WO2000024784A1 - Substance bioactive a base de dextran - Google Patents

Substance bioactive a base de dextran Download PDF

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Publication number
WO2000024784A1
WO2000024784A1 PCT/RU1998/000343 RU9800343W WO0024784A1 WO 2000024784 A1 WO2000024784 A1 WO 2000024784A1 RU 9800343 W RU9800343 W RU 9800343W WO 0024784 A1 WO0024784 A1 WO 0024784A1
Authority
WO
WIPO (PCT)
Prior art keywords
dextran
biologically active
compound
activity
active substance
Prior art date
Application number
PCT/RU1998/000343
Other languages
English (en)
Russian (ru)
Inventor
Elena Alexandrovna Izaxon
Original Assignee
Elena Alexandrovna Izaxon
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Elena Alexandrovna Izaxon filed Critical Elena Alexandrovna Izaxon
Priority to PCT/RU1998/000343 priority Critical patent/WO2000024784A1/fr
Priority to AU24432/99A priority patent/AU2443299A/en
Publication of WO2000024784A1 publication Critical patent/WO2000024784A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0021—Dextran, i.e. (alpha-1,4)-D-glucan; Derivatives thereof, e.g. Sephadex, i.e. crosslinked dextran
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof

Definitions

  • the compound is primarily intended for use in medical practice and may be used in veterinary medicine.
  • the positive activity is manifested in different types of materi- als, including those of positive polysaccharides and their outcomes, which are not necessarily inconsistent.
  • GICH Humanity
  • polysaccharides hemparins
  • hemparins natural polysaccharides
  • Such products can be obtained from polysaccharide isolated from acid glycoprotein, processed pyridine - an acid solution of 70% acid. [6].
  • linear (dextran, liborate, acid, and other) and branched (glycosyldextrans, and manganese sulfate) were tested. They were treated with pyperidine sulfonic acid in ⁇ with the subsequent neutralization of ⁇ . It was found that all the relevant polysaccharides showed high antiviral activity and had an inhibitory effect on their health.
  • Judging ⁇ d ⁇ s ⁇ u ⁇ nym is ⁇ chni ⁇ am invariant ⁇ matsii, nesul ⁇ as ⁇ de ⁇ zhaschie ⁇ lisa ⁇ a ⁇ idy - de ⁇ s ⁇ any not ⁇ azali ni ⁇ a ⁇ y ⁇ iv ⁇ vi ⁇ usn ⁇ y a ⁇ ivn ⁇ s ⁇ i
  • surfactants can be used from the market.
  • the culture of the L-4 person’s cell is corrected and installed, which means that the service is less likely than the other.
  • INSTALLED ALSO The biological activity of the polysaccharide depends on the molecular mass and the degree of growth of the polysaccharide. [11]. However, since it was noted earlier, they are inactive when they are in a group of viruses.
  • compositions use oral medicine at a dose of 500 mg per day or not at a dose of 300 mg / day to inhibit the production of HIV. They do not have a large toxicity and do not disrupt normal reactions.
  • De-propanaldehyde is often used for the creation of physiologically active exemptions, but in the form of a carrier for the purpose of operating and disinfecting drugs
  • Dextropanaldehyde was also used to bind antipyretic antimicrobial agents [14; fifteen; 16]. When using the dextran in the quality of the matrix, 0 were obtained . derivatives of ampicillin, penicillin, streptomycin, canamycin, levomycetin [17; 18; 19].
  • the objective of the invention is the production of a new chemical compound having a high effective activity, in particular - by the loss of circulation.
  • the task of the invention is reduced to a chemical synthesis of biologically active material possessing beneficial activity.
  • Dextranalpalidehyde-Resorbin may be obtained as follows. A mixture of 20 g of dextran in 1 liter of water is mixed with a mixture of 21.4 g of methane in 1 liter of water; C in the dark. After the reaction is reduced, the concentration is concentrated in a vacuum (20–25 mm or more) at 5 times, dialyzed for 48 hours and the solution is distilled. The yield of dextropanaldehyde is 80-90%. The composition of the aldehyde group in the polysaccharide is 1.1 ⁇ 0.1 moles per mole of multiples. ⁇ title solution of 15 mmol of rubber in 15 ml 0.5 n of water
  • the product of the reaction is an amorphous product that is directly affected by the water, and is not soluble in the product and other products of the company.
  • composition of the rubber in dextrosepropionic aldehyde disintegrates the inactivating compound.
  • ⁇ 50 mg add 1 ml 0.1 N of water and bring it up to 25 ml. Then select ⁇ / ⁇ 8 / 00343
  • C 3 ⁇ add ' ⁇ k' Yk / a - 114 ' ⁇ k' ⁇ ⁇ .
  • ⁇ is the acidity, mol / l
  • ⁇ - the amount of acid that went into the sale (shared by the program)
  • a - a sample of the substance in aliquot, mg
  • Hadd is the molar mass of the link of the original dextran-polyaldehyde.
  • ⁇ 1 g of the product contains 0.27 ⁇ 0.03 g of the residues of the product.
  • the potent activity was shared with the type I virus ( ⁇ PG- ⁇ ) on the switchable cell culture.
  • the cakes were cultivated in 96-well plates for the growth of the minority in the environment of ⁇ -1640, which comprised 10% of the yield of food.
  • a flavoring insulin with a concentration of ⁇ PG- ⁇ 10 ⁇ ID 5 o / ml was applied to the cellulary.
  • Tested substances at a concentration of 100, 10 and 1 mg / l. After incubation at 37 ° C in a C0 2 incubator, the virus was removed for 1 hour and the environment changed. The results resulted in a specific, specific, viral effect on the cells after cultivation at 37 ° C in a C0 2 -input for 36 hours.
  • * - ⁇ ID - tkanevy infectious dose * - ⁇ ID - tkanevy infectious dose.
  • the inventive compound in the form of a homogeneous suspension in ⁇ réelle ⁇ -80 introduced an oral with an optional gastric probe at a dose of 300 mg / kg or slightly less than 18 mg 72 hours
  • a dose of 300 mg / kg or slightly less than 18 mg 72 hours The absence of symptoms, the property of toxic effects and the absence of death of animals during the course of the indicated period resulted in a loss of liabilities.
  • infantile white mice were intranasally infected with ⁇ PG- ⁇ in the dose of Yu 3 ⁇ IZ ⁇ / mouse.
  • the investigated material was introduced internally in the form of a homogeneous suspension in in the amount of 50 mg / kg for therapeutic treatment: for 24 and
  • the activity of the investigated substance was manifested in a decrease in the quantity and the area of the foci of inflammation, the degree of the expressed outcry of the disease, the incidence of the disease is 4
  • the performance indicators of the tested material are absorbed in the case of the cyclist. ⁇ / ⁇ 8 / 00343

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention se rapporte au domaine de la médecine, plus précisément à celui de la pharmacie et de la médecine vétérinaire, et concerne des substances bioactives synthétiques à base de dextran qui possèdent une activité antivirale, notamment à l'encontre des virus de l'herpès simplex. Cette invention permet de produire un nouveau composé chimique qui possède une forte activité antivirale, notamment contre les virus du groupe de l'herpès. En d'autres termes, cette invention concerne la synthèse chimique d'une substance bioactive ayant une action antivirale. Cette invention consiste donc à synthétiser un nouveau composé à base de dextran, c'est à dire dextranpolyaldéhyde-résorcine, correspondant à la formule générale (I). Cette invention est détaillée plus profondément dans la description à l'aide d'un exemple du procédé de production de ce composé, des résultats de son identification, de trois séries d'expériences permettant de déterminer son activité biologique et sa toxicité, et de deux tableaux.
PCT/RU1998/000343 1998-10-26 1998-10-26 Substance bioactive a base de dextran WO2000024784A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/RU1998/000343 WO2000024784A1 (fr) 1998-10-26 1998-10-26 Substance bioactive a base de dextran
AU24432/99A AU2443299A (en) 1998-10-26 1998-10-26 Dextran-containing biologically active substance

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU1998/000343 WO2000024784A1 (fr) 1998-10-26 1998-10-26 Substance bioactive a base de dextran

Publications (1)

Publication Number Publication Date
WO2000024784A1 true WO2000024784A1 (fr) 2000-05-04

Family

ID=20130277

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU1998/000343 WO2000024784A1 (fr) 1998-10-26 1998-10-26 Substance bioactive a base de dextran

Country Status (2)

Country Link
AU (1) AU2443299A (fr)
WO (1) WO2000024784A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017175132A1 (fr) 2016-04-04 2017-10-12 Uniwersytet Jagiellonski Utilisation d'un dérivé cationique de dextrane pour l'inhibition des virus de l'herpès simplex

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2392672A1 (fr) * 1977-05-31 1978-12-29 Personal Products Co Procede pour inhiber l'activite microbienne utilisant des dialdehydo-polysaccharides insolubles
SU1530630A1 (ru) * 1986-12-30 1989-12-23 Научно-производственное объединение "Биолар" Способ получени диальдегиддекстрана
DE3921761A1 (de) * 1989-07-01 1991-01-03 Hoechst Ag Substituierte polysaccharide, verfahren zu deren herstellung sowie deren verwendung zur prophylaxe und behandlung von viruserkrankungen

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2392672A1 (fr) * 1977-05-31 1978-12-29 Personal Products Co Procede pour inhiber l'activite microbienne utilisant des dialdehydo-polysaccharides insolubles
SU1530630A1 (ru) * 1986-12-30 1989-12-23 Научно-производственное объединение "Биолар" Способ получени диальдегиддекстрана
DE3921761A1 (de) * 1989-07-01 1991-01-03 Hoechst Ag Substituierte polysaccharide, verfahren zu deren herstellung sowie deren verwendung zur prophylaxe und behandlung von viruserkrankungen

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
IOZEP A.A.: "Spektrofotometrichesky metod analiza vodorastvorimykh polisakharidaldegidov", ZHURNAL PRIKLADNOI KHIMII, vol. 71, no. 7, July 1998 (1998-07-01), pages 1202 - 1205 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017175132A1 (fr) 2016-04-04 2017-10-12 Uniwersytet Jagiellonski Utilisation d'un dérivé cationique de dextrane pour l'inhibition des virus de l'herpès simplex

Also Published As

Publication number Publication date
AU2443299A (en) 2000-05-15

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