# US 8,541,383 B2 · Synergistic phytochemical composition for the treatment of obesity

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- Number: US 8,541,383 B2
- Document ID: US8541383B2
- Status: Granted
- Kind: B2
- Application number: 12/784,295
- Filed: 2010-05-20
- Published: 2010-09-09
- Granted: 2013-09-24
- Earliest claimed: 2007-11-22
- Assignees: Laila Nutraceurticals
- Applicants: Ganga Raju Gokaraju; Rama Raju Gokaraju; Trimurtulu Golakoti; Venkateswara Rao Chirravuri; Venkateswarlu Somepalli; Kiran Bhupathiraju
- Inventors: Ganga Raju Gokaraju; Rama Raju Gokaraju; Trimurtulu Golakoti; Venkateswara Rao Chirravuri; Venkateswarlu Somepalli; Kiran Bhupathiraju
- Web page: https://patentgrep.com/patent/US8541383B2

## CPC

- A61K 36/185: Magnoliopsida (dicotyledons)
- A61K 8/602: {Glycosides, e.g. rutin}
- A61K 8/9789: Magnoliopsida [dicotyledons]
- A61K 36/75: Rutaceae (Rue family)
- A61K 36/9066: Curcuma, e.g. common turmeric, East Indian arrowroot or mango ginger
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61Q 19/06: for countering cellulitis
- A61K 2800/782: Enzyme inhibitors; Enzyme antagonists
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Synergistic anti-adipogenic and pro-lipolytic compositions for the prevention and amelioration of adipogenesis and lipolysis mediated diseases, comprising at least two extracts selected from enriched demethylated curcuminoids obtained from Curcuma longa, Moringa oleifera and Murraya koenigii. The anti-adipogenic and pro-lipolytic compositions optionally contain one or more anti-obesic agents. These compositions are useful for preventing anti-inflammatory and free radical mediated diseases.

## Claims

### Claim 1

A synergistic anti-adipogenic and pro-lipolytic composition for the amelioration of adipogenesis and lipolysis mediated diseases, comprising:
about 10% by weight of enriched demethylated curcuminoids obtained from Curcuma longa; and
a combination of a Moringa oleifera leaf extract and a Murraya koenigii leaf extract;
said compositions optionally further containing at least one anti-obesic agent, at least one biologically acceptable carrier, or a mixture thereof;
wherein said composition contains said Moringa oleifera leaf extract in the range of 30-70% by wt., and said Murraya koenigii leaf extract in the range of 15-45% by wt.

### Claim 2 (depends on 1)

The composition as claimed in claim 1, wherein the enriched demethylated curcuminoids comprise at least one compound selected from the group consisting of a compound of the formula I, a compound of the formula II, a compound of the formula III, a compound of the formula IV, and a mixture thereof:
said at least one compound being obtained by demethylation of Curcuma longa extract.

### Claim 3 (depends on 1)

The composition as claimed in claim 1, wherein said Moringa oleifera leaf extract contains at least two of the following compounds: Kaempferol-3-O-glucoside of formula V, Quercitin-3-O-glucoside of formula VI, Niazinin A of formula VII, and Niazinin B of formula VIII:

### Claim 4 (depends on 3)

The composition as claimed in claim 3, wherein said Moringa oleifera leaf extract comprises Kaempferol-3-O-glucoside of formula V in the range of 0.2-5% by wt., Quercitin-3-O-glucoside of formula VI in the range of 0.5-20% by wt., Niazinin A of formula VII in the range of 0.01-3% by wt., and Niazinin B of formula VIII in the range of 0.001-3% by wt.

### Claim 5 (depends on 1)

The composition as claimed in claim 1, wherein said Murraya koenigii leaf extract is obtained by extracting a Murraya koenigii leaf with a solvent selected from the group consisting of water, methanol, ethanol, propanol, butanol, ethyl acetate, chloroform, dichloromethane, acetone and mixtures thereof.

