FATMODIX PRO: MODULATION OF FAT TASTE PERCEPTION USING GYMNEMIC ACID AND FLAVONE DERIVATIVE IN LOZEN

Abstract

The current invention relays to a novel technique for modulating the perception of dietary fats, leveraging the unique properties of gymnemic acids derived from Gymnema sylvestre in combination with a flavone derivative. The invention targets fat taste receptors, specifically CD36 and. GPR120, and interferes with the PLC~2 signaling pathway to alter fat taste perception. By incorporating gymnemic acids and flavone derivatives into a slow-dissolving oral formulation, such as a lozenge, the invention effectively reduces the preference associated with consuming fatty foods, thereby aiding in the management of dietary fat intake and promoting healthier eating habits. This approach offers potential applications in dietary management, food products, and therapeutic interventions aimed at reducing fat consumption and improving overall health outcomes. The invention also describes a method for stabilizing gymnemic acids during extraction to maintain their efficacy in modulating fat taste.

Specification

The present invention pertains to the fieid of taste modification, particularly focusing on the
modulation of fat taste perception. Specifically, it involves the use of a combination of
Gymnema sylvestre extracts gymnemic acids into a lozenge and flavone derivatives to alter fat
taste by influencing fat taste receptors such as CD36 and GPR120, as well as interfering with
key signaling pathways like PLC2. This invention has applications in dietary management,
food products, and therapeutic interventions aimed at reducing fat consumption and improving
overall health outcomes.
The consumption of Gymnema sylvestre leaves known to eliminate the perception of
sweetness for a few hours after chewing them. This characteristic earned the herb the name
"gurmar," meaning "sugar destroyer." For instance, a century ago, Captain Edgeworth
experienced this effect when villagers from India introduced them to the plant; after chewing
the leaves, the sweetness in their tea disappeared. This effect is attributed to gymnemic acid, the
active compound in Gymnema sylvestre, which temporarily blocks sweet receptors on the
tongue, preventing the perception of sweetness in foods consumed afterward. Over the years,
researchers have isolated gymnemic acid as the key agent responsible for this suppression of
sweetness. Studies such as "Antisweet Activity of Gymnemic Acid A1 and Its Derivatives"
(Kurihara, 1969) and "Gymnemic Acid, the Antisaccharine Principle of Gymnema sylvestre"
(Dateo et al., 1973) have explored its effectiveness in blocking sweetness, typically by
administering oral rinses of gymnemic acid. Gymnemic acid has since been used in various oral
compositions, including chewable gums and tablets, as dietary aids, as disclosed in US. Patent
US-5605698-A to Ueno.
Several patents highlight its role in diabetes treatment. For example, Patent US-5980902
by Shanmugasundaram et al. details the application of GS as augment to help regulate blood
sugar levels in diabetic patients. Similarly, Patent US- 5900240 by Tomer supports its
effectiveness as a dietary supplement for reducing blood glucose levels in those with diabetes
mellitus. U.S. Patent No. 5730988 by Womack discusses its potential to block glucose
absorption in the intestines, while Patent US- 4 761286 by Hiji also explores its glucose
inhibition properties. Its benefits extend beyond metabolism, as Patent US-49120R9 hy Hiji
mentions its ability to help prevent the formation of dental plaque, contributing to improved
oral health.
The present invention builds upon these findings but extends the application of
Gymnema sylvestre beyond sweetness suppression to include fat taste modification. Gymnemic
acid, when incorporated into a pleasant-tasting lozenge or similar slow-dissolving oral
formulation, is distributed evenly throughout the mouth, occupying and blocking fat receptors.
In addition, the present invention utilizes flavone derivative to modify the perception of dietary
fat, reducing the pleasure associated with consuming fatty foods. This combined approach
creates a novel method of modifying taste, particularly for fats and sweets. The suppression of
fat taste helps to reduce cravings for calorie-dense foods. The lozenge, by gradually releasing
the active ingredients, blocks the taste receptors responsible for fat taste, leading to an aversion
to these food types. Over time, the user develops healthier eating habits by naturally avoiding
sweet and fatty foods.
To gain a stronger intellect of the type and intents of the current invention, reference is
made to the detailed description provided below, in conjunction with the accompanying
drawings, where corresponding parts are indicated by consistent reference characters across the
various figures. The objects, features, and advantages of the disclosed embodiments can be
better appreciated through the following description and accompanying illustrations. The
drawings are not intended to restrict the scope of the claims but rather to clarify key concepts,
principles, and embodiments. Not all elements may be labeled in every figure, and the drawings
may not be to scale, as the focus is on effectively illustrating the concepts. Accordingly, the
features and benefits of the invention will become more evident from the detailed description of
exemplary embodiments, presented alongside the drawings.
Flavones are well-known for their bitter taste properties, and various methods have been
explored to alter taste sensations - such as sourness, saltiness, sweetness, and overall flavour -
in products including foods, cosmetics, and pharmaceuticals. Methods to modify fat perception
often involve altering lipid types, while effective, these methods can cause browning reactions
and alter physical and chemical properties, limiting their applicability. The present invention
extends these insights into the modification of fat taste.
Research has demonstrated that gymnemic acids derivative from Gymnema sylvestre are
effective in modulating taste sensations, particularly with regard to dietary fats. Gymnemic
acids, characterized by the general formula (1), can be categorized into four types based on their
