Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Neo-clerodane diterpenoid compound, and preparation method and medical application thereof

A compound and drug technology, applied in the field of Crotane-type diterpenoids and their preparation, can solve the problems of separation and identification of unseen flavonoid components and monomers

Inactive Publication Date: 2016-03-09
XINING YIGE INTPROP CONSULTING SERVICE
View PDF0 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The reported components of cardamom are mainly volatile oils, polysaccharides and proteins, and it is speculated that they also contain flavonoids, but so far no flavonoids have been isolated and identified

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Neo-clerodane diterpenoid compound, and preparation method and medical application thereof
  • Neo-clerodane diterpenoid compound, and preparation method and medical application thereof
  • Neo-clerodane diterpenoid compound, and preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0023] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0024] Preparation method: (a) The dried and mature fruit (10kg) of cardamom is pulverized, extracted with 80% ethanol under heat reflux (25L×3 times), the extracts are combined, concentrated to no alcohol smell (3L), and sequentially extracted with petroleum ether (3L ×3 times), ethyl acetate (3L×3 times) and water-saturated n-butanol (3L×3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract (398g) and n-butanol extract respectively; (b) In the step (a), the ethyl acetate extract is removed with AB-8 type macroporous resin, first eluted with 10% ethanol for 8 column volumes, then with 75% et...

Embodiment 2

[0026] Embodiment 2: compound (I) pharmacological action test

[0027] 1. Materials and Instruments

[0028] K562 cells were provided by Shanghai Institute of Biological Cells, Chinese Academy of Sciences. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. RPMI-1640 dry powder medium was purchased from Gibco. Calf serum was purchased from Hangzhou Sijiqing Institute of Bioengineering Materials. Penicillin and streptomycin were purchased from Huabei Pharmaceutical Factory. Glutamine, MTT, DMSO were purchased from AMRESCO. Annexinv-FITC cell apoptosis detection kit was purchased from Nanjing KGI Biotechnology Development Co., Ltd. MOPS, Rnasin, agarose, olfactory ethidium, bromophenol blue Huamei Bioengineering Company Huamei Bioengineering Company.

[0029] CO 2 Incubator (Thermo Company, USA), ultra-clean bench (Suzhou Purification Equipment Factory), magnetic stirrer (Shanghai Nanhui Telecommunication Equipment Factory), inverted microscope ...

Embodiment 3

[0052] Preparation of tablets: firstly prepare compound (I) according to the method of Example 1, and utilize organic acids such as tartaric acid, or citric acid, formic acid or oxalic acid, etc., inorganic acids such as hydrochloric acid or sulfuric acid or phosphoric acid to make salts, according to its The weight ratio of the excipient to the excipient is 1:9, and the excipient is granulated and compressed into tablets.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a neo-clerodane diterpenoid compound and a preparation method and medical application thereof, and provides the structure of the compound, a pharmaceutical composition containing the compound and a preparation method and application of the pharmaceutical composition. The compound is reported for the first time, is a neo-clerodane diterpenoid compound with a novel structure and can be extracted, separated and purified from dried mature fruit of cardamom. In-vitro test results prove that the compound can directly inhibit propagation of K562 cells, and the inhibition capability of the compound is improved with increase of concentration and prolongation of action time. Meanwhile, the compound can induce apoptosis of K562 cells, and the apoptosis promotion effect is improved with increase of concentration and time. The compound (I) may provide a potential means for treatment of chronic granulocytic leukemia and can be used for developing medicines for treating chronic granulocytic leukemia.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a crowane-type diterpene compound isolated from the dried ripe fruit of cardamom and capable of treating chronic myeloid leukemia and a preparation method thereof. Background technique [0002] Cardamom is a perennial herb. Rhizome stout, brownish red. The leaves are in two rows, the blades are narrow and long-lanceolate, and the leaf sheaths are brownish-yellow pilose. Spikes emerge from the base of the stem. The inflorescence is markedly elongated, the flowers are sparsely arranged, and the corolla is white. The fruit is oblong, with tough skin and not easy to crack. The seed mass is divided into 3 petals, with 5 to 9 seeds in each petal, and the smell of the seeds is fragrant and strong. Mainly produced in Vietnam, Sri Lanka and the Malabar (Malabar) coast of southern India. Harvest when the fruit is ripe, remove the residual fruit stalk, and dry in the sun...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D493/10A61K31/365A61P35/02
CPCC07D493/10
Inventor 杨辉
Owner XINING YIGE INTPROP CONSULTING SERVICE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com