HERIPENES WITH PAIN-RELIEVING EFFECT, ACTIVE SUBSTANCES OF Hericium erinaceus MYCELIUM AND THE PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE HERIPENES OR ACTIVE SUBSTANCES

a technology of hericium erinaceus and active substances, which is applied in the field of active substances with pain-relieving effects, can solve the problems of few effective drugs that thoroughly inhibit pain, difficult treatment, tolerance and dependence problems,

Inactive Publication Date: 2017-11-02
GRAPE KING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0053]Preferably, the heripene compound above has a pain-relieving effect.

Problems solved by technology

Among the various types of pain, the ones that are hard to treat are neuropathy-induced neuropathic pain and cancer pain.
One reason is that there are few efficient drugs that thoroughly inhibit pain.
If patients are administered with a morphine analgesic for a long time, this could cause tolerance and dependence problems.
This results in side effects such as stomach injury, kidney injury and so on, and inhibits the platelet aggregation which results in frequent bleeding.

Method used

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  • HERIPENES WITH PAIN-RELIEVING EFFECT, ACTIVE SUBSTANCES OF Hericium erinaceus MYCELIUM AND THE PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE HERIPENES OR ACTIVE SUBSTANCES
  • HERIPENES WITH PAIN-RELIEVING EFFECT, ACTIVE SUBSTANCES OF Hericium erinaceus MYCELIUM AND THE PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE HERIPENES OR ACTIVE SUBSTANCES
  • HERIPENES WITH PAIN-RELIEVING EFFECT, ACTIVE SUBSTANCES OF Hericium erinaceus MYCELIUM AND THE PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE HERIPENES OR ACTIVE SUBSTANCES

Examples

Experimental program
Comparison scheme
Effect test

embodiment 3

ion of the Alcohol Extract Mixture

[0092]The freeze-dried powder and an equal amount of the alcohol extract were mixed, and then centrifuged to obtain the supernatant. The supernatant was freeze-dried to obtain a mixture of the H. erinaceus mycelia and the alcohol extract (hereinafter abbreviated as “the alcohol extraction mixture”).

embodiment 4

ion and Analysis of the Erinacine S Standard

[0093]The preparation method for the erinacine S standard is described as follows. The H. erinaceus mycelia alcohol extract was subjected to liquid-liquid partition (H2O:ethyl acetate (EA)=1:4 (v / v)), and the obtained ethyl acetate extract was further subjected to column chromatography on silica gel and Sephadex® LH-20 silica gel, followed by the gradient elution of n-hexane:EA (10:1, 3:1, 3:2, 1:1, 1:2, 0:1; v / v), to obtain 7 sub-partitions. The sub-partition 3 (which was eluted with n-hexane:EA=3:2 (v / v)) was further subjected to column chromatography on the Sephadex LH-20 silica gel to obtain a new compound, erinacine S (i.e. formula (I)), whose structural formula was identified via chemical analysis, and characteristic analysis was performed via high performance liquid chromatography (HPLC). The erinacine S was obtained using a reverse chromatography column Cosmosil 5C18-AR-II (Nacalai USA, California, U.S.A.) at 40° C. and eluted usin...

embodiment 5

hment and Analysis of the Cell Model for P2R

[0096]1. The incubation of cells:

[0097]Three cell lines, i.e. rat pheochromocytoma cell line PC12, human neuroblastoma cell line SH-SY5Y and human osteosarcoma cell line HOS, were used. PC12 cells were incubated in a Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% (v / v) horse serum (HS) and 5% (v / v) fetal bovine serum (FBS) (Kao et al., Toxicol. Sci., 2012, 125(2):462-472). Human neuroblastoma SH-SY5Y cells were incubated in a DMEM / F-12 medium supplemented with 10% (v / v) FBS (Liu et al., J. Toxicol. Sci., 2009, 34(3):255-263). HOS cells were incubated in a minimum essential medium (MEM) (containing Earle's salts, 2 mM L-glutamine and 0.1 mM non-essential amino acids) supplemented with 1.5 g / L sodium bicarbonate and 1 mM pyruvate sodium, and an extra 5% (v / v) FBS was added during use. Cells were grown in a 5% CO2 humidified incubator at 37° C. The medium was replaced every 2-3 days, and cells were sub-cultured using trypsin-et...

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Abstract

The present invention is related to an active substance of Hericium erinaceus having a pain-relieving effect, and a pharmaceutical composition including the active substance. The active substance is prepared using the following steps: (a) inoculating a mycelium of H. erinaceus on an agar plate and incubating at 15-32° C. for 8-16 days; (b) inoculating the incubated H. erinaceus mycelia from step (a) into a medium in a flask and incubating at 20-30° C. and pH 4.5-6.5 for 3-5 days; (c) inoculating the incubated H. erinaceus mycelia from step (b) into a medium in a fermentation tank and incubating at 24-32° C. and pH 4.5-5.5 for 8-16 days to obtain a fermented medium of the H. erinaceus mycelia; and (d) desiccating the fermented medium of the H. erinaceus mycelia from step (c) to obtain the powder of the H. erinaceus mycelia, which is further purified and isolated to obtain a novel compound of H. erinaceus.

Description

FIELD OF THE INVENTION[0001]The present invention is related to an active substance with a pain-relieving effect, in particular, an active substance originated from Hericium erinaceus. BACKGROUND OF THE INVENTION[0002]The neural transduction pathway of nociception and the P2-purinoceptor (P2R)[0003]The generation of nociception involves the transduction of pain signals on a series of neural pathways, finally arriving at the cerebrum, so that a human body feels pain. The neural transduction pathway of nociception starts from the generation of stimulation, followed by transforming this stimulation into neurosignals by nociceptors. The neurosignals are transmitted to the dorsal root ganglion (DRG), followed by transmission to the spinal cord and finally arrive at the nociception area in the thalamus of the cerebrum. In the preceding research, it is indicated that the distribution of the P2-purinoceptors (P2Rs) can be seen on a series of neural transduction pathways, e.g. the sensory ne...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/343C12P17/18A61K9/14A61K36/07
CPCA61K31/343A61K36/07A61K9/14A61K2236/53A61K2236/11A61K2236/33A61K2236/331C12P17/181C07D493/06A61P25/04C12R2001/645C12N1/145
Inventor LIU, PEI-SHANCHEN, CHIEN-CHIHCHEN, CHIN-CHULEE, LI-YACHEN, WAN-PINGLIN, TING-WEIHSU, JUI-HSIACHU, WEI-CHING
Owner GRAPE KING
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