### Claim 6 (depends on 1)

The composition as claimed in claim 1, wherein the anti-obesic agents for optional addition are selected from the group consisting of Holoptelia integrifolia extract, Piper betle, standardized Curcuma longa extract, Boerhaavia diffusa extract, Tribulus terrestris extract, Garcinia cambogia extract, green tea extract, green coffee bean extract, Eucalyptus plant extract, Gymnema sylvestre extract, Banaba extract, carnitine, Phaseolus vulgaris extract, Bitter orange (Citrus aurantium) extract, chitosan, conjugated linoleic acid, Glucomannan (Konjac plant extract), green coffee bean extract, Caralluma extract, seaweed extract, Hoodia Gordonii extract, Commiphora mukul gum resin extract, Zingiber officinalis extract, Allium sativum extract, chromium picolinate, chromium nicotinate, chromium polynicotinate (niacin-bound chromium), chromium histidinate, caproic acid, caprylic acid, capric acid, myristic acid and lauric acid, 5-hydroxy-L-tryptophan, 4-hydroxyisoleucine, hydroxy methylbutyrate, branched-chain amino acids, double salts of (−)hydroxycitric acid from Garcinia species, DHEA, 7-KetoDHEA, sibutramine, orlistat and mixtures thereof.

### Claim 7 (depends on 1)

The composition as claimed in claim 1, further comprising effective amounts of at least one pharmaceutically or nutritionally or dietetically acceptable antioxidant, adaptogen, anti-inflammatory agent, antidiabetic agent, Curcuma longa extract, Piper nigrum or Piper longum extract, trace metal, or mixture thereof to form a formulation.

### Claim 8 (depends on 1)

The composition as claimed in claim 1, wherein the said compositions are in the form of a dietary formulation as a food for specified health uses.

### Claim 9 (depends on 1)

The composition as claimed in claim 1, wherein said composition further comprise a pharmaceutically or nutraceutically or dietetically or veterinary acceptable additive, selected from the group consisting of a binder, a diluent, an antioxidant and a lubricant.

### Claim 10 (depends on 1)

The composition as claimed in claim 1, wherein said enriched demethylated curcuminoids and said combination of said Moringa oleifera extract and said Murraya koenigii extract are present in amounts which are effective to reduce adipose tissue mass, body weight, total serum cholesterol level, phospholipids and triglycerides.

### Claim 11 (depends on 1)

A therapeutic formulation, comprising a composition as claimed in claim 1, wherein said enriched demethylated curcuminoids and said combination of said Moringa oleifera leaf extract and said Murraya koenigii leaf extract are present in said therapeutic formulation in amounts which are effective for inhibiting 5-lipoxygenase.

### Claim 12 (depends on 1)

The composition as claimed in claim 1, said compositions being in the form of pharmaceutical or dietary or veterinary or nutraceutical or cosmetic formulations.

### Claim 13 (depends on 1)

A therapeutic formulation containing a composition as claimed in claim 1, said composition being present in an effective amount for reduction of adipose tissue mass, body weight, total serum cholesterol level, phospholipids, and triglycerides.

### Claim 14 (depends on 2)

The composition as claimed in claim 2, wherein the enriched demethylated curcuminoids comprise from 90% to 95% by weight of the enriched demethylated curcuminoids of at least one compound selected from the group consisting of a compound of the formula I, a compound of the formula II, a compound of the formula III, a compound of the formula IV, and a mixture thereof.

### Claim 15 (depends on 8)

The composition as claimed in claim 8, wherein the food for specified health uses is a chocolate bar, a nutritional bar, a cream, a jam a gel, a coffee, a tea, a milk-containing beverage, a lactic acid bacteria-containing beverage, a drop, a candy, a chewing gum, a chocolate, a gummy candy, a yoghurt, an ice cream, a pudding, a soft adzuki-bean jelly, a jelly, or a cookie.

### Claim 16 (depends on 1)

The composition as claimed in claim 1, wherein said Murraya koenigii leaf extract contains at least two of the following compounds: Mahanine of formula IX, Mahanimbine of formula X, isomahanine of formula XI and Ecuchrisitm-B of formula XII:

### Claim 17 (depends on 16)

The composition as claimed in claim 16, wherein said Murraya koenigii leaf extract comprise Mahanine of formula IX in the range of 0.1-10% by wt, Mahanimbine of formula X in the range of 0.01-5% by wt, isomahanine of formula XI in the range of 0.01-3% by wt and Ecuchrisitm-B of formula XII in the range of 0.01-2.5% by wt.

