Indole carbazole alkaloid and its preparing method and use

A technology of alkaloids and uses, applied in the field of novel indolecarbazole alkaloid compounds

Inactive Publication Date: 2005-10-19
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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Method used

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  • Indole carbazole alkaloid and its preparing method and use
  • Indole carbazole alkaloid and its preparing method and use
  • Indole carbazole alkaloid and its preparing method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Fermentative production and separation and purification of compound I

[0026] 1 Fermentation production

[0027] Fermentative culture of toxin-producing bacteria According to the conventional method of cultivating microorganisms, take an appropriate amount of Actinomadura sp.007 CCTCC M204076, inoculate it on the solid slant medium of Gaoshi Synthetic No. 1 agar, and cultivate it in an incubator at 28 degrees Celsius for 7 sky.

[0028] Get the appropriate amount of Actinomadura sp.007 CCTCC M204076 that the slant cultivated for 7 days, inoculate into one containing 100 milliliters of seed culture fluid (substratum composition: 20.0 grams of glucose, K 2 HPO 4 0.5 g, MgSO 4 0.5g, beef extract 3.0g, corn steep liquor 3.0g, yeast extract 10.0g, starch 10.0g, CaCO 3 2.0 g, 1 liter of artificial seawater, adjusted to pH 7.0) in an Erlenmeyer flask, cultured on a shaker at 28°C and 120 rpm for 48 hours to obtain a seed culture solution. Take the seed cultu...

Embodiment 2

[0035] Example 2 In Vitro Antitumor Activity Test of Compound I

[0036] 1 Experimental samples and experimental methods

[0037] Preparation of the test sample solution The test sample is the pure compound I isolated and refined in the above-mentioned Example 1. Accurately weigh an appropriate amount of sample, and prepare a solution with the required concentration with methanol for activity measurement.

[0038] Cell lines and subculture of cells Use human lung cancer A549 cells, human liver cancer BEL-7402 cells, human leukemia HL60 cells, mouse breast cancer tsFT210 cells and mouse leukemia P388 cells and other cancer cell lines. All kinds of cells were cultured in RPMI-1640 medium containing 10% FBS at 32°C (tsFT210 and P388 cells) or at 37°C (A549, HL60 and BEL-7402 cells) in an incubator filled with 5% carbon dioxide. subculture.

[0039] Cell Proliferation Inhibitory Activity Test Method

[0040] Human lung cancer A549 cells, human liver cancer BEL-7402 cells or mo...

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PUM

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Abstract

The present invention relates to indole carbazole alkaloid and its preparation process and use. The present invention adopts Actinomadura sp.007 from ocean in fermentation to prepare indole carbazole alkaloid compound with novel chemical structure. Test shows that the indole carbazole alkaloid compound may be used as cell period inhibitor, tumor cell proliferation inhibitor and antitumor preparation.

Description

Technical field: [0001] The present invention relates to a novel indolecarbazole alkaloid compound, a method for preparing the indolecarbazole alkaloid compound by fermenting Actinomyces madurasp. agents, tumor cell proliferation inhibitors or antineoplastic agents. Background technique: [0002] Indolecarbazole alkaloid staurosporine (staurosporine) is isolated from Streptomyces AM-2282 product (S.Omura, Y.Iwai, A.Nalagawa, et al., J.Antibiot., 1977,30 , 275; A.Furusaki, N.Hashiba, T.Matsumoto, et al., J.Chem.Soc.Chem.Comm., 1978, 800-801) have been found to have a variety of important biological activities, such as antibacterial, Dilation of blood vessels, cytotoxic activity, inhibition of platelet aggregation and inhibition of protein kinase C, etc. Since staurosporine aglycon is of great significance to its related biological activities (D. Meksurriyen, G.A. Cordell, J. Nat. Prod. 1988, 51, 884-892), staurosporine aglycon is used as the parent Indolecarbazole alkaloid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/553A61P35/00C07D498/22C12P17/18
Inventor 崔承彬韩小贤顾谦群朱伟明刘红兵
Owner OCEAN UNIV OF CHINA
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