KR101467395B1 - Extracts from sorghum and sorghum by-product including polyphenol compounds and pharmaceutical composition for treating and preventing inflammatory disease comprising the same - Google Patents

Abstract

The present invention relates to an extract containing a polyphenolic compound derived from a water-soluble and a by-product, and a pharmaceutical composition for the prevention and treatment of inflammatory diseases containing the extract as an active ingredient. More particularly, the present invention relates to a polyphenol compound Extracts containing polyphenolic compounds derived from aquatic and marine by-products which can be used as raw materials for food medicines as well as natural anti-inflammatory agents using the same, and an extract containing the same as an active ingredient To a pharmaceutical composition for the prevention and treatment of inflammatory diseases.

Description

TECHNICAL FIELD [0001] The present invention relates to an extract containing a polyphenolic compound derived from a water-soluble and a by-product, and a pharmaceutical composition for preventing and treating an inflammatory disease containing the same as an active ingredient. the same}

The present invention relates to an extract containing a polyphenolic compound derived from water and a by-product which can be applied to natural anti-inflammatory agents and food medicines by separating a polyphenolic compound exhibiting an anti-inflammatory effect from a water extract, and a method for preventing inflammatory diseases And pharmaceutical compositions for therapeutic use.

An inflammatory reaction is a mechanism of restoring or regenerating a damaged tissue as one of biological tissue defense against physical, chemical stimulation or bacterial infection from the outside. Inflammatory mediators such as nitric oxide (NO), prostaglandin E ₂ (PGE ₂ ), and inflammatory cytokines are secreted. NO, an indicator of inflammatory response, is synthesized by NO synthase (NOS) in L-arginine. There are three types of NOS: endothelial NOS, neuronal NOS, and inducible NOS (iNOS). NO production by iNOS plays a pathological role. However, the excessive production of NO by iNOS induced by lipopolysaccharide (LPS) or inflammatory cytokine induces the inflammatory response and causes tissue damage, gene mutation and nerve damage. Cyclooxygenase (COX) is an enzyme that catalyzes the conversion of arachidonic acid into PG. Especially, COX-2 is induced by various stimuli of inflammation, growth factors and cytokines caused by cancer cells. (IL-6) and IL-1, and macrophages secrete these pro-inflammatory cytokines, which mediate a variety of inflammatory responses. The proinflammatory cytokines that increase expression during inflammatory reaction include NO, TNF, interleukin Induce PGE ₂ production.

Korean Patent Publication No. 2011-0085237 discloses a prophylactic and therapeutic agent for inflammatory diseases which inhibits the production of cyclooxygenase-2 dependent prostaglandin D ₂ , which is involved in inflammation and allergic reactions, and inhibits 5-lipoxygenase-dependent leukotriene C ₄ and inhibiting the production of nitric oxide from macrophages as an active ingredient has been proposed. However, a pharmaceutical composition for the prevention and treatment of inflammatory diseases has been proposed, There are disadvantages.

Korean Patent Laid-Open Publication No. 2010-0122543 discloses a water-soluble extract having antimicrobial activity as an environmentally friendly natural substance that inhibits the growth of bacteria and does not cause adverse effects due to human toxicity, residue and accumulation, and a pharmaceutical composition for antibacterial use containing the extract However, there is little information on the anti-inflammatory effect of sorghum.

