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Diarylheptanes

A diaryl heptane and compound technology, applied in the field of diaryl heptane compounds, can solve problems such as hindering cellular immune response and large side effects, and achieve the treatment of Alzheimer's disease, treatment of inflammation, and inhibition of nitric oxide generated effect

Active Publication Date: 2021-03-30
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term inhibition of MAPKs signaling pathways will produce large side effects, which may hinder normal physiological functions such as normal immune responses of cells

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 2

[0045] Example 1 Extraction, separation and identification of diaryl heptane compounds

[0046] 1.1 Instruments and materials

[0047] Perkin-Elmer FT-IR infrared spectrophotometer, KBr pellets; nuclear magnetic resonance experiments using BrukerAVANCE 400 nuclear magnetic resonance; using ES-TOFMS and ES-MS mass spectrometry using Bruker microTOF and aFinnigan LC-Q II mass spectrometer; JASCO-1020 polarimeter; high performance liquid chromatography: Agilent 1260HPLC, the preparative column uses Kromasil 100-10-C18; Merck silica gel 60 (fine than 0.063 mm) and cross-linked dextran LH-20 from Pharmacia. The rhizomes of Curcuma comosa are in Nakhon Pathom, Sakon Nakhon and Prachin Buri, Thailand, and voucher specimens (Apichart Suksamrarn, Nos. 052 and 074) are deposited at the Faculty of Science, Ramkhamhaeng University.

[0048] 1.2 Separation and extraction of compounds

[0049] The rhizome (5.2kg) of C.comosa was sliced, air-dried, ground and sequentially soaked with n-hex...

Embodiment 2

[0156] Example 2 The activity of diarylheptane compounds in inhibiting NO production.

[0157] 1 material

[0158] Compounds (1-37, 39-49); mouse RAW264.7 macrophages; endotoxin (LPS, 0.5 μg / mL); BAY (10 μM, positive control) NO detection kit (Beyotime, Haimen, China).

[0159] 2 main instruments

[0160] Fluorescent microplate reader (Thermo Scientific, Waltham, MA, USA)

[0161]3 methods

[0162] 3.1 Determination of NO production by LPS-stimulated RAW264.7 macrophages

[0163] RAW264.7 macrophages were seeded in 96-well plates, and the seeding volume per well was 1×10 4 After the cells were inoculated and adhered to the wall, the compounds to be tested (1-37, 39-49) were added to incubate for 2 h, and then LPS (final concentration: 0.5 μg / mL) was added to continue culturing for 24 h. Finally, take the 96-well plate culture medium and use the NO kit to detect the NO content by measuring its OD 550 To represent. Three replicate wells were taken for each experiment, and...

Embodiment 3 2

[0173] Example 3 Inhibitory effect of diarylheptane compounds on macrophage proliferation

[0174] 1 material

[0175] Compounds (1-37, 39-49); mouse RAW264.7 macrophages; Alamar-Blue reagent.

[0176] 2 main instruments

[0177] Fluorescent microplate reader (Thermo Scientific, Waltham, MA, USA)

[0178] 3 methods

[0179] 3.1 Effects of compounds (1-37, 39-49) on the proliferation of RAW264.7 macrophages

[0180] Inoculate RAW264.7 macrophages in 96-well plate, inoculate 1×10 per well 4 After the cells are inoculated and attached to the wall, the compounds to be tested (1-37, 39-49) are added and incubated for 24 hours. Then add Am-Blue cell proliferation and activity detection reagent (SunBio TM ) 10 μL and incubate in the incubator for 2-6 hours. When the color of the culture medium changed from indigo blue to pink, the relative fluorescence unit (RFU value) of each well was measured with a fluorescent microplate reader, the excitation light wavelength was 560nm, an...

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Abstract

The invention discloses a diarylheptanoid compound shown as a formula (A). The compound provided by the invention can be used for remarkably inhibiting transcription and protein expression of iNOS, IL-1beta and IL-6 and a phosphorylation level of IkappaB protein, and can be used for treating inflammation and other various diseases including ichorrhemia and Alzheimer disease. (The formula (A) is shown in the description.).

Description

technical field [0001] The present invention relates to diaryl heptane compounds. Background technique [0002] Inflammation is a local or systemic reaction caused by a living body being infected by bacteria or viruses, pathological changes of tissues and organs, abnormality of the immune system, stimulation of harmful substances or physical damage. Inflammation is associated with the initiation and progression of various diseases. As early as 1983, Rudolf Virchow proposed that cancer cells originate inflammatory sites. After the body is damaged, the occurrence of inflammation may also lead to the canceration of normal cells. The inflammatory microenvironment in the tumor can promote the deterioration, proliferation, survival, migration of tumor cells, and inhibit the organism's own immune response. In addition, inflammation has been linked to diseases such as atherosclerosis, obesity, heart disease, diabetes, and Alzheimer's disease. Under normal physiological condition...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/255C07C43/23C07C39/12C07C39/21C07C69/157C07C69/16C07C69/18C07C251/40A61K31/12A61K31/085A61K31/09A61K31/05A61K31/065A61K31/15A61K31/222A61P29/00A61P19/02A61P25/06A61P31/04A61P31/10A61P31/12A61P35/00A61P9/10A61P19/06A61P19/04A61P1/00A61P13/12A61P17/00A61P27/02A61P17/06A61P17/02A61P25/28A61P37/00A61P27/00A61P9/00A61P3/10
CPCC07C39/12C07C39/21C07C43/23C07C49/255C07C69/157C07C69/16C07C69/18C07C251/40
Inventor 王飞阿皮恰德苏克萨穆然张国林康佳娜旺克阿将林源沈晓飞
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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