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Polyketone compound, preparation method and application thereof

A technology of polyketone compounds and compounds, applied in the field of medicine, to achieve the effect of low cytotoxicity

Inactive Publication Date: 2019-01-18
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report about the activity of polyketides isolated from this fungus to inhibit osteoclastogenesis

Method used

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  • Polyketone compound, preparation method and application thereof
  • Polyketone compound, preparation method and application thereof
  • Polyketone compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of Compounds 1-16

[0037] 1. Preparation of Total Crude Extract

[0038] 20L of the fermentation broth of the strain was ultrasonically extracted with conventional ethyl acetate, and the extract was concentrated under reduced pressure to obtain 25.0 g of the total crude extract.

[0039] 2. Separation and purification

[0040] The total crude extract was separated by normal phase silica gel chromatography (200-300 mesh), followed by petroleum ether: ethyl acetate = 10:1, 5:1, 3:1, dichloromethane: methanol = 50:1, 30 :1, 20:1, 10:1, 5:1, 3:1, 100% methanol eluent for gradient elution, according to TLC monitoring, according to the difference in polarity of each fraction, a total of 10 fractions were collected from small to large Partial eluate, expressed as Fraction A-Fraction J (Fr.A-Fr.J).

[0041] Fraction Fr.H was chromatographed on a Sephadex LH-20 gel column (mobile phase was dichloromethane:methanol=2:1), and 7 fractions were obtained, represented ...

Embodiment 2

[0091] Compounds 1-16 of the present invention inhibit the formation of osteoclasts

[0092] 1. Experimental animal strains

[0093] Female C57BL / 6 mice (18-20 g) were purchased from Shanghai Slack Experimental Animal Co., Ltd. All experimental operations were carried out in strict accordance with the national regulations on the use and maintenance of experimental animals, in line with the guidelines established by the experimental animal center of the author's unit, and approved by the Animal Ethics Committee of the Second Military Medical University.

[0094] 2. Experimental reagents, consumables and instruments

[0095] Three sets of ophthalmic scissors and ophthalmic tweezers; high-pressure steam sterilizer; three petri dishes; one 5ml sterile syringe; one T75 bottle; α-mem; gbico FBS (10%); PS (1%); Sulfone DMSO (sigma); pipette (Corning); 96-well plate (Corning); CO 2 Incubator (SANYO); TRAP stain.

[0096] 3. Experimental drugs

[0097] Compounds 1-16 of the presen...

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PUM

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Abstract

The invention discloses a polyketone compound, a cis-trans-isomer, a solvate or a pharmaceutical salt thereof. The structure is as follows. According to the invention, the polyketone compound is extracted and separated from epiphytic fungus Xylaria feejeenisis fermentation liquor of Stylissa massa. The polyketone compound has an activity of restraining cytopoiesis from marrow primary cells to osteoclasts, is low in cytotoxicity and can be used for preparing drugs for restraining generation of osteoclast.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a polyketide compound and its preparation method and application. Background technique [0002] The host sponge, Stylissa massa, belongs to the invertebrates of the class Heteroscleromorpha, the order Scopolinida, and the family Scopolinidae. There are few studies on the symbiotic fungi of the sponge Stylissa massa, and there are only 6 reports in the literature. At present, the compounds isolated from this sponge are mainly alkaloids, diterpenes and cyclic peptides (Deniz, T.; Robert, M.; Michael, G.; et al., Aldisine Alkaloids from the Philippine Sponge Stylissa massa Are Potent Inhibitors of Mitogen-Activated Protein Kinase Kinase-1 (MEK-1). Journal of Medicinal Chemistry 2002,45:529-532; Naphatson, C.; Supreeya, Y.; Chatchai, W.; et al. ,BifunctionalizedAmphilectane Diterpenes from the Sponge Stylissa cf.massa.Journal of Natural Products 2012,75:789-792; Masaki...

Claims

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Application Information

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IPC IPC(8): C07D313/00C07D309/38A61P19/08A61K31/366A61K31/365C12P17/02C12P17/06C12R1/645
CPCA61P19/08C07D309/38C07D313/00C12P17/02C12P17/06
Inventor 张文汤华王洁庄春林
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY