawaic acid derivatives, including 22 new ones (1–8, 14–19, 27–32, 37, and 38), the South China Sea mangrove-derived fungus Penicillium steckii SCSIO 41025. Penicisteck F (2), one of derivatives showing most potent NF-κB inhibitory activity, remarkably inhibited osteoclast generation in vitro. Mechanistically, 2 reduced RANKL-induced IκBα degradation, p65 nuclear translocation, activation...

Atherosclerosis is a chronic inflammatory vascular disease characterized by lipid metabolism disorder and accumulation. Equisetin (EQST) hemiterpene compound isolated from fungus of marine sponge origin, which has antibacterial, anti-inflammatory, lipid-lowering, weight loss effects. Whether EQST anti-atherosclerotic activity not been reported. In this study, we revealed that displayed anti- atherosclerosis effects through inhibiting macrophage response, uptake foam cell formation in vitro,...

Eleven diketopiperazine and fumiquinazoline alkaloids (1–11) together with a tetracyclic triterpenoid helvolic acid (12) were obtained from the cultures of deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures these compounds (1–12) determined mainly by extensive NMR, ESIMS spectra data comparison previously described compounds. Besides, anti-tuberculosis, cytotoxic, antibacterial, COX-2 inhibitory antiviral activities evaluated. Gliotoxin (3), 12,13-dihydroxy-fumitremorgin...

Nitrobenzoyl sesquiterpenoids are rare from natural sources. Two new nitrobenzoyl sesquiterpenoids, insulicolide B (1) and C (3), the product 14-O-acetylinsulicolide A (2) were isolated culture extracts of marine-derived fungus Aspergillus ochraceus Jcma1F17, together with three known (4–6) a derivative sesquiterpenoid (7). The structures compounds, including their absolute configurations, determined by NMR MS spectroscopic data analyses comparison between calculated experimental ECD...

Two new alkaloids, fumigatosides E (1) and F (2), a natural product, 3, 7-diketo-cephalosporin P1 (6) along with five known compounds (3–5, 7, 8) were isolated from deep-sea derived fungal Aspergillus fumigatus SCSIO 41012. Their structures determined by extensive spectroscopic data analysis, including 1D, 2D nuclear magnetic resonance (NMR) mass spectrometry (MS), comparison between the calculated experimental electronic circular dichroism (ECD) spectra. In addition, all tested for...

Anti-renal cell carcinoma (RCC) agents with new mechanisms of action are urgently needed. Twenty-seven natural products the piericidin class, including 17 ones, obtained from a marine-derived Streptomyces strain, and several them show strong inhibitory activities against ACHN renal cells. By exploring two representative compounds, A (PA) glucopiericidin (GPA), peroxiredoxin 1 (PRDX1) is detected as potential target by transcriptome data PA-treated cells, well paired RCC tumor versus adjacent...

Influenza A virus (IAV) is a severe worldwide threat to public health and economic development due its high morbidity mortality. Marine-derived fungi have been evidenced as prolific source for the discovery of pharmacologically-active lead compounds. During course our search novel bioactive substances from marine microorganisms, six new polyketides, including two octaketides (1-2), one chromone derivative (13), highly substituted phthalides (17-18), α-pyrone (21) along with 22 known...

Human dihydroorotate dehydrogenase (hDHODH) is an attractive tumor target essential to de novo pyrimidine biosynthesis. Novel potent hDHODH inhibitors with low toxicity are urgently needed. Herein, we demonstrate the isolation of 25 ascochlorin (ASC) derivatives, including 13 new ones, from coral-derived fungus Acremonium sclerotigenum, and several them showed pronounced inhibitions against triple-negative breast cancer (TNBC) cell lines, MDA-MB-231/-468. Interestingly, found that required...

One new depsidone derivative, aspergillusidone H (3), along with seven known biosynthetically related chlorinated polyketides, were obtained from the Beibu Gulf coral-derived fungus Aspergillus unguis GXIMD 02505. Their structures determined by comprehensive physicochemical and spectroscopic data interpretation. Notably, X-ray crystal structure of 2 previously unknown absolute configuration 8, assigned ECD calculations, are described here for first time. Compounds 1–5, 7 8 exhibited...

An unprecedented di-seco-indole diterpenoid, peniditerpenoid A (1), and a rare N-oxide-containing indole diterpenoid derivative, B (2), together with three known ones (3–5), were obtained from the mangrove-sediment-derived fungus Penicillium sp. SCSIO 41411. Their structures determined by analysis of spectroscopic data, quantum chemical calculations, X-ray diffraction analyses. Peniditerpenoid (1) inhibited lipopolysaccharide-induced NF-κB an IC50 value 11 μM further effectively prevented...

