Studies on the Surface Anesthetic Activity of Bufadienolides Isolated from Ch’ an Su

Abstract

The surface anesthetic activities of ten bufadienolides, i.e., resibufogenin, bufalin, bufotalin, desacetyl-bufotalin, cinobufagin, desacetyl-cinobufagin, cinobufotalin, desace-tyl-cinobufotalin, telocinobufagin and marinobufagin, were studied using the guinea pig cornea. With exceptions of resibufogenin and marinobufagin, all substances tested were more effective than cocaine. Their anesthetic activities were in the following order: bufalin>telocinobufagin>bufotalin> cinobufagin > cinobufotalin > desacetyl-bufotalin ≧ desacetyl-cinobufagin≧desacetyl-cinobufotalin. Resibufogenin and marinobufagin had no appreciable effect on the cornea. There is some correlation between the chemical structure and the surface anesthetic activity in the bufadienolides tested. © 1976, The Pharmaceutical Society of Japan. All rights reserved.