SIRT1 inhibitory diterpenoids from the Vietnamese medicinal plant Croton tonkinensis

Trong Tuan Dao; Thi Van Le; Phi Hung Nguyen; Phuong Thien Thuong; Pham Thi Minh; Eun-Rhan Woo; Kwang Youl Lee; Won Keun Oh

doi:10.1055/s-0029-1240863

SIRT1 inhibitory diterpenoids from the Vietnamese medicinal plant Croton tonkinensis

Trong Tuan Dao, Thi Van Le, Phi Hung Nguyen, Phuong Thien Thuong, Pham Thi Minh, Eun-Rhan Woo, Kwang Youl Lee, Won Keun Oh

18 Citations (Scopus)

Abstract

Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of Croton tonkinensis resulted in the isolation of a new ent-kaurane diterpenoid (1) along with 11 known compounds (212). The structure of the new compound 1 was determined to be ent-11α-acetoxy-7β-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 69, 11, and 12 exhibited SIRT1 inhibitory activity in an in vitro assay, with IC₅₀ values ranging from 16.08±0.11 to 44.34±2.32μ M. This is the first report showing the potential of ent-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.

Original language	English
Journal	Planta Medica
Volume	76
Issue number	10
Pages (from-to)	1011-4
Number of pages	4
ISSN	0032-0943
DOIs	https://doi.org/10.1055/s-0029-1240863
Publication status	Published - Jul 2010

Keywords

Croton
Diterpenes, Kaurane
Enzyme Inhibitors
Humans
Molecular Structure
Plant Extracts
Plant Leaves
Sirtuin 1
Letter
Research Support, Non-U.S. Gov't

UN SDGs

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

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10.1055/s-0029-1240863

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title = "SIRT1 inhibitory diterpenoids from the Vietnamese medicinal plant Croton tonkinensis",

abstract = "Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of Croton tonkinensis resulted in the isolation of a new ent-kaurane diterpenoid (1) along with 11 known compounds (212). The structure of the new compound 1 was determined to be ent-11α-acetoxy-7β-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 69, 11, and 12 exhibited SIRT1 inhibitory activity in an in vitro assay, with IC50 values ranging from 16.08±0.11 to 44.34±2.32μ M. This is the first report showing the potential of ent-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.",

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AU - Dao, Trong Tuan

AU - Le, Thi Van

AU - Nguyen, Phi Hung

AU - Thuong, Phuong Thien

AU - Minh, Pham Thi

AU - Woo, Eun-Rhan

AU - Lee, Kwang Youl

AU - Oh, Won Keun

N1 - Georg Thieme Verlag KG Stuttgart.New York.

PY - 2010/7

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N2 - Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of Croton tonkinensis resulted in the isolation of a new ent-kaurane diterpenoid (1) along with 11 known compounds (212). The structure of the new compound 1 was determined to be ent-11α-acetoxy-7β-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 69, 11, and 12 exhibited SIRT1 inhibitory activity in an in vitro assay, with IC50 values ranging from 16.08±0.11 to 44.34±2.32μ M. This is the first report showing the potential of ent-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.

AB - Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of Croton tonkinensis resulted in the isolation of a new ent-kaurane diterpenoid (1) along with 11 known compounds (212). The structure of the new compound 1 was determined to be ent-11α-acetoxy-7β-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 69, 11, and 12 exhibited SIRT1 inhibitory activity in an in vitro assay, with IC50 values ranging from 16.08±0.11 to 44.34±2.32μ M. This is the first report showing the potential of ent-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.

KW - Croton

KW - Diterpenes, Kaurane

KW - Enzyme Inhibitors

KW - Humans

KW - Molecular Structure

KW - Plant Extracts

KW - Plant Leaves

KW - Sirtuin 1

KW - Letter

KW - Research Support, Non-U.S. Gov't

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JO - Planta Medica

JF - Planta Medica

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ER -

SIRT1 inhibitory diterpenoids from the Vietnamese medicinal plant Croton tonkinensis

Abstract

Keywords

UN SDGs

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