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Preparation method and application of 2-isobutylmalate glucosyloxybenzyl ester extract from Baijizhong

A technology of oxybenzyl esters and malate, which is applied in the field of cosmetics, extracts and preparations of 2-isobutylglucosyloxybenzyl malate in white and middle-aged plants, and tyrosinase inhibitors in In the field of pharmaceuticals, it can solve problems such as poor effect, cytotoxicity, and poor stability, and achieve the effect of improving the therapeutic effect

Active Publication Date: 2021-02-09
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 application of 2-isobutylmalate glucosyloxybenzyl ester extract from Baijizhong
  • Preparation method and application of 2-isobutylmalate glucosyloxybenzyl ester extract from Baijizhong
  • Preparation method and application of 2-isobutylmalate glucosyloxybenzyl ester extract from Baijizhong

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, after crushing, add 10L of water and heat and reflux to extract twice, each time for 2 hours, the combined extracts are filtered through gauze, centrifuged at 1000rpm for 5 minutes, the supernatant is 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 invention discloses a preparation method and application of a 2-isobutylmalate glucosyloxybenzyl ester extract from Baiji Zhong, belonging to the fields of medicine and daily chemical industry. The extract of Radix Rhizoma Radix is ​​preferably tuber and / or fibrous root. The white and 2-isobutylmalate glucosyloxybenzyl ester extracts can be used as tyrosinase inhibitors to prepare cosmetics, pharmaceuticals or skin external preparations for melanin production inhibitors or whitening agents. It has good preventive, improvement and therapeutic effects on post-tanned skin and hyperpigmentation such as spots, age spots, and freckles.

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 Patents(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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