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Novel diterpenoid compound for treating liver cancer

A technology for the treatment of liver cancer, compounds, applied in the field of medicine, can solve problems such as susceptibility to disease, aggravation of disease, and weak antiviral ability

Inactive Publication Date: 2015-12-23
ZIBO KUAKE MEDICINE TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The body's immune ability is low, and it is easy to be invaded by viruses and bacteria, or damaged cells, necrotic cells, and deformed cells are not quickly cleared, so they are vulnerable to attack, weak anti-virus ability, and are more prone to disease than normal people. Disease, same condition or aggravation of disease

Method used

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  • Novel diterpenoid compound for treating liver cancer
  • Novel diterpenoid compound for treating liver cancer
  • Novel diterpenoid compound for treating liver cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0025] Sources of medicinal materials and reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane are analytically pure, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, analytically pure, are purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd. The dried whole herb of the urophyll fragrant tea vegetable was purchased from the Chinese herbal medicine market in Bozhou, Anhui, and the place of origin is Guangdong.

[0026] Preparation method: (a) Grind the dried whole herb (8kg) of C. urophylla, heat-reflux extraction with 75% ethanol (25L x 3 times), combine the extracts, concentrate until no alcohol smell (6L), and successively use Petroleum ether (6L×3 times), ethyl acetate (6L×3 times) and water-saturated n-butanol (6L×3 times) were extracted and concentrated to obtain petroleum ether extract and ethyl acetate extract (315g) respectively and...

Embodiment 2

[0028] Embodiment 2: compound (I) pharmacological action test

[0029] 1. Materials and Instruments

[0030] HepG2 human liver cancer cell line was purchased from the Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences. The L02 normal human liver cell line was donated by the Liver Cancer Institute, Zhongshan Hospital, Fudan University. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. RPMI-1640 medium and trypsin were purchased from Gibco. Standard calf serum was purchased from Biowest. 3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide (MTT), dimethylsulfoxide (DMSO), trypan blue (TrypanBLue), dichlorofluorescence Diacetate diacetate (DCFH-DA) was purchased from Shanghai Sinopharm Chemical Reagent Co., Ltd. Other commonly used reagents were of analytical grade.

[0031] Microbalance (Mettler-Toledo, Switzerland, METTLRERAE2000). Ordinary desktop centrifuge (Shanghai Anting Scientific Instrument Factory). Digital...

Embodiment 3

[0056] Preparation of tablets: firstly prepare compound (I) according to the method of Example 1, and utilize organic acids such as tartaric acid, or citric acid, formic acid or oxalic acid, etc., inorganic acids such as hydrochloric acid or sulfuric acid or phosphoric acid to make salts, according to its The weight ratio of the excipient to the excipient is 1:9, and the excipient is granulated and compressed into tablets.

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Abstract

The invention discloses a novel diterpenoid compound for treating a liver cancer, belongs to the field of medicines, and particularly relates to the novel diterpenoid compound obtained by separation from a dry whole herb of plectranthus excises, and a preparation method and medical application thereof. Based on a first report, the compound can be obtained by extraction, separation and purification from the dry whole herb of the plectranthus excises, and is high in purity. An in-vitro test proves that the compound can effectively inhibit the growth and proliferation of HepG2 cells, the decrease degree and the concentration of the compound (I) present a certain dosage effect trend, and a medicine for treating the liver cancers can be further researched and developed.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a novel diterpene compound isolated from the dried whole herb of C. urophylla and its preparation method and medical application. Background technique [0002] Isodonexcisa (maxim.) hara belongs to the genus Isodonexcisa, which is widely distributed in East Asia and West Africa. There are about 150 species in the world, and about 90 species and 25 varieties in China, which are widely distributed throughout the country. Among them, about 30 kinds are available for medicinal use among the people, mainly used as clearing heat and detoxifying, anti-cancer, anti-inflammatory, invigorating the spleen, promoting blood circulation, and antibacterial drugs. [0003] Caucus urophylla contains diterpenoids, triterpenes, sterols, fatty acids, and a small amount of flavonoids, sesquiterpenes, glycosides and other active ingredients, among which diterpenoids are the main ingredients, and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/618C07C67/48C07C67/56A61K31/216A61P35/00
CPCC07C67/48C07C67/56C07C69/618
Inventor 高忠青
Owner ZIBO KUAKE MEDICINE TECH
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