Meanwhile, Sorghum (Sorghum, Sorghum bicolor L. Moench is a perennial plant of the alopecia plantus and is one of the major grains following rice, barley, wheat and corn, and is a major grain food crop in many parts of the world. And in Asia and Africa as food resources and folk remedies (Ryu et al., 2006, The Korean Journal of Food and Nutrition, 19, 176182). Sorghum is rich in secondary metabolites such as tannins, phenols, anthocyanins, plant sterols, and policosanols, which are known to significantly affect human health (Awika & Rooney, 2004, Phytochemistry, 65, 1199-1221) . Recent studies have shown that antimicrobial activity of sorghum (Choi et al., 2006, Food Chemistry, 103, 130-138), anticancer effect (Kwak et al., 2004, Journal of Korean Society of Food Science Nutrition, 33, 921-929) , And cholesterol lowering effects (Ha et al., 1998, Korean Journal of Food Science and Technology, 30, 224-229) and reported that it could reduce cardiovascular disease (Cho et al., 2000, Journal of the Federation of American Societies for Experimental Biology, 14, A249). Furthermore, sorghum has DPPH radical scavenging activity and has been reported to have an antimutagenic effect. (Kwak et al., 2004, Journal of Korean Society of Food Science Nutrition, 33, 921-929). HMG-CoA reductase inhibitory activity was detected in the methanol extract of Acer. (Ha et al., 1998, Korean Journal of Food Science and Technology, 30, 224-229). However, the anti-inflammatory effect of sorghum has not yet been studied.

The anti-inflammatory drugs developed so far have been focused on the development of anti-inflammatory drugs without side effects since the side effects are not clearly confirmed when they are accumulated in the body as synthetic compounds. For this reason, anti-inflammatory agents using natural substances capable of replacing harmful chemical components have been attracting attention.

As a result of efforts to find out substances which are involved in inflammatory diseases derived from millet and aquatic byproducts in order to solve these problems, the present inventors have completed the present invention by isolating the substances exhibiting antiinflammatory activity from the extracts of the millet and identifying them.

Accordingly, it is an object of the present invention to provide a pharmaceutical composition for preventing and treating inflammatory diseases containing, as an active ingredient, an extract from Aspergillus sp.

It is another object of the present invention to provide a pharmaceutical composition for the prevention and treatment of inflammatory diseases containing as an active ingredient a fraction obtained by separating from the extract.

In order to solve the above problems, the present invention provides a pharmaceutical composition for the prevention and treatment of inflammatory diseases containing an extract of Aspergillus as an active ingredient.

The present invention also relates to a pharmaceutical composition comprising an extract of anhydrous extract comprising at least one polyphenol compound selected from the group consisting of epigenin represented by the following formula (1) and a quercetin compound represented by the following formula (5) A pharmaceutical composition for prevention and treatment of diseases is provided.

[Chemical Formula 1]

[화학식 5]

[Chemical Formula 5]

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According to the present invention, a water extract and a polyphenol compound isolated therefrom inhibit the formation of iNOS or COX-2 involved in an inflammatory reaction and inhibit nitric oxide production from macrophages, thereby being useful for prevention and treatment of inflammatory diseases And can be used as a raw material for food and medicine as well as a natural anti-inflammatory agent using the same.

FIG. 1 is a graph showing the NO inhibitory activity of the extracts of the by-products and the by-products prepared in Example 1 according to the present invention.
FIG. 2 is a graph showing the NO inhibitory activity of the polyphenol compounds isolated from the water and the by-product extracts prepared in Examples 1 and 2 according to the present invention.
FIG. 3 is a photograph showing the effect of TPA irritation mitigation in the mouse ear edema model on the extracts of the water-borne and the by-product extracts prepared in Examples 1 and 2 and fractions separated therefrom according to the present invention.
FIG. 4 is a graph showing the TPA irritation mitigation effect on the water and the by-product extracts prepared in Examples 1 and 2 and fractions separated therefrom according to the present invention.
FIG. 5 is a graph showing inhibitory activities of iNOS on the extracts of water-borne and marine by-products prepared in Examples 1 and 2 and fractions separated therefrom according to the present invention.
FIG. 6 is a graph showing the COX-2 expression inhibitory activity of the extracts of marine and marine by-products prepared in Examples 1 and 2 and fractions separated therefrom according to the present invention.

Hereinafter, the present invention will be described in more detail as an embodiment.

The present invention is characterized by a pharmaceutical composition for the prevention and treatment of inflammatory diseases containing an extract of Aspergillus as an active ingredient.

