CN106074566B - The purposes of ganoderma lucidum triterpene compounds - Google Patents
The purposes of ganoderma lucidum triterpene compounds Download PDFInfo
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- CN106074566B CN106074566B CN201610378137.XA CN201610378137A CN106074566B CN 106074566 B CN106074566 B CN 106074566B CN 201610378137 A CN201610378137 A CN 201610378137A CN 106074566 B CN106074566 B CN 106074566B
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- ganoderma lucidum
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- triterpene compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/569—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
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- Pharmacology & Pharmacy (AREA)
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Abstract
The invention belongs to pharmaceutical technology fields, the specifically purposes of natural product active ingredient.The present invention investigates the activity that 22 ganoderma lucidum triterpene compounds inhibit mouse BV-2 microglia NO release using Griess method.In addition to compound 4, remaining ganoderma lucidum triterpene compounds is on the survival rate of BV-2 microglia without influence, it can preferably inhibit LPS induction BV-2 microglia release NO, wherein compound 6,11,13,14,17,18,22 shows significant inhibitory activity, IC5010 μM are below, shows that these compounds are likely to become lead compound.
Description
Technical field
The invention belongs to pharmaceutical technology fields, the specifically purposes of natural product active ingredient.
Background technique
Nerve retrograde affection is a kind of even dead for pathological characters with the normal function and structure of neuron loss
Disease, including Parkinson's disease (PD), Alzheimer disease (AD), multiple sclerosis (MS) etc., the generation and development of these diseases
It is all closely related with neuroinflamation.Microglia is the intrinsic immunocyte of central nervous system, the spy with macrophage
Sign, is distributed widely in brain and spinal cord." tranquillization " state and the microglia moderately activated can play important being immunized and prevent
Imperial, immunosurveillance maintains ambient stable in nervous system.Excessively or the microglia of persistent activation then mediates mind
Through inflammation, the inflammatory mediator including IL-1 β, TNF-α, nitric oxide and reactive oxygen species etc. is discharged, secondary nerve is caused
Damage.
Ganoderma lucidum is the general name of Ganodermataceae, belongs to mycota, and one kind of Basidiomycota, Basidiomycetes, Aphyllophorales is high
Equal basidiomycetes, be China successive dynasties medicine scholar praise highly strengthening by means of tonics, righting reinforcing precious drug, long term usage has macrobiosis of making light of one's life by commiting suicide
Effect.Ganoderma lucidum is classified as top grade by Shennong's Herbal.About ganoderma lucidum chemical component and its bioactivity research, always all for many years
It is one of the research hotspot of domestic and international pharmaceutical field.The overwhelming majority research concentrate on red sesame Ganoderma Lucidum this
Kind occasionally relates to purple sesame Ganoderma sinense, Ganoderma tsugae Ganoderma tsugae, Ganoderma capuse Ganoderma
The kinds such as capense, ganoderma lipsiense Ganoderma applanatum.
Modern pharmacology shows that ganoderma lucidum has antitumor, anti-oxidant, anti-aging, anti-HIV-1 virus, blood pressure lowering, immune tune
Section, protecting liver and detoxication and it is antibacterial the effects of.
Summary of the invention
The object of the present invention is to provide the purposes of ganoderma lucidum triterpene compounds.
The technical scheme to solve the above technical problems is that
1. the activity that ganoderma lucidum triterpene compounds inhibit LPS induction BV-2 microglia release NO.
Benefit effect of the invention is as follows:
1. provide the possibility lead compound of nerve retrograde affection, these compounds parent nucleus having the same and similar
Substituent group, for structure-activity relationship etc. in next step research have great role.
Specific embodiment
The present invention will be further described below with reference to examples.
Embodiment 1
22 ganoderma lucidum triterpene compounds for pharmacological activity experiment are detailed in Table 1:
Table 1 Compounds isolated from EtOAc parts of Ganoderma curtisii.
Pharmacological activity experiment: the present invention is investigated ganoderma lucidum triterpene compounds using Griess method and inhibits the small glue of mouse BV-2
The activity of cell plastid NO release.
