Compositions and methods for controlling carbohydrate and fat metabolism

Inventors

Peltier, SebastienSirvent, PascalMaugard, Thierry

Assignees

Centre National de la Recherche Scientifique CNRSLa Rochelle UniversiteUniversite Clermont AuvergneValbiotis SA

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Publication Number

US-10736930-B2

Patent

Publication Date

2020-08-11

Expiration Date


Abstract

A composition comprising at least: a single extract obtained from a mixture of at least two plants selected from Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus, Piper and Olea europaea. This composition is particularly useful as a nutritional product or health product for preventing and/or combating carbohydrate and/or fat metabolism disorders in humans and animals.

Core Innovation

The invention relates to a composition comprising a single extract obtained from a mixture of at least two plants selected from Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus, Piper and Olea europaea. The composition further comprises at least one molecule selected from apigenin 7-O-glucuronide, chrysanthellin A, chrysanthellin B, caffeic acid, luteolin, maritimetin, eriodictyol, isookanin, apigenin, luteolin 7-O-glucoside, maritimein, marein, eriodictyol 7-O-glucoside, flavomarein, apigenin 8-C-α-L-arabinoside-6-C-β-D-glucoside (shaftoside), apigenin 6,8-C-di-β-D-glucopyranoside (vicenin-2), dicaffeoylquinic acid, sulfo-monocaffeoylquinic acid, luteolin 7-O-glucuronide, apigenin 7-O-glucoside, cynaropicrin, or analogs thereof, as well as at least one molecule selected from monocaffeoylquinic acid, delphinidin 3-galactoside, delphinidin 3-glucoside, cyanidin 3-galactoside, delphinidin 3-arabinoside, cyanidin 3-glucoside, petunidin 3-galactoside, cyanidin 3-arabinoside, petunidin 3-glucoside, peonidin 3-galactoside, petunidin 3-arabinoside, peonidin 3-glucoside, malvidin 3-glucoside, malvidin 3-arabinoside, or analogs thereof. The composition also comprises at least one molecule selected from oleuropein, hydroxytyrosol, and analogs thereof, and defines a “mixture” and a “single extract” from plant mixes.

The invention further describes extracts from Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus plus piperine, optionally including Olea europaea, together with formulation and excipient options and named constituents including apigenin 7-O-glucuronide and chrysanthellins, as well as flavonoids and phenolics such as caffeic and quinic acids and anthocyanins. The single extract is not obtained from a mixture of five plants: Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus, Piper and Olea europaea.

The problem being solved is preventing or combating carbohydrate and fat metabolism disorders, notably type 2 diabetes and non-alcoholic steatohepatitis (NASH), and also cardiovascular risks, by addressing carbohydrate metabolism and fat metabolism. In vivo db/db mouse studies show reductions in fasting glycemia, improved carbohydrate tolerance and insulin sensitivity, decreased body/fat mass, improved lipid markers such as HDL increase and triglyceride reduction, and increased hepatic AMPK, while in vitro enzyme inhibition targets HMG-CoA reductase, α-glucosidase, and DPP-IV.

Claims Coverage

The partial content identifies one independent claim. It covers a composition defined by a single extract obtained from a specified mixture of at least two plants, with selected molecules in the extract and/or added, plus oleuropein, hydroxytyrosol, or analogs, while excluding the specific five-plant mixture scenario.

Single extract from a mixture of at least two selected plants

A composition comprising at least a single extract obtained from a mixture of at least two plants selected from Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus, Piper and Olea europaea.

Selected molecules present in and/or added to the single extract

The composition comprises at least one molecule selected from apigenin 7-O-glucuronide, chrysanthellin A, chrysanthellin B, caffeic acid, luteolin, maritimetin, eriodictyol, isookanin, apigenin, luteolin 7-O-glucoside, maritimein, marein, eriodictyol 7-O-glucoside, flavomarein, apigenin 8-C-α-L-arabinoside-6-C-β-D-glucoside (shaftoside), apigenin 6,8-C-di-β-D-glucopyranoside (vicenin-2), dicaffeoylquinic acid, sulfo-monocaffeoylquinic acid, luteolin 7-O-glucuronide, apigenin 7-O-glucoside, cynaropicrin, or analogs thereof, and at least one molecule selected from monocaffeoylquinic acid, delphinidin 3-galactoside, delphinidin 3-glucoside, cyanidin 3-galactoside, delphinidin 3-arabinoside, cyanidin 3-glucoside, petunidin 3-galactoside, cyanidin 3-arabinoside, petunidin 3-glucoside, peonidin 3-galactoside, petunidin 3-arabinoside, peonidin 3-glucoside, malvidin 3-glucoside, and malvidin 3-arabinoside, or analogs thereof.

Oleuropein and hydroxytyrosol constituents

The composition also comprises at least one molecule selected from oleuropein, hydroxytyrosol, and analogs thereof.

Exclusion of the five-plant mixture scenario

The single extract is not obtained from a mixture of five plants: Chrysanthellum indicum, Cynara scolymus, Vaccinium myrtillus, Piper and Olea europaea.

Overall, the independent claim is directed to a composition defined by a single extract from a mixture of at least two specified plants, together with defined small molecules present in and/or added to that extract, plus oleuropein, hydroxytyrosol, or analogs, while explicitly excluding the case where the single extract is obtained from the five-plant mixture.

Stated Advantages

Reductions in fasting glycemia.

Improved carbohydrate tolerance and insulin sensitivity.

Decreased body/fat mass.

Improved lipid markers, including HDL increase and triglyceride reduction.

Increased hepatic AMPK.

Absence of acute hypoglycemia.

Multi-enzyme inhibition targeting HMG-CoA reductase, α-glucosidase, and DPP-IV.

Documented Applications

Preventing and/or treating pathological disorders of carbohydrate and/or fat metabolism in humans or animals.

Use associated with carbohydrate and fat metabolism disorders including type 2 diabetes, NASH, and cardiovascular risks.

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