Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Use of dipolymer of phthalide

A technology of anti-tumor drugs and compositions, which is applied in the field of preparation of anti-tumor drug compositions, can solve the problems of limited clinical application, toxic and side effects, etc., and achieve enhanced killing of tumor cells, fast effect, and multi-drug resistance sex-reducing effect

Active Publication Date: 2007-08-15
JIANGSU MICRODIAG BIOMEDICINE TECH CO LTD
View PDF4 Cites 0 Cited by
  • 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 reverse the concentration in the effective body, and the clinical application is very limited.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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 for isolating and purifying the compound LA from Chuanxiong or Angelica sinensis can be seen in the flow chart of FIG. 1 .

[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 material obtained from Ligusticum chuanxiong according to the process steps in Fig. 1 in the present invention is a colorless transparent crystal, which is identified by LC-MS and HNMR. The LC-MS real-time chromatographic data of Chuanxiong extract at 294nm are shown in 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...

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. ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
hydrophobicityaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com