22 ganoderma lucidum triterpene compounds and positive drug Quercetin are dissolved with DMSO and are diluted to suitable concentration, -20
It DEG C saves backup.BV-2 microglia is adjusted to 2 × 105A/mL is inoculated in 96 porocyte culture plates, and every hole is added
100 μ L cell suspending liquids, 37 DEG C, 5%CO2After culture overnight, each hole is loaded by following grouping situation: (1) lipopolysaccharides
(1ipopolysaccharide, LPS) group is added without tested sample；(2) blank control group (isometric DMSO)；(3) through LPS
(LPS that final concentration of 1 μ g/mL is added is incubated for 30min to the ganoderma lucidum triterpene compounds of pretreated various concentration, then adds respectively
Enter the sample that concentration is 40,20,10,2.5,1.0,0.5,0.1 μM), each concentration sets 3 parallel holes.In 37 DEG C, 5%CO2It is permanent
After being cultivated for 24 hours in warm incubator, 100 μ L of culture solution supernatant is drawn into ELISA Plate, isometric Griess reagent, room temperature is added
The light absorption value at 540nm is measured after reaction 15min.It is respectively the NaNO of 1,2,5,10,20,40,60,100 μm of ol/L with concentration2
Standard curve is drawn, according to NaNO2Standard curve calculates NO in cell culture supernatant2 -Concentration and to NO release inhibition
Rate, inhibiting rate calculation formula are as follows:
The macrophage release NO that measurement sample induce LPS inhibitory activity simultaneously, sample is evaluated using mtt assay
Cytotoxicity ,-: without obvious cytotoxicity, cell survival rate > 85%；+: weak cytotoxicity, 70% < cell survival rate <
85%；++: intermediate cell toxicity, 50% < cell survival rate < 70%；+++ strong cytotoxicity, cell survival rate < 50%；Such as
Sample is because having cytotoxicity to lead to cell death, and the inhibitory activity that measurement result occurs is false positive, therefore in evaluation sample
It should be in conjunction with the cytotoxicity comprehensive descision that sample shows when product Activity Results.Only do not influencing cell normal proliferative
Concentration range in, show to microglia release NO inhibitory activity just there is real meaning.
MTT solution (200 μ g/mL of final concentration) is added in the every hole of above-mentioned culture plate, is placed in 37 DEG C, 5%CO2In incubator
Continue after cultivating 4h, discard supernatant, blot residual liquid, 150 μ L of DMSO is added, shaking 10min fills the first a ceremonial jade-ladle, used in libation generated crystallization
After dividing dissolution, light absorption value is measured at 570nm using 630nm as reference wavelength.Cell survival rate calculation formula are as follows:
Specific experiment result is shown in Table 2:
Table 2 Inhibitory effect of tested compounds on NO production
induced by LPS in microglial cell
* Cell viability is expressed as a percentage (%) of the LPS-only
treatment group.
#Positive control.
The results show that remaining ganoderma lucidum triterpene compounds is to the survival rate of BV-2 microglia without shadow in addition to compound 4
It rings, can preferably inhibit LPS induction BV-2 microglia release NO, wherein 6,11,13,14,17,18,22 table of compound
Reveal significant inhibitory activity, IC5010 μM are below, shows that these compounds are likely to become lead compound.
Claims (1)
1. following compound (6), (11), (18), (22) are in the purposes for preparing treatment nerve retrograde affection drug:
。
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| CN201610378137.XA CN106074566B (en) | 2016-06-02 | 2016-06-02 | The purposes of ganoderma lucidum triterpene compounds |
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| CN201610378137.XA CN106074566B (en) | 2016-06-02 | 2016-06-02 | The purposes of ganoderma lucidum triterpene compounds |
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| Publication Number | Publication Date |
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| CN106074566B true CN106074566B (en) | 2019-11-12 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018082034A1 (en) * | 2016-11-04 | 2018-05-11 | Trineo Biotechnology Co., Ltd | Uses of triterpenoid mixture for treating multiple sclerosis |
| CN107056867A (en) * | 2017-04-27 | 2017-08-18 | 峨眉山国芝堂生物科技有限公司 | Ganodenic acid compound, its Pharmaceutical composition and its application |
| CN108969526A (en) * | 2018-09-06 | 2018-12-11 | 中国药科大学 | Application of the Lanost-8-en-26-oic acid,3,7,12-trihydroxy-11,15,23-trioxo-,(3BETA,7BETA,12BETA)- in terms of neurodegenerative disease |
| CN115286679B (en) * | 2022-08-18 | 2023-06-02 | 中国科学院昆明植物研究所 | Ganoaplin A and Ganoaplin B, and pharmaceutical composition and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105050609A (en) * | 2012-11-26 | 2015-11-11 | 吴淑芬 | Method and composition for inducing autophagy |
| WO2016062239A1 (en) * | 2014-10-20 | 2016-04-28 | Mycomagic Biotechnology Co., Ltd | New use of immunomodulatory protein from ganoderma in promoting neurite outgrowth |
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2016
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105050609A (en) * | 2012-11-26 | 2015-11-11 | 吴淑芬 | Method and composition for inducing autophagy |
| WO2016062239A1 (en) * | 2014-10-20 | 2016-04-28 | Mycomagic Biotechnology Co., Ltd | New use of immunomodulatory protein from ganoderma in promoting neurite outgrowth |
Non-Patent Citations (1)
| Title |
|---|
| "Ganoderma lucidum Protects Dopaminergic Neuron Degeneration through Inhibition of Microglial Activation";Ruiping Zhang et al.;《Evidence-Based ComplementaryandAlternativeMedicine》;20111231;摘要和第7页左