Method for producing pigment complex of bisnaphthazarin

FIELD: medicine.

SUBSTANCE: method for producing a pigment complex of bisnaphthazarin for preventing inflammatory diseases, involving demineralising commercial sea urchins' crusts and needles in an organic acid solution, separating organic acid salts and protein, applying pigment solution on a chromatographic column, washing the column with diluted mineral acid and distilled water, eluting the pigment complex, combining fractions containing the pigments, removing ethanol, lyophilising concentrate in the certain environment. The complex of pigments bisnaphthazarins for preventing inflammatory diseases.

EFFECT: complex of pigments prepared by the above method is effective for preventing the inflammatory diseases.

3 cl, 2 dwg, 2 tbl, 4 ex

 

The invention relates to the technology of processing of natural objects and relates to a method of producing a pigment complex of benefciaries enriched ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene) from wastes of commercial sea urchin Strongylocentrotus droebachiensis.

Known for more than 1500 quinones found in nature, including 45 found in the family of Echinodermata, including sea urchins.

Shell and needle sea urchin are a byproduct of obtaining edible gonads and are calcareous education. The main valuable minor components of shells and needles sea urchins are give color pigments polyhydroxyalkanoates series - echinochrome a and spinorama exhibiting antioxidant properties [Lebedev AV, Ivanova MV, Levitsky DO. Iron chelators and free radical scavengers in naturally occurring polyhy-droxylated 1,4-naphthoquinones // Hemoglobin, 2008. - 32(1-2). - P. 165-179; Kuwahara R, Hatate H, Yuki T, et al. Antioxidant property of polyhydroxylated naphthoquinone pigments from shells of purple sea urchin Anthocidaris crassispina // LWT. - Food Science and Technology, 2009. - 42. - P. 1296-1300].

It is established that polyhydroxyalkanoate pigments shells and needles sea urchins (naphazoline, SYN. naphthoquinones, spinorama) unlike endogenous antioxidants, such as vitamin E and ubiquinone, is able to neutralize the action of the main proponents of non-enzymatic oxidation of membrane lipids - cations of iron, nakaplivalos�HSA in the area of ischemic tissue damage [R. Kuwahara, Hatate H., Yuki T. et al. Antioxidant property of polyhydroxylated naphthoquinone pigments from shells of purple sea urchin Anthocidaris crassispina // LWT. - Food Science and Technology, 2009, Vol.42, P. 1296-1300]. Such features of the mechanism of action allocate naphazoline of a number of known bioantioxidants and open up prospects for the creation on their basis of drugs of new generation.

Known natural polyhydroxyalkane - echinochrome A, possess antiischemic and protivojinfectini activity [Cardioprotective effect of antioxidant) in cardiology and cardiac clinic / S. A. Afanasiev et - Tomsk: STT, 2012. - 150 p.].

Known drug) used to treat inflammatory diseases of the retina and cornea of the eye, representing 0.02% of the isotonic solution of di - and trinatrium salts pigment from the group of spinorama - echinochrome A [Pat. EN 2134107 C1, publ. 10.08.1999].

Among polyhydroxyalkanoic the pigments bikinni and higher oligomers of quinones are a unique group of natural compounds that possess diverse biological activity.

A method of producing a monomer quinone - 2,3,6,7-tetrahydroquinazoline (spinorama E), where the raw materials used waste recycling commercial black sea urchin S. nudus, which was washed with water, degreased with 96% ethanol, then extracted with techcrete% ethyl alcohol with addition of phosphoric acid (pH 3.0-3.5) in the ratio raw:extractant 1,0:(1,0-1,2) within 12-24 hours. The resulting extract was passed through a column with chitosan, the column was washed with 96% ethanol, and then eluted pigments 96% ethyl alcohol with addition of hydrochloric acid (pH 2-4). Next, the eluate is passed through a column of polychrome-1, the column was washed with distilled water, then eluted the desired product 40-50% aqueous solution of ethanol, the solvent is distilled off in vacuo, the aqueous residue lyophilized. Then spirogram E sublimit at 195-200°C and recrystallized from ethanol [Pat. EN 2411939 C1, publ. 20.02.2011].

The disadvantage of this method is a multistage, high consumption of ethanol, the use of inorganic acids requiring special handling waste.

