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New application of artesunate and composition containing artesunate

A kind of technology of artesunate and composition, applied in the new application field of composition

Pending Publication Date: 2021-12-03
香港浸会大学深圳研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the effect of artesunate on BRAF (V600E) inhibitor-resistant tumors, or the effect of the combination of ginsenoside Rg3 and artesunate on BRAF (V600E) inhibitor-resistant tumors

Method used

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  • New application of artesunate and composition containing artesunate
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  • New application of artesunate and composition containing artesunate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1. Effects of ginsenoside Rg3 and artesunate alone and in combination on the proliferation of melanoma cells resistant to BRAF (V600E) targeting drugs

[0048] 1.1. Experimental materials

[0049] (1) Ginsenoside 20-R-Rg3: purchased from Nanjing Yuanzhi Biotechnology Co., Ltd.; weigh a certain amount of ginsenoside 20-R-Rg3, and dissolve it into 20 mM Rg3 solution (mother liquor) with dimethyl sulfoxide (DMSO) ), subpackage, and store in a -20°C refrigerator for later use.

[0050] (2) Artesunate: purchased from Chengdu Mansite Biotechnology Co., Ltd.; weigh a certain amount of artesunate, dissolve it in DMSO to 50mM artesunate solution (mother solution), subpackage, and store at -20°C Refrigerator for spare.

[0051] (3) Vemurafenib: produced by LC Laboratories; a certain amount of vemurafenib was weighed, dissolved in DMSO to form a 10 mM vemurafenib solution (mother solution), subpackaged, and stored in a -20°C refrigerator for later use.

[0052] (4) A375...

Embodiment 2

[0081] Example 2. Effects of ginsenoside Rg3 and artesunate alone and in combination on normal cell survival

[0082] 2.1. Experimental materials

[0083] (1) Ginsenoside 20-R-Rg3: purchased from Nanjing Yuanzhi Biotechnology Co., Ltd.; weigh a certain amount of ginsenoside Rg3, dissolve it in DMSO into a 20mM Rg3 solution (mother solution), subpackage it, and store it in a -20°C refrigerator for later use .

[0084] (2) Artesunate: purchased from Chengdu Mansite Biotechnology Co., Ltd.; weigh a certain amount of artesunate, dissolve it in DMSO to 50mM artesunate solution (mother solution), subpackage, and store at -20°C Refrigerator for spare.

[0085] (3) Normal cell line: human immortalized keratinocyte HaCaT; purchased from ATCC cell bank in the United States and stored in liquid nitrogen.

[0086] (4) DMEM medium powder: produced by Gibco, USA.

[0087] (5) 0.5% trypsin-EDTA (10X) (Trypsin): 100 mL / bottle, produced by Gibco, USA.

[0088] (6) Fetal bovine serum: 500 ...

Embodiment 3

[0106] Example 3, Effects of Ginsenoside Rg3 Combined with Artesunate on Melanoma Mice Bearing Resistance to BRAF (V600E) Inhibitors

[0107] 3.1. Experimental materials

[0108] Experimental animals: male BALB / c-nu / nu nude mice (about 8 weeks old), provided by the Animal Experiment Center of the Chinese University of Hong Kong. They were raised in a sterile environment with constant temperature and pressure in the Experimental Animal Center of Hong Kong Baptist University.

[0109] Cells A375R with acquired resistance to vemurafenib: A375 cells were purchased from the ATCC cell bank in the United States. Melanoma cells A375R resistant to vemurafenib were established in Example 1, and subsequently treated with 2 μM vemurafenib and The cells were cultured in DMEM with 10% FBS to maintain their drug resistance.

[0110] Ginsenoside Rg3 intragastric solution: Weigh 7.2mg ginsenoside Rg3 and dissolve it in 0.3mL of DMSO, then dilute it to 6mL with carboxymethylcellulose sodium (...

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Abstract

The invention relates to an application of artesunate in preparation of a medicine for preventing and treating a tumor tolerant to a BRAF (V600E) inhibitor, and an application of a ginsenoside Rg3 and artesunate composition in preparation of a medicine for preventing and treating a tumor tolerant to the BRAF (V600E) inhibitor, so that the treatment effect on the tumor tolerant to the BRAF (V600E) inhibitor can be enhanced.

Description

technical field [0001] The present invention relates to a new application of medicine, in particular to a new application of artesunate and a composition containing it. Background technique [0002] BRAF is a serine / threonine-specific protein kinase and a member of the growth signal transduction protein kinase family. The T1799A point mutation of BRAF gene (i.e. V600E mutation) will lead to continuous activation of BRAF protein, thereby activating the downstream mitogen-activated protein kinase (MAPK) / extracellular regulated protein kinase (ERKs) signaling cascade pathway, stimulating cell proliferation and differentiation , inhibits apoptosis and ultimately promotes cancer progression. This mutation occurs in a variety of cancers, such as hairy cell leukemia (about 100%), Erdheim-Chester blood cancer (about 54%), papillary thyroid carcinoma (about 50%), melanoma (40%-60%), tumor Colorectal cancer (about 12%) and non-small cell lung cancer (about 7%) and so on. Vemurafeni...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/704A61K45/06A61P35/00A61P35/02
CPCA61K31/357A61K31/704A61K45/06A61P35/00A61P35/02A61K2300/00
Inventor 禹志领符秀琼金艳霞
Owner 香港浸会大学深圳研究院
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