Preparation method and use of 2-isobutyl malate glucooxybenzyl ester extract in rhizoma bletillae

A technology of oxybenzyl esters and malate esters, applied in the fields of pharmaceuticals and daily chemicals, can solve problems such as poor effect, inability to meet consumer market demand, cytotoxicity, etc., and achieve the effect of improving the therapeutic effect

Active Publication Date: 2020-02-11
厦门市食品药品质量检验研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, a variety of tyrosinase inhibitors are used to improve or treat skin pigmentation, and have been commercialized, such as L-ascorbic acid, kojic acid, hydroquinone, but due to poor stability, poor effect or cytotoxicity, etc. problems, unable to meet the growing consumer market demand

Method used

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  • Preparation method and use of 2-isobutyl malate glucooxybenzyl ester extract in rhizoma bletillae
  • Preparation method and use of 2-isobutyl malate glucooxybenzyl ester extract in rhizoma bletillae
  • Preparation method and use of 2-isobutyl malate glucooxybenzyl ester extract in rhizoma bletillae

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Baihe 2-isobutylmalate glucosyloxybenzyl ester extract

[0025] 1 kg of white and fibrous roots, crushed, added 10L of water, heated and refluxed twice, each time for 2 hours, the combined extracts were filtered through gauze, centrifuged at 1000rpm for 5 minutes, the supernatant was concentrated, freeze-dried into a dry soak Cream Jidebai and Extract BJ (110g). Take 100g of the extract of Baiji, dissolve it in an appropriate amount of water, filter it, and take the filtrate and go through macroporous resin D101 open column chromatography, ethanol-water gradient elution. Respectively recover under reduced pressure to obtain water elution fraction (51.5g), 50% (v / v) ethanol-water elution fraction (28.0g), and 95% (v / v) ethanol-water elution fraction (12.5g ). Among them, the 50% (v / v) ethanol-water eluted part is the extract of Baihe 2-isobutylmalate glucosyloxybenzyl ester.

Embodiment 2

[0026] Example 2: Establishment of liquid mass TIC characteristic spectrum and identification of main chromatographic peaks of extracts of Baihe 2-isobutylmalate glucosyloxybenzyl ester

[0027] Take an appropriate amount of the white and 2-isobutylmalate glucosyloxybenzyl ester extracts obtained in Example 1, accurately weighed, add methanol to dissolve and make a 10.0 mg / mL solution, and pass through a 0.45 μm filter membrane, that is, Obtain the test solution.

[0028]Precisely take 1 μl of the above-mentioned test product, inject it into a high-performance liquid chromatography-mass spectrometer for analysis, and record the TIC diagram ( figure 1 ). The liquid chromatography conditions are: 0.1% formic acid aqueous solution (A) - acetonitrile (B) gradient elution: 5% B→15% B (0~10min), 15% B→20% B (10~20min), 20% B(20~23min), 20%B→25%B(23~28min), 25%B(28~31min), 25%B→31%B(31~40min), 31%B→36%B( 40~45min), 36%B→45%B (45~50min), 45%B→100%B (50~60min). Mass Spectrometry Co...

Embodiment 3

[0032] Example 3: Investigation on the reproducibility of the TIC characteristic spectrum of the extracts of Baihe 2-isobutylmalate glucosyloxybenzyl ester

[0033] Get 4 batches of Baiji from different origins (Yunnan, Guizhou, Hubei, Yunnan), and process them sequentially according to the preparation method in Example 1 to obtain 4 batches of Baiji and 2-isobutylmalate glucosyloxybenzyl ester extracts (BJB1801, BJB1802, BJB1803, BJB1804), according to the processing method and the condition in embodiment 2, analyze respectively, obtain 4 batches of white and the TIC feature collection of 2-isobutylglucosylmalate oxybenzyl ester extracts, The relative retention time of each chromatographic peak calculated by taking the chromatographic retention time of militarine as 1 and the corresponding chemical substances of each chromatographic peak are as follows:

[0034] Peak 1: 0.52±0.02 (dactylorhin E)

[0035] Peak 2: 0.56±0.02 (bleformin J)

[0036] Peak No. 3: 0.67±0.02 (gymnos...

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Abstract

The present invention discloses a preparation method and a use of a 2-isobutyl malate glucooxybenzyl ester extract in rhizoma bletillae and belongs to the fields of medicine and daily chemical industry. The rhizoma bletillae extract is preferably tuber and/or fibrous root. The rhizoma bletillae 2-isobutyl malate glucooxybenzyl ester extract can be used as a tyrosinase inhibitor in preparation of cosmetics, pharmaceuticals or skin external preparations of melanin production inhibitors or skin-whitening agents, and has good prevention, improvement and treatment effects on skin pigmentation of skin tanning, stain, age spots, freckles, etc. after ultraviolet radiation.

Description

technical field [0001] The invention belongs to the field of pharmaceuticals and daily chemical industry, and particularly relates to an extract of 2-isobutylmalate glucosyloxybenzyl malate and its preparation method as well as its use as a tyrosinase inhibitor in the fields of medicines and cosmetics Applications. Background technique [0002] Bletilla striata (Thunb) Rchb.f. is the dry tuber of orchid plant Bletilla striata (Thunb) Rchb.f., also known as Gangen, Baigen, Lianjicao, Bletilla striata, etc. Li Shizhen explained its name: Its roots are white, and they grow together, so it is called Baiji. It was first used as a medicine in "Shen Nong's Materia Medica". Bacteria plants are widely distributed in my country. The Yangtze River Basin is the ecological region with the most abundant species of Bletilla species and the most suitable climate conditions. It is mainly produced in Guizhou, Sichuan, Yunnan, Hunan, Hubei, Anhui and other provinces. It tastes bitter, sweet,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/08A61K31/7034A61K8/60A61K8/9794A61Q19/00A61Q19/02A61P17/16A61P17/00A61K36/898
CPCA61K8/602A61K31/7034A61K36/898A61K2800/782A61Q19/004A61Q19/02A61K8/9794A61P17/00A61P17/16C07H1/08C07H15/203
Inventor 段营辉陈惠玲黄澜朱樵苏黄惠琼李玲玲
Owner 厦门市食品药品质量检验研究院
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