Beinoni of gray sea urchin S. intermedius were first allocated N. To. Utkina et al. [Utkina NK, Shchedrin AR, Maksimov OB. A new binaphthoquinone from Strongylocentrotus intermedius // Khimiya Prirodnykh Soedinenii, 1976, No. 4, pp.439-441]. In 1978, these compounds were also detected in the green sea urchin S. droebachiensis [Kol'tsova EA, Denisenko VA, Maksimov OB. Quinoid pigments of Echinodermata V. Pigments of the sea urchin Strongylocentrotus droebachiensis // Khimiya Prirodnykh Soedinenii, 1978, No. 4, pp.438-441].

In experimental preclinical studies conducted on mice, found that the complex polyhydroxyalkanoate pigments and minerals from the shells of sea urchins reduces the concentration of glucose in the blood stimulates Synthe� of liver phospholipids and exhibits antioxidant activity [Kovaleva, MA Ivanova SA, Makarova MN, etc. the Impact of the integrated product from the shells of sea urchins on glucose concentration and parameters of oxidative stress in models of diabetes mellitus type II // Experimental and clinical pharmacology, 2013, Vol. 76, No. 8, Pp. 27-30].

Known agent containing as an active ingredient a biologically active complex derived from the carapace and needles of green sea urchins Strongylocentrotus droebachiensis, containing from 0.02% to 10% pigment complex containing spinorama b and D, as well as the dimeric polyhydroxyalkane and from 7.5% to 20% of the mineral component of the shell of sea urchins (calcium, magnesium, phosphorus, sodium, potassium) in the form of water soluble salts, for local application in the form of eye drops, nasal drops and spray, providing anti-inflammatory and antiallergic action (Pat. EN. 2488402 C1, publ. 27.07.2013). It was found that binationale pigments from the carapace of green sea urchins possess antiradical activity against DPPH free radical-radical, which is higher than that of Monomeric echinochrome A [Pozharitskaya ON, Ivanova SA, Shikov AN, Makarov VG. Evaluation of free radical-scavenging activity of sea urchin pigments using HPTLC with post-chromatographic derivatization // Chromatographia, 2013. Vol.76. P. 1353-1358].

The use of beginnow in medicine is hampered by a low content in natural sources, complexity and low yields when used�esewani synthesis [V. F. Anufriev Hydroxylated naphazoline and [2,3-B]pranoprofen. Synthesis and reactivity. - Author. Dis.... DSC - Vladivostok, 2000. - 51 p.].

The known method of laboratory receipt of spinorama of sea urchins Strongylocentrotus droebachiensis by dissolving needles in concentrated hydrochloric acid, filtration, extraction with diethyl ether, washing with NaCl solution and drying. Next, the resulting residue was dissolved in ethanol and separated into two fractions by thin-layer chromatography on plates Kieselgel 60 F 254, impregnated with oxalic acid, in the system chloroform-methanol-acetic acid-water(5/1.1/0.5/0.2), eluted with methanol and then analyzed by HPLC [Shikov AN, Ossipov VI, Martiskainen O. et al. The offline combination of thin-layer chromatography and high-performance liquid chromatography with diode array detection and micrOTOF-Q mass spectrometry for the separation and indentification of spinochromes from sea urchin (Strongylocentrotus droebachiensis) shells // J Chromatogr A, 2011, Vol.1218, P. 9111-9114].

However, the known method is by laboratory analysis. Unattaching were selected as two of only fractions by thin-layer chromatography for the purpose of identification. Get this way the pigment complex in an amount sufficient to confirm its activity, is not possible.

Closest to the claimed method is a method of recycling the shells of sea urchins [Pat. EN 2441661 C1, �publ. 10.02.2012], namely that the shells with needles of sea urchins washed, dried, crushed, demineralized weak organic acid, centrifuged, salt of organic acid is precipitated by adding an organic solvent miscible with water, filtered off, the filtrate was concentrated, neutralized, concentrated under vacuum, freeze dried antioxidant pigment complex pererastayut organic solvent.

However, this method does not provide a set of individual pigments.

Preparative chromatography has attracted particular attention as a method for the isolation and purification of individual compounds in the pharmaceutical and biotechnology industry and in other industries. theoretical basis of the method set out in article [Seidel-Morgenstern A. preparative gradient chromatography // ROS. Chem. J., 2003, vol. XLVII, No. 1, Pp. 80-89].

However, the specific implementation methods of separation of benefciaries this article is not described.

