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2015.03.17생명공학부2847
- 일시 : 2015.03.27
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◈ 주 제 : Research Works on Natural Products
◈ 연 사 : Wei Li
◈ 소 속 : 영남대학교
◈ 일 시 : 2015년 3월 27일(금) 오후 3시
30분
◈ 장 소 : 영남대학교 생명공학관 333호
< Abstract >
Pulsatilla
koreana Nakai in the family Ranunculaceae is a species
endemic to Korea. It is an important herb in traditional medicine that has been
used to treat amoebic dysentery, malaria, epistaxis, leucorrhoea, scrofula,
internal hemorrhoids and also as a contraceptive. Phytochemical study of the
root of P. koreana resulted in the
isolation of thirty-eight compounds,
including one new oleanane-type triterpenoid saponin, pulsatilloside F (16),
along with thirty-seven known compounds (1–15 and 17–38).
Compounds 8–12 and
21–25 significantly diminished the proliferation of HL-60 cells
with IC50 values from 0.3 to 4.2 μM. Furthermore, apoptotic
characteristics such as chromatin condensation and increase in the population
of sub-G1 hypodiploid cells were observed after the HL-60 cells were treated
with these compounds. Compounds 7, 20–25, 29, 30,
41, 44, 45 and 50 inhibited NF-κB activation
stimulated by TNF α in a dose-dependent manner, with IC50 values ranging from 0.75 to 9.89 μM. PPARs
activation and PPAR subtype transcriptional activity of compounds 39–50were measured in HepG2 cells. Compounds 8–12 and 21–25activated the transcriptional activity of PPARs in a dose-dependent manner, with EC50 values ranging from 0.9
to 10.8 μM.
Zanthoxylum
schinifolium is an aromatic shrub, and its pericarp and
leaves are widely used in culinary applications in East Asian countries. It has also long been used in traditional
Oriental medicine for treating the common cold, stomach ache,
diarrhea, and jaundice. In this
study, we identified four new compounds, schinifolisatin (10), zanthoxyloside (12),
schinifolisatin A (36), and
zanthoxyloside A (37), along with 44
known compounds (1–9,11, 13–35, and 38–48), from a methanol extract of the
stems of Z. schinifolium.The chemical structures of the compounds were determined by mass, 1D-, and 2D
NMR spectroscopy. The anticancer effect of the isolated compounds were examined
in three human cancer cell lines. Compounds 7–9 significantly
reduced the proliferation of HL-60 leukemia cells with IC50 values
of 4.62-5.12 μM. Treatment of PC-3 prostate cancer cells and SNU-C5 colorectal
cancer cells with compound 9resulted in potent antiproliferative activity, with IC50 values of 4.39
and 6.26 μM, respectively. Also, compounds 7–9 induced the apoptosis of three cancer
cells. Furthermore, the induction of apoptosis was accompanied by down-regulation of p-ERK1/2 MAPK, p-AKT, and
c-myc levels, in a time-dependent manner. Compounds 16, 37, 43, and 44 exhibited significant inhibition of NF-κB
activation and inhibited TNFα-induced expression of iNOS
and ICAM-1 mRNA and dose-dependent inhibition of iNOS promoter
activity.
This study is the first time to integrated chemical investigation
on oleanane-type triterpenoid saponins from P.
koreana root, and this is the
first report of the anti-inflammatory and the effects on NF-κB
inhibition and anti-cancer of isolated compounds from Z. schinifolium. These results may provide a scientific basis
for the active components in P.
koreana and Z. schinifolium,
as well as for the development of novel anti-inflammatory and anti-cancer
agents.
영남대학교 생명공학연구소장
▲문의처 : TEL : 810-3598 (생명공학연구소 http://biotech.yu.ac.kr)