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Anticancer application of sesquiterpene

A sesquiterpene, cancer technology, applied in the field of anti-cancer application of sesquiterpene ths-cy-7, can solve the problems of unreported biological effects

Inactive Publication Date: 2011-07-06
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] ths-cy-7 is a sesquiterpenes extracted from marine organisms, Hakim, Euis Holisotan et al. (11, Hakim, Euis Holisotan.et al., Structural studies of three sesquiterpenes from Litsea spp.1993, 46 (9) : 1355-1362) and Wang, Jian et al. .) The sesquiterpene ths-cy-7 was isolated from different plants, but its biological role was not reported

Method used

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  • Anticancer application of sesquiterpene

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Sesquiterpene ths-cy-7 induces tumor cell apoptosis

[0032] 1) Sesquiterpene ths-cy-7 induces PARP protein degradation in cells

[0033] Liver cancer cells HepG2 were selected, cultured in 6-well tissue culture plates at 37°C and 5% carbon dioxide incubator, and treated with 20 μmol / L ths-cy-7 serum-free DMEM for 3, 6, 12, and 24 hours after 24 hours.

[0034] Liver cancer cells 7703 and cervical cancer cells Hela were selected, cultured in 6-well tissue culture plates at 37°C and 5% carbon dioxide incubator, and treated with 20 μmol / L ths-cy-7 serum-free DMEM for 24 hours after 24 hours.

[0035] Cells were lysed on ice for 30 min with modified RIPA lysis buffer (50 mM Tris-Hcl, pH 7.4; 150 mM NaCl; 5 mM EDTA; 1% NP-40, 0.5% sodium deoxycholate, 0.1% SDS). With the same loading amount, 8% SDS-PAGE electrophoresis, transfer membrane, block with 5% skimmed milk powder TBST (50mM Tris-HCl (pH 7.4), 150mM NaCl and 0.1% Tween-20) at room temperature for 1h, at r...

Embodiment 2

[0039] Effect of embodiment 2ths-cy-7 on Nur77 transcript level expression

[0040] 1) Cell culture

[0041] Select the human lung cancer cell line NIH-H460, in 10% calf serum DMEM medium (purchased from Hyclone), 37 ° C containing 5% CO 2 The cells were cultured in a 6-well tissue culture plate in a 6-well tissue culture box, and after 24 hours, the serum-free medium was changed to starve for 12 hours, and then the drug (serum-free) was added for treatment. ths-cy-7 was dissolved in DMSO (DMSO final concentration <0.2%), treated with 1 and 10 μmol / L respectively for 3 h, the negative control group was treated with the same concentration of DMSO for 3 h, and the positive control group was treated with phorbol ester 100 ng / mL ( TPA) processing 3h, concrete processing is as follows:

[0042] (1) negative control group (DMSO);

[0043] (2) positive control group (TPA);

[0044] (3) ths-cy-7 group (1 μmol / L);

[0045] (4) ths-cy-7 group (10 μmol / L).

[0046] Cells are collec...

Embodiment 3

[0049] Example 3 Induction of ths-cy-7 to Nur77 protein level expression

[0050] 1) Cell culture

[0051] In order to confirm the dose-effect relationship between ths-cy-7 and Nur77 expression, liver cancer cell HepG2 and lung cancer cell A549 were selected, and DMEM medium containing 10% fetal bovine serum (purchased from Hyclone) was used at 37°C with 5% CO 2 The cell culture box was cultured in a 6-well tissue culture plate. After 24 hours, the cells were treated with ths-cy-7. The treatment concentrations were 1, 5, 10, and 20 μmol / L, respectively, and the treatment time was 3 hours. The cells without any treatment were used as control.

[0052] In order to confirm the temporal relationship between ths-cy-7 and Nur77 expression, four cancer cells were selected: liver cancer cell HepG2, cervical cancer cell Hela, colon cancer cell HCT-116, and lung cancer cell A549, and the specific treatments were as follows:

[0053] (1) HepG2 cells were treated with ths-cy-7 at a conc...

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Abstract

The invention relates to an anticancer application of sesquiterpene, particularly provides application of sesquiterpene ths-cy-7 in preparing anticancer drugs and application of orphan receptor Nur77 as a target in screening marine living resources. The sesquiterpene ths-cy-7 can induce apoptosis of cancer cells and expression of orphan receptor Nur77, and the apoptotic effect on cancer cells is dependent on the extranuclear expression of Nur77. The sesquiterpene ths-cy-7, as a regulatory factor targeting Nur77 apoptotic pathway, becomes a very effective therapeutic drug on cancer. The anticancer drugs use the orphan receptor Nur77 as an action target.

Description

technical field [0001] The invention relates to a sesquiterpene, in particular to the anticancer application of a sesquiterpene ths-cy-7. Background technique [0002] Orphan receptor Nur77 (also known as TR3 or NGFI-B) is an important member of the nuclear receptor superfamily, encoded by the immediate early gene NR4A1, and its expression can be controlled by serum, growth factors, tetradecanoylphorbol acetate-13 (TPA), intracellular calcium ions, and some chemotherapeutic drugs rapidly induce (1, Zhang XK. et al, Expert Opin Ther Tar 2007; 11:69-79; 2, Moll UM, et al, Oncogene 2006; 25 : 4725-4743.). Multiple signal transduction pathways may be involved in the expression and function regulation of Nur77, including protein kinase A (PKA), protein kinase C (PKC), mitogen-activated protein kinase (MAPK), JNK, p38 and NF-κB pathways, etc. [0003] The expression of Nur77 has dual functions of promoting cell proliferation and apoptosis. It is highly expressed in many tumors a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/047A61P35/00A61P1/00A61P1/16A61P11/00A61P15/00
Inventor 曾锦章张晓坤陈鲤群林文翰
Owner XIAMEN UNIV
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