According to a preferred embodiment of the present invention, the water extract can be obtained by extracting Sorghum biclor (L.) Moench, a by-product or a mixture thereof with an organic solvent. At this time, the above-mentioned species can be classified into three types, namely, golden bug, milo bug, red bug, bug bug, bug bug, mulberry bug, mugwort mug, mugwort mug, small singe mug, longevity mug, red mulberry mug, And water-in-oil emulsions. Most preferably, it is preferable to use gold wire or millet wire. The organic solvent may be at least one selected from the group consisting of alcohol, hexane, ethyl acetate, dimethylformamide, tetrahydrofuran, chloroform, diethyl ether and butanol. The organic solvent is preferably a lower alcohol having 1 to 4 carbon atoms It is good to use.

According to a preferred embodiment of the present invention, the water extract can exhibit NO formation inhibitory activity, wherein the inhibitory concentration of NO generation of the water extract can exhibit a maximal inhibitory activity in the range of 1 to 400 ppm.

According to a preferred embodiment of the present invention, the hydrolyzed extract may exhibit iNOS or COX-2 expression inhibiting activity.

The present invention relates to an inflammatory disease comprising an extract of anhydrous extract comprising at least one polyphenol compound selected from the group consisting of epigenin represented by the following formula (1) and quercetin compound represented by the following formula (5) Characterized by a pharmaceutical composition for prevention and treatment.

[Chemical Formula 1]

[Chemical Formula 5]

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According to a preferred embodiment of the present invention, it is preferable that the fraction is obtained by fractionating the hydrolyzed extract into at least one selected from n-hexane, butanol, ethyl acetate and chloroform. Most preferably, the ethyl acetate fraction and the chloroform fraction obtained by fractionation with ethyl acetate and chloroform are used.

According to a preferred embodiment of the present invention, in the polyphenol compound, epigenin or quercetin may exhibit NO formation inhibitory activity, wherein the NO formation inhibitory activity of the polyphenol compound is such that the NO production inhibitory concentration of the fraction is in the range of 1 to 80 mM Inhibitory activity.

According to a preferred embodiment of the present invention, the fraction may exhibit iNOS or COX-2 expression inhibiting activity.

According to a preferred embodiment of the present invention, the inflammatory disease is selected from the group consisting of inflammatory bowel disease, systemic lupus erythematosus, inflammatory collagen vascular disease, glomerulonephritis, inflammatory skin disease, sarcoidosis, retinitis, gastritis, hepatitis, enteritis, pancreatitis and nephritis Or a combination thereof.

Therefore, as described above, the extract and the polyphenol compound isolated therefrom inhibit the formation of iNOS or COX-2 involved in the inflammatory reaction and inhibit nitric oxide production from macrophages, thereby being useful for the prevention and treatment of inflammatory diseases And can be used as a raw material for food and medicine as well as a natural anti-inflammatory agent using the same.

Hereinafter, the present invention will be described in detail with reference to the following examples, but the present invention is not limited thereto.

Example  1: Extraction, separation and purification of polyphenolic compounds from sorghum, by-products or mixtures thereof

By-products collected in 2010 were crushed to a size of 100 mesh using a crusher. 1 kg of the millet and millet by-product powder obtained from the crusher was placed in an extraction vessel and washed with 80% methanol aqueous solution (3 L) at room temperature for 2 days do. The extracted sample was filtered through a filter paper, and then concentrated under reduced pressure to obtain a cyan-blue extract (325 g).

To the suspension, 1 L of purified water was added, and the mixture was suspended and fractionated in the order of n-hexane, ethyl acetate and butanol to obtain 32 g of n-hexane fraction, 85 g of ethyl acetate fraction, 94 g of butanol fraction and 78 g of water fraction . From the butanol fraction (94 g), a mixed solvent of chloroform: methanol (45: 1 to 1:10 mixture ratio) and methanol were sequentially used as a mobile phase solvent using silica gel column chromatography (600 g, 70 to 230 mesh, Merk) To obtain five fractions (Fr.B1 to Fr.B5).

