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Bisabolane type sesquiterpenoids as well as preparation method and application thereof

A compound and drug technology, applied in the field of bisabolane-type sesquiterpenoids and their preparation, can solve the problem of lack of vasodilation and the like

Active Publication Date: 2022-03-22
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the paper "A New Sesquiterpene Component of Sesquiterpene in Turmeric" extracted a new compound of Sesquiterpene from Turmeric, the test proved that the compound did not have the effect of dilating blood vessels.

Method used

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  • Bisabolane type sesquiterpenoids as well as preparation method and application thereof
  • Bisabolane type sesquiterpenoids as well as preparation method and application thereof
  • Bisabolane type sesquiterpenoids as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0078] Embodiment 1, the compound of the present invention [(+)-(1S,7S,9E)-bisabola-2(3),4(15),9(10)-trien-11-ol,(+)-(1S, Preparation of 7S,9E)-bisabolane-2(3),4(15),9(10)-trien-11-ol]

[0079] 1) Separation and purification of components

[0080] ① Extraction of medicinal materials: take 50 kg of dried turmeric slices, soak them overnight with 95% ethanol, then heat and reflux extraction with 95% ethanol, the weight-to-volume ratio of dried turmeric slices to 95% ethanol is 1: (8-24) kg / L Extract 3 times, extract for the first time for 3 hours, extract for the second time for 2 hours, and extract for the third time for 1.5 hours, concentrate the filtrate under reduced pressure to obtain the turmeric extract; suspend the turmeric extract in water, the weight volume of the turmeric extract and water The ratio is 7:20kg / L; then the suspension is extracted with petroleum ether and ethyl acetate successively, and concentrated under reduced pressure to obtain the turmeric petroleu...

experiment example 1

[0102] Experimental example 1, the vasodilation activity test of myrrhalkane-type sesquiterpenes of the present invention

[0103] (1) Experimental materials:

[0104] ①Drugs

[0105] Test compound A was configured into 5×10 with DMSO -2 mol / L stock solution, stored at -10°C. Positive drugs (Methoxyverapamil and Phentolamine Mesylate) were dissolved in pure water.

[0106] ② Animals and cells

[0107] SD rats, SPF grade, female, weighing 180-220 g, were purchased from Chengdu Dashuo Animal Technology Co., Ltd. Experimental animal production license number: SCXK (Sichuan) 2015-030.

[0108] Human umbilical vein endothelial cells (HUVECs) were obtained from Zhongqiao Xinzhou Biotechnology Co., Ltd. (Shanghai, China). HUVECs were cultured in DMEM medium containing 10% fetal bovine serum (FBS), 100 U / mL penicillin and 100 μg / mL streptomycin.

[0109] ③ Reagent

[0110] Methoxyverapamil, Sigma;

[0111] Phentolamine Mesylate, sold by Selleck;

[0112] Krebs-Henselei nutri...

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Abstract

The invention provides bisabolane type sesquiterpenoids as well as a preparation method and application thereof, and belongs to the technical field of chemical drugs. The bisabolane type sesquiterpenoids compound is a compound as shown in a formula I, or a crystal form thereof, or a salt of the bisabolane type sesquiterpenoids compound. Wherein R1 to R5 are respectively or simultaneously selected from hydrogen, C1-C6 alkyl, halogen, hydroxyl, C1-C6 alkoxy, amino and carboxyl. The sesquiterpenoids with a good blood vessel relaxing effect are obtained through extraction, separation and purification of rhizoma curcumae longae. The compound can be used for vasodilation, and a new choice is provided for clinical screening and / or preparation of vasodilation drugs.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines, and in particular relates to a myrrhalkane-type sesquiterpene compound and its preparation method and application. Background technique [0002] Cardiovascular disease (CVD) refers to the general designation of hypertension, coronary heart disease, stroke, myocardial infarction and other diseases caused by abnormal heart or blood vessel function. The World Health Organization lists it as one of the world's three major diseases to prevent and treat. Prevention and treatment of CVD is a scientific problem to be solved urgently in contemporary medicine. [0003] The medicinal material of turmeric is the dry rhizome of Curcuma longa L., a plant of the ginger family (Zigiberaceae). It is a traditional traditional Chinese medicine for promoting blood circulation and removing blood stasis. Dysmenorrhea, amenorrhea, lump in the abdomen, rheumatic shoulder and arm pain, tumbling, swelling and ...

Claims

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Application Information

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IPC IPC(8): C07C33/14C07C29/74C07C29/76C07C29/86A61K31/045A61P9/00A61P9/08
CPCC07C33/14C07C29/74C07C29/76C07C29/86A61P9/00A61P9/08C07B2200/07C07C2601/16
Inventor 熊亮彭成刘菲谯明鸣陈金凤
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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