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C20 ditepenoid alkaloids with anti-inflammatory and analgesic effects in radix aconiti carmichaeli and application thereof

A CH2CH3, drug technology, applied in the field of C20 diterpene alkaloid compounds, can solve the problems such as anti-inflammatory and analgesic that no one has reported

Active Publication Date: 2019-06-28
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0074] Although literature reports have obtained various chemical constituents from Aconite as mentioned above and the pharmacological activity of the chemical constituents in Aconite extracts and parts of Aconite, so far, the present invention relates to C with a novel skeleton. 20 Diterpene alkaloids and their derivatives have not only been obtained from aconite, but also no one has isolated them from other animals, plants and microorganisms through separation and purification, or prepared them through chemical synthesis and biosynthesis; and no one has reported them. These compounds or their derivatives have anti-inflammatory and analgesic functions

Method used

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  • C20 ditepenoid alkaloids with anti-inflammatory and analgesic effects in radix aconiti carmichaeli and application thereof
  • C20 ditepenoid alkaloids with anti-inflammatory and analgesic effects in radix aconiti carmichaeli and application thereof
  • C20 ditepenoid alkaloids with anti-inflammatory and analgesic effects in radix aconiti carmichaeli and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1, compound 1-3 is the novel C that extracts separation and purification from aconite 20 Diterpene alkaloids, its separation and purification process is as follows:

[0115] Dried aconite 50Kg, crushed and extracted with water at 40°C for 3 times, each time for 6 hours, the extracts were combined, the solvent was recovered under reduced pressure to 120L, and separated by macroporous resin (HPD-110, 19kg) column chromatography (20×200cm) , sequentially eluted with water (50L), 30% ethanol (120L), 50% ethanol (120L), and 95% ethanol (100L), and the solvent was recovered under reduced pressure to obtain the corresponding eluted fractions (A-D), in which part C was eluted with MCI The resin (CHP 20P) was separated and eluted sequentially with water (10L), 30% ethanol (30L), 50% ethanol (20L) and 95% ethanol (10L) to obtain the corresponding eluted fractions (C1-C4). The fraction eluted with 30% ethanol (C2, 600g) was separated with MCI resin (CHP 20P) again, fol...

Embodiment 2

[0116] Embodiment 2 anti-inflammatory effect, the impact of compound 3 on mouse ear swelling

[0117] The mouse ear swelling model induced by croton oil mixed with inflammatory solution is widely used at home and abroad. The model is stable and the inflammation lasts for a long time. It is the most commonly used model for screening anti-inflammatory drugs. In croton oil, the main inflammatory component is phorbol ester (TPA). TPA can change vascular permeability, activate macrophages, promote the accumulation of inflammatory cells, increase the release of inflammatory mediators, such as cyclooxygenase-2 (COX-2), induce NO synthase (iNOS), and secrete Inflammatory factors such as IL-6, IL-1β, TNF-α. Therefore, the croton oil-induced mouse ear swelling model is a mature model for evaluating anti-inflammatory drugs. [Wei Wei, Wu Ximei, Li Yuanjian. Pharmacological Experimental Methodology. People's Health Publishing House. 4th Edition. p742.]

[0118] Experimental animals: hea...

Embodiment 3

[0127] Embodiment 3 analgesic effect, the impact of compound 3 on acetic acid-induced pain in mice

[0128] The acetic acid writhing test is a classic model of peripheral analgesia, and is often used as one of the methods for evaluating and screening analgesics. Inject a certain volume and concentration of acetic acid into the abdominal cavity of mice, stimulate the visceral and parietal peritoneum, cause a large area of ​​deep inflammatory pain for a long time, and cause the mice to appear concave in the abdomen, trunk and hind legs stretched, and high hips. Behavioral responses are called writhing responses. The frequency of this reaction is high within 15 minutes after injection, so the number of times of writhing within 15 minutes after injection or the number of mice with reaction is used as the quantitative index of pain. [Wei Wei, Wu Ximei, Li Yuanjian. Pharmacological Experimental Methodology. People's Medical Publishing House. 4th Edition. p770.]

[0129] Experiment...

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Abstract

The invention discloses anti-inflammatory or analgesic activity of novel C20 ditepenoid alkaloid compounds (I) and (II) which can be dose-dependently achieved under safe dosage. Animal experiment results prove that the compounds 3 have a remarkable effect of inhibiting ear swelling of mice and an analgesic effect, and is expected to become a medicine for treating diseases related to inflammation and / or pains.

Description

technical field [0001] The invention relates to C with a novel skeleton extracted, separated and purified from the traditional Chinese medicine 20 Application of diterpene alkaloid compounds, derivatives and medicinal salts thereof in the preparation of prevention and treatment of acute inflammation, acute or chronic pain and other diseases. It belongs to the field of medical technology. Background technique [0002] Aconitum is a processed product of the lateral roots of Aconitum carmichaelii Debx., a plant of the genus Aconitum in the family Ranunculaceae. It is excavated from late June to early August, and the mother root, fibrous root and sediment are removed to obtain what is commonly called "Aconitum carmichaelii Debx". After processing, medicinal products such as "Salt Fuzi", "Heishun Pian" and "Baifu Pian" and other commonly used and customary specifications are obtained. [1] . Aconite has the functions of recovering yang and resuscitating adverse events, tonifyin...

Claims

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Application Information

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IPC IPC(8): C07D221/22A61K31/439A61P29/00A61P37/00A61P25/04
Inventor 石建功张天泰郭庆兰史高娜夏欢徐成博朱承根
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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