Two sulfur-containing ansamycin antibiotics fromStreptomyces albolongus

Summary Two sulfur-containing ansamycin antibiotics were isolated from the culture broth ofStreptomyces albolongus C-46366; the major one was identical with awamycin and the minor one was a new ansamycin antibiotic, ansathiazin. Their structures were elucidated from their reactions and spectroscopic analyses. These antibiotics were active against gram-positive bacteria, acid-fast bacteria and a protozoan.We thank Dr I. Umezawa for his generous gift of awamycin. We are grateful to Drs K. Morita, Y. Nakao, H. Okazaki and H. Ono for their interest throughout this work. Thanks are also due to Messrs Y. Kono, K. Koyama, H. Fujiuchi and Y. Nakano, and Mrs K. Jinno for their skillful technical assistance.     

Flambamycin,a new antibiotic fromStreptomyces hygroscopicus DS 23 230

Résumé La flambamycine, nouvel antibiotique produit parStreptomyces hygroscopicus DS 23 230, est un hétéroside dont l'aglycone est l'acide dichloroisoéverninique, précédemment mis en évidence dans l'avilamycine, la curamycine et l'éverninomycine. Tant in vitro qu'in vivo elle inhibe fortement la croissance des cocci gram-positifs ou-négatifs, mais thérapeutiquement elle n'est utilisable que par la voie parentérale.     

Emericid,a new polyether antibiotic fromStreptomyces hygroscopicus (DS 24 367)

Summary Emericid is a new polyether polycyclic ionophore antibiotic excreted byStreptomyces hygroscopicus (DS 24 367). Active in vitro against Gram-positive bacteria, it is ineffective in vivo. At a 0.006–0.02% level in the diet it protects chickens and rabbits against coccidiosis.From a recent paper byN. Otake (Tetrahedron Lett.1970, 4147) emericid and lonomycin would be identical.     

Paracelsin, a peptide antibiotic containing alpha-aminoisobutyric acid, isolated from Trichoderma reesei Simmons. Part A

A peptide antibiotic has been isolated from Trichoderma reesei QM 9414. Although crystalline and uniform in TLC, this antibiotic could be resolved by HPLC into 3 sequence analogues. The close relationship to alamethicin was proved by chemical and spectroscopic methods, and the formation of ion-conducting pores in lipid bilayers.     

Pancreastatin,a chromogranin A-derived peptide,inhibits leptin and enhances UCP-2 expression in isolated rat adipocytes

Leptin, the ob gene product, is an adipocyte-secreted hormone that centrally regulates weight by decreasing caloric intake and increasing energy expenditure. Expression of leptin is regulated by dietary status, insulin, glucocorticoids and catecholamines. Pancreastatin (PST), a chromogranin A-derived peptide, correlates with catecholamine levels, and may play a role in the physiology of stress, modulating endocrine secretion and metabolism. Thus, PST has been found to exert a lipolytic and anti-insulin effect in white adipocytes. The aim of the present work was to investigate a possible role of PST modulating the expression of key genes involved in lipid storage and metabolism: leptin, PPAR-2, UCP-1 and UCP-2. We incubated isolated rat epididymal adipocytes with 100 nM PST for 16 and 24 h. Leptin, UCP-2 and UCP-1 mRNA levels were assessed by RT-PCR, followed by Southern blot. Leptin secretion was also measured by ELISA. PST inhibited leptin expression and secretion at 16-h incubation, but this effect was no longer observed after 24 h. On the other hand, PST stimulated the expression of UCP-2 after 16 h. However, the effect was still significant after 24 h. The inhibitory effect of PST on leptin expression and secretion and the stimulation of UCP-2 expression were prevented by blocking PKC. UCP-1 and PPR-2 expression did not change after PST stimulation. Leptin differentially regulates the expression of key genes in the rat adipocyte, upregulating the expression of UCP-2 and inhibiting the expression and secretion of leptin by a mechanism that involves PKC activity. These effects may contribute to the metabolic action of catecholamines in physiological and pathophysiological conditions with increased sympathetic activity.Received 5 September 2003; received after revision 6 October 2003; accepted 14 October 2003     

A crystalline,toxic, peptide metabolite ofTrichoderma spp. isolated from soil

Summary Isolates ofTrichoderma spp. from pasture soils of Nova Scotia produce at least 7 toxic peptides, probably related to alamethicin, some of which inhibit the growth of cellulase producing rumen bacteria. One of the peptides has been obtained in crystalline form and crystal data on this material is reported.     

Partricin methyl ester,a semisynthetic polyene antibiotic

Zusammenfassung Es wurde der Methylester von Partricin, eines polyenischen Antibiotikums, hergestellt. Das Produkt zeigte eine gesteigerte Aktivität gegen Hefen und eine verminderte Toxizität.     

Determination of the structure of the peptide moiety of the antibiotic albomycin

Zusammenfassung Der Peptidteil des Antibioticums Albomycin wurde aufgeklärt durch Überführung der -Hydroxy-ornithinreste in Glutaminsäurereste und anschliessende saure Partialhydrolyse, wobei sechs Peptide resultierten, deren Kombination eine eindeutige Strukturformel lieferten.     

The structure of a novel antitumor antibiotic,saframycin A

Summary A structure is assigned to saframycin A, a novel antitumor antibiotic fromStreptomyces lavendulae No. 314, on the basis of¹³C NMR-spectral data.     

The total synthesis of racemic cryptosporiopsin,a fungitoxic antibiotic

Résumé L'antibiotique cryptosporiopsine, produit métabolique deSporormia affinis ainsi que d'une espèce deCryptosporiopsis a été synthétisé à partir de la dihydrocryptosporiopsine synthétique.     

Neuromuscular blocking activity of dibekacin,a new semisynthetic aminoglycoside antibiotic

Summary Dibekacin possesses the untoward effect of producing a neuromuscular blockade. Neostigmine is unable to reverse the neuromuscular blockade produced by dibekacin. Calcium has not only the ability to restore the neuromuscular transmission but also to exert protective action against the neuromuscular blocking activity of dibekacin.     

Unexpected antibiotic properties of a cephalosporin]

The presence of an oximino group on the methylene of the (2-aminothiazol 4-yl)-acetyl side chain bound to the 7-amino cephalosporanic acid affords derivatives with syn or anti configuration. Whereas the anti isomers display low antibiotic activities, the syn isomers possess a surprising high efficiency against gram negative bacteria, enhanced a factor of 10 to 100 as compared with the cephalosporins known at the moment.     

Ceralbol,a new sesterterpenic alcohol isolated from insect wax

Summary The isolation and structural elucidation of ceralbol (1), a new sesterterpene from the insect waxCeroplastes albolineatus are reported.Contribution No. 465 from Instituto de Quimica de la Universidad Nacional Autonoma de Mexico.This work was supported by a grant from Syntex laboratories, S.A., Mexico, D.F.