Note : Les descriptions sont présentées dans la langue officielle dans laquelle elles ont été soumises.
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
PUMPKIN AND ROSE HIPS WEIGHT LOSS COMPOSITION
Field of the Invention
[0001] The present invention relates to compositions and methods for
maintaining or reducing body weight in mammals. More specifically, the present
invention relates to combinations of herbal ingredients for supporting weight
loss.
Summary of the Invention
[0002] It is an object of the present invention to provide methods and
compositions for supporting weight loss directed at impinging specific
biochemical pathways.
[0003] The present invention provides a method of maintaining or reducing the
body weight of subjects by promoting an increase in lipolysis and promoting a
decrease in lipogenesis, in subjects.
[0004] According to one embodiment of the present invention, a method for
promoting weight loss is provided comprising administration of a composition
comprising Cucurbita moschata and at least one of the group consisting of Rosa
canina, Cissus Quadrangularis, Nelumbo nucifera, flex paraguariensis,
astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf,
anhydrous
caffeine, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus
roseus, Acorus ca/amus, Euphorbia ba/samifera, Jatropha curcas, Origanum
majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii.
In certain embodiments, the composition ingredients are provided as plant
extracts. In particular embodiments, the composition comprises Rosa canina and
Cucurbita moschata, and the Rosa canina comprises trans-tiliroside.
[0005] According to another embodiment of the present invention, a composition
is provided comprising Cucurbita moschata and at least one of the group
consisting of Rosa canina, Cissus Quadrangularis, Nelumbo nucifera, flex
paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green
tea
leaf, anhydrous caffeine, Astragalus membranaceus, Alisma plantago aquatica,
Catharanthus roseus, Acorus ca/amus, Euphorbia ba/samifera, Jatropha curcas,
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria
thomsonii. In certain embodiments, the composition is a weight loss
composition,
and may comprise Rosa canina and Cucurbita moschata. The Rosa canina and
Cucurbita moschata may be provided as plant extracts.
Detailed Description of the Invention
[0006] In the following description, for the purposes of explanation, numerous
specific details are set forth in order to provide a thorough understanding of
the
present invention. It will be apparent, however, to one skilled in the art
that the
present invention may be practiced without these specific details.
[0007] The present invention, according to the various embodiments thereof, is
directed to methods and compositions for maintaining or reducing body weight.
This is achieved by providing compositions, and methods employing said
compositions, directed at increasing lipolysis, while substantially
simultaneously
decreasing lipogenesis.
[0008] As used herein, the term "maintaining or reducing body fat" refers to
the
act or a state of a static amount of body fat or a dynamic state of decreasing
body
fat. It is herein understood that the amount of body fat is regulated by
multiple
mechanisms, such as, for example, fat synthesis, fat esterification and fat
storage
(collectively, herein termed lipogenesis), and fat oxidation, fat breakdown
and fat
mobilization (collectively, herein termed lipolysis). Furthermore, it is
herein
understood that the amount of body fat may be maintained or reduced by
affecting any mechanism, both directly or indirectly, that regulates the
amount of
body fat, and that affecting multiple fat regulation mechanisms will have
greater
efficacy than affecting any single mechanism. It is herein understood that
decreasing lipogenesis and/or increasing lipolysis will advantageously
maintain or
reduce body fat.
[0009] As used herein, the term "subject" refers to mammals and non-mammals.
Mammals refers to any member of the Mammalia class including, but not limited
to, humans; non-human primates such as chimpanzees and other apes and
monkey species; farm animals such as cattle, horses, sheep, goats, and swine;
domestic animals such as rabbits, dogs, and cats; laboratory animals including
-2-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
rodents, such as rats, mice, and guinea pigs; and the like. Examples of non-
mammals include, but are not limited to, birds, and the like. In preferred
embodiments of the present invention the subjects are human.
[0010] As used herein, the term "oral administration" refers to acceptable
oral
dosage forms taken by conventional routes of administration known by one of
skill in the art and include, for example, powder beverage mixes, liquid
beverages, ready-to-eat bars, soft and hard capsules, liquid capsules,
tablets,
caplets and dietary gels. The preferred dosage forms of the present invention
are
caplets and capsules.
[0011] Furthermore, the dosage form of the nutritional supplement is provided
in
accordance with customary processing techniques for herbal and nutritional
supplements in any of the forms mentioned above. Additionally, the nutritional
supplement set forth in the example embodiment herein disclosed may contain
any appropriate number and type of excipients, as is well known in the art.
