Unlock instant, AI-driven research and patent intelligence for your innovation.

Application of triptolide in preparation of antimalarial drugs, and pharmaceutical composition comprising triptolide

A technology of triptolide and its composition, which is applied in the field of carrier pharmaceutical compositions, and can solve the problems of antimalarial effect and drug resistance of triptolide that have not yet been seen

Inactive Publication Date: 2017-08-18
GUANGDONG XTEM BIOTECH CO LTD
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the 1950s, chloroquine, piperaquine and other 4-aminoquinoline drugs were used for antimalarial treatment, but with the application of these drugs, drug resistance appeared after 12 years of use
Triptolide has considerable potential application value and market prospect, but there is no report that triptolide has antimalarial effect

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of triptolide in preparation of antimalarial drugs, and pharmaceutical composition comprising triptolide
  • Application of triptolide in preparation of antimalarial drugs, and pharmaceutical composition comprising triptolide
  • Application of triptolide in preparation of antimalarial drugs, and pharmaceutical composition comprising triptolide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: triptolide extraction separation method

[0021] Extraction: Weigh 25kg of the whole herb of Tripterygium wilfordii, add 15L of 75% ethanol, and stir evenly. After the raw material is soaked for a set time, it is loaded into the extraction column, and the two ends of the extraction column are covered with medical gauze to prevent the filter of the extraction column from clogging and the fine particles of the material from entering the pipeline. Then hang the extraction column into the extraction kettle and seal it. Open the pipeline of the equipment to allow CO2 to enter the extraction kettle, adjust the pressure and temperature to the set value, close the pipeline of the extraction kettle, and keep it static for the set time, then open the pipeline and adjust the pressure and temperature of the separation kettle to the set value Value, dynamic cycle extraction. After the dynamic circulation extraction starts, the product is received from the split tank....

Embodiment 2

[0024] Example 2: Determination of triptolide antimalarial activity in vitro

[0025] Antimalarial activity can be determined by measuring the content of Plasmodium dsDNA (Corey, V.C., et al., A broad analysis of resistance development in the malaria parasite. Nat Commun, 2016.7: p.11901.). Add erythrocyte suspension (100 μL, cultured in RPMI1640) infected with 3D7 strain P. Add 5g / L AlbuMAX (Gibco) and 50mg / L Gentamicin (Sigma) to base (Gibco) to make malaria parasitemia reach 0.5%, hematocrit reach 2%), then place at 37°C, 5% Cultivate for 48 hours in a CO2 incubator. Cells were lysed with lysate (Tris 2.4g / L, EDTA 1.86g / L, Saponin 0.08g / L, TritonX-100 0.8mL / L) from Sigma, and dsDNA content was determined with 10000X SYBR Green I reagent (invitrogen) , the determination procedure refers to the literature (Plouffe, D., et al., In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl AcadSci U S A, 2008.1...

Embodiment 3

[0028] Example 3: In vitro toxicity test to mammalian cells

[0029]Carried out in 96-well tissue culture plates (J.Mustafa, S.I.Khan, G.Ma, L.A.Walker and I.A.Khan, Synthesis and Anticancer Activities of Fatty Acid Analogs of Podophyllotoxin.Lipids.2004,39(2):167-172 .). 25x10 in a 96-well plate 3 African green monkey kidney aneuploid cells (Vero) were planted at a density of one per well and incubated for 24 hours. Samples of different concentrations, ie, triptolide compound solutions, were added at concentrations of 1 μM, 3 μM, and 10 μM, and incubated for 48 hours. The number of surviving cells was determined by the Neutral Red assay method, and the IC was calculated from the dose-effect curve 50 . Doxorubicin was used as a positive control drug. Triptolide IC on Vero 50 The values ​​are as follows:

[0030]

[0031] The results showed that triptolide had no obvious cytotoxicity at 1-10 μM in vitro.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention provides application of triptolide in preparation of antimalarial drugs. The structural formula of the triptolide is as shown in the description. The invention also provides a pharmaceutical composition containing the triptolide as an active ingredient and a pharmaceutically acceptable carrier. The weight of the active ingredient, that is, triptolide, in the pharmaceutical composition accounts for 5-95%. Through the determination of antimalarial activity in vivo and in vivo, results show that triptolide has the relatively high antiplasmodial activity. Therefore, the triptolide can be used for preparation of drugs for treatment of malaria, and has a relatively great clinical application value.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of compound triptolide in the preparation of medicines for treating malaria, and in particular to a pharmaceutical composition in which triptolide is used as an active ingredient and a pharmaceutically acceptable carrier. Background technique [0002] Malaria (Malaria) Malaria is one of the major infectious diseases that seriously endanger people's health and life safety. According to the report of the World Health Organization, malaria is currently prevalent in 99 countries and regions around the world, about 3.3 billion people are threatened by malaria, and about 200 million people suffer from malaria every year. cases, 660,000 people died from malaria infection. Malaria is caused by Plasmodium, which includes Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae and Plasmodium ovale, among which Plasmodium falciparum has the highest fatality rate. A...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61P33/06
CPCA61K31/585Y02A50/30
Inventor 单磊刘裕婷乔志平周宝珠
Owner GUANGDONG XTEM BIOTECH CO LTD