A Systematic Review and Meta-Analysis of the Efficacy and Safety of Regorafenib in the Treatment of Metastatic Colorectal Cancer.

Background And Objective: Colorectal cancer (CRC) is a leading cause of cancer-related mortality worldwide. Despite advances in treatment, metastatic colorectal cancer (mCRC) remains a significant challenge due to its heterogeneity and resistance to therapy. Regorafenib, a multikinase inhibitor, can inhibit tumor progression through multiple mechanisms, thereby improving patient prognosis.

Terpestacin and Its Derivatives: Bioactivities and Syntheses.

Terpestacin (1), fusaproliferin (2), and their derivatives are a class of sesterterpenes featured by a trans-fused 5/15-membered ring skeleton. There are 45 natural products (1, 2, 4-27, 65-83) isolated from various wild fungi (Fusarium sp., Bipolaris sorokiniana, Arthrinium sp.

Two new Aspera chaetominines A and B, and a new derivative of terrein, isolated from marine sponge associated fungus SCSIO XWS04 F52.

Two new alkaloids, Aspera chaetominines A () and B (), a new derivative () of terrein, and together with known compounds () were isolated from marine sponge sp. -derived fungus SCSIO XWS04 F52, which was identified on the basis of morphology and ITS sequence analysis. The planar structures of were determined by spectroscopic (H, C NMR, HSQC, HMBC, and H-H COSY), and MS analysis.

C500 variants conveying complete mucosal immunity against fatal infections of pigs with serovar Choleraesuis C78-1 or F18+ Shiga toxin-producing .

serovar Choleraesuis ( Choleraesuis) C500 strain is a live, attenuated vaccine strain that has been used in China for over 40 years to prevent piglet paratyphoid. However, this vaccine is limited by its toxicity and does not offer protection against diseases caused by F18+ Shiga toxin-producing (STEC), which accounts for substantial economic losses in the swine industry. We recently generated a less toxic derivative of C500 strain with both and deletion ( Choleraesuis C520) and assessed its efficacy in mice.

Exploring Diverse Bioactive Secondary Metabolites from Marine Microorganisms Using Co-Culture Strategy.

The isolation and identification of an increasing number of secondary metabolites featuring unique skeletons and possessing diverse bioactivities sourced from marine microorganisms have garnered the interest of numerous natural product chemists. There has been a growing emphasis on how to cultivate microorganisms to enhance the chemical diversity of metabolites and avoid the rediscovery of known ones. Given the significance of secondary metabolites as a means of communication among microorganisms, microbial co-culture has been introduced.

A Chinese Herb Prescription "Fang-gan Decoction" Protects Against Damage to Lung and Colon Epithelial Cells Caused by the SARS-CoV-2 Spike Protein by Regulating the TGF-β/Smad2/3 and NF-κB Pathways.

Objective To explore the effects and mechanisms of a traditional Chinese medicine (TCM) prescription, "Fang-gan Decoction" (FGD), in protecting against SARS-CoV-2 spike protein-induced lung and intestinal injuries in vitro and in vivo.Methods Female BALB/c mice and three cell lines pretreated with FGD were stimulated with recombinant SARS-CoV-2 spike protein (spike protein). Hematoxylin-eosin (HE) staining and pathologic scoring of tissues, cell permeability and viability, and angiotensin-converting enzyme 2 (ACE2) expression in the lung and colon were detected.

Design, Synthesis, and Anticancer Activity of Novel 3,6-Diunsaturated 2,5-Diketopiperazines.

Based on the marine natural products piperafizine B, XR334, and our previously reported compound , fourteen novel 3,6-diunsaturated 2,5-diketopiperazine (2,5-DKP) derivatives (, , -, -), together with two known ones ( and ), were designed and synthesized as anticancer agents against the A549 and Hela cell lines. The MTT assay results showed that the derivatives , - and had moderate to good anticancer capacities, with IC values ranging from 0.7 to 8.

New Meroterpenoids and Anti-Osteoclastogenic Polyketides from the Mangrove-Derived fungus Arthrinium sp. SCSIO 41306.

Two new meroterpenoids, arthrinones A and B (1 and 2), along with six known compounds (3-8), were obtained from the fungus Arthrinium sp. SCSIO 41306. Comprehensive methods such as chiral-phase HPLC analysis and ECD calculations were applied to determine the absolute configurations.

Novel terpestacin derivatives with l-amino acid residue as anticancer agents against U87MG-derived glioblastoma stem cells.