The study aims to explore the sperm parameters that affect early embryo development in vitro fertilization (IVF) and their relationship with zinc homeostasis seminal plasma antioxidation. semen samples were incubated at 37°C for 1, 2, 3, 4 h, progressive motility (PR) was analyzed. We found PR significantly decreased after 3 h of incubation ( p < 0.01) further 0.001). correlation analysis showed significant positively correlated transferable rate r = 0.155, 0.026) blastocyst formation...

Sixteen polyketides, including six new compounds (1–2, and 5–8), were isolated from the culture of marine sponge-associated fungus Neopestalotiopsis sp. SCSIO 41422. Their structures elucidated through NMR, MS spectroscopic analyses, calculated electronic circular dichroism, quantum chemical NMR calculations, X-ray single-crystal diffraction. To screen evaluate inhibitory activity these polyketides in renal fibrosis, a TGF-β1-stimulated HK-2 cell model was used. All tested (1, 5–8, 11–12) at...

Three new polyketides named trichbenzoisochromen A (1), 5,7-dihydroxy-3-methyl -2-(2-oxopropyl)naphthalene-1,4-dione (2) and 7-acetyl-1,3,6-trihydroxyanthracene-9,10- dione (3) together with six known compounds (4-9) were isolated from a sponge-derived fungus Trichoderma sp. SCSIO41004. The structures of three (1-3) determined by the extensive spectroscopic analysis, including 1D, 2D NMR HRESIMS data. absolute configuration compound 1 was confirmed specific optical rotation value CD spectra...

Four novel 1-oxa-8,10-diazaspiro[5.5]undecane containing diketopiperazine alkaloids from <italic>Aspergillus versicolor</italic> SCSIO 41016.

A strategy integrating in silico molecular docking with LXRα and phenotypic assays was adopted to discover anti-hypercholesterolemia agents a small library containing 205 marine microorganism-derived natural products, collected by our group recent years. Two fumitremorgin derivatives, 12R,13S-dihydroxyfumitremorgin C (1) tryprostatin (3), were identified as potential agonists, real-time qPCR Western blot (WB) analysis, together surface plasmon resonance (SPR) assay. The...

Malbranchea circinata SDU050, a fungus derived from deep-sea sediment, is prolific producer of diverse secondary metabolites. Genome sequencing revealed the presence at least 69 biosynthetic gene clusters (BGCs), including 30 encoding type I polyketide synthases (PKSs). This study reports isolation and identification four classes metabolites wild-type M. alongside five additional metabolite classes, three novel cytochalasins (7–9), obtained mutant strain through metabolic blockade strategy....

ABSTRACT Two new compounds, 5‐methoxymethylmellein ( 1 ) and 6‐benzyl‐2‐hydroxy‐5‐methoxy‐3‐methylpyradine 2 ), along with nine known compounds 3–11 were obtained from the mangrove endophytic fungus Diaporthe sp. SCSIO 41011. Their structures determined based on extensive spectroscopic analysis by comparison literature. The absolute configuration of was assigned electronic circular dichroism calculations. structure naturally rare compound unambiguously confirmed single‐crystal X‐ray...

Two new polyketides, xerucitrinin A (1) and coniochaetone M (8), one steroid, 16α-methylpregna-17α,19-dihydroxy-(9,11)-epoxy-4-ene-3,18-dione-20-acetoxy (13), together with eleven known analogues were isolated from fungus Penicillium citrinum SCSIO 41017 associated the sponge Callyspongia sp. Their structures absolute configurations elucidated by NMR spectra, MS, CD, optical rotation, X-ray crystallography, compared literature data. Biological evaluation results revealed that 5 exhibited...

Osteoclasts are unique cells to absorb bone. Targeting osteoclast differentiation is a therapeutic strategy for osteolytic diseases. Natural marine products have already become important sources of new drugs. The naturally occurring nitrobenzoyl sesquiterpenoids first identified from fungi in 1998 bioactive compounds with special structure, but their pharmacological functions largely unknown. Here, we investigated six fungus-derived on osteoclastogenesis and elucidated the...

Seven new 18-residue peptaibols, trichorzins A–G (1–7), were isolated from the sponge-derived fungus Trichoderma sp. GXIMD 01001. Their structures and configurations characterized by a comprehensive interpretation of NMR spectroscopic data, MS/MS fragmentation, Marfey's method, ECD analysis. The general sequences are as follows: Ac-Aib1-Ala/Ser2-Ala3-Aib/Iva4-Iva5-Gln6-Aib/Iva7-Val/allo-Ile8-Aib9-Gly10-Leu11-Aib12-Pro13-Leu14-Aib15-Aib16-Gln17-Trpol/Pheol18. obtained compounds assessed for...