| Full text | |
| Author(s): |
da Silva, Jaff Ribeiro
[1, 2]
;
de Cerqueira e Silva, Mariana Barros
[2]
;
Philadelpho, Biane Oliveira
[1]
;
de Souza, Victoria Cruz
[1]
;
Machado dos Santos, Johnnie Elton
[1]
;
Castilho, Marcelo Santos
[1]
;
Ferreira, Ederlan de Souza
[1]
;
Cilli, Eduardo Maffud
[2]
Total Authors: 8
|
| Affiliation: | [1] Univ Fed Bahia, Sch Pharm, Barao de Jeremoabo St, BR-40170115 Salvador, BA - Brazil
[2] Sao Paulo State Univ, Inst Chem, UNESP, Rua Prof Francisco Degni, BR-14800060 Araraquara, SP - Brazil
Total Affiliations: 2
|
| Document type: | Journal article |
| Source: | FOOD BIOSCIENCE; v. 44, n. B DEC 2021. |
| Web of Science Citations: | 0 |
| Abstract | |
Two newly designed peptides, Pyr-GF and GSTLN, enhance pravastatin inhibition of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase (HMGCoAR). In silica experiments have demonstrated the interaction of these peptides with the catalytic and NADPH sites of HMGCoAR. In vitro, the Pyr-GF (IC50 = 117.4 mu M) and GSTLN (IC50 = 278.1 mu M) peptides exhibit dose-dependent inhibition on the HMGCoAR activity, and the effects are more significant than those observed for original peptides obtained from cowpea and adzuki beans. Compared to pravastatin alone, the Pyr-GF/pravastatin combination produced a small decrease (8%) in HMGCoAR activity, whereas the GSTLN/pravastatin combination produced a significant decrease of 41% on HMGCoAR activity. The association between Pyr-GF/GSTLN peptides decreased the IC50 to 71.8 mu M. These results suggest their interaction with different sites; Pyr-GF and pravastatin mainly act on the catalytic site and GSTLN on the NADPH site. Hence, the Pyr-GF and GSTLN peptides and their combination exhibit a cholesterol-lowering effect and act as adjuvants upon association with pravastatin. (AU) | |
| FAPESP's process: | 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery |
| Grantee: | Glaucius Oliva |
| Support Opportunities: | Research Grants - Research, Innovation and Dissemination Centers - RIDC |
| FAPESP's process: | 14/50926-0 - INCT 2014: biodiversity and natural products |
| Grantee: | Vanderlan da Silva Bolzani |
| Support Opportunities: | BIOTA-FAPESP Program - Thematic Grants |