Compositions and methods for treating diabetes, fatty liver, cardiopathies, insulin resistance, 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-9962420-B2

Patent

Publication Date

2018-05-08

Expiration Date


Abstract

This disclosure provides compositions formulated in the form of tablets, wafer capsules, gel capsules, sticks, sachets, vials, droppers or in injectable form. The compositions comprise a mixture of: an extract of Chrysanthellum indicum, an extract of Cynara scolymus, an extract of Vaccinium myrtillus, an extract of Olea europaea, and pipeline. This disclosure also provides methods of treating pathological disorders of carbohydrate and/or fat metabolism in a patient by administering to the patient the compositions.

Core Innovation

A composition is provided in tablets, wafer capsules, gel capsules, sticks, sachets, vials, droppers, or in injectable form. The composition contains a mixture of an extract of Chrysanthellum indicum, an extract of Cynara scolymus, an extract of Vaccinium myrtillus, an extract of Olea europaea, and piperine selected from synthetic piperine and/or an extract of Piper containing piperine.

The composition further comprises at least one molecule from a first group of selected molecules including apigenin 7-O-glucuronide, chrysanthellin A, chrysanthellin B, caffeic acid, luteolin, maritimetin, eriodictyol, isookanin, apigenin, and related analogs. It also comprises at least one molecule from a second group including a dicaffeoylquinic acid, a sulfo-monocaffeoylquinic acid, luteolin, luteolin 7-O-glucoside, luteolin 7-O-glucuronide, apigenin 7-O-glucoside, cynaropicrin, or analogs thereof.

In addition, the composition comprises at least one molecule selected from monocaffeoylquinic acids and multiple delphinidin, cyanidin, petunidin, peonidin, and malvidin glycosides, or analogs thereof. The composition further comprises at least one molecule selected from oleuropein, hydroxytyrosol, and analogs thereof.

The described invention addresses preventing and/or treating type 1 diabetes, type 2 diabetes, insulin resistance, non-alcoholic fatty liver disease (NAFLD), and/or non-alcoholic steatohepatitis (NASH), as well as dyslipidemia, obesity/overweight, cardiovascular pathologies, and cardiovascular risk factors.

Claims Coverage

The independent claim covers one multi-extract, piperine-containing composition in specified dosage forms that includes multiple defined groups of selected molecules. The inventive features comprise the specific plant extracts, the piperine selection, the inclusion of three groups of polyphenol/flavonoid-type molecules, and the further inclusion of oleuropein and hydroxytyrosol.

Multi-extract composition with piperine

A composition in tablets, wafer capsules, gel capsules, sticks, sachets, vials, droppers, or injectable form, containing a mixture of an extract of Chrysanthellum indicum, an extract of Cynara scolymus, an extract of Vaccinium myrtillus, an extract of Olea europaea, and piperine selected from synthetic piperine and/or an extract of Piper containing piperine.

Defined apigenin- and flavonoid-type molecule group

At least one molecule selected from apigenin 7-O-glucuronide, chrysanthellin A, chrysanthellin B, caffeic acid, luteolin, maritimetin, eriodictyol, isookanin, apigenin, and related analogs.

Defined dicaffeoylquinic and related molecule group

At least one molecule selected from a dicaffeoylquinic acid, a sulfo-monocaffeoylquinic acid, luteolin, luteolin 7-O-glucoside, luteolin 7-O-glucuronide, apigenin 7-O-glucoside, cynaropicrin, or analogs thereof.

Defined monocaffeoylquinic and anthocyanin glycoside molecule group

At least one molecule selected from monocaffeoylquinic acids and multiple delphinidin, cyanidin, petunidin, peonidin, and malvidin glycosides, or analogs thereof.

Oleuropein and hydroxytyrosol inclusion

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

Claim coverage is centered on a single independent claim defining a multi-herbal, piperine-containing composition that includes multiple specified groups of selected molecules plus oleuropein and hydroxytyrosol.

Stated Advantages

Improved fasting glycemia in db/db mice.

Improved carbohydrate tolerance.

Improved insulin sensitivity.

Body/fat mass reduction.

Increased HDL.

Reduced hepatic triglycerides.

Reduced serum triglycerides.

Synergistic effects for specific combinations.

Superiority versus metformin for the reported comparison composition.

Increased hepatic AMPK.

In vitro inhibition of alpha-glucosidase, DPP-IV, and HMG-CoA reductase.

Documented Applications

Preventing and/or treating type 1 diabetes.

Preventing and/or treating type 2 diabetes.

Preventing and/or treating insulin resistance.

Preventing and/or treating non-alcoholic fatty liver disease (NAFLD) and/or non-alcoholic steatohepatitis (NASH).

Preventing and/or treating dyslipidemia.

Preventing and/or treating obesity/overweight.

Preventing and/or treating cardiovascular pathologies.

Preventing and/or treating cardiovascular risk factors.

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