functional groups F,, F,, and F,, as shown in Figure I. The present invention innovatively targets the modification of fat taste by altering the
expression of fat taste receptors, such as CD36 or GPR120, or by blocking the phospholipase C
beta 2 (PLC~2) signaling pathway. Gymnemic acids affect fat taste perception by modulating
these mechanisms, thereby altering the perception of fat taste without relying on traditional
methods that may cause undesirable side effects. The invention provides a novel approach for
modifying fat taste perception, leveraging Gymnema sylvestre and flavone derivatives to
enhance dietary fat taste modulation. By influencing fat taste receptors or blocking specific
signaling pathways, this method offers a unique solution for improving taste quality and aiding
in dietary management
The technical and scientific terms used in this document should be interpreted as they are
generally understood by professionals skilled in the relevant field, unless specifically redefined
herein. The definitions provided are intended to clarify the current application and should not
be applied to any other cases, including those that may be related or under common ownership.
While similar or equivalent methods and materials to those described here may be used in
practice or testing, the preferred approaches are outlined in this document. Thus, the
terminology presented is meant to describe specific embodiments and is not intended to impose
any limitations. The current invention associates to a technique for altering fat taste perception
using extracts of Gymnema sylvestre, specifically targeting fat taste receptors and associated
signaling pathways. The invention is based on the discovery that gymnemic acids, compounds
extracted from Gymnema sylvestre, can alter fat taste perception by modulating the expression
of fat taste receptors such as CD36 or GPR 120 or by inhibiting the phospholipase C beta 2
(PLCP2) pathway.
Composition and Structure of Gymnemic Acids
Gymnemic acids, the active compounds extracted from Gymnema sylvestre, are represented by
the general formula (I) and can be classified into four types (I, 2, 3, and 4) depending on the
functional groups F,, F,, and F,. As depicted in Figure I, these functional groups may include
tigroyl, 2-methyl butyroyl, acetyl, or hydrogen atoms. These gymnemic acids, through lheir
unique molecular structure, interact with fat taste receptors in a way that diminishes the
perception of fat. The presence of acyl groups in gymnemic acids significantly influences their
effectiveness in modulating taste sensations.
Mechanism of Action
The invention targets thy modification of fat taste perception through three pnmary
mechanisms:
I. Modulation of Fat Taste Receptors CD36 and GPR120:
CD36 and GPR 120 are key receptors involved in the detection of dietary fats.
Gymnemic acids have been found to modulate the expression or activity of these
receptors, leading to a decrease in the intensity of fat taste perception. By influencing
the expression of these receptors on the tongue, the compounds can alter how dietary
fats are perceived, reducing their palatability or richness.
2. Inhibition of the PLCIJ2 Pathway:
The phospholipase C beta 2 (PLCP2) pathway plays a significant role in taste signal
transduction, particularly in the gustatory system. When fats are detected by the taste
buds, this pathway is activated, leading to the sensation of fat taste. Gymnemic acids
block this pathway, thereby interfering with the signal that transmits the sensation of fat
taste to the brain. By inhibiting PLCP2, gymnemic acids effectiv ly dampen The gymnemic acids exhibit a dose-dependent effect on fat taste perception. For example,
gymnemic acids (I) and (2), with both F, and F, acylated, show greater activity in modulating
fat taste as compared to gymnemic acids (3) and (4), where only one acyl group is present. This
suggests that the presence and number of acyl groups are critical for the efficacy of the
gymnemic acids in taste modification. The mechanism by which gymnemic acids modulate fat
taste involves their interaction with CD36 and GPR 120 receptors, which play key roles in fat
taste detection, as well as the inhibition of the PLC~2 pathway, which transduces fat taste
signals to the brain. By affecting these pathways, gymnemic acids reduce the intensity of fat
taste, thereby decreasing the perceived richness and palatability of high-fat foods.
Applications
The invention can be applied in various tields, including food and beverage manufacturing,
pharmaceuticals, and nutraceuticals. It is particularly valuable in· the development of functional
foods designed to promote healthier eating habits by reducing the appeal of high-fat foods
Claim 1: A method for modulating fat taste perception in mammals compnsmg the
administration of a composition containing gymnemic acids derived from Gymnema
sylvestre and a flavone derivative, wherein said gymnemic acids interact with fat
taste receptors, CD36 and GPRI20, and inhibit the PLC~2 signaling pathway.
Claim 2: The composition of Claim I, wherein the gymnemic acids are selected from the
group consisting of gymnemic acid (I), gymnemic acid (2), gymnemic acid (3), and
gymnemic acid (4), with each having varying degrees of acylation at F,, Fz, and F,
positions.
Claim 3: The method of Claim I, wherein the composition is provided in a slow-dissolving
oral formulation such as a lozenge, which gradually releases the active ingredients
in the oral cavity to block the taste receptors responsible for fat taste perception.
Claim 4: A method of reducing dietary fat consumption in a subject, compnsmg the
administration of the composition of Claim I, resulting in decreased preference
associated with consuming fatty foods and subsequent reduction in fat intake.
Claim 5: The composition of Claim I, wherein the flavone derivative is represented by the
compound (I) and is used to develop the fat taste modulation effect of the
gymnemic acids.
Claim 6: The method of Claim I, wherein the modulation of fat taste perception leads to longterm
changes in dietary habits by reducing cravings for calorie-dense foods, thus
aiding in weight management and overall health improvement

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