284 



DESCRIPTIONS OF ANTIIMOTICS 



per ml, such us strains of .1. hovis, Br. siiis, ('lus- 

 tridium hemolijticum, Corynebacterium diphtheriae, 

 D. pneumoniae, E. coli, H. influenzae, Neisseria 

 catarrhalis, Sh. paradysenteriae, and Streptococcus 

 pyogenes. Among the nonsensitive bacteria are 

 strains of K. pneumoniae, Staph, aureus, Pr. 

 vulgaris, and Ps. aeruginosa. No activity against 

 fungi, Endamoeba histolytica, Trichomonas foetus, 

 Trypanosoma crnzi, or T. rhodesiense. Active 

 against H. pertussis in mice. Not active against 

 experimental tuberculosis of mice. Active against 

 bovine mastitis caused by Staph, aureus, Staph, 

 albus, or E. coli, and against infectious bronchitis 

 of chickens. Limited antirickettsial activity 

 against Miyagawanella ornithosis and M. psittacii 

 in mice, and Rickettsia prowazekii in eggs. Inactive 

 against viruses in embryonated eggs (1). 



Toxicity: LD50 (mice) 75 mg per kg intrave- 

 nously, >100 mg per kg intraperitoneally, >100 

 mg per kg subcutaneously. Maximal tolerated dose 

 (mice) 50 mg per kg intraperitoneally. Not irritat- 

 ing when instilled into the udders of lactating 

 cows (1). 



References : 



1. Bartz, Q. R. et al. Antibiotics Ann. 777- 



805, 1954-1955. 



2. Ames, D. E. e? oi. J. Chem. Soc. 4260-4263, 



1955. 



3. Ames, D. E. and Bowman, R. E. J. Chem. 



Soc. 4264-4270, 1955. 



4. Ames, D. E. and Bowman, R. E. J. Chem. 



Soc. 2925-2928, 1956. 



5. Anderson, L. E. et al. Antibiotics & Chemo- 



therapy 6: 100-115, 1956. 



Grizin 



Produced by: Streptomyces sp. of the S. griseus 

 group (1). 



Synonyms: Grizemin, antibiotic lEM 1. 



Method of extraction: Broth treated with char- 

 coal at pH 3. Filtrate adjusted to pH 4.5, refiltered, 

 and antibiotic adsorbed at pH 7.5. Elution with 

 40 to 50 per cent ethanol at pH 3. Neutralization 

 followed by concentration in vacuo. Purified by 

 formation of various crystalline salts, e.g., picrate 

 and helianthate (1). 



Chemical and physical properties: Basic anti- 

 biotic. Helianthate: Brown powder; m.p. 194- 

 196°C (decomposition). Hydrochloride: White 

 powder. Soluble in water and methanol. Stable 

 as dry powder and to boiling for 10 minutes. Posi- 

 tive biuret, ninhydrin, and Bert rand tests. Test 

 for glucosamine positive. Negative Sakaguchi, 

 maltol, and histidine tests. N = 13.6 to 14.9% 

 (helianthate) in the form of a-amino nitrogen (1). 

 Probably a polypeptide. 



Biological activity: Active on gram-negative and 

 gram-positive bacteria, yeasts, and fungi. Active 

 on dysentery in mice. Effective on angular leaf 

 spot of cotton, and lemon and mandarin necrosis 

 {Bacterium citriputeale). Prevents withering of 

 apricot {Bad. armeniaca). EfTective against a 

 lemon tree disease (Deuterophoma tracheiphilla) 



(1). 

 Toxicity: Mice tolerate 0.5 mg per day for 6 days 



(1). 



Utilization: Dysentery in children (1). 



Reference: 1. Krassilnikov, N. A. et al. Mikro- 

 biologiya 26: 418-425, 1957. 



Grubilin 



Produced by: Streptomyces sp. 



Method of extraction: Isolated from the mycelium 

 with organic solvents. 



Chemical and physical properties: Green-yellow 

 substance. Base: Insoluble in water and organic 

 solvents. Gives color reactions and an ultraviolet 

 absorption spectrum typical of a heptaene. Xa 

 salt: Water-soluble. 



Biological activity: Active on yeasts and fila- 

 mentous fnngi; not active on bacteria or Strepto- 

 myces. 



Toxicity: LD50 (mice) 15 mg per kg intrave- 

 nously, 30 mg per kg intraperitoneally, and >500 

 mg per kg subcutaneously. 



Reference: 1. Uri, J. et al. Abstr. Communs. 

 Symposium on Antil)iotics, Prague. 46-47, 1959. 



Heliomyciu 



Produced by: Streptomyces flavochrouiogenes var. 

 heliomycini . 



Synonyms: Resistomycin, antibiotic X 340. 



Method of extraction: Mycelium washed and 

 pressed. Extracted with 3 volumes of technical 

 acetone per volume of wet mycelium. Extraction 

 repeated with one half the volume of acetone. To 

 the combined acetone-extracts, saturated barium 

 hydroxide is added until no further precipitation 

 occurs. The precipitated barium salt of heliomycin 

 is suspended in water. HCl added to bring the pH 

 to 3.0; this solubilizes barium as barium chloride, 

 which is removed by filtration. The precipitated 

 heliomycin is put in solution in acetone at pH 7.5 

 and impurities filtered off. Precipitation of yellow 

 crystalline heliomycin upon acidification to pH 

 3.0 with HCl. Recrystallization from acetone or 

 dioxane. 



Chemical and physical properties: Yellow needle- 

 shaped crystals. Soluble in dioxane, acetone, ethyl 

 acetate, butyl and ethyl alcohols. Less soluble in 

 chloroform, ether, and benzene. Poorly soluble in 

 carl)on tetrachloride. The solubility in organic 



