Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β

Jing Zhen Deng; Shelley R. Starck; Sidney M. Hecht

doi:10.1016/S0968-0896(99)00276-X

Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β

Jing Zhen Deng, Shelley R. Starck, Sidney M. Hecht

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

31 Scopus citations

Abstract

In a survey of crude plant extracts for DNA polymerase β inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase β. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase β inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC₅₀ values ranging from 7.5 to 16 μM in the presence of bovine serum albumin (BSA) and 2.6-5.8 μM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo. (C) 2000 Elsevier Science Ltd.

Original language	English (US)
Pages (from-to)	247-250
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry
Volume	8
Issue number	1
DOIs	https://doi.org/10.1016/S0968-0896(99)00276-X
State	Published - Jan 1 2000
Externally published	Yes

Keywords

Chemotherapy
Enzyme inhibitors
Nucleic acids
Terpenes and terpenoids

ASJC Scopus subject areas

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

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10.1016/S0968-0896(99)00276-X

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title = "Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β",

abstract = "In a survey of crude plant extracts for DNA polymerase β inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase β. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase β inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC50 values ranging from 7.5 to 16 μM in the presence of bovine serum albumin (BSA) and 2.6-5.8 μM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo. (C) 2000 Elsevier Science Ltd.",

keywords = "Chemotherapy, Enzyme inhibitors, Nucleic acids, Terpenes and terpenoids",

author = "Deng, {Jing Zhen} and Starck, {Shelley R.} and Hecht, {Sidney M.}",

note = "Funding Information: We thank Dr. Xiangyang Wang and Hongge Wang for the DNA polymerase β preparation employed in this work, and Professor Shou-Xun Zhao, China Pharmaceutical University, Nanjing, China, for the gifts of oleanolic acid and ursolic acid. This work was supported by Research Grant CA50771 from the National Cancer Institute. ",

year = "2000",

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doi = "10.1016/S0968-0896(99)00276-X",

language = "English (US)",

volume = "8",

pages = "247--250",

journal = "Bioorganic and Medicinal Chemistry",

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TY - JOUR

T1 - Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β

AU - Deng, Jing Zhen

AU - Starck, Shelley R.

AU - Hecht, Sidney M.

N1 - Funding Information: We thank Dr. Xiangyang Wang and Hongge Wang for the DNA polymerase β preparation employed in this work, and Professor Shou-Xun Zhao, China Pharmaceutical University, Nanjing, China, for the gifts of oleanolic acid and ursolic acid. This work was supported by Research Grant CA50771 from the National Cancer Institute.

PY - 2000/1/1

Y1 - 2000/1/1

N2 - In a survey of crude plant extracts for DNA polymerase β inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase β. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase β inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC50 values ranging from 7.5 to 16 μM in the presence of bovine serum albumin (BSA) and 2.6-5.8 μM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo. (C) 2000 Elsevier Science Ltd.

AB - In a survey of crude plant extracts for DNA polymerase β inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase β. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase β inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC50 values ranging from 7.5 to 16 μM in the presence of bovine serum albumin (BSA) and 2.6-5.8 μM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo. (C) 2000 Elsevier Science Ltd.

KW - Chemotherapy

KW - Enzyme inhibitors

KW - Nucleic acids

KW - Terpenes and terpenoids

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U2 - 10.1016/S0968-0896(99)00276-X

DO - 10.1016/S0968-0896(99)00276-X

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AN - SCOPUS:0034100291

SN - 0968-0896

VL - 8

SP - 247

EP - 250

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 1

ER -

Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β

Abstract

Keywords

ASJC Scopus subject areas

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