Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines

Shiming Li; Min Hsiung Pan; Ching Shu Lai; Chih Yu Lo; Slavik Dushenkov; Chi Tang Ho

doi:10.1016/j.bmc.2007.03.021

Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines

Shiming Li, Min Hsiung Pan, Ching Shu Lai, Chih Yu Lo, Slavik Dushenkov, Chi Tang Ho

School of Environmental and Biological Sciences, Food Science

Rutgers, The State University

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

136 Scopus citations

Abstract

Fifteen polymethoxyflavones (PMFs) and hydroxylated PMFs were isolated from sweet orange (Citrus sinensis) peel extract and synthesized to investigate their biological activity. All obtained compounds were tested in HL-60 cancer cell proliferation and apoptosis induction assays. While some PMFs and hydroxylated PMFs had moderate anti-carcinogenic activities, 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone and 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.

Original language	American English
Pages (from-to)	3381-3389
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	15
Issue number	10
DOIs	https://doi.org/10.1016/j.bmc.2007.03.021
State	Published - May 15 2007

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Keywords

5-Demethylnobiletin
5-Hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone
HL-60 cell lines
PMF synthesis

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10.1016/j.bmc.2007.03.021

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title = "Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines",

abstract = "Fifteen polymethoxyflavones (PMFs) and hydroxylated PMFs were isolated from sweet orange (Citrus sinensis) peel extract and synthesized to investigate their biological activity. All obtained compounds were tested in HL-60 cancer cell proliferation and apoptosis induction assays. While some PMFs and hydroxylated PMFs had moderate anti-carcinogenic activities, 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone and 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.",

keywords = "5-Demethylnobiletin, 5-Hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone, HL-60 cell lines, PMF synthesis",

author = "Shiming Li and Pan, \{Min Hsiung\} and Lai, \{Ching Shu\} and Lo, \{Chih Yu\} and Slavik Dushenkov and Ho, \{Chi Tang\}",

note = "Funding Information: The authors thank Mr. Ted Lambros of Hoffmann-La Roche Inc. for his assistance in the separation of PMFs. This work was partially supported by a grant from the National Science Council of Taiwan (NSC 95-2313-B-022-005 MY3 to M.H.P.).",

year = "2007",

month = may,

day = "15",

doi = "10.1016/j.bmc.2007.03.021",

language = "American English",

volume = "15",

pages = "3381--3389",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

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T1 - Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines

AU - Li, Shiming

AU - Pan, Min Hsiung

AU - Lai, Ching Shu

AU - Lo, Chih Yu

AU - Dushenkov, Slavik

AU - Ho, Chi Tang

N1 - Funding Information: The authors thank Mr. Ted Lambros of Hoffmann-La Roche Inc. for his assistance in the separation of PMFs. This work was partially supported by a grant from the National Science Council of Taiwan (NSC 95-2313-B-022-005 MY3 to M.H.P.).

PY - 2007/5/15

Y1 - 2007/5/15

N2 - Fifteen polymethoxyflavones (PMFs) and hydroxylated PMFs were isolated from sweet orange (Citrus sinensis) peel extract and synthesized to investigate their biological activity. All obtained compounds were tested in HL-60 cancer cell proliferation and apoptosis induction assays. While some PMFs and hydroxylated PMFs had moderate anti-carcinogenic activities, 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone and 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.

AB - Fifteen polymethoxyflavones (PMFs) and hydroxylated PMFs were isolated from sweet orange (Citrus sinensis) peel extract and synthesized to investigate their biological activity. All obtained compounds were tested in HL-60 cancer cell proliferation and apoptosis induction assays. While some PMFs and hydroxylated PMFs had moderate anti-carcinogenic activities, 5-hydroxy-6,7,8,3′,4′-pentamethoxyflavone and 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.

KW - 5-Demethylnobiletin

KW - 5-Hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone

KW - HL-60 cell lines

KW - PMF synthesis

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U2 - 10.1016/j.bmc.2007.03.021

DO - 10.1016/j.bmc.2007.03.021

M3 - Article

C2 - 17391969

SN - 0968-0896

VL - 15

SP - 3381

EP - 3389

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 10

ER -

Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines

Abstract

ASJC Scopus subject areas

Keywords

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