Stochastic-Based
Descriptors Studying
Biopolymers Biological
Properties: Extended
MARCH-INSIDE Methodology
Describing Antibacterial
Activity of Lactoferricin
Derivatives
Ronal Ramos de Armas
1,2
Humberto Gonza ´ lez Dı ´az
1,3
Reinaldo Molina
1,4
Eugenio Uriarte
3
1
Chemical Bioactives Center,
Central University of “Las
Villas” 54830, Cuba
2
Department of Chemistry,
Central University of “Las
Villas” 54830, Cuba
3
Department of Organic
Chemistry,
Faculty of Pharmacy,
University of Santiago de
Compostela 15782, Spain
4
Universita ¨ t Rostock, FB
Chemie,
Albert-Einstein-Str. 3a, D
18059 Rostock, Germany
Received 16 September 2004;
revised 25 October 2004;
accepted 27 October 2004
Published online 28 January 2005 in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/bip.20202
Abstract: Lactoferricin are a number of related peptides derived from the enzymatic cleavage of
lactoferrin, an iron-binding protein. These peptides, and other peptides derived from them by simple
amino acid substitutions, have shown interesting antibacterial activity. In this paper we applied the
MARCH-INSIDE methodology extended to peptide and proteins, to a QSAR study related to
antibacterial activity of 31 derivatives of lactoffericin against E. Coli and S. Aureus by means of
Linear Discriminant (LDA) and Multiple Linear Regression Analysis (MLR). In the case of LDA we
obtained models that classify correctly more than 80% of all cases (85.7% for E. Coli antibacterial
activity and 83.9 for S. Aureus). With the application of a Leave-One-Out Cross Validation
Procedure, the percentage of good classification of both classification models remained near the
above reported values (87.1% for E. Coli antibacterial activity and 83.9 for S. Aureus). We obtained
several linear regression models taking into account total and local descriptors. The inclusion of
those local descriptors improved the correlation parameters, the statistical quality, and the pre-
dictive power of the former model obtained only with total descriptors. The best models explained
more than 80% of the experimental variance in the antimicrobial activity of those compounds. These
Correspondence to: R. Ramos de Armas; email:
ronalr@qf.uclv.edu.cu or ronal@medinews.com
Biopolymers, Vol. 77, 247–256 (2005)
© 2005 Wiley Periodicals, Inc.
247