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Friedelane triterpenoid and preparation method as well as application thereof

A technology of triterpenoids and compounds of suberane type, which is applied in the fields of steroids, organic chemistry, and pharmaceutical formulations, etc.

Inactive Publication Date: 2013-08-14
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To sum up, there are very few reports on the biological activities of secosurane compounds, and there are only research reports on the inhibition of COX-2 and AGEs by these compounds

Method used

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  • Friedelane triterpenoid and preparation method as well as application thereof
  • Friedelane triterpenoid and preparation method as well as application thereof
  • Friedelane triterpenoid and preparation method as well as application thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0055] 1. Preparation of compounds

[0056] (1) Take 10kg of dried Viola vine herb, reflux with 120L, 100L and 80L of 95% ethanol for 2 hours, combine the ethanol extract, recover the ethanol and concentrate it under reduced pressure to nothing. Alcoholic taste, get the total extract;

[0057] (2) Dissolve the total extract in water, then extract 3 times with 1.4L petroleum ether, 3L ethyl acetate and 3L water-saturated n-butanol successively, take the n-butanol extract, concentrate under reduced pressure to remove the solvent, and obtain Butanol extract 168g;

[0058] (3) Dissolve 84g of n-butanol extract in 600ml of water, pass through a D-101 macroporous resin column, and then use water, ethanol with a concentration of 10%, ethanol with a concentration of 30%, ethanol with a concentration of 60%, and ethanol with a concentration of Elute with 90% ethanol and 95% ethanol; collect the 95% ethanol eluate through a 200-300-mesh silica gel column, use petroleum ether-ethyl ace...

example 2

[0067] Example 2: (injection)

[0068] Take 1000 mg of the compound obtained by the method described in Example 1 above, add 1000 ml of water for injection, adjust the pH value to 7-7.5 with sodium carbonate, stir to dissolve, sterilize and filter, potting, and circulate steam at 100 ° C for 15 minutes Sterilize and make each 2mg / 2ml injection for injection.

example 3

[0069] Example 3: (capsules)

[0070] Take the compound 5000mg obtained by the method described in the above-mentioned Example 1 and fully mix with auxiliary materials such as 4000mg microcrystalline cellulose, 500mg sodium carboxymethyl starch, 400mg sodium lauryl sulfate, and carry out dry granulation by roller compaction, and then mix with An appropriate amount of magnesium stearate is mixed, filled into 3# hollow capsules, and made into capsules with a specification of 100 mg / grain for oral use.

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Abstract

The invention relates to a 3,4-seco-friedelolactone triterpenoid. The molecular structure of the compound is shown in the formula (I) in the specification. The compound is obtained by carrying out ethanol reflux extraction, organic solvent extraction and column chromatography separation and purification on viola diffusa ging. The compound has anti-HBV (hepatitis B virus) activity and can be used for preparing medicines for preventing and treating hepatitis B.

Description

technical field [0001] The present invention relates to an oxygen-containing heterocyclic compound, in particular to a 3,4-splitting cycloberene-type triterpenoid compound. Background technique [0002] Scleotene compounds are rarely distributed in nature. In 1968, apetalactone, the first scleotene compound apetalactone, was isolated from the leaves of the genus Calophyllum apetalum in 3 and 4 positions. (Govindachari TR, Prakash D, Viswanathan N. Apetalactone, a New Triterpene Lactone from Calophyllum Species. J Chem Soc (C), 1968, 1323-1324). Subsequently, the compound was also isolated from the same genus Calophyllum tomentosum and Calophyllum moonii (Dharmaratne HRW, Sotheeswaran S, Balasubramaniam S. Triterpenes and Neoflavonoids of Calophyllum Lankaensis and Calophyllum Thwaitesii.Phytochemistry, 1984, 23 (11): 2601-2603; Bandara BMR, Dharmaratne HRW, Sotheeswaran S, Balasubramaniam S. Phytochemistry, 1986, 25(2):425-428). In 1975, Lithocarpic lactone, another cleava...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/585A61P31/20
Inventor 朱全红戴娇娇陶华明
Owner SOUTHERN MEDICAL UNIVERSITY
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