Inhibitors of Type-I Interleukin-1 Receptor from Microbial Metabolites.

Stefanelli, Stefania; Corti, Emiliana; Montanini, Nicoletta; Denaro, Maurizio; Sarubbi, Edoardo

doi:10.7164/antibiotics.50.484

Cited by 9 publications

(5 citation statements)

References 10 publications

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“…Biochemically, avipin inhibits electron transport, oxidative phosphorylation and protein synthesis, possibly as a result of the aromatic orthodialdehyde functionality cross-linking lysine residues in the proteins of cytochrome C and mitochondrial membranes (White & Elliott, 1972Madrigal & Melgarejo, 1994). Other biochemical effects include inhibition of interleukin-1 receptors and glucose-6-phosphat e translocase (Stefanelli et al, 1997;Vertesy et al, 1999).…”

Section: Discussionmentioning

confidence: 95%

Isolation of flavipin, a fungus compound antagonistic to plant-parasitic nematodes

Nitao¹,

Meyer²,

Oliver³

et al. 2002

Nematol

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An isolate of the fungus Chaetomium globosum produced culture broths that inhibited in vitro egg hatch and juvenile mobility of root-knot nematode (Meloidogyne incognita) and hatch of soybean cyst nematode (Heterodera glycines). Extraction and bioassay-directed fractionation of the culture broth ltrate determined that avipin, a low molecular weight compound, was the fungus metabolite responsible for most of the nematode-antagonistic activity. Synthesis of avipin permitted evaluation of the compound as a suppressor of nematode populations on plants in glasshouse studies. Muskmelon (Cucumis melo) plants in steamed and unsteamed soil were inoculated with root-knot nematodes and various concentrations of avipin were applied to the soil. Contrary to expectations from the in vitro studies, the number of galls per g of roots increased with avipin treatment at the 14-day harvest. No effect of avipin on nematode populations was found at the 55-day harvest. In general, plant growth and nematode populations were greater in plants grown in steamed soil.

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Section: Discussionmentioning

confidence: 95%

Isolation of flavipin, a fungus compound antagonistic to plant-parasitic nematodes

Nitao¹,

Meyer²,

Oliver³

et al. 2002

Nematol

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“…Azalomycin F has remarkable bioactivities against Gram-positive bacteria, yeast, fungi, and protozoa [17,34,73,75], and some clinical studies on its anti-trichomoniasis and anti-candida infectious effects were performed [34], while no corresponding drug was approved in the clinic. Stefanelli et al discovered that niphimycin ( 28 ) and azalomycin F ( 8 – 10 ) could inhibit the type-I interleukin-1 receptor [55]. Moreover, they had remarkable activities against phytopathogenic fungi, such as Fusarium oxysporum , Fusarium moliniforme , Asparagus officinalis , Rhizoctonia solani, Colletotrichum gloeosporioides , and Alternaria mali [17,36].…”

Section: Bioactivitymentioning

confidence: 99%

Guanidine-Containing Polyhydroxyl Macrolides: Chemistry, Biology, and Structure-Activity Relationship

Song

Yuan

et al. 2019

Molecules

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Antimicrobial resistance has been seriously threatening human health, and discovering new antimicrobial agents from the natural resource is still an important pathway among various strategies to prevent resistance. Guanidine-containing polyhydroxyl macrolides, containing a polyhydroxyl lactone ring and a guanidyl side chain, can be produced by many actinomycetes and have been proved to possess many bioactivities, especially broad-spectrum antibacterial and antifungal activities. To explore the potential of these compounds to be developed into new antimicrobial agents, a review on their structural diversities, spectroscopic characterizations, bioactivities, acute toxicities, antimicrobial mechanisms, and the structure-activity relationship was first performed based on the summaries and analyses of related publications from 1959 to 2019. A total of 63 guanidine-containing polyhydroxyl macrolides were reported, including 46 prototype compounds isolated from 33 marine and terrestrial actinomycetes and 17 structural derivatives. Combining with their antimicrobial mechanisms, structure-activity relationship analyses indicated that the terminal guanidine group and lactone ring of these compounds are vital for their antibacterial and antifungal activities. Further, based on their bioactivities and toxicity analyses, the discovery of guanidyl side-chain targeting to lipoteichoic acid of Staphylococcus aureus indicated that these compounds have a great potency to be developed into antimicrobial and anti-inflammatory drugs.

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“…There are about thirty 36-membered polyhydroxyl macrolides identified so far, and almost all of them were produced by Streptomyces . These compounds possess broad-spectrum antimicrobial activity, and azalomycin F was also an inhibitor of type-I interleukin-1 receptor [27]. In our research on biological activity of azalomycin F analogs produced by Streptomyces sp.…”

Section: Resultsmentioning

confidence: 99%

New Azalomycin F Analogs from Mangrove Streptomyces sp. 211726 with Activity against Microbes and Cancer Cells

et al. 2013

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Seven new azalomycin F analogs (1–7) were isolated from the broth of mangrove Streptomyces sp. 211726, and respectively identified as 25-malonyl demalonylazalomycin F5a monoester (1), 23-valine demalonylazalomycin F5a ester (2), 23-(6-methyl)heptanoic acid demalonylazalomycins F3a ester (3), F4a ester (4) and F5a ester (5), 23-(9-methyl)decanoic acid demalonylazalomycin F4a ester (6) and 23-(10-methyl)undecanoic acid demalonylazalomycin F4a ester (7). Their structures were established by their spectroscopic data and by comparing with those of azalomycins F3a, F4a and F5a. Biological assays exhibited that 1–7 showed broad-spectrum antimicrobial and anti HCT-116 activities.

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Inhibitors of Type-I Interleukin-1 Receptor from Microbial Metabolites.

Cited by 9 publications

References 10 publications

Isolation of flavipin, a fungus compound antagonistic to plant-parasitic nematodes

Isolation of flavipin, a fungus compound antagonistic to plant-parasitic nematodes

Guanidine-Containing Polyhydroxyl Macrolides: Chemistry, Biology, and Structure-Activity Relationship

New Azalomycin F Analogs from Mangrove Streptomyces sp. 211726 with Activity against Microbes and Cancer Cells

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