KR-20260062853-A - Pharmaceutical compositions for treating arthritis comprising Gynostemma pentaphyllum extract with increased Damulin A and Damulin B or thereof fractions

Abstract

Gynostemma pentaphyllum extracts and fractional extracts with increased content of damulin A, damulin B, or damulin A and B have superior anti-inflammatory effects and joint health improvement effects, including cartilage regeneration in animal experiments, compared to the Gynostemma pentaphyllum extract. As a result, the damulin A, damulin B, or Gynostemma pentaphyllum extract with increased damulin A and B content provides a new pharmaceutical composition and health functional food for treating osteoarthritis, rheumatoid arthritis, gout, and psoriatic arthritis, which has an excellent cartilage-promoting arthritis treatment effect.

Inventors

• 허태린
• 도은주
• 이선희
• 김혁진
• 김지은

Assignees

• 주식회사 티지 바이오텍

Dates

Publication Date

20260507

Application Date

20251023

Priority Date

20241029

Claims (20)

1. A pharmaceutical composition for improving or treating arthritis characterized by containing a compound of damulin A or damulin B of the following chemical structural formula, or damulin A and damulin B as active ingredients.
2. In Article 1, The above pharmaceutical composition is a pharmaceutical composition for improving and treating arthritis characterized by promoting the proliferation of cartilage cells.
3. In Article 1, A pharmaceutical composition for improving and treating arthritis, characterized in that the above arthritis is osteoarthritis.
4. A health functional food for preventing or improving arthritis, characterized by containing a compound of Damulin A or Damulin B, or Damulin A and Damulin B as active ingredients.
5. In Article 4, The above-mentioned health functional food is a health functional food for preventing or improving arthritis characterized by promoting the proliferation of cartilage cells.
6. In Article 5, A health functional food for the prevention or improvement of arthritis, characterized in that the above arthritis is osteoarthritis.
7. As a Gynostemma pentaphyllum fraction prepared by treating Gynostemma pentaphyllum extract at high temperature and high pressure, A fraction of *Gynostemma pentaphyllum* characterized by containing a total content of 2.8 to 99.0% (w/w) of damulin A, damulin B, gypenoside L, and gypenoside LI.
8. In Article 7, The above Gynostemma fraction is characterized by comprising 0.6~2.2% (w/w) of damulin A, 0.6~2.0% (w/w) of damulin B, 0.8~2.6% (w/w) of gypenoside L, and 0.5~2.2% (w/w) of gypenoside LI.
9. In Article 7, The above Gynostemma fraction is a fraction from which the non-saponin water-soluble fraction (wsAN) has been removed, characterized by comprising 2.3~7.8% (w/w) of damulin A, 2.4~7.9% (w/w) of damulin B, 2.9~8.4% (w/w) of gypenoside L, and 1.8~6.5% (w/w) of gypenoside LI.
10. In Article 7, The above Gynostemma fraction is a fraction from which the non-saponin water-soluble fraction (wsAN) has been removed, characterized by comprising 10.9~28.6% (w/w) of damulin A, 9.7~23.6% (w/w) of damulin B, 10.6~21.3% (w/w) of gypenoside L, and 7.9~15.2% (w/w) of gypenoside LI.
11. A Gynostemma fraction according to any one of paragraphs 7 through 10, used for the improvement or treatment of arthritis.
12. A pharmaceutical composition for improving and treating arthritis, characterized by comprising a fraction of the Gynostemma pentaphyllum of claim 11.
13. In Article 12, A pharmaceutical composition for improving and treating arthritis, characterized in that the above arthritis is osteoarthritis.
14. In Article 13, The above pharmaceutical composition is a pharmaceutical composition for improving and treating arthritis characterized by promoting the proliferation of cartilage cells.
15. In Article 13, The above pharmaceutical composition is a pharmaceutical composition for improving and treating arthritis characterized by inhibiting inflammation.
16. A health functional food for preventing or improving arthritis, characterized by containing a fraction of *Gynostemma pentaphyllum* according to any one of claims 7 to 10 as an active ingredient.
17. In Article 16, A health functional food for the prevention or improvement of arthritis, characterized in that the above arthritis is osteoarthritis.
18. In Article 16, The above-mentioned health functional food is a health functional food for preventing or improving arthritis characterized by promoting the proliferation of cartilage cells.
19. In Article 16, The above health functional food is a health functional food for preventing or improving arthritis characterized by inhibiting inflammation.
20. A method for preparing a composition comprising damulin A, damulin B, damulin L, and damulin LI by treating purified zipenoside LVI, zipenoside XLVI, or a mixture thereof at high temperature and high pressure.