Fr. B3 fraction (5.6 g) was adsorbed onto silica gel (10 g, 70-230 mesh) and silica gel column chromatography (100 g, 230-400 mesh) was carried out. The mobile phase solvent was chloroform: methanol To obtain a pale yellow precipitate, which was purified to obtain Formula 1 (68 mg). In addition, fractions of Fr.B4 (3.9 g) were adsorbed on silica gel (8 g, 70-230 mesh) and then subjected to silica gel column chromatography (80 g, 230-400 mesh) 40: 1 to 1:10 mixing ratio). A pale yellow precipitate was obtained by using a mixed solvent. The resulting precipitate was purified to obtain Formulas 2 (45 mg) and 3 (52 mg). In addition, silica gel column chromatography (150 g, 230-400 mesh) was performed after adsorbing Fr.B5 (8.5 g) on silica gel (15 g, 70-230 mesh), and mobile phase solvent was chloroform: methanol (30: 1 to 1:20 mixing ratio). A yellowish precipitate was obtained by using a mixed solvent. The yellowish precipitate was purified to obtain Formula 4 (36 mg) and Formula 5 (9 mg).

Silica gel thin layer chromatography (TLC) of the separated polyphenol compounds was performed, and the TLC pattern corresponding thereto was shown in FIG.

Example  2: Structural analysis of polyphenolic compounds isolated from sorghum, sorghum by-products or mixtures thereof

The molecular weight and molecular formula of the compound obtained in Example 1 were determined by HPLC-MS (mass spectrometry). The structure of the compound was determined by nuclear magnetic resonance analysis (Bruker AMX 500) by ¹ H NMR , it was done by analyzing the ¹³ C-NMR, homo koji (HOMO-COSY), HMQC ( 1 H-Detected heteronuclear Multiple-Quantum Coherence), HMBC (Heteronuclear Multiple-Bond Coherence), DEPT (Distortionless Enhancement by Polarization) spectrum.

(4 ', 5,7-trihydroxyflavone; epigenin), 4', 5,7-trihydroxyflavone (4 ', 5,7- , 5,7-Trihydroxyflavylium; epigeninide), Formula 3 is 3 ', 4', 5,7-tetrahydroxyflavylium (ruthenoridine (4), hesperetin 7-rhamnoglucoside (hesperidin), and 5, 3, 3 ', 4', 5, 7-pentahydroxy-2-phenylchroman- 3,3 ', 4', 5,7-pentahydroxy-2-phenylchromen-4-one; quercetin).

The structures of the separated polyphenol compounds are shown in Table 1 below, and the structural characteristics of the respective compounds are as follows.

compound rescue Material name One

4 ', 5,7-trihydroxyflavone: Epigenin 2

4 ', 5,7-trihydroxyflavinium: epigenidin 3

3 ', 4', 5,7-Tedla hydroxyflavinium: ruthelinidine 4

Hesperetin 7-rhamnoglucoside: hesperidin 5

3, 3 ', 4', 5, 7-pentahydroxy-2-phenylchroman-
Quercetin

4 ', 5,7-tetrahydroxyflavone (epigenin)

1) Properties: Light yellow amorphous crystals

2) Molecular weight: 270.24

3) Molecular formula: C ₁₅ H ₁₀ O ₅

^{4) 1 H-NMR (500MHz} , Methanol- d 4) δ 7.87 (2H, d, J = 14.9 Hz), 6.94 (2H, d, J = 14.9 Hz), 6.62 (1H, s), 6.47 (1H, d, J = 3.5 Hz), 6.23 (1H, d, J = 3.5 Hz)

