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Dihydro-triterpenes in treatment of viral infections, cardiovascular disease, inflammation, hypersensitivity or pain

A technology of triterpene and dihydrogen, which is applied in the direction of cardiovascular system diseases, antiviral agents, and medical raw materials derived from angiosperms, can solve problems such as lack of efficacy, achieve inflammation or pain relief, have no serious side effects, and inhibit Effects of viral infection and inflammation or hypersensitivity

Inactive Publication Date: 2004-08-11
BSP PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] Due to the lack of efficacy of existing drugs and the large number of undesired side effects associated therewith, there is a strong need for new antiviral and anti-inflammatory drugs.

Method used

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  • Dihydro-triterpenes in treatment of viral infections, cardiovascular disease, inflammation, hypersensitivity or pain
  • Dihydro-triterpenes in treatment of viral infections, cardiovascular disease, inflammation, hypersensitivity or pain
  • Dihydro-triterpenes in treatment of viral infections, cardiovascular disease, inflammation, hypersensitivity or pain

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0158] Research overview

[0159] A composition of the present invention comprising 3.1% (w / w) dihydrobutyryl cetyl acetate and 2.8% (w / w) dihydrolupeyl acetate formulated in triglycerides, respectively Its possible antiviral effect against herpes simplex virus and influenza A virus was evaluated in monkey kidney (Vero) cells and MDCK cells (dot test).

[0160] IC of the composition of the present invention at 40-200 μg / ml 50 Both viruses were inhibited at doses.

[0161] test substance

[0162] A composition according to the invention is prepared by hydrogenation and fractionation of Shea Butter (Butyros permum parkii). The composition was analyzed by GC-MS, EI in full scan mode. A HP-5 column 30 m, ID 0.25 mm, 0.25 μm film thickness (5% diphenyl, 95% dimethylpolysiloxane) was used. The sample was dissolved in ethyl acetate (1 mg / mL), and the components were quantified using stigmasterol as an internal standard (0.02 mg / mL in ethyl acetate). The composition was found to...

example 2

[0175] overview

[0176] The composition of the invention described in Example 1 was evaluated for acute oral toxicity in mice. The substance was found to produce no toxicity or mortality at a dose of 2000 mg / kg. Therefore, it can be concluded that the LD 50 Above 2000mg / kg body weight.

[0177] test substance

[0178] The composition of the invention described in Example 1 was used in this experiment.

[0179] research description

[0180] Acute oral toxicity in rats is in accordance with the OECD guideline No 420, "Acute Oral Toxicity-fixed Dose Method", July 1992 and the EEC Directive Published in: "Official Journal of the European Communities" No: L 383A, volume 35, 29.12.1992 , Part B1 "Acute Toxicity (Oral)-Fixed Dose Method" recommended method for determination.

[0181] The study was initiated with a study in which 2000 mg of the composition / kg body weight was administered to one dam. No clinical signs of toxicity were observed in this mouse.

[0182] According...

example 3

[0186] overview

[0187] The composition of the invention described in Example 1 was evaluated for its acute topical anti-inflammatory effect in the phorbolester ear edema test in mice. At the two tested doses, the composition of the present invention was able to significantly suppress ear edema.

[0188] Target

[0189] When it has been confirmed in a separate experiment, the composition of Example 1 of the present invention, under laboratory conditions, is able to inhibit the production of inflammatory cytokines (TNF-α and IL-6) in liposugar-stimulated peritoneal phagocytes (mouse). secretion, we decided to test the efficacy of the composition under natural conditions in the otitis test induced by phorbol acetate (TPA) in mice, which is a commonly used method for screening and Methods for evaluating anti-inflammatory drugs. Locoid(R) infected skin solution (0.1% hydrocortisone 17-butyrate) was used as a positive control.

[0190] Test Articles and Excipients

[0191] Th...

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Abstract

The present invention relates to a composition containing the triterpenes dihydrobutyrylcetol, dihydrolupeol and / or dihydroparkeol, said composition being suitable for use as a medicament, a food supplement or as a cosmetic. Furthermore, the present invention relates to the use of such compositions for the preparation of a medicament, a food supplement or a cosmetic for immunomodulation in mammals such as inhibition of viral infections, cardiovascular diseases, cancer, hypersensitivity reactions and / or or inflammatory response. The triterpenes may be present in the form of the free alcohol or its derivatives, preferably derivatives of cinnamic acid, acetic acid or fatty acids. Additionally, the triterpene may be an extract available from a natural source or may be prepared by synthetic methods.

Description

field of invention [0001] The present invention relates to compositions containing dihydrobutyryl cetyl alcohol, dihydrolupeol or dihydroparkeol, or mixtures thereof. The composition can be formulated with pharmaceutically acceptable carriers and / or excipients for oral, parenteral, topical administration. The composition can be used as a medicine, a food supplement or a cosmetic. The present invention also relates to the use of such composition for preparing immunoregulatory drugs such as inhibiting hypersensitivity, inflammatory response or virus infection. Background of the invention [0002] Hypersensitivity is an altered reaction state in which there is an exaggerated immune response to a substance (antigen). Hypersensitivity reactions can be caused by exogenous or endogenous antigens. [0003] Hypersensitivity reactions can cause a myriad of diseases. Among them, the state of allergies and autoimmunity is the most important. The classification of hypersensitivity d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A23L1/30A61K8/00A61K8/63A61K8/96A61K8/97A61K31/045A61K31/216A61K31/22A61K31/23A61K31/56A61K31/575A61K36/00A61K36/18A61K45/06A61P1/04A61P3/06A61P9/00A61P9/10A61P11/02A61P11/06A61P13/08A61P17/00A61P17/04A61P17/06A61P19/02A61P19/06A61P29/00A61P31/04A61P31/10A61P31/12A61P31/16A61P31/22A61P35/00A61P37/02A61P37/06A61P37/08A61Q19/00
CPCA61K8/63A61K31/045A61K31/216A61K31/22A61K31/23A61K31/575A61K45/06A61Q19/005A61P1/04A61P11/02A61P11/06A61P13/08A61P17/00A61P17/04A61P17/06A61P19/02A61P19/06A61P29/00A61P31/04A61P31/10A61P31/12A61P31/16A61P31/22A61P35/00A61P3/06A61P37/02A61P37/06A61P37/08A61P9/00A61P9/10Y02A50/30
Inventor 莫滕·斯洛斯·韦德纳
Owner BSP PHARMA
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