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WO1991001742A1 - Biologically active compositions - Google Patents

Biologically active compositions Download PDF

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Publication number
WO1991001742A1
WO1991001742A1 PCT/GB1990/001182 GB9001182W WO9101742A1 WO 1991001742 A1 WO1991001742 A1 WO 1991001742A1 GB 9001182 W GB9001182 W GB 9001182W WO 9101742 A1 WO9101742 A1 WO 9101742A1
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WO
WIPO (PCT)
Prior art keywords
composition
officinalis
plant
valeariana
extract
Prior art date
Application number
PCT/GB1990/001182
Other languages
French (fr)
Inventor
Christer Stenbacka
Gert Rolad Ohlsson
Sven Thorngvist
Original Assignee
Ruffles, Graham, Keith
Medical Resource (Holdings) Limited
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 Ruffles, Graham, Keith, Medical Resource (Holdings) Limited filed Critical Ruffles, Graham, Keith
Publication of WO1991001742A1 publication Critical patent/WO1991001742A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/19Acanthaceae (Acanthus family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/537Salvia (sage)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/84Valerianaceae (Valerian family), e.g. valerian
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/899Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane

Definitions

  • the present invention provides biologically active compositions, notably anti-viral compositions, and in particular compositions effective against HIV.
  • compositions of this invention are based on one or more active ingredients present in the plant Valeariana officinalis and/or Andrographis paniculata, especially active ingredients present in the roots of such plants.
  • compositions of this invention are based on active ingredients present in dry comminuted roots of V ; _ officinalis and/or A. paniculata. If desired, the roots or other part of the plant can be subjected to an ethanol or aqueous extraction in conventional manner.
  • compositions are preferably based on Valeariana officinalis, which ingredient preferably comprises 35 to 60 % of the composition, typically 40 to 50 % of the composition.
  • compositions of this invention are non-toxic, and preferably take the form of compositions for oral administration, such as tablets, though other dosage forms are not precluded.
  • the compositions can contain auxilliary components, such as enzyme precursors, coenzymes, and related bioactive compounds, for example ⁇ hymotripsinogen A, coenzyme Q 1Q , lecithin, alpha-tocopherol, vitamins, nicotini ⁇ acid, and/or pyridoxine hydrochloride.
  • Royal jelly is another useful ingredient. Extracts of other plants may also be incorporated, for instance extracts of Epilobium roseum, Agropyron ⁇ aninum, and/or Salvi officinalis.
  • compositions based on the active ingredients without necessarily obtaining these active ingredients from the plant sources. If the enzyme theory expressed below is substantiated, then the one or more enzymes can be adopted.
  • Retrovirus like HIV can not reproduce without having access to DNA.
  • the HIV-virus has to enter a cell in which it produces a DNA replica of its own RNA moiety.
  • the active signal substance enters the protein shell of the virus infected cell and give orders which make the protein shell decompose. The remainder of the virus-infected cell will then be taken care of by the T-cells.
  • compositions Apart from activity against HIV, the present compositions have a more general anti-viral activity and also have antineoplastic, antibacterial and immunomodulatory activity.
  • the resulting mixture prepared in this manner is identified by us as NR-2, and was submitted for testing.
  • Figure 1 shows the results of toxicity testing of the tablets at the various indicated dilutions.
  • Figure 2 shows the results of related toxicity testing using cells infected with HIV.
  • Figure 3 shows the results on testing at various dilutions on a human tumour cell line.
  • Figure 4 shows the results on testing at various dilutions on a human melanoma cell line.
  • Example 3 0.5g tablets. A normal dose is calculated to be 4 tablets per day.
  • the test diagrams are the same for the tablets as for the powder of Example 1.
  • Effective tablets can also be made by grinding the dried roots.
  • the following ingredients are then particularly suitable:
  • the Valeriana officinalis, o-tocopherol, and vitamins are pre-mixed, dried at 80 * C, ground to a powder, and then mixed with the other ingredients before tabletting in conventional manner.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Medicinal Chemistry (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compositions with anti-viral, antineoplastic, antibacterial and/or immunomodulatory activity include one or more ingredients obtained from the plant Valeariana officinalis and/or Andrographis paniculata.