Based on the natural product terpestacin, seventeen derivatives (1-17) with various l-amino acid side chains were designed and synthesized. Their anticancer activities against U87MG-derived glioblastoma stem cells (GSCs) were evaluated, and compounds 5, 11, 13 and 15 showed strong abilities to inhibit the proliferation (IC = 2.8-6.

Three unusual hybrid sorbicillinoids with anti-inflammatory activities from the deep-sea derived fungus Penicillium sp. SCSIO06868.

Under the guidance of MS/MS based molecular networking, bisorbicillchaetones A-C, three undescribed hybrid sorbicillinoids, were isolated from cultures of the deep-sea derived fungus Penicillium sp. SCSIO06868. The planar structures and absolute configurations of these compounds were determined by extensive spectroscopic analyses.

Suppression of Berberine and Probiotics ( and ) on the Growth of Colon Cancer With Modulation of Gut Microbiota and Butyrate Production.

Background And Objective: An increasing number of evidence has revealed that the gut microbiome functions in immunity, inflammation, metabolism, and homeostasis and is considered to be crucial due to its balance between human health and diseases such as cancer, leading to the emergence of treatments that target intestinal microbiota. Probiotics are one of them. However, many challenges remain regarding the effects of probiotics in cancer treatment.

Asperbenzophenone A and Versicolamide C, New Fungal Metabolites from the Soft Coral Derived Aspergillus sp. SCSIO 41036.

Two new compounds, asperbenzophenone A (1) and versicolamide C (5), together with fifteen known compounds were isolated from a soft coral derived fungus Aspergillus sp. SCSIO 41036. Their structures were elucidated by spectroscopic methods, ECD analysis, and by a comparison with data from the literature.

-Terphenyls as Anti-HSV-1/2 Agents from a Deep-Sea-Derived sp.

Guided by Global Natural Products Social molecular networking, two -terphenyl derivatives and one 4,5-diphenyl-2-pyrone analogue, peniterphenyls A-C (-), together with five known -terphenyl derivatives (-) and sulochrin (), were obtained from a deep-sea-derived sp. SCSIO41030. Their structures were elucidated using extensive NMR spectroscopic and HRESIMS data and by comparing the information with literature data.

Citrinin and α-pyrone derivatives with pancreatic lipase inhibitory activities from sp. SCSIO 41302.

One new citrinin monomer derivative (), and two new natural products α-pyrone analogues ( and ), were isolated from the sponge derived fungus sp. SCSIO 41302. Their structures were determined by extensive spectroscopic analysis, chiral-phase HPLC analysis, modified Mosher's method, ECD calculations, and X-ray single-crystal diffraction.

A glyoxylate-containing benzene derivative and butenolides from a marine algicolous fungus sp. SCSIO 41304.

A new glyoxylate-containing benzene derivative, methyl 2-(4-hydroxy-3-(3'-methyl-2'-butenyl)phenyl)-2-oxoacetate (), together with ten known compounds (-), were isolated from the marine algicolous fungus, sp. SCSIO 41304. Their planar structures and absolute configurations were elucidated by detailed NMR, MS spectroscopic analysis and comparing with literature data.

Gold-catalyzed oxidation of terminal alkynes to glyoxals and their reactions with 2-phenylimidazo[1,2-]pyridines: one-pot synthesis of 1,2-diones.

A novel one-pot protocol for the convenient and efficient synthesis of (2-phenylimidazo[1,2-]pyridin-3-yl)alkane-1,2-diones (3) in good yields (32-88%) from 2-phenylimidazo[1,2-]pyridines (1) and terminal alkynes (2) has been established with a wide range of substrate scope. A tandem reaction sequence containing gold-catalyzed double oxidations of terminal alkynes to generate glyoxals, nucleophilic addition of 2-phenylimidazo[1,2-]pyridines to glyoxals to yield α-hydroxyl ketones, and oxygenation of the α-hydroxyl ketones to afford the final products 3 under air atmosphere is involved in this method. Simple operation, mild reaction conditions, and widely available substrates make this strategy more affordable.

Intermittent fasting therapy promotes insulin sensitivity by inhibiting NLRP3 inflammasome in rat model.

Background: Substantial studies have demonstrated that fasting therapy (FT) can inhibit the inflammatory response and improve insulin resistance (IR); however, the underlying mechanisms are still unclear. This study aimed to explore the related mechanisms of intermittent FT for the treatment of IR.

Methods: A rat IR model was established through collaboration of a high-fat diet with streptozotocin (STZ) injection.

Discovery of a Dimeric Zinc Complex and Five Cyclopentenone Derivatives from the Sponge-Associated Fungus .

