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Uncaria amide A as well as pharmaceutical composition and application thereof

A technology of rhynchiferamide and composition, which is applied in the direction of drug combination, sugar derivatives, sugar derivatives, etc., and can solve the problems of no rhynchamide A pharmaceutical composition, no rhynchiferamide A, etc.

Active Publication Date: 2018-03-23
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report of rhynchamide A (1) in the prior art, and there is no report of a pharmaceutical composition with rhynchamide A (1) as an active ingredient, and there is no report of rhynchamide A (1) and a pharmaceutical composition thereof as an active ingredient. Melatonin receptor agonists, and application reports for treating or improving central nervous system diseases related to melatonin receptors

Method used

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  • Uncaria amide A as well as pharmaceutical composition and application thereof
  • Uncaria amide A as well as pharmaceutical composition and application thereof
  • Uncaria amide A as well as pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of compound 1:

[0024] Take the dried hooked stems and branches of Uncaria uncaria, crush them, extract twice with 70% ethanol under reflux, each time for 3 hours, combine the ethanol extracts, recover the ethanol under reduced pressure to obtain the extract. The extract was dissolved in 5 times the amount of water, and the D101 macroporous resin column chromatography was used for ethanol-water gradient elution. Combine the fractions eluted with 50% ethanol, concentrate, dissolve in methanol, adsorb on silica gel, place at room temperature to evaporate the solvent, grind and sieve, and perform silica gel column chromatography, elute with chloroform-methanol-water (7:3:0.3), Four fractions A-D were obtained. Fraction C was further prepared by medium-pressure MCI CHP-20P gel column, methanol-water gradient elution (1:9~9:1), and 5 fractions were obtained, C-1~C-5. Fraction C-2 was purified by HPLC using Rp-C 18 Column, acetonitrile-water gradient elution (...

Embodiment 2

[0042] Compound 1 on melatonin receptor MT 1 and MT 2 Agonistic activity of the receptor.

[0043] 1 Materials and methods

[0044] 1.1 Materials:

[0045] melatonin receptor MT 1 and MT 2 The cell lines used for agonistic activity screening correspond to human kidney epithelial cells HEK293-MT 1 and HEK293-MT 2 ; Cell culture medium (Dulbecco's Modified Eagle Medium, DMEM) containing 10% fetal bovine serum; No-wash calcium flow kit.

[0046] 1.2 Instrument: CO 2 Constant temperature incubator Thermo Forma 3310 (USA); Inverted biological microscope XD-101 (Nanjing); Flexstation 3Benchtop Multi-Mode Microplate Reader (Molecular Devices, Sunnyvale, California, USA).

[0047] 1.3 Experimental process

[0048] Coat the 96-well black-walled transparent-bottom cell culture plate with the substrate BD Matrigel, put it in a constant temperature incubator at 37°C for 1 hour, absorb the supernatant, and dilute it with 4×10 4 Density per well, the corresponding HEK293 cells wer...

preparation Embodiment

[0055] 1. Compound 1 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, water for injection was added as usual, finely filtered, potted and sterilized to make an injection.

[0056] 2. Compound 1 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, it was dissolved in sterile water for injection, stirred to dissolve, filtered with a sterile suction filter funnel, then sterile fine filtered, and packed In the ampoule, freeze-dried at low temperature and sealed aseptically to obtain powder injection.

[0057] 3. According to the method of Example 1, the compound 1 was first prepared, and the excipient was added according to the ratio of its weight to the excipient at a ratio of 9:1 to make a powder.

[0058] 4. According to the method of Example 1, Compound 1 was firstly prepared, and the weight ratio of compound 1 to the excipient was 5:1, and the excipient was added, granulated and compre...

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Abstract

The invention provides novel indole alkaloid triglycoside shown in a structural formula (I), uncaria amide A (1), pharmaceutical composition comprising an effective quantity of compounds 1 for treatment and pharmaceutical carriers or excipients, a preparation method of the compounds 1 and the pharmaceutical composition containing the same as well as applications of the uncaria amide A as an MT (melatonin) receptor stimulant and in preparation of a drug for treating or relieving MT receptor related central nervous system diseases.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to a new indole alkaloid triglycoside, rhynchophylamide A (1), a pharmaceutical composition with compound 1 as an active ingredient, its application as a melatonin receptor agonist, and its use in the preparation of Application in drugs for treating or improving central nervous system diseases related to melatonin receptors. Background technique: [0002] Melatonin (MT) is an endogenous hormone secreted by the pineal gland of mammals. Its secretion has obvious circadian and seasonal rhythms, and plays an important role in regulating the circadian rhythm, reproduction, and aging of organisms. Melatonin plays a role in the body by activating specific melatonin receptors. It has physiological activities such as improving sleep, anti-aging, and improving immunity. In addition, it also has regulatory effects on depression, anxiety, and pain. Human melatonin receptors incl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/00C07H1/08A61K31/706A61P25/28
CPCC07H1/08C07H17/00
Inventor 耿长安陈纪军张建钢黄晓燕马云保李天泽杨通华张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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