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Cryptolepis sinensis zinc (II) complex with in-vivo and in-vitro high activity as well as synthesis method and application thereof

The invention relates to a technology for zinc and a synthesis method of vine leaves, which can be applied in the field of medicine and can solve the problems of restricting the curative effect and long-term use.

Active Publication Date: 2022-06-03
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Cisplatin drugs have achieved very obvious results in clinical cancer chemotherapy, but their drug resistance restricts their efficacy and long-term use (Guo, Z.; et al. Chem. Soc. Rev., 2013, 42:202– 224.)

Method used

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  • Cryptolepis sinensis zinc (II) complex with in-vivo and in-vitro high activity as well as synthesis method and application thereof
  • Cryptolepis sinensis zinc (II) complex with in-vivo and in-vitro high activity as well as synthesis method and application thereof
  • Cryptolepis sinensis zinc (II) complex with in-vivo and in-vitro high activity as well as synthesis method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis of Ligand BQTC:

[0039] Weigh 1.00mol of 1,4,7-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecane, 1.20mol of 7-hydroxyheptanoic acid, 2.00mol of 1-ethyl-3( 3-Dimethylpropylamine) carbodiimide (EDCI) and 5.0 mL of pyridine were reacted at 70.0 ° C for 16.0 hours to obtain yellow compound 1 with a yield of 28.8%; Compound 1, 1.20 mol of compound BQ and 5.00 mol of NaH were dissolved in 5.0 mL of dimethylacetamide solution (DMA) and reacted at 100.0 °C for 3.0 hours to obtain yellow compound 2 with a yield of 32.5%; Add 5.00mol HCl / dioxane solution (HCl / dioxane) and 5.0mL CH to 1.00mol compound 2 2 Cl 2 (DCM), reacted at 25.0° C. for 16.0 hours, and passed through the column to obtain the yellow ligand BQTC with a yield of 53.5%.

[0040] Identification of the resulting product:

[0041] (1) Electrospray mass spectrometry of compound 1, its spectrum is as follows figure 1 shown.

[0042] ESI-MS m / z: 601.5[M+H] + , where M is the molecular weight of c...

Embodiment 2

[0077] In a 15.0 mL high temperature pressure-resistant tube, 1.0 mmol of ligand BQTC and 1.0 mmol of zinc (II) chloride solid were weighed, respectively, and 3.0 mL of methanol and 0.5 mL of dichloromethane solution were added, and the coordination reaction was carried out at 45 °C. 72h, the product was washed 3 times with 2.5mL methanol-diethyl ether mixed solution (v:v=1:1), and dried in a vacuum drying oven at 45°C to obtain the yellow target product Zn(BQTC), yield: 50.1% .

Embodiment 3

[0079] In a 15.0 mL high-temperature pressure-resistant tube, weigh 1.0 mmol of ligand BQTC and 1.0 mmol of zinc (II) chloride solid, add 1.0 mL of methanol and 5.5 mL of chloroform solution, and carry out the coordination reaction at 45 °C 12h, the product was washed 3 times with 2.5mL methanol-diethyl ether mixed solution (v:v=1:1) and dried in a vacuum drying oven at 45°C to obtain the yellow target product Zn(BQTC), yield: 70.5 %.

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PUM

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Abstract

The invention discloses a cryptolepis sinensis zinc (II) complex with in-vitro and in-vivo high activity, belongs to the field of medicines, and mainly solves the technical problem of lung cancer cis-platinum drug resistance in the prior art, and the chemical formula of the cryptolepis sinensis zinc (II) complex is [Zn (BQTC)] Cl2. A synthetic method of the compound specifically comprises the following steps: reacting 1, 4, 7-tritert-butyloxycarbonyl-1, 4, 7, 10-tetraazacyclododecane, 7-hydroxyheptanoic acid, 1-ethyl-3 (3-dimethyl propylamine) carbodiimide and pyridine to obtain a compound 1; reacting the compound 1, cryptolepine derivative BQ and NaH to generate a yellow compound 2; adding an HCl / dioxane solution and CH2Cl2 into the compound 2, and reacting to generate a yellow ligand BQTC; and carrying out coordination reaction on the ligand BQTC and zinc chloride to obtain the cryptolepis sinensis zinc (II) complex. The cryptolepine zinc complex inhibits growth of a human lung adenocarcinoma-resistant cis-platinum strain A549R in a targeted manner, in-vivo tumor inhibition experiments show that the cryptolepine zinc complex Zn (BQTC) has a good tumor inhibition effect on a nude mouse model bearing the human lung adenocarcinoma-resistant cis-platinum strain A549R, the inhibition rate reaches up to 55.9%, and the cryptolepine zinc complex Zn (BQTC) has potential medicinal value and is expected to be used for preparing various antitumor drugs.

Description

technical field [0001] The present invention relates to the technical field of medicine, more particularly, it relates to a zinc (II) complex with high activity in vivo and in vitro, and a synthesis method thereof. The present invention also relates to the application of the zinc (II) complex of Alpinia chinensis. Background technique [0002] Cisplatin has achieved remarkable results in clinical cancer chemotherapy, but its drug resistance limits its efficacy and long-term use (Guo, Z.; et al. Chem. Soc. Rev., 2013, 42: 202– 224.). Therefore, there is an urgent need to develop a non-platinum antitumor drug that overcomes cisplatin resistance. In addition, zinc has a good coordination geometric environment and flexible coordination number. As a necessary trace element in the human body after iron, it participates in the synthesis of DNA and RNA polymerase, and plays an important role in the maintenance of protein structure and protein structure in the body. Function plays...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/048A61K31/555A61P35/00
CPCC07D491/048A61P35/00Y02A50/30Y02P20/55
Inventor 周振覃其品谭明雄潘凤华曹慧思韦俏嫦李金贤
Owner YULIN NORMAL UNIVERSITY
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