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Rhododendron molle diterpene effective part as well as preparation process method and application thereof

A technology of effective parts and preparation process, which is applied in the research field of anti-rheumatoid arthritis drug use, can solve the problems of limited clinical use, high toxicity, and lack of suitable quality control standards for the content of diterpenoids, and achieves convenient The effect of industrial production, low toxicity and controllable quality

Inactive Publication Date: 2020-05-26
SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the medicinal parts such as the fruit, flower or root of the goat's henna are highly toxic, and there is no suitable quality control standard for the content of diterpenoids, so the clinical use of the goat's goat is greatly restricted

Method used

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  • Rhododendron molle diterpene effective part as well as preparation process method and application thereof
  • Rhododendron molle diterpene effective part as well as preparation process method and application thereof
  • Rhododendron molle diterpene effective part as well as preparation process method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Take 200 g of dried fruit of Rhododendron molle G. Don, add 8 times the volume of 70% ethanol to heat and reflux for extraction three times, each time for 2 hours, the extraction temperature is 60°C, combine the extracts, and concentrate to 10% ethanol concentration After standing still for 12 hours, centrifuge at 4000 rpm, centrifuge for 8 min, take the supernatant and put it on the macroporous resin column. times the column volume per hour, the elution flow rate is 4 times the column volume per hour, the diameter-to-height ratio is 1:10, eluted with pure water for 5 times the column volume, and 30% ethanol for 7 times the column volume, and collected diterpene-containing The sample is concentrated to obtain the extract of the effective part of the diterpene of A. chinensis, and the extract is mixed with the normal phase silica gel. The mass ratio of the extract and the sample normal phase silica gel is 1:2, and the normal phase silica gel column is put on. The mass ra...

Embodiment 2

[0041] Take 7 kg of dry fruit of Rhododendron molle G. Don, add 10 times the volume of 95% ethanol to heat and reflux to extract twice, each time for 3 hours, the extraction temperature is 80°C, combine the extracts, concentrate until there is no ethanol smell Stand still for 8 hours, centrifuge at 7000 rpm, and centrifuge for 14 min, take the supernatant and put it on a macroporous resin column, the loading amount is 1 kg of mulberry fruit / kg macroporous resin, and the loading flow rate is 4 times The column volume is 1 hour, the elution flow rate is 2 times the column volume per hour, and the diameter-to-height ratio is 1:7, followed by elution with pure water for 3 times the column volume, 20% ethanol for 10 times the column volume, and collecting diterpene-containing The sample is concentrated to obtain the extract of the effective part of the diterpene of A. chinensis. The extract is mixed with the normal phase silica gel. The mass ratio of the extract and the normal phase...

Embodiment 3

[0043] Take 12 kg of dry fruit of Rhododendron molle G. Don, add 5 times the volume of 70% ethanol to heat and reflux for extraction 4 times, each time for 1 hour, the extraction temperature is 50°C, combine the extracts, concentrate until there is no ethanol smell Stand still for 10 hours, filter with a 300-mesh sieve, take the filtrate and put it on a macroporous resin column, the loading amount is 1.5 kg of Azalea fruit / kg macroporous resin, the loading flow rate is 3 times the column volume per hour, and the elution flow rate 3 times the column volume per hour, the diameter-to-height ratio is 1:5, sequentially eluted with pure water for 7 times the column volume, and 50% ethanol for 5 times the column volume, collected and concentrated the samples containing diterpene to obtain the diterpene For the active part extract, mix the extract with normal phase silica gel, the mass ratio of the extract and the normal phase silica gel is 1:3, put it on the normal phase silica gel co...

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Abstract

The invention discloses a rhododendron molle diterpene effective part and a preparation process method thereof. The preparation process comprises the following steps: crushing medicinal parts such asrhododendron molle (Rhododendron molle G.Don) fruits, flowers or roots into coarse powder; extracting with ethanol, concentrating, centrifuging or filtering, taking a supernatant, sequentially passingthrough macroporous resin and normal-phase silica gel column chromatography to obtain the rhododendron molle diterpene effective part, and calculating according to the total content of rhododendron molle toxin III and rhododendron molle toxin VI to be more than 50%. The invention further discloses an application of the rhododendron molle diterpene effective part in preparation of anti-rheumatoidarthritis drugs, a type II collagen-induced arthritis model, an xylene-induced mouse auricle swelling inflammation model, an acetic acid twisting method analgesia model and a hot plate method analgesia model prove that the medicine has an obvious rheumatoid arthritis resisting effect, and a new medicine choice is provided for clinic application.

Description

Technical field: [0001] The present invention belongs to the field of traditional Chinese medicine chemistry, and relates to an effective part of the diterpene of the genus hibiscus and its preparation process and application, in particular to a method for preparing the diterpene of the roe roe by using ethanol extraction, centrifugation, separation and purification of macroporous resin and normal-phase silica gel The process of the effective part, and the research on its anti-rheumatoid arthritis drug use. Background technique: [0002] Azalea is a plant of Rhododendronaceae. It is also known as Naoyanghua, Balima, Sesame Root, Bashanhu, etc. It is a traditional Chinese medicine in my country. It is recorded in medical books such as "Good Prescriptions" that the fruits, roots and flowers of Azalea can be used as medicine, and Azalea is commonly used in folks to treat rheumatoid arthritis. Modern pharmacological studies have shown that the extract of the root of the roe deer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/45A61P19/02
CPCA61K36/45A61K2236/15A61K2236/333A61K2236/39A61K2236/51A61K2236/53A61K2236/55A61P19/02
Inventor 阮克锋梁爽张继全房鑫冯怡
Owner SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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