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Orally bioavailable stilbenoids- compositions and therapeutic applications thereof

a technology of stilbenoids and compositions, applied in the field of natural fat modulators, can solve the problems of totally ineffective adipogenesis of stilbenoids, and achieve the effect of inhibiting adipogenesis and enhancing the ability to prevent accumulation

Inactive Publication Date: 2010-08-12
SAMI LABS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015]1. A novel, safe and bioavailable stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis and cosmeceutical, pharmaceutical and nutraceutical compositions thereof useful for anti-cellulite and anti-obesity therapy.

Problems solved by technology

While some stilbenoids better others in inhibiting adipogenesis, there are stilbenoids which totally fail to inhibit adipogenesis also.

Method used

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  • Orally bioavailable stilbenoids- compositions and therapeutic applications thereof
  • Orally bioavailable stilbenoids- compositions and therapeutic applications thereof
  • Orally bioavailable stilbenoids- compositions and therapeutic applications thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

FIG. I—Adipogenesis Inhibitory Activity

[0031]Principle:

[0032]A common assay to measure adipocyte differentiation in cell culture is with the dye Oil Red-O, which is a lipid-soluble red dye. Since terminal differentiation of adipocytes is accompanied by the accumulation of great amounts of lipids in large cytoplasmic vesicles, a strong, bright, staining of the cytoplasm with this dye is a reliable indicator of adipocyte differentiation.

[0033]Methodology:

[0034]3T3-L1 mouse adipocyte cells are seeded at a density of 5000 cell / 200 μl of adipocyte induction medium in a 96 well plate. After 48 hrs varying concentrations of the sample are added. After 72 hrs, the medium is changed to adipocyte progression medium along with the sample. The medium is similarly changed after another 48 hours. The plates are washed gently after 48 hrs with 100 μl of PBS. 100 μl of 10% formalin is used to fix the cells for 30 min keeping at RT. The cells are then washed twice with 60% isopropanol gently. 100 μl...

example 2

FIGS. IA and 1B

[0044]SIRT-1 activation / inhibition was measured using the SIRT 1 Direct fluorescent Screening Assay kit (Catalog No. 10010401) and instructions provided therein of Cayman Chemical Company, 1180 East Ellsworth Road, Ann Arbor, Mich. 48108 USA. (http: / / www.caymanchem.com / pdfs / 10010401.pdf)

TABLE APercentage SIRT 1 modulation by stilbenoidsSirtinol2-[(2-Hydroxynaphthalen-Sirtinol2-[(2-Hydroxynaphthalen-Concentration1-Concentrationylmethylene)amino]-3-hydroxyPterostilbene(μg / ml)N-(1-phenyl-ethyl)•benzamideResveratrolPterostilbeneGnetol(3hp)Oxyresveratrol164.44137.782.22104.44224.4477.7810−23326.67291.1111.111846.67668.8924.4450−57517.781137.7853.333686.671946.6760.00100−60093.331471.11113.334151.113146.67202.22250−56544.441902.22231.114826.673771.11297.78

[0045]Results (Table A) and Discussion

[0046]It may be known from Table A that both 3,5-dimethoxy-3,4′-dihydroxystilbene (3-hydroxypterostilbene) and 2,3′,5′,6-tetrahydroxy-trans-stilbene (gnetol) show enhanced percentage S...

example 3

Tables B, C, D and E

[0047]Antimicrobial Studies of 3-Hydroxy Pterostilbene Against Propionibacterium acnes

[0048]Objective: To compare the effect of 3-Hydroxypsterostilbene and Resveratrol on Propionibacterium acnes growth.

[0049]Propionibacterium acnes is a gram-positive, non-spore forming, anaerobic, pleomorphic rod found in clinical specimens. In human body P.acnes thrives on areas most exposed to air, such as the face and the nose. Its ability to live as an anaerobic in an air-exposed environment comes from the fact that P.acnes lives in the microhabitat sebaceous follicles thus causing acne vulgaris.

[0050]Method: Disc diffusion method was done to study Minimum inhibitory concentration (MIC).

[0051]Materials[0052]1. Propionibacterium acnes ATCC 11827[0053]2. Physiological saline or Buffered peptone water (BPW).[0054]3. Reinforced clostridium medium (RCM) Hi-media[0055]4. Reinforced clostridium agar (RCA) Hi-media[0056]5. Anaerobic chamber.[0057]6. Gassing manifold Nitrogen, mixed...

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Abstract

A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.

Description

[0001]This application is a continuation-in-part of U.S. patent application Ser. No. No. 12 / 367,840 filed on Feb. 9, 2009.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention in general relates to natural fat modulators. More specifically, the present invention relates to novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene possessing an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis. Useful compositions thereof for anti-obesity and anti-cellulite therapy are also described in the invention. Further the present invention also discloses the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene and 2,3′,5′,6-tetrahydroxy-trans-stilbene. In addition, the present invention also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes and compositions thereof.[...

Claims

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Application Information

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IPC IPC(8): A61K31/09C07C43/243A61P3/04
CPCA61K31/09A61K31/05C07C43/23C07C39/21A61P3/04
Inventor MAJEED, MUHAMMEDREINHARDT, JEFFREYNAGABHUSHANAM, KALYANAMTHOMAS, SAMUEL MANOHARANJAYARAMAN, KRISHNAMANI
Owner SAMI LABS LTD
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