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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Schistosomicidal activity of kaurane, labdane and clerodane-type diterpenes obtained by fungal transformation

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Oliveira, Larissa Costa [1] ; Porto, Thiago Souza [1] ; Colmanette Junior, Arthur Henrique [1] ; Conceicao Santos, Mario Ferreira [1] ; Ramos, Henrique Pereira [1] ; Braun, Glaucia Hollaender [1] ; de Lima Paula, Lucas Antonio [1] ; Bastos, Jairo Kenupp [2] ; Jacometti Cardoso Furtado, Niege Aracari [2] ; Tame Parreira, Renato Luis [1] ; Sola Veneziani, Rodrigo Cassio [1] ; Magalhaes, Lizandra Guidi [1] ; Ambrosio, Sergio Ricardo [1]
Total Authors: 13
[1] Univ Franca, Nucleus Res Technol & Exact Sci, BR-14404600 Franca, SP - Brazil
[2] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Process Biochemistry; v. 98, p. 34-40, NOV 2020.
Web of Science Citations: 1

Schistosomiasis continues to be a huge challenge for researchers, pharmaceutical companies, and governments in developing countries. Diterpene compounds are good source for the development of novel potential leading compounds to treat schistosomiasis. We are reporting herein the schistosomicidal activity of ent-kaurenoic acid, ent-copalic acid, ent-hardwickiic acid, isolated from oleoresins of Copaifera spp, and of their derivatives obtained by fungal transformation with strains of Aspergillus fumigants, A. terreus, A. phoenicis and A. ochraceus, and of Cunninghamella echinulata e C. elegans. The in vitro antiparasitical assays were performed using adult worm pairs of Schistosoma mansoni for the evaluation of the worm pairing, egg production, and eggs development. Ten kaurane, labdane and clerodane-type diterpenes were obtained by fungal transformation and 7 alpha-acetoxy-ent-kaur-16-en-19-oic acid and ent-hardwickiic acid were the most active ones by causing mortality of 100 % of the parasites within 24 h (concentrations of 100.0 and 200.0 mu M) and displaying respective IC50 values for 24, 48 and 72 h of 56.7, 37.6 and 29.2 mu M and 29.6, 30.8 and 25.7 mu M. Additionally, 7a-acetoxy-em-kaur-16-en-19-oic acid and ent-hardwickiic acid highly reduced the number of laid eggs at 6.25 and 12.5 mu M, respectively. These diterpenes should be further investigated as potential candidates for antiparasitic drug discovery. (AU)

FAPESP's process: 11/21638-8 - Biotransformation of kaurenoic acid by filamentous fungi and evaluation of the anti-phytopathogenic properties of the obtained metabolites.
Grantee:Thiago Sousa Porto
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 17/02592-3 - Biotransformation of cubebin and hardwickiic acid by Cunninghamella echinulata and biological activities evaluation
Grantee:Larissa Costa Oliveira
Support type: Scholarships in Brazil - Master
FAPESP's process: 11/13630-7 - Chemical and pharmacological validation of extracts and active compounds of Copaifera species
Grantee:Jairo Kenupp Bastos
Support type: Research Projects - Thematic Grants