A FORMULATION DISPLAYING AN ANTI-CARCINOGENIC EFFECT BY SUPPRESSING VCAM-1 EXPRESSION TRIGGERED BY TNF-A

Field of Invention

The present herewith discloses a formulation developed to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a.

Background of the Related Technology

Tumor necrosis factor (TNF), is a cytokine that is secreted by various types of cells and manages lysis of cancer cells. It is a glycoprotein hormone with 185 amino acids, but some cells may secrete longer or shorter isoforms of the hormone. It is encoded on 7^th chromosome of humans. It has two forms: 1. TNF alpha (TNFα, cachectin/ cachexin), 2. TNF beta (TNFβ, lymphotoxin). Genes encoding both are located on MHC. TNFα, is produced by macrophages and some other cells. On the other hand TNFβ is produced by T cell lymphocytes.

In state of art technology, invention no “WO 1998/003516", with title “Phospinate based inhibitors of matrix metalloproteases” and under classification number “A61K 31/66" discloses compound of the formula (I) wherein R1, R2, R3, R4, R5, R6 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, synergy with cytotoxic anticancer agents, tissue ulceration, macular degeneration (speckles), restenosis (reconstruction of a dilated channel), periodontal diseases, epidermolysis bullosa, scleritis, in combination with standard NSAID'S and analgesics and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.

Again invention no “WO 1998/034918", with title “Arylsulfonyl hydroxamic acid derivatives" and under classification number “C07D 211/62" discloses compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer

Again invention no “EP1663244B1", with title “Pteridine derivatives for the treatment of tnf-alpha-related diseases” and under classification number “A61K 31/519" relates to the use of polysubstituted pteridines for the prevention and/or the treatment of toxic side effects, disorders and diseases related to or resulting from the exposure of patients to abnormally high levels of tumor necrosis factor-alpha (hereinafter referred as TNF-α) in general, and particularly following the administration of TNF-α in cancer treatment in humans. This invention also relates to the use of polysubstituted pteridines for the treatment or prevention of alcohol-induced hepatitis and of cachexia

Again invention no “WO 1996/027583", with title “Arylsulfonylamino hydroxamic acid derivatives" and under classification number “C07C 311/29" discloses a compound of formula (I), where the referred composition is useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.

To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a.

Objective of the Invention

To overcome the disadvantages experienced in state of art technology;

• One objective of the present invention is to trigger tnf-alpha expression.
• One other objective of the invention is to, reduce interleukin 6 level.
• One other objective of the invention is to suppress VCAM-1 expression.

The present invention, which is aimed to achieve the above-mentioned advantages, is intended to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a  and is a formulation  that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate, 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol.

Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.

Detailed Description of the Invention

The present herewith discloses a formulation developed to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a. Referred formulation triggers tnf-alpha expression, reduces interleukin 6 level and suppresses VCAM-1 expression.

The formulation of the invention presented herewith contains; 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate, 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol .

The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;

• 10-90% of 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate,
• 90-10% of 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol.   

Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.

The present invention at the same time discloses using the above-referred formulation intended to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a  and manufacturing it for such purpose;.

CLAIMS

1. A formulation intended to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a, which consists of combining the components selected from the group; 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate, 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol in a single form or in combinations thereof.

1. The formulation of Claim 1 which is characterized by containing  10-90% of 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate by weight.

1. The formulation of Claim 1 which is characterized by containing  90-10% of 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol by weight.

1. Using the compositions obtained by selecting singly or in combination of components from the group of; 7-dimethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromane-5cumaroyl leucinate, 2,7-tris(4-hexahydroxy-3-prop-2-enyl-phenyl)- 4-prop-2-methoxyfenol from any one as given in Claims 2-3 in manufacturing the formulation intended to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a. 

SUMMARY

A FORMULATION DISPLAYING AN ANTI-CARCINOGENIC EFFECT BY SUPPRESSING VCAM-1 EXPRESSION TRIGGERED BY TNF-A

The present herewith discloses a formulation developed to display an anti-carcinogenic effect by suppressing vcam-1 expression which is triggered by tnf-a. Referred formulation triggers tnf-alpha expression, reduces interleukin 6 level and suppresses VCAM-1 expression.