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Application of cyathane diterpene compound in antitumor drug

A compound and drug technology, applied in the application field of ornithane diterpenoids in the preparation of anti-tumor drugs, can solve the problems that have not been reported on the anti-tumor activity of this type of compounds

Active Publication Date: 2013-01-02
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In addition, in the domestic and foreign patent literature reports, there is no report on the anti-tumor activity of this type of compound.

Method used

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  • Application of cyathane diterpene compound in antitumor drug
  • Application of cyathane diterpene compound in antitumor drug
  • Application of cyathane diterpene compound in antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. The acquisition of the strain Cyathus africanus L38 producing cyathane diterpenoids 11-O-acetylcyathatriol and 15-O-acetylcyathatriol

[0026] 1. Isolation of African black egg nest (Cyathus africanus) L38

[0027] On the basis of the high-throughput screening of active compounds of microbial secondary metabolites, the inventor obtained a solid fermented extract of Cyathus africanus isolated from the fruiting body of Cyathus africanus in Wutai Mountain, Shanxi Province. Antitumor activity: Through further separation and purification under the guidance of activity tracking, a strain with high yield and easy purification to the compound was obtained, and the strain was named L38.

[0028] The specific isolation method is as follows: firstly, the surface of the collected sporocarp is sterilized with disinfectant alcohol, and then washed with sterile water; then, the packet is cut into small pieces; finally, it is inoculated on PDA medium, and the bacterial strai...

Embodiment 2

[0036] Example 2. Production of 11-O-acetylcyathatriol and 15-O-acetylcyathatriol by Cyathus africanus L38

[0037] 1. Strain activation, fermentation culture

[0038] 1. Obtaining the seed solution:

[0039] Inoculate African black egg nest (Cyathus africanus) L38 on the slant of PDA test tube agar medium for pre-cultivation; the pre-cultivation conditions are: 25°C, dark culture for 7 days (PDA medium composition: 200g of potatoes, 20g of glucose, Agar powder 16g, dilute to 1L with purified water (pH natural)). After the mycelia covered the entire slope, the mycelium was transferred to a liquid medium for cultivation under sterile conditions to obtain a seed culture solution; the conditions for liquid cultivation were: 25° C., protected from light for 7 days. Liquid medium: glucose 4.0g / L, malt extract (Malt Extract) 10.0g / L, yeast (Yeast Extract) 4.0g / L, water to 1L; yeast extract (Yeast Extract) was purchased from Oxoid Ltd. , lot number 1074139.

[0040] 2. Solid ferm...

Embodiment 3

[0055] Anti-tumor cell proliferation activity test of the compound shown in embodiment 3, formula I

[0056] Human liver cancer cell HepG2 (ATCC HB-8065), human prostate cancer cell PC3 (ATCC CRL-1435), human lung cancer cell A549 (ATCC CCL-185), human colorectal cancer cell HCT-15 (ATCC CCL-225 ), human Cervical cancer cells Hela (ATCC CCL-2), human leukemia K562 cells, human gastric cancer cells SGC-7901 (ATCCSGC-7901), and human breast cancer cells MCF-7 (ATCC HCC1428) were purchased from the Animal Laboratory of Zhongshan Medical University.

[0057] Human liver cancer HepG2 cells, human prostate cancer PC3 cells were cultured in DMEM medium containing 10% (volume percentage) fetal bovine serum, human lung cancer A549 cells, human colorectal cancer cells HCT-15, human cervical cancer Hela cells, human Leukemia K562 cells, human gastric cancer SGC-7901 cells, and human breast cancer cells MCF-7 were cultured with RPMI 1640 medium containing 10% (volume percentage) fetal bov...

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Abstract

The invention discloses an application of a compound shown in formula I shown in the specification in preparation of a drug for inhibiting tumor cell proliferation or prevention and / or treatment of tumor. In the formula I, R1 is acetyl or H, and R2 is acetyl or H. By the proving of the experiment, an MTT (methyl thiazolyl tetrazolium) method is adopted to test the inhabitation of compounds 11-O-acetylcyathatriol and 15-O-acetylcyathatriol to human hepatoma cells HeG2, human prostatic cancer cells PC3, human lung carcinoma cells A549, human colorectal cancer cells HCT-15, human cervical carcinoma cells Hela, human leukemia cells K562, human gastric carcinoma cells SGC-7901 and human breast cancer cells MCF-7. The experiment proves that the compounds play the role of proliferation and inhabitation of the eight cancer cells. Compared with other prepared antitumor drugs reported by the literature, the compound has the advantages of simpleness and easiness in obtaining and obvious activity.

Description

technical field [0001] The invention relates to the application of a cyathane diterpenoid compound in the preparation of antitumor drugs. Background technique [0002] Tumor is one of the well-known diseases that seriously endanger human health (CA-Cancer J. Clin. 2011, 61, 69-90). Among the many current treatment methods, chemotherapy (including immunotherapy) plays an irreplaceable role in the treatment of primary cancer, secondary metastatic cancer and leukemia because chemotherapy drugs can reach all parts of the body with the blood circulation (Nat. Rev. Cancer 2005, 5, 65-72). An ideal chemotherapeutic drug should have a specific target, specifically target tumor tissue in vivo, have a clear mechanism of action, and have little toxic side effects on normal tissues (Science 2001, 293, 58-59). Due to the continuous emergence of toxicity, side effects and drug resistance of traditional chemotherapy drugs, the curative effect of anti-tumor chemotherapy is reduced or inva...

Claims

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Application Information

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IPC IPC(8): A61K31/22A61P35/00A61P35/02
Inventor 刘宏伟韩俊杰宝丽
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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