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Triterpenoids as well as preparation method and application thereof

A kind of technology of triterpenoids and compounds, applied in the field of triterpenoids and preparations thereof

Active Publication Date: 2022-03-04
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Queer tongue is mainly used in the folks in Henan for the treatment of lung cancer, viral hepatitis, nephritis and paralysis. better inhibitory effect, while the chemical constituents and pharmacological activities of the other eight species of Bugia plants are also blank, and there is no literature report

Method used

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  • Triterpenoids as well as preparation method and application thereof
  • Triterpenoids as well as preparation method and application thereof
  • Triterpenoids as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Take 18.0kg of dry whole herb of A. chinensis, grind it, heat and reflux with 75% ethanol to extract 3 times, the ratio of solid to liquid is 1:8, each time for 2h, recover the solvent under reduced pressure, disperse the extract with distilled water, and use etc. Volume of petroleum ether, chloroform, ethyl acetate and n-butanol extraction 3 times to obtain petroleum ether layer extract 126.4g (extract 1), chloroform layer extract 26.7g (extract 2), ethyl acetate layer extract 36.1g g (extract 3), n-butanol layer extract 162.3g (extract 4).

[0111] The obtained chloroform layer extract 26.7g, adopt normal phase silica gel column chromatography to separate, and mobile phase selects sherwood oil: ethyl acetate (100:0-1:1) and dichloromethane: methanol (50:1-1:1) ) gradient elution, the obtained components were analyzed by silica gel thin-layer chromatography, and 15 parts of eluates were obtained after merging the same components.

[0112] Petroleum ether:ethyl acetate...

Embodiment 2

[0114] Take 27.1 kg of dried Leptopus clarkei (Hook.f.) Pojark., crush it, heat and reflux with dichloromethane to extract 3 times, the ratio of solid to liquid is 1:8, each time for 1.5h, and recover under reduced pressure Solvent, the extract is dissolved in chloroform, acetone and methanol respectively. Take 37.3 g of chloroform layer extract, separate by silica gel column chromatography, elute with a solvent system composed of petroleum ether-ethyl acetate and petroleum ether-acetone, supplemented with 1-2 drops of glacial acetic acid, and obtain 12 parts of fractions, Petroleum ether: ethyl acetate = 50:1 component 1.7g was repeatedly separated by silica gel column chromatography, and the yellow solid powder was separated by preparative HPLC to obtain compounds 3, 4, 13, and 14; at 8:1, for The yellow solid powder was separated by semi-preparative HPLC to obtain compounds 5, 9, 16, 18, and 24. Petroleum ether:ethyl acetate=25:1 component 2.3g was separated. Silica gel c...

Embodiment 3

[0116]Leptopus chinensis (Bunge) Pojark dried whole herb 19.2kg, pulverized, heated and refluxed with 60% ethanol to extract 3 times, the ratio of solid to liquid is 1:8, each time for 1.5h, the solvent is recovered under reduced pressure, used for extract Disperse with distilled water and centrifuge to take the supernatant. After the supernatant is treated with non-polar macroporous resin D101, it is sequentially eluted with water and alcohol gradients, and the eluted fractions of 30% to 100% alcohol are collected. Or HPLC (210nm) screening, screening is rich in the effective part of triterpenoid compound, promptly obtains triterpene crude extract; Gained triterpene crude extract 35.7g, adopts normal phase silica gel column chromatography to separate, with n-hexane-di A solvent system consisting of methyl chloride, dichloromethane-ethyl acetate, and dichloromethane-methanol was used for gradient elution, and the obtained components were analyzed by silica gel thin-layer chroma...

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Abstract

The invention belongs to the technical field of medicines, relates to a triterpenoid compound as well as a preparation method and application thereof, in particular to a triterpenoid compound obtained from stellaria plants, such as stellaria alpina, stellaria lanceolata, stellaria yunnanensis and stellaria glandulifera, as well as a preparation method and application thereof, and belongs to the technical field of medicines. The compound and the salt thereof are as shown in a formula (I) or (II), wherein R1 to R4 are as shown in the claims and the description. The triterpenoids have good anti-tumor activity and can be used for preparing anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to triterpenoids and their preparation methods and applications, in particular to triterpenoids obtained from Buchus genus plants, Buchus linearis, Buchus yunnanensis and Buchus glandularis The triterpenoid compound and its preparation method and application belong to the technical field of medicine. Background technique [0002] Euphorbiaceae (Euphorbiaceae) genus Leptopus, also known as the genus Leptopus, has about 20 species in the world, distributed from the northern Himalayas to southeastern Asia, through Malaysia to Australia. There are nine species in my country, distributed in southern China, mainly in Sichuan, Guangdong, Guangxi, Yunnan, Guizhou, Hainan and other places. Perennial herbaceous plants such as Leptopus lolonum (Hand.-Mazz.) Pojark., Laptopus lolonum (Hand.-Mazz.) Pojark., Laptopus yunnanensis, and Laptopus glandularis, grow in mountain bushes at an altitude of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P35/00
CPCC07J63/008A61P35/00Y02A50/30
Inventor 高慧媛齐世洲隆李萍刘婷张鑫鑫井文华
Owner SHENYANG PHARMA UNIVERSITY