Compositions and methods for treating inflammation and inflammation-related disorders by plectranthus amboinicus extracts

A composition and extract technology, applied in the direction of drug combination, medical raw materials derived from angiosperms, anti-inflammatory agents, etc.

Inactive Publication Date: 2010-10-06
梁启铭
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Other compounds have also been shown to have inhibitory activity

Method used

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  • Compositions and methods for treating inflammation and inflammation-related disorders by plectranthus amboinicus extracts
  • Compositions and methods for treating inflammation and inflammation-related disorders by plectranthus amboinicus extracts
  • Compositions and methods for treating inflammation and inflammation-related disorders by plectranthus amboinicus extracts

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0136] Example 1: Anti-inflammatory activity of PA extract

[0137] The effect of PA on LPS (lipopolysaccharide)-induced expression of 17 cytokines and 5 chemokines is shown in Table 1. Human umbilical vein endothelial (HUVEC) cells were co-incubated with LPS with or without 1 mg / ml PA crude extract. Cytokine expression profiles were determined using Luminex. The results showed that PA crude extract significantly reduced the expression of cytokines IL-6, IL-8, IL-12, MCP-1, and RANTES.

[0138] Table 1. Effect of PA extract on LPS-induced expression

[0139]

[0140]

Embodiment 2

[0141] Example 2: Inhibition of AP-1 binding activity with PA extract

[0142] Since AP-1 activity is involved in inflammatory signaling, the effect of PA crude extract on AP-1 / DNA binding activity was examined. Such as figure 1 As shown, the effect of PA crude extract on the DNA binding activity of the AP-1 transcription factor was determined using an ELISA-based assay. Nuclear extracts prepared from TPA-activated HeLa or K562 cells were used as a source of AP-1 protein. After colocalization with oligonucleotides containing the AP-1 binding site, the AP-1 / DNA complex was detected with an anti-c-Fos antibody complexed with HRP. It was found that the in vitro DNA binding activity of AP-1 was inhibited by PA crude extract, and these effects were dose-dependent.

Embodiment 3

[0143] Example 3: Inhibition of AP-1 Binding Activity with Fraction 10, CHM9102, and Rosmarinic Acid

[0144] The PA crude extract was further fractionated by preparative HPLC using a C18 column. Such as figure 2 As shown, it separates the crude extract of P. chinensis into 16 fractions. Fraction 10 showed an inhibitory effect against AP-1 binding. This fraction was further purified on another C18 column using a solvent gradient from 2% acetonitrile to 90% acetonitrile containing 0.1% trifluoroacetic acid. The main peak is collected, and then its structure is determined by MASS and NMR analysis, such as image 3 shown. These studies lead to structural deduction for the active component CHM9102. Rosmarinic acid (an analog of CHM9102) was also tested for AP-1 inhibitory activity.

[0145] Although the methods and reagents have been described in terms of what are presently considered to be the most practical and preferred implementations, it should be understood that the...

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Abstract

The crude extract of Plectranthus Amboinicus (PA) has anti-inflammatory effects and can inhibit AP-1 binding in vitro. The incubation with PA crude extract resulted in significant inhibition of the LPS-induced expression of IL-6, IL-12, MCP- 1, and RANTES in HUVEC cells. After the crude extract was further fractionated using preparative HPLC, fraction 8, 9, 10 and 11 were identified to inhibit the AP-1 binding activity. The active component of fraction 8 is Mena 987; fraction 9 is Mena 998; fraction 10 is Mena 9102; and fraction 11 is rosmarinic acid and the synthestic rosmarinic acid analogues. Other compounds showed inhibitory activities as well. These compounds have inhibitory effects on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression or activities of AP-1 are involved.

Description

[0001] Related applications [0002] This disclosure is incorporated by reference and claims Paris Convention priority in US Provisional Application No. 60 / 973,164 (filed September 17, 2007). Background technique [0003] Plectranthus amboinicus (PA) is a traditional Chinese medicine used for cough, sore throat, and nasal congestion, but it can also be used for many other conditions, such as infection, rheumatism, and flatulence. Although the chemical composition of PA has been extensively studied, its active ingredient for inhibiting AP-1 binding has not been reported. [0004] Transcription factor activator protein-1 (AP-1) regulates various expression of genes. In mammalian cells, the AP-1 complex is mainly formed by members of Fos and Jun-related proteins. The AP-1 protein contains a characteristic amino acid sequence known as the bZIP domain. This protein domain has two parts; it contains a helical configuration and serves as the interface for dimerization. The inter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/53A61K36/18A61K31/337
CPCA61K31/235A61K31/215A61K36/53A61P29/00
Inventor 翁启惠郑义循余惠敏郑婷仁吴宗益方俊民
Owner 梁启铭
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