Chinese Academy of Medical Sciences, Institute antibiotic in 1969 from China Zhejiang Wenzhou Pingyang, Pingyang soil Streptomyces isolated and produced from a variety of bleomycin was selected components of a single component, that PYM (PYM).
PYM experimental studies, animal experiments on rats and mice Walker carcinosarcoma 256 of 180 sarcoma, sarcoma 37, liver cancer , melanoma, significantly inhibit about 90%. Colon cancer in mice subcutaneously C26, and Lewis lung cancer esophageal SGA73 have strong anti-tumor effect. In vitro experiments on liver cancer BEL7402, gastric cancer MGC-803, esophageal Ecal09 and caEs17, nasopharyngeal carcinoma CNE, HT29 colon cancer and oral squamous cell carcinoma KB cell killing effect. PYM's role is to inhibit DNA synthesis and cut off the DNA chain.
To the inoculation of Ehrlich ascites carcinoma bearing mice injected with PYM, determination of kidney, stomach, lung, liver, spleen, heart, muscle, blood, bone tumor and the drug concentration, in addition to kidney, the tumor drug concentration in the highest Compared with the plasma concentration of 4:1. Rabbits after intravenous injection of PYM for 15min, the maximum plasma concentration, after the rapid decline, 2h after undetectable. After intramuscular injection of 15min, the maximum plasma concentration, but the peak concentration is lower than the intravenous injection, the concentration decreased slowly, 4h after only a trace.
PYM experimental study of acute toxicity tests in mice, intravenous administration of LDso to 165mg / Zhi, intraperitoneal administration is 188mg/kg. PYM drug irritation: a rabbit intramuscular injection, no injection stimulus response time, multiple injections of local mild congestion.
Comparison with the BLM Pingyangmycin: PYM on dogs no effect on liver function; BLM had liver toxicity, but recoverable. Bone marrow suppression and immune function, the two drugs had no effect.
The main side effects BLM pulmonary toxicity, skin toxicity and fever, little or no bone marrow suppression. Its incidence: lung toxicity and dose and age have a certain relationship, BLM total more than 450mg, aged 70 years or older, increased incidence of pulmonary toxicity.
Experimental Study of Bleomycin, BLM has been involved in head and neck squamous cell carcinoma, malignant lymphoma , testicular cancer and esophageal cancer combined with chemotherapy such as BPV, BACOP, BFP and other chemotherapy regimens, and improved efficacy.