TY - JOUR
T1 - Iheyamides A-C, Antitrypanosomal Linear Peptides Isolated from a Marine Dapis sp. Cyanobacterium
AU - Kurisawa, Naoaki
AU - Iwasaki, Arihiro
AU - Jeelani, Ghulam
AU - Nozaki, Tomoyoshi
AU - Suenaga, Kiyotake
N1 - Funding Information:
This work was supported by JSPS KAKENHI (Grant Numbers 18K14346, 19H04662, and 16H03285) and Keio Gijuku Academic Development Funds.
Publisher Copyright:
© 2020 American Chemical Society and American Society of Pharmacognosy.
PY - 2020/5/22
Y1 - 2020/5/22
N2 - Iheyamides A (1), B (2), and C (3), new linear peptides, were isolated from a marine Dapis sp. cyanobacterium. Their structures were elucidated by spectroscopic analyses and degradation reactions. Iheyamide A (1) showed moderate antitrypanosomal activities against Trypanosoma brucei rhodesiense and Trypanosoma brucei brucei (IC50 = 1.5 μM), but the other two analogues, iheyamides B (2) and C (3), did not (IC50 > 20 μM, respectively). The structure-activity relationship clarified that an isopropyl-O-Me-pyrrolinone moiety was necessary for the antitrypanosomal activity. Furthermore, the cytotoxicity of 1 against normal human cells, WI-38, was 10 times weaker than its antitrypanosomal activity (IC50 = 18 μM).
AB - Iheyamides A (1), B (2), and C (3), new linear peptides, were isolated from a marine Dapis sp. cyanobacterium. Their structures were elucidated by spectroscopic analyses and degradation reactions. Iheyamide A (1) showed moderate antitrypanosomal activities against Trypanosoma brucei rhodesiense and Trypanosoma brucei brucei (IC50 = 1.5 μM), but the other two analogues, iheyamides B (2) and C (3), did not (IC50 > 20 μM, respectively). The structure-activity relationship clarified that an isopropyl-O-Me-pyrrolinone moiety was necessary for the antitrypanosomal activity. Furthermore, the cytotoxicity of 1 against normal human cells, WI-38, was 10 times weaker than its antitrypanosomal activity (IC50 = 18 μM).
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U2 - 10.1021/acs.jnatprod.0c00250
DO - 10.1021/acs.jnatprod.0c00250
M3 - Article
C2 - 32352773
AN - SCOPUS:85085264943
SN - 0163-3864
VL - 83
SP - 1684
EP - 1690
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 5
ER -
