WO2010058272A2 - Cosmetics extracts obtainable from apiceae vegetables and especially from carrot taproots - Google Patents

Cosmetics extracts obtainable from apiceae vegetables and especially from carrot taproots Download PDF

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Publication number
WO2010058272A2
WO2010058272A2 PCT/IB2009/007509 IB2009007509W WO2010058272A2 WO 2010058272 A2 WO2010058272 A2 WO 2010058272A2 IB 2009007509 W IB2009007509 W IB 2009007509W WO 2010058272 A2 WO2010058272 A2 WO 2010058272A2
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Prior art keywords
dependent
sections
root
vegetables
carrot
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PCT/IB2009/007509
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French (fr)
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WO2010058272A3 (en
Inventor
Daniel Dizer
Rafael Alon
Yossef Kanner
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Yoffi Agshach Ltd.
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Publication of WO2010058272A2 publication Critical patent/WO2010058272A2/en
Publication of WO2010058272A3 publication Critical patent/WO2010058272A3/en

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Classifications

    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • A01N65/08Magnoliopsida [dicotyledons]
    • A01N65/10Apiaceae or Umbelliferae [Carrot family], e.g. parsley, caraway, dill, lovage, fennel or snakebed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00Anti-perspirants or body deodorants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005Antimicrobial preparations

Definitions

  • the family comprises various identified members, such as ((E,3R,8S)-Heptadeca-l,9-dien-4,6- diyne-3,8-diol) falcarindiol (FDOL); (l,9-heptadecadiene-4,6-diyn-3-ol) falcarinol (FOL); falcarindiol 3 -acetate, «-O-methylfalcarindiol, such as 3-O-methylfalcarindiol or 8-0- methylfalcarindiol etc, and derivatives thereof.
  • FDOL ((E,3R,8S)-Heptadeca-l,9-dien-4,6- diyne-3,8-diol) falcarindiol
  • FOL falcarinol
  • falcarindiol 3 -acetate «-O-methylfalcarindiol, such as 3-O-methylfalcarindiol or 8-0- methylfalcarindiol etc, and
  • US5455278 discloses food preservatives, pharmaceutical compositions and production method thereof, useful for inhibiting gram-positive bacteria, especially Listeria, Clostridium botulinum and Staphylococcus aureus in a food medium or other medium which comprises a chemical derivative of FDOL in an amount which is safe and effective to inhibit any such gram-positive bacteria which may be present in the medium.
  • the FDOL is obtained by a two- steps solvent extraction process, in which whole carrot roots are effectively contacted with solvents selected from hexane, petroleum ether, ethyl acetate, methylene chloride and ethanol.
  • Extracts obtained from shredded whole carrot taproot were demonstrated to have overall weak bactericide properties.
  • Hao et al. Food Microb., 1998, 15, 367-378
  • Glisic et al. Food Chem., 2007, 105, 346-352
  • MIC minimum inhibition concentration
  • super-critical carbon dioxide treatment of the extract provides selective biocidic properties, i.e., higher activity towards Gram-positive bacteria compared to Gram-negative bacteria.
  • the biocidic effect towards Bacillus subtilis was more than 15 times higher than towards E. coli.
  • US5455278 also teaches that FDOL-containing carrot extract are innocuous to Gram-negative bacteria such as Salmonella typhimurium and Escherichia coli.
  • Gram-negative bacteria such as Salmonella typhimurium and Escherichia coli.
  • Babic et al. (J. Appl. Bacter. 1994, 75, 135-141) found that purified whole carrot extract was 1,000 to 10,000 times more active biocide against Gram-positive bacteria (Leuconostoc mesenteroides, Staphylococcus aureus, and Listeria monocytogenes) than against Gram- negative bacteria (E. coli and Pseudomonas fluorescens).
  • Literature suggests well targeted use of polyacetylenes, especially FDOL and FOL in treating humans, especially in decreasing lipopolysaccharide-induced expression of inflammatory proteins in macrophage and endothelial cells (See Metzger et al., J. Agrc. Food Chem., 2008, 56, 3554-3560). Polyacetylenes have also found specific importance in inhibition of the mutagenicity of 2-nitrofluorene and 3-nitrofluoranthene (See Tang et al., Food Chem. Toxi., 1997, 35, 373-378), and antiproliferation activity of cancer cell (See Netzel et al., Inno., Food Sci. Emer.
  • deodorants are applied to the body, particularly the armpits, .
  • a subgroup of deodorants are "antiperspirants", which prevent odor and reduce sweat produced by parts of the body.
  • Aluminium chloride, aluminium chlorohydrate, and aluminium-zirconium compounds are the most widely used antiperspirants. Nevertheless, aluminum has been established as a neurotoxin, and an increased amount of aluminum was found in the brains of many Alzheimer's patients. Moreover, particular substances in deodorants, such as preservatives called parabens, or salts such as aluminum chloride used in antiperspirants, get into the bloodstream or accumulate in breast tissue, where they enhance or emulate the effects of estrogen, which stimulates the growth of cancerous breast cells. A connection between deodorants and renal dysfunction was also suggested. [13] A natural -bome non-toxic and non-irritant effective deodorant for eliminating or otherwise inhibiting fermenting bacteria is thus a long felt need.
  • the present invention relates to a cosmetic composition
  • a cosmetic composition comprising a cosmetically acceptable ingredient extractable from predetermined sections of Apiaceae vegetables' root, said ingredient is characterized by inhibiting effect towards pathogenic microorganisms located inside the body of a patient .
  • a ⁇ -carotene free cosmetic composition based on the cosmetically acceptable ingredient is disclosed.
  • the invention relates also to a use of a cosmetic composition based one the cosmetically acceptable ingredient in either human or animal
  • the cosmetic composition concerned may be adapted for applying dermally either in a continuous or non-continuous manner.
  • the cosmetic composition according the present invention comprise at least one additive selected from a group consisting of anti-infectives, antimicrobials, prebiotics, probiotics, acidif ⁇ ers, antivirals, antibiotics, markers, biomarkers, dyes, pigments, radio-labeled materials, glues, adhesives, lubricants, nutrients, peptides, amino acids, polysaccharides, enzymes, hormones, chelators, multivalent ions, emulsifying or de-emulsifying agents, binders, fillers, thickfiers, factors, co-factors, anticaries agents, anticellulites, antidandruff, antifungal, anti- inflammatories, anti-irritants, antimicrobials, antioxidants, astringents, antiperspirants, antiseptics, antistatic agents, binders, buffers, additional carriers, chelators, cell stimulants, cleansing agents, conditioners, deodorants, depilatories, detergents, dispersants
  • the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable are selected either from (i) the pericyclic parenchyma, or from (U) the phloem part, close to the secondary cambium, or a combination thereof.
  • the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable include the xylem.
  • the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable include either its fiber-containing sections or from its fibrous sections .
  • predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable may include in its various embodiments colored sections, or pigment-containing sections selected in a non-limiting manner from a group consisting of carotenes, chlorophylls, carotenoids, flavonoids and phytochrome.
  • the Apiaceae vegetables from which the cosmetically acceptable ingredient can be obtained are selected from carrot, celery, fennel, parsley, parsnip
  • the Apiaceae vegetables are carrot (Daucus carota L) taproots.
  • an effective measure of at least one polyacetylene compound is included as a means for providing Gram-positive bacteria inhibition property, thereby adjusting the selectivity (S) of the composition to a desirable value, e.g. 1.1, or e.g. 8.
  • the polyacetylene is selected from a group consisting of ((E,3R,8S)- Heptadeca-l,9-dien-4,6-diyne-3,8-diol) falcarindiol; (l,9-heptadecadiene-4,6-diyn-3-ol 1,9- heptadecadiene-4,6-diyn-3-ol) falcarinol; falcarindiol 3-acetate, n-0-methylfalcarindiol, especially 3-O-methylfalcarindiol or 8-O-methylfalcarindiol, or any mixture thereof.
  • a method of providing skin, nails and/or hair care is also within the scope of the present invention, the method comprise inhibiting topical pathogenic contaminations of microorganisms in a patient, by (a) obtaining at least one composition comprising a cosmetically acceptable ingredient from predetermined sections of Apiaceae vegetables' root and, (b) topically introducing an effective dose of said cosmetic to the skin, nails or hair of either a human or animal patient.
  • topical introduction of the cosmetic may be provided by a means of an applicator or effecter,.
  • Said applicator or effecter may be for example either a rigid or a non-rigid brush, pad, spray of fluids.
  • the method according to the present invention further comprise in various of its embodiments admixing or otherwise adding the cosmetic at least one additive.
  • Such at least one additive may include anti-infectives, antimicrobials, prebiotics, probiotics, acidifiers, antivirals, antibiotics, markers, biomarkers, dyes, pigments, radio-labeled materials, glues, adhesives, lubricants, nutrients, peptides, amino acids, polysaccharides, enzymes, hormones, chelators, multivalent ions, emulsifying or de-emulsifying agents, binders, fillers, thickfiers, factors, co-factors, anticaries agents, anticellulites, antidandruff, antifungal, anti- inflammatories, anti-irritants, antimicrobials, antioxidants, astringents, antiperspirants, antiseptics, antistatic agents, binders, buffers, additional carriers, chelators, cell stimulants, cleansing agents, conditioners, deodorants, depilatories, detergents, dispersants, emollients, emulsifiers, enzymes, essential oils,
  • the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extracted are from either (i) the pericyclic parenchyma, (H) the phloem part, close to the secondary cambium, or a combination thereof.
  • the method comprise selecting predetermined sections of the root of Apiaceae vegetables from the xylem sections for extracting the cosmetically acceptable ingredient thereof.
  • the method comprise selecting the predetermined sections of the root of Apiaceae vegetables from its fiber-containing sections or from its fibrous sections for extracting the cosmetically acceptable ingredient thereof.
  • the method comprise selecting the predetermined sections of the root of Apiaceae vegetables from its colored sections or pigment-containing sections (e.g. sections comprising carotenes, chlorophylls, carotenoids, flavonoids and phytochrome).
  • sections or pigment-containing sections e.g. sections comprising carotenes, chlorophylls, carotenoids, flavonoids and phytochrome.
  • the Apiaceae vegetables are selected from a group consisting of carrot, celery, fennel, parsley, parsnip, or any combination of the same.
  • the Apiaceae vegetables are of one or more species and types of carrot (Daucus carota L) taproots.
  • the method according to the invention further provides for selectively inhibiting Gram- negative bacteria contaminating a medium while significantly less inhibiting Gram-positive bacteria in the medium.
  • the method may also comprise obtaining at least one polyacetylene compound from predetermined sections of the root of Apiaceae vegetables, useful for adjusting the selectivity ratio of the cosmetic composition, e.g. to a selectivity (S) between 1.1 and 10.
  • the invented method further concerns extracting outer sections of the root of Apiaceae vegetables by means of at least one first solvent until a final extract is obtained.
  • the method comprises a step of evaporating the extract in a manner that at least a portion of the at least one first solvent is eliminated from the final condensate product.
  • At least one step of re-extracting the obtained condensate by means of at least one second solvent may be a part of the method in yet further embodiments.
  • Re-evaporating the at least one second extract until a dry condensate final product is obtained may be included in the method as well.
  • the at least one first solvent is selected from a group of polar solvents, dipolar aprotic solvents, volatile solvents, water-miscible diluents, organic solvents with high dielectric constants (6.0-9.0), non-polar solvents (hexane, petroleum ether), extractants or any mixtures of the same.
  • Said at least one first solvent may comprise one or more of the following groups: Group A comprising at least one polar solvent; Group B comprising at least one dipolar solvent; and Group C comprising at least one non-polar solvent.
  • Group A comprises a first polar solvent and second polar solvent, the volume ratio between the first and second polar solvents ranging from 1 : 10 to 10: 1 (v/v).
  • B comprises a first bipolar solvent and second bipolar solvent, the volume ratio between the first and second bipolar solvents ranging from 1 :15 to 15:1 (v/v).
  • Group C comprises a first non-polar solvent and second non-polar solvent, the volume ratio between the first and second polar solvents ranging from 1 : 12 to 12: 1 (v/v).
  • the volume ratio between Group A to B is ranging from 1 :100 to 100:1 (v/v); wherein the volume ratio between Group B to C is ranging from 1 : 100 to 100:1 (v/v); and further wherein the volume ratio between Group A to C is ranging from 1 :100 to 100: 1 (v/v).
  • volume ratio between Group A to B is ranging from 1 :50 to 20:1 (v/v); wherein the volume ratio between Group B to C is ranging from 1:10 to 10:1 (v/v); and further wherein the volume ratio between Group A to C is ranging from 1 :50 to 15:1 (v/v).
  • the volume ratio between Group A, B and C is from 1 : 1 : 1 to 100: 10: 1 (v/v/v), respectively.
  • the invention further relates to cosmetics according to the description, characterized in both a proven inhibiting effect towards pathogenic microorganisms located inside the body of a patient and a therapeutic added value.
  • the cosmetic according to the invention may provide for treating acne by inhibiting Gram- positive Propionibacterium acnes bacteria.
  • a preparation of (i) oral rinse (ii) skin cleanser (iii) soap (e.g., toilet soap, laundry soap) (iv) shampoo (v) tooth brush paste comprising the cosmetic disclosed are also included in the scope of the present invention. .
  • the solvents were denoted by three different groups: Group A comprising at least one polar solvent; Group B comprising at least one dipolar solvent; and Group B comprising at least one non-polar solvent.
  • Group A comprising at least one polar solvent
  • Group B comprising at least one dipolar solvent
  • Group B comprising at least one non-polar solvent.
  • Various mixtures were tested, whereas combinations of volatile organic solvents with high dielectric constants (6.0-9.0) in acidic conditions and elevated temperature were found effective. Biocidal activity of the extract has been found unaffected (or at least nondestructively affected) by these conditions.
  • a zone inhibition assay was conducted to test the susceptibility of a species of microorganisms according to the diffusion agar assay (DAA) method.
  • DAA diffusion agar assay
  • Table 1 was obtained.
  • the term 'Body' refers to the carrot taproot inner section, whereas the term 'Peel' refers to the carrot taproot external sections as defined in the present invention.
  • solvents refers to extraction of either the body or peel sections by a solvent mixture, and the term water refers to similar systems whereat the sections were contacted with a water phase.
  • selectivity value (S) of the biocide defined as the ratio of
  • Gram-positive bacteria e.g., P. ph ⁇ seoli
  • the measure of its ability in inhibiting Gram-negative bacteria e.g., H. pylori
  • a deodorant simulating system made of carrot extract was produced according to the methods detailed in Example II.

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Abstract

Cosmetics useful for both human and animal care is disclosed comprising extracts obtainable from either the inner and/or outer sections of the root of Apiaceae vegetables, wherein the outer sections are selected from the (i) pericyclic parenchyma, and (ii) the phloem part, close to the secondary cambium, of carrot taproots. The present invention also relates to methods producing the cosmetics and to natural methods for treating the human and animal skin, hair and nails.

Description

COSMETICS COMPRISING EXTRACTS OBTAINABLE FROM APIACEAE VEGETABLES, AND ESPECIALLY FROM CARROT TAPROOTS
FIELD OF THE INVENTION [01] The present invention generally pertains to cosmetics based on Apiaceae vegetables.
BACKGROUND OF THE INVENTION
[02] It is known that the taproot that is the edible part of Apiaceae vegetables, namely carrot, celery, fennel, parsley and parsnip is exposed to soil throughout its growth and development. Considering the abundance of microbes such as bacteria, fungi, yeasts and moulds in soil, the resistance of the vegetable taproots to spoilage and rot during growth, as well as under cool storage conditions, might be an indication of the presence of natural antimicrobials in these plants.
[03] Polyacetylenes from the Apiaceae vegetables are known biocides with cytotoxic activities, See Zidron et al., J Agric. Food Chem. 2005 53(7), 2518-2523. Polyacetylenes are obtained from their vegetable source by various unit operations, such as liquid-liquid extract, solvent extraction and especially one-step or multistep solid-liquid extraction and back-extraction, distillation, super-critical based processes, filtration, evaporation, precipitation etc. The family comprises various identified members, such as ((E,3R,8S)-Heptadeca-l,9-dien-4,6- diyne-3,8-diol) falcarindiol (FDOL); (l,9-heptadecadiene-4,6-diyn-3-ol) falcarinol (FOL); falcarindiol 3 -acetate, «-O-methylfalcarindiol, such as 3-O-methylfalcarindiol or 8-0- methylfalcarindiol etc, and derivatives thereof.
[04] Research by Baranska et al., Analyst, 2005, 130, 855- 859 teaches that polyacetylenes are accumulated as conglomerates in the outer section of the root, namely the pericyclic parenchyma, and in the phloem part close to the secondary cambium. Similarly, Olsson et al., J. Phytopathology 1996, 144, 441-447 showed that FDOL and FOL concentrations in the peel section of carrots is five and two times higher than in carrot's core section, respectively. Christensen et al. J. Sep. ScL 2007, 30, 483-490 have shown similar results for FDOL and FOL by using HPLC-DAD analytical measurements. Davies et al. New phytol. 1981, 88, 109- 119 demonstrated similar results for various other compositions, namely 6-methoxymellein , p-hydroxybenzoic acid and chlorogenic acid, suspected to be characterized by biocidic properties.
[05] US5455278 discloses food preservatives, pharmaceutical compositions and production method thereof, useful for inhibiting gram-positive bacteria, especially Listeria, Clostridium botulinum and Staphylococcus aureus in a food medium or other medium which comprises a chemical derivative of FDOL in an amount which is safe and effective to inhibit any such gram-positive bacteria which may be present in the medium. The FDOL is obtained by a two- steps solvent extraction process, in which whole carrot roots are effectively contacted with solvents selected from hexane, petroleum ether, ethyl acetate, methylene chloride and ethanol.
[06] Brandt et al., Tren. Food ScL Tech. 2004, 15, 384-393 discloses that FOL content was significantly reduced (about 40% reduction) after short bleaching (70 s) by high temperature water (900C).
[07] Extracts obtained from shredded whole carrot taproot were demonstrated to have overall weak bactericide properties. For example a study presented by Hao et al. (Food Microb., 1998, 15, 367-378), utilizing such extracts for inhibiting Gram-positive bacteria. Glisic et al., (Food Chem., 2007, 105, 346-352) studied the minimum inhibition concentration (MIC) of extracts obtained from shredded whole carrot taproot on various bacteria, and showed that super-critical carbon dioxide treatment of the extract provides selective biocidic properties, i.e., higher activity towards Gram-positive bacteria compared to Gram-negative bacteria. Hence, the biocidic effect towards Bacillus subtilis was more than 15 times higher than towards E. coli. US5455278 also teaches that FDOL-containing carrot extract are innocuous to Gram-negative bacteria such as Salmonella typhimurium and Escherichia coli. Similarly, Babic et al., (J. Appl. Bacter. 1994, 75, 135-141) found that purified whole carrot extract was 1,000 to 10,000 times more active biocide against Gram-positive bacteria (Leuconostoc mesenteroides, Staphylococcus aureus, and Listeria monocytogenes) than against Gram- negative bacteria (E. coli and Pseudomonas fluorescens).
[08] Literature suggests well targeted use of polyacetylenes, especially FDOL and FOL in treating humans, especially in decreasing lipopolysaccharide-induced expression of inflammatory proteins in macrophage and endothelial cells (See Metzger et al., J. Agrc. Food Chem., 2008, 56, 3554-3560). Polyacetylenes have also found specific importance in inhibition of the mutagenicity of 2-nitrofluorene and 3-nitrofluoranthene (See Tang et al., Food Chem. Toxi., 1997, 35, 373-378), and antiproliferation activity of cancer cell (See Netzel et al., Inno., Food Sci. Emer. Tech., 2007, 8, 365-372; Rauscher et al., Mut. Res. 1998, 413, 129-142 and de Meija et al., Mut. Res., 1997, 389, 219-226). A focused study role of polyacetylenes in anti- steroidogenic activity was demonstrated by Majumder et al., (J. Ethnopharmacology, 1997, 57, 209-212).
[09] US20060193819 discloses a topical cosmetic composition with skin rejuvenation benefits^ comprising a blend of a vast list of plant species, essentially including neem seed cell broth and one or more botanical ingredients selected from the group consisting of Salvia miltorrhiza extract, pomegranate fruit extract, grape seed extract, cucumber extract, carrot extract, rosemary extract, Iris root extract, white birch extract, and Laminaria algae extract. The carrot extract was utilized solely for introducing β-carotene and vitamin A. β carotene has been associated with elevated risks of lung and prostate cancer especially in smokers and people exposed to high levels of asbestos (See Speizer et al., Cancer Causes and Control 1999, 10(5), 475-482). Hypervitaminosis is also correlated with uptake of both vitamin A and carotenes. Thus calculated uptake or administration of β -carotene-containing cosmetics and pharmaceuticals is advisable.
[10] Human sweat is largely odorless until it is fermented by bacteria. When adult armpits are washed with pH basic soaps, the skin loses its acid mantel (pH 4.5 - 6), raising the pH to become basic. Bacteria thrive in high pH or base environments. Creating such an environment in the armpit makes it more susceptible to bacterial colonization.
[1 1] In order to reduce body odor caused by bacteria, deodorants are applied to the body, particularly the armpits, . A subgroup of deodorants are "antiperspirants", which prevent odor and reduce sweat produced by parts of the body.
[12] Aluminium chloride, aluminium chlorohydrate, and aluminium-zirconium compounds, most notably Aluminium zirconium tetrachlorohydrex gly and Aluminium zirconium trichlorohydrex gly, are the most widely used antiperspirants. Nevertheless, aluminum has been established as a neurotoxin, and an increased amount of aluminum was found in the brains of many Alzheimer's patients. Moreover, particular substances in deodorants, such as preservatives called parabens, or salts such as aluminum chloride used in antiperspirants, get into the bloodstream or accumulate in breast tissue, where they enhance or emulate the effects of estrogen, which stimulates the growth of cancerous breast cells. A connection between deodorants and renal dysfunction was also suggested. [13] A natural -bome non-toxic and non-irritant effective deodorant for eliminating or otherwise inhibiting fermenting bacteria is thus a long felt need.
[14] It is hence a long felt need to obtain biocompatible (i.e., non toxic and non irritant) naturally- obtained cosmetics having both proven inhibiting effect towards pathogenic microorganisms, and skin-care properties.
SUMMARY OF THE INVENTION
[15] The present invention relates to a cosmetic composition comprising a cosmetically acceptable ingredient extractable from predetermined sections of Apiaceae vegetables' root, said ingredient is characterized by inhibiting effect towards pathogenic microorganisms located inside the body of a patient .
[16] According to one broad aspect of the invention a β-carotene free cosmetic composition based on the cosmetically acceptable ingredient is disclosed.
[17] The invention relates also to a use of a cosmetic composition based one the cosmetically acceptable ingredient in either human or animal
[18] The cosmetic composition concerned may be adapted for applying dermally either in a continuous or non-continuous manner.
[19] The cosmetic of the present invention is selected from a group consisting of skin-care creams, creams, sticks, roll-on formulations, mousses, sprays, aerosols, pad-applied formulations, masks, lotions, powders, perfumes, lipsticks, fingernail and toe nail polish, eye and facial makeup, permanent waves, colored contact lenses, hair colors, hair sprays and gels, deodorants, baby products, bath oils, bubble baths, bath salts, butters, baby products, baby shampoos, lotions, powders and creams; bath preparations, bath oils, tablets and salts, bubble baths, bath fragrances, bath capsules; eye makeup preparations, eyebrow pencil, eyeliner, eye shadow, eye lotion, eye makeup remover, mascara; fragrance preparations, colognes, toilet waters, powders and sachets; non-coloring hair preparations, hair conditioner, hair spray, hair straighteners, permanent waves, rinses, shampoos, tonics, dressings and other grooming aids; color cosmetics; hair coloring preparations, hair dye, hair tints, hair color sprays, hair lighteners and hair bleaches; makeup preparations, face powders, foundations, leg and body paints, lipstick; makeup bases, rouges and makeup fixatives; manicuring preparations, basecoats, undercoats, cuticle softeners, nail creams, nail extenders, mail polish and enamel, and remover, oral hygiene products, dentrifices, mouthwashes; personal cleanliness, bath soaps, laundry soaps, detergents, deodorants, douches and feminine hygiene products; shaving preparations, aftershave lotion, beard softeners, men's talcum shaving cream, shaving soap, pre-shave lotions; skin care preparations, skin cleansing preparations, skin antiseptics, depilatories, face and neck cleansers, body and hand cleansers, foot powders; moisturizers, night preparations, paste masks, skin fresheners; and suntan preparations, suntan creams, gels and lotions, and indoor tanning preparations.
[20] In various of its embodiments the cosmetic composition according the the present invention comprise at least one additive selected from a group consisting of anti-infectives, antimicrobials, prebiotics, probiotics, acidifϊers, antivirals, antibiotics, markers, biomarkers, dyes, pigments, radio-labeled materials, glues, adhesives, lubricants, nutrients, peptides, amino acids, polysaccharides, enzymes, hormones, chelators, multivalent ions, emulsifying or de-emulsifying agents, binders, fillers, thickfiers, factors, co-factors, anticaries agents, anticellulites, antidandruff, antifungal, anti- inflammatories, anti-irritants, antimicrobials, antioxidants, astringents, antiperspirants, antiseptics, antistatic agents, binders, buffers, additional carriers, chelators, cell stimulants, cleansing agents, conditioners, deodorants, depilatories, detergents, dispersants, emollients, emulsifiers, enzymes, essential oils, exfoliants, fibers, film forming agents, fixatives, foaming agents, foam stabilizers, foam boosters, fungicides, gellants, glosser, hair conditioner, hair set resins, hair sheen agents, hair waving agents, humectants, lubricants, moisture barrier agents, moisturizers, ointment bases, opacifier, plasticizer, polish, polymers, powders, propellant, protein, refatting agents, sequestrant, silicones, skin calming agents, skin cleansers, skin conditioners, skin healing, skin lightening agents, skin protectants, skin smoothing agents, skin softening agents, skin soothing agents, stabilizers, sunscreen agents, surfactants, suspending agents, tanning accelerators, thickeners, vitamins, waxes, wetting agents, liquefiers, colors, flavors and/or fragrances, enzymatic-inhibitors, organoleptic agents, magnetic or paramagnetic materials, ferromagnetic and non-ferromagnetic materials, UV absorbers, UV enhancers, blood coagulators, inhibitors of blood coagulation, e.g., heparin and the like, anti-allergenics, antiinflammatories, anti-fungals, anticholinesterases, nutritional agents, cardiovascular agents, anti-hypertensive agents and chemotherapeutic agents, or any combination thereof.
[21] In various preferred embodiments of the invention the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable are selected either from (i) the pericyclic parenchyma, or from (U) the phloem part, close to the secondary cambium, or a combination thereof. [22] In some embodiments of the invention the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable include the xylem.
[23] In yet further embodiments of the invention the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable include either its fiber-containing sections or from its fibrous sections .
[24] Furthermore the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extractable may include in its various embodiments colored sections, or pigment-containing sections selected in a non-limiting manner from a group consisting of carotenes, chlorophylls, carotenoids, flavonoids and phytochrome.
[25] The Apiaceae vegetables from which the cosmetically acceptable ingredient can be obtained are selected from carrot, celery, fennel, parsley, parsnip
[26] In various preferred embodiments of the invention the Apiaceae vegetables are carrot (Daucus carota L) taproots.
[27] The cosmetic composition according to the present invention is especially useful for selectively inhibiting Gram-negative bacteria contaminating a medium while significantly less inhibiting Gram-positive bacteria in the medium.
[28] A selectivity (S) of the Gram-negative bacteria biocide according to the present invention, is defined as the ratio between the measure of inhibiting Gram-positive negative bacteria and the measure of inhibiting Gram-negative positive bacteria. According to various embodiments of the invention S is ranging between 1.1 to 100,000. According to some preferred embodiments, S is ranging between 10 to 10,000, and according to other preferred embodiments S is ranging between 100 to 1 ,000.
[29] In some embodiments of the invention an effective measure of at least one polyacetylene compound is included as a means for providing Gram-positive bacteria inhibition property, thereby adjusting the selectivity (S) of the composition to a desirable value, e.g. 1.1, or e.g. 8.
[30] It is another object of the present invention to disclose the cosmetic composition as defined above, wherein the polyacetylene is selected from a group consisting of ((E,3R,8S)- Heptadeca-l,9-dien-4,6-diyne-3,8-diol) falcarindiol; (l,9-heptadecadiene-4,6-diyn-3-ol 1,9- heptadecadiene-4,6-diyn-3-ol) falcarinol; falcarindiol 3-acetate, n-0-methylfalcarindiol, especially 3-O-methylfalcarindiol or 8-O-methylfalcarindiol, or any mixture thereof. [31] A method of providing skin, nails and/or hair care is also within the scope of the present invention, the method comprise inhibiting topical pathogenic contaminations of microorganisms in a patient, by (a) obtaining at least one composition comprising a cosmetically acceptable ingredient from predetermined sections of Apiaceae vegetables' root and, (b) topically introducing an effective dose of said cosmetic to the skin, nails or hair of either a human or animal patient.
[32] Without departing from the scope of the present invention the topical introduction of the cosmetic may be provided by a means of an applicator or effecter,.
[33] Said applicator or effecter may be for example either a rigid or a non-rigid brush, pad, spray of fluids.
[34] The method according to the present invention further comprise in various of its embodiments admixing or otherwise adding the cosmetic at least one additive.
[35] Such at least one additive may include anti-infectives, antimicrobials, prebiotics, probiotics, acidifiers, antivirals, antibiotics, markers, biomarkers, dyes, pigments, radio-labeled materials, glues, adhesives, lubricants, nutrients, peptides, amino acids, polysaccharides, enzymes, hormones, chelators, multivalent ions, emulsifying or de-emulsifying agents, binders, fillers, thickfiers, factors, co-factors, anticaries agents, anticellulites, antidandruff, antifungal, anti- inflammatories, anti-irritants, antimicrobials, antioxidants, astringents, antiperspirants, antiseptics, antistatic agents, binders, buffers, additional carriers, chelators, cell stimulants, cleansing agents, conditioners, deodorants, depilatories, detergents, dispersants, emollients, emulsifiers, enzymes, essential oils, exfoliants, fibers, film forming agents, fixatives, foaming agents, foam stabilizers, foam boosters, fungicides, gellants, glosser, hair conditioner, hair set resins, hair sheen agents, hair waving agents, humectants, lubricants, moisture barrier agents, moisturizers, ointment bases, opacifier, plasticizer, polish, polymers, powders, propellant, protein, refatting agents, sequestrant, silicones, skin calming agents, skin cleansers, skin conditioners, skin healing, skin lightening agents, skin protectants, skin smoothing agents, skin softening agents, skin soothing agents, stabilizers, sunscreen agents, surfactants, suspending agents, tanning accelerators, thickeners, vitamins, waxes, wetting agents, liquefiers, colors, flavors and/or fragrances, enzymatic-inhibitors, organoleptic agents, magnetic or paramagnetic materials, ferromagnetic and non- ferromagnetic materials, UV absorbers, UV enhancers, blood coagulators, inhibitors of blood coagulation, e.g., heparin and the like, anti-allergenics, anti-inflammatories, anti-fungals, anticholinesterases, nutritional agents, cardiovascular agents, anti-hypertensive agents and chemotherapeutic agents, or any combination thereof.
[36] In various embodiments of the present invention the predetermined sections of the root of Apiaceae vegetables from which the cosmetically acceptable ingredient is extracted are from either (i) the pericyclic parenchyma, (H) the phloem part, close to the secondary cambium, or a combination thereof.
[37] In some of its embodiments the method comprise selecting predetermined sections of the root of Apiaceae vegetables from the xylem sections for extracting the cosmetically acceptable ingredient thereof.
[38] In some of its embodiment the method comprise selecting the predetermined sections of the root of Apiaceae vegetables from its fiber-containing sections or from its fibrous sections for extracting the cosmetically acceptable ingredient thereof.
[39] In some of its embodiment the method comprise selecting the predetermined sections of the root of Apiaceae vegetables from its colored sections or pigment-containing sections ( e.g. sections comprising carotenes, chlorophylls, carotenoids, flavonoids and phytochrome).
[40] In different embodiments of the method the Apiaceae vegetables are selected from a group consisting of carrot, celery, fennel, parsley, parsnip, or any combination of the same.
[41] In some preferred embodiments the Apiaceae vegetables are of one or more species and types of carrot (Daucus carota L) taproots.
[42] The method according to the invention further provides for selectively inhibiting Gram- negative bacteria contaminating a medium while significantly less inhibiting Gram-positive bacteria in the medium.
[43] The method may also comprise obtaining at least one polyacetylene compound from predetermined sections of the root of Apiaceae vegetables, useful for adjusting the selectivity ratio of the cosmetic composition, e.g. to a selectivity (S) between 1.1 and 10.
[44] The invented method further concerns extracting outer sections of the root of Apiaceae vegetables by means of at least one first solvent until a final extract is obtained.
[45] In some embodiments the method comprises a step of evaporating the extract in a manner that at least a portion of the at least one first solvent is eliminated from the final condensate product. [46] At least one step of re-extracting the obtained condensate by means of at least one second solvent may be a part of the method in yet further embodiments. [47] Re-evaporating the at least one second extract until a dry condensate final product is obtained may be included in the method as well. [48] The at least one first solvent is selected from a group of polar solvents, dipolar aprotic solvents, volatile solvents, water-miscible diluents, organic solvents with high dielectric constants (6.0-9.0), non-polar solvents (hexane, petroleum ether), extractants or any mixtures of the same.
[49] Said at least one first solvent may comprise one or more of the following groups: Group A comprising at least one polar solvent; Group B comprising at least one dipolar solvent; and Group C comprising at least one non-polar solvent.
[50] According to various embodiments of the invention, Group A comprises a first polar solvent and second polar solvent, the volume ratio between the first and second polar solvents ranging from 1 : 10 to 10: 1 (v/v).
[51] According to various embodiments of the invention B comprises a first bipolar solvent and second bipolar solvent, the volume ratio between the first and second bipolar solvents ranging from 1 :15 to 15:1 (v/v).
[52] According to various embodiments of the invention Group C comprises a first non-polar solvent and second non-polar solvent, the volume ratio between the first and second polar solvents ranging from 1 : 12 to 12: 1 (v/v).
[53] In various embodiments of the invention the volume ratio between Group A to B is ranging from 1 :100 to 100:1 (v/v); wherein the volume ratio between Group B to C is ranging from 1 : 100 to 100:1 (v/v); and further wherein the volume ratio between Group A to C is ranging from 1 :100 to 100: 1 (v/v).
[54] More preferably the volume ratio between Group A to B is ranging from 1 :50 to 20:1 (v/v); wherein the volume ratio between Group B to C is ranging from 1:10 to 10:1 (v/v); and further wherein the volume ratio between Group A to C is ranging from 1 :50 to 15:1 (v/v).
[55] The volume ratio between Group A, B and C is from 1 : 1 : 1 to 100: 10: 1 (v/v/v), respectively.
[56] The invention further relates to cosmetics according to the description, characterized in both a proven inhibiting effect towards pathogenic microorganisms located inside the body of a patient and a therapeutic added value. [57] The cosmetic according to the invention may provide for treating acne by inhibiting Gram- positive Propionibacterium acnes bacteria.
[58] A preparation of (i) oral rinse (ii) skin cleanser (iii) soap (e.g., toilet soap, laundry soap) (iv) shampoo (v) tooth brush paste comprising the cosmetic disclosed are also included in the scope of the present invention. .
DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS
[59] The following description is provided, alongside all chapters of the present invention, so as to enable any person skilled in the art to make use of the invention and to set forth the best modes contemplated by the inventor of carrying out this invention. Various modifications, however, will remain apparent to those skilled in the art, without departing from the scope of the present invention.
Example I (extraction)
[60] Carrot taproots were washed in water and peeled. The peels and the core were treated separately by the same procedure: a. 80 g of carrot material were crushed in a homogenizer with 90 ml of a solvent mixture. b. The carrot cells were homogenized by ultrasound for 10 minutes. c. The mixture was frozen at -8O0C for half an hour and lyophilized for 24 hours. d. The carrot material was put in a Soxhlet extractor (referred to also as 'soccelate') system and extracted in 600 ml of a solvent at 1000C for 5 hours, until extraction was completed. e. The desired concentration was achieved by triple boiling of the extract. f. 10 ml of the solution were transferred to Vacuum speedvac for evaporation of the solvents during 24 hrs. g. The substance was emulsified in 5 ml distilled water and subjected to multibio 3D mixing for 24 hours.
[61] A sample of 6 μl of each of the extracts was taken from peels and from core separately and used separately for zone inhibition assays with different microorganisms. [62] Various solvent mixtures characterized by being volatile organic solvents with high dielectric constants (6.0-9.0) were tested. In one embodiment, water, methanol, ethanol and/or acetic acid were utilized as polar solvents. In another embodiment, ethyl acetate was tested as dipolar aprotic solvent. Hexane, heptane and/or benzene were tested as non-polar solvents.
[63] The solvents were denoted by three different groups: Group A comprising at least one polar solvent; Group B comprising at least one dipolar solvent; and Group B comprising at least one non-polar solvent. Various mixtures were tested, whereas combinations of volatile organic solvents with high dielectric constants (6.0-9.0) in acidic conditions and elevated temperature were found effective. Biocidal activity of the extract has been found unaffected (or at least nondestructively affected) by these conditions.
Example II (extraction)
[64] Carrot taproots were washed in water and peeled. The peels and the core were treated separately by the same procedure: a. 80g of carrot material were crushed in a homogenizer with 90 ml of distilled water. b. The carrot cells were homogenized by ultrasound for 10 minutes. c. The mixture was frozen at -800C for half an hour and lyophilized for 24 hours. d. The carrot material was put in a soccelate system and extracted in 600 ml of a solvent mixture at 1000C for 5 hours, until extraction was completed. e. The desired concentration was achieved by triple boiling of the extract. f. 10ml of the solution were transferred to vacuum speedvac for evaporation of solvents during 24 hrs. g. The substance was emulsified in 5ml distilled water and subjected to multibio 3D mixing for 24 hours.
[65] A sample of 6 μl of each of the extracts was taken from peels and from core separately and used separately for zone inhibition assays with different microorganisms. Here again, various mixtures were tested, whereas combinations of volatile organic solvents with high dielectric constants (6.0-9.0) in acidic conditions and elevated temperature were found effective. Example III (test)
[66] A zone inhibition assay was conducted to test the susceptibility of a species of microorganisms according to the diffusion agar assay (DAA) method.
[67] An amount of lOOμl of a culture of a species of microorganism such as bacteria, moulds or yeasts selected from the above list was evenly dispersed on a suitable agar substrate in a Petri plate. A 5-10μl sample of a carrot extract provided by method defined in Example 1 was delicately applied to the microorganism by placing 3mm discs of absorbent paper saturated with the carrot extract on top of the dispersed culture.
[68] The assay was incubated for 24 hours and checked for the appearance of inhibition halos around the absorbent paper discs.
[69] Table 1 was obtained. The term 'Body' refers to the carrot taproot inner section, whereas the term 'Peel' refers to the carrot taproot external sections as defined in the present invention. The term solvents refers to extraction of either the body or peel sections by a solvent mixture, and the term water refers to similar systems whereat the sections were contacted with a water phase.
[70] Table 1 Both water and solvents extracts obtained from outer sections of carrot taproot were more effective inhibiting Gram-negative bacteria (E. coli, a known simulator of the pathogenic H. pylori bacteria) than Gram-positive bacteria (e.g., P. phαseolϊ)
Figure imgf000013_0001
[71] In this test, selectivity value (S) of the biocide, defined as the ratio of
[72] (i) Body the measure of the inner portion of the taproot control sections in inhibiting
Gram-positive bacteria (e.g., P. phαseoli) divided with the measure of its ability in inhibiting Gram-negative bacteria (e.g., H. pylori); and,
[73] (0 Peel the measure of the outer sections of the taproot in inhibiting Gram-positive bacteria divided with the measure of its ability in inhibiting Gram-negative bacteria: Example IV (oral rinse)
[74] An oral rinse and skin cleanser made of carrot extract was produced according to the methods detailed in Example I. Its effective activity is hereby presented in the in vitro ex vivo simulating-systems defined in table 2. Example V (deodorant)
[75] A deodorant simulating system made of carrot extract was produced according to the methods detailed in Example II.
[76] [77] Example VI (water/solvent extracts)
[78] Table 2 Both water extracts and solvents extracts obtained from outer sections of carrot taproots and inner sections of the same.
Figure imgf000014_0001
Example VII (water/solvent extracts)
[79] Table 3 Both water and solvents extracts obtained from outer sections of carrot taproots and inner sections of the same.
Figure imgf000014_0002

Claims

1. A cosmetic composition comprising a cosmetically acceptable ingredient obtainable from predetermined sections of of Apiaceae vegetables' root, the ingredient is characterized in having proven inhibiting effect towards pathogenic microorganisms.
2. The cosmetic composition of claim 1 or to any of its dependent claims, comprising β- carotene free extraction obtained from Apiaceae vegetables.
3. The cosmetic composition of claim 1 or to any of its dependent claims, adapted to be applied dermally either in a continuous or non-continuous manner.
4. The cosmetic according to claim 1 or to any of its dependent claims, wherein the predetermined sections of the root of Apiaceae vegetables are selected from (i) the pericyclic parenchyma, or from (U) the phloem part, close to the secondary cambium, or a combination thereof.
5. The cosmetic according to claim 1 or to any of its dependent claims, wherein the predetermined sections of the root of Apiaceae vegetables are selected from the xylem.
6. The cosmetic according to claim 1 or to any of its dependent claims, wherein the predetermined sections of the root of Apiaceae vegetables are selected from its fibrous sections or fiber-containing sections.
7. The cosmetic according to claim 1 or to any of its dependent claims, wherein the predetermined sections of the root of Apiaceae vegetables are selected from its colored sections or pigment-containing sections; and the said pigments are selected from a group comprising carotenes, chlorophylls, carotenoids, flavonoids and phytochrome.
8. The cosmetic according to claim 1 or to any of its dependent claims, wherein the Apiaceae vegetables are carrot (Daucus carota L) taproots.
9. Use of the cosmetic according to claim 1 or to any of its dependent claims, for selectively inhibiting Gram-negative bacteria contaminating a medium while significantly less inhibiting Gram-positive bacteria in the medium.
10. Use of a cosmetic according to claim 9 or to any of its dependent claims, wherein the selectivity value (S) is between 1.1 to 20.
1 1. A method of providing skin, nails and/or hair care while inhibiting topical pathogenic contaminations of microorganisms in a patient, said method comprising a. obtaining a cosmetically acceptable ingredient obtainable from predetermined sections of the root of Apiaceae vegetables and having proven inhibiting effect towards pathogenic microorganisms; and, b. topically introducing an effective dose of said cosmetic to the skin, nails or hair of a patient.
12. The method according to claim 11 or to any of its dependent claims, comprising selecting the predetermined sections of the root of Apiaceae vegetables from (i) the pericyclic parenchyma, or from (H) the phloem part, close to the secondary cambium, or a combination thereof.
13. The method according to claim 11 or to any of its dependent claims, wherein the Apiaceae vegetables are are carrot (Daucus carota L) taproots.
14. The method according to claim 11 or to any of its dependent claims, comprising selectively inhibiting Gram-negative bacteria contaminating a medium while significantly less inhibiting Gram-positive bacteria in the medium.
15. The method of claim 11, comprising the provision of a biocide having a selectivity value (S) ranging between 1.1 to 20. The method of claim 20 or any of its dependent claim, additionally comprising steps of conditioning the extracted phase to a predetermined pH; wherein the pH is selected from a group consisting of (/) acidic pH ranging from about 2.5 to about 5.5; (H) mild acidic pH ranging from about 55 to about 6.9; (HI) natural pH ranging from about 7.0 to about 7.5; and (iv) mild basic pH ranging from about 7.5 to about 10.0.
16. The method of claim 11 or any of its dependent claims, comprising exposing the extracted phase to temperature ranging from about 75 0C to about 1210C
17. The method of claim 11 or to any of its dependent claims, additionally comprising steps of conditioning the extracted phase to a predetermined water activity (Aw).
18. A cosmetic according to claim 1 or to any of its dependent claims, characterized in both a proven inhibiting effect towards pathogenic microorganisms located inside the body of a patient and a therapeutic added value.
19. Use of a cosmetic according to claim 1 for treating acne by inhibiting Gram-positive Propionibacterium acnes bacteria.
0. A cosmetic according to claim 1, adapted as a preparation of (i) oral rinse (ii) skin cleanser (iii) soap (iv) shampoo (v) tooth brush paste
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