In devotion to investigating structurally novel and biologically active marine natural products, a dimer of a zinc complex, dizinchydroxyneoaspergillin (), aspernones A-E (-), five cyclopentenone derivatives together with known polyketides (-), and neoaspergillic acid analogues (-) were isolated from the sponge-associated fungus SCSIO 41018. Their structures were elucidated on the basis of spectroscopic analysis, electronic circular dichroism (ECD) analysis, and X-ray diffraction. Dizinchydroxyneoaspergillin () displayed significant bactericide effects toward methicillin-resistant , , , , and with MIC values of 0.

Pyrrolyl 4-quinolone alkaloids from the mangrove endophytic fungus Penicillium steckii SCSIO 41025: Chiral resolution, configurational assignment, and enzyme inhibitory activities.

Six undescribed 4-quinolone alkaloids, including four racemic mixtures, (±)-oxypenicinolines A-D, and two related ones, penicinolines F and G, together with seven known analogues, were isolated from the mangrove-derived fungus Penicillium steckii SCSIO 41025 (Trichocomaceae). The racemates were separated by HPLC using chiral columns. Their structures including absolute configurations were elucidated by extensive spectroscopic analysis, electronic circular dichroism (ECD) experiments, and single-crystal X-ray diffraction analysis.

Induction of ferroptosis in human nasopharyngeal cancer cells by cucurbitacin B: molecular mechanism and therapeutic potential.

Cucurbitacin B (CuB) is a widely available triterpenoid molecule that exhibits various biological activities. Previous studies on the anti-tumour mechanism of CuB have mostly focused on cell apoptosis, and research on the ferroptosis-inducing effect has rarely been reported. Herein, we first discovered the excellent cytotoxicity of CuB towards human nasopharyngeal carcinoma cells and elucidated its potential ferroptosis-inducing mechanisms.

Structurally diverse polyketides and phenylspirodrimanes from the soft coral-associated fungus Stachybotrys chartarum SCSIO41201.

Four undescribed polyketide derivatives, named arthproliferins A-D (1-4), and one undescribed phenylspirodrimane derivative, named arthproliferin E (7), along with 11 known metabolites (5, 6, 8-16) were isolated from the soft coral-associated fungus Stachybotrys chartarum SCSIO41201. Their structures were determined through spectroscopic methods, X-ray crystallography, and ECD analysis. Compounds 1 and 3-15 were evaluated for their cytotoxic, and antibacterial activities.

Lipopeptide Epimers and a Phthalide Glycerol Ether with AChE Inhibitory Activities from the Marine-Derived Fungus SCSIO41401.

A pair of novel lipopeptide epimers, sinulariapeptides A () and B (), and a new phthalide glycerol ether () were isolated from the marine algal-associated fungus SCSIO41401, together with three known chromanone derivates (-). The structures of the new compounds, including the absolute configurations, were determined by comprehensive spectroscopic methods, experimental and calculated electronic circular dichroism (ECD), and Mo (OAc)-induced ECD methods. The new compounds - showed moderate inhibitory activity against acetylcholinesterase (AChE), with IC values of 1.

Bioactive secondary metabolites from the deep-sea derived fungus Aspergillus sp. SCSIO 41029.

Two new compounds classified as one new lumazine peptide, penilumamide K (1) and one new sesquiterpene (2), were obtained from the deep-sea derived fungus Aspergillus sp. SCSIO 41029, together with eleven known compounds (3-13). The structures of 1-13 including absolute configurations were determined by detailed NMR spectroscopy, HR-ESI-MS, chemical derivatization, and optical rotation data.

Four new steroids from the marine soft coral-derived fungus Penicillium sp. SCSIO41201.

Penicildiones A-D (1-4), four new steroids derivatives together with three known compounds including 16α-methylpregna-17α,19-dihydroxy-(9,11)-epoxy-4-ene-3,18-dione-20-acetoxy (5), stachybotrylactone B (6) and stachybotrin (7) were isolated from the soft coral-derived fungus Penicillium sp. SCSIO41201, cultured in the 1% NaCl PDB substrate. Their structures were determined through spectroscopic methods and X-ray crystallography.

Antioxidant CPA-type indole alkaloids produced from the deep-sea derived fungus sp. SCSIO 41024.

Twelve indole alkaloids, including α-cyclopiazonic acid (CPA) (), nine 2-oxo indole CPA derivatives (-), and two open-ring indole CPA derivatives ( and ), were isolated from the fermentation broth of a deep-sea derived fungus sp. SCSIO 41024. Their structures and absolute configurations were elucidated mainly by using extensive NMR spectroscopic, mass spectrometric and single crystal X-ray diffraction analysis.