Skip to main content
. Author manuscript; available in PMC: 2016 Jul 12.
Published in final edited form as: Curr Opin Mol Ther. 2004 Dec;6(6):657–665.
Study Type Effect Studied Experimental Model Result Reference
In vitro Selectivity. A549, HT29 and LoVo cells or
P388 and KB cells.
Kahalalide F displayed selectivity against solid
tumor cell lines with IC50 values of 2.5, 0.25 and
< 1.0 µg/ml against A549, HT29 and LoVo,
respectively, while IC50 values against P388 and
KB cells were 10 and > 10 µg/ml, respectively.
506285
In vitro Efficacy. Various prostate and breast
cancer cell lines, as well as cell
lines derived from normal human
tissues.
Kahalalide F displayed potent cytotoxic activity
against various prostate and breast cancer cell
lines (DU145, LNCaP, SKBR3, BT474 and MCF7)
with IC50 values ranging from 0.07 (PC3) to 0.28
µM. However, non-tumor human cell lines derived
from various origins (MCF10A, HUVEC, HMEC-1
and IMR90) were 5- to 40-fold less sensitive, with
IC50 values of 1.6 to 3.1 µM.
526699
In vitro Activity. PC3 cells incubated with
kahalalide F at 0.25 or 0.5 µM for
12 to 48 h and analyzed by flow
cytometry, and PC3 cells
incubated with 0.5 µM for 2 to 24
h followed by DNA analysis by
agarose gel electrophoresis.
No hypodiploid peak (characteristic of apoptosis)
nor arrest in any phase of the cell cycle for PC3
cells was observed and there was no evidence of
a ladder typical of the DNA degradation caused by
apoptosis.
526699
In vitro Toxicity. Murine-derived cardiac (H9 c2
(2-1)), skeletal muscle (L8), liver
(AML-12), kidney (NRK-52E),
and myelogenous stem (FDC-P1)
cells exposed to kahalalide F.
LD50 values against H9 c2 (2-1), L8, AML-12,
NRK-52E and FDC-P1 cells were 5 mM, 0.6 mM,
0.17 µM, 1.6 µM and 14 µM, respectively.
389847
In vitro Toxicity. Immunohistochemical method to
determine viability of neural cells
after kahalalide F exposure.
At 10 µM, kahalalide F was toxic to CNS neurons,
but spared astrocytes, sensory and motor neurons
in the spinal cord.
389847