Scopaisoester, preparation method and application thereof, and pharmaceutical composition

An isoester and semi-preparative technology, applied in the field of extraction and separation of natural compounds, to achieve the effect of novel structure, good immunosuppressive activity, and simple operation

Active Publication Date: 2021-06-01
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, there is no good acquisition channel for the above-mentioned heteroditerpenoids, and no matter whether it is the technology of extracting from natural products or the technology of artificial synthesis, it still needs further development.

Method used

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  • Scopaisoester, preparation method and application thereof, and pharmaceutical composition
  • Scopaisoester, preparation method and application thereof, and pharmaceutical composition
  • Scopaisoester, preparation method and application thereof, and pharmaceutical composition

Examples

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preparation example Construction

[0033] The embodiment of the present invention also provides a kind of preparation method of above-mentioned isoesterin, which comprises:

[0034] Grinding the stem and / or leaves of the broom-shaped tea leaves, extracting them with an extraction solvent, and desolventizing to obtain the broom-shaped tea leaves extract; using silica gel column chromatography, reversed-phase Column chromatography, and semi-preparative HPLC separation to obtain broom-like isoesterin.

[0035] Wherein, the extraction solvent includes at least one of ethanol, acetone, methanol, ethyl acetate and water. Preferably, the extraction solvent includes a solution formed by mixing at least one of ethanol, acetone, methanol and ethyl acetate with water. More preferably, the extraction solvent includes any one of ethanol, 70%-100% acetone, 70%-100% methanol or ethyl acetate with a volume fraction of 70%-100%.

[0036] Further, the above preparation method includes:

[0037] Grinding the stem and / or leaf o...

Embodiment 1

[0049] The present embodiment provides a broom-like isoesterin, its structural formula is

[0050]

[0051] Its preparation method includes:

[0052] S1. the stem and leaf of 4kg broom-shaped fragrant tea dish is pulverized into powder, add in the extraction tank, add 20L volume content and be 70% ethanol aqueous solution, soak 3 days at 25 ℃, soak 3 times altogether, filter and merge filtrate, reduce Concentrate under reduced pressure to obtain a crude extract.

[0053] S2. The above crude extract was dispersed in 2L of water, extracted 3 times with 2L of ethyl acetate respectively, the ethyl acetate layers were combined, and concentrated under reduced pressure to obtain 250g of tea coriander extract.

[0054] S3. Mix and dissolve the above-mentioned broom-shaped tea coriander extract with 600mL methanol, mix the sample with 400g of 80-100 mesh silica gel, and pack the column with 4kg of 200-300 mesh silica gel, and use volume ratios of 1:0, 19:1, and 9, respectively. :1...

Embodiment 2

[0058] The present embodiment provides a broom-like isoesterin, its structural formula is

[0059]

[0060] Its preparation method includes:

[0061] S1. the stem and leaf of 4kg broom-like fragrant tea dish is pulverized into powder, add in the extraction tank, add 20L volume content and be the methanol aqueous solution of 70%, soak 3 days at 25 ℃, soak 3 times altogether, filter and merge the filtrate, reduce Concentrate under reduced pressure to obtain a crude extract.

[0062] S2. The above crude extract was dispersed in 2.5L of water, extracted three times with 2.5L of ethyl acetate respectively, the ethyl acetate layers were combined, and concentrated under reduced pressure to obtain 335g of broom-shaped tea coriander extract.

[0063] S3. Mix and dissolve the above-mentioned broom-shaped tea coriander extract with 750mL methanol, mix the sample with 500g of 80-100 mesh silica gel, and pack the column with 4.5kg of 200-300 mesh silica gel, and use volume ratios of 1:...

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Abstract

A scopaisoester and a preparation method and application thereof relate to the technical field of drugs. The scopaisoester is novel in structure, has an inhibition effect on T and B lymphocyte proliferation, has selectivity on the inhibition effect on T lymphocytes and can be widely applied to preparation of immunosuppressive drugs. The preparation method of the scopaisoester is simple to operate, and the scopaisoester can be rapidly and efficiently extracted from isodon scoparius. The invention also discloses a pharmaceutical composition, which comprises the scopaisoester and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition has good immunosuppressive activity and can be used as an immunosuppressive agent.

Description

technical field [0001] The invention relates to the technical field of extraction and separation of natural compounds, in particular to a bristle-like isoesterin, its preparation method and application, and a pharmaceutical composition. Background technique [0002] The plants of the genus Fragrantia are one of the important medicinal plant resources in our country. Among them, Dongling grass has been included in the Chinese Pharmacopoeia. At the same time, many plants of this genus are widely used as herbal medicines in our country for clearing away heat and detoxification, anti-inflammatory and antibacterial , anti-tumor and so on. Plants of this genus are rich in diterpene compounds with various structures, which have activities in antitumor, antibacterial and immunosuppressive aspects, such as oridonin A, eelin B and kachagenin B have significant antitumor activity . Isodonscoparius [Isodonscoparius C.Y.Wu et H.W.Li(Dunn) Kudo] belongs to the genus Isodonscoparius of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/757C07C67/48C07C67/56A61P37/06A61K31/216
CPCC07C69/757A61P37/06C07C2603/08
Inventor 普诺·白玛丹增颜秉超周敏杜雪孙汉董
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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