Application of terpene lactone compound for improving gastric motility disorder

A technology of gastric motility disorders and ester compounds, which is applied in the field of pharmaceutical compounds, can solve the problems of large side effects and poor effects, and achieve the effects of improving toxic and side effects, safety of applicable people, and wide application of people

Active Publication Date: 2020-03-17
武汉联合药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Drugs currently on the market for the treatment of gastric motility disorders have problems such as poor efficacy and large side effects. The

Method used

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  • Application of terpene lactone compound for improving gastric motility disorder
  • Application of terpene lactone compound for improving gastric motility disorder
  • Application of terpene lactone compound for improving gastric motility disorder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of compound of formula II

[0052] 1) Extraction: take 20kg of valerian herbal material, pulverize and extract with 50% ethanol (referring to an aqueous ethanol solution with a weight content of 50%) for 2 times of reflux extraction, each time for 2 hours, and the amount of ethanol each time is 120kg.

[0053] 2) Extraction: The ethanol extracts were combined and concentrated under reduced pressure to a clear paste with a relative density of 1.20, then n-hexane was added for extraction, and the n-hexane extract was collected.

[0054] 3) Separation: Weigh 700 g of 200-300 mesh silica gel, dry column packing, use petroleum ether (60-90 ° C) to elute and equilibrate, and pass the above-mentioned extract as a sample solution through a silica gel chromatographic column to make the effective components of the sample solution completely. Adsorbed on silica gel. Then use the mixed solvent of petroleum ether (60-90°C) and ethyl acetate with a volume ratio...

Embodiment 2

[0058] Example 2 Structure identification and analysis of the compound of formula II

[0059] 1) Light yellow oil.

[0060] 2) UV (λ MeOH max ) spectrum, 269nm, indicating the existence of a conjugated system.

[0061] 3) IR(νmax KBr )cm -1 : 3443.84, 2929.24, 2871.71, 1735.32, 1677.59, 1622.83, 1453.35, 1376.10;

[0062] The above data show that there are functional groups such as methyl, methylene, carbonyl, and olefinic bonds in this structure.

[0063] 4) EI-MS (me / z): 291.29, 279.25, 263.31, 234.16, 219.04 (100%), 204.98, 190.95, 178.96, 173.06, 148.92, 144.99, 130.92, 119.11, 107.15, 104.92, 90.9 , 54.94;

[0064] MALDI-TOF MS (me / z): 315.1, 299.1, 273.0, 257.0, 235.0.

[0065] spectrum, 219.04 (100%), but no molecular ion peak is given.

[0066] 5) 1 H-NMR (CDCL 3 , 500MHz) δppm: 9.28(s, 1H), 6.35(d, J=9.5Hz, 1H), 5.35(dd, J=5.5Hz, J=11.5Hz, 2H), 4.18(d, J=12.0Hz, 1H), 4.15 (d, J=12.0Hz, 1H), 2.91 (m, 1H), 2.85 (dd, 1H), 2.26 (m, 1H, C14-H), 2.02 (t, 2H, C12...

Embodiment 3

[0074] Example 3 The effect of the compound of formula II on gastric motility

[0075] The effect of the compound on gastric motility was evaluated by observing the effect of the compound of formula II on gastric emptying in mice loaded with atropine and dopamine.

[0076] (1) The effect of the compound of formula II on gastric emptying of atropine-loaded mice

[0077] SPF grade NIH mice, half male and half male, 18-20g. Mice were randomly divided into 5 groups, namely blank control group, model control group, formula II compound dose group 1 (0.3 mg / kg), formula II compound dose group 2 (0.6 mg / kg), formula II compound dose group 3 ( 1.2 mg / kg). Mice were given intragastric administration (0.2mL / 10g) for 3 days. Before the last administration, mice were fasted for 12 hours, and the test drug was administered by intragastric administration. The blank control group and the model control group were intragastrically administered with an equal volume of water. 20 minutes later,...

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Abstract

The invention belongs to the technical field of medical compounds, and particularly relates to an application of a terpene lactone compound for improving gastric motility disorder. The invention provides the application of the terpene lactone compound as shown in a formula I in preparation of a medicine, wherein the medicine is used for preventing and/or treating the gastric motility disorder or diseases or symptoms related to gastric motility disorder. The compound shown in the formula I can prevent and/or treat gastric motility disorder or diseases or symptoms related to gastric motility disorder, and provides more choices for development of drugs for treating and/or preventing gastric motility disorder.

Description

[0001] This application claims the priority of the previous application filed with the State Intellectual Property Office of China on September 10, 2018 with the patent application number 201811052387.X and the invention title "Use of Terpene Lactone Compounds for Improving Gastric Motility Disorder". The entirety of this prior application is incorporated by reference into the present application. technical field [0002] The invention belongs to the technical field of medical compounds, and in particular relates to the use of terpene lactone compounds for improving gastric motility disorders. Background technique [0003] Gastric motility refers to the peristaltic force of gastric muscle contraction, including the strength and frequency of gastric muscle contraction. Gastric dysmotility disease is also "dyspepsia". Gastric dysmotility is the main cause of non-ulcer dyspepsia. Factors causing gastric motility disorders include mental and emotional changes, gastric secretio...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P1/14A61P1/08A61P1/04
CPCA61K31/366A61P1/14A61P1/08A61P1/04A61K36/185
Inventor 刘朝胜刘敏付雯吴瑜罗京余明森王根才周红晖袁建新徐发新
Owner 武汉联合药业有限责任公司
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