[0012] As used herein, the term "plant extracts" refers to whole plant or any
portion(s) thereof, fresh or dried, treated by any means as are commonly known
to those of skill in the art, to obtain a portion which contains one or more
active
compounds. Such extracts are typically liquid but may subsequently be provided
as a dry powder. Preferably, the extracts are standardized to some know
compound present in the isolated extract. Examples of common extracts methods
include aqueous and alcohol extractions. Those of skill in the art will also
know of
the various suitable solvents such as methylene dichloride, acetone, ethanol,
methanol, methanol/chloroform/water and water. Extracts, as used herein,
includes both crude extracts and extracts obtained from more elaborate methods
such as solid-phase extraction, solid-phase microextraction, supercritical-
fluid
extraction, pressurized-liquid extraction, microwave-assisted extraction, and
surfactant-mediated extraction. Plant extract, as used herein, may also
include
extracted oils such as those referred to as essential oils. Alternatively,
forms of
unprocessed, or raw, plants may be used in embodiments of the present
invention. Such forms may be whole or part and may be fresh or dried. In
preferred embodiments of the present invention, plant extracts are used.
-3-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
[0013] As used herein, the term `nutritional composition' includes dietary
supplements, diet supplements, nutritional supplements, supplemental
compositions and supplemental dietary compositions or those similarly
envisioned and termed compositions not belonging to the conventional
definition
of pharmaceutical interventions as is known in the art. Furthermore,
`nutritional
compositions' as disclosed herein belong to category of compositions having at
least one physiological function when administered to a subject by
conventional
routes of administration.
[0014] Alternatively, formulations and nutritional compositions belonging
to the present invention may be considered to be nutraceuticals. As used
herein,
the term `nutraceutical' is recognized and used in the art to describe a
specific
chemical compound or combination of compounds found in, organic matter for
example, which may prevent, ameliorate or otherwise confer benefits against an
undesirable condition. As is known in the art, the term `nutraceutical' is
used to
refer any substance that is a food, a part of food, or an extract of food
which is
suitable for consumption by an individual and providing physiological benefit
which may be medical or health-related. Furthermore, the term has been used to
refer to a product isolated, extracted or purified from foods or naturally-
derived
material suitable for consumption by an individual and usually sold in
medicinal
forms, such as caplets, tablet, hard and soft capsules, and the like, not
associated with food.
[0015] In accordance with various embodiments of the present invention, one or
more components are processed so as to form fine-milled particles. For
instance,
in various embodiments, one or more ingredients of the dietary supplemental
are
processed by a large-scale milling technique that produces fine particles that
have a smaller average particle size. The use of milling techniques, in
combination with excipients and polymers, to form fine-milled particles has
been
shown to improve flow and dispersability, stability, resistance to moisture,
bioavailability, and dissolution/release properties. Formulations benefit by
containing fine-milled particles for the purpose of providing the one or more
ingredients in particle sizes that optimize one or more of: the flow and
dispersability, stability, resistance to moisture, bioavailability, and
-4-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
dissolution/release properties of the one or more ingredients in a dietary
supplement.
[0016] One of the main modulators of lipolysis is the peroxisome proliferator-
activated receptor (PPAR) family, a family of nuclear receptors involved in
energy
homeostasis. Three types are known in humans: PPAR-a, PPAR-y and PPAR-b.
PPAR-a is predominantly expressed in liver and regulates fatty acid
catabolism.
PPAR-y is expressed primarily in adipose tissue and is involved in regulating
adipogenesis and fat storage. PPAR-b is expressed in several tissue types.
Activation of PPARs leads to and improved glucose and lipid homeostasis.
Specific activation of PPAR-a results in increased lipid oxidation. PPAR
agonists
are a class of pharmaceutical intervention aimed at treating several
conditions,
including obesity. Both selective PPAR-a agonists and various combination
therapies have been shown to be efficacious.
[0017] Several other factors involved in lipolysis are known such as the
enzymes Lipoprotein lipase (LPL), Acyl-CoA oxidase-1 (ACO-1), carnitine
palmitoyltransferase-1 (CPT-1). Uncoupling proteins (UCPs) are also factors
involved in lipolysis. They act to disconnect food metabolism and ATP
production,
allowing energy to be dissipated as heat.
[0018] Several other factors are known that are involved in fat metabolism in
the
context of lipogenesis. Sterol Regulatory Element Binding Protein-1 c (SREBP-1
c)
is a transcription factor that regulates genes involved in fatty acid
synthesis, two
such target genes being the enzymes stearoyl-CoA desaturase (SCD) and fatty-
acid synthase (FAS). Another important lipogenic enzyme is acetyl-coenzyme A
carboxylase (ACC).
[0019] It is understood that other genes and their respective protein products
involved in fat metabolism, aside from those specifically disclosed herein,
may be
included within the scope of the present invention.
[0020] Rosa canina L. is a prickly shrub found in Scotland and other parts of
Europe. Traditionally the fruit of this plant have been used as diuretic,
laxative
and for anti-gout purposes. The principal constituent, trans-tiliroside, has
been
shown to increase the expression of PPAR-a. Several other plants have reported
-5-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
PPAR agonist activity, including Salvia officinalis (Sage), Rosmarinus
officinalis
(Rosemary), Astragalus membranaceus, Alisma plantago aquatica, Catharanthus
roseus, Acorus ca/amus, Euphorbia ba/samifera, Jatropha curcas, Origanum
majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii.
[0021] Embodiments of the present invention comprise at least one compound
that increases lipolysis in a subject. It is herein understood that increasing
lipolysis in a subject will act to maintain or reduce body fat in the subject.
The
preferred route of increasing lipolysis is through modulating PPAR activity.
It is
herein understood that increasing PPAR activity, preferably PPAR-a activity,
will
increase lipolysis, thereby acting to decrease body fat. Preferred embodiments
of
the present invention comprise Rosa canina as a source of compound that
increases PPAR activity. The preferred PPAR activity increasing compound is
trans-tiliroside.
[0022] Alternatively, various embodiments of the present invention may include
one or more compound that increases the activity of a lipolytic factor other
than
(or in addition to) PPAR. Astaxanthin is known to increase CPT-1 activity.
Nelumbo nucifera is an aquatic plant that has demonstrated activity towards
increasing UCP-3 activity. Ilex paraguariensis (also known as Yerba mate) is a
common tree in Southern Brazil, Northeastern Argentina, Paraguay and Uruguay
that may increase UCP2 and UCP3 expression
[0023] Cucurbita moschata, commonly called pumpkin, has displayed anti-
obesity effects in mouse models. Oral administration of an extract of
Cucurbita
moschata decreased the weights of various adipose tissues. The size of the
adipocytes and thickness of fat pad in subcutaneous area was also markedly
decreased in treated animals. The mRNA level of SREBP-Ic and SCD-1 and FAS
were markedly decreased in treated mice, while the mRNA of lipolytic factors
PPAR-a, ACO-1, CPT-1, and UCP-2 were increased. This indicates that oral
administration of Cucurbita moschata may suppress body fat accumulation by
down-regulating mRNA expression of lipogenic genes and up-regulating the
expression of lipolytic genes.
-6-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
[0024] It is herein understood that the activity of any factors controlling or
regulating any aspect of fat metabolism may be modulated through dietary
interventions such as those of the present invention. Furthermore, such
interventions may exert said modulations through effecting any biological,
chemical or biochemical pathway such as those including but not limited to:
DNA
replication or amplification, RNA transcription, RNA stability, RNA
translation,
post-translational modifications such as phosphorylation, ligand binding, and
transport, either directly or indirectly. Accordingly, such interventions are
supportive of promoting weight loss.
[0025] The methods and compositions of the present invention are suited for
use for individuals wishing to maintain or reduce their body weight at the
expense
of body fat. Advantageously, the methods and compositions of the present
invention may be used in combination with other like-directed ingredients or
compositions to maintain or reduce their body weight. Other like-directed
ingredients or compositions will be known by those of skill in the art.
-7-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
Examples
Example 1
[0026] A composition for supporting weight loss in an individual comprising
the
following ingredients per serving is prepared for consumption as 2 caplets to
be
consumed twice daily:
about 1.5 g Cucurbita moschata and about 0.06 g Rosa canina.
Example 2
[0027] A composition for supporting weight loss in an individual comprising
the
following ingredients per serving is prepared for consumption as 2 caplets to
be
consumed twice daily:
about 1.5 g Cucurbita moschata and about 0.06 g Rosa canina
(standardized to trans-tiliroside 40%).
Example 3
[0028] A composition for supporting weight loss in an individual comprising
the
following ingredients per serving is prepared for consumption as 2 caplets to
be
consumed twice daily:
about 1.5 g Cucurbita moschata, about 0.06 g Rosa canina, about 0.2 g
anhydrous caffeine, about 0.15 g Cissus Quadrangularis, and about 0.46 g
Green tea leaf (standardized to 45% EGCG, 75% catechins, 90%
polyphenols).
Example 4
[0029] A composition for supporting weight loss in an individual comprising
the
following ingredients per serving is prepared for consumption as 2 capsules to
be
consumed twice daily:
about 1.5 g Cucurbita moschata, about 0.06 g Rosa canina, about 0.2 g
anhydrous caffeine, about 0.001 g astaxanthin, about 0.001 g Nelumbo
nucifera.
-8-
CA 02743266 2011-05-10
WO 2010/054470 PCT/CA2009/001621
Extensions and Alternatives
[0030] In the foregoing specification, the invention has been described with
specific embodiments thereof; however, it will be evident that various
modifications and changes may be made thereto without departing from the
broader spirit and scope of the invention.
[0031] All publications which are cited herein are hereby specifically
incorporated by reference into the disclosure for the teachings for which they
are
cited.
-9-
