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Series of open-loop abietane diterpene compounds, and pharmaceutical compositions and application thereof in pharmacy

A kind of compound, technology of rosinane, applied in a series of ring-opening rosinane type diterpenoids and their pharmaceutical compositions and their application fields in pharmacy

Active Publication Date: 2018-03-02
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

That is, there is no ring-opening abietane type diterpenoid compound Rxh-126(1), Rxh-125(2), Rxh isolated from Kangding sage (Salvia pratii) related to the present invention in the prior art -129(3), Rxh-138(4), Rxh-119(5), Rxh-169(6), Rxh-164(7), Rxh-163(8), Rxh-137(9), Rxh- 131(10) and their reported vasodilatory activity

Method used

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  • Series of open-loop abietane diterpene compounds, and pharmaceutical compositions and application thereof in pharmacy
  • Series of open-loop abietane diterpene compounds, and pharmaceutical compositions and application thereof in pharmacy
  • Series of open-loop abietane diterpene compounds, and pharmaceutical compositions and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Compounds Rxh-126(1), Rxh-125(2), Rxh-129(3), Rxh-138(4), Rxh-119(5), Rxh-169(6), Rxh-164(7), Preparation and structural data of Rxh-163(8), Rxh-137(9), Rxh-131(10):

[0022] The whole herb of Sage Kangding is 38kg, crushed and cold-soaked with acetone at room temperature for 3 times (48 hours / time), combined the extracts, and distilled under reduced pressure to obtain the extract. It was dissolved in silica gel to mix the sample, and the silica gel column chromatography was eluted with chloroform, ethyl acetate, and methanol respectively to obtain a chloroform fraction (667 g). The chloroform part was mixed with silica gel, silica gel column chromatography, and mixed with petroleum ether / chloroform / ethyl acetate (50:1:1, 20:1:1, 10:1:1, 5:1:1, 1:1: 1) Elution yields 7 sections A-G. Among them, section B (223g) was mixed with polyamide, passed through the MCI column, and carried out gradient elution with methanol-water (70:30-100:0) as the mobile phase to obtain 8 sec...

Embodiment 2

[0052] Effects of compounds 1-10 on isolated rat thoracic aorta:

[0053] 1. Preparation of vascular rings: Take out the rat thoracic aorta quickly, carefully remove the surrounding connective tissue of the blood vessel wall, and cut the blood vessels into 3-4mm vascular rings. Transfer the vascular ring to a bath filled with 5mL krebs solution, kept at a constant temperature of 37°, and continuously pass mixed oxygen, and fix it on a hook in the bath, and connect the other hook to a tension transducer, and record it with the RM-6240 system Tension of vascular rings. Before the experiment, the blood vessels were given a basic tension of 1.5g in advance, and the blood vessels were balanced for 60 minutes, and the liquid was changed every 15 minutes during this period. After the balance of the vascular ring is stable, use phenylephrine 10 -5 mol / L pre-constricted vascular ring reaches the peak value, add acetylcholine 10 -5 mol / L to verify the integrity of the endothelium. If...

Embodiment 3

[0059] Preparation of tablets:

[0060] Obtain ring-opening abietane type diterpenoids 1-10 by the method for embodiment 1-5, and utilize organic acid (tartaric acid, citric acid, formic acid, oxalic acid etc.) or mineral acid (hydrochloric acid, sulfuric acid, phosphoric acid etc.) ) made salt, adding excipients in the ratio of 1:5-1:10 by weight to the excipients, granulating and compressing into tablets.

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Abstract

The invention provides a series of open-loop abietane diterpene compounds or pharmaceutical salts thereof, pharmaceutical compositions composed of the compounds as effective ingredients and at least one pharmaceutically acceptable carrier, and a preparation method and an application of the compounds or the pharmaceutical salts thereof in preparation of drugs or functional foods for prevention and(or) treatment of hypertension, heart disease, myocardial ischemia, stroke and other cardiovascular and cerebrovascular diseases. The compounds 1-8 are novel open-loop abietane diterpene compounds, have significant vasodilation activity on KCl preshrunk rat thoracic aorta, have a novel chemical structure, and have many advantages as vasodilation drugs. The compounds 9 and 10 are known compounds, also have significant vasodilating effects on KCl preshrunk rat thoracic aorta, and have no reports in vasodilation at present.

Description

Technical field: [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a series of ring-opening abietane-type diterpenoids, pharmaceutical compositions using them as active ingredients, their preparation methods, and their application in pharmacy, especially in the preparation of vasodilation The application of drugs or drugs for treating cardiovascular and cerebrovascular diseases, and the application in the preparation of drugs for treating hypertension, heart disease, myocardial ischemia, stroke and other cardiovascular and cerebrovascular diseases. Background technique: [0002] There are about 1,000 species of Salvia Linn (Salvia Linn) in the family Labiatae, all over the warm regions of the world. There are 79 species in China, distributed all over the country, especially in the southwest region. There are nearly 30 kinds of medicinal plants, most of which use their roots as medicine to treat cardiovascular and cerebro...

Claims

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Application Information

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IPC IPC(8): C07D311/78C07D307/77C07D307/88C07D493/10A61K31/352A61K31/343A61P9/12A61P9/10A61P9/00A61P25/00A61P9/08
CPCC07D307/77C07D307/88C07D311/78C07D493/10
Inventor 许刚纪旭夏凡罗丹
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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