Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus Samsoniella aurantia

• Rita Toshe,
• Syeda J. Khalid,
• Blondelle Matio Kemkuignou,
• Esteban Charria-Girón,
• Paul Eckhardt,
• Birthe Sandargo,
• Kunlapat Nuchthien,
• J. Jennifer Luangsa-ard,
• Till Opatz,
• Hedda Schrey,
• Sherif S. Ebada and
• Marc Stadler

Beilstein J. Org. Chem. 2025, 21, 327–339, doi:10.3762/bjoc.21.23

• activity assay. Farinosone B (3) and beauvericins A–C (4–6) showed significant cytotoxic activities with IC50 values in the low micromolar to nanomolar range against several mammalian cell lines. On the other hand, farinosone A (2), which lacked potent cytotoxic effects, revealed potent antibiofilm

• activity, inhibiting approximately 70% of Staphylococcus aureus biofilms at concentrations as low as 3.9 µg/mL. Keywords: antibiofilm; antiproliferative; beauvericin; insect pathogen; Samsoniella; Introduction A microbial biofilm represents an assemblage of planktonic cells to overcome hostile living

• exacerbates healthcare and economic burdens, thereby prompting the urgent need for novel therapeutic strategies and antibiofilm agents. During our ongoing research targeting potential antibiofilm metabolites from fungi, we explored entomopathogenic species such as those belonging to the genera Beauveria and

Photoswitchable glycoligands targeting Pseudomonas aeruginosa LecA

• Yu Fan,
• Ahmed El Rhaz,
• Stéphane Maisonneuve,
• Emilie Gillon,
• Maha Fatthalla,
• Franck Le Bideau,
• Guillaume Laurent,
• Samir Messaoudi,
• Anne Imberty and
• Juan Xie

Beilstein J. Org. Chem. 2024, 20, 1486–1496, doi:10.3762/bjoc.20.132

• number of glycomimetic inhibitors of PA LecA and LecB have also been reported, with antibiofilm formation activity for some of them [5][6][7][8]. Photochromic molecules, which may be reversibly converted between different isomers upon illumination, offer numerous opportunities for reversibly

A facile approach to spiro[dihydrofuran-2,3'-oxindoles] via formal [4 + 1] annulation reaction of fused 1H-pyrrole-2,3-diones with diazooxindoles

• Pavel A. Topanov,
• Anna A. Maslivets,
• Maksim V. Dmitriev,
• Irina V. Mashevskaya,
• Yurii V. Shklyaev and
• Andrey N. Maslivets

Beilstein J. Org. Chem. 2022, 18, 1532–1538, doi:10.3762/bjoc.18.162

• heterocyclic systems are heteroanalogues of antimicrobial and antibiofilm fungal metabolites. The developed reaction represents the first example of involving 1H-pyrrole-2,3-diones fused at the [e]-side in a [4 + 1] annulation reaction. Keywords: [4 + 1] annulation; catalyst-free; diazooxindole; 1H-pyrrole

Pigmentosins from Gibellula sp. as antibiofilm agents and a new glycosylated asperfuran from Cordyceps javanica

• Soleiman E. Helaly,
• Wilawan Kuephadungphan,
• Patima Phainuphong,
• Mahmoud A. A. Ibrahim,
• Kanoksri Tasanathai,
• Suchada Mongkolsamrit,
• Janet Jennifer Luangsa-ard,
• Souwalak Phongpaichit,
• Vatcharin Rukachaisirikul and
• Marc Stadler

Beilstein J. Org. Chem. 2019, 15, 2968–2981, doi:10.3762/bjoc.15.293

• metabolite profiles using analytical HPLC coupled with diode array detection and mass spectrometry (HPLC–DAD–MS) revealed that the production of pigmentosin B (2) was apparently specific for Gibellula sp., while the glycoasperfuran 3 was specific for C. javanica. Keywords: antibiofilm agents; natural

• in combination with biofilm inhibitors [7]. Since finding an effective strategy to control biofilm formation remains a challenge, the effort to search for an effective antibiofilm agent was herein made. Invertebrate-pathogenic fungi, in particular the spider-pathogenic fungi, have recently proved to

• , respectively. Notably, 1 also weakly inhibited proliferation of HeLa KB3.1 cells, with an IC50 of 17 μg/mL. This compound was reported by Grove and co-workers [32] to be active against B. subtilis (MIC 20 μg/mL). Although both compounds showed neither nematicidal activity against C. elegans nor antibiofilm

Repurposing the anticancer drug cisplatin with the aim of developing novel Pseudomonas aeruginosa infection control agents

• Mingjun Yuan,
• Song Lin Chua,
• Yang Liu,
• Daniela I. Drautz-Moses,
• Joey Kuok Hoong Yam,
• Thet Tun Aung,
• Roger W. Beuerman,
• May Margarette Santillan Salido,
• Stephan C. Schuster,
• Choon-Hong Tan,
• Michael Givskov,
• Liang Yang and
• Thomas E. Nielsen

Beilstein J. Org. Chem. 2018, 14, 3059–3069, doi:10.3762/bjoc.14.284

• . aeruginosa to macrophages. Cisplatin treatment of P. aeruginosa in the P. aeruginosa-macrophage co-cultures caused significant less death of the mouse macrophages compared to control samples (Figure 5b), suggesting the effectiveness of cisplatin against P. aeruginosa infection. Antibiofilm effect of

• there was a significant reduction in the bacterial loads from the cisplatin treated corneas as compared to the control corneas (Figure 7). Conclusion Here, we have demonstrated how cisplatin displays antivirulence and antibiofilm effects against the opportunistic pathogen P. aeruginosa. Since biofilms

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

• Christian Schütz and
• Martin Empting

Beilstein J. Org. Chem. 2018, 14, 2627–2645, doi:10.3762/bjoc.14.241

• antibiofilm effects of two clinically relevant drugs. When growing biofilms for 48 h in presence or absence of M64 (42), followed by treatment of 10 µg/mL of meropenem or tobramycin for 24 h, the activity of the otherwise ineffective antibiotics could be restored. Especially in the case of meropenem, which

• their dual inhibitor, the group investigated the effect of adding 56 to ciprofloxacin. The combination of this QSI together with the antibiotic significantly increased antibiofilm activity at the used concentrations ([CIPX] = 1 µM, [56] = 50 µM). The compound also proved to be active in a Galleria