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Norcenane sesquiterpenes, pharmaceutical composition, preparation method and application thereof

A compound and drug technology, applied in the field of natural medicinal chemistry, can solve problems such as no medicinal records

Active Publication Date: 2022-02-25
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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  • Norcenane sesquiterpenes, pharmaceutical composition, preparation method and application thereof
  • Norcenane sesquiterpenes, pharmaceutical composition, preparation method and application thereof
  • Norcenane sesquiterpenes, pharmaceutical composition, preparation method and application thereof

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] ‒ (calcd for C 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 ) from the tail vein to collect blood, apply a thin blood film, fix with methanol, stain with Wright-Giemsa mixed staining method, and observe under a 10×100 oil microscope. If no Plasmodium asexual body is found after randomly checking 50 fields of view, it will be judged as negative, and if a positive thin blood film is randomly counted, 5 fields of view should be randomly counted, and the total number of red blood cells should not be less than 1000, and then the Plasmodium inhibition rate should be calculated a...

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Abstract

The invention relates to a preparation method and application of a class of norcine sesquiterpenes and a pharmaceutical composition thereof, belonging to the field of natural medicine chemistry. Formula (I) noreucalyptane sesquiterpenoids, a pharmaceutical composition with such compounds as active ingredients, and its preparation method is to take the root or rhizome or the whole plant of the Anacardiaceae genus genus, and use the organic solvent petroleum ether Or chloroform or ethyl acetate or acetone or methanol or ethanol or water direct cold immersion or heat reflux or ultrasonic or microwave auxiliary extraction, or use the above-mentioned organic solvent or water cold immersion or reflux or ultrasonic or microwave auxiliary extraction and then use acetic acid The total extract was obtained by extraction with ethyl ester, and the compound of the present invention was obtained from the total extract through repeated chromatography. An antimalarial drug compound with the compound of the present invention as an active ingredient. Use of the compound of the present invention in the preparation of antimalarial 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 fo...

Claims

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Application Information

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Patent Type & Authority Patents(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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