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Antineoplastic effect of a group of cycloart-one triterpene compound

A technology of cyclopine and compound, which is applied in the field of cyclopine triterpenoids, to achieve the effect of preventing damage and scavenging free radicals

Inactive Publication Date: 2005-11-02
肖培根 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Three 9,19 cyclolanolane triterpenoids 23-O-acetylcimigenol-3-Oxy-β-D-xyloside (23-O-acetylcimigenol-3-O-β-D-xylopyranoside), 24-O-acetylcimigenol-3-oxo-β-D-xyloside (24-O-acetylcimigenol-3-O-β-D-xylopyranoside), 25-O-acetylcimigenol-3-oxo- β-D-xyloside (25-O-acetylcimigenol-3-O-β-D-xylopyranoside), all extracted from the aerial part of Cimicifuga officinalis, so far there is no report about its activity

Method used

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  • Antineoplastic effect of a group of cycloart-one triterpene compound
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  • Antineoplastic effect of a group of cycloart-one triterpene compound

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Cytotoxicity test:

[0030] 1. Materials: human hepatoma cell line (HepG2), human acute promyelocytic leukemia cell line (HL-60), all obtained from ATCC (American Type Culture Collection), and drug-resistant human hepatoma cell line (HepG2-R) is Doxorubicin-resistant cells (a gift from City University of Hong Kong). Mouse hepatocytes were isolated from the liver of Kunming mice (purchased from the Experimental Animal Center of Guangzhou University of Traditional Chinese Medicine, animal qualification certificate number: Yuejian Zhengzi No. 2001A054) and obtained through primary culture. Medium RPMI1640, DMEM, and fetal bovine serum were all purchased from Gibico.

[0031]MTT (3-(4,5-DIMETHYLTHIAZOL-2-YL)-2,5-diphenyl tetrazolium bromide) is a product of AMRESCO, subpackaged by Shanghai Bioengineering Co., Ltd., batch number: 0481B50. Adriamycin (doxirubicine), product of Sigma Company.

[0032] 2. Primary culture of mouse hepatocytes: Disinfect and expose the liver a...

Embodiment 2

[0038] Cell morphology test (cell cycle and apoptosis):

[0039] 1. Method: In a 35×10mm culture dish containing HepG2 and HL-60 cells, administer the drug separately. After a period of time, add 400ul AO / EB staining solution (100ug / ml AO solution, 100ug / ml EB solution, use PBS Preparation), mix well, and immediately observe under a 40×10 fluorescent inverted microscope. AO solution can stain both living cells and dead cells, while EB solution only stains cells that have lost membrane integrity, and living cells still show a uniform green color. Early apoptotic cells appear green with bright green spots in their nuclei due to chromatin condensation and nuclear lysis. Late apoptotic cells can be stained orange by EB, but unlike dead cells, the nuclei of late apoptotic cells appear condensed and often lysed. Necrotic cells stain orange but have live-cell-like nuclear morphology and do not exhibit condensed chromatin.

[0040] 2. Results: The effects of the three compounds on ...

Embodiment 3

[0042] Cell Cycle Assay:

[0043] 1. Materials: RNase A (product of USB Company), 81.4 units / mg, batch number: 110266-007; PI (propidiumiodide) (product of Sigma Company, batch number: 042k3655).

[0044] 2. Methods: HepG2 and HL-60 cells were cultured by conventional methods, collected after administration, washed twice with PBS and fixed overnight with 70% alcohol. Centrifuge at 1000rpm / 10min to remove ethanol, wash twice with PBS containing 1% fetal bovine serum, resuspend with 2ml of PBS containing 1% fetal bovine serum, add RNase enzyme (final concentration 0.5mg / ml) to digest for 1 hour, and then Add PI (2.5ug / ml) for staining, place on ice for 20min, and then detect with flow cytometry.

[0045] 3. Results: The three compounds can stop HepG2 in the G2 / M phase at 30um in a time-dependent manner (Table 2). At 20um for 12 hours, HL-60 cells were arrested in G2 / M phase with obvious apoptosis (Table 3) (Figures 16-19).

[0046] compound

[0047] compoun...

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Abstract

The invention relates to a the antineoplastic action of a group of looped pineapple confectionery terpenoid, which is three 9, 19 looped lanolinum alkyl triterpenoid (23-oxygen-acetyl cimicifugol - 3 -oxygen - beta - D - xyloside, 24 - oxygen - acetyl cimicifugol - 3 -oxygen-beta-D-xyloside and 25-oxygen-acetyl cimicifugol - 3 -oxygen - beta - D - xyloside) extracted from cimicifuga rhizome. Experimental investigation has shown that they have cell toxic action for blood tumor and entity tumor.

Description

Technical field: [0001] The present invention relates to a group of cyclopine (9,19 cyclolanolane) triterpenoids obtained from Cimicifuga cimicifolia, which have cytotoxic effects on blood tumors and solid tumors, induce apoptosis, affect cell cycle, and resist Oxidation and its application in the clinical prevention and treatment of tumors. Background technique: [0002] Cimicifuga is a plant of the genus Cimicifuga (Cimicifuga I.) in the family Ranunculaceae, including Cimicifuga or Cimicifugafoetida (Cimicifugafoetida), Northern Cohosh or Xing'an Cimicifuga (Cimicifuga dahurica) and Cimicifuga nanchuanensis). According to records, Cimicifuga has the functions of clearing heat and detoxifying, promoting Yang Qi, and expelling rashes. It is mainly used to treat wind-heat headache, toothache, sore throat, and uterine prolapse. The rhizome of C.dahurica Turcz.Maxim. has been included in the Chinese Pharmacopoeia (2000 edition) as a commonly used traditional Chinese medicine,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/704A61P35/00
Inventor 肖培根杨梦甦田泽斯建勇陈迪华
Owner 肖培根
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