Current opinion in critical care favours the early use of antibiotics, guided by local pathogen surveillance, usually of a broad spectrum and high potency, that is equally applicable to all clinical settings in patients with suspected severe sepsis [ 1].
Hydroxytyrosol, derived from oleuropein by enzymatic hydrolysis was reported to have a more broad spectrum and a higher potency by inhibiting Haemophilus influenzae and Moraxella catharralis; its MIC values were between 0.24 and 7.85 μg/ml for ATCC strains and between 0.97 and 31.25 μg/ml for clinical isolates [ 34].
Such end-tagged peptides were found to display limited toxicity combined with high microbicidal potency of broad spectrum, also at physiological ionic strength and in the presence of serum, as well as ex vivo and in vivo.
Hymenochirin-1Pa shows broad spectrum anti-bacterial activity, including high potency against multidrug-resistant clinical isolates of Staphylococcus aureus, Acinetobacter baumannii, and Stenotrophomonas maltophilia.
Previously characterized chemical mimics of host defense peptides belonging to the oligo-acyl-lysyl (OAK) family have so far failed to demonstrate broad-spectrum antibacterial potency combined with selectivity toward host cells.
We demonstrate that a single amino-acid substitution in a banana lectin, replacing histidine 84 with a threonine, significantly reduces its mitogenicity, while preserving its broad-spectrum antiviral potency.
Following i.p. administration to rats OM-TMCD demonstrated a broad spectrum of anticonvulsant activity and showed better potency than VPA in the maximal electroshock seizure and subcutaneous pentylenetetrazole tests as well as in the hippocampal kindling model.
Compounds 15, 20, 21 and 30 showed considerable activity against the Gram-positive bacteria Staphylococcus aureus while 24 and 30 proved active against Bacillus subtilis with a magnitude of potency comparable to the broad spectrum antibiotic Ciprofloxacin.
Chalcones is a versatile pharmacophore as compounds bearing this structural synthon possess a broad spectrum of biological activities such as anticancer potencies towards human leukemia HL-60, mouse lymphoma P388 cells [10], HeLa cell lines [11] as well as possessing antileishmanial activity [12].
The in vitro potency, alongside the tolerability and broad spectrum activity of SG2000 against human tumours in vivo (with breast carcinoma, melanoma and haematological malignancies being amongst the most sensitive), suggests that this agent is a promising candidate as a novel cancer therapeutic against spontaneously occurring malignancies in dogs.
