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Natural extracts for modulating pp2a methylation, and providing antioxidant and anti inflammatory activity

a technology of pp2a methylation and natural extracts, which is applied in the directions of pharmaceutical delivery mechanism, plant/algae/fungi/lichens ingredients, coniferophyta medical ingredients, etc., can solve the problem of needing ad therapies

Inactive Publication Date: 2017-08-10
SIGNUM BIOSCIENCES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent is for a product that is meant to help keep the skin healthy and prevent skin issues like aging. It is designed for people who are at risk for skin-related medical conditions.

Problems solved by technology

The demographics of aging in the United States population, combined with a lack of effective treatments, have heightened the need for AD therapies.

Method used

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  • Natural extracts for modulating pp2a methylation, and providing antioxidant and anti inflammatory activity
  • Natural extracts for modulating pp2a methylation, and providing antioxidant and anti inflammatory activity

Examples

Experimental program
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Effect test

example 1

Preparation of Extracts

[0148]Various water-soluble oligosaccharides and starch in botanicals can reduce the specific activity of the extract, making the extract prone to bacterial contamination and growth; and change its appearance to sticky thick oil or to glassy caramel-looking substance. These properties make most of aqueous extracts difficult in manufacture (drying, emptying from reactor, drumming, etc.) and affect products shelf life and overall safety. Furthermore, removing various naturally occurring in a given botanic extract non-biologically active oils and lipids result in final extract to be a free flowing powder improving ease of manufacturing and blending into a product. Therefore, a process for manufacturing these extracts was designed to take these factors into account.

[0149]A raw botanical (10 g) was shaken with isopropyl alcohol (100 mL) in a flask at 65° C. for 16 hrs. The resulting isopropanolic extract was filtered and concentrated to dryness on a rotavap. The cr...

example 2

Natural Extracts Effect on PP2A Methylation

[0150]Extracts, as shown in Tables 1-4 below, were created using isopropanol or toluene-based extraction methods at 65° C. as generally described in Example 1. These extracts were assayed for their ability to preserve the methylation status of PP2A AC dimer in the presence of protein phosphatase methylesterase-1 (PME-1), using a radioactive filter binding assay. Methylated PP2A was made by incubating PP2A, protein phosphatase methyl transferase (PPMT) and [3H]-SAM for 1 hr. PME-1 was incubated with varying concentrations of botanical extracts prior to the addition of 50 nM of methylated PP2A. The reaction was allowed to continue for 30 minutes at room temperature. 10% TCA was added to stop the reaction and incubated for 1 hour. Remaining buffer was filtered and total counts remaining on the filter plate were measured using a scintillation counter. IC50 values were generated from dose-response curves using a four-parameter logistic curve fit...

example 3

Natural Extracts Effect on ROS Scavenging (Antioxidant)

[0153]Botanical extracts ability to prevent oxidation of ABTS by metmyoglobin was analyzed. The antioxidant capacity of select botanical extracts was evaluated in vitro using the ABTS (2, 2′-Azino-bis-[3-ehthylbenzthiazoline sulphonate]) antioxidant kit (Cayman Chemical Company; Ann Arbor, Mich.). Botanical extracts were incubated with both metmyoglobin and chomogen, ABTS. The reaction was initiated upon addition of hydrogen peroxide and the oxidation of the ABTS to ABTS•+ was monitored via absorbance at 750 nm. EC50 values were generated from dose-response curves using a four-parameter logistic curve fit (SigmaPlot), and are shown below in Table 5.

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Abstract

Compositions containing natural and botanical extracts for use in inhibiting one, two, or three of (a)-(c): (a) demethylation of PP2A by PME-1 methylesterase; (b) formation of free radicals and reactive oxygen species; and / or (c) inflammation. These compositions include an extract of one or more botanicals selected from the group consisting of: juniper berry fruit, schisandra fruit, strawberry fruit, avocado seeds, black raspberry seeds, blueberry seeds, celery seeds, cranberry seeds, fennel seeds, grape seeds, guarana seeds, red raspberry seeds, maca root, goldenseal root, turmeric root, magnolia bark, pygeum bark, red raspberry leaf, almond, cocoa powder, Echinacea angustifolia, prickly pear cactus and walnut.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 62 / 027,607, filed Jul. 22, 2014, and herein incorporated by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to compositions containing natural and botanical extracts for use in inhibiting demethylation of PP2A by PME-1 methylesterase; formation of free radicals and reactive oxygen species; and / or inflammation.BACKGROUND[0003]Protein phosphatase 2A (PP2A), a major serine / threonine phosphatase, has been implicated in a broad range of cellular functions anywhere from development to disease. Consisting of a scaffolding (A), regulatory (B) and catalytic (C) subunit, as shown in FIG. 1, this trimeric holoenzyme is highly regulated through structural assembly, post-translational modifications and small molecule interactions. Methylation of PP2A's carboxy-terminal tail has not only been implicated in modulating its activity and specificity but it has also bee...

Claims

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Application Information

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IPC IPC(8): A61K36/9066A61K36/736A61K36/54A61K36/73A61K36/45A61Q19/08A61K36/33A61K9/00A61K8/97A61K36/23A61K36/185A61K36/28A61K36/235A61K36/71A61K36/77A61K36/14A61K36/31A61K36/575A61K36/79A61K36/52A61K36/87
CPCA61K36/9066A61K2800/5922A61K36/736A61K36/54A61K36/73A61K36/45A61Q19/08A61K36/33A61K9/0053A61K9/0014A61K8/97A61K36/23A61K36/185A61K36/28A61K36/235A61K36/71A61K36/77A61K36/14A61K36/31A61K36/575A61K36/79A61K36/52A61K2800/782A61K2236/31A61K2236/53A61K2236/51A61K2236/33A61K2236/331A61K2236/39A61K2800/92A61K2800/805A61K36/87A61K45/06A61K2236/00A61K2300/00
Inventor HUBER, KRISTENVORONKOV, MICHAELFERNANDEZ, JOSEROUZARD, KARLPEREZ, EDUARDOSTOCK, MAXWELLSTOCK, JEFFRY
Owner SIGNUM BIOSCIENCES INC
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