Description

Pharmaceutical compositions for treating arthritis comprising Gynostemma pentaphyllum extract with increased Damulin A and Damulin B content or fractions thereof The present invention relates to a composition for the prevention or treatment of arthritis comprising, as an active ingredient, an extract of Gynostemma pentaphyllum (Actiponin) in which the content of damulin A and damulin B is increased by treating the extract of Gynostemma pentaphyllum (GPE) at high temperature and high pressure. The present invention relates to a composition for the prevention or treatment of arthritis comprising, as active ingredients, a Gynostemma pentaphyllum extract (Actiponin) in which the content of damulin A and damulin B is increased by treating the Gynostemma pentaphyllum extract (GPE) at high temperature and high pressure to further fractionate the extract (Actiponin), thereby enhancing the content of damulin A, damulin B, gypenoside L, and gypenoside LI (Actiponin-F, Actiponin-F), and a Gynostemma pentaphyllum extract fraction (TGBA-2) in which the content of the four major components is further enhanced. The present invention relates to a composition for the prevention or treatment of arthritis comprising damulin A or damulin B isolated from Gynostemma pentaphyllum extract as an active ingredient. The human body is composed of approximately 200 joints. A joint is the area where bones meet. Joints are composed of cartilage, joint capsules, synovial membranes, ligaments, tendons, and muscles to allow for smooth movement between bones, and they serve to absorb shock generated during movement. Arthritis is a disease caused by inflammation in the joints of the human body. Types include osteoarthritis, rheumatoid arthritis, gout, and psoriatic arthritis, with 95% of arthritis patients suffering from osteoarthritis. Osteoarthritis is a disease characterized by localized degenerative changes as joint cartilage wears away, and it is also known as degenerative arthritis. Osteoarthritis is a representative degenerative disease closely associated with aging; approximately 10–15% of the total population suffers from this disease, and notably, about 60–80% of the elderly population aged 65 or older suffer from osteoarthritis. Osteoarthritis is a degenerative arthritis characterized by degenerative changes in the cartilage and surrounding bone of synovial joints. It is a disease marked by the gradual loss of articular cartilage, hypertrophy of the bone located beneath the cartilage, bone formation at the joint margins, and non-specific synovial inflammation. Osteoarthritis progresses through five stages: the chondrosis stage (Stage 1), where increased water content within the cartilage causes edema; the fibrillation stage (Stage 2), where cartilage is destroyed, causing the surface to crack and tear, exposing the bone and narrowing the joint cavity; the stage (Stage 3), where cartilage cells begin to regenerate to repair the cartilage, but destruction occurs faster than regeneration, leading to an overall reduction in cartilage; the bone change stage (Stage 4), where bone deformation results in joint deformity and dysfunction; and the joint soft tissue change stage (Stage 5), where soft tissue thickens. The causes of osteoarthritis are closely related to aging and excessive body weight, and it occurs more frequently in women as age increases. The mechanism by which osteoarthritis is induced is known to involve increased production of pro-inflammatory cytokines and increased secretion of MMPs (Matrix Metalloproteinases), such as collagenase and stromelysin, which cause damage to the articular cartilage matrix. Drugs currently used to treat osteoarthritis include analgesics, steroids, and non-steroidal anti-inflammatory drugs, as well as methods using chondroprotective agents such as hyaluronic acid, glucosamine, and chondroitin, and surgical treatment methods such as arthroscopic surgery, proximal tibial osteotomy, partial joint replacement, and total knee replacement. However, drug treatments only have the effect of non-specifically alleviating pain or inflammatory responses, and chondroprotectors merely protect the joints by supplying nutrients to cartilage cells or cushioning impact, failing to serve as a fundamental treatment method. Furthermore, existing arthritis medications are known to have disadvantages depending on the type, including various systemic side effects such as gastrointestinal disorders (including stomach ulcers and bleeding), weight gain, diabetes, hypertension, osteoporosis, and cataracts; increased risk of infection, thrombosis, and cardiovascular risks observed when using biological agents; and inconvenience of treatment, delayed onset of action, and cost burden when using injectable formulations. Therefore, there is a need to develop new, safer treatments that can treat osteoarthritis more effectively without side effects. Gynostemma pentaphyllum is a perennial vine belonging to the Cucurbitaceae family.