CA2743266A1

CA2743266A1 - Pumpkin and rose hips weight loss composition

Info

Publication number: CA2743266A1
Application number: CA2743266A
Authority: CA
Inventors: Raza Bashir; Ken Clement; Megan Thomas
Original assignee: Northern Innovations and Formulations Corp
Current assignee: Northern Innovations and Formulations Corp
Priority date: 2008-11-17
Filing date: 2009-11-16
Publication date: 2010-05-20
Also published as: WO2010054470A1

Abstract

The present invention relates to methods and compositions for maintaining or reducing body weight through the administration of compositions directed at increasing fat-burning and lipolytic activity, while substantially simultaneously de-creasing fat-storage activity. The compositions disclosed comprise Cucurbita moschata and at least one of Rosa canina, Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, an-hydrous caffeine, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsam-ifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii.

Description

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, 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 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.

[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 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 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.

[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.

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.

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.

Claims

1. A method of maintaining or reducing body fat in a subject comprising providing a composition comprising Cucurbita moschata and at least one of the group consisting of Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, anhydrous caffeine, Rosa canina, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsamifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii to said subject.

2. The method of claim 1, wherein the Cucurbita moschata and the at least one of the group consisting of Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, anhydrous caffeine, Rosa canina, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsamifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii are provided as plant extracts.

3. The method of claim 1, wherein the composition comprises Rosa canina and Cucurbita moschata.

4. The method of claim 3, wherein the Rosa canina comprises trans-tiliroside.

5. The method of claim 1, wherein the composition comprises Cucurbita moschata and Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, or Rosa canina.

6. The method of claim 1, wherein the composition is in the form of powder beverage mixes, liquid beverages, ready-to-eat bars, soft and hard capsules, liquid capsules, tablets, caplets or dietary gels.

7. The method of claim 1, wherein the subject is a mammal.

8. A composition comprising Cucurbita moschata and at least one of the group consisting of Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, anhydrous caffeine, Rosa canina, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsamifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii.

9. The composition of claim 8, wherein the Cucurbita moschata and the at least one of the group consisting of Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, anhydrous caffeine, Rosa canina, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsamifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii are provided as plant extracts.

10. The composition of claim 8, wherein the composition comprises Rosa canina and Cucurbita moschata.

11. The composition of claim 10, wherein the Rosa canina comprises trans-tiliroside.

12. The composition of claim 8, wherein the composition comprises Cucurbita moschata and Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis astaxanthin, or Rosa canina.

13. The composition of claim 8, wherein the composition is in the form of powder beverage mixes, liquid beverages, ready-to-eat bars, soft and hard capsules, liquid capsules, tablets, caplets or dietary gels.

14.A weight loss composition comprising Rosa canina and Cucurbita moschata.

15. The weight loss composition of claim 14, wherein the Rosa canina and Cucurbita moschata are provided as plant extracts.

16. Use of a weight loss composition comprising Cucurbita moschata and at least one of the group consisting of Cissus Quadrangularis, Nelumbo nucifera, Ilex paraguariensis, astaxanthin, Salvia officinalis, Rosmarinus officinalis, Green tea leaf, anhydrous caffeine, Rosa canina, Astragalus membranaceus, Alisma plantago aquatica, Catharanthus roseus, Acorus calamus, Euphorbia balsamifera, Jatropha curcas, Origanum majorana, Zea mays, Capsicum frutescens, Urtica dioica and Pueraria thomsonii for the preparation of a medicament to maintain or reduce body fat in a subject.