PENGARUH PENINGKATAN LIPOFILISITAS PADA SENYAWA ANALOG UK-3A DALAM MENGHAMBAT PERTUMBUHAN SEL KANKER P-388
Abstract: Antibiotic UK-3A
contains a 9-membered dilactone ring. It had been isolated as a minor component
from the mycelium of 5trepyomyces sp. 51701.The antibiotic was hypothesized to
be potential to inhibit the growth of leukemia cancer cell line of P388 and KB
with ICso 38 and 20 Dg/mL, respectively. To understand the effect of
lipophilicity increase of the analogues on their anticancer activities based on
QSAR parameter (Log P) and binding energy to BcL-xL protein. To produce
analogues of UK-3A, 3hydroxypicolinyl serine methyl ester (A) was synthesized
from 3-hydroxypicolinic acid and L-serine methyl ester. The product was then
esterified by pentanoic (1), hexanoic (2), heptanoic (3), and octanoic (4). The
final products were confirmed with IHand 13C FT-NMR and FTIR spectra, and also
MS spectra. Then they were tested against P388 Murine Leukemia cells. The
result of bioassay showed lipophilicity increase of3hydroxypicolinyl serine
methyl octhyl ester (PSMOE) correlated positively with their anticancer
activity increase, withICso 15.4mg/mL against P388 cell lines.
Penulis: Hanafi M, Y Anita,
AMJ. Putra, A. Darmawan, N. Artanti, Linar Z. Udin
Kode Jurnal: jpkimiadd090257
