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

Eremophilone lactones acid natural product and application thereof

A technology of lactone acid and lactone, which is applied in the field of natural medicinal chemistry and pharmacology, can solve the problems that the research on biological activity has not been reported yet

Inactive Publication Date: 2007-03-07
ZHEJIANG UNIV
View PDF0 Cites 93 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the chemical constituents and biological activity of Ligularia black purple

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
  • Eremophilone lactones acid natural product and application thereof
  • Eremophilone lactones acid natural product and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation of compound (A)

[0021] Take 5.0 kg of dry underground part of Ligularia spp., crush it into powder, add 50 liters of 95% ethanol to soak it. Soak 3 times at room temperature, 7 days each time. The ethanol extracts were combined, and the solvent was recovered under reduced pressure to dryness to obtain 462 grams of extract, dispersed with 3 liters of water, and then extracted with 60-90° petroleum ether, ethyl acetate, and n-butanol in sequence. The ethyl acetate extract was recovered under reduced pressure to obtain 89.0 g of extract. The extract was chromatographed on 800 g of 100-200 mesh silica gel column, and chloroform-methanol (50:0-0:1) gradient eluted. TLC detection The same fractions were combined, and the fractions containing compound (A) were concentrated in the 20:1 and 10:1 eluents. The solvent was evaporated to dryness under reduced pressure to obtain 6.9 grams of extract, which was then purified by column chromatography ...

Embodiment 2

[0025] Embodiment 2: the cytotoxic activity of compound (A) to KB cell

[0026] KB (oral epithelial carcinoma) cells were cultured with RPMI 1640 medium containing 10% fetal bovine serum, 100 U / mL penicillin and 100 U / mL streptomycin. cells in 5×10 per well 3 concentration into a 96-well plate at 37 °C with 5% CO 2 Incubate for 24 hours in a humidified incubator.

[0027]Cell viability was determined by the modified MTT method. After the cells were incubated for 24 hours, the newly prepared dimethyl sulfoxide solution of compound (A) was added to each well in a concentration gradient, so that the final concentrations of compound (A) in the wells were 100 μg / mL, 33.3 μg / mL, respectively. mL, 11.1 μg / mL and 3.7 μg / mL. After 72 hours, add 10 μL of MTT (5 mg / mL) in phosphate buffer, continue to incubate at 37 ° C for 4 hours, centrifuge for 5 minutes to remove unconverted MTT, and add 200 μL of dimethyl sulfoxide to each well to dissolve the reduced MTT crystal formazan (form...

Embodiment 3

[0030] Example 3: Cytotoxic activity of compound (A) on HL-60 cells

[0031] HL-60 (human myeloid leukemia cells) were cultured with RPMI 1640 medium containing 10% calf serum, 100 U / mL penicillin and 100 U / mL streptomycin. cells at 1×10 per well 4 Seed into 96-well plates at 37 °C with 5% CO 2 Incubate for 24 hours in a humidified incubator.

[0032] The assay of cell viability uses the improved MTT method, and the specific method is the same as in Example 2. Wherein compound (A) half inhibitory concentration (IC) to HL-60 cell 50 ) obtained from the dose-response curve.

[0033] IC of compound (A) 50 For: 2.08×10 -4 M; while the IC of positive control cisplatin on HL-60 cells 50 is 2.07×10 -5 M.

[0034] Experimental conclusion: This experiment shows that the natural product of erimofen lactone acid has strong cytotoxicity to HL-60 cells, and it may be developed into a new drug with the effect of treating leukemia and related tumors.

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

No PUM Login to View More

Abstract

The invention discloses an eremophilane lactone compound with chemical name as 3beta-chiretta acyloxy group-eremophile-7(11)-alkylene-12, 8beta-lactone-14-acid, which can inhibit the biological activity of HL-60, CNE, KB, Hela and P338D1.

Description

technical field [0001] The invention belongs to the technical field of natural medicinal chemistry and pharmacology. Specifically, it relates to a natural product of erimofen lactone and its medical application. Background technique [0002] At present, due to environmental pollution and other problems brought about by industrial development, the quality of human living environment is continuously declining, and the incidence and mortality of tumor diseases are also increasing. However, the selectivity of cytotoxic antineoplastic drugs currently used in clinical practice is not high, resulting in malignant killing of normal cells, which limits the universal use of such drugs. Therefore, searching for and discovering new highly selective cytotoxic antitumor drugs is a worldwide research hotspot. We are also working on the research of this class of drugs. [0003] Ligularia atroviblacea (Franch.) Hand.-Mazz. is a plant of the genus Ligularia in the family Asteraceae. It is ...

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
IPC IPC(8): C07D307/92A61K31/343A61K9/00A61P35/00
Inventor 赵昱周长新施树云王晓雨巫秀美张勇民白骅
Owner ZHEJIANG UNIV
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