Clerodane type diterpene compound for treating neuroglioma

A glioma and compound technology, applied in organic chemistry, antineoplastic drugs, drug combination, etc., can solve the problems of separation and identification of unseen flavonoid components

Inactive Publication Date: 2016-03-23
吴金凤
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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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  • Clerodane type diterpene compound for treating neuroglioma
  • Clerodane type diterpene compound for treating neuroglioma
  • Clerodane type diterpene compound for treating neuroglioma

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0026] 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.

[0027] Preparation method: (a) crush the dried near-ripe fruit (8kg) of cardamom, extract with 75% ethanol under heat reflux (25L×3 times), combine the extracts, concentrate until no alcohol smell (6L), and successively add 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-butanol Alcohol extract; (b) ethyl acetate extract in step (a) is dissolved to 2L with purified water, and medical absorbent cotton is filtered, and filtrate is separated with AB-8 t...

Embodiment 2

[0029] Embodiment 2: compound (I) pharmacological action test

[0030] 1. Materials and Instruments

[0031] In this experiment, the human brain malignant glioblastoma U251 cell line was purchased from the American Type Culture Collection. DMEM high-glucose medium was purchased from Hyclone Company of the United States; sodium chloride, sodium hydroxide, potassium chloride, oxygen chloride, sodium hydroxide, disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, and methanol were purchased from Nanjing chemical plant. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. Glycine, Tris, Tween20, and dimethyl sulfoxide (DMEM) were purchased from Sigma, USA; Aimexin-V / PI cell death kit was purchased from Invitrogen, USA; cell lysate, 0.25% trypsin, CellCountingKit-8 kit , penicillin, streptomycin, Hoechst33258, nuclear dye DAPI, PMSF, Westernblot gel preparation kit, nuclear protein extraction kit, Coomassie brilliant...

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 clerodane type diterpene compound for treating neuroglioma, belongs to the field of medicine, and specifically relates to a novel clerodane type diterpene compound which is separated from dry nearly-matured fruits of cardamom, a preparation method and medical applications thereof. The compound is reported for the first time and is extracted from the dry nearly-matured fruits of cardamom, the extract is separated and purified, and the purity is high. The in-vitro experiment results show that the compound can inhibit human brain malignant glioblastoma U251 cell by inhibiting cell proliferation and inducing apoptosis and can be further developed to prepare drugs for treating neuroglioma.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to a novel crotane-type diterpene compound isolated from the dried near-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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/06A61K31/365A61P35/00
CPCC07D493/06A61K9/0019A61K9/0053A61K9/0095A61K9/08A61K9/19
Inventor 吴金凤
Owner 吴金凤
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