CONTEXT: Praziquantel (PZQ) is the drug available for the treatment of schistosomiasis. The reported reduced cure rates, the failure of treatment after PZQ administration in patients and the existence of resistant parasite strains, reinforce the need to rapidly discover new effective molecules against Schistosoma parasite. OBJECTIVE: To screen the methanol extracts of 79 marine organisms for their schistosomicidal activities against Schistosoma mansoni adult worms in vitro and perform bio-assay directed chromatography for the most active extracts to isolate the active compounds. MATERIALS AND METHODS: Screening of the marine organisms and bio-assay directed chromatography of the most active extracts together with identification of the active isolates using 1D and 2D NMR analysis, were investigated. RESULTS: RESULTS indicated that the isolates echinosides A and B from the sea cucumbers Actinopyga echinites Jaeger and Holothuria polii Delle Chiaie (Holothuriidae) were highly active. Their LC(50) values were equal to 0.19 μg/ml and 0.27 μg/ml, respectively. Detailed (1)HNMR data for echinosides A and B are reported here for the first time. DISCUSSION AND CONCLUSION: These findings demonstrate that the isolated echinosides possess potential in vitro schistosomicidal activity against S. mansoni adult worms. Therefore, echinosides are promising as lead compounds for the development of new schistosomicidal agents.
CONTEXT: Praziquantel (PZQ) is the drug available for the treatment of schistosomiasis. The reported reduced cure rates, the failure of treatment after PZQ administration in patients and the existence of resistant parasite strains, reinforce the need to rapidly discover new effective molecules against Schistosoma parasite. OBJECTIVE: To screen the methanol extracts of 79 marine organisms for their schistosomicidal activities against Schistosoma mansoni adult worms in vitro and perform bio-assay directed chromatography for the most active extracts to isolate the active compounds. MATERIALS AND METHODS: Screening of the marine organisms and bio-assay directed chromatography of the most active extracts together with identification of the active isolates using 1D and 2D NMR analysis, were investigated. RESULTS: RESULTS indicated that the isolates echinosides A and B from the sea cucumbers Actinopyga echinites Jaeger and Holothuria polii Delle Chiaie (Holothuriidae) were highly active. Their LC(50) values were equal to 0.19 μg/ml and 0.27 μg/ml, respectively. Detailed (1)HNMR data for echinosides A and B are reported here for the first time. DISCUSSION AND CONCLUSION: These findings demonstrate that the isolated echinosides possess potential in vitro schistosomicidal activity against S. mansoni adult worms. Therefore, echinosides are promising as lead compounds for the development of new schistosomicidal agents.
Authors: Lara Soares Aleixo de Carvalho; Vinícius Carius de Souza; Vinícius C Rodrigues; Aline Correa Ribeiro; Jorge Willian Leandro Nascimento; Priscila V S Z Capriles; Priscila de F Pinto; Josué de Moraes; Ademar Alves da Silva Filho Journal: Pharmaceutics Date: 2022-05-17 Impact factor: 6.525
Authors: Muhammad A Alsherbiny; Shymaa A El Badawy; Hesham Elbedewy; Shahira M Ezzat; Fatma S Elsakhawy; Mostafa A Abdel-Kawy Journal: Pharmacognosy Res Date: 2018 Jan-Mar
Authors: Alejandro M S Mayer; Abimael D Rodríguez; Orazio Taglialatela-Scafati; Nobuhiro Fusetani Journal: Mar Drugs Date: 2017-08-29 Impact factor: 5.118
Authors: Mike Kareh; Rana El Nahas; Lamis Al-Aaraj; Sara Al-Ghadban; Nataly Naser Al Deen; Najat Saliba; Marwan El-Sabban; Rabih Talhouk Journal: SAGE Open Med Date: 2018-11-02