### Claim 18 (depends on 4)

The composition as claimed in claim 4, wherein the Moringa oleifera leaf extract is prepared by a process comprising the steps of:
(i) drying a Moringa oleifera leaf in shade, followed by powdering said leaf to form a dry powder;
(ii) extracting the dry powder with a suitable solvent and filtering; and
(iii) distilling off the solvent at reduced pressure to obtain a residue.

### Claim 19 (depends on 18)

The composition as claimed in claim 18, wherein the process for preparing the Moringa oleifera leaf extract further comprises:
(iv) dissolving the said residue in 30% methanol to form a solution;
(v) charging the said solution to a resin column followed by washing with water;
(vi) eluting with 80% methanol to obtain a solution of active fraction; and
(vii) evaporating the solvent from the solution of active fraction to obtain the active fraction.

### Claim 20

An anti-adipogenic and prolipolytic composition for the amelioration of adipogenesis and lipolysis mediated diseases, consisting essentially of:
a Moringa oleifera leaf extract and a Murraya koenigii leaf extract,
wherein said Moringa oleifera leaf extract is in the range of 50-67% by wt., based on the combined weight of said Murraya koenigii leaf extract and said Moringa oleifera leaf extract; said Moringa oleifera leaf extract comprising at least two of Kaempferol-3-O-glucoside, Quercitin-3-O-glucoside, Niazinin A, and Niazinin B,
said anti-adipogenic and pro-lipolytic composition optionally further comprising a biologically acceptable carrier;
wherein said anti-adipogenic and pro-lipolytic composition do not include enriched demethylated curcuminoids.

### Claim 21 (depends on 20)

The composition as claimed in claim 20, wherein said compositions further comprise a pharmaceutically or nutraceutically or dietetically or veterinary acceptable additive, selected from binder, diluent, antioxidant and a lubricant.

### Claim 22

A composition consisting essentially of:
a Murraya koenigii leaf extract, and
a Moringa oleifera leaf extract in the range of 50-67% by wt., based on the combined weight of said Murraya koenigii leaf extract and said Moringa oleifera leaf extract;
said Moringa oleifera leaf extract comprising at least two of Kaempferol-3-O-glucoside, Quercitin-3-O-glucoside, Niazinin A, and Niazinin B;
wherein said composition does not include enriched demethylated curcuminoids.

### Claim 23 (depends on 22)

A composition for oral administration, comprising the composition of claim 22.

### Claim 24 (depends on 1)

A method of weight control, comprising administering an effective amount of the composition as claimed in claim 1, said composition being formulated as a dairy product, an alcoholic beverage, a non-alcoholic beverage, or a snack bar.

### Claim 25 (depends on 1)

A method for treating a subject to reduce adipose tissue mass, body weight, total serum cholesterol level, phospholipids or triglycerides comprising administering a biologically acceptable amount of the composition as claimed in claim 1.

### Claim 26 (depends on 25)

The method of claim 25, wherein the subject is a mammal.

### Claim 27 (depends on 20)

A process for the preparation of the composition according to claim 20, comprising the steps of:
(i) drying a Moringa oleifera leaves in shade, followed by powdering said plant part to form a dry powder;
(ii) extracting the dry powder with a suitable solvent and filtering;
(iii) distilling off the solvent at reduced pressure to obtain a residue;
(iv) optionally dissolving the said residue in 30% methanol to form a solution;
(v) optionally charging the said solution to a resin column followed by washing with water;
(vi) optionally eluting with a polar solvent to obtain a solution of active fraction; and
(vii) optionally evaporating the solvent from the solution of active fraction to obtain the active fraction; and
(viii) combining the residue of step (iii) or the active fraction of step (vii) with Murraya koenigii leaf extract in the range of 33-50% by wt.

### Claim 28 (depends on 27)

The process as claimed in claim 27, wherein the said suitable solvent for extraction is selected from the group consisting of water, methanol, ethanol, isopropanol, ethyl acetate, acetone, and mixtures thereof.

### Claim 29 (depends on 27)

The process as claimed in claim 27, wherein the said resin column comprises a resin selected from the group consisting of cationic exchange resin, anionic exchange resin, and synthetic adsorbent resins; and the solvent for elution is water or alcohol or mixtures thereof.

### Claim 30 (depends on 20)

A method for treating a subject to reduce adipose tissue mass, body weight, total serum cholesterol level, phospholipids and triglycerides comprising administering a biologically acceptable amount of a composition as claimed in claim 20.