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The chemical synthesis of 16beta-hydroxyandrosterone was described preparatory to studies of the disulphates of the 16-oxygenated ketonic C19 steroids present in the bile of female rats dosed with [3H]androsterone sulphate. The biliary metabolites were separated by chromatography on Sephadex LH-20 to afford monosulphate and diconjugate fractions. After solvolysis of the diconjugate fraction, the liberated steroids were separated by partition chromatography on Celite 545 and analyzed by gas chromatography-mass spectometry. In addition to 3alpha, 17beta-dihydroxy-5alpha-androstan-16-one isolated previously, 16beta-hydroxyandrosterone was identified as a disulphate.

From experimental observations, Peplomycin was expected to be more active against a variety of tumors and to be less toxic for the lung than the parent compound. An intermittent dose(10mg. twice a week) of peplomycin was tested in patients with malignant lymphoma or squamous cell carcinoma who had failed conventional treatment. There were two cases of CR and five cases of PR in twelve cases with malignant lymphoma, and two cases of PR in fourteen cases with squamous cell carcinoma. Out of 26 cases treated with peplomycin, fever was seen in ten cases(38.5%) and pulmonary complication was seen in five cases (19.2%). These data obtained from peplomycin treatment were compared with the results obtained from our previous experiences with bleomycin. Response rate, spectrum and frequency of side reactions of peplomycin treatment were substantially identical with those of bleomycin treatment. However, remission duration and life span were much longer in peplomycin treatment. In this respect, peplomycin seems to be superior than bleomycin to a certain extent.

We found that PSK has an antiviral effect on human immunodeficiency virus (HIV) in vitro. One of the mechanisms of this effect is attributable to the inhibition of binding of HIV with lymphocytes. Here, we found that PSK inhibits reverse transcriptase in a non-competitive way in vitro. Such inhibition may be important in its anti-HIV effect as well as its inhibitory effect on the binding of HIV with lymphocytes.

To elucidate the effects of PSK, a protein-bound polysaccharide from Coriolus versicolor, on gene expression in tumor cells, we prepared cDNA clone libraries from PSK-treated and untreated cells of a rat ascites hepatoma line, AH66, which was previously shown to be susceptible to the antitumor action of this compound. Two PSK-induced and one suppressed cDNA clones were selected from these libraries by using a differential colony hybridization and RNA blot hybridization. PSK was thus shown to have a direct effect on the transcription and consequently on the translation of tumor cells.