PMID- 158571 OWN - NLM STAT- MEDLINE DCOM- 19791220 LR - 20190902 IS - 0367-8377 (Print) IS - 0367-8377 (Linking) VI - 14 IP - 2 DP - 1979 Aug TI - A lipophilic derivative of neocarzinostatin. A polymer conjugation of an antitumor protein antibiotic. PG - 81-7 AB - A lipophilic derivative of neocarzinostatin (NCS), an antitumor antibiotic, was prepared by reaction with a synthetic water-soluble polymer, [(styrene)1 approximately 3-(maleic acid 4 approximately 7/anhydride 1)]. The reaction was carried out at pH 8.6 for 3 h and aimed at modifying the two nonessential amino groups (alpha-amino of Ala-1, epsilon-amino of Lys-20). The NCS-polystyrene (SMANCS) was purified on a column of Sephadex G-100 in 0.05 M ammonium bicarbonate and the main product was obtained as a single peak. The elemental analysis showed an increased C and a decreased N content. U.v. and i.r. absorption spectra for SMANCS showed the presence of styrene. SDS-acrylamide gel electrophoresis at pH 8.5 and the decreased N content suggested a molecular weight of about 25 000, indicating the numbers of polymers conjugated to be about six units, two of which were found attached to the two amino groups. SMANCS was soluble in organic solvents, in contrast to NCS, and in water. SMANCS exhibited increased chemical and biological stability and appeared to possess similar in vitro biological activity. FAU - Maeda, H AU - Maeda H FAU - Takeshita, J AU - Takeshita J FAU - Kanamaru, R AU - Kanamaru R LA - eng PT - Journal Article PL - Denmark TA - Int J Pept Protein Res JT - International journal of peptide and protein research JID - 0330420 RN - 0 (Amino Acids) RN - 0 (Antibiotics, Antineoplastic) RN - 0 (Polymers) RN - 9014-02-2 (Zinostatin) SB - IM MH - Amino Acids/analysis MH - *Antibiotics, Antineoplastic/*chemical synthesis MH - Chromatography, Gel MH - Electrophoresis, Polyacrylamide Gel MH - Polymers MH - Zinostatin/analogs & derivatives/analysis/*chemical synthesis EDAT- 1979/08/01 00:00 MHDA- 1979/08/01 00:01 CRDT- 1979/08/01 00:00 PHST- 1979/08/01 00:00 [pubmed] PHST- 1979/08/01 00:01 [medline] PHST- 1979/08/01 00:00 [entrez] AID - 10.1111/j.1399-3011.1979.tb01730.x [doi] PST - ppublish SO - Int J Pept Protein Res. 1979 Aug;14(2):81-7. doi: 10.1111/j.1399-3011.1979.tb01730.x.