Use of dipolymer of phthalide

A composition and technology of anti-tumor drugs, applied in the application field of preparing anti-tumor drug compositions, can solve problems such as toxic side effects, limited clinical application, etc., achieve fast effect, enhanced killing of tumor cells, and multi-drug resistance Sex-reducing effect

Active Publication Date: 2005-10-12
JIANGSU MICRODIAG BIOMEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the known reversal agents have obvious toxic and side effects when they revers

Method used

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  • Use of dipolymer of phthalide
  • Use of dipolymer of phthalide
  • Use of dipolymer of phthalide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Isolation and identification of LA

[0035] The process steps of separating and purifying compound LA from Chuanxiong or Angelica can be found in figure 1 flow chart.

[0036] The separation method of LA can be found in the articles of wang PS et al. (Phytochemistry 1984; 23; 2033-8 and Chinese Pharmaceutical Industry 1988; 19:553-9) or Kaouadji M et al. (J Nat Prod 1986; 49:872-7) and Naito Two articles by T et al. (Heterocycles 1991; 32: 2433-42).

[0037] The invention according to figure 1 The process steps obtained from Rhizoma Chuanxiong are colorless and transparent crystals, which are identified by LC-MS and HNMR. The real-time chromatographic data of LC-MS detected by chuanxiong extract at 294nm Figure 2A and Figure 2B .

[0038] Embodiment 2-7 is to the cytological utility evaluation of compound LA

[0039] Among them, the cell lines used are k562 (human chronic myelogenous leukemia cell line) and k562 / adr (k562 cell line resistant to chemo...

Embodiment 2

[0044] Example 2: Measuring the main drug resistance mechanism of each drug-resistant strain

[0045] Collect cultured 5×10 6 K562, k562 / adr, kb, kbv200 cells were washed twice with PBS, followed by the instructions of the P-gp fluorescent antibody kit (UIU2), and FACS was performed to detect the expression of P-gp, and 10,000 cells were counted for each sample.

[0046]The determination results of the main drug resistance mechanism of each drug-resistant strain:

[0047] k562: P-gp expression 1.02%; k562 / adr: P-gp high expression up to 83.6%;

[0048] kb: P-pg expression was 0.87%; kbv200: P-gp was highly expressed to 76.3%.

[0049] The above experiments proved that the main drug resistance mechanism of the two drug-resistant cell lines k562 / adr and kbv200 was overexpression of P-pg, while the expression of p-gp in the sensitive strains was negative.

Embodiment 3

[0050] Embodiment 3: Measuring the multiples of drug resistance of each drug-resistant strain to doxorubicin and vincristine

[0051] 1).k562 / adr cell line

[0052] Take cells in the logarithmic growth phase, use RPMI1640 culture medium containing 10% calf serum to make cell suspension, add 100ul per well to a 96-well plastic culture plate, so that the number of cells per well is 2×10 4 After 30 minutes, add 100ul chemotherapeutic drugs doxorubicin and vincristine according to the concentration gradient of 0, 0.01, 0.1, 0.5, 1, 5, 10, and 20ug / ml respectively. The volume is 200ul, and the insufficient part is made up with RPMI 1640, placed in a carbon dioxide incubator, 37°C, saturated humidity, 5% CO 2 cultured under the condition of CO 2 conditions for 68 hours. Add 50ul of MTT (2mg / ml) to each well to remove the supernatant, add 120ul of DMSO to each well, oscillate with a micro-oscillator to fully dissolve the drug, and detect the OD value at 590nm wavelength by Elisa. ...

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Abstract

An application of the phenyl phthaleine dipolymer Levistolide A (LA) in preparing antineoplastic medicines is disclosed. Said compound features broad spectrum, high effect to kill cancer cells and low toxic by-effect to cardiovascular system and immune system.

Description

technical field [0001] The invention relates to the application of a phthalide dimer and the compound Levistolide A (LA) in the preparation of an antitumor drug composition. Background technique [0002] Tumor multidrug resistance (multidrug resistance, MDR) is an important reason for the failure of chemotherapy. Multidrug resistance refers to the cross-resistance of tumor cells to various anticancer drugs with different chemical structures, functions and mechanisms of action. In a sense, 90% of cancer deaths are related to primary or acquired drug resistance. [0003] The mechanism causing MDR is relatively complicated, but the overexpression of the main "drug pump" P-gp protein on the tumor cell membrane is an important cause of MDR. The product of mdr1 gene, P-gp (p-glycoprotein), is a transmembrane glycoprotein that reduces the accumulation of cytotoxic drugs in cells through an energy-dependent mechanism and acquires multidrug resistance. Solid tumors, including colo...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P35/00
Inventor 陈菲王弢吴一峰张弘钱凯先
Owner JIANGSU MICRODIAG BIOMEDICINE TECH CO LTD
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