Bioefficacy of ursolic acid and its derivatives isolated from Catharanthus roseus (L) G. Don leaf against Aedes aegypti, Culex quinquefasciatus, and Anopheles stephensi larvae

The aim of the presentstudy was to identify the active principle from Catharanthus roseus leaf using larvicidal bioassay against three mosquito species viz. Aedes aegypti, Culex quinquefasciatus, and Anopheles stephensi. Preliminary studies of the three successive extracts such as hexane, chloroform, and methanol against Ae. aegypti larvae showed that the chloroform extract was more active with LC50 and LC90 values of 40.09 ppm and 189.15 ppm respectively. Bioassay guided fractionation of the active chloroform extract resulted in the isolation of a triterpenoid (ursolic acid) as the active constituent. Three derivatives acetate, formate, and benzoate were prepared using this, and they were tested for their larvicidal activity against three mosquito species. The acetyl derivative was highly active against all the three species compared to the parent compound ursolic acid; the activities of benzoate and formate were higher than ursolic acid when tested against Cx. quinquefasciatus. This is the first report related to ursolic acid from C. roseus with mosquito larvicidal activity. The pure compound could be considered for medicinal and other pharmacological applications in future.

Automated summary

The aim of this study was to identify the active principle from the leaves of Catharanthus roseus against three mosquito species. The chloroform extract showed the highest larvicidal activity, and a triterpenoid called ursolic acid was isolated as the active constituent. Derivatives of ursolic acid were prepared and tested for their larvicidal activity, with the acetyl derivative showing the highest activity against all three mosquito species. This is the first report of ursolic acid from C. roseus with larvicidal activity.