CN103356542A - Application of Sarcaboside B in preparation of medicines for treating lung cancer - Google Patents
Application of Sarcaboside B in preparation of medicines for treating lung cancer Download PDFInfo
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- CN103356542A CN103356542A CN 201310263254 CN201310263254A CN103356542A CN 103356542 A CN103356542 A CN 103356542A CN 201310263254 CN201310263254 CN 201310263254 CN 201310263254 A CN201310263254 A CN 201310263254A CN 103356542 A CN103356542 A CN 103356542A
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- sarcaboside
- lung cancer
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Abstract
The invention discloses an application of Sarcaboside B in preparation of medicines for treating lung cancer. The Sarcaboside B has good anti-lung cancer activity and can be used for the preparation of anti-lung cancer medicines, belonging to the technical field of new applications of medicines. The Sarcaboside B can be used for obviously inhibiting non-small cell lung cancer cells A549 cultured in vitro, giant cell lung cancer cells NCI-H460, lung squamous carcinoma cells HTB-8 and human lung epidermoid carcinoma cells QG-5 and has a little inhibiting effect on human normal hepatic cells LO2 and peripheral blood mononuclear cells and obvious selectivity. The application of the Sarcaboside B in preparation of the medicines for treating lung cancer is disclosed by the invention for the first time. As the skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpected strong inhibitory activity on lung cancer cells.
Description
Technical field
The present invention relates to field of antineoplastic medicaments, relate in particular to the application of Sarcaboside B in the preparation antitumor drug.
Background technology
Malignant tumor is the disease of serious threat human life health, and clinical chemotherapeutics commonly used has also damaged normal structure and cell greatly in killing tumor cell at present, and this has just limited its application.Searching is efficient, the medicine of the treatment tumor of low toxicity has become current cancer therapy drug research direction and urgent task.Searching is efficient, the low toxicity antitumor drug has been considered to a kind of effective approach.
The present invention has confirmed the non-small cell lung cancer cell A of Sarcaboside B to In vitro culture by experiment
549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5 have significant inhibitory action, and be and little on the impact of Human normal hepatocyte strain L02 and peripheral blood lymphocyte, shows obvious selectivity.
The compound S arcaboside B that the present invention relates to is one and delivered (Li in 2012, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.) New skeleton compound, this chemical compound has brand-new framework types, there is not at present the report about activity, belong to open first for the purposes in preparation treatment lung-cancer medicament that the present invention relates to, because framework types belongs to brand-new framework types, and its cytotoxicity for lung carcinoma cell is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the treatment that is used for simultaneously pulmonary carcinoma obviously has significant progress.
Summary of the invention
The objective of the invention is provides the application of Sarcaboside B in anti-pulmonary carcinoma pharmacy by studying Sarcaboside B at external anti-lung cancer activity
The invention provides Sarcaboside B as the application of preparation treatment lung-cancer medicament.
Described compound S arcaboside B structure is shown in formula I:
Formula I
The purposes of the Sarcaboside B that the present invention relates in preparation treatment lung-cancer medicament belongs to open first, because framework types belongs to brand-new framework types, and its cytotoxicity for lung carcinoma cell is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the treatment that is used for simultaneously pulmonary carcinoma obviously has significant progress.
The specific embodiment
The preparation method of compound S arcaboside B involved in the present invention is referring to document (Li, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound S arcaboside B tablet involved in the present invention:
Get 20 and digest compound Sarcaboside B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound S arcaboside B capsule involved in the present invention:
Get 20 and digest compound Sarcaboside B, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: Sarcaboside B is on the inhibited proliferation of the lung carcinoma cell of In vitro culture and on the impact of human normal cell line
Lung carcinoma cell (the non-small cell lung cancer cell A of trophophase takes the logarithm
549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5) and human normal liver cell L 02 be inoculated on 96 well culture plates, every hole inoculum concentration is respectively 3000 ~ 4000/100uL and 6000/100uL; Aseptic collection healthy blood donor's venous blood 15 mL, anticoagulant heparin separates mononuclearcell with the Ficoll density－gradient centrifuga－tion method, and with the RPMI1640 preparation individual cells suspension that contains 10% hyclone, transferring cell concentration is 2 * 10
5Individual/mL, be inoculated in 96 well culture plates, every hole 100 uL.Behind above-mentioned each culture plate cell culture 24h, experimental group adds Sarcaboside B 100 uL of variable concentrations, and each concentration is done three multiple holes; Negative control group Ensure Liquid liquid 100uL, blank hole Ensure Liquid liquid 100 uL are used for the instrument zeroing.Behind the effect different time (48h and 72h), every hole adds MTT 20 uL of 5mg/mL, continues to cultivate 4h, gets rid of supernatant, and every hole adds dimethyl sulfoxine 150 uL.Measure the absorbance (A in 570 each hole of nm with microplate reader (BIO-RAD product)
570), each group is averaged, and calculates suppression ratio: suppression ratio=(1-experimental group A
570/ control group A
570) * 100%.Carry out statistical analysis with SPSS13.0, and calculate IC
50
The result: Sarcaboside B all has obvious increment inhibitory action to above-mentioned lung carcinoma cell; And Sarcaboside B is to Human normal hepatocyte and peripheral blood lymphocyte inhibitory action less (table 1).As seen Sarcaboside B has obvious selective inhibitory to tumor cell.
Table 1 Sarcaboside B is to tumor cell and Normocellular half-inhibition concentration
Conclusion: Sarcaboside B can significantly suppress the non-small cell lung cancer cell A of In vitro culture
549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5, and less to the inhibitory action of Human normal hepatocyte LO2 and peripheral blood lymphocyte, show obvious selectivity.Therefore, can be used for pulmonary carcinoma is treated.
Claims (1)
1.Sarcaboside B the treatment pulmonary carcinoma medicine in application, described compound S arcaboside B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310263254 CN103356542A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in preparation of medicines for treating lung cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310263254 CN103356542A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in preparation of medicines for treating lung cancer |
Publications (1)
| Publication Number | Publication Date |
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| CN103356542A true CN103356542A (en) | 2013-10-23 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN 201310263254 Pending CN103356542A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in preparation of medicines for treating lung cancer |
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| Country | Link |
|---|---|
| CN (1) | CN103356542A (en) |
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2013
- 2013-06-27 CN CN 201310263254 patent/CN103356542A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20131023 |