Tetrandrine gallate and drug composition, preparation method and applications thereof

A technology of tetrandrine and stearate, which is applied in the directions of drug combination, carboxylate preparation, pharmaceutical formulation, etc., can solve the problems of complicated process and insufficient compound activity, and achieves the effect of broad application prospect.

Active Publication Date: 2013-01-30
NAT INST OF PHARMA R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There have been structural modifications for tetrandrine, such as various structural modifications of tetrandrine into quaternary ammonium salts or core substituents (CN1111160C; Supramolecular Chemistry (2008), 20(4), 427-435. ), its disadvantage is that the activity of the modified compound is not good enough or the process is complex, etc.

Method used

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  • Tetrandrine gallate and drug composition, preparation method and applications thereof
  • Tetrandrine gallate and drug composition, preparation method and applications thereof
  • Tetrandrine gallate and drug composition, preparation method and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1-5

[0051] The preparation of embodiment 1-5 tetrandrine gallate

[0052] The raw material formula and reaction parameters for synthesizing tetrandrine gallate (Formula I) are shown in Table 1:

Embodiment 1

[0055] Example 1. Synthesis of Tetrandrine Gallate (Formula I)

[0056] With reference to the aforementioned synthetic route represented by the structural formula and the raw material formula and reaction conditions shown in Table 1, the synthetic method of tetrandrine gallate (formula I) of the present invention is as follows: room temperature, dark, tetrandrine (10g , 0.016mol) into 600mL of absolute ethanol, stirred, white turbidity, added dropwise gallic acid (6.01g, 0.035mol) dissolved in 50mL of absolute ethanol, after the addition was completed, the temperature was controlled at about 30°C, stirred for 24 hours, concentrated under reduced pressure Evaporate about 500 mL of ethanol, stir at room temperature for 2 h, filter with suction, wash with ethanol, and dry to obtain a milky white solid; concentrate the filtrate, filter with suction, wash with ethanol, dry, and combine the filter cakes to obtain a total of 14.88 g of a milky white solid, with a yield of 95%. The te...

Embodiment 2

[0059] Example 2, Synthesis of Tetrandrine Gallate (Formula I)

[0060] With reference to the aforementioned synthetic route represented by the structural formula and the raw material formula and reaction conditions shown in Table 1, the synthesis method of Tetrandrine gallate (Formula I) in Example 2 was the same as in Example 1, and 28.19 g of a milky white solid was obtained. Yield 90%. Test result m.p.176-177℃, 1 H-NMR (d 6 -DMSO, 300MHz) was the same as in Example 1, and was confirmed to be tetrandrine gallate (Formula I).

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Abstract

The invention discloses tetrandrine gallate and a drug composition, a preparation method and applications thereof. The structure of tetrandrine is modified, and a novel derivative of the tetrandrine is prepared, namely, the tetrandrine gallate. Physical and chemical constant tests show that the solubility of the tetrandrine gallate is increased by 43 times than the tetrandrine. A pharmacology experiment shows that the tetrandrine gallate has an obvious inhibiting effect on the proliferation of tumor strain cells, and the effect is superior than that of the tetrandrine; and the tetrandrine gallate shows obvious blood pressure lowering, anti-inflammatory and pain easing effects which are higher than those of the tetrandrine, and the toxicity is smaller than that of the tetrandrine. Accordingly, the tetrandrine gallate is active ingredients and can be used for preparing anti-tumor, blood pressure lowering, anti-inflammatory and pain easing drugs, and the application range is wide.

Description

technical field [0001] The present invention belongs to the new compound in the field of medicine and its preparation method and application, and specifically relates to a new tetrandrine derivative, i.e. tetrandrine gallate, and also discloses its preparation method and its use in preparing Tumor, blood pressure lowering, anti-inflammatory, analgesic and other drugs. Background technique [0002] Most of the ingredients from natural sources are widely distributed, have diverse structures, and have significant activities. Structural modification, transformation, and total synthesis of them have always been a main idea in the development of new drugs and one of the hotspots in natural medicinal chemistry research. [0003] Tetrandrine (Tet), also known as Tetrandrine, is a bisbenzylisoquinoline compound (see formula II), which is derived from the natural product Tetrandrine (Stephania tetrandra S. Moore). root. Modern pharmacological studies have confirmed that tetrandrine ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/18C07C65/03C07C51/41A61K31/4748A61P35/00A61P9/12A61P29/00
Inventor 孙从新冀蕾郑礼
Owner NAT INST OF PHARMA R & D CO LTD
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