No abstract

Tuberculosis (TB) ranks as the leading cause of death from a single infectious agent (ranking more lethal than HIV/ AIDS) over the course of the past decade. More concerning is that reports of multi-drug-resistant (MDR) and extensively drugresistant (XDR) strains of TB have been dramatically increasing. It continues to become ever more clear that novel anti-TB drugs with improved efficacies and reduced toxicities are urgently needed. We report here the discovery of 12 new ilamycin analogues, ilamycins G−R (1−12), bearing various nonproteinogenic amino acids, along with ilamycins E 1 (13) and F ( 14), from a 200 L scale culture of the marine-derived mutant actinomycete Streptomyces atratus SCSIO ZH16 ΔilaR. Importantly, bioassays against Mycobacterium tuberculosis H37Rv revealed that all 12 new agents displayed antitubercular activities with MIC values ranging from 0.0096 to 10 μM. The structures of 1−12 were elucidated on the basis of HRESIMS, 1D and 2D NMR, and X-ray single-crystal diffraction studies. In addition, compound 10 was found to be moderately cytotoxic against a panel of tumor human cell lines. From these data we can formulate tentative structure−activity relationships for the antitubercular and antitumor activities of the ilamycins.

No abstract

Jinding laying ducks (n = 648) were subjected to one of six dietary treatments (0, 1, 5, 25, 50, or 100 mg of melamine/kg of diet) to investigate the toxicity of melamine and determine the melamine residue in eggs. Ducks were fed melamine-supplemented diets for 21 days followed by a 21 day withdrawal period. Dietary melamine had no adverse effects on laying performance. Renal lesions were correlated with increasing levels of dietary melamine. Melamine residue in eggs increased with dietary melamine during the first 21 days and reached the maximum content (1.35 mg/kg) in the 100 mg of melamine/kg of diet group. Melamine residue in eggs decreased rapidly during the withdrawal period. The depletion time for egg melamine residue increased with dietary melamine level. These results indicated that a dietary level of > or = 50 mg of melamine/kg of feed induces obvious renal injury. The residue level and withdrawal time for melamine clearance in eggs correlated with the dietary melamine level.