Nocardicin A
Nocardicin A is a monocyclic β-lactam antibiotic with broad-spectrum activity against Gram-negative bacteria. Nocardicin A inhibits bacterial cell wall synthesis and synergistically stimulates the phagocytic and bactericidal functions of polymorphonuclear leukocytes (PMN). Nocardicin A can be used in research on Gram-negative bacterial infections.
For research use only. We do not sell to patients.
- CAS No.: 39391-39-4
- Formula: C23H24N4O9
- Molecular Weight:500.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
IC50 & Target
[1]|
β-lactam |
In Vitro
Nocardicin A (25 mcg/mL; overnight) converts Pseudomonas aeruginosa NCTC 10490 to protoplasts/spheroplasts after overnight incubation on agar containing 20% sucrose[2].
Nocardicin A inhibits Pseudomonas aeruginosa, Proteus spp., Serratia marcescens, and Escherichia coli isolates in A-No.3/A-No.5 medium with MICs of 3.13-200 μg/mL[3].
Nocardicin A exhibits higher MICs against Pseudomonas aeruginosa strains 191, 195, 201, and 161 and Proteus mirabilis strains 60, 100, and 105 in HI agar (> 800 μg/mL and 100-200 μg/mL, respectively), but lower MICs in A-No.3/A-No.5 agar (12.5-800 μg/mL and 6.25-12.5 μg/mL, respectively)[3].
Nocardicin A potently inhibits B. thiaminolyticus IFO 3115 with an MIC of 0.78 μg/mL[4].
Nocardicin A (1 mg/mL; 37°C overnight) activity against P. aeruginosa IFO 3080 is significantly antagonized by Glycine (HY-Y0966), D-Alanine (HY-41700), and D-Leucine (HY-Y0378), and partially antagonized by L-Alanine (HY-N0229) and L-Leucine (HY-N0486)[4].
Nocardicin A is highly stable to the tested β-lactamases, with relative hydrolysis rates ranging from <0.01-6.55[4].
Nocardicin A exhibits no β-lactamase inhibitory activity against the tested penicillinases and cephalosporinases (I50 > 100 μg/mL)[4].
Nocardicin A (100-1000 μg/mL; added after 2.5 h, with growth monitored until 7 h) exhibits the strongest lytic activity against P. aeruginosa IFO 3080 among the tested compounds, although it does not cause lysis at its MIC concentration[4].
Nocardicin A (up to 100 μg/mL) binds PBP 1B but not PBP 1A in P. aeruginosa IFO 3080[4].
Nocardicin A (incubated for 18 h) inhibits E. coli W-7, KN126, SP6, and SP61, with MIC ranging from 24-43 µM[6].
Nocardicin A (40-160 µM) alone produces a slow bactericidal/lytic effect on E. coli W-7 at 40-80 µM, and a more rapid lytic response at 160 µM[6].
Nocardicin A (40 µM) combined with Mecillinam (HY-A0269) (3 µM) rapidly induces lysis of E. coli W-7 and inhibits peptidoglycan synthesis[6].
Nocardicin A (approximately 20 µM) and Mecillinam (0.1 µM) synergistically trigger lysis of E. coli W-7 and KN126, consistent with their respective MICs[6].
Nocardicin A (40 µM) combined with Mecillinam (3 µM) induces lysis in E. coli KN126 and SP61 with normal PBP2 function, but does not induce lysis in the PBP2-deficient SP6[6].
Nocardicin A combined with Amoxicillin (HY-B0467A) (4 µM) induces Mecillinam-like lysis in E. coli W-7, indicating that Mecillinam is not absolutely required as a PBP2 modulator[6].
Nocardicin A (1 μg/mL; 18 h) in combination with Nva-Ala (P) exhibits a synergistic effect against Pseudomonas aeruginosa 511030, with an FICI of 0.25[7].
Nocardicin A (3.6 μg/mL; 18 h) combined with Nva-Ala (P) exhibits the most pronounced synergy against Pseudomonas aeruginosa (20 isolates; mean FICI 0.24), and shows broader synergy in P. mirabilis, indole-positive Proteus spp., and S. marcescens[7].
Nocardicin A (2 μg/mL; 2 h) combined with Nva-Ala (P) causes synergistic lysis of uridine-prelabeled Pseudomonas aeruginosa 511030, with a FICI of 0.18[7].
Nocardicin A exhibits moderate anti-pseudomonal activity in vitro (MIC = 32 mg/L; MBC = 256 mg/L), shows partial inhibitory synergy with Carbenicillin (HY-B0525A), but has no bactericidal synergy against Ps. aeruginosa 30[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PMN cells
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Concentration:5, 10, 20 μg/mL
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Incubation Time:2 h
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Result:Did not affect the directed or random migration of human PMNs at 10 and 5 μg/mL, but it impairs motility in an under-agarose migration assay at 20 μg/mL.
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Cell Line:Ps. aeruginosa 30 and PNM cells
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Concentration:0.1, 1, 10 μg/mL
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Incubation Time:30 min
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Result:Enhanced intracellular killing of Ps. aeruginosa 30 by human PMNs.
In Vivo
Nocardicin A (0.1-50 mg/kg; s.c.; administered at 1 and 3 h post-infection, with an additional dose at 5 h against P. aeruginosa) produces efficacy against multiple Gram-negative bacteria in a mouse sepsis model, shows the lowest ED50 value against Haemophilus influenzae, and exhibits synergy with Nva-Ala (P) in 10 of 23 infections[7].
Nocardicin A (40-80 mg/kg; s.c.; administered at 1 h and 6 h post-infection, followed by twice daily; 4 days) significantly improves survival in the CS1 mouse model of Ps. aeruginosa sepsis[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 4 weeks old, 22-24 g)[3]
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Dosage:22, 87, 348 mg/kg
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Administration:s.c.; single administration; counting after 9 h
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Result:Reduced the counts of surviving Pr. mirabilis cells in the livers and kidneys of infected mice
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Animal Model:CS1 (male albino, 20-25 g)[8]
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Dosage:40, 80 mg/kg
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Administration:s.c.; administered at 1 h and 6 h post-infection, followed by twice daily; 4 days
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Result:Protected almost all the animals when given alone at 80 mg/kg, and consistently protected all animals when combined with carbenicillin at 40 mg/kg.
Generated peritoneal macrophages with enhanced ability to kill Ps. aeruginosa.
Chemical Information
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CAS No. 39391-39-4
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Molecular Weight 500.46
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Formula C23H24N4O9
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SMILES
OC([C@@H](C1=CC=C(C=C1)O)N2C([C@H](C2)NC(/C(C3=CC=C(C=C3)OCC[C@@H](N)C(O)=O)=N\O)=O)=O)=O
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Structure Classification
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Initial Source
Nocardia
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Aoki H, et al. Nocardicin A, a new monocyclic β-lactam antibiotic I. Discovery, isolation and characterization. The Journal of antibiotics. 1976;29(5):492-500. [Content Brief]
[4]. KATAYAMA N, et al. Formadicins, new monocyclic β-lactam antibiotics of bacterial origin I. Taxonomy, fermentation and biological activities. The Journal of antibiotics. 1985;38(9):1117-27. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)