5) ¹³ C-NMR (125 MHz, methanol- d ₄ )? 184.2, 166.8, 166.6, 163.6, 159.9, 151.4, 147.5, 124.1, 120.7, 117.2, 114.6, 105.5, 104.3, 100.6, 95.4,

4 ', 5,7-trihydroxyflavinium (epigenidin)

1) Properties: Light yellow amorphous crystals

2) Molecular weight: 255.24

3) Molecular formula: C ₁₅ H ₁₁ O ₄

^{4) 1 H-NMR (500MHz} , Methanol- d 4) δ 9.09 (1H, d, J = 14.5 Hz), 8.30 (2H, d, J = 14.9 Hz), 8.05 (1H, d, J = 14.5 Hz) , 7.08 (1H, d, J = 14.9 Hz), 6.95 (1H, d, J = 1.2 Hz), 6.66 (1H, d, J = 1.2 Hz)

^{5) 13 C-NMR (125MHz} , Methanol- d 4) δ 173.2, 172.8, 167.7, 160.9, 160.4, 149.9, 133.6, 133.6, 121.7, 118.8, 118.8, 114.2, 100.8, 103.6, 96.5

3 ', 4', 5,7-tetrahydroxyflavinium (ruthelinidine)

1) Properties: Yellow amorphous crystals

2) Molecular weight: 271.24

3) Molecular formula: C ₁₅ H ₁₁ O ₅

^{4) 1 H-NMR (500MHz} , Methanol- d 4) δ 9.05 (1H, d, J = 14.3 Hz), 8.00 (1H, d, J = 14.6 Hz), 7.89 (1H, d, J = 14.0 Hz) , 7.75 (1H, s), 7.04 (1H, d, J = 14.1 Hz), 6.92

^{5) 13 C-NMR (125MHz} , Methanol- d 4) δ 173.2, 172.5, 160.9, 160.4, 156.8, 149.5, 148.7, 125.7, 122.2, 118.2, 116.4, 114.0, 111.1, 103.6, 96.4

Hesperetin 7-rhamoglucoside (hesperidin)

1) Properties: Light yellow amorphous crystals

2) Molecular weight: 612.53

3) Molecular formula: C ₂₇ H ₃₂ O ₁₆

^{4) 1 H-NMR (500MHz} , DMSO- d 6) δ 6.93 (2H, m), 6.13 (2H, m), 5.50 (1H, m), 5.39 (1H, d, J = 8.0 Hz), 5.18 ( 2H, dd, J = 7.2, 7.8 Hz), 4.99 (1H, dd, J = 7.5, 11.9 Hz), 4.69 (1H, dd, J = 5.8, 9.1 Hz), 4.62 (1H, t, J = 9.1 Hz ), 4.50 (2H, m), 3.13-3.45 (7H, O-rhamnoglucoside)

^{5) 13 C-NMR (125MHz} , DMSO- d 6) δ 197.5, 165.3, 163.5, 162.9, 148.4, 146.9, 131.4, 118.4, 114.6, 112.5, 103s.8, 101.1, 99.8, 96.9, 95.8, 78.1, 76.7 , 76.0, 73.5, 72.5, 71.2, 70.7, 70.1, 68.8, 66.1, 56.2, 49.0

3, 3 ', 4', 5, 7-pentahydroxy-2-phenylchromen-4-one (quercetin)

 1) Properties: Light yellow amorphous crystals

2) Molecular weight: 302.3

3) Molecular formula: C ₁₅ H ₁₀ O ₇

^{4) 1 H-NMR (500MHz} , DMSO- d 6) δ 6.17 (1H, d, J = 2.0 Hz, H- 6), 6.39 (1H, d, J = 2.0 Hz H-8), 6.87 (1H, d, J = 8.0 Hz, H-5 '), 7.53 (1H, dd, J = 2.0, 8.0 Hz, H-6'), 7.66 (1H, d, J = 2.0Hz, H- 1H, s, C5-OH)