Description

Biologically Active Compositions
BACKGROUND OF THE INVENTION
The present invention provides biologically active compositions, notably anti-viral compositions, and in particular compositions effective against HIV.
SUMMARY OF THE INVENTION
The compositions of this invention are based on one or more active ingredients present in the plant Valeariana officinalis and/or Andrographis paniculata, especially active ingredients present in the roots of such plants.
PREFERRED EMBODIMENTS
For ease of manufacture, the compositions of this invention are based on active ingredients present in dry comminuted roots of V;_ officinalis and/or A. paniculata. If desired, the roots or other part of the plant can be subjected to an ethanol or aqueous extraction in conventional manner.
The compositions are preferably based on Valeariana officinalis, which ingredient preferably comprises 35 to 60 % of the composition, typically 40 to 50 % of the composition.
The compositions of this invention are non-toxic, and preferably take the form of compositions for oral administration, such as tablets, though other dosage forms are not precluded. Apart from one or more active ingredients originating from V^ officinalis and/or A. paniculata, the compositions can contain auxilliary components, such as enzyme precursors, coenzymes, and related bioactive compounds, for example σhymotripsinogen A, coenzyme Q1Q, lecithin, alpha-tocopherol, vitamins, nicotiniσ acid, and/or pyridoxine hydrochloride. Royal jelly is another useful ingredient. Extracts of other plants may also be incorporated, for instance extracts of Epilobium roseum, Agropyron σaninum, and/or Salvi officinalis.
Within the present invention it is also possible to prepare compositions based on the active ingredients without necessarily obtaining these active ingredients from the plant sources. If the enzyme theory expressed below is substantiated, then the one or more enzymes can be adopted.
Without being bound by theory, it is theorized that a Retrovirus like HIV can not reproduce without having access to DNA. The HIV-virus has to enter a cell in which it produces a DNA replica of its own RNA moiety. The active signal substance enters the protein shell of the virus infected cell and give orders which make the protein shell decompose. The remainder of the virus-infected cell will then be taken care of by the T-cells. By the catalysing process of the enzymes in the plant materials, with the enzymes which are in the protein shell of the infected virus cell, a completely selective process has takes which does not effect any other cells and which does not have nor need any toxic components at all.
Apart from activity against HIV, the present compositions have a more general anti-viral activity and also have antineoplastic, antibacterial and immunomodulatory activity.
EXAMPLES OF THE INVENTION
The present invention is illustrated by the following non-limiting Examples.
Example 1
Take one part (weight) of Valeriana officinalis to seven parts of water.
Boil the mixture for five hours.
Filter the mixture through a fine metal filter.
Let the filtration liquid cool down completely then centrifuge it at 5000RPM for 15 minutes. Decant the clear content and let it dry at 95*C until it is almost dry. Lower the temperature to 70*C and let it dry completely. Then grind it to a fine powder.
For storage keep it in a dry and airtight container.
Take one part of Epilobilum roseum to seven parts of water.
Boil the mixture for five hours.
(Proceed exactly as under 1. above)
Take one part of Salvia officinalis to seven parts of water.
Boil the mixture for five hours.
(Proceed exactly as under 1. above)
Now mix the above powders 1-3 as follows (weight %) Powder No. 1 Valeriana officinalis 48.6% Powder No. 2 Epilobilum roseum 11.0%
Powder No. 3 Salvia officinalis 1.1%
5. Mix well and then add the following:
Royal jelly 17.3%
Nicotinic Acid 11.0%
Pyridoxine Hydroσhloridum 11.0%
The resulting mixture prepared in this manner is identified by us as NR-2, and was submitted for testing.
The test results are illustrated by the accompanying figures. * *
DESCRIPTION OF THE DRAWINGS
Figure 1 shows the results of toxicity testing of the tablets at the various indicated dilutions.
Figure 2 shows the results of related toxicity testing using cells infected with HIV.
Figure 3 shows the results on testing at various dilutions on a human tumour cell line.
Figure 4 shows the results on testing at various dilutions on a human melanoma cell line.
Example 2
Take one part of Valeriana officinalis to seven parts of water.
Boil the mixture for five hours.
(Proceed exactly as under 1. above)
Figure imgf000006_0001
8. Take one part of Epilobilum roseum to seven parts of water.
Boil the mixture for five hours. (Proceed exactly as under 1. above)
9. Take one part of Salvia officinalis to seven parts of water.
Boil the mixture for five hours. (Procees exactly as under 1. above)
10. Take one part of Agropyron caninum germs to seven • parts of water.
Heat the water to boiling and pour it over the Agropyron caninum germs.
Wait five minutes then filter the mixture. (For the rest proceed as under 1. above)
11. Now mix the above powders 7-10 as follows (weight %)
Powder No.7 Valeriana officinalis 45.0%
Powder No.8 Epilobilum roseum 10.0%
Powder No.9 Salvia officinalis 1.0%
Powder No.10 Agropyron caninum germs 9.0%
12. Mix well and then add the following:
Royal Jelly 16.0%
Nicotinic Acid 1.0%
Pyridoxine Hydrochloridum 1.0%
Sodium Carbonate 10.0%
Wheat Pulp 4.0%
Magnesium Stearate 3.0%
13. The mix is then fed to a tablet machine to press
0.5g tablets. A normal dose is calculated to be 4 tablets per day. The test diagrams are the same for the tablets as for the powder of Example 1. Example 3
Effective tablets can also be made by grinding the dried roots. The following ingredients are then particularly suitable:
(%)
Valeriana officinalis 45
Lecithin 4
Salvia officinalis 4
DL-α-tocopherol 1
A-D vitamins 1 pyridoxine hydrochloride 1 nicotinic acid 1 dolomite powder 5 flavouring 2 magnesium stearate 1.5 lactose 34.5
The Valeriana officinalis, o-tocopherol, and vitamins are pre-mixed, dried at 80*C, ground to a powder, and then mixed with the other ingredients before tabletting in conventional manner.

