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Pregnane alkaloid, and preparation method and application thereof to treatment of tumor

A technology of pregnane steroid biology and pregnane, which is applied in the field of tumor treatment, and can solve problems such as the systematic research on the chemical components and pharmacological effects of the alkaloids of osmanthus osmanthus.

Active Publication Date: 2015-07-29
FUDAN UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there have been no reports on the systematic research on the chemical components and pharmacological effects of the alkaloids of Qingxianggui

Method used

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  • Pregnane alkaloid, and preparation method and application thereof to treatment of tumor
  • Pregnane alkaloid, and preparation method and application thereof to treatment of tumor
  • Pregnane alkaloid, and preparation method and application thereof to treatment of tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Extraction and separation of embodiment 1 compound 1

[0049] The rhizome of Sarcococca ruscifolia was pulverized (635g) and infiltrated with 95% alcohol. Concentrate under reduced pressure to obtain alcohol extract, suspend in water and extract with petroleum ether, chloroform and ethyl acetate respectively to obtain three parts of petroleum ether, chloroform, ethyl acetate and water layer.

[0050] After the chloroform part was separated by alumina column chromatography, the C 18 Separation by reverse phase chromatography, gradient elution with water-methanol (20:80-10:90), gave compound 1: white powder, 10.1mg; mp134-136℃; IR (KBr): 3384cm -1 , 1664cm -1 , 1643cm -1 ,1511cm -1 ;[α] D 16.8 : +37.50 (c:0.064, CHCl 3 ); ESI-MS m / z 427.3[M+H] + ; NMR data are shown in Table 1.

Embodiment 2

[0051] Extraction and separation of embodiment 2 compound 2

[0052] Get the above-mentioned Qingxiang cinnamon chloroform part after separation by alumina column chromatography, and then use C 18 Separation by reverse-phase chromatography, eluting with water-methanol (15:85), gave compound 2: white powder, 9.1 mg; mp265-267°C; IR (KBr): 3418cm -1 , 1665cm -1 ,1641cm -1 ;[α] D 17.7 : +42.00 (c:0.1, CHCl 3 ); ESI-MSm / z425.4[M+H] + ; NMR data are shown in Table 1.

Embodiment 3

[0053] Extraction and separation of embodiment 3 compound 3

[0054] Get the above-mentioned Qingxiang cinnamon chloroform part after separation by alumina column chromatography, and then use C 18 Separation by reverse phase chromatography, eluting with water-methanol (10:90), gave compound 3: white powder, 8mg; mp186-188°C; IR (KBr): 3388cm -1 , 1642cm -1 1,1603cm -1 , 1574cm -1 , 1488cm -1 , 720cm -1 ;[α] D 17.4 : -40.63 (c:0.064, CHCl 3 ); ESI-MS m / z 449.4[M+H] + ; NMR data are shown in Table 2.

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Abstract

The present invention belongs to the pharmaceutical field, relates to a monomer compound containing pregnane alkaloid and separation preparation and application thereof to the treatment of tumor. The invention conducts systematic study on the chemical constituents and pharmacological effects of sarcococca and its affinis plant pachysandra axillaris belonging to Pachysandra, and obtains a pregnane alkaloid and a monomer compound thereof through separation. Pharmacological tests show that the obtained compound has good anti-tumor activity. The pregnane alkaloid monomer compound and combination thereof can be applied to preparation of antineoplastic drugs in the forms of a carrier or an excipient for systemic or topical administration, and can be used for the treatment of colon cancer, lung cancer, brain cancer and breast cancer.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a monomer compound containing pregnane alkaloid, its separation and preparation, and its use for treating tumors. Background technique [0002] According to reports, malignant tumors are one of the major diseases that endanger people's health. Currently, tumor treatment options in clinical practice include surgery, radiotherapy, and chemotherapy. Chemotherapy, as one of the three traditional means of tumor treatment, occupies an important position in tumor treatment. Known chemical drugs for the treatment of tumors include chemically synthesized drugs and traditional Chinese medicine extracts, etc. Finding and discovering active ingredients from natural drugs has always been a hot spot in the research of anti-tumor drugs in the industry. [0003] A variety of plants of the genus Wildfania in the Buxus family are Chinese folk medicinal materials, which are mainly used to treat stomach prob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J41/00A61K31/57A61P35/00
CPCC07J41/0005C07J75/00
Inventor 程科军俞培忠石智张鹏胡昌奇程文亮
Owner FUDAN UNIV
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