A new antitumor antibiotic, FR-900482. III. Antitumor activity in transplantable experimental tumors.
نویسندگان
چکیده
FR-900482 (4-formyl-6,9-dihydroxy-14-oxa-1,11-diazatetracyclo[7.4.1.02,7, O10,12]tetradeca-2,4,6-triene-8-ylmethyl carbamate), a new antibiotic with antitumor activity was isolated from fermentation broth of Streptomyces sandaensis. Its antitumor activities were studied and compared with that of mitomycin C (MMC) in animals. FR-900482 in doses of 0.32 approximately 10 mg/kg (ip) prolonged the life of mice bearing ascitic P388, L1210, B16, MM46, Ehrlich or EL4 tumors and rats bearing ascitic AH130 or AMC60 tumors. FR-900482 in doses of 5.6 approximately 18 mg/kg (iv) inhibited human LX-1, MX-1, SC-6 and LC-6 tumors xenografted sc in nude mice. FR-900482 was more effective than or equally effective to MMC in all the tumors used. FR-900482 was ineffective against cyclophosphamide-resistant P388, but was effective against MMC- or vincristine-resistant P388. The results suggest that FR-900482 may have clinical potential.
منابع مشابه
A new antitumor antibiotic, FR-900482. IV. Hematological toxicity in mice.
The new antibiotic FR-900482 (4-formyl-6,9-dihydroxy-14-oxa-1,11-diazatetracyclo-[7.4.1.02,7. O10,12]tetradeca-2,4,6-triene-8-ylmethyl carbamate) possesses an antitumor activity equal to or greater than that of mitomycin C (MMC). The hematotoxicity of equivalent effective doses of the two compounds was compared in mice. A single iv injection of either compound similarly decreased the number of ...
متن کاملA new antitumor antibiotic, FR-900482: V. Interstrand DNA-DNA cross-links in L1210 cells.
FR-900482 (Fig. 1) is a new antitumor antibiotic isolated from the culture broth of Streptomyces sandaensis No. 68971~3). It has potent cytotoxic effects against murine and human tumor cells2>4), and weak myelosuppressive effects in mice5). The mechanisms by which FR-900482 induces cytotoxic effects have not been defined. Some antitumor drugs induce interstrand DNA-DNA cross-links or DNA strand...
متن کاملPrecursors in the biosynthesis of FR-900482, a novel antitumor antibiotic produced by Streptomyces sandaensis.
isolated from the culture broth of Streptomyces sandaensis No. 6897, was found to have unique structure1*^. FR-900482 differs from the mitomycin family of antibiotics due to the lack of a quinoid structure, although FR-900482 resembles the mitomycins with respect to the aziridine function and a carbamoyloxymethyl group. Examination of the structure suggests that the biosynthesis of FR-900482 ma...
متن کاملSynthesis, characterization, theoretical calculations and biological studies of nano Sodium tetrafluoroborate (III)
Synthesis, characterization, spectral and theoretical calculations of sodium tetrafluoroborate (III) (STFB) has been studied in this research. Sodium tetrafluoroborate (III) was synthesized by a sonochemical method and characterized by IR, UV/VIS, 11B-NMR and Mass spectrometer techniques. The nano compound was characterized by scanning electron microscopy (SEM), X-ray powder diffract...
متن کاملSynthesis, characterization, theoretical calculations and biological studies of nano Sodium tetrafluoroborate (III)
Synthesis, characterization, spectral and theoretical calculations of sodium tetrafluoroborate (III) (STFB) has been studied in this research. Sodium tetrafluoroborate (III) was synthesized by a sonochemical method and characterized by IR, UV/VIS, 11B-NMR and Mass spectrometer techniques. The nano compound was characterized by scanning electron microscopy (SEM), X-ray powder diffract...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- The Journal of antibiotics
دوره 40 5 شماره
صفحات -
تاریخ انتشار 1987