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Application of triterpenoid compound in preparation of antitumor medicines

An anti-tumor drug, triterpenoid technology, applied in the field of biomedicine, can solve the problems of drug resistance, unsatisfactory drug effect, lack of selectivity, etc., and achieve the effect of inhibiting proliferation

Inactive Publication Date: 2015-06-03
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the high dosage of clinical antineoplastic drugs in the prior art, the unsatisfactory drug effect, the lack of selectivity, the generation of drug resistance and the inhibition of the toxicity of the hematopoietic system, digestive system, immune system, nervous system and endocrine system. Shortcomings and deficiencies such as side effects provide a kind of application of triterpenoids in the preparation of antitumor drugs

Method used

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  • Application of triterpenoid compound in preparation of antitumor medicines
  • Application of triterpenoid compound in preparation of antitumor medicines
  • Application of triterpenoid compound in preparation of antitumor medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Prepares Tormentic acid from Raspberry palmatum

[0033] (1) 5Kg of the palm leaf raspberry 5Kg purchased will be pulverized and sieved, mixed in batches with 10 times the amount (mass) of ethanol with a volume fraction of 95% to extract three times under reflux, combine the extracts, filter, and use a rotating The evaporator concentrated and evaporated to dryness under reduced pressure at 40°C, recovered ethanol, and obtained the ethanol crude extract of raspberry palmate;

[0034] (2) the raspberry palmate ethanol crude extract extract prepared by step (1) is dissolved with 1.5L of methanol, then add an equal volume of sherwood oil solvent (i.e. add the volume of sherwood oil volume=crude extract+methanol ), fully vibrate and mix, and let stand for 2h. After the two-phase solvents are completely separated, suck out the petroleum ether phase in the upper layer; repeat the extraction three times, combine the petroleum ether extracts, concentrate under reduced ...

Embodiment 2

[0036] Example 2 Determine the structure of compound 1

[0037] Compound 1 (trace amount) prepared in Example 1 was dissolved in chromatographic methanol, and analyzed by ESI-MS of Esquire HCTplus type large-capacity ion trap LC / MS. The mass-to-charge ratio m / z scanning range: 200 to 2000, obtained Sample positive ion mass spectrum ( figure 1 ). Dissolve compound 1 with pyridine, a deuterated reagent, and place it in a nuclear magnetic resonance tube. Using a Bruker DRX-400 nuclear magnetic resonance instrument, tetramethylsilane (TMS) is used as an internal standard to measure its hydrogen spectrum (1H-NMR), full decoupling Carbon spectrum (13C-NMR).

[0038] Compound 1 is a white amorphous powder. ESI-MS m / z:511[M+Na] + (Introduction molecular formula is C30-H48-O5). 1 H-NMR (C 5 D. 5 N)δ: 1.02(3H, s), 1.11(3H, s), 1.13(3H, s), 1.15(3H, d, J=6.5Hz), 1.30(3H, s), 1.44(3H, s) ,1.74(3H,s),3.08(1H,s,18-H),3.41(1H,d,J=9.3Hz,3-H),4.13(1H,m,2-H),5.59(1H, brs,12-H). 13 C-N...

Embodiment 3

[0039] Example 3 Tormentic acid inhibits the proliferation of tumor cells of different histological types

[0040] Vigorously growing human liver cancer HepG-2 cells, human liver cancer Bel-7402 cells, human lung cancer A549 cells and human breast cancer MCF-7 cells were taken respectively, centrifuged at 1000rpm for 5min, discarded the supernatant, and used fetal tissue containing 10% mass fraction. The DMEM medium of bovine serum adjusted the cell number to 3×10 4 / mL, 100 μL was inoculated in a 96-well culture plate, placed in 5% CO 2 After culturing at 37°C for 24 h in the incubator, the supernatant was discarded, and DMEM medium containing Tormentic acid was added to each group (the final concentrations of Tormentic acid were 6.25 μg / mL, 12.5 μg / mL, 25 μg / mL, 50 μg / mL, respectively). mL and 100 μg / mL). At 37°C, 5% CO 2 Culture in an incubator for 24 hours, discard the supernatant, wash twice with PBS, add 200 μL of serum-free DMEM medium and 20 μL of thiazolyl blue (MT...

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Abstract

The invention belongs to the field of biological medicines, and particularly relates to an application of a triterpenoid compound in preparation of antitumor medicines. A structural formula of the triterpenoid compound (tormentic acid) is shown in a formula I; and the tormentic acid is capable of obviously inhibiting proliferation of tumor cells, and significantly promoting apoptosis, so as to cause tumor cell death. The dosage of the tormentic acid is low; the toxic and side effects are lower than those of clinical common chemotherapeutic medicines; and the triterpenoid compound can be used as a novel anti-tumor medicine, is applied to treatment of tumors, and is simple in medication way and easy to operate.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the application of a triterpenoid compound in the preparation of antitumor drugs. Background technique [0002] Tumor mortality ranks first or second in the world, which is a great threat to human survival and health. Tumor treatment has always been a difficult problem for the medical community, and surgery, chemotherapy and radiotherapy are the usual treatments. However, most of the existing treatment methods will have serious side effects, such as bleeding, cognitive impairment, multiple hairs, etc., which are mainly related to their non-selective cytotoxicity. For chemotherapy, resistance to emerging drugs is another serious problem. Finding new anticancer drugs with less toxic side effects and selective killing has always been one of the main research goals of scientists all over the world. Natural products, including plants, marine organisms and microorganisms, have...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P35/00
Inventor 姜建国张恬恬
Owner SOUTH CHINA UNIV OF TECH
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