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Eudesmane norsesquiterpenoids and pharmaceutical composition thereof, preparation method and application of pharmaceutical composition

A technology of compound and hydroxyl, which is applied in the field of natural medicinal chemistry, can solve problems such as no medicinal records, and achieve good antimalarial activity

Active Publication Date: 2019-10-08
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are no records of its medicinal use and other active research reports

Method used

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  • Eudesmane norsesquiterpenoids and pharmaceutical composition thereof, preparation method and application of pharmaceutical composition
  • Eudesmane norsesquiterpenoids and pharmaceutical composition thereof, preparation method and application of pharmaceutical composition
  • Eudesmane norsesquiterpenoids and pharmaceutical composition thereof, preparation method and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Extraction, separation and purification of compound 1-9 of the present invention:

[0041]Dry the rhizomes (19 kg) of the genus Chiapodium in the shade, crush them to 30 meshes, extract them three times with 95% methanol at room temperature, 70 L each time for 24 hours, combine the extracts, and concentrate the extracts under reduced pressure to obtain Suspend the extract with an appropriate amount of water, and distribute it several times with ethyl acetate to obtain an ethyl acetate extract (1.5 kg). The extract is dissolved in an appropriate amount of chloroform / acetone and mixed with silica gel 80-100 mesh, and then mixed with 650 G silica gel 200-300 mesh was used for column chromatography, and the gradient elution was carried out with chloroform / acetone (1 : 0-0 : 1), and 8 main parts were obtained. The pure chloroform part, 9: 1 chlorine / acetone Part and part of 8:2 chlorine / propane were subjected to silica gel column chromatography, and gradient elution was carr...

Embodiment 2

[0043] Physical and spectral data of compound 1 of the present invention:

[0044] Compound 1: white powder. [α] D 25 ‒41.4 ( c 0.11, MeOH); UV (MeOH) lambda max (log ε ) 216.0(4.26) nm; IR (KBr) ν max 3452, 2944, 1709, 1615, 1453, 1368, 1246, 1168, 1079,669 cm -1 ; 1 H and 13 C NMR data, see Table 1; HRESIMS m / z 307.1918 [M‒H] ‒ (calcdforC 18 h 27 o 4 , 307.1915).

[0045] Table 1 Compound 22 1 H NMR [ δ H (ppm), ( J Hz)] and 13 C NMR [ δ C (ppm)] Data a

[0046]

[0047] a Measured by Bruker Avance III-400 MHz nuclear magnetic resonance instrument, the chemical shift value is expressed in ppm, and the solvent is CD 3 COCD 3 .

Embodiment 3

[0049] Antimalarial activity detection of compounds of the present invention:

[0050] Using the internationally accepted 4-day inhibition test method, each mouse was inoculated intraperitoneally with 1×10 7 Plasmodium-infected red blood cells were given intragastric administration 3 hours after inoculation with Plasmodium, and then administered once every 24 hours for 4 consecutive days (the inoculation day was D 0 , the next day is D 1 , and so on), on day 5 (D 4 ) blood from the tail vein, coated with a thin blood film, fixed in methanol, stained with Wright-Giemsa mixed staining method, and observed under a 10×100 oil microscope. If no Plasmodium asexual body is found after randomly checking 50 fields of view, it is judged as negative, and the positive thin blood film is randomly counted in 5 fields of view, and the total number of red blood cells is not less than 1000, and then the inhibition rate of Plasmodium is calculated according to the following formula .

[005...

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Abstract

The invention relates to eudesmane norsesquiterpenoids and a preparation method and application of a pharmaceutical composition of the eudesmane norsesquiterpenoids, and belongs to the field of natural pharmaceutical chemistry. The eudesmane norsesquiterpenoids shown in a formula (1) is the pharmaceutical composition taking the eudesmane norsesquiterpenoids as active ingredients, and the preparation method includes the following steps that roots or rhizomes or the whole plants of dobinea plants of anacardiaceae are taken, and organic solvent petroleum ether or chloroform or ethyl acetate or acetone or methanol or ethanol or water is used for assisted extraction through direct cold soaking or hot reflux or ultrasonic or microwave, and the like, or first, assisted extraction is conducted through the organic solvent or the cold soaking by water or the reflux or the ultrasonic or the microwave, and the like, second, total extract is extracted with the ethyl acetate, the eudesmane norsesquiterpenoids is obtained through repeated chromatography. The eudesmane norsesquiterpenoids is an anti-malarial drug compound with active components, and the eudesmane norsesquiterpenoids is applied inthe preparation of anti-malarial agents.

Description

Technical field: [0001] The invention belongs to the field of natural medicinal chemistry, and specifically relates to a new class of norcine sesquiterpene compounds, a preparation method thereof, a drug combination with the compounds as active ingredients, and an antimalarial application thereof. [0002] technical background: [0003] Nine children ( Dobinea ) plants belong to Anacardiaceae or Podoaceae, and are shrubs or perennial subshrub-like herbs with hypertrophic rhizomes. There are 2 species in the world, Gastrodia chinensis ( Dobinea delavayi (Baill.) Baill.) and Gongshan Jiuzimu ( D. vulgaris Buch.-Ham. ex D. Don), all produced in my country. Gastrodia chinensis is a perennial subshrub-like herb with thick rhizomes. It is named after it is shaped like a horn after processing; it is produced in the central to northwestern part of Yunnan and southwestern Sichuan; it grows in sunny grass slopes or shrubs at an altitude of 1100-2300 meters . Folks are used for ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/533C07C67/48C07C229/38C07C227/40A61K31/22A61P33/06
CPCC07C69/533C07C229/38A61P33/06
Inventor 姜北肖朝江沈怡崔淑君陈浩沈磊董相王敏
Owner DALI UNIV
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