DESCRIPTIONS OF ANTIBIOTICS 



305 



range from 0.0005 to 1.0 /ug per ml; B, from 0.05 to 

 5.0 /xg per ml. Partial cross-resistance with strep- 

 tomycin (1, 5). Inactive in mice on D. pneu- 

 moniae, Snl. enteritidis, and Leptospira ictero- 

 liaeiuonhagiae. Active on Rickettsia tsutsiujaniushi . 

 Inactive on MiyagawaneUa and viruses (6). Both 

 are active on Yoshida sarcoma in rats and P]hrlich 

 carcinoma (ascitic form) in mice (1, 4). Mitomy- 

 cins A and B are equally active against tumors; 

 C is said to be about one fourth to one fifth as 

 active. Some effect on the solid form of Khrlich 

 carcinoma (4). Mitomycin A-like: Same as mito- 

 mycins A and B (9). Mitomycin C: Same in vitro 

 activity as A and B (9), but only one twentieth 

 as active as A on B. subtilis (4). Active in vi:o on 

 D. pneumoniae, Sal. enteritidis, L. icterohaemor- 

 rhagiae, R. tsutsugamushi, and MiyagawaneUa 

 (sheep). Inactive on toxoplasmosis (mice) or in- 

 fections caused by other small viru.ses (5, 6). Anti- 

 ascarid activity (12). Active on the following neo- 

 plasms: sarcoma 180 (ascitic), Ehrlich carcinoma 

 (ascitic), adenocarcinoma EO 771, Bashford car- 

 cinoma 63, Miyono adenocarcinoma, carcinoma 

 1025, Wagner osteogenic sarcoma, Ridgeway 

 osteogenic sarcoma, Lewis lung carcinoma, Hard- 

 ing-Passey melanoma, glioma 26, Friend virus 

 leukemia, Flexner-Jobling carcinoma. Walker 

 carcinosarcoma 256, Gardiner lymphosarcoma, 

 Jen.sen sarcoma, Murphy-Sturm lymphosarcoma, 

 Crabb hamster sarcoma, Iglesias functional rat 

 adrenal tiunor, Iglesias functional rat ovarian 

 tumor, diploid and tetraploid Hirosaki sarcoma 

 (ascites and solid), Usubuchi sarcoma (ascitic), 

 sarcoma-3-B (ascitic), ascites hepatoma 7974, 

 Yoshida sarcoma, and mouse lymphatic leukemia 

 SN36 (7, 10, 13). May interfere with the de novo 

 synthesis of purines (11). Fraction R: Moderately 

 active on Ehrlich carcinoma (ascitic), but not on 

 bacteria (9). Fraction Y: Same as mitomycins A 

 and B (9). 



Toxicity: Mitomycin A: LD.50 (mice) 1.0 to 1.5 

 mg per kg intravenously (5). Mitomycin A -like: 

 LD50 (mice) 2.5 mg per kg intravenously. Mito- 

 mycin C: More toxic for rats and hamsters than 

 for mice (13). LD.=,o (mice) 5 mg per kg (9) or 7.5 

 to 10.0 mg per kg (5) intravenously, 9 mg per kg 

 iiitraperitoneally (9). Toxicity also studied in rats 

 and rabbits (14). Fraction R: LD51) >500 mg per 

 kg (no route given) (9). 



Utilization: Mitomycin C(X) has been reported 

 clinically effective in certain neoplastic diseases 

 (8, 12). " 



References: 



1. Hata, T. et al. J. Antil)iotics (Ja])an) 9A: 

 141-146, 1956. 



2. Sugawara, R. and Hata, T. J. Antibiotics 



(Japan) 9A: 147-151, 1956. 



3. Japanese Patent 2,898, April 17, 1956. 



4. Kanamori, H. et al. J. Antibiotics (Japan) 



lOA: 120-127, 1957. 



5. Matsmnae, A. et al. Japan. J. Microbiol. 



1: 183-189, 1957. 



6. Saito, Y. et al. Japan. J. Microbiol. 1: 



191-196, 1957. 



7. Usubuchi, I. et al. Cann 48: 447-448, 



1957. 



8. Sakai, K. Chemotherapy (Tokyo) 5: 322, 



1957. 



9. Wakaki, S. et al. Antibiotics & Chemo- 



therajjy 8: 228-240, 1958. 



10. Usubuchi, I. et al. Chemotheraijy (Tokvo) 



6: 378-392, 1958. 



11. Reilly, H. C. and Cappuccino, J. (1. Proc. 



Am. Assoc. Cancer Research 2: 338, 1958. 



12. Shiraha, Y. et al . Antibiotics Ann. 533- 



540, 1958-1959. 



13. Sugiura, K. Cancer Research 19: 438- 



445, 1959. 



14. Sokoloff, B., et al. (Irowth 24: 1-27. 1960. 



Moldcidin A 



Produced by: Sfreptomyces sp. 



Remarks: Moldcidin B, another pentaene, has 

 been shown to be identical with pentamycin. 



Method of extraction: Extraction of the mycelium 

 with methyl alcohol. Concentration of solvent in 

 vacuo to '10 volume. Precipitate collected and 

 dried. Extract dissolved in methyl alcohol, fil- 

 tered, water added. Upon concentration, crystals 

 precipitate. 



Chemical and physical properties: Pentaene. 

 Light -absorption maxima at 324, 339, and 358 niyu. 

 Insoluble in butanol, ether, petroleum ether, ethyl 

 acetate, and 0.01 X HCl. Slightly soluble in water, 

 acetone, ethyl alcohol, and 0.1 A' NaOH. Soluble 

 in methyl alcohol, 80 per cent acetone, glacial 

 acetic acid, and pyridine. Positive ninhydrin re- 

 action. Negative biuret, IVhling, Molisch, Saka- 

 guchi, and FeCL tests. Slow melting between 180 

 and 230°C. No loss of activity of 1 mg per ml in 

 methyl alcohol at 5°C during 24 hours. Inactivated 

 by ultraviolet light. C = 55.87%; H = 8.84%; N = 

 1.50%. 



Biological activity: Active against a numljer of 

 yeasts and filamentous fungi at levels of 0.5 to 30 

 /ig per ml. No activity against l)acteria. Active 

 against Trichomonas vaginalis. 



Toxicity: \A):,» (mice) 10 mg per kg intrave- 

 nouslv. 



