Assessment of the cytotoxic and clastogenic activities of the sesquiterpene lactone lynchnopholide in mammalian cells in vitro and in vivo.

Lychnopholide (LNP), a sesquiterpene lactone with antitumor, trypanocidal, and antimicrobial activities, was isolated from Vanillosmopsis erythropappa. The present study was carried out to assess the cytotoxic and clastogenic potential of this new agent in human cultured lymphocytes and Swiss bone marrow cells before the agent was used in medicine. The mitotic index, chromosomal aberrations (CAs), sister chromatid exchanges (SCEs), and proliferation index were investigated. There was no alteration in the number of CAs and SCEs in the continuous in vitro treatment. However, the highest concentration (0.2 microg/ml) of LNP was cytotoxic. LNP (0.1, 0.2, and 0.4 microg/ml) induced a significant increase in CA frequency at the G2 phase in all treated cultures. Only the highest concentration (26.67 mg/kg) caused a significant increase in the total number of CAs in the in vivo investigation. On the basis of these results, LNP had a clastogenic effect on both test systems and a cytotoxic effect in vitro.

Glaucolide B, A Molluscicidal Sesquiterpene Lactone, and Other Constituents of Vernonia eremophila.

The sesquiterpene lactone glaucolide B was isolated from the molluscicidal extract of VERNONIA EREMOPHILA Mart, and shown to be responsible for the molluscicidal activity. Hydrogenolysis of glaucolide B resulted in the disappearance of the activity. Other inactive constituents of the extract were 3,7-dimethoxy-5,3',4'-trihydroxyflavone and two transformation products, possibly artefacts, of glaucolide B. Glaucolide B exhibited strong antimicrobial activity against B, CEREUS and moderate activity against S. AURENS, but was inactive in several other systems.

Sesquiterpene Lactones in the Molluscidal Extract of Eremanthus glomerulatus.

The eremantholides 1A, 1B, 1E, 1G, 1H, 1J and the germacranolides 2A, B were found in the molluscidal extract from EREMANTHUS GLOMERULATUS L.