Claims

CLAI MS
1. A composition effective against HIV, including one or more active ingredients present in the plant Valeariana officinalis and/or Andrographis paniculata.
2. The composition of claim 1, wherein the active ingredient is taken from the root of the plant.
3. The composition of claim 1, wherein the plant is Valeariana officinalis.
4. The composition of claim 1, wherein the active ingredient is employed as a dry powder obtained after aqueous extraction of the plant.
5. The composition of claim 1, in the form of a powder or a tablet.
6. The composition of claim 1, which further contains at least one auxiliary material chosen from enzyme precursors, coenzymes, and related bioactive compounds,- for example chymotripsinogen A, coenzy e Q10. lecithin, alpha-tocopherol, vitamins, nicotinic acid, and/or pyridoxine hydrochloride; royal jelly; an extract of Epilobium roseum; an extract of Agropyron caninum; and/or an extract of Salvia officinalis.
7. A composition with anti-viral, antineoplastic, antibacterial and/or immunomodulatory activity, which includes one or more ingredients obtained from the plant Valeariana officinalis and/or Andrographis paniculata.
8. A method for combatting a virus, neoplasm, or bacterium, or a method of immunomodulation, which employs a composition which includes one or more ingredients obtained from the plant Valeariana officinalis and/or Androqraphis paniculata.
PCT/GB1990/001182 1989-07-28 1990-07-30 Biologically active compositions WO1991001742A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB8917295.1 1989-07-28
GB898917295A GB8917295D0 (en) 1989-07-28 1989-07-28 Anti-viral compositions

Publications (1)

Publication Number Publication Date
WO1991001742A1 true WO1991001742A1 (en) 1991-02-21

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GB (1) GB8917295D0 (en)
WO (1) WO1991001742A1 (en)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996017605A1 (en) * 1994-12-06 1996-06-13 Paracelsian, Inc. Use of andrographolide compounds to treat or prevent pathogenicity of diseases
WO1999033866A3 (en) * 1997-12-27 1999-09-10 Gsf Forschungszentrum Umwelt Antivirally active oligopeptide isolated from royal jelly
WO2001085710A1 (en) * 2000-05-05 2001-11-15 Dr. Reddy's Research Foundation Novel anticancer compounds: process for their preparation and pharmaceutical compositions containing them
US6410590B1 (en) 2000-02-03 2002-06-25 Dr. Reddy's Research Foundation Compounds having antitumor activity: process for their preparation and pharmaceutical compositions containing them
US6486196B2 (en) 2000-05-05 2002-11-26 Dr. Reddy's Research Foundation Anticancer compounds: process for their preparation and pharmaceutical compositions containing them
US6576662B2 (en) 2000-05-05 2003-06-10 Dr. Reddy's Laboratories Limited Compounds having anticancer activity : process for their preparation and pharmaceutical compositions containing them
US7135164B2 (en) * 2001-11-09 2006-11-14 Mahidol University Andrographis paniculata gel as an adjunct in the treatment of periodontitis

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE149731C (en) * 1902-11-20

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE149731C (en) * 1902-11-20

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996017605A1 (en) * 1994-12-06 1996-06-13 Paracelsian, Inc. Use of andrographolide compounds to treat or prevent pathogenicity of diseases
WO1999033866A3 (en) * 1997-12-27 1999-09-10 Gsf Forschungszentrum Umwelt Antivirally active oligopeptide isolated from royal jelly
US6410590B1 (en) 2000-02-03 2002-06-25 Dr. Reddy's Research Foundation Compounds having antitumor activity: process for their preparation and pharmaceutical compositions containing them
WO2001085710A1 (en) * 2000-05-05 2001-11-15 Dr. Reddy's Research Foundation Novel anticancer compounds: process for their preparation and pharmaceutical compositions containing them
US6486196B2 (en) 2000-05-05 2002-11-26 Dr. Reddy's Research Foundation Anticancer compounds: process for their preparation and pharmaceutical compositions containing them
US6576662B2 (en) 2000-05-05 2003-06-10 Dr. Reddy's Laboratories Limited Compounds having anticancer activity : process for their preparation and pharmaceutical compositions containing them
US7135164B2 (en) * 2001-11-09 2006-11-14 Mahidol University Andrographis paniculata gel as an adjunct in the treatment of periodontitis

Also Published As

Publication number Publication date
GB8917295D0 (en) 1989-09-13
AU6272490A (en) 1991-03-11

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