Methods of obtaining pigments of benefciaries enriched ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene), from wastes of fishing sea urchins Strongylocentrotus droebachiensis available in patent and other scientific and technical literature is not found.

Sea urchin species Strongylocentrotus droebachiensis are industrial�charger. After extraction of eggs shells with needles fall to waste. However, they can serve as a source of biologically active substances - benefciaries.

Object of the invention is to provide a method for obtaining pigments of benefciaries enriched ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene) waste from industrial processing of sea urchins (shells and needles of sea urchins Strongylocentrotus droebachiensis) and receive from it the amount of purified benefciaries.

The technical result provided by the invention, is to expand the spectrum of biologically active substances derived from industrial waste processing sea urchins.

As a result of implementation of the invention receive the purified complex of benefciaries that can serve as the basis for the development of new drugs or SUPPLEMENTS that reduce the risk of inflammatory and related diseases.

The essence of the proposed method is as follows.

Shells with needles commercial green sea urchin, remaining after extraction of caviar, fresh or defrosted, washed with water to remove mechanical impurities and residues of the innards. The crushed shells of sea urchins subjected to a demineralization solution of organic acid at a temperature of 40-90°C until complete decomposition of the carbonate skeleton of hedgehogs.

Semi�enny aqueous acid extraction the mixture was filtered to remove undissolved residues of raw, if necessary, centrifuge to remove microparticles. To the resulting supernatant (aqueous-acid extract of sea urchin pigments) was added an excess of an organic solvent, miscible with water, for example: ethyl alcohol, acetone, acetonitrile. The precipitate was salts of organic acids and protein are separated. The resulting solution was colored compounds is applied to a chromatographic column with cation exchange resin and the adsorbed components were washed off impurities with a weak solution of mineral acid and distilled water. Elution of the pigment complexes with the cation exchange resin is carried out stepwise gradient of ethanol. Fractions containing pigments, pooled, ethanol is removed concentrated in vacuo. Concentrate liofilizat. Get dark red lyophilic powder, which is a complex of pigments benefciaries shell and needles sea urchins, purified from proteins, salts and minerals. The yield is 0.1-0.2% by weight of the feedstock.

Common features in the prototype method and the present method are:

- raw sea urchin;

- demineralization of the shell with an organic acid solution;

- deposition of organic acid salts.

The distinctive features in the prototype method and the present method are:

- separation of protein by excess'or�anceschi solvent, miscible with water;

- the application of the mortar pigments chromatography on a column of cation exchange resin, sequential rinsing of the column with a weak solution of mineral acid and distilled water;

- pigment elution of the complex with a cation exchanger step gradient of ethanol, concentrating under vacuum and liofilizirovanny.

The invention is illustrated by the following examples.

EXAMPLE 1. 100 g of washed and crushed shells with needles sea urchins demineralized 500 ml of 50% aqueous solution of lactic acid at 80°C. the resulting solution was centrifuged to remove undissolved small particles. To the supernatant poured 1200 ml of 95% ethanol, stirred, solution, left in the cold (2-8°C) for precipitation of calcium lactate and protein. The precipitate was filtered off. The resulting filtrate is passed through a chromatographic column filled with cation exchange resin type KU-2-8 adsorbed components were washed off impurities with a weak solution of mineral acid and distilled water. Elution of the pigment complex with a cation exchanger is carried out stepwise gradient of ethanol. Fractions containing pigments, pooled, ethanol was removed by concentration in vacuo at a temperature not exceeding 40°C. the Concentrate liofilizat. Get dark red�th lyophilic powder, which is a complex of pigments benefciaries shell and needles sea urchins, purified from proteins, salts and minerals. The yield is 0,18.

EXAMPLE 2. To confirm the composition of the product analysis of samples of complex pigments of benefciaries by high performance liquid chromatography (HPLC). HPLC was performed on a chromatograph Shimadzu LC-20 (Kyoto, Japan) equipped with a DAD-detector SPD M20, two pumps LC20AD, autosampler SIL-20 A, degasser DGU-20 A3 and column Luna C18 5 µm (250 mm×4.6 mm) with protective 5 µm column (4.0 mm×30 mm). The separation of impurities was carried out with a mixture of solvent A (0.1% formic acid) and b (acetonitrile - methanol 5:9) in the following mode: 0-25 min gradient, 30-80 B in A. the feed Rate of the solvent to 1 ml/min.

