Sesquiterpene naphthoquinone compound as well as preparation method and medical application thereof

A compound and composition technology, applied in the field of sesquiterpene naphthoquinone compounds and their preparation, can solve the problems of separation and identification of monomers of flavonoids that have not been seen

Inactive Publication Date: 2015-11-25
林天样
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The reported components of cardamom are mainly volatile oils, polysaccharides and proteins, and it is speculated that they also contain flavonoids, but so far no flavonoids have been isolated and identified

Method used

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  • Sesquiterpene naphthoquinone compound as well as preparation method and medical application thereof
  • Sesquiterpene naphthoquinone compound as well as preparation method and medical application thereof
  • Sesquiterpene naphthoquinone compound as well as preparation method and medical application thereof

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 and mature fruits of cardamom were purchased from the Bozhou Traditional Chinese Medicine Market in Anhui Province, and the place of origin is Fujian.

[0026] Preparation method: (a) The dried and mature fruit (10kg) of cardamom is crushed to the size of mung bean, extracted with 80% ethanol under heat reflux (25L×3 times), the extracts are combined, concentrated until 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 ac...

Embodiment 2

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

[0029]1. Materials and Instruments

[0030] Human gastric cancer cell line SGC-7901 was purchased from Purcell Reagent Company; compound (I) was self-made, and the normalized purity was greater than 98%; CTX (cyclophosphamide, positive drug), trypsin, MTT, dimethyl sulfoxide ( DMSO), agarose, and glacial acetic acid were purchased from Sigma Company in the United States; RPMI-1640 medium and PBS phosphate buffer solution were purchased from GIBCO Company in the United States; fetal bovine serum was purchased from Shandong Yinxiang Weiye; trypan blue was purchased from Beijing Zhongshan Jinqiao Biology Co., Ltd.; TUNEL kit was purchased from KGI Biotechnology Development Co., Ltd.; formaldehyde was purchased from Fisher Company of the United States; catalase was purchased from Tianjin Tianxin Fine Chemical Center.

[0031] WD-9403C ultraviolet analyzer was purchased from Germany Biometra Company; RKI-1002 carbon d...

Embodiment 3

[0063] 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 sesquiterpene naphthoquinone compound as well as a preparation method and a medical application thereof, belongs to the field of medicines, and particularly relates to a novel sesquiterpene naphthoquinone compound obtained through separation of dried and mature fruits of cardamom, a preparation method and a medical application. The compound is reported for the first time, can be obtained through extraction, separation and purification of the dried and mature fruits of the cardamom and is high in purity. In-vitro tests prove that the compound can inhibit proliferation of gastric cancer cells, can realize the inhibitory activity separately and can also be combined with other anti-cancer medicines to enhance the inhibitory activity, and a medicine for treating the gastric cancer can be prepared from the compound through development.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to a sesquiterpene naphthoquinone compound isolated from the dried ripe fruit of cardamom, a preparation method and a medical application thereof. Background technique [0002] Cardamom is a perennial herb. Rhizome stout, brownish red. The leaves are in two rows, the blades are narrow and long-lanceolate, and the leaf sheaths are brownish-yellow pilose. Spikes emerge from the base of the stem. The inflorescence is markedly elongated, the flowers are sparsely arranged, and the corolla is white. The fruit is oblong, with tough skin and not easy to crack. The seed mass is divided into 3 petals, with 5 to 9 seeds in each petal, and the smell of the seeds is fragrant and strong. Mainly produced in Vietnam, Sri Lanka and the Malabar (Malabar) coast of southern India. Harvest when the fruit is ripe, remove the residual fruit stalk, and dry in the sun. Use the dried fruit of ca...

Claims

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Application Information

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IPC IPC(8): C07D307/92A61K31/343A61P35/00
CPCC07D307/92
Inventor 林天样
Owner 林天样
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