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cyclic lipopeptide daptomycin  (Eli Lilly)

 
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    Eli Lilly cyclic lipopeptide daptomycin
    Cyclic Lipopeptide Daptomycin, supplied by Eli Lilly, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/daptomycin+is+a+cyclic+lipopeptide/daptomycin/pm32209367-19-19-33
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    Article Title: Engineering biosynthetic enzymes for industrial natural product synthesis
    Article Snippet: Biotica also applied their starter unit modication strategy to rapamycin by feeding alternative carboxylic acids to a rapK deleted mutant of the native strain, thereby producing new anticancer candidate mTOR and kinase inhibitors that were licensed to Wyeth Laboratories (now Pzer).27 This journal is © The Royal Society of Chemistry 2020 The spinosyn efforts continued at Dow, where articial neural network modelling was combined with a synthetic modication program, resulting in the identication of a hydrogenated and 30-O-ethylated spinosyn analog with broad improvement in insecticidal activity.60 This required starting from a 30-O-desmethyl rhamnose spinosyn (J and L, Fig. 1), and strains with mutations that eliminated this methylation were identied through an extensive classical strain improvement program conducted at Lilly and Dow. .. The resulting product, Spinetoram, a semisynthetic derivative of spinosyns J and L, received the Green Chemistry award in 2008.61,62 Cubist Pharmaceuticals' scientists produced novel daptomycin derivatives (Fig. 2) by exchanging modules to build 30 combinatorial biosynthetic pathways.28 Daptomycin is a cyclic lipopeptide produced by an NRPS in Streptomyces roseosporus and is bactericidal to methicillin-resistant Staphylococcus aureous (MRSA).63 Daptomycin was discovered by Eli Lilly, licensed to Cubist Pharmaceuticals in 1997, and received FDA approval in 2003.64 Fermentations of the Nat. ..



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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and <t>sulbactam</t> sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.
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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and <t>sulbactam</t> sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.
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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and <t>sulbactam</t> sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.
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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and <t>sulbactam</t> sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.
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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and <t>sulbactam</t> sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.
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    Selected antibiotics tested against B. burgdorferi
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    Selected antibiotics tested against B. burgdorferi
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    cyclic lipopeptide daptomycin  (Cubist Pharmaceuticals)
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    Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and sulbactam sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.

    Journal: mSystems

    Article Title: Valine potentiates cefoperazone-sulbactam to kill methicillin-resistant Staphylococcus aureus

    doi: 10.1128/msystems.01244-24

    Figure Lengend Snippet: Antibacterial efficacy by SCF in the absence or presence of valine. ( A ) Percent survival of MRSA2 in the presence of the indicated antibiotics with or without 5 mM valine. SCF, cefoperazone sodium and sulbactam sodium; ASPC, amoxicillin sodium clavulanate potassium. Antibiotic doses are as follows: 200 µg/mL for SCF; 300 µg/mL for ceftriaxone, cefradine, ceftazidime, cefazolin; 150 µg/mL for vancomycin; and 400 µg/mL for the others. ( B ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of SCF plus 5 mM valine. ( C ) Percent survival of MRSA2 in the absence or presence of the indicated concentrations of valine plus 200 µg/mL SCF. ( D ) Percent survival of MRSA2 in the absence or presence of the indicated incubation time with 5 mM valine and 200 µg/mL SCF. ( E ) Percent survival of 18 MRSA isolates (2.5 × 10 7 CFU/mL) in the absence or presence of 5 mM valine, 200 µg/mL SCF, and both. ( F ) Bacterial load of liver, kidney, and spleen of mice infected with MRSA2. Mice were intraperitoneally infected with 2.5 × 10 6 CFU of MRSA2 and divided into four groups, four male Balb/c mice per group. The four groups were separately intravenously injected with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both in an hour later. Spleen, kidney, and liver of these treated mice were collected at 24 h and homogenized for spot plate counting. ( G ) Percent survival of mice in the absence or presence of the indicated dose of SCF or/and the indicated dose of valine. Mice were intraperitoneally infected with 2.5 × 10 7 CFU of MRSA2 and divided into eight (sub)groups to be treated as the indicated post 1 h of infection, 10 mice per group. Survival of mice was monitored for 7 days. ( H ) Bacterial load of mouse thigh infected with MRSA2. Mice were intramuscularly infected with 2.8 × 10 5 CFU of MRSA2 and divided into four groups. The four groups were separately treated with saline solution, 200 mg/kg SCF, 200 mg/kg valine, or both post 2 h infection. The thigh muscle infected was collected at 26 h and homogenized for spot plate counting. ( I ) Percent survival of MRSA2 in the absence or presence of 5 mM leucine or isoleucine plus 200 µg/mL SCF. Data are mean ± SD from three biological replicates. *, P < 0.05; **, P < 0.01.

