Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Cheon Soo Park; Yongchel Ahn; Dahae Lee; Sung Won Moon; Ki Hyun Kim; Noriko Yamabe; Gwi Seo Hwang; Hyuk Jai Jang; Heesu Lee; Ki Sung Kang; Jae Wook Lee

doi:10.1016/j.bmcl.2015.10.093

Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Cheon Soo Park
, Yongchel Ahn
, Dahae Lee
, Sung Won Moon
, Ki Hyun Kim
, Noriko Yamabe
, Gwi Seo Hwang
, Hyuk Jai Jang
, Heesu Lee
, Ki Sung Kang
, Jae Wook Lee

Department of Pharmacy

University of Ulsan
Gachon University
Gangneung-Wonju National University
Korea Institute of Science and Technology
University of Science and Technology UST

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

Original language	English
Pages (from-to)	5705-5707
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2015.10.093
State	Published - 15 Dec 2015

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Anticancer
Apoptosis
Chalcone
HepG2

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10.1016/j.bmcl.2015.10.093

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title = "Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells",

abstract = "Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.",

keywords = "Anticancer, Apoptosis, Chalcone, HepG2",

author = "Park, \{Cheon Soo\} and Yongchel Ahn and Dahae Lee and Moon, \{Sung Won\} and Kim, \{Ki Hyun\} and Noriko Yamabe and Hwang, \{Gwi Seo\} and Jang, \{Hyuk Jai\} and Heesu Lee and Kang, \{Ki Sung\} and Lee, \{Jae Wook\}",

note = "Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd.",

year = "2015",

month = dec,

day = "15",

doi = "10.1016/j.bmcl.2015.10.093",

language = "English",

volume = "25",

pages = "5705--5707",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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}

TY - JOUR

T1 - Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

AU - Park, Cheon Soo

AU - Ahn, Yongchel

AU - Lee, Dahae

AU - Moon, Sung Won

AU - Kim, Ki Hyun

AU - Yamabe, Noriko

AU - Hwang, Gwi Seo

AU - Jang, Hyuk Jai

AU - Lee, Heesu

AU - Kang, Ki Sung

AU - Lee, Jae Wook

PY - 2015/12/15

Y1 - 2015/12/15

N2 - Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

AB - Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

KW - Anticancer

KW - Apoptosis

KW - Chalcone

KW - HepG2

UR - https://www.scopus.com/pages/publications/84947280056

U2 - 10.1016/j.bmcl.2015.10.093

DO - 10.1016/j.bmcl.2015.10.093

M3 - Article

C2 - 26564263

AN - SCOPUS:84947280056

SN - 0960-894X

VL - 25

SP - 5705

EP - 5707

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Abstract

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Keywords

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