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Biomedical application of ophiobollin to preparation of Gli gene inhibitor and liver cancer prevention and treatment drug

A technology of staurosporine and biomedicine, which is applied in the direction of drug combination, pharmaceutical formula, medical preparation containing active ingredients, etc., and can solve the problem of confidentiality and other issues.

Inactive Publication Date: 2018-05-08
赖旭宇
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, some foreign R&D institutions are developing these types of cephalosporins, and the specific indications are still kept secret.

Method used

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  • Biomedical application of ophiobollin to preparation of Gli gene inhibitor and liver cancer prevention and treatment drug
  • Biomedical application of ophiobollin to preparation of Gli gene inhibitor and liver cancer prevention and treatment drug
  • Biomedical application of ophiobollin to preparation of Gli gene inhibitor and liver cancer prevention and treatment drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Effects of Ophioporin A, C and 6-Epichoporin N on the Proliferation of Human Liver Cancer HepG2 Cells

[0028] 1. Experimental materials

[0029] Human liver cancer HepG2 cell line was purchased from Shanghai Jikai Gene Technology Co., Ltd.;

[0030] DMEM medium, fetal bovine serum and PBS were purchased from Gibco Company; TRIzol was purchased from Invitrogen Company; the reverse transcription kit was purchased from Fermentas Company of the United States, and the fluorescent quantitative PCR kit was purchased from TaKaRabao Bioengineering (Dalian) Co., Ltd.; cell lysate , SDS-PAGE protein loading buffer (5×), BCA protein concentration test kit, 20×TPBS buffer, etc. were purchased from Jiangsu Biyuntian Biotechnology Research Institute, PVDF membrane was purchased from Millipore, USA; CCK-8 kit Purchased from Tongren Institute of Chemistry in Japan; Gli1, Gli2 and GAPDH primers were synthesized by Shanghai Sangon Bioengineering Company;

[0031] Rabbit anti...

Embodiment 2

[0064] Example 2: Effects of Ophioporin A, C, and 6-Epichoporin N on the Proliferation of Human Liver Cancer SMMC-7721 Line Cells

[0065] 1. Experimental materials

[0066] Human liver cancer SMMC-7721 cell line was purchased from Shanghai Jikai Gene Technology Co., Ltd.;

[0067] DMEM medium, fetal bovine serum and PBS were purchased from Gibco Company; TRIzol was purchased from Invitrogen Company; the reverse transcription kit was purchased from Fermentas Company of the United States, and the fluorescent quantitative PCR kit was purchased from TaKaRabao Bioengineering (Dalian) Co., Ltd.; cell lysate , SDS-PAGE protein loading buffer (5×), BCA protein concentration test kit, 20×TPBS buffer, etc. were purchased from Jiangsu Biyuntian Biotechnology Research Institute, PVDF membrane was purchased from Millipore, USA; CCK-8 kit Purchased from Tongren Institute of Chemistry in Japan; Gli1, Gli2 and GAPDH primers were synthesized by Shanghai Sangon Bioengineering Company;

[006...

Embodiment 3

[0101] Example 3: Effects of Ophioporin A, C and 6-Epichoporin N on the Growth of Liver Cancer Transplanted Tumors in Nude Mice

[0102] HepG2 cells in a well-growth logarithmic growth phase were digested with trypsin, centrifuged and counted with trypan blue, and made 1×10 with normal saline 7 cells / mL of cell suspension were inoculated at 0.5 cm of the right axilla of nude mice, and each nude mouse was inoculated with 0.1 mL of cell suspension. Use a vernier caliper to measure the diameter of the transplanted tumor in nude mice, and wait until the tumor grows to about 100mm 3 At that time, the nude mice were randomly divided into cephalosporin A group, cephalosporin C group, 6-epichosporin N group and control group, with 10 mice in each group. At the same time, the nude mice in each group began to be administered, and the administration regimen of the cephalosporin A group, the cephalosporin C group, and the 6-epichosporin N group was: intragastric administration, 25 mg / kg / ...

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Abstract

The invention discloses biomedical application of ophiobollin to preparation of a Gli gene inhibitor and a liver cancer prevention and treatment drug. The invention discovers that ophiobollin A and Cand 6-epi-ophiobolin N can significantly inhibit the proliferation of liver cancer cells through inhibiting Gli1 and Gli2 gene expression, and the inhibiting effect shows an obvious dosage dependence;the ophiobollin A and C and the 6-epi-ophiobolin N are effective inhibitors for Gli1 and Gli2 genes and can be used for preparing the liver cancer prevention and treatment drug. Technical personnel in the field know that the inhibition of the Gli1 and Gli2 gene expression is a more mature anticancer molecular pathway, and the ophiobollin A and C and the 6-epi-ophiobolin N play an anti-cancer rolethrough the pathway. The prior art does not disclose research results of the invention.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the new application of known compounds, in particular to the biomedical application of cephalosporin for preparing Gli gene inhibitors and preventing and treating liver cancer drugs. Background technique [0002] Ophioporin A, Ophioporin C, and 6-Epichoporin N are three types of Ophioporin compounds with various pharmacological activities. At present, some foreign R&D institutions are developing these types of cephalosporins, and the specific indications are still kept secret. [0003] The chemical structures of cephalosporin A, cephalosporin C and 6-epichosporin N are as follows: [0004] [0005] These three cephalosporins were first discovered in nature, but have been mass-produced by chemical synthesis (references: ZG Brill, HK Grover, TJ Maimone; Enantioselective synthesis of anophiobolin sesterterpene via aprogrammed radical cascade, Science, 2016 , 352:1078). [0006] When th...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K31/122A61P35/00
CPCA61K31/122A61K31/343
Inventor 赖旭宇陈世伟
Owner 赖旭宇
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