In Fig.1 shows a chromatogram of a complex of pigments benefciaries enriched ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene), obtained from shell and needles of sea urchins. 1 - beginon; 2 - agitation-6,6'-bis(2,3,7-tri-hydroxynaphthalene); 3 - ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene); 4 - isomer anhydration-6,6'-bis(2,3,7-tri-hydroxy naftizina).

In Fig.2 shows the absorption spectrum of ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene), obtained from shell and needles of sea urchins. The spectral maxima λmax: 265, 334, 485, 540 sq.

EXAMPLE 3. Anti-inflammatory effect �and models "carrageenophyte air pouch in rats".

To explore antiexudative properties used a classical model of acute inflammation "carrageenophyte air pouch in rats" [Current protocols in pharmacology..., 2003]. Air pouch was formed by subcutaneous injection of 20 ml of air in the back of the rat. Induction of acute inflammation caused by the introduction of the 6 days inside the pouch 3 ml of 0.5% solution of λ-carrageenin (Sigma-Aldirch, USA). Complex pigments of benefciaries of example 1 was administered at a dose of 2 mg/kg, 0.2 mg/kg and 0.02 mg/kg inside the bag immediately after the injection of a solution carragenin. The solvent served as water for injections. The reference drug diclofenac (solution for injection 25 mg/ml, Hemopharm, Serbia) was injected inside the bag immediately after the injection of a solution carragenin at a dose of 2 mg/kg After 6 hours was carried out by the fence of fluid for analysis total number of leukocytes using veterinary Hematology analyzer (Abacus Unior Vet, Austria), as well as the concentration of Pro-inflammatory mediators prostaglandin PGE2and TNFα using a commercially available enzyme-linked immunosorbent assay kits (Cayman Chemicals, USA).

Acute inflammation after 6 hours was characterized by infiltration of leukocytes to 14.1×106cells/ml, the production of proinflammatory mediators TNFα and up to 4.3 ng/ml and up to 2654 PG/ml of prostaglandin PGE2(Table 1).

Table 1
Anti-inflammatory effects of complex pigments of benefciaries on the model karagayskogo air pouch in rats (M±m, N=7)
GroupDose, mg/kgThe total number of leukocytes, ×106cells/mlTNFα, ng/mlPGE2, ng/ml
Intact (without induction of inflammation)-0,3±0,10±00±0
Control (solvent)80,014,1±0,8*4,3±0,5*2654±309*
Diclofenac2,003,3±0,9*#0,8±0,1*#61±25*#
Complex pigments of benefciaries Ave 12,005,4±1,5*#2,3±0,3*#1343±281*#
Complex pigments of benefciaries Ave 1 0,207,8±2,0*#2,9±0,4*#1976±273*
Complex pigments of benefciaries Ave 10,0212,2±1,4*4,1±0,4*2877±422*
Note:*- statistically significant differences with the intact group by t-student test at p<0,05; * - statistically significant differences with the control group by t-student test at p<0,05.

The reference drug diclofenac was statistically significantly inhibited the infiltration of cells by 75%, the level of TNFα by 81% and reduced the concentration of PGE2almost 0. Complex pigments of benefciaries of example 1 showed dose-dependent anti-inflammatory effect. At a dose of 2 mg/kg there was a decrease in the infiltration of leukocytes in the area of inflammation by 62%, the concentration of TNFα by 47% and PGE250% in comparison with the control.

EXAMPLE 4. Anti-inflammatory effects in models of allergic conjunctivitis in rabbits

Allergic conjunctivitis was simulated by application of the polymer Compound 48/80 on conjunctiva of a rabbit. Complex pigments of benefciaries of example 1 and the comparison medication) was administered 1 drop in �oz 2 mg/kg into each conjunctival cavity for 3 days before induction of pathology. On the day of induction drugs were administered 60 minutes prior to the application of "Compound 48/80 and after - after 10, 30, 45 and 100 minutes. Assessment of the allergic damage of the conjunctiva were performed after 5, 15, 60, 120 minutes and 24 hours after application of the inductor. The effectiveness of was evaluated by swelling of the conjunctiva, edema of the century, lacrimation and redness of the conjunctiva in scores from 0 to 4. Cumulative clinical indicator was calculated as the sum of the scores of each of the four parameters with a range from 0 to 16. Before the experiment all the eyes of the rabbits had a clinical score of zero. In the cornea was determined the content of histamine by HPLC. The data presented in table 2.

