Euphorbia splendens extract as well as preparation method and application to preparation of drugs for preventing and treating EBV (Epstein-Barr Virus) infection

An extract, the technology of Tiehaitang, applied in the application field of Tietang extract and its preparation, and preparation of drugs for the prevention and treatment of EBV virus infection, can solve the problems of no compound inhibiting virus cleavage and replication, and no anti-EBV virus cleavage and replication activity. , to achieve the effect of low host cell toxicity

Active Publication Date: 2017-06-20
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, there is no report on the anti-EBV virus cleavage and replication activity of the extract of T. chinensis and its diterpene components, and there is no report on the compound’s inhibition of virus cleavage and replication.

Method used

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  • Euphorbia splendens extract as well as preparation method and application to preparation of drugs for preventing and treating EBV (Epstein-Barr Virus) infection
  • Euphorbia splendens extract as well as preparation method and application to preparation of drugs for preventing and treating EBV (Epstein-Barr Virus) infection
  • Euphorbia splendens extract as well as preparation method and application to preparation of drugs for preventing and treating EBV (Epstein-Barr Virus) infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The method for preparing compound 1~19 from Tiehaitang (Euphorbia milii):

[0049]The aerial part (3kg) of Euphorbia milii was dried in the sun, pulverized, soaked and extracted with 80% acetone water for 3 times, each time for 24 hours, and the concentrated solutions were combined to obtain a crude extract (400g), extracted with ethyl acetate, Ethyl acetate (180g) was directly subjected to silica gel column chromatography (1500g, 200-300 mesh, 7.0×100cm), cyclohexane-ethyl acetate (0:100, 10:90, 30:70, 50:50, 70:30, 80:20, 90:10, 100:0, V / V) gradient elution, each 500mL was collected, and the same fraction was combined for TLC detection, and a total of 3 fractions Fr.A-C were obtained. Part of Fr.B (50g) was eluted with silica gel column chromatography (250g, 200-300 mesh, 4.5×60cm) with dichloromethane-ethyl acetate (200:1, V / V) to obtain six fractions Fr. B1-6. Fr.B1 (300mg) was eluted with SephadexLH-20 with dichloromethane-methanol (1:1) to give compounds 17 (3mg...

Embodiment 2

[0052] According to the method of Example 1, compounds 1-19 were routinely added with water for injection, finely filtered, potted and sterilized to make an injection.

Embodiment 3

[0054] According to the method of Example 1, compounds 1-19 were dissolved in sterile water for injection, stirred to dissolve, and filtered with a sterile suction filter funnel. Then aseptically finely filtered, divided into 2 ampoules, freeze-dried at low temperature, and aseptically melt-sealed to obtain a powder injection.

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Abstract

The invention discloses a euphorbia splendens extract. The structure formula of the euphorbia splendens extract is expressed as formula (I), wherein R1 and R2 are cyclized to form cyclohexene or phenyl; any one or more hydrogen groups on cyclohexene or phenyl are substituted by R4; R4 is selected from hydrogen, hydroxyl, carbonyl, C1-C5 alcohol group or C1-C5 alkyl; or R4 and carbon on cyclohexene or phenyl form carbonyl; R3 is hydrogen, hydroxyl or carbonyl. The euphorbia splendens extract provided by the invention has obvious inhibition effect on lytic replication split period of EBV, is relatively low in toxicity to host cells, has certain safety and can be used for preparing drugs for preventing and treating EBV infection. The formula (I) is shown in the description.

Description

technical field [0001] The invention belongs to the technical field of active ingredients of traditional Chinese medicines and medicines, and more specifically relates to an extract of T. chinensis and its preparation method and its application in the preparation of medicines for preventing and treating EBV virus infection. Background technique [0002] Epstein-Barr virus (EBV) was first successfully isolated from African malignant lymphoma cells by Epstein and Barr et al. It belongs to the γ subfamily of herpesviruses in the oncovirus family and belongs to the γ-type human herpesvirus. EBV mainly infects B lymphocytes and epithelial cells, and the infected cells are prone to morphological changes and malignant proliferation, and express a variety of EBV virus genes, causing disease in patients. Epstein-Barr virus is associated with a variety of human tumors, such as Burkitt's lymphoma, Hodgkin's disease, nasopharyngeal carcinoma, and gastric cancer. The above cancers have ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/743C07C49/747C07C45/78C07C45/79C07C35/42C07C29/74C07C29/76C07C39/23C07C37/68C07C37/82A61P31/22
CPCC07C29/74C07C29/76C07C35/42C07C37/685C07C37/82C07C39/23C07C45/78C07C45/79C07C49/743C07C49/747C07B2200/07
Inventor 顾琼徐峻刘少南
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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