5) ¹³ C-NMR (125 MHz, DMSO- d ₆ )? 146.9, 135.7,175.7,160.7,98.2,163.9,93.4,156.2,103.0,122.0,115.3,145.0,147.6,115.6,120.0

Experimental Example  1: extracts of water-soluble and water-containing by-products and polyphenol compounds separated therefrom NO  Generation inhibitory effect

In order to confirm the degree of inhibition against various inflammatory diseases of the water and the by-product extracts obtained in Examples 1 and 2 and the polyphenol compounds separated therefrom, they were confirmed using mouse or human macrophages and animal experiments, (IL-1β) and TNF-α (tumor necrosis factor-α) were measured and the expression of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2) , The possibility of the natural pigment as an anti-inflammatory substance was confirmed.

Macrophages (Raw 264.7 cells) were seeded in 96-well plates at 1 × 10 ⁴ cells and cultured for 24 hours. LPS (lipopolysaccharide) was dissolved in 1 / ml and treated with 100 ml of each well. NO (nitric oxide) produced by LPS was measured using an assay kit.

As shown in Table 2, the NO production 50% inhibitory concentrations of the extracts of the water and the by-products were 47.78 and 482.15 ppm, respectively. The NO production 50% inhibitory concentration of the fractions isolated from the water and the by-product extract was 33.88 μM and quercetin were 48.21 μM and the remaining apigeninidin, hesperidin and luteolinidin were not active at 200 μM or more.

Compound No. rescue NO production inhibitory activity
(IC ₅₀ = mM) - Sorghum extract 47.78 ppm - By-product extract 482.15ppm One

33.88 2

200 or more 3

200 or more 4

200 or more 5

48.21

As shown in Table 2, NO produced during the inflammatory reaction by LPS stimulation in macrophages tended to be inhibited by the extracts of marine and by-products, and the suppressive effect was more excellent in the extracts of marine organisms . In addition, it was confirmed that apigenin and quercetin exhibited excellent NO inhibitory activity in the polyphenol compounds separated from the extracts of the water and the by-products of the by-products (see FIGS. 1 and 2).

Experimental Example  2: extracts of millet and sorghum by-products and extracts thereof Fraction  Inflammation relieving effect

As macrophage (or monocyte) cells, mouse macrophage RAW 264.7 (or human macrophage THP-1 cells) was used. RAW 264.7 cells were cultured in Dulbecco's Modified Eagle Medium (Gibco) containing 10% heat inactivated FBS (Gibco) and 5% penicillin-streptomycin (Gibco) and cultured in a thermostat supplied with 5% CO ₂ at 37 ° C Respectively. THP-1 cells were cultured in RPMI 1640 (Gibco) containing 10% heat inactivated FBS (Gibco) and 5% penicillin-streptomycin (Gibco) and cultured in a thermostat supplied with 5% CO ₂ at 37 ° C .

The composition of the mouse inflammation model induced by TPA (phorbol myristate acetate; TPA), which induces inflammation on the extracts of the mite and marl by-products and fractions separated therefrom prepared in Examples 1 and 2, .

Classification Composition Nor normal TPA TPA alone treat group GC5 TPA + gold wax 5 mg / kg GC10 TPA + gold-plated 10 mg / kg GEt1 TPA + golden stool Ethyl acetate fraction extract 1 mg / kg GCh1 TPA + Golden Cherry Chloroform fraction extract 1 mg / kg MC5 TPA + Milo 5 mg / kg MC10 TPA + Milo Protocol 10 mg / kg MEt1 TPA + Milo Acyl Ethyl acetate fraction extract 1 mg / kg MCh1 TPA + Milo Syrup Chloroform fraction extract 1 mg / kg NB 250 TPA + blackberry 250 mg / kg NB 500 TPA + black charcoal 500 mg / kg BB 250 TPA + germanium barley 250 mg / kg BB 500 TPA + sprout barley 500 mg / kg

As shown in FIGS. 3 and 4, the inflammation was alleviated in both the gold-scintillation counting system and the milo-syringae, as shown in the analysis of the anti-inflammatory effect of the extracts of the water and the by-products and the fractions separated therefrom in the mice induced by the inflammation inducing factor TPA. In addition, the thickness and weight of the mouse ear showed that inflammation was alleviated by the water extract.

