{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Annang F"],"funding":["instituto de salud carlos iii subdirección general de redes y centros de investigación cooperativa-red de investi-gación cooperativa en enfermedades tropicales","fp7 people: marie-curie actions","ministerio de ciencia e innovación","fp7 people: marie-curie actions (paramet)","plan nacional","instituto de salud carlos iii subdirección general de redes y centros de investigación cooperativa-red de investi-gación cooperativa en enfermedades tropicales","junta de andalucía","ministerio de ciencia e innovación"],"pagination":["457"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8647499"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["20(1)"],"pubmed_abstract":["Background
Malaria is a global health problem for which novel therapeutic compounds are needed. To this end, a recently published novel family of antiplasmodial macrolides, strasseriolides A-D, was herein subjected to in vivo efficacy studies and preclinical evaluation in order to identify the most promising candidate(s) for further development.Methods
Preclinical evaluation of strasseriolides A-D was performed by MTT-based cytotoxicity assay in THLE-2 (CRL-2706) liver cells, cardiotoxicity screening using the FluxOR™ potassium assay in hERG expressed HEK cells, LC-MS-based analysis of drug-drug interaction involving CYP3A4, CYP2D6 and CYP2C9 isoforms inhibition and metabolic stability assays in human liver microsomes. Mice in vivo toxicity studies were also accomplished by"],"journal":["Malaria journal"],"pubmed_title":["Preclinical evaluation of strasseriolides A-D, potent antiplasmodial macrolides isolated from Strasseria geniculata CF-247,251."],"pmcid":["PMC8647499"],"funding_grant_id":["PID2019-109623RB-100 and SAF 2016-79957-R","290080","RICET: RD16/0027/0014","BIO-199","RD16/0027/0015, and RD12/0018/0005","PCT- 010000-2010-4 (NMR), INP-2011-0016-PCT-010000 ACT6 (polarimeter, HPLC, and IR), and PCT-01000-ACT7, 2011-13 (plate reader)]"],"pubmed_authors":["Sanchez P","Annang F","Tanghe S","Ruiz-Perez LM","Reyes F","Gonzalez-Pacanowska D","Rodriguez A","Perez-Moreno G","Vicente F","Gonzalez-Menendez V","Del Palacio JP","de Pedro Montejo N","Cantizani J","Perez-Victoria I","Genilloud O","Diaz C"],"additional_accession":[]},"is_claimable":false,"name":"Preclinical evaluation of strasseriolides A-D, potent antiplasmodial macrolides isolated from Strasseria geniculata CF-247,251.","description":"Background
Malaria is a global health problem for which novel therapeutic compounds are needed. To this end, a recently published novel family of antiplasmodial macrolides, strasseriolides A-D, was herein subjected to in vivo efficacy studies and preclinical evaluation in order to identify the most promising candidate(s) for further development.Methods
Preclinical evaluation of strasseriolides A-D was performed by MTT-based cytotoxicity assay in THLE-2 (CRL-2706) liver cells, cardiotoxicity screening using the FluxOR™ potassium assay in hERG expressed HEK cells, LC-MS-based analysis of drug-drug interaction involving CYP3A4, CYP2D6 and CYP2C9 isoforms inhibition and metabolic stability assays in human liver microsomes. Mice in vivo toxicity studies were also accomplished by","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Dec","modification":"2025-05-18T13:22:25.313Z","creation":"2025-05-18T13:22:25.313Z"},"accession":"S-EPMC8647499","cross_references":{"pubmed":["34865639"],"doi":["10.1186/s12936-021-03993-8"]}}