Table 2
Antiallergic action of a complex of pigments benefciaries on the model of allergic conjunctivitis in rabbits (N=6)
GroupClinical indicators, scoreCumulative clinical score, scoreThe content of histamine in the cornea, ug/g (M±M)
Conjunctival edemaEyelid edemaAfter�techenie Conjunctival redness
Intact000004,5±0,9
Control13,26,011,57,5the 38.214,4±1,6
Complex pigments of benefciaries Ave 12,72,27,5113,422,1±2,9
A)3,22,08,52,5the 16.214,2±0,9

In the application of complex pigments of benefciaries Ave 1 observed a marked reduction of edema of the conjunctiva and eyelid, reduction of lacrimation and redness of the conjunctiva compared with control animals (table.2). The level of histamine in the cornea of rabbits treated with the drug comparison), did not differ from that in control�Noi group (table.2). The level of histamine in the group treated with the complex of pigments benefciaries Ave 1, was significantly higher than in the control group, which is associated with a possible mechanism of action - binding to H1-receptors and a competitive blocking them for histamine. Thus, the complex pigments of benefciaries Ave 1 prevents allergic reactions again, depleting reserves of mediators of Allergy and blocking the binding with specific receptors. Histological evaluation demonstrated that in the group treated with the complex of pigments benefciaries Ave 1, the severity of pathological changes in the structures of the eye was lower than in the control group and the group treated with the drug comparison). The use of investigational drugs helped limit the spread of inflammatory and allergic processes deep into the eye, reducing the number of damaged goblet cells of the retina.

1. The method of producing a pigment complex of benefitsharing for the prevention of inflammatory diseases, enriched behenna, anhydration-6,6'-bis(2,3,7-tri-hydroxynaphthalene), ethyliden-6,6'-bis(2,3,7-tri-hydroxynaphthalene isomer and anhydration-6,6'-bis(2,3,7-tri-hydroxynaphthalene, including the demineralization of the shell with needles of fishing sea urchins Strongylocentrotus droebachiensis organic solution Ki�lots at a temperature of 40-90°C, the separation of salts of organic acids and protein excess organic solvent miscible with water, applying the solution of pigments on a chromatographic column with cation exchange resin, washing the column with a weak solution of mineral acid and distilled water, elution of the pigment complex of the cation exchanger with a step gradient of ethanol, the pooling of the fractions containing pigments, removal of ethyl alcohol by concentration in vacuo and lyophilization concentrate.

2. A method according to claim 1, where the organic solvent is a solvent selected from the group: ethanol, acetone, acetonitrile.

3. Complex pigments of benefciaries obtained by the method according to claim 1, for the prevention of inflammatory diseases.



 

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2 dwg, 12 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc.

EFFECT: reducing the negative side action of diacerein.

18 cl, 23 ex, 33 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to microbiology, namely to using bacteria, and describes a composition containing microorganisms, a method for preparing probiotics with the anti-inflammatory action and a method for preparing an anti-inflammatory composition containing the probiotics. The composition according to the invention is characterised by the microorganism count subject to the short-time high-temperature processing at 120-140°C for 5-15 seconds.

EFFECT: invention can be used for preparing the compositions for treating or preventing the inflammatory disorders for the probiotics for dairy products.

10 cl, 7 dwg

Antiviral compounds // 2541571

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I, such as below, or its pharmaceutically acceptable salts. What is described is a method for preparing them.

,

wherein: A independently from B means phenyl,

, or ,

and B independently from A means phenyl,

, or ,

and the values Z, Y, D, L1, L2, L3, Z1, Z2 are presented in the patent claim.

EFFECT: compounds are effective for hepatitis C virus (HCV) replication inhibition.

17 cl, 3 tbl, 8 dwg, 177 ex

FIELD: chemistry.

SUBSTANCE: method of producing dry earthworm powder includes: contacting live earthworms with chloride(s) of at least one metal selected from a group consisting of potassium, sodium, magnesium and calcium; subsequently contacting the live earthworms with powder of a hydroxycarboxylic acid(s) (or aqueous solution) and diluting the obtained mixture with water to adjust pH to 2-5, followed by leaving the live earthworms to stand for 3-180 minutes, washing the live earthworms with water, grinding the washed live earthworms and freeze-drying the obtained ground product (version).

EFFECT: method enables to obtain powder with high enzymatic activity.

6 cl, 8 tbl, 2 ex

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