Application of a kind of nano-carrier mil-100(fe) on the loading of acanthine chloride

A technology of chlorinated syringamine and nano-carrier, applied in the field of nano-carrier research, can solve the problem of not finding liver toxicity, and achieve the effects of saving experimental raw materials and costs, reducing toxicity, and being easy to operate.

Active Publication Date: 2022-04-08
GUANGXI UNIV FOR NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the use of MOF as NC carrier, and no carrier has been found that can reduce the hepatotoxicity of NC and improve the anticancer activity in vitro, and at the same time, the drug loading and release characteristics can achieve good results.

Method used

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  • Application of a kind of nano-carrier mil-100(fe) on the loading of acanthine chloride
  • Application of a kind of nano-carrier mil-100(fe) on the loading of acanthine chloride
  • Application of a kind of nano-carrier mil-100(fe) on the loading of acanthine chloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A kind of preparation method of nanocarrier MIL-100 (Fe), is to ferric nitrate, H 3 BTC, H 2 O, HNO 3 According to the molar ratio of 1:0.66:208:2, mix and place in an autoclave, heat and react at 100°C for 12 hours, filter and separate after the reaction, wash the filtered powder, and dry it in a vacuum at 100°C overnight. The nanocarrier MIL-100(Fe) is obtained; the washing method is: disperse the powder in hot water at 60°C for 3 hours according to the solid-to-liquid ratio of 1g:500mL, and then disperse the powder at 60°C according to the solid-to-liquid ratio of 1g:100mL ℃ dispersed in ethanol for 3h.

[0037] The obtained nano-carrier MIL-100 (Fe) is subjected to electron microscope scanning detection, and the obtained SEM image is as follows: figure 2 Shown; Use the particle size distribution of further characterizing MIL-100 (Fe) of nano particle size analyzer DLS, the particle size distribution figure that obtains is as image 3 shown.

[0038] figure 2 f...

Embodiment 2

[0040] The nano-carrier MIL-100 (Fe) prepared in Example 1 is applied to load acanthine chloride:

[0041] Specifically, the MIL-100(Fe) was put into methanol and acanthine chloride, stirred at room temperature for 5 days, and then centrifuged at room temperature at 1000rpm for 15 minutes to obtain loaded particles, denoted as NC@MIL-100;

[0042] Wherein, the consumption of described, methyl alcohol, dihedral chloride is as shown in table 1. The load rate after testing is shown in Table 1.

[0043]

[0044] Table 1

[0045] serial number MIL-100(Fe) / mg Methanol / ml NC / mg Load rate (w%) 1 1 10 1 11.63±1.31 2 1 10 2 23.23±2.35 3 1 10 3 33.43±1.14 4 1 10 4 33.53±2.15 5 1 10 5 33.8±0.98

Embodiment 3

[0047] In order to evaluate the crystal structures of MIL-100(Fe) obtained in Example 1 and NC@MIL-100 obtained in Example 2, XRD analysis was performed on them, and a simulated group of MIL-100(Fe) was added for comparison.

[0048] Figure 4 It is the XRD pattern of MIL-100(Fe), NC@MIL-100. Compared with the spectrum of the simulated group, the MIL-100 (Fe) obtained in Example 1 has a better matching degree with its diffraction peaks, indicating that the synthesis of MIL-100 (Fe) crystals is successful; the NC@MIL-100 obtained in Example 2 The XRD profile exhibited can be similar to that of MIL-100(Fe), implying that its crystalline structure is maintained after drug encapsulation.

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Abstract

The present invention provides a kind of application of nano-carrier MIL-100 (Fe) on the load of chlorinated acetine, which belongs to the technical field of nano-carrier research. The present invention uses hydrothermal method to synthesize nano-mil-100 (Fe), and its As a nano-carrier to transfer epichloride (NC), through the loading experiment, MIL-100(Fe) has a high loading capacity of 33.43wt% on NC, and the loaded NC@MIL-100(Fe) in phosphate buffer (pH=7.4), NC can be gradually released, and 68% is released within 4 days; NC@MIL‑100(Fe) has significantly reduced toxicity to the healthy liver cell line LO2, and higher inhibitory activity to the liver cancer cell line HepG2.

Description

technical field [0001] The invention belongs to the technical field of nano-carrier research, in particular to the application of a nano-carrier MIL-100 (Fe) on the loading of chlorinated acanthine. Background technique [0002] Cinnaline chloride (NC) is a natural alkaloid whose chemical structure is as follows: figure 1 shown. Previous studies have reported that NC has antifungal, antimalarial, anti-inflammatory and analgesic effects. In recent years, NC has demonstrated antitumor activity in liver cancer, Lewis lung cancer, renal cancer, and Ehrlich ascites carcinoma. Studies have reported that NC inhibits the growth of liver cancer cells through the Janus-activated kinase 1 / signal transducer and activator of transcription 3 (JAK1 / STAT3) signaling pathway; NC induces SMMC through pathways related to p53, p21, Bax and Bcl-2 -7721 human hepatoma cells undergo apoptosis; additionally, NC has been shown to inhibit tumor growth in HepG2 xenografted mice. However, the low b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G83/00A61P35/00A61K31/4741A61K9/51
CPCC08G83/008A61K9/5123A61K31/4741A61P35/00
Inventor 吴健毕佳瑞郑宇
Owner GUANGXI UNIV FOR NATITIES
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