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Dendrobium loddigesii rolfe Loddigesiinols G-K as well as preparation method and application thereof

A technology of stilbene compound and Dendrobium huancao, which is applied in the field of medicine, can solve the problem that the medicinal material basis of Dendrobium huancao is not clear, the effective hypoglycemic components of Dendrobium huancao extract are not clarified, and the good application of Dendrobium huancao is not fully exerted. and other problems to achieve the effect of lowering blood sugar and reducing insulin

Inactive Publication Date: 2014-03-26
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Dendrobium ring grass is also called Dendrobium xiaohuanchai, Dendrobium meihua, Dendrobium pink, mainly distributed in Guizhou, Guangxi, Yunnan and Guangdong provinces, and has been included in the Chinese Pharmacopoeia since 2000. It is a widely used medicinal material of Dendrobium in traditional Chinese medicine. However, the effective material basis of Dendrobium candidum is not clear. Due to the variety of active ingredients in traditional Chinese medicine, the existing technology research has not clarified the effective components of the extract of Dendrobium candidum for lowering blood sugar, and failed to give full play to the good application of Dendrobium candidum.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of Dimeric Stilbene Compounds Loddigesiinols G~K (New Compounds 1~5) from Dendrobium cyclamen

[0034] 4 kg of Dendrobium candidum (stem) was cold soaked twice in methanol (35 L of methanol for each cold soak, 72 hours for each cold soak), and the extract was concentrated under reduced pressure at 55°C to obtain 110 g of extract.

[0035] Suspend 110 g of the extract in 3 L of water, extract twice with 3 L of petroleum ether, ethyl acetate and n-butanol in sequence, concentrate the extract under reduced pressure, select the ethyl acetate extract and concentrate under reduced pressure at 55°C to obtain the extract Cream 35g.

[0036] Ethyl acetate extracted extract was subjected to Sephadex LH-20 gel column chromatography, eluted with methanol, and the red fraction was collected. The concentrated red fractions were combined. The concentrated red fraction was separated by high performance liquid chromatography. The chromatographic column was an Ul...

Embodiment 2

[0037] Example 2 Determination of the physical and chemical parameters and molecular structure of the new compounds 1-5

[0038] The properties, molecular weight and other physical and chemical parameters of compounds (1)~(5) are shown in Table 1. Compounds (1)~(2) 1 HNMR and 13 The CNMR data are shown in Table 2, compounds (3)~(4) 1 H NMR and 13 C NMR data are shown in Table 3, compound (5) 1 H NMR and 13 See Table 4 for C NMR data.

[0039] Table 1 Properties, molecular mass, IR, UV data of compounds

[0040] .

[0041] Table 2 loddigesiinols G (1) (500 MHz, C 2 D. 6 CO), loddigesiinols H (2). (600 MHz, C 2 D. 6 CO) NMR data

[0042] .

[0043] Table 3 NMR data of loddigesiinols I (3), loddigesiinols J (4) (600 MHz, C 2 D. 6 CO)

[0044] .

[0045] Table 4 loddigesiinols K (5) (400 MHz, C 2 D. 6 CO) NMR data

[0046] .

[0047] Through the above NMR, infrared and ultraviolet test results, it can be determined that the structural formulas of the fi...

Embodiment 3

[0049] Example 3 Determination of α-glucosidase inhibitory activity of Dendrobium officinalis dimer stilbene compound Loddigesiinols G~K

[0050] The determination of α-glucosidase inhibitory activity refers to the method of Lin Ma et al. (Zhi-yun Du , Lin Ma et al. ): With p-nitrophenol-alpha-glucoside (PNPG) as substrate, measure the relative activity of the inhibitory enzyme by measuring the change of absorbance A over time at λ=400nm at different concentrations of dimer stilbene compounds. Then use the concentration of dimer stilbene compounds to plot the relative activity of inhibitory enzymes to obtain the half-inhibitory concentration IC of the above five dimer stilbene compounds to α-glucosidase 50 value.

[0051] Instrument used: Shimadzu uv-2501 ultraviolet-visible spectrophotometer.

[0052] Reagents used:

[0053] 1. Buffer solution: KH 2 PO 4 and K 2 HPO 4 For analytically pure reagents, prepared as KH 2 PO 4 -K 2 HPO 4 Buffer solution (50 mM, pH = 7...

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Abstract

The invention relates to dendrobium loddigesii rolfe Loddigesiinols G-K as well as a preparation method and an application thereof in preparation of hypoglycemic drugs. The Loddigesiinols G-K are prepared by the steps as follows: (1), an extracting solution obtained after dendrobium loddigesii rolfe is extracted by methyl alcohol is subjected to pressure-reduction concentration so as to obtain an extract; (2), the extract is sequentially extracted by petroleum ether, ethyl acetate and n-butyl alcohol; and (3), an ethyl acetate extract is repeatedly purified with a Sephadex LH-20 gel column chromatography technology and separated with an HPLC (high performance liquid chromatography) technology, so that five active Loddigesiinols G-K are obtained. Experiments show that dendrobium loddigesii rolfe Loddigesiinols G-K can be used as a hypoglycemic drug, a hyperglycemic health care product and a drug and health care product for preventing and curing cardiovascular disease.

Description

Technical field [0001] The present invention is a drug field, which involves specifically involved the compounds and application methods and applications of Dendrobium Dendrobium. Especially, the Displastic compounds of Dendrobium Dendrobium and its preparation methods and applications in the preparation of blood glucose drugs. Background technique [0002] Diabetes Mellitus is a group of metabolic disease groups that are caused by the interaction of genetic and environmental factors.Lamry, fatigue, etc.Diabetes and hypertension and hyperlipidemia together are called "three highs", which is one of the most common chronic diseases.The insulin in the human body is relatively insufficient or absolutely insufficient, or the sensitivity of the target cells to insulin, or the lack of insulin itself has structural defects, which cause carbohydrates, fat, and protein metabolic disorders, causing some tissue or organs to change the morphological structure and dysfunction of dysfunction an...

Claims

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Application Information

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IPC IPC(8): C07C50/34C07C46/10C07D307/77C07D311/62A61P3/10A61P9/00A61P39/06A23L1/29A23L33/00
CPCC07C50/34C07D307/77C07D311/62
Inventor 王军林永成刘岚
Owner SUN YAT SEN UNIV
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