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Eremophilane sesquiterpenes with antineoplastic activity and preparation method thereof

A technology of erimofantane and anti-tumor activity, which is applied in the field of erimofnan sesquiterpene and its preparation, can solve problems such as unexplained exact relationship between lactone ring and activity, and achieve the effect of simple preparation method

Active Publication Date: 2018-06-08
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the above reports only show that this type of sesquiterpene with a lactone ring has antitumor activity, and have not elaborated on the exact relationship between the lactone ring and the activity.

Method used

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  • Eremophilane sesquiterpenes with antineoplastic activity and preparation method thereof
  • Eremophilane sesquiterpenes with antineoplastic activity and preparation method thereof
  • Eremophilane sesquiterpenes with antineoplastic activity and preparation method thereof

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Embodiment 1

[0035] Embodiment 1: preparation compound 1~4

[0036] Because the present invention involves many compounds with complicated names, in order to explain and explain more conveniently, the important compounds are numbered throughout the text. The numbering method is: compound + number. As shown in this example, 1α-hydroxyl-petasin is abbreviated as : Compound 1.

[0037] 1. Compounds 1-4 were obtained by isolation:

[0038] Dry 10 kg of the whole herb of Ligularia tibetanus, crush it, and cold-soak it with 100% methanol (50 L each time) at room temperature for 3 times, 2 days each time. After the extract was concentrated, 2.5 kg of extract was obtained, and the sample was mixed with 100-200 mesh (about 4 kg) silica gel, passed through a normal-phase silica gel column, and petroleum ether: ethyl acetate in a volume ratio of 1:0, 100:1, 20 :1, 10:1, 5:1, 2:1, carry out gradient elution, and combine the same parts through TLC detection to obtain 5 components. Pigments to obtain...

Embodiment 2

[0064] Embodiment 2: the antitumor activity of compound 1~4

[0065] 1. Prepare reagents

[0066] (1) RPMI-1640, IMDM and DMEM medium, and fetal bovine serum were purchased from Gibco (Life technologies corporation);

[0067] (2) Dimethyl sulfoxide (DMSO) and tetramethylazozolate (MTT) were purchased from Sigma (USA);

[0068] (3) taxol was purchased from Chengdu Master Company.

[0069] 2. Prepare cells to be tested

[0070] (1) Human leukemia cell line MV4-11, human lung cancer cell line A549, human gastric cancer cell line HGC-27, and human cervical cancer cell line Hela were all purchased from ATCC Company in the United States and kept in our laboratory.

[0071] (2) Each cell culture medium contains 10% fetal bovine serum, 100 U / ml penicillin and 100 μg / ml streptomycin. A-549 and HGC-27 cells were cultured with RPMI-1640; MV4-11 cells were cultured with IMDM; Hela cells were cultured with DMEM. Culture conditions: 5% CO 2 , 37°C.

[0072] 3. Inhibition of tumor cel...

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Abstract

The invention belongs to the field of medicinal chemistry, and specifically relates to eremophilane sesquiterpenes with antineoplastic activity and a preparation method thereof. The eremophilane sesquiterpenes with excellent antineoplastic activity are separated from ligularia lessicotal plants through smashing, drying, cold leaching, decoloration and elution, a novel active structure is providedfor the sesquiterpenes, and a new thought is provided for structural modification and development utilization of the sesquiterpenes. The eremophilane sesquiterpenes provided by the invention are simple in preparation method, and can be actually applied to the prevention and curing of the diseases such as liver cancer, gastric cancer, cervical cancer, leucocythemia and the like.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a class of erimofnan sesquiterpene with antitumor activity and a preparation method thereof. Background technique [0002] The genus Ligonia belongs to the family of Compositae, Senecio family, including 130 species, mainly distributed in Asia; more than 100 species are distributed in my country, mainly concentrated in the southwest region. The roots and rhizomes of many plants of the genus Ligonia are used as asters in folk medicine. They have the effects of warming the lungs and relieving phlegm, relieving asthma and relieving coughs, moistening the lungs and reducing qi, and are often used especially in Xinjiang, Yunnan, Qinghai and Tibet. Compounds extracted from plants of the genus Ligularia have antibacterial activity, cytotoxic activity, insecticidal and antifeedant activity, anti-hepatotoxic activity, etc. [0003] Sesquiterpenoids are widely found in Compo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C67/48C07C69/24C07C69/533A61P35/00A61P35/02
CPCC07C69/24C07C69/533
Inventor 周燕达娃卓玛叶烨曹治兴
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S