Effects of homo-aza-steroidal ester of p-BIS(2-chloroethyl)amino phenyl acetic acid on lymphocytes stimulated with phytohemagglutinin in vitro

Abstract

The effect of 2- bis(2-chloroethyl)amino phenyl acetic acid( I) of lactam( II) and of lactam ester( III) were tested in a 48 h culture of human lymphocytes from normal subjects. The experiments yielded evidence that (a) for compound I there is a concentration-dependent increase progressively in the cell damage from the lowest (0.128 × 10 −8 M/ml) the highest concentration used (0.384 × 10 −8 M/ml). On the whole, it was indicated that compound I was rendering the cells almost unable to divide and to incorporate [ 3H]-thymidine proportionally to the concentration used; (b) for compound II no cell damage was observed and its role remains obscure; (c) for compound III there was evidence that in a concentration of 1.42 sx 10 −9 M/ml (which is actually half the corresponding concentration of compound I) it exhibits inhibition of DNA synthesis and low number of mitosis as well as chromosome damage. A fact worth mentioning is that mitotic index and [ 3H]-thymidine incorporation showed the same pattern of response in the lymphocytes examined.