In vivo activity of anprocide alone, and in vitro activity in combination with conventional antibiotics against Staphylococcus aureus and Staphylococcus epidermidis biofilms.
The alarming spread of multiple drug resistance in Staphylococcus aureus, combined with the frequent occurrence of S. aureus and Staphylococcus epidermidis in biofilm-type infections, indicates a growing need for new therapies. The experimental steroidal amide anprocide [3beta-acetoxy-17beta-(l-prolyl)amino-5alpha-androstane] significantly reduced c.f.u. ml(-1) per suture (P <0.0001) in a murine model of topical S. aureus infection. In chequerboard assays with planktonic-grown S. aureus and S. epidermidis, anprocide was synergistic with bacitracin, oxacillin, clindamycin or ceftriaxone. Anprocide was also synergistic in combination with bacitracin or oxacillin against some isolates of biofilm-grown S. aureus and S. epidermidis.
Pettit
Robin K
RK
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, AZ 85287, USA.
Weber
Christine A
CA
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, AZ 85287, USA.
Lawrence
Stacey B
SB
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, AZ 85287, USA.
Pettit
George R
GR
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, AZ 85287, USA.
Kean
Melissa J
MJ
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, AZ 85287, USA.
Cage
Gary D
GD
Phoenix Children's Hospital, Phoenix, AZ 85016, USA.
D000731:Androstanes / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000494:pharmacology*; D018441:Biofilms; D004305:Dose-Response Relationship, Drug; D051379:Mice; D011392:Proline / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D013207:Staphylococcal Skin Infections / Q000188:drug therapy / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000502:physiology*; D013212:Staphylococcus epidermidis / Q000187:drug effects* / Q000502:physiology*
C417166:3-acetoxy-17-prolylaminoandrostane; D000731:Androstanes; D000900:Anti-Bacterial Agents; D011392:Proline