Quantitative analysis of anti-inflammatory activity of orengedokuto: Importance of combination of flavonoids in inhibition of PGE2 production in mouse macrophage-like cell line J774.1

Naohiro Oshima, Yuuji Narukawa, Noriyasu Hada, Fumiyuki Kiuchi

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14 Citations (Scopus)

Abstract

Orengedokuto is a Kampo formula which has been used for removing "heat" and "poison" to treat inflammation, hypertension, gastrointestinal disorders, and liver and cerebrovascular diseases. In this report, we quantitatively analyzed the anti-inflammatory effect of the component crude drugs of orengedokuto and their constituents, using inhibition of prostaglandin E2 (PGE2) production in the murine macrophage-like cell line J774.1. First, we compared PGE2 production inhibitory activities of extracts of combinations of the component crude drugs, which showed that the activity could be ascribed to Scutellaria Root. Next, as baicalin (1), one of the major constituents of Scutellaria Root, did not show any activity, and baicalein (2), the aglycon of 1, showed only weak activity (IC50 92 μM), a hot-water extract of Scutellaria Root was fractionated under the guidance of the activity to give wogonin (3) (IC 50 28 μM), 6-methoxywogonin (4) (IC50 7.2 μM) and oroxylin A (5) (IC50 45 μM) from the most active fraction. However, the activities of these compounds at concentrations equivalent to those in the extract were weaker than that of the extract, and none of these compounds alone could explain the activity of the extract. Therefore, we examined the activity of combinations of compounds 2-5. Comparison of all combinations of the four compounds in a ratio which is the same as in the extract revealed that wogonin (3) had an essential role in the activity, and a combination of baicalein (2) and wogonin (3), together with 6-methoxywogonin (4) or oroxylin A (5), was necessary to show activity equivalent to that of the extract.

Original languageEnglish
Pages (from-to)281-288
Number of pages8
JournalJournal of Natural Medicines
Volume67
Issue number2
DOIs
Publication statusPublished - 2013 Apr

Fingerprint

Scutellaria
Macrophages
Dinoprostone
Flavonoids
Inhibitory Concentration 50
Anti-Inflammatory Agents
Cells
Cell Line
Chemical analysis
Kampo Medicine
Cerebrovascular Disorders
Poisons
Pharmaceutical Preparations
Liver
Liver Diseases
Hot Temperature
Hypertension
Inflammation
Water
wogonin

Keywords

  • Anti-inflammatory
  • Flavonoid
  • Orengedokuto
  • Scutellaria Root
  • Wogonin

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Complementary and alternative medicine

Cite this

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title = "Quantitative analysis of anti-inflammatory activity of orengedokuto: Importance of combination of flavonoids in inhibition of PGE2 production in mouse macrophage-like cell line J774.1",
abstract = "Orengedokuto is a Kampo formula which has been used for removing {"}heat{"} and {"}poison{"} to treat inflammation, hypertension, gastrointestinal disorders, and liver and cerebrovascular diseases. In this report, we quantitatively analyzed the anti-inflammatory effect of the component crude drugs of orengedokuto and their constituents, using inhibition of prostaglandin E2 (PGE2) production in the murine macrophage-like cell line J774.1. First, we compared PGE2 production inhibitory activities of extracts of combinations of the component crude drugs, which showed that the activity could be ascribed to Scutellaria Root. Next, as baicalin (1), one of the major constituents of Scutellaria Root, did not show any activity, and baicalein (2), the aglycon of 1, showed only weak activity (IC50 92 μM), a hot-water extract of Scutellaria Root was fractionated under the guidance of the activity to give wogonin (3) (IC 50 28 μM), 6-methoxywogonin (4) (IC50 7.2 μM) and oroxylin A (5) (IC50 45 μM) from the most active fraction. However, the activities of these compounds at concentrations equivalent to those in the extract were weaker than that of the extract, and none of these compounds alone could explain the activity of the extract. Therefore, we examined the activity of combinations of compounds 2-5. Comparison of all combinations of the four compounds in a ratio which is the same as in the extract revealed that wogonin (3) had an essential role in the activity, and a combination of baicalein (2) and wogonin (3), together with 6-methoxywogonin (4) or oroxylin A (5), was necessary to show activity equivalent to that of the extract.",
keywords = "Anti-inflammatory, Flavonoid, Orengedokuto, Scutellaria Root, Wogonin",
author = "Naohiro Oshima and Yuuji Narukawa and Noriyasu Hada and Fumiyuki Kiuchi",
year = "2013",
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T1 - Quantitative analysis of anti-inflammatory activity of orengedokuto

T2 - Importance of combination of flavonoids in inhibition of PGE2 production in mouse macrophage-like cell line J774.1

AU - Oshima, Naohiro

AU - Narukawa, Yuuji

AU - Hada, Noriyasu

AU - Kiuchi, Fumiyuki

PY - 2013/4

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N2 - Orengedokuto is a Kampo formula which has been used for removing "heat" and "poison" to treat inflammation, hypertension, gastrointestinal disorders, and liver and cerebrovascular diseases. In this report, we quantitatively analyzed the anti-inflammatory effect of the component crude drugs of orengedokuto and their constituents, using inhibition of prostaglandin E2 (PGE2) production in the murine macrophage-like cell line J774.1. First, we compared PGE2 production inhibitory activities of extracts of combinations of the component crude drugs, which showed that the activity could be ascribed to Scutellaria Root. Next, as baicalin (1), one of the major constituents of Scutellaria Root, did not show any activity, and baicalein (2), the aglycon of 1, showed only weak activity (IC50 92 μM), a hot-water extract of Scutellaria Root was fractionated under the guidance of the activity to give wogonin (3) (IC 50 28 μM), 6-methoxywogonin (4) (IC50 7.2 μM) and oroxylin A (5) (IC50 45 μM) from the most active fraction. However, the activities of these compounds at concentrations equivalent to those in the extract were weaker than that of the extract, and none of these compounds alone could explain the activity of the extract. Therefore, we examined the activity of combinations of compounds 2-5. Comparison of all combinations of the four compounds in a ratio which is the same as in the extract revealed that wogonin (3) had an essential role in the activity, and a combination of baicalein (2) and wogonin (3), together with 6-methoxywogonin (4) or oroxylin A (5), was necessary to show activity equivalent to that of the extract.

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