Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK

Ya ming Xu; Jeffrey A. Smith; Deborah A. Lannigan; Sidney M. Hecht

doi:10.1016/j.bmc.2006.01.066

Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK

Ya ming Xu, Jeffrey A. Smith, Deborah A. Lannigan, Sidney M. Hecht

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

23 Scopus citations

Abstract

A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2″,4″-O-diacetyl-α-l-rhamnopyranoside) (1), kaempferol 3-O-(3″,4″-O-diacetyl-α-l-rhamnopyranoside) (2), and kaempferol-3-O-(4″-O-acetyl-α-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC₅₀ value of 89 nM.

Original language	English (US)
Pages (from-to)	3974-3977
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	11
DOIs	https://doi.org/10.1016/j.bmc.2006.01.066
State	Published - Jun 1 2006
Externally published	Yes

Keywords

Acetylated kaempferol-3-O-α-l-rhamnopyranosides
Apocynaceae
Forsteronia refracta
RSK inhibitors

ASJC Scopus subject areas

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

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10.1016/j.bmc.2006.01.066

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@article{4d97e2122f304bcb91a0b600e7d81396,

title = "Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK",

abstract = "A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2″,4″-O-diacetyl-α-l-rhamnopyranoside) (1), kaempferol 3-O-(3″,4″-O-diacetyl-α-l-rhamnopyranoside) (2), and kaempferol-3-O-(4″-O-acetyl-α-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC50 value of 89 nM.",

keywords = "Acetylated kaempferol-3-O-α-l-rhamnopyranosides, Apocynaceae, Forsteronia refracta, RSK inhibitors",

author = "Xu, {Ya ming} and Smith, {Jeffrey A.} and Lannigan, {Deborah A.} and Hecht, {Sidney M.}",

note = "Funding Information: This work was supported by NIH research Grants CA50771 and CA95335 awarded by the National Cancer Institute.",

year = "2006",

month = jun,

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doi = "10.1016/j.bmc.2006.01.066",

language = "English (US)",

volume = "14",

pages = "3974--3977",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

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T1 - Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK

AU - Xu, Ya ming

AU - Smith, Jeffrey A.

AU - Lannigan, Deborah A.

AU - Hecht, Sidney M.

N1 - Funding Information: This work was supported by NIH research Grants CA50771 and CA95335 awarded by the National Cancer Institute.

PY - 2006/6/1

Y1 - 2006/6/1

N2 - A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2″,4″-O-diacetyl-α-l-rhamnopyranoside) (1), kaempferol 3-O-(3″,4″-O-diacetyl-α-l-rhamnopyranoside) (2), and kaempferol-3-O-(4″-O-acetyl-α-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC50 value of 89 nM.

AB - A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2″,4″-O-diacetyl-α-l-rhamnopyranoside) (1), kaempferol 3-O-(3″,4″-O-diacetyl-α-l-rhamnopyranoside) (2), and kaempferol-3-O-(4″-O-acetyl-α-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC50 value of 89 nM.

KW - Acetylated kaempferol-3-O-α-l-rhamnopyranosides

KW - Apocynaceae

KW - Forsteronia refracta

KW - RSK inhibitors

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AN - SCOPUS:33646057985

SN - 0968-0896

VL - 14

SP - 3974

EP - 3977

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 11

ER -

Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK

Abstract

Keywords

ASJC Scopus subject areas

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