Preparation method of spermacoce latifolia triterpenoids and application of spermacoce latifolia triterpenoid in preparation of glycosidase inhibitor medicine

A technology of glycosidase inhibitors and triterpenes, which is applied in the preparation of triterpenoids and its application in the preparation of glycosidase inhibitors, and achieves the effects of high safety, easy storage and abundant sources

Inactive Publication Date: 2015-04-08
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Six kinds of triterpenoid mesembryanthemoidigenic acid (1), 29-hydroxyhederagenin (2), 3β,6β-dihydroxy-olean-12-ene-28-oic acid (3), scutellaric acid (4), arjunic acid (5), 3β, 6β, 23-trihydroxy-olean-12-en-28-oic acid (6) were isolated from other plants (see literature: Magina et al., Quim Nova, 2012, 35:1184-1188; Huu et al., J Chem, 2007, 45:363-367; Kuo et al., Chem Pharm Bull, 1988, 36:3619-3622; Ponou et al., Chem Biodivers, 2011, 8:1301-1309; Lavaud et al. al., Phytochemistry, 2001,57:469-478; Khan et al., J Nat Prod, 1993,56:2163-2165), their chemical structural formula is shown in the following formula (I), and these compounds have not been seen so far It has been reported to have glycosidase inhibitor activity, and there is no report on its isolation from Spermacoce latifolia plants

Method used

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  • Preparation method of spermacoce latifolia triterpenoids and application of spermacoce latifolia triterpenoid in preparation of glycosidase inhibitor medicine
  • Preparation method of spermacoce latifolia triterpenoids and application of spermacoce latifolia triterpenoid in preparation of glycosidase inhibitor medicine
  • Preparation method of spermacoce latifolia triterpenoids and application of spermacoce latifolia triterpenoid in preparation of glycosidase inhibitor medicine

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Embodiment 1

[0024] Embodiment 1: Preparation of six kinds of triterpenoids in broad-leaved abundant flowers and plants

[0025] 1.1 Plant source and identification

[0026] The whole plant of Spermacoce latifolia Aubl.K.Schum. was collected from South China Botanical Garden, Guangzhou City, Guangdong Province in September 2012, and was identified by Xing Fuwu, a researcher of South China Botanical Garden, Chinese Academy of Sciences.

[0027] 1.2 Extraction and separation

[0028] The whole plant (5.0Kg) of the dried Herba chinensis (5.0Kg) was crushed and extracted at room temperature with 95% ethanol aqueous solution, the extracts were combined and concentrated under reduced pressure to obtain an alcohol-free extract. The extract was suspended in water, and extracted four times with petroleum ether and ethyl acetate in turn; after concentration under reduced pressure, petroleum ether extract (330 g) and ethyl acetate extract (202 g) were obtained. The obtained petroleum ether extract ...

Embodiment 2

[0036] Embodiment 2: α-glucosidase inhibitory activity detection of described six kinds of triterpenoids

[0037] 2.1 Instruments and reagents

[0038] Experimental instrument: Genois microplate reader (Tecan GENios, Switzerland).

[0039]Reagent samples: α-glucosidase was purchased from Sigma Chemical Co. (Sigma-Aldrich, St.Louis, USA); Acarbose was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); Phenol-α-D-glucopyranoside (PNPG) was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); six triterpenoid mesembryanth emoidigenic acid (compound 1), 29-hydroxyhederagenin (compound 2), 3β ,6β-dihydroxy-olean-12-en e-28-oic acid (compound 3), scutellaric acid (compound 4), arjunic acid (compound 5), 3β,6β,23-tr ihydroxy-olean-12-en- 28-oic acid (compound 6) is prepared by the method of Experimental Example 1 above, and can also be prepared according to the literature Magina et al., Quim Nova, 2012, 35:1184-1188; Huu et al., J Chem, 2007, 45: 363-367; Ku o et al., ...

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Abstract

The invention provides a preparation method of spermacoce latifolia triterpenoids and an application of the spermacoce latifolia triterpenoids in preparation of a glycosidase inhibitor medicine. Six compounds for intensively inhibiting the activity of alpha-glycosidase provided by the invention are natural compounds which are high in safety, and can be naturally degraded rapidly without a residue in the environment. The compounds can be separated from plant materials such as spermacoce latifolia; the plant materials are abundant in source; and the preparation process is easy to operate. Monomers of the six compounds are relatively stable and easy to store; the alpha-glycosidase inhibiting activity is obviously higher than that of clinical medicine acarbose; and the compounds are extremely likely to be further developed into the effective and safe alpha-glycosidase inhibitor medicines for preventing and treating type 2 diabetes mellitus, and have relatively good prospects.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and in particular relates to six triterpenoids, namely mesembryanthemoidigenic acid (1), 29-hydroxyhederagenin (2), 3β, 6β-dihydroxy-olean-12-ene-28-oic acid (3), scutellaric acid (4), arjunic acid (5), 3β, 6β, 23-trihydroxy-olean-12-en-28-oic acid (6) or pharmaceutically acceptable salts thereof in the preparation of glycosidase inhibitors or drugs applications, and their preparation methods. Background of the invention [0002] Diabetes is a clinically common endocrine and metabolic disorder disease, which has an important correlation with the annual increase in cardiovascular diseases and cancers, and is an important killer of human health. At present, the incidence of diabetes is increasing worldwide. In my country, the prevalence of diabetes is more than 100 million, and it shows a trend of increasing year by year. Diabetes is causing more and more serious losses to our people's ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P3/10C07J63/00C07J75/00
CPCA61K31/56C07J63/008
Inventor 谭建文罗应周忠玉任慧徐巧林
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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