Dihydroxy isoquinoline and preparation method and application thereof from centipedes

A technology of dihydroxyisoquinoline and centipede, which is applied in the application fields of antimalarial, antibacterial and antitumor active drugs, and can solve the problems of complex components and limitations in the application of centipede

Active Publication Date: 2016-03-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no research to prove that the components with anti-tumor or antibacterial activity in centipede are specific substances. Because the components of centipede extract are complex and may also contain toxic components similar to bee venom, centipede is used in the preparation of anti-tumor or antibacterial substances. Application in the field of antibacterial drugs has been limited

Method used

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  • Dihydroxy isoquinoline and preparation method and application thereof from centipedes
  • Dihydroxy isoquinoline and preparation method and application thereof from centipedes
  • Dihydroxy isoquinoline and preparation method and application thereof from centipedes

Examples

Experimental program
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Effect test

Embodiment 1

[0054] Preparation and Structure Identification of 3,8-Dihydroxyisoquinoline from Centipede

[0055] A. water extraction method and alcohol extraction method prepare centipede extract:

[0056] (1) Grinding the dry body of the centipede to obtain centipede powder, adding 10 times the volume of the centipede powder (5-10 times the volume is acceptable, preferably 10 times in this embodiment, and the same reasoning behind), and then performing ultrasonic crushing;

[0057] (2) Carry out refrigerated centrifugation to the homogenate, get the supernatant, freeze-dry to obtain centipede aqueous extract

[0058] (3) Take the precipitate obtained in step (2), add 55% (volume fraction, the same reason behind) ethanol homogenization of 10 times the volume of the precipitate, then leaching at 4°C, and freeze and centrifuge the leaching solution again , take the supernatant, freeze-dry to obtain centipede 55% ethanol extract;

[0059] (4) Take the precipitate obtained in step (2), add ...

Embodiment 2

[0085] The step of extracting active component in the present embodiment is basically the same as embodiment 1, and difference is: 1) during water extraction, the PBS solution volume that adds is 5 times of centipede powder volume, during alcohol extraction, the volume fraction of alcoholic solution is 45%; 2) When adopting Sephadex gel chromatography to separate and purify centipede ethanol extract, centipede ethanol extract is configured to 20mg / mL, mobile phase is 50% ethanol, loading volume is 8mL, and flow rate is 0.6mL / min.

[0086] The result of this example is the same as Example 1, and the active substance finally obtained is identified as 3,8-dihydroxyisoquinoline (isoquinoline-3,8-diol) by structure, and the molecular formula is C 9 h 7 NO 2 , the molecular weight is 161.1, and the structural formula is:

[0087]

Embodiment 3

[0089] The step of extracting active component in the present embodiment is basically the same as embodiment 1, and difference is: 1) during water extraction, the PBS solution volume that adds is 8 times of centipede powder volume, during alcohol extraction, the volume fraction of alcoholic solution is 65%; 2) When adopting Sephadex gel chromatography to separate and purify centipede ethanol extract, centipede ethanol extract is configured to 35mg / mL, mobile phase is 30% ethanol, sample volume is 6mL, and flow rate is 1.5mL / min.

[0090] The result of this example is the same as Example 1, and the active substance finally obtained is identified as 3,8-dihydroxyisoquinoline (isoquinoline-3,8-diol) by structure, and the molecular formula is C 9 h 7 NO 2 , the molecular weight is 161.1, and the structural formula is:

[0091]

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Abstract

The invention discloses dihydroxy isoquinoline and a preparation method and application thereof from centipedes, and belongs to the field of medicine. The dihydroxy isoquinoline is 3,8-dihydroxy isoquinoline, is extracted from centipedes and can be used for treating malaria and solid tumors and killing bacteria. The malaria is plasmodium vivax, malaria plasmodium, plasmodium falciparum and plasmodium ovale parasitizing the human body. The bacteria are escherichia coli, staphylococcus aureus, pseudomonas aeruginosa, alpha / beta hemolytic streptococcus, streptococcus pneumoniae and haemophilus influenzae. The tumors are primary or secondary cancers and sarcomas deriving from the head and neck portion, brain, thyroid gland, pancreas, lungs, liver, esophagus, stomach, mammary gland, kidneys, gall bladder, colon or rectum, ovary, uterus, cervix uterus, prostate, bladder and testis of the human body. The dihydroxy isoquinoline has small toxic and side effects, and can be used for treatment and auxiliary treatment of various cancers.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the extraction of a new compound 3,8-dihydroxyisoquinoline from centipedes and the application of the active substance in drugs with antimalarial activity, antibacterial activity and antitumor activity. Background technique [0002] Malignant tumors are the primary killer of human health. Although traditional tumor therapy has a certain curative effect, due to the non-specific cytotoxicity of chemical drugs, it has relatively large toxic and side effects on patients, and it is also prone to drug resistance, which brings great pain to tumor patients. Since Folkman put forward the theory of tumor angiogenesis in 1972, there have been a large number of reports of treating tumors by inhibiting tumor angiogenesis, and achieved great success. Tumor angiogenesis is the morphological basis of tumor growth and metastasis. The vast majority of malignant solid tumors such as ovarian cancer, liver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D217/24A61P33/06A61P31/04A61P35/00
CPCC07D217/24Y02A50/30
Inventor 徐寒梅丁丹
Owner CHINA PHARM UNIV
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