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C20-diterpenoid alkaloid compound and preparation method and application thereof

A technology for diterpene alkaloids and compounds, which is applied in the field of altigen-type C20-diterpenoid alkaloids, and can solve unseen problems and the like

Active Publication Date: 2021-05-18
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Zou Yuansheng et al. reported that amides could selectively inhibit the activity of acetylcholinesterase (AChE) (Zou Y S, Zeren D, Lin C Z, et al. New Amides alkaloids from Delphinium brunonianum Royle[J]. Fitoterapia, 136(2019), doi .org / 10.1016 / j.fitote.2019.104186.), but there is no C 20 -Reports on biological activities of diterpene alkaloids promoting energy metabolism, lowering blood sugar, lowering lipids and protecting liver

Method used

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  • C20-diterpenoid alkaloid compound and preparation method and application thereof
  • C20-diterpenoid alkaloid compound and preparation method and application thereof
  • C20-diterpenoid alkaloid compound and preparation method and application thereof

Examples

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example 1

[0115] 1. Preparation of compounds

[0116] (1) Take 5 kg of Delphinium delphinium, immerse and extract with 15 and 10 times of ethanol with a volume concentration of 80% respectively, combine the extracts, recover ethanol and concentrate under reduced pressure until there is no alcohol smell, to obtain 746 g of total extract;

[0117] (2) Dissolving the total extract in water, then, extracting with sherwood oil and ethyl acetate successively, getting the ethyl acetate extract, concentrating under reduced pressure to remove the solvent to obtain 72g of the ethyl acetate extract;

[0118] (3) Mix the ethyl acetate extract into blank silica gel, pass through a silica gel column, and sequentially use dichloromethane-methanol (100:1→2:1) gradient elution; collect dichloromethane-methanol (10:1 ) eluate through a Sephadex LH-20 Sephadex column, eluting with methanol with a volume concentration of 80% as a solvent, collecting the eluate, and concentrating to obtain colorless needle-...

example 2

[0130] Example 2: (tablet)

[0131] Take 2000 mg of the compound obtained by the method described in Example 1 above, mix it with HPMC, lactose and starch in a ratio of 1:9:9:12, granulate with 95% ethanol at 20 mesh, dry below 50°C for 1 hour, 16 mesh Sieve the granules, then add 1% magnesium stearate, mix evenly, and compress into tablets to make tablets with a specification of 100 mg / tablet for oral use.

example 3

[0132] Example 3: (dropping pills)

[0133] Mix 2000 mg of the compound obtained by the method described in Example 1 above with PEG4000 and PEG6000 at a ratio of 1:20:50, melt, drop into the coolant methyl silicone oil to obtain drop pills (50 mg / granule).

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Abstract

The invention relates to a C20-diterpenoid alkaloid compound. The molecular structure of the compound is shown in the following formula (I). The compound disclosed by the invention is obtained by carrying out ethanol reflux extraction, organic solvent extraction and column chromatography separation and purification on delphinium spp. The compound disclosed by the invention has the biological activities of promoting energy metabolism, resisting inflammation, reducing blood sugar, reducing lipid, protecting liver and the like, and can be used for preparing medicines for preventing and treating the non-alcoholic fatty liver disease.

Description

technical field [0001] The present invention relates to N-containing heterocyclic compounds, in particular to C 20 - diterpene alkaloids, especially atilesen-type C with an oxazole ring 20 - Diterpene alkaloids. Background technique [0002] The oxazole ring-N-C(20)-O-C(7)-atilene-type alkaloid is rarely distributed in nature. Since 2001, the first oxazole ring- N-C(20)-O-C(7)-Atisine (Mericli A H, Mericli F, Desai H K. Diterpenoid Alkaloids from Delphinium virgatum Poiret. Chinese Chemical Letters, Die Pharmazie, 2001,32(32):418- 419.). Subsequently, two oxazole rings-N-C(20)-O-C(7)-athepine-type alkaloids delphatisine A and delphatisine B were also isolated from the whole plant of the same genus Delphinium chrysotrichum (Yangqing He, Xiaomei Wei, Yili Han, Liming Gao. Two new diterpene alkaloids from Delphinium chrysotrichum. Chinese Chemical Letters, 2007, 18(5):545-547). Diterpene alkaloids have important biological activities, and many of them have been developed i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/10A61P1/16A61P3/00A61P3/10A61P29/00A61P3/06A61K31/4188A61K9/20A61K9/48
CPCC07D498/10A61K9/2059A61K9/2031A61K9/4858A61P1/16A61P3/00A61P3/10A61P29/00A61P3/06
Inventor 林朝展祝晨蔯姚宇峰袁月
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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