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Composition for inhibiting cellular senescence comprising quercetin-3-O-beta-D-glucuronide

A technology for inhibiting cells and glucuronide, which can be used in medical preparations containing active ingredients, drug combinations, active ingredients of heterocyclic compounds, etc., and can solve the problems that are not mentioned.

Inactive Publication Date: 2015-06-17
RES COOPERATION FOUND OF YEUNGNAM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] On the other hand, the present inventors disclosed in Korean Patent Publication No. 10-2011-0041710 a pharmaceutical composition for inhibiting aging, including rhubarb (Rhei rhizoma), echinacea (Cirsii Radix), plantago seed (Plantaginis semen), cinnamon (Cinnamoni cortex), Cinnamoni cortex spissus, Euonimi lignum suberalatu, Salicis radicis cortex, Polygoni avicularis herba, and crabapple root (Chaenomelis langenariae radix) as the active ingredient, but Quercetin-3-O-β-D-glucuronide (Q3GA) compounds not mentioned in the present disclosure

Method used

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  • Composition for inhibiting cellular senescence comprising quercetin-3-O-beta-D-glucuronide
  • Composition for inhibiting cellular senescence comprising quercetin-3-O-beta-D-glucuronide
  • Composition for inhibiting cellular senescence comprising quercetin-3-O-beta-D-glucuronide

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Experimental program
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Embodiment 1

[0036] Separation and structural identification of quercetin-3-O-β-D-glucuronide (Q3GA)

[0037] 1. Separation of quercetin-3-O-β-D-glucuronide (Q3GA)

[0038] The dried aerial parts (9 kg) of the stock (P. aviculare L.) were extracted with 70%, 90% and 100% MeOH at reflux for 24 hours sequentially, and the combined MeOH solutions were evaporated to dryness (1.4 kg). The dried MeOH extract (1.4 kg) was resuspended in 1.5 L of distilled water, and the solution was sequentially washed with n-hexane (1.5 L × 3), ethyl acetate (EtOAc, 1.5 L × 3) and n-butanol (n-butanol, 1.5 l×3) for layering. After drying, n-hexane (120g), ethyl acetate (65g), n-BuOH (140g) and H 2 O (21 g) 4 solvent extracts.

[0039] The n-BuOH extract (10 g) was loaded into a Sephadex LH-20 column (4 x 90 cm), and the column was eluted with MeOH. The eluents were combined based on TLC to give 17 fractions (PAB 1-17). In these fractions, by using MeOH-H 2 Reverse phase column chromatography (4 x 50 cm) w...

Embodiment 2

[0045] Examination of the Cell Senescence Inhibitory Action of Quercetin-3-O-β-D-glucuronide (Q3GA) in Human Fibroblasts and Umbilical Vein Endothelial Cells

[0046] 1. Materials

[0047] Human dermal fibroblasts (HDFs) and human umbilical vein endothelial cells (HUVECs) were obtained from Lonza (Walkersvill, MD, USA). Dulbecco's modified Eagle's medium (DMEM), fetal bovine serum (FBS) and penicillin-streptomycin solution were from WelGene (Daegu, Korea), respectively. Epidermal Growth Medium-2 (EGM-2) was from Lonza (Walkersvill, MD, USA). Antibodies against p53 and p21 were from Santa Cruz Biotech. Inc. (Santa Cruz, CA, USA), and antibodies against phosphorylated S6 kinase were from Cell Signaling Technology Inc. (Beverly, MA, USA). Rabbit polyclonal antibody against glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was kindly provided by Dr. K.S. Kwon (KRIBB, Daejeon, Korea). Adriamycin was purchased from IIdong Pharmaceutical Co., Ltd. (Seoul, Korea).

[0048] 2. Cell...

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Abstract

The present invention relates to a composition for inhibiting cellular senescence comprising quercetin-3-O-beta-D-glucuronide (Q3GA) as an active ingredient, and provides a composition for inhibiting cellular senescence of fibroblasts or umbilical vein endothelial cells induced by adriamycin or replicative senescence of fibroblasts or umbilical vein endothelial cells. Specifically, the quercetin-3-O-beta-D-glucuronide (Q3GA) is characterized by being isolated from Polygoni avicularis herba extract. The composition may be usefully used for treating aging-related diseases, for example, skin aging, rheumatoid arthritis, osteoarthritis, hepatitis, chronically damaged skin tissue, arteriosclerosis, prostatic hyperplasia and liver cancer, by inhibiting a cellular senescence process of human fibroblasts and umbilical vein endothelial cells.

Description

technical field [0001] The present invention relates to a composition for inhibiting cell senescence, comprising quercetin-3-O-β-D-glucuronide (Q3GA) as an active ingredient. Background technique [0002] Normal somatic cells reveal a limited amount of proliferation due to cellular senescence. Cellular senescence is induced by a variety of factors, such as telomere shortening due to DNA end replication problems (Collado et al., Cell. (2007) 130:223-233), changes in the activity of tumor suppressor genes and oncogenes, Inflammation, oxidative stress chemotherapeutic agents and exposure to ultraviolet radiation and ionizing radiation (Kuilman et al., Genes & Development. (2010) 24:2463-2479). Senescent cells display enlarged and flattened cell morphology, growth arrest, DNA damage foci in the nucleus, senescence-associated secretory phenotype (SASP) and senescence-associated β-galactosidase (SA-β-gal) activity ( Dimri et al., Proc Natl Acad Sci U S A. (1995) 92:9363-9367; Ro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/35A61P17/00A61P19/02
CPCA61K31/7048A61K36/704A61P17/00A61P19/02A61K31/35A61K31/352A61K2236/35
Inventor 金栽龙孙种根梁孝贤皇甫敬
Owner RES COOPERATION FOUND OF YEUNGNAM UNIV
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