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- NISHIKAWA KIYOHIRO
- Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co., Ltd.
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- SHIBASAKI CHIEKO
- Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co., Ltd.
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- TAKAHASHI KATSUTOSHI
- Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co., Ltd.
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- NAKAMURA TERUYA
- Central Research Laboratory, Takara Shuzo Co., Ltd.
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- TAKEUCHI TOMIO
- Institute of Microbial Chemistry
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- UMEZAWA HAMAO
- Institute of Microbial Chemistry
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説明
Spergualin (SGL), a novel antitumor antibiotic, exhibited strong antitumor activity against transplantable leukemias in mice: L1210, L1210(IMC), P388, P815, C1498, EL-4 and RL ♂ 1. It also exhibited antitumor activity against M5076 fibrosarcoma, AH66 and AH66F rat hepatomas, but not against Meth-A fibrosarcoma, B16 melanoma, Lewis lung carcinoma (LL) and C26 colon adenocarcinoma. The antitumor activity of SGL was administration-schedule dependent. The strongest activity against L1210 was obtained by ip continuous infusion for 7 days or daily ip administration for 9 days. Single ip injection of SGL<br>at 100 mg/kg to mice caused convulsion and death within 15 minutes after injection. Such acute toxicity was not observed by continuous infusion. SGL showed its strongest activity at subtoxic dose against sensitive tumors except for L1210(IMC). Mice implanted ip with L1210(IMC) were cured by treatment with SGL at 3.13 mg/kg/day for 9 days, but died from the tumor at 50 mg/kg/day ×9. The cured mice rejected a second inoculation of up to 106 tumor cells. The tumor cells isolated from mice after treatment with the high dose showed resistance to SGL in vivo. Mice implanted sc with L1210(IMC) were also cured by 9 daily ip administrations of SGL at 12.5 mg/kg/day, but solid tumor was observed at the implantation site until 3 days after the final injection of SGL in some cured mice. These results suggest that the therapeutic effect of SGL has a relatively high specificity for leukemias and that the immunological effect is involved in the antitumor activity.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 39 (10), 1461-1466, 1986
公益財団法人 日本感染症医薬品協会
