Potent Anti-Calmodulin Activity of Cyclotetradepsipeptides Isolated from Isaria fumosorosea Using a Newly Designed Biosensor-Reference-Cited by-同舟云学术

Potent Anti-Calmodulin Activity of Cyclotetradepsipeptides Isolated from Isaria fumosorosea Using a Newly Designed Biosensor

Published:2015-01 Issue:1 Volume:10 Page:1934578X1501000
ISSN:1934-578X
Container-title:Natural Product Communications
language:en
Short-container-title:Natural Product Communications

Author:

Madariaga-Mazón Abraham¹,González-Andrade Martín²,Toriello Conchita³,Navarro-Barranco Hortensia³,Mata Rachel¹

Affiliation:

1. Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico

2. Departamento de Bioquímica, Facultad de Medicina, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico

3. Departamento de Microbiología y Parasitología, Facultad de Medicina, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico

Abstract

Seven cyclotetradepsipeptides, namely beauverolides C (1), F (2), I (3), Ja (4), L (5), M (6), and N (7), were isolated from the entomopathogenic fungus Isaria fumosorosea. The beauverolides were evaluated as potential calmodulin (CaM) inhibitors using the newly designed CaM biosensor hCaM M124C- AF350; these peptides displayed high affinity to the protein with dissociation constants ( Kd) ranging from 0.078 μM to 3.44 μM. Beauverolide Ja, the only one containing a tryptophan residue in its structure, showed the highest affinity. The docking study predicted that beauverolides could bind to CaM in the same site of interaction as chlorpromazine, a well-known calmodulin ligand.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

Link

http://journals.sagepub.com/doi/pdf/10.1177/1934578X1501000128

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