New prenylated flavanones from erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity

Long Cui; Hyun Sun Lee; Derek Tantoh Ndinteh; Joseph Tanyi Mbafor; Young Ho Kim; Thi Van Thu Le; Phi Hung Nguyen; Won Keun Oh

doi:10.1055/s-0029-1240682

New prenylated flavanones from erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity

Long Cui, Hyun Sun Lee, Derek Tantoh Ndinteh, Joseph Tanyi Mbafor, Young Ho Kim, Thi Van Thu Le, Phi Hung Nguyen, Won Keun Oh

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

29 Citations (Scopus)

Abstract

As the insulin and leptin signaling pathway can be regulated by PTP1B, it has been suggested that compounds that reduce PTP1B activity or expression levels can be used for treating type 2 diabetes and obesity. In the course of our screening efforts on new PTP1B inhibitors, six new flavanones (16) with dihydrofuran moiety and two known flavanones (7 and 8) were isolated from the stem bark of Erythrina abyssinica (Leguminosae). Their structures were elucidated on the basis of spectroscopic (including UV, CD, MS, 1D, and 2DNMR) and physicochemical analyses. With the exception of 3 and 5, the compounds inhibited PTP1B activity in an in vitro assay with IC₅₀ values ranging from 15.2±1.2 to 19.6±2.3μM, whereas RK-682 as a positive control displayed an IC₅₀ value of 4.7±0.5μM.

Original language	English
Pages (from-to)	713-718
Number of pages	6
Journal	Planta Medica
Volume	76
Issue number	7
DOIs	https://doi.org/10.1055/s-0029-1240682
Publication status	Published - 2010
Externally published	Yes

Keywords

Diabetes
Dihydrofuranoflavanones
Erythrina abyssinica
Leguminosae
Protein tyrosine phosphatase 1B

ASJC Scopus subject areas

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and Alternative Medicine
Organic Chemistry

UN SDGs

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

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10.1055/s-0029-1240682

Cite this

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title = "New prenylated flavanones from erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity",

abstract = "As the insulin and leptin signaling pathway can be regulated by PTP1B, it has been suggested that compounds that reduce PTP1B activity or expression levels can be used for treating type 2 diabetes and obesity. In the course of our screening efforts on new PTP1B inhibitors, six new flavanones (16) with dihydrofuran moiety and two known flavanones (7 and 8) were isolated from the stem bark of Erythrina abyssinica (Leguminosae). Their structures were elucidated on the basis of spectroscopic (including UV, CD, MS, 1D, and 2DNMR) and physicochemical analyses. With the exception of 3 and 5, the compounds inhibited PTP1B activity in an in vitro assay with IC50 values ranging from 15.2±1.2 to 19.6±2.3μM, whereas RK-682 as a positive control displayed an IC50 value of 4.7±0.5μM.",

keywords = "Diabetes, Dihydrofuranoflavanones, Erythrina abyssinica, Leguminosae, Protein tyrosine phosphatase 1B",

author = "Long Cui and Lee, {Hyun Sun} and Ndinteh, {Derek Tantoh} and Mbafor, {Joseph Tanyi} and Kim, {Young Ho} and Le, {Thi Van Thu} and Nguyen, {Phi Hung} and Oh, {Won Keun}",

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doi = "10.1055/s-0029-1240682",

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T1 - New prenylated flavanones from erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity

AU - Cui, Long

AU - Lee, Hyun Sun

AU - Ndinteh, Derek Tantoh

AU - Mbafor, Joseph Tanyi

AU - Kim, Young Ho

AU - Le, Thi Van Thu

AU - Nguyen, Phi Hung

AU - Oh, Won Keun

PY - 2010

Y1 - 2010

N2 - As the insulin and leptin signaling pathway can be regulated by PTP1B, it has been suggested that compounds that reduce PTP1B activity or expression levels can be used for treating type 2 diabetes and obesity. In the course of our screening efforts on new PTP1B inhibitors, six new flavanones (16) with dihydrofuran moiety and two known flavanones (7 and 8) were isolated from the stem bark of Erythrina abyssinica (Leguminosae). Their structures were elucidated on the basis of spectroscopic (including UV, CD, MS, 1D, and 2DNMR) and physicochemical analyses. With the exception of 3 and 5, the compounds inhibited PTP1B activity in an in vitro assay with IC50 values ranging from 15.2±1.2 to 19.6±2.3μM, whereas RK-682 as a positive control displayed an IC50 value of 4.7±0.5μM.

AB - As the insulin and leptin signaling pathway can be regulated by PTP1B, it has been suggested that compounds that reduce PTP1B activity or expression levels can be used for treating type 2 diabetes and obesity. In the course of our screening efforts on new PTP1B inhibitors, six new flavanones (16) with dihydrofuran moiety and two known flavanones (7 and 8) were isolated from the stem bark of Erythrina abyssinica (Leguminosae). Their structures were elucidated on the basis of spectroscopic (including UV, CD, MS, 1D, and 2DNMR) and physicochemical analyses. With the exception of 3 and 5, the compounds inhibited PTP1B activity in an in vitro assay with IC50 values ranging from 15.2±1.2 to 19.6±2.3μM, whereas RK-682 as a positive control displayed an IC50 value of 4.7±0.5μM.

KW - Diabetes

KW - Dihydrofuranoflavanones

KW - Erythrina abyssinica

KW - Leguminosae

KW - Protein tyrosine phosphatase 1B

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DO - 10.1055/s-0029-1240682

M3 - Article

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SN - 0032-0943

VL - 76

SP - 713

EP - 718

JO - Planta Medica

JF - Planta Medica

IS - 7

ER -

New prenylated flavanones from erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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