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Novel withanolides compound, novel withanolides compound preparation method and medical application of novel withanolides compound

A compound and composition technology, applied in the field of new withanolide compounds and their preparation, can solve the problems of few literature reports on pharmacological activity research and the like

Inactive Publication Date: 2015-12-16
林天样
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Hainan, Guangxi, Guangdong, Fujian and other places have always used Dongfengju to treat acute and chronic bronchitis, and achieved good clinical results, but there are relatively few literature reports on the pharmacological activity of this product

Method used

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  • Novel withanolides compound, novel withanolides compound preparation method and medical application of novel withanolides compound
  • Novel withanolides compound, novel withanolides compound preparation method and medical application of novel withanolides compound
  • Novel withanolides compound, novel withanolides compound preparation method and medical application of novel withanolides compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0028] 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 roots of Dongfengju were purchased from the Chinese herbal medicine market in Bozhou, Anhui Province, and were produced in Fujian.

[0029] Preparation method: (a) The dry root (8kg) of Dongfeng orange is crushed to the size of mung bean, extracted with 70% ethanol under hot reflux (25L×3 times), the extracts are combined, concentrated to no alcohol smell (6L), and sequentially washed with 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, ethyl acetate extract (315g) and n-butan...

Embodiment 2

[0031] Embodiment 2: compound (I) pharmacological action test

[0032] 1. Materials and Instruments

[0033] DMEM / F12 high glucose culture medium was purchased from Beijing Hyclone Company. The improved RPMI-l640 medium was purchased from Beijing Hyclone Company. Standard fetal bovine serum was purchased from Tianjin TBD Company. CCK-8 cell viability assay reagents were purchased from Tongjin Chemical Research Institute, Japan. AnnexinV-FITC / PI apoptosis detection kit was purchased from Shanghai Yanbin Chemical Technology Co., Ltd. JC-1 mitochondrial membrane potential probe was purchased from Jiangsu Biyuntian Biotechnology Research Institute. Dimethylsulfite (DMSO) and phosphate buffered saline (PBS) were purchased from Sigma.

[0034] -70°C low-temperature refrigerator (Forma Scientific Inc., the United States), electronic balance (Shimadzu AEL-200 type, Japan), ultra-clean workbench (SW-CJ-IC type, Suzhou), constant temperature oscillator (THZ-C type, Domestic), high...

Embodiment 3

[0057] 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 belongs to the field of medicines, discloses a novel withanolides compound, a novel withanolides compound preparation method and a medical application of the novel withanolides compound and particularly relates to a novel withanolides compound obtained by separation from dried roots of attalanteae buxifoliae, a preparation method of the novel withanolides compound and a medical application of the novel withanolides compound. The novel withanolides compound which is reported for the first time can be obtained by separation and purification after extraction from the dried roots of attalanteae buxifoliae, and high purity is achieved. According to in-vitro tests, the novel withanolides compound with an effect of in-vitro resistance to breast cancers is capable of inhibiting proliferation of various breast cancer cells, shows high in-vitro cytotoxicity and can be further researched and developed for preparation of breast cancer treatment medicines.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a new withanide compound isolated from the dry root of dongfengju and its preparation method and medical application. Background technique [0002] Dongfengju Atalantiabuxifolia (Poir).Oliv. is a plant of the Rutaceae wine cake genus, which was first recorded in "Lingnan Herb Collection", and is currently an appendix to the third volume of traditional Chinese medicine preparations in "National Compilation of Chinese Herbal Medicine" and "Drug Standards of the Ministry of Health" load. The medicinal roots and rhizomes of Dongfeng orange are pungent, bitter, and slightly warm in nature, and return to the lung, stomach, and spleen meridian. Hainan, Guangxi, Guangdong, Fujian and other places have always used this product to treat acute and chronic bronchitis, and the clinical effect is good. In addition, studies have shown that it has good effects on reducing phlegm, relieving ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/585A61P35/00
Inventor 林天样
Owner 林天样
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