Experimental Example  3: extracts of millet and sorghum by-products and extracts thereof Fraction  Inflammation Parameter  Protein expression effect

Since the extracts of rumen extracts showed antiinflammatory effects on the mouse ears induced by TPA, the effects of the above-mentioned extracts of the water and the by-products on the expression of COX-2 and iNOS in order to identify the effect of the TPA on the expression of inflammatory mediator proteins The effect of the fractions separated from these fractions was measured by western blot.

After dissolving 10 mg of TPA in 100 ml of acetone, 10 ml of the TPA was applied to the inside of the right ear of each mouse using a pipette, followed by drying to induce inflammation. After 24 hours of induction of inflammation, the thickness of the ear tip was measured using a Bernier caliper. After observing the efficacy, the mice were excised from the cervical vertebra, the ear was excised, and the punch was punched in the same size. The punching samples were lysed and the expression of the proinflammatory proteins COX-2 and iNOS was measured by western blot and shown in FIGS. 5 and 6.

As a result, as shown in FIGS. 5 and 6, the expression of COX-2 and iNOS was increased in the mouse ear induced by TPA than in the mice not inducing inflammation. The expression of COX-2 and iNOS, which were increased by TPA, was effectively suppressed in the mouse ears containing the fractions. The expression of COX-2 and iNOS in TPA was most effectively suppressed in the gold streaks of GEt1 (TPA + golden stool Ethyl acetate fraction extract) and GCH1 (TPA + golden stalk Chloroform fraction extract), and in milo strains MEt1 (TPA + Ethyl acetate fraction extract), and Mch1 (TPA + Milo sorghum Chloroform fraction extract) (see FIGS. 5 and 6). This indicates that the fractions separated from the above-mentioned water-soluble and water-containing by-product extracts have far superior inhibitory activity to the expression of COX-2 and iNOS, which are increased by TPA, than those of the water and water by-product extracts.

Therefore, the water extract and the polyphenol compound isolated therefrom are effective for the prevention and treatment of inflammatory diseases by inhibiting the formation of iNOS or COX-2 involved in the inflammatory reaction and inhibiting the production of nitric oxide from macrophages can confirm.

Claims (14)

delete delete delete delete delete delete delete delete Sorghum bicior (L.) Of Moench A pharmaceutical composition for the prophylaxis and treatment of inflammatory diseases, which comprises as an active ingredient a fraction of the extract of the present invention comprising a polyphenol compound of the quercetin compound represented by the following formula (5) isolated from an extract.
[Chemical Formula 5]

[Claim 11] The pharmaceutical composition according to claim 9, wherein the fraction is obtained by fractionating a water extract of at least one selected from n-hexane, butanol, ethyl acetate and chloroform.
10. The pharmaceutical composition according to claim 9, wherein the polyphenol compound quercetin exhibits NO-inhibiting activity.
12. The pharmaceutical composition for the prevention and treatment of inflammatory diseases according to claim 11, wherein the NO formation inhibitory activity is a fraction in which the NO production inhibitory concentration is 1 to 80 mM.
10. The pharmaceutical composition according to claim 9, wherein the fraction exhibits an iNOS or COX-2 expression inhibiting activity.
14. The method of any one of claims 9 to 13 wherein the inflammatory disease is selected from the group consisting of inflammatory bowel disease, systemic lupus erythematosus, inflammatory collagen vascular disease, glomerulonephritis, inflammatory skin disease, sarcoidosis, retinitis, gastritis, Pancreatitis, and nephritis. ≪ RTI ID = 0.0 > 21. < / RTI >

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