Tyrosinase inhibitor microemulsion as well as preparation method and application thereof

A technology for tyrosinase and inhibitors, applied in the field of tyrosinase inhibitor microemulsion and its preparation and application, can solve the problems of insolubility and solubility of natural tyrosinase inhibitors, achieve clarification and stability of the system, and wide application , cheap effect

Inactive Publication Date: 2014-02-26
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The first technical problem to be solved in the present invention is to provide a kind of microemulsion of tyrosinase inhibitor, especially a kind of microemulsion of natural tyrosinase inhibitor with high activity, non-toxicity and nano particle size, to solve the problem of natural tyrosinase inhibitor. Problems of insolubility and low solubility in water of aminoacidase inhibitors

Method used

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  • Tyrosinase inhibitor microemulsion as well as preparation method and application thereof
  • Tyrosinase inhibitor microemulsion as well as preparation method and application thereof
  • Tyrosinase inhibitor microemulsion as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] The preparation method one of embodiment 1 Norartocarpetin microemulsion

[0027] Norartocarpetin is extracted from jackfruit. 2kg jackfruit wood (wood collected from Wenchang County, Hainan Province) was extracted twice by ultrasonic wave with 6 times the amount of 95% ethanol, 1 hour each time, concentrated to dryness under reduced pressure, and weighed. Then dissolved in 95% ethanol, filtered with qualitative filter paper, added to Amberlite XAD16, air-dried or evaporated to dryness under reduced pressure, and applied to Amberlite XAD16 chromatography column with 20%, 30%, 40%, 50% and 95% ethanol respectively Elute for 6 column volumes, collect the 40% ethanol elution fraction, concentrate to obtain a dry sample, dissolve in methanol and separate it by glucose gel column chromatography, and elute with methanol-water (v / v, 1:1), that is, The compound norartocarpetin was obtained.

[0028] The NMR spectral data of Norartocarpetin are as follows:

[0029] 1 H NMR (D...

Embodiment 2

[0036] Embodiment 2 The preparation method two of Norartocarpetin microemulsion

[0037] With reference to the above-mentioned preparation method, with Tween 60 as surfactant, with PEG400 as co-surfactant, with peppermint oil as oil phase, the ratio of the three in the mixed solution is 43%: 43%: 14%, the obtained microemulsion The concentration of norartocarpetin in the system is 1.21 mg / mL, the water content is 80%, the system is clear, transparent and stable, and the solubility of norartocarpetin is increased by 53 times.

Embodiment 3

[0038] Example 3 Evaluation of tyrosinase inhibitory activity of microemulsion

[0039] Dilute the prepared microemulsion with deionized water to 20, 10, 5, 2.5, and 1.25 μg / mL, and take 1 mL of each sample microemulsion of five concentrations. The positive control kojic acid was prepared into 500, 250, 125, 62.5, and 31.25 μg / mL solutions with DMSO, respectively. Take 300 μL of each of the five concentrations of kojic acid solution, and use 700 μL of pH6.8 phosphate buffer solution to prepare 1 mL. To the positive control and sample microemulsion, 1 mL of 0.1 mg / mL tyrosine solution and 1 mL of 200 U / mL tyrosinase solution prepared from phosphate buffer solution with pH 6.8 were added, and incubated at 37 °C for 20 min. Absorbance was measured at 492 nm.

[0040] Enzyme activity inhibition rate = [(A 2 -A 1 )-(B 2 -B 1 )] / (A 2 -A 1 )×100%

[0041] A 1 is the absorption value without inhibitor at 0min; A 2 is the absorption value without inhibitor added after 20min; ...

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Abstract

The invention discloses tyrosinase inhibitor microemulsion as well as a preparation method and an application thereof, and belongs to the technical fields of foods, medicines and cosmetics. The microemulsion contains a matrix, a tyrosinase inhibitor norartocarpetin and water, wherein the matrix comprises 40%-60% of surface active agent, 20%-45% of cosurfactant and 5%-20% of oil phase; and the microemulsion is prepared by adding raw components according to a certain ratio. The tyrosinase inhibitor microemulsion can be used for overcoming the defects that the solubility of the natural tyrosinase inhibitor norartocarpetin in water is extremely low. The method provided by the invention is simple to operate and can be used for the spontaneous formation of the microemulsion. Nanoscale microemulsion can be formed by using water or an aqueous solution for diluting the tyrosinase inhibitor microemulsion. The obtained microemulsion can be used for effectively resisting enzymatic browning of fruits and vegetables, and preparing whitening cosmetics and other medicines for preventing and treating human hyperpigmentation diseases and melanomas (caused by excessive melanin) needing to inhibit the activity of tyrosinase.

Description

technical field [0001] The invention relates to a tyrosinase inhibitor microemulsion, a preparation method and application thereof, and belongs to the technical fields of food, medicine and cosmetics. Background technique [0002] Tyrosinase (EC1.14.18.1), a kind of polyphenol oxidase, is widely present in organisms. Through catalysis, the monophenol is first hydroxylated to ortho-diphenol, and then the ortho-diphenol is further oxidized to ortho-diquinone, and then undergoes a series of complex non-enzymatic reactions to finally generate melanin. In this process, tyrosinase plays a key role. The melanin produced in the human body can protect the human skin from the sun's ultraviolet rays. At the same time, the content and type of different melanin in the skin determines the skin color and hair color of human beings, but excessive melanin secretion can cause serious cosmetic problems, such as pigmentation, Dark spots, age spots, etc. During food processing, tyrosinase cat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/49A61K8/06A61K31/352A61K9/107A61Q19/02A61P17/00A23B7/154
Inventor 郑宗平陈洁兰山
Owner JIANGNAN UNIV
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