Application of oldenlandia diffusa in resisting against human brain glioma cell proliferation, promoting apoptosis, resisting against metastasis and resisting against invasion

A technology of Hedyotis diffusa and human glioma, which is applied in the directions of antitumor drugs, medical preparations containing active ingredients, and the determination/examination of microorganisms. Months, easy to produce drug resistance and other problems, to achieve the effect of stable drug concentration, saving experimental time, and simple operation

Inactive Publication Date: 2018-11-27
FIRST AFFILIATED HOSPITAL OF DALIAN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In terms of drug treatment for glioma, at present, the new oral alkylating agent-temozolomide is the main chemotherapy drug for high-grade glioma, but similar to other chemotherapy drugs, there are still problems such as low efficacy and easy drug resistance.
With the classic treatment method: surgical resection in the maximum safe range, combined with radiotherapy and chemotherapy with temozolomide, the median survival time of patients can only be increased by 6 to 14.6 months

Method used

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  • Application of oldenlandia diffusa in resisting against human brain glioma cell proliferation, promoting apoptosis, resisting against metastasis and resisting against invasion
  • Application of oldenlandia diffusa in resisting against human brain glioma cell proliferation, promoting apoptosis, resisting against metastasis and resisting against invasion
  • Application of oldenlandia diffusa in resisting against human brain glioma cell proliferation, promoting apoptosis, resisting against metastasis and resisting against invasion

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Experimental program
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Effect test

Embodiment 1

[0037] Experimental study on anti-proliferative activity, anti-apoptosis, anti-migration and anti-invasion of Hedyotis diffusa extract.

[0038] 1 Preparation of Hedyotis diffusa 80% ethanol extract and drug-containing medium

[0039] 1) Preparation of Hedyotis diffusa 80% ethanol extract

[0040] Precisely weigh 25g of Hedyotis diffusa, put it in a 1000mL round bottom flask, add 20 times the amount of 80% ethanol, heat and reflux for extraction twice, the first extraction is 2 hours, and the second extraction is 1 hour. Combine the extracts, concentrate to dryness by rotary evaporation, transfer the concentrate to a 50mL volumetric flask, and dilute to the mark with 80% ethanol to obtain a solution of Hedyotis diffusa extract with a concentration of 500mg / mL (mass of medicinal material / mL), and seal it at 4°C Store in the refrigerator.

[0041] 2) Preparation of drug-containing medium

[0042] According to different experimental conditions, draw an appropriate amount of He...

Embodiment 2

[0074] UPLC-Q-TOF-MS chromatographic analysis of possible active components of Hedyotis diffusa against glioma.

[0075] Chromatographic analysis was performed using an Agilent 1290 ultra-high pressure liquid chromatograph-G6530B Q-TOF mass spectrometer. The automatic sampling system was set in the standard injection mode, and the injection volume was 0.5 μL. The HPLC analytical column is Agilent Eclipse Plus C18 (4.6×150mm, 3.5μm), and the operating temperature is 40°C. The mobile phase condition of gradient elution is: 0.1% formic acid water (A)-acetonitrile (B); 3-30 minutes B 20%-99%, 30-35 minutes B 99%-20%; mobile phase flow rate is 0.350mL / min. The mass spectrometry is in positive ion mode, the desolvation temperature is 350°C, the desolvation gas flow rate is 10L / min, the cone temperature is 400°C, the cone gas flow rate is 12L / min, the capillary voltage is 4000V, the nozzle voltage is 500V, and the fragmentation voltage is 120V. Figure 8 It is the UPLC-Q-TOF-MS p...

Embodiment 3

[0082] Network pharmacology analysis of the possible mechanism of Hedyotis diffusa anti-glioma migration and invasion.

[0083] 1) Analysis of the potential active components and their targets of Hedyotis diffusa. The potential mechanism of Hedyotis diffusa against human malignant glioma was analyzed by the system network pharmacology method based on the analysis of chemical, pharmacological and molecular biological data. By searching the TCMSP database, the discovered components of Hedyotis diffusa and their pharmacology and pharmacokinetic parameters were collected, and two key parameters were used: oral availability (OB ≥ 30%) and drug similarity (DL ≥0.18%) were screened, and 24 components were retained for further analysis. Among them, several components with obvious biological activity have been regarded as important active component indicators of traditional Chinese medicine. The two parameter values ​​of OB and DL did not meet the screening standards and were also ret...

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Abstract

The invention discloses an application of oldenlandia diffusa in resisting against human brain glioma cell proliferation, promoting apoptosis, resisting against metastasis and resisting against invasion. Specifically, the oldenlandia diffusa extract with the concentration of 4-8mg/mL is capable of effectively reducing the proliferation activity of human glioblastoma U87 cells and promoting apoptosis; under the low concentration of 1-2mg/mL without obvious influence on cell activity, the oldenlandia diffusa extract is capable of obviously reducing the cell metastasis and invasive capacity in atwo-dimensional experiment; the oldenlandia diffusa extract with the concentration of 0.5mg/mL is capable of obviously reducing the transferring amount of the cells in a Transwwell metastasis experiment; the oldenlandia diffusa extract with the concentration of 1-3mg/mL is capable of obviously restraining the U87 cell invasion capacity in a three-dimensional experiment. The functions of the oldenlandia diffusa in resisting against human brain glioma cell proliferation and invasion and the acting mechanism analysis thereof provided by the invention can supply a new clue and a new thought for the clinic treatment of glioblastoma relapse, metastasis and invasion and the further research on the acting mechanism of the oldenlandia diffusa in resisting against glioma.

Description

technical field [0001] The invention belongs to the evaluation and screening of related drugs in the field of human glioma treatment, and specifically relates to the application of Hedyotis diffusa in anti-proliferation, promotion of apoptosis, anti-migration and anti-invasion of human malignant glioma cells. Background technique [0002] Glioma is the most common primary intracranial tumor, accounting for 81% of brain tumors. The World Health Organization (WHO) classification system divides gliomas into four grades from I to IV according to the degree of malignancy. According to the classification, glioblastoma belongs to grades III and IV with higher malignant grades. It is the most common type of malignant glioma, accounting for 45% of all gliomas. At present, its 5-year relative survival rate is still lower than 5%. %, is one of the malignant tumors that seriously threaten human life and health. At present, the treatment methods that can be used clinically for malignan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/748A61P35/00A61P35/04G01N33/50C12Q1/02
CPCA61K36/748A61K2236/333A61P35/00A61P35/04G01N33/5011
Inventor 刘晶韩春辉马静云
Owner FIRST AFFILIATED HOSPITAL OF DALIAN MEDICAL UNIV
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