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Application of physalis pubescens lactone B in preparing anti-cancer drugs

An anti-cancer drug, physalis technology, applied in the direction of drug combination, anti-tumor drugs, pharmaceutical formulations, etc., can solve the problem of synergistic effect that has not been reported in detail, and achieve the goal of being conducive to market promotion, improving anti-cancer activity, The effect of broad application prospects

Active Publication Date: 2014-08-06
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Modern pharmacological studies have shown that Physalis pilosula has anti-inflammatory, antibacterial, anti-cancer and other activities. Withanide active compounds, although it has been reported in the literature that it has anti-tumor activity, but its synergistic effect with chemotherapy drugs in combination with anti-tumor has not yet been reported in detail

Method used

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  • Application of physalis pubescens lactone B in preparing anti-cancer drugs
  • Application of physalis pubescens lactone B in preparing anti-cancer drugs
  • Application of physalis pubescens lactone B in preparing anti-cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: physapubescin B has an inhibitory effect on the proliferation of human non-small cell lung cancer cell NCI-H1975.

[0039] The specific implementation method is as follows:

[0040] Human non-small cell lung cancer cells NCI-H1975 were cultured in RPMI1640 medium containing 10% (wt) fetal bovine serum (FBS) (37°C, 5% CO 2 ), digested and counted by conventional methods, and the cells in the logarithmic growth phase were divided into 4×10 4Inoculate 200 μl at a concentration of / ml in a 96-well culture plate, set a blank control group, a drug group of physapubescin B (2.5 μM, 5 μM, 7.5 μM, 10 μM, 15 μM) and a solvent dimethyl sulfoxide (DMSO) blank control group, Each group made 3 replicate holes. When the cell growth density reaches 60%-70%, add different concentrations of physapubescin B respectively, after continuing to cultivate for 24h and 48h, add 5mg / ml tetramethylazozolium salt (MTT) 20μl solution, after continuing to cultivate for 4 hours, Terminat...

Embodiment 2

[0042] Embodiment 2: physapubescin B inhibits STAT3 kinase 705 tyrosine (Tyr 705 ) phosphorylation level.

[0043] The specific implementation method is as follows:

[0044] NCI-H1975 was cultured with RPMI1640 medium containing 10% (wt) FBS (GIBCO). When the cells grew to 70%-80%, different concentrations (0, 2.5 μM, 5 μM, 10 μM, 15 μM) of the drug physapubescin B were added. After 24 hours, the cells were collected into a 15ml Eppendorf tube, centrifuged at 800rpm for 5min. After the supernatant was discarded, the cells were transferred to a 1.5ml Eppendorf tube, centrifuged at 8000rpm for 5min. Discard the supernatant, add RIPA lysate containing 1% (wt) phosphorylase inhibitor, pipette evenly, lyse the cells on ice for 30 min, and shake once every 10 min. After the cells are fully lysed, centrifuge at 13,000rpm for 10min, take the supernatant, measure the protein concentration with a BCA protein quantification kit, add an equal volume of 2×SDS loading buffer, denature in...

Embodiment 3

[0046] Example 3: Physapubescin B down-regulates the protein expression levels of the downstream genes Bcl-2 and XIAP in human non-small cell lung cancer cells NCI-H1975STAT3.

[0047] The specific implementation method is as follows:

[0048] NCI-H1975 was cultured with RPMI1640 medium containing 10% (wt) FBS (GIBCO). When the cells grew to 70%-80%, drugs of different concentrations (0, 2.5 μM, 5 μM, 10 μM, 15 μM) were added. After 24 hours, the cells were collected into 15 ml Eppendorf tubes, centrifuged at 800 rpm for 5 min. After the supernatant was discarded, the cells were transferred to a 1.5ml Eppendorf tube, centrifuged at 8000rpm for 5min. Discard the supernatant, add RIPA lysate containing 1% (wt) phosphorylase inhibitor, pipette evenly, lyse the cells on ice for 30 min, and shake once every 10 min. After the cells are fully lysed, centrifuge at 13,000rpm for 10min, take the supernatant, measure the protein concentration with a BCA protein quantification kit, add ...

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Abstract

The invention discloses application of physalis pubescens lactone B in preparing anti-cancer drugs. The physalis pubescens lactone B is a compound having a structure as shown in formula I; the physalis pubescens lactone B is combined with cis-platinum in use to prepare anti-cancer drugs; the compound having the structure as shown in the formula I serves as a novel STAT3 inhibitor, and simultaneously acts as a chemotherapy synergist which, combined with the cis-platinum, can take a synergistic action to greatly improve an anti-cancer activity. Test results show that the physalis pubescens lactone B, as a novel STAT3 inhibitor, has an anti-cancer activity and can be used for preparing anti-cancer drugs. When combining the physalis pubescens lactone B and the cis-platinum in use, a strong synergistic action is generated; compared to single use of the cis-platinum, the combination of the physalis pubescens lactone B and the cis-platinum shows stronger anti-cancer activity; the anti-cancer drugs prepared by the combination of the physalis pubescens lactone B and the cis-platinum are favorable for market promotion and have wide application prospect. The formula I is as shown in the specification.

Description

technical field [0001] The invention relates to the field of anticancer drugs, in particular to the application of physalis lactone B in the preparation of anticancer drugs. Background technique [0002] In recent years, the morbidity and mortality of malignant tumors have been on the rise, and they have become a serious threat to human life and health. Chemotherapy is one of the indispensable links in the comprehensive treatment of malignant tumors, but it lacks targeting, has large toxic and side effects, brings great pain to patients, and is prone to multi-drug resistance during the course of medication, resulting in the failure of chemotherapy . Therefore, improving the chemotherapy efficacy of chemotherapy drugs and prolonging the survival period of patients is an urgent problem to be solved at present. [0003] Signal transducer and activator of transcription 3 (STAT3) is a kinase that can be activated by various upstream cytokines and oncogenes, and is widely involv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P35/00A61K33/24
Inventor 陈喆周丽婷马忠俊王慧中吕望朱凡凡
Owner 浙江美新控股有限公司
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