Aminoethyl biphenyl compound as well as preparation method and application thereof

A technology of aminoethylbiphenyl and ethylbiphenyl, which is applied in the field of medicine, can solve the problems of less chemical components and pharmacological effects of pseudophyllum, and achieve the effect of inhibiting tumor cell proliferation

Active Publication Date: 2021-11-02
SHENYANG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Native to southern Europe, there are relatively few domestic and foreign research reports on the chemical components and pharmacological effects of pseudoleaf trees

Method used

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  • Aminoethyl biphenyl compound as well as preparation method and application thereof
  • Aminoethyl biphenyl compound as well as preparation method and application thereof
  • Aminoethyl biphenyl compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: extract aminoethyl biphenyl compound from pseudoleaf tree

[0051] 1.1 Experimental materials

[0052] The false leaf tree was purchased in Anguo Market, Hebei Province in June 2016. The plant was identified by Professor Ning Wei of the College of Horticulture, Shenyang Agricultural University, and the plant samples were preserved in the Animal Pharmacy Experimental Center of Shenyang Agricultural University.

[0053] 1.2 Test method

[0054] a) 2.5kg of the rhizome of the pseudoleaf tree was extracted with 20L 95% ethanol at 80°C under reflux, the extraction was repeated 3 times, the obtained extracts were combined, and concentrated under reduced pressure to obtain 61g of the extract;

[0055] b) Suspend the extract obtained in step a) in water, extract with n-hexane, ethyl acetate, and n-butanol in sequence, each solvent is according to the volume ratio of the aqueous phase and the organic phase 1:1, to obtain ethyl acetate Extract;

[0056] c) The et...

Embodiment 2

[0067] Example 2: Aculebiphenyl A inhibits the proliferation of human leukemia cell lines

[0068] 2.1 Experimental materials

[0069] aculebiphenyl A (extracted and isolated from Pseudomonas japonica); human acute myeloblastic leukemia cell line HL-60, human chronic myeloid leukemia cell line K562, and human acute monocytic leukemia cell line THP-1 were provided by Shenyang Pharmaceutical University Huahui Donated by Professor Ming; fetal bovine serum, penicillin, streptomycin and RPMI1640 were purchased from Invitrogen, USA; 5-fluorouracil was purchased from Sigma, USA.

[0070] 2.2 Test method

[0071] HL-60, K562, and THP-1 cells were cultured in RPMI1640 medium containing 10% heat-inactivated fetal bovine serum, 100 IU / mL penicillin, 100 μg / mL streptomycin, and 1 mmol / L L-glutamine. 37°C, 5% CO 2 Incubate in a saturated humidity incubator and use it when the cell tile area reaches 70%-80%.

[0072] 0.4% trypan blue solution: weigh trypan blue, add a small amount of di...

Embodiment 3

[0079] Embodiment 3: Aculebiphenyl A antibacterial experiment

[0080] 3.1 Experimental materials

[0081] The tested strains Escherichia coli ATCC25922, Salmonella C7731, Staphylococcus aureus ATCC29213 and Streptococcus ATCC49619 were purchased from the Culture Collection Center of China Veterinary Drug Control Institute. The positive control drug gentamicin sulfate was purchased from Dalian Meilun Biotechnology Co., Ltd.

[0082] 3.2 Preparation of bacteria solution

[0083] Inoculate the preserved Staphylococcus aureus, Streptococcus, Escherichia coli, and Salmonella on the mannitol sodium chloride agar plate medium, the modified Edward agar plate medium, the MacConkey agar plate medium and the SS agar respectively in a streaking manner Incubate in plate culture medium at 37°C for 24 hours. Pick typical single colonies on the 4 kinds of culture medium and place them in nutrient broth (NB) culture medium, shake culture at 37°C and 150rpm until OD600=0.4-0.6, at this time...

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Abstract

The invention discloses an aminoethyl biphenyl compound as well as a preparation method and application thereof, and belongs to the technical field of medicines. The method comprises the following steps: firstly, extracting roots and stems of ruscus aculeata by using an ethanol water solution to obtain a crude extract, and then sequentially carrying out organic solvent extraction, ODS (Octadecylsilyl) chromatographic column and HPLC (High Performance Liquid Chromatography) multi-stage separation to obtain the aminoethyl biphenyl compound. The aminoethyl biphenyl compound disclosed by the invention can obviously inhibit proliferation of a human acute promyelocytic leukemia cell strain HL-60, a human chronic myeloid leukemia cell strain K562 and a human acute monocyte leukemia cell strain THP-1, and has a certain antibacterial activity on escherichia coli, salmonella, staphylococcus aureus and streptococcus; and the compound is expected to be used as an active component for preparing medicines for treating leukemia or resisting bacteria.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an aminoethylbiphenyl compound and its preparation method and application. Background technique [0002] Leukemia, also known as blood cancer, is a malignant tumor of the hematopoietic system. It is estimated that there are 200,000 to 250,000 new cases of leukemia every year in the world, and the annual incidence of leukemia in my country is about 2.76 / 100,000, accounting for the sixth male malignant tumor and the eighth female nausea tumor. The National Children's Tumor Surveillance Center released the first issue of the "National Children's Tumor Surveillance Annual Report 2020". The annual report shows that among the monitored discharges of children with cancer, leukemia has the highest prevalence rate, accounting for 57.21%. According to statistics, about 15,000 new children with leukemia are added every year in my country, and the incidence of childhood tumors ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/48C07C213/10A61P35/00A61P35/02A61P31/04A61K31/137
CPCC07C215/48A61P35/00A61P35/02A61P31/04Y02A50/30
Inventor 牛生吏李林董婧李应东张德显吕甜梦
Owner SHENYANG AGRI UNIV
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