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Kaurane-type diterpenoid compound as well as preparation method and medical application thereof

A kind of technology of kaurine type and compound, which is applied in the field of medicine

Inactive Publication Date: 2010-07-28
BEIHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The present invention is the first time to obtain a kaurane-type dither compound from the Asteraceae plant, which has the function of inhibiting protein tyrosine phosphatase 1B. Significant activity, after literature search, there is no report on this type of compound

Method used

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  • Kaurane-type diterpenoid compound as well as preparation method and medical application thereof
  • Kaurane-type diterpenoid compound as well as preparation method and medical application thereof
  • Kaurane-type diterpenoid compound as well as preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Preparation of Kaurane-Type Ditiertyl Compounds

[0064] Soak 2.0Kg of dried and pulverized whole herb of Siberia chinensis in 10L of methanol (or ethanol) at room temperature for 3 days to extract once, and extract three times in total. The combined methanol or ethanol extracts were concentrated under reduced pressure to obtain extract (148 g). The extract was dissolved in 0.6L of water to form a suspension and extracted with 3.0-2.0L of n-hexane, and the n-hexane extract was concentrated under reduced pressure to obtain n-hexane extract (49g).

Embodiment 2

[0066] Compound 1 was isolated:

[0067] The n-hexane extract prepared in Example 1 was subjected to 200-300 mesh silica gel column chromatography, and gradient elution was carried out with n-hexane:ethyl acetate (V / V, 100:0-1:1) as the mobile phase, and the collected The components of the separated components were detected by silica gel thin layer chromatography, and the separated components with the same composition were combined and concentrated to obtain 7 separated components from A to G. Fraction C (363.4 mg, 12-16% ethyl acetate) was subjected to reverse-phase high performance liquid chromatography using C 18 Column (10μm, 250×10mm), with acetonitrile: H 2 O=80:20-100:0 (V / V) was used as the gradient elution of the mobile phase, the flow rate was 2 mL / min, the column temperature was 25° C., and the detection was performed at a wavelength of 210 nm for 60 min. The eluate was collected for 30-33 min, and the collected solution was concentrated to obtain compound 1 (24.5...

Embodiment 3

[0069] Compound 2 was isolated:

[0070] The n-hexane extract prepared in Example 1 was subjected to 200-300 mesh silica gel column chromatography, and gradient elution was carried out with n-hexane:ethyl acetate (V / V, 100:0-1:1) as the mobile phase, and the collected The isolated fractions were detected by silica gel thin-layer chromatography. The isolated fractions with the same composition were combined and concentrated to obtain 7 isolated fractions from A to G. Part F (268.9 mg, 25-30% ethyl acetate) was subjected to reversed-phase high-performance liquid chromatography, using C 18 Column (10μm, 250×10mm), with acetonitrile: H 2 O=70:25-92:8 (V / V) was used as gradient elution of the mobile phase, the flow rate was 2mL / min, the column temperature was 25°C, and the detection was carried out at a wavelength of 210nm for 70min. The eluate was collected for 10.3-13.9 min, and the collected solution was concentrated to obtain compound 2 (35.8 mg). That 1 H and 13 C-NMR spe...

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Abstract

The invention relates to a kaurane-type diterpenoid compound which is a new compound and has the inhibitory activity of protein tyrosine phosphatase 1B (PTP1B). The invention also provides a preparation method and the medical application of the kaurane-type diterpenoid compound simultaneously. The kaurane-type diterpenoid compound which is prepared from feverfew herba siegesbeckiae by adopting extracting and separating processes has remarkable PTP1B inhibitory activity, can be applied to preparing medicines for treating diabetes, obesity and complications thereof and has important significant on the development and the utilization of Chinese medicinal plant resources.

Description

technical field [0001] The invention discloses a kaurane-type ditherne compound, and also provides its preparation method and medical application, and relates to the technical field of medicine. technical background [0002] At present, diabetes is usually divided into two types: insulin-dependent (IDDM, type I diabetes) and non-insulin-dependent (NIDDM, type II diabetes), wherein type II diabetes accounts for 90% of diabetes. WHO predicts that the number of people with diabetes will rise from 135 million in 1995 to 300 million by 2025 due to aging population, obesity, unhealthy diet and inactive lifestyle. [0003] Type II diabetes is characterized by resistance to the action of insulin in insulin-sensitive tissues such as skeletal muscle, liver, and adipose tissue. Although its specific mechanism is unclear, the weakening or even blocking of insulin signaling in its transduction pathway must be directly related. PTPases play a role in multiple links in the insulin signal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/24C07C62/06C07C69/28C07C67/56C07C51/47A61K31/22A61K31/19A61P3/10A61P3/04A61P5/50
Inventor 崔龙吴学安宗石李东浩
Owner BEIHUA UNIV
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