TY - JOUR
T1 - Biological activities of 1,1,6-trisubstituted indanes
T2 - Beyond magainin 2
AU - Numao, Naganori
AU - Hirota, Yukiko
AU - Iwahori, Akiyo
AU - Kidokoro, Shun Ichi
AU - Sasatsu, Masanori
AU - Kondo, Isamu
AU - Itoh, Sachiko
AU - Itoh, Etsuko
AU - Katoh, Tadashi
AU - Shimozono, Noriko
AU - Yamazaki, Akiko
AU - Takao, Ken Ichi
AU - Kobayashi, Susumu
PY - 1999/1
Y1 - 1999/1
N2 - MSI-78 is a peptide analog of naturally occurring magainin 2 isolated from the skin of Xenopus laevis. The peptide is known to have one of the strongest antibacterial activities in magainin 2 analogs against methicillin- resistant Staphylococcus aureus (MRSA). To find novel compounds superior to MSI-78, we have further designed, synthesizing 1,1-di(4-aminobutyl)-6- benzylindane (PM4) and 1,1-dibenzyl-6-(4-aminobutyl) indane (PM5), and tested their inhibitory ability of the growth of S. aureus. In an in vitro assay, PM4 showed the same antibacterial activity against the bacterium as MSI-78, and non-hemolytic activity against human red blood cells (RBCs) at the MIC (minimum inhibitory concentration) value, in contrast to the latter. On the other hand, PM5 showed stronger antibacterial activity than MSI-78, but being still accompanied with hemolysis at the MIC value. Otherwise, stronger decarboxylase activity for oxaloacetate was observed in PM5, rather than magainin 2 analogs or Oxaldie 1 as a control peptide, but not in PM4.
AB - MSI-78 is a peptide analog of naturally occurring magainin 2 isolated from the skin of Xenopus laevis. The peptide is known to have one of the strongest antibacterial activities in magainin 2 analogs against methicillin- resistant Staphylococcus aureus (MRSA). To find novel compounds superior to MSI-78, we have further designed, synthesizing 1,1-di(4-aminobutyl)-6- benzylindane (PM4) and 1,1-dibenzyl-6-(4-aminobutyl) indane (PM5), and tested their inhibitory ability of the growth of S. aureus. In an in vitro assay, PM4 showed the same antibacterial activity against the bacterium as MSI-78, and non-hemolytic activity against human red blood cells (RBCs) at the MIC (minimum inhibitory concentration) value, in contrast to the latter. On the other hand, PM5 showed stronger antibacterial activity than MSI-78, but being still accompanied with hemolysis at the MIC value. Otherwise, stronger decarboxylase activity for oxaloacetate was observed in PM5, rather than magainin 2 analogs or Oxaldie 1 as a control peptide, but not in PM4.
KW - Antibacterial activity
KW - Decarboxylase activity
KW - Indane derivative
KW - Magainin 2 analog
KW - Peptidomimetic
KW - S. aureus
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U2 - 10.1248/bpb.22.73
DO - 10.1248/bpb.22.73
M3 - Article
C2 - 9989665
AN - SCOPUS:0033054821
VL - 22
SP - 73
EP - 76
JO - Biological and Pharmaceutical Bulletin
JF - Biological and Pharmaceutical Bulletin
SN - 0918-6158
IS - 1
ER -