    Article Snippet: All antibiotics tested, including vancomycin (glycopeptides), cefoperazone sodium and sulbactam sodium (cephalosporins), daptomycin (cyclic lipopeptides), oxacillin (penicillins) were purchased from Sangon Biotech (BBI) Limited (Shanghai, China).

    Techniques: Incubation, Infection, Injection, Saline

    Selected antibiotics tested against B. burgdorferi

    Journal: Antimicrobial Agents and Chemotherapy

    Article Title: Borrelia burgdorferi , the Causative Agent of Lyme Disease, Forms Drug-Tolerant Persister Cells

    doi: 10.1128/AAC.00864-15

    Figure Lengend Snippet: Selected antibiotics tested against B. burgdorferi

    Article Snippet: Daptomycin cyclic lipopeptide (Sigma) was dissolved in a 5 μg/ml solution of calcium chloride.

    Techniques:

    Killing of B. burgdorferi by daptomycin. Time-dependent killing of stationary-phase B. burgdorferi exposed to daptomycin (81 μg/ml) (n = 3). Error bars represent standard errors.

    Journal: Antimicrobial Agents and Chemotherapy

    Article Title: Borrelia burgdorferi , the Causative Agent of Lyme Disease, Forms Drug-Tolerant Persister Cells

    doi: 10.1128/AAC.00864-15

    Figure Lengend Snippet: Killing of B. burgdorferi by daptomycin. Time-dependent killing of stationary-phase B. burgdorferi exposed to daptomycin (81 μg/ml) (n = 3). Error bars represent standard errors.

    Article Snippet: Daptomycin cyclic lipopeptide (Sigma) was dissolved in a 5 μg/ml solution of calcium chloride.

    Techniques:

    Infection Parameter

    Journal: Journal of Cardiothoracic Surgery

    Article Title: Treatment of gram-positive deep sternal wound infections in cardiac surgery -experiences with daptomycin-

    doi: 10.1186/1749-8090-6-112

    Figure Lengend Snippet: Infection Parameter

    Article Snippet: The first in a novel class of cyclic lipopeptide antibiotics daptomycin (Cubicin; Cubist Pharmaceuticals, Inc., Lexington, MA), has already been proven to be effective in the treatment of bacteremia and endocarditis caused by MRSA and several case reports document about its effectiveness in the field of cardiac surgery [ - ].

    Techniques: Infection

    Laboratorial data

    Journal: Journal of Cardiothoracic Surgery

    Article Title: Treatment of gram-positive deep sternal wound infections in cardiac surgery -experiences with daptomycin-

    doi: 10.1186/1749-8090-6-112

    Figure Lengend Snippet: Laboratorial data

    Article Snippet: The first in a novel class of cyclic lipopeptide antibiotics daptomycin (Cubicin; Cubist Pharmaceuticals, Inc., Lexington, MA), has already been proven to be effective in the treatment of bacteremia and endocarditis caused by MRSA and several case reports document about its effectiveness in the field of cardiac surgery [ - ].

    Techniques: