US20120121699A1 - Lycopene and resveratrol dietary supplement - Google Patents

Lycopene and resveratrol dietary supplement Download PDF

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Publication number
US20120121699A1
US20120121699A1 US13/320,507 US200913320507A US2012121699A1 US 20120121699 A1 US20120121699 A1 US 20120121699A1 US 200913320507 A US200913320507 A US 200913320507A US 2012121699 A1 US2012121699 A1 US 2012121699A1
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Prior art keywords
lycopene
resveratrol
dietary supplement
composition according
supplement composition
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US13/320,507
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Kun Lung Hsieh
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HSIEHS BIOTECH (SINGAPORE) Pte Ltd
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HSIEHS BIOTECH (SINGAPORE) Pte Ltd
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Assigned to HSIEHS BIOTECH (SINGAPORE) PTE LTD reassignment HSIEHS BIOTECH (SINGAPORE) PTE LTD ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: HSIEH, KUN LUNG
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    • 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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • 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
    • A61K31/01—Hydrocarbons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Definitions

  • This invention generally relates to dietary supplement. It relates specifically to such dietary supplement compositions comprising lycopene and resveratrol exhibiting certain therapeutic effects, including anti-oxidant, anti-arthritis, suppressing carcinoma growth and mitigating hyperlipoidemia.
  • Lycopene with a molecular formula of C 40 H 56 and molecular weight of 536.85, has a molecular structure shown below.
  • lycopene It is a carotenoid and the major target organs and tissues of lycopene in the human body are testis, prostate, liver and intestines. It is found to reduce incidence of prostatic carcinoma, metrocarcinoma, and pancreatic carcinoma more effectively than ⁇ -carotene (Giovannucci E., 1999, Gann P. H., 1999). As early as 1989, lycopene has been found to have the highest activity in quenching oxygen-singlet among all carotenoids including ⁇ -carotene (Di Mascio P.). The anti-oxidative activity of lycopene is found to be about 3.2-fold of that of ⁇ -carotene, and 100 times of that of vitamin E. Applied orally and absorbed through the intestinal tract, lycopene quenches free-radicals and thus protects tissues, cells, and DNA from oxidation by the free-radicals.
  • lycopene is now recognized as a star healthy food supplements in the 21st century and is gaining in popularity world-wide. Especially in developed countries including the U.S., Western Europe, Japan and Israel, huge wealth and efforts have been invested in related researches and in development of lycopene-containing drugs, food supplements, foods and cosmetics since 1990.
  • Resveratrol with a molecular formula C 14 H 12 O 3 and a molecular weight of 228.25, is a terpenoid which is mainly contained in grape skin, peanut, pineapple and knotweed rhizome. This compound appears as an insipidity white crystal powder, slightly soluble in water but soluble in organic solvents such as ethanol and acetone.
  • the structural formula of resveratrol is shown below.
  • Resveratrol is known as an antioxidant, and has been found to decrease blood viscidity, suppress platelet-coagulation, enhance vasodilation and thus promote blood circulation. Because of its hypolipidemic feature, resveratrol plays an important role in preventing atherosclerosis and ischemic heart diseases. Resveratrol also has antineoplastic effect and is a natural substitute of estrogen. Further functionalities of resveratrol include anti-ageing effect, preventing oxidation of low-density lipoprotein (LDL) cholesterol, anti-inflammation and anti-allergic effect.
  • LDL low-density lipoprotein
  • resveratrol The main application of resveratrol is directed to acute infectious hepatitis, menostasis, rheumatism, bone and muscle pain, bronchitis, cholecystolithiasis, hypercholesterol and hypertriglyceride condition.
  • the major target organs and tissues of resveratrol in human body are heart, blood vessels and skins.
  • New Zealand Patent No. 526350 (al-Shakarchi) disclosed lycopene in 0.1-2% w/v and resveratrol in 0.05-1.5% w/v in a preferred combination of a main complex composition which comprises metal salts, amino acids, amino alcohol and vitamin B complex.
  • the lycopene resveratrol disclosed is in the range of 1:15-40:1.
  • a dietary supplement composition comprising lycopene and resveratrol in a range of ratio of lycopene:resveratrol from 1:10 to 10:1.
  • the ratio is 1:2 to 1:4.
  • the lycopene is preferably of ⁇ 95% purity and resveratrol is of ⁇ 98% purity.
  • Both lycopene and resveratrol may preferably comprise of nano-sized particles.
  • the particles are in the form of crystal powder to optimize intestinal absorption upon oral intake in the form of capsule or tablet. In small dosage, it should preferably include a minimum of 5 mg of lycopene and 10 mg of resveratrol.
  • lycopene:resveratrol in a second aspect of our composition, various range of ratios of lycopene:resveratrol are provided for specific therapeutic purposes including 1:4 for symptomatic relief of arthritis, 1:2 for inhibiting melanoma or carcinoma malignancy, and 1:3 for inhibiting hyperlipoidemia.
  • our dietary supplement composition may be used as an agent for anti-ageing, anti-oxidative, inhibiting development of cardiovascular diseases, relieving menopause symptoms and remission of post-operative cancer patients.
  • FIG. 1 is a column chart showing pain index of arthritis patients in placebo group, group treated with resveratrol only, group treated with lycopene only and group treated with combination of both resveratrol and lycopene;
  • FIG. 2 is a line graph illustrating growth of melanoma graft in nude mice: untreated control, treated only with resveratrol, treated only with lycopene and combination of both resveratrol and lycopene;
  • FIG. 3 is a column chart showing triglycerides levels in untreated control group, group treated with resveratrol only, group treated with lycopene only and group treated with combination of both resveratrol and lycopene.
  • Our new composition is formulated based on the results of our research over years which revealed synergistic and complementary effects of the two potent anti-oxidative compounds, i.e. lycopene and resveratrol, as active ingredients.
  • One main aspect of our findings concerns the bioavailability of these two compounds upon oral intake, and their respective distribution or deposition upon uptake in the human body.
  • lycopene and resveratrol are to be admixed in a range of ratio of lycopene:resveratrol from 1:10 to 10:1 with the range of 1:2 to 1:4 considered as optimal ratio.
  • the bio-absorption of the two compounds following oral intake may be increased with the compounds provided in a certain high levels of purity and specific microscopic structural form.
  • “microscopic” we mean particle size of a scale lower than micrometer, i.e. including nanometer and ⁇ scale.
  • Lycopene is preferably provided in purity ⁇ 95% while resveratrol is preferably provided in purity ⁇ 98%. Both compounds are also preferably provided in form of nano-sized particles, particularly micro-crystalline particles, or nano-crystals. These microscopic crystalline forms of lycopene and resveratrol may be produced with suitable conventional controlled recrystallization techniques such as single or multi-solvent solvent recrystallization, hot filtration recrystallization, and seeding, or a proprietary technology such as Elan Pharmaceutical's NanoCrystalTM technology for synthesizing nano-scale crystals optimized for water-solubility.
  • composition comprising lycopene and resveratrol in various ratio are given in the following:
  • our dietary supplement may be formulated as having, for example, 5 mg of lycopene and 10 mg of resveratrol in a 15 mg capsule or tablet.
  • Conventional methods may be employed to make tablets such as the use of binding agent such as starch and/or magnesium stearate.
  • binding agent such as starch and/or magnesium stearate.
  • lycopene resveratrol composition in 1:3 ration 100 grams of lycopene with a purity of 95% and 300 g of resveratrol with a purity of 98% may be mixed with 40 g starch, and then mixed with 200 g starch slurry before tablet-making.
  • the second major aspect of our present invention concerns certain combination ratios of lycopene to resveratrol for therapeutic use in specific ailments including arthritis, carcinoma generally and melanoma specifically, and in mitigating hyperlipoidemia.
  • resveratrol e.g. 400 mg/person/day
  • lycopene e.g. 100 mg/person/day
  • Five grades were designed for patients to define their painfulness.
  • FIG. 2 Inhibition of melanoma growth is shown in FIG. 2 where the subjects are C57 mouse which are grafted with B16 murine melanoma tumour cells. From the line graph of FIG. 2 , it is apparent that the combination of both lycopene and resveratrol has synergistic effect in suppressing growth of melanoma grafts.
  • the optimal ratio of lycopene: resveratrol is suggested to be in the range of 1:2 for efficacious suppression of growth of carcinoma including melanoma.
  • a man with a tonsil tumor sized 3 ⁇ 3 cm reported shrinkage of the tumor a size below the detectable range of magnetic resonance imaging after three-month intake of our dietary supplement comprising lycopene and resveratrol according to the aforesaid ratio.
  • our dietary supplement comprising lycopene and resveratrol according to the aforesaid ratio.
  • the combination of resveratrol and lycopene showed synergistic effect in suppressing growth of tumor.
  • Further health promoting effects of our preparation of lycopene and resveratrol may be expected to include anti-ageing, anti-oxidative, inhibiting cardiovascular diseases, relieving menopause symptoms and remission of post-operative cancer patients.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Botany (AREA)
  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
  • Nutrition Science (AREA)
  • Mycology (AREA)
  • Toxicology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
US13/320,507 2009-05-14 2009-08-27 Lycopene and resveratrol dietary supplement Abandoned US20120121699A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SG200903301-0A SG166688A1 (en) 2009-05-14 2009-05-14 Lycopene and resveratrol dietary supplement
SG200903301-0 2009-05-14
PCT/SG2009/000300 WO2010132021A1 (fr) 2009-05-14 2009-08-27 Complément alimentaire à base de lycopène et de resvératrol

Related Parent Applications (1)

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PCT/SG2009/000300 A-371-Of-International WO2010132021A1 (fr) 2009-05-14 2009-08-27 Complément alimentaire à base de lycopène et de resvératrol

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US14/536,245 Continuation US9610255B2 (en) 2009-05-14 2014-11-07 Lycopene and resveratrol dietary supplement

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US (2) US20120121699A1 (fr)
EP (1) EP2429508B1 (fr)
JP (1) JP2012526806A (fr)
KR (1) KR101755350B1 (fr)
CN (1) CN102438605B (fr)
DK (1) DK2429508T3 (fr)
HK (1) HK1170182A1 (fr)
SG (3) SG166688A1 (fr)
TW (1) TWI430802B (fr)
WO (1) WO2010132021A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103690487A (zh) * 2013-12-17 2014-04-02 武汉工程大学 一种无载体微纳米白藜芦醇药物及其制备和应用
US9669006B2 (en) 2015-07-28 2017-06-06 U.S. Nutraceuticals, LLC Composition and method to treat and alleviate symptoms of hot flashes in a female subject

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG166716A1 (en) * 2009-05-14 2010-12-29 Hsiehs Biotech Singapore Pte Ltd Lycopene and resveratrol compositions for nk cell activation resulting in anti-neoplastic effect
JP5948871B2 (ja) * 2011-12-28 2016-07-06 株式会社東洋新薬 ポリフェノール含有組成物
JP5901547B2 (ja) * 2012-03-28 2016-04-13 富士フイルム株式会社 組成物、これを含む皮膚外用剤、又は機能性食品
AU2017100368A4 (en) * 2016-09-23 2017-05-18 The University Of Newcastle Methods for improving cerebrovascular function and cognition in peri- and post-menopausal women
JP2018172346A (ja) * 2017-03-31 2018-11-08 株式会社東洋新薬 妊娠サポート用組成物
JPWO2023008218A1 (fr) * 2021-07-28 2023-02-02
WO2023143988A1 (fr) 2022-01-26 2023-08-03 Eth Zurich Nouveaux composés et leur utilisation comme agent anti-âge ou comme activateur d'exercice

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US20060020046A1 (en) * 2002-02-15 2006-01-26 Dms Ip Assets B.V. Compositions comprising lycopene for the treatment and prevention of angiogenesis associated pathologies
WO2004000043A2 (fr) * 2002-06-21 2003-12-31 Dietetic S.P.A. Compositions nutraceutiques et supplements alimentaires renfermant du nadh
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103690487A (zh) * 2013-12-17 2014-04-02 武汉工程大学 一种无载体微纳米白藜芦醇药物及其制备和应用
US9669006B2 (en) 2015-07-28 2017-06-06 U.S. Nutraceuticals, LLC Composition and method to treat and alleviate symptoms of hot flashes in a female subject
US10172826B2 (en) 2015-07-28 2019-01-08 U.S. Nutraceuticals, LLC Composition and method to treat and alleviate symptoms of hot flashes in a female subject

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CN102438605B (zh) 2013-11-27
HK1170182A1 (en) 2013-02-22
JP2012526806A (ja) 2012-11-01
SG10201402135QA (en) 2014-10-30
CN102438605A (zh) 2012-05-02
WO2010132021A1 (fr) 2010-11-18
EP2429508B1 (fr) 2015-12-16
SG166688A1 (en) 2010-12-29
US20150132373A1 (en) 2015-05-14
US9610255B2 (en) 2017-04-04
KR101755350B1 (ko) 2017-07-07
KR20120028891A (ko) 2012-03-23
EP2429508A4 (fr) 2013-05-29
EP2429508A1 (fr) 2012-03-21
DK2429508T3 (en) 2016-01-11
SG176070A1 (en) 2011-12-29
TWI430802B (zh) 2014-03-21
TW201039838A (en) 2010-11-16

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