WO2009121600A2 - Hydroxytyrosol formulations for the treatment and prevention of dna oxidative damages in post-menopausal conditions - Google Patents
Hydroxytyrosol formulations for the treatment and prevention of dna oxidative damages in post-menopausal conditions Download PDFInfo
- Publication number
- WO2009121600A2 WO2009121600A2 PCT/EP2009/002416 EP2009002416W WO2009121600A2 WO 2009121600 A2 WO2009121600 A2 WO 2009121600A2 EP 2009002416 W EP2009002416 W EP 2009002416W WO 2009121600 A2 WO2009121600 A2 WO 2009121600A2
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- WO
- WIPO (PCT)
- Prior art keywords
- extract
- formulations
- hydroxytyrosol
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- treatment
- Prior art date
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- Ceased
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Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- 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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/592—9,10-Secoergostane derivatives, e.g. ergocalciferol, i.e. vitamin D2
-
- 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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
-
- 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)
- A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
- A61K36/232—Angelica
-
- 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)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
- A61K36/537—Salvia (sage)
-
- 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)
- A61K36/63—Oleaceae (Olive family), e.g. jasmine, lilac or ash tree
-
- 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)
- A61K36/74—Rubiaceae (Madder family)
- A61K36/742—Coffea, e.g. coffee
-
- 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)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/894—Dioscoreaceae (Yam family)
- A61K36/8945—Dioscorea, e.g. yam, Chinese yam or water yam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Definitions
- the present invention relates to compositions comprising hydroxytyrosol (HT) and other biophenols, useful to counteract the DNA oxidative damages in post-menopausal conditions.
- HT hydroxytyrosol
- EP 1623960 A process for the preparation of highly pure HT, suitable as an ingredient for use in the pharmaceutical, alimentary and cosmetic fields is disclosed in EP 1623960 in the Applicant's name.
- EP 1623960 also discloses formulations comprising HT for use in the pharmaceutical, food and cosmetic fields.
- a number of scientific publications concerning the beneficial activities of hydroxytyrosol and other biophenols are known.
- Simonetta Salvini et al.- Daily consumption of a high- phenol extra-virgin olive oil reduces oxidative DNA damage in postmenopausal women - British Journal of Nutrition (2006), 95, 742-751] disclose the beneficial effects of a diet rich in extra- virgin olive oil with high HT content in the control of the post-menopausal syndrome.
- Dioscorea extract - calcium and/or magnesium ions
- biophenol and/or carotenoid compounds is particularly effective in the treatment and prevention of the oxidative stress, in particular on cell DNA, responsible for the post-menopausal syndrome.
- the invention therefore relates to pharmaceutical or dietetic formulations containing said combination as the active ingredient.
- the invention further relates to the use of said combination for the preparation of compositions for the treatment of the post-menopausal syndrome.
- biophenol means a phenol compound of vegetable origin having antioxidizing activity: examples of said compounds include gallic acid, caffeic acid, tyrosol, catechin, epicatechin, epigallocatechin, quercetin, resveratrol, ellagic acid.
- carotenoids examples include lutein, lycopene, zeaxanthin, tocopherols.
- formulations comprising hydroxytyrosol combined with: - Olea europea extracts; extracts of Dioscorea, Angelica sinensis, Salvia officinalis; Passion fruit; caffeic acid, gallic acid, lutein, tyrosol; calcium and/or magnesium ions; and - vitamin D; useful as osteoporosis preventive agents for keeping bone density and solidity constant.
- the Angelica sinensis extract is useful against hot flashes.
- the Salvia officinalis extract exerts tonic, stimulating and astringent actions and reduces sweating, particularly night sweats.
- the Passion fruit extract has sedative activity free from depressant effects, useful in conditions of nervous insomnia, agitation, anxiety, cramps and intestinal pain.
- the combinations of the invention are particularly effective as they are able to effectively, synergistically control post-menopausal syndrome symptoms and causes.
- the formulations of the invention are preferably in the form of tablets or similar oral solid forms, which are advantageous in terms of convenience of administration, stability (up to three years or more) and possibility to deliver hydroxytyrosol in much higher amounts than those from the diet intake. It should be noted, indeed, that the hydroxytyrosol content in olive oil can vary depending on the cultivar, pedo-climatic conditions, olive pressing time and techniques, etc. and anyway cannot provide sufficiently high concentrations.
- hydroxytyrosol content in the formulations of the invention may range from 0.1 to 10 mg per unit dose, while the dosages of the other components may range within wide limits, according to what is known for products comprising such active ingredients.
- the content in each single component may be comprised within the range of ⁇ 50% of the values reported in the following Examples, which illustrate the invention in greater detail.
- Tablet comprising HT + Olea europaea dry extract
- Tablet comprising HT + Olea europaea dry extract + caffeic acid + Passion fruit, Angelica, Salvia and Dioscorea extracts
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- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Inorganic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Plant Substances (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Pharmaceutical or dietetic formulations comprising hydroxytyrosol and at least one of the following components: - Angelica sinensis extract; - Salvia officinalis extract; - Passion fruit extract; - Olea europea extract; - Dioscorea extract; - calcium and/or magnesium ions; - vitamin D; - one or more biophenol and/or carotenoid compounds.
Description
HYDROXYTYROSOL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF DNA OXIDATIVE DAMAGES IN POSTMENOPAUSAL CONDITIONS
The present invention relates to compositions comprising hydroxytyrosol (HT) and other biophenols, useful to counteract the DNA oxidative damages in post-menopausal conditions.
Technological Background A process for the preparation of highly pure HT, suitable as an ingredient for use in the pharmaceutical, alimentary and cosmetic fields is disclosed in EP 1623960 in the Applicant's name. EP 1623960 also discloses formulations comprising HT for use in the pharmaceutical, food and cosmetic fields. A number of scientific publications concerning the beneficial activities of hydroxytyrosol and other biophenols are known.
In particular, Simonetta Salvini et al.- Daily consumption of a high- phenol extra-virgin olive oil reduces oxidative DNA damage in postmenopausal women - British Journal of Nutrition (2006), 95, 742-751] disclose the beneficial effects of a diet rich in extra- virgin olive oil with high HT content in the control of the post-menopausal syndrome.
Disclosure of the Invention
It has now been found that a combination of hydroxytyrosol with at least one of the following components: - Angelica sinensis extract;
- Salvia officinalis extract;
- Passion fruit extract;
- Olea europea extract;
- Dioscorea extract;
- calcium and/or magnesium ions;
- vitamin D;
- one or more biophenol and/or carotenoid compounds, is particularly effective in the treatment and prevention of the oxidative stress, in particular on cell DNA, responsible for the post-menopausal syndrome.
The invention therefore relates to pharmaceutical or dietetic formulations containing said combination as the active ingredient.
The invention further relates to the use of said combination for the preparation of compositions for the treatment of the post-menopausal syndrome.
In the following, the term "biophenol" means a phenol compound of vegetable origin having antioxidizing activity: examples of said compounds include gallic acid, caffeic acid, tyrosol, catechin, epicatechin, epigallocatechin, quercetin, resveratrol, ellagic acid.
Examples of carotenoids include lutein, lycopene, zeaxanthin, tocopherols.
According to the invention, particularly preferred are formulations comprising hydroxytyrosol combined with: - Olea europea extracts; extracts of Dioscorea, Angelica sinensis, Salvia officinalis; Passion fruit; caffeic acid, gallic acid, lutein, tyrosol; calcium and/or magnesium ions; and - vitamin D; useful as osteoporosis preventive agents for keeping bone density and solidity constant.
The Angelica sinensis extract is useful against hot flashes. The Salvia
officinalis extract exerts tonic, stimulating and astringent actions and reduces sweating, particularly night sweats.
The Passion fruit extract has sedative activity free from depressant effects, useful in conditions of nervous insomnia, agitation, anxiety, cramps and intestinal pain.
The combinations of the invention are particularly effective as they are able to effectively, synergistically control post-menopausal syndrome symptoms and causes.
The formulations of the invention are preferably in the form of tablets or similar oral solid forms, which are advantageous in terms of convenience of administration, stability (up to three years or more) and possibility to deliver hydroxytyrosol in much higher amounts than those from the diet intake. It should be noted, indeed, that the hydroxytyrosol content in olive oil can vary depending on the cultivar, pedo-climatic conditions, olive pressing time and techniques, etc. and anyway cannot provide sufficiently high concentrations.
The hydroxytyrosol content in the formulations of the invention may range from 0.1 to 10 mg per unit dose, while the dosages of the other components may range within wide limits, according to what is known for products comprising such active ingredients. In principle, the content in each single component may be comprised within the range of ± 50% of the values reported in the following Examples, which illustrate the invention in greater detail.
EXAMPLE 1
Tablet comprising HT
EXAMPLE 2
Tablet comprising HT + Olea europaea dry extract
EXAMPLE 3
Tablet com risin HT + Olea euro aea dr extract + caffeic acid
EXAMPLE 4
Tablet comprising HT + Olea europaea dry extract + caffeic acid + Passion fruit, Angelica, Salvia and Dioscorea extracts
Claims
1. Pharmaceutical or dietetic formulations comprising hydroxytyrosol and at least one of the following components: - Angelica sinensis extract;
- Salvia officinalis extract;
- Passion fruit extract;
- Olea europea extract;
- Dioscorea extract; - calcium and/or magnesium ions;
- vitamin D;
- one or more biophenol and/or carotenoid compounds.
2. Formulations as claimed in claim 1 comprising Olea europea.
3. Formulations as claimed in claim 1 or 2 wherein biophenols and/or carotenoids are selected from caffeic acid, gallic acid, tyrosol.
4. Formulations as claimed in any one of claims 1 to 3 comprising extracts of Dioscorea, Angelica sinensis, Salvia officinalis, Passion fruit.
5. Formulations as claimed in any one of claims 1 to 4 comprising calcium ions, magnesium ions and vitamin D.
6. Formulations as claimed in any one of claims 1 to 5 in the form of tablets.
7. The use of a combination of hydroxytyrosol with at least one of the following components:
- Angelica sinensis extract; - Salvia officinalis extract;
- Passion fruit extract;
- Olea europea extract;
- Dioscorea extract; - calcium and/or magnesium ions;
- vitamin D;
- one or more biophenol and/or carotenoid compounds; for the preparation of compositions for the treatment of the post-menopausal syndrome.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TCMI2008A000589 | 2008-04-04 | ||
| IT000589A ITMI20080589A1 (en) | 2008-04-04 | 2008-04-04 | HYDROXYSEROSOL FORMULATIONS ONLY FOR THE PREVENTIVE AND CURATIVE TREATMENT OF DAMAGES PRODUCED BY THE OXIDATIVE EFFECTS ON THE DNA IN POST-MENOPAUSAL SITUATIONS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2009121600A2 true WO2009121600A2 (en) | 2009-10-08 |
| WO2009121600A3 WO2009121600A3 (en) | 2010-01-21 |
Family
ID=40296854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2009/002416 Ceased WO2009121600A2 (en) | 2008-04-04 | 2009-04-02 | Hydroxytyrosol formulations for the treatment and prevention of dna oxidative damages in post-menopausal conditions |
Country Status (2)
| Country | Link |
|---|---|
| IT (1) | ITMI20080589A1 (en) |
| WO (1) | WO2009121600A2 (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103599239A (en) * | 2013-11-01 | 2014-02-26 | 于明儒 | Traditional Chinese medicine ointment for treating osteoporosis |
| WO2014161872A1 (en) * | 2013-04-05 | 2014-10-09 | Nestec S.A. | Compositions for use in stimulating bone growth |
| IT201900000343A1 (en) * | 2019-01-10 | 2020-07-10 | Herbal E Antioxidant Derivatives S R L Ed In Forma Abbreviata H&Ad S R L | COMPOSITIONS FOR THE TREATMENT OF MENOPAUSE, OSTEOPENIA AND OSTEOPOROSIS, METABOLIC AND VASCULAR DISORDERS RELATED TO CLIMATER |
| WO2020229539A1 (en) * | 2019-05-13 | 2020-11-19 | Société des Produits Nestlé S.A. | Compositions and methods using a combination of calcium and at least one of oleuropein or metabolite thereof |
| WO2022066513A1 (en) * | 2020-09-24 | 2022-03-31 | Mars, Incorporated | Food compositions and applications thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0417884A (en) * | 2003-12-30 | 2007-04-27 | Med Care S R L | compositions comprising vitamins and / or derivatives thereof, stabilized with European oil extract and / or ionene polymers |
| ITMI20041627A1 (en) * | 2004-08-06 | 2004-11-06 | Lachifarma S R L Lab Chimi Co | PROCESS FOR THE RECOVERY OF THYROSOL HYDROXYTYROSOL AND OTHER PHENOLIC COMPONENTS FROM VEGETATION WATERS AND METHOD OF CATALYTIC OXIDATION OF THYROXIS TO HYDROXYSIROSOL |
| KR101435228B1 (en) * | 2006-07-14 | 2014-08-28 | 디에스엠 아이피 어셋츠 비.브이. | Compositions, and uses thereof for the treatment, combination therapy or prophylaxis of inflammatory diseases |
-
2008
- 2008-04-04 IT IT000589A patent/ITMI20080589A1/en unknown
-
2009
- 2009-04-02 WO PCT/EP2009/002416 patent/WO2009121600A2/en not_active Ceased
Cited By (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022031660A (en) * | 2013-04-05 | 2022-02-22 | ソシエテ・デ・プロデュイ・ネスレ・エス・アー | Composition for use in stimulating bone growth |
| CN105050591B (en) * | 2013-04-05 | 2020-08-07 | 雀巢产品有限公司 | Composition for stimulating bone growth |
| CN105050591A (en) * | 2013-04-05 | 2015-11-11 | 雀巢产品技术援助有限公司 | Compositions for use in stimulating bone growth |
| JP2016520544A (en) * | 2013-04-05 | 2016-07-14 | ネステク ソシエテ アノニム | Composition for use in stimulating bone growth |
| AU2014247122B2 (en) * | 2013-04-05 | 2018-12-06 | Société des Produits Nestlé S.A. | Compositions for use in stimulating bone growth |
| JP2020058351A (en) * | 2013-04-05 | 2020-04-16 | ソシエテ・デ・プロデュイ・ネスレ・エス・アー | Compositions for use in stimulating bone growth |
| US10675290B2 (en) | 2013-04-05 | 2020-06-09 | Societe Des Produits Nestle S.A. | Compositions for use in stimulating bone growth |
| JP2024150494A (en) * | 2013-04-05 | 2024-10-23 | ソシエテ・デ・プロデュイ・ネスレ・エス・アー | Compositions for use in stimulating bone growth - Patents.com |
| WO2014161872A1 (en) * | 2013-04-05 | 2014-10-09 | Nestec S.A. | Compositions for use in stimulating bone growth |
| US11166965B2 (en) | 2013-04-05 | 2021-11-09 | Societe Des Produits Nestle S.A. | Compositions for use in stimulating bone growth |
| CN103599239A (en) * | 2013-11-01 | 2014-02-26 | 于明儒 | Traditional Chinese medicine ointment for treating osteoporosis |
| WO2020144588A1 (en) * | 2019-01-10 | 2020-07-16 | Herbal E Antioxidant Derivatives S.R.L. Ed In Forma Abbreviata H&Ad S.R.L. | Compositions for treatment of the menopause, osteopenia and osteoporosis, and menopause/related metabolic and vascular disorders |
| IT201900000343A1 (en) * | 2019-01-10 | 2020-07-10 | Herbal E Antioxidant Derivatives S R L Ed In Forma Abbreviata H&Ad S R L | COMPOSITIONS FOR THE TREATMENT OF MENOPAUSE, OSTEOPENIA AND OSTEOPOROSIS, METABOLIC AND VASCULAR DISORDERS RELATED TO CLIMATER |
| WO2020229539A1 (en) * | 2019-05-13 | 2020-11-19 | Société des Produits Nestlé S.A. | Compositions and methods using a combination of calcium and at least one of oleuropein or metabolite thereof |
| AU2020274411B2 (en) * | 2019-05-13 | 2025-08-14 | Société des Produits Nestlé S.A. | Compositions and methods using a combination of calcium and at least one of oleuropein or metabolite thereof |
| WO2022066513A1 (en) * | 2020-09-24 | 2022-03-31 | Mars, Incorporated | Food compositions and applications thereof |
| JP2023544118A (en) * | 2020-09-24 | 2023-10-20 | マース インコーポレーテッド | Food compositions and their uses |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009121600A3 (en) | 2010-01-21 |
| ITMI20080589A1 (en) | 2009-10-05 |
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