WO2007004912A1 - Anti-allergene - Google Patents

Anti-allergene Download PDF

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Publication number
WO2007004912A1
WO2007004912A1 PCT/RU2005/000471 RU2005000471W WO2007004912A1 WO 2007004912 A1 WO2007004912 A1 WO 2007004912A1 RU 2005000471 W RU2005000471 W RU 2005000471W WO 2007004912 A1 WO2007004912 A1 WO 2007004912A1
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WO
WIPO (PCT)
Prior art keywords
shock
animals
guinea pigs
reaction
dose
Prior art date
Application number
PCT/RU2005/000471
Other languages
English (en)
Russian (ru)
Inventor
Larisa Petrovna Kovalenko
Elena Vladimirovna Shipaeva
Andrei Dmitreevich Durnev
Vladimir Vladimirovich Balakshin
Aleksey Nikolaevich Chistyakov
Original Assignee
Obschestvo S Ogranichennoi Otvetstvennostju 'berezovy Mir'
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 Obschestvo S Ogranichennoi Otvetstvennostju 'berezovy Mir' filed Critical Obschestvo S Ogranichennoi Otvetstvennostju 'berezovy Mir'
Publication of WO2007004912A1 publication Critical patent/WO2007004912A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents

Definitions

  • the invention relates to medicine, and more specifically to finding new anti-allergenic drugs.
  • Allergy is an extremely important medical and social problem. According to various sources, it affects 20 to 40% of the population, while the last 30 years, the incidence of allergies doubled every ten years.
  • anti-allergens There are a fairly large number of widely known histamine preparations (anti-allergens) used in modern medicine, however, the problem of finding new, effective anti-allergens continues to be relevant, in particular, due to the expansion of the spectrum of allergens due to the consequent environmental degradation.
  • anti-allergens In folk medicine, a number of plants are considered anti-allergens. Among them is the warty birch, the leaves and juice of which can be used to prepare anti-allergens.
  • the inventors of the present invention discovered the possibility of using an extract of the white part of birch bark (birch bark) as an antiallergen, and its effectiveness was very high, at the level of such well-known and widely used synthetic antihistamines as suprastin (the international non-proprietary name is chloropyramine) and clarithin (international nonproprietary name - loratodyne).
  • Birch bark extract can be obtained by various known methods. So, in accordance with documents SU 382657 and SU 2172178, extraction is carried out using alcohol. In accordance with the patent RU 2192879, which belongs to the applicant, birch bark extraction is carried out with toluene, with obtaining as a final product a dry crystalline substance, the main component of which (up to 97%) is betulin - triterpene diatomic alcohol.
  • mice of the control and experimental groups were orally immunized with a 0.6% solution of chicken egg protein (CJA) at a dose of 1 ml per 250 g of body weight for three days (dissolved in physiological solution of CJA to guinea pigs was administered orally through a soft plastic probe) (2).
  • CJA chicken egg protein
  • Ni is the number of guinea pigs who developed severe shock; N 2 - the number of guinea pigs that developed moderate, shock; Nz - the number of guinea pigs that developed a mild shock; N 4 - Guinea pigs in which there was no shock.
  • the Weigle index is 4 (++++). In severe shock - 3 (+++), in moderate shock - 2 (++), in mild shock - 1 (+), in the absence of anaphylactoid reactions in guinea pigs - the index is 0 (3). Inflammation reaction to concanavalin A (con A)
  • the inflammation reaction to Con A (a pseudo-allergic reaction) is based on Con A's ability non-specifically, i.e. without the participation of reagins with allergens on the membranes of target cells, as a result of a direct action on mast cell membranes and basophilic leukocytes, they release inflammatory mediators (histamine, serotonin, leukotrienes, etc.).
  • the experiments were performed on mice of males of the CBA line weighing 18-20 g. Two routes of administration of the test substances were used - intraperitoneal and oral, the introduction was carried out in 1% starch gel.
  • BAS was administered at doses of 5 mg / kg, 50 mg / kg and 100 mg / kg
  • betulin was administered at doses of 10 mg / kg and 100 mg / kg
  • reference preparations, suprastin and clarithin were administered at doses of 5 mg / kg and 50 mg / kg.
  • BAS was administered at doses of 5 mg / kg, 50 mg / kg and 100 mg / kg
  • betulin was administered at doses of 50 mg / kg and 100 mg / kg
  • suprastin and clarithin at doses of 5 mg / kg and 50 mg / kg
  • the animals in the control group were similarly injected with an appropriate volume of starch gel.
  • Con A (20 ⁇ l of the solution at a concentration of 5 mg / ml) was administered to mice of the experimental and control groups after 2 hours subplanarly (into the pads of the back foot), and the same volume of physiological saline was applied to the contralateral limb. After an hour, the mice were sacrificed, the mass of paws was determined, and the inflammatory response index (And p ) was calculated by the formula: P to
  • a severe anaphylactic shock was determined in one animal, a weak shock developed in 4 guinea pigs, and an anaphylactic reaction was not detected in 4 guinea pigs (the Weigle reaction index was 1, 1).
  • BES was administered at a dose of 1000 mg / kg, 1 pig out of 10 died, a severe anaphylactic shock developed in the 1st animal, moderate shock was determined in 3 pigs, and there was no reaction in 5 guinea pigs (Weigle index - 1, 3).
  • the data presented in Table 2 show that the intraperitoneal administration of BAS at a dose of 50 mg / kg suppressed the intensity of the systemic anaphylaxis reaction in animals of the experimental groups compared to the control.
  • the reaction index in the control group of animals was 2.1 (in 4 guinea pigs severe anaphylactic shock was determined, in 3 - moderate shock, in 3 - mild shock).
  • 3 guinea pigs developed moderate shock, 4 weak mild shock, 3 anaphylactic reaction was not detected (Weigle reaction index was 1, 0).
  • BAS suppresses anaphylactic shock in the anaphylaxis reaction in guinea pigs immunized with CJD.
  • the suppression of anaphylactic shock with the introduction of BAS is more pronounced than with the introduction of the reference drug, claritin.
  • CBA resulted in a statistically significant inhibition of the inflammatory response to Con A by 72.7% (Table 6).
  • the introduction of BAS in doses of 5 mg / kg and 100 mg / kg did not cause a significant suppression of the reaction of inflammation to Con A.
  • With a single administration of reg os betulin at doses of 5 mg / kg and 100 mg / kg and suprastin at doses of 5 mg / kg and 50 mg / kg did not suppress the inflammation response to Con A.
  • Comparison drug, clarithin, administered orally at doses of 5 mg / kg and 50 mg / kg statistically significant dose-dependent inhibition of the inflammatory response to Con A by 45.5% and 83.2%, respectively.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Pulmonology (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne l'utilisation de l'écorce de bouleau dans la lutte contre les allergies.
PCT/RU2005/000471 2005-07-06 2005-09-16 Anti-allergene WO2007004912A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2005121151 2005-07-06
RU2005121151 2005-07-06

Publications (1)

Publication Number Publication Date
WO2007004912A1 true WO2007004912A1 (fr) 2007-01-11

Family

ID=37604688

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2005/000471 WO2007004912A1 (fr) 2005-07-06 2005-09-16 Anti-allergene

Country Status (1)

Country Link
WO (1) WO2007004912A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10287582A (ja) * 1997-04-09 1998-10-27 Ogawa Koryo Kk 樹皮抽出物からなるヒスタミン遊離抑制剤
FR2802818A1 (fr) * 1999-12-24 2001-06-29 Greentech Sa Procede d'obtention d'un extrait d'ecorce de bouleau, betula alba, et especes apparentees
RU2206572C1 (ru) * 2002-03-12 2003-06-20 Общество с ограниченной ответственностью Химико-биологическое объединение при РАН "Фирма Вита" Способ выделения бетулинола
RU2254032C2 (ru) * 2003-08-14 2005-06-20 Закрытое акционерное общество "СНС-фарма" Композиция биологически активных веществ

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10287582A (ja) * 1997-04-09 1998-10-27 Ogawa Koryo Kk 樹皮抽出物からなるヒスタミン遊離抑制剤
FR2802818A1 (fr) * 1999-12-24 2001-06-29 Greentech Sa Procede d'obtention d'un extrait d'ecorce de bouleau, betula alba, et especes apparentees
RU2206572C1 (ru) * 2002-03-12 2003-06-20 Общество с ограниченной ответственностью Химико-биологическое объединение при РАН "Фирма Вита" Способ выделения бетулинола
RU2254032C2 (ru) * 2003-08-14 2005-06-20 Закрытое акционерное общество "СНС-фарма" Композиция биологически активных веществ

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Mir", RUKOVODSTVO PO MEDITSINE, DIAGNOSTIKA I TERAPIYA, M, vol. 1, 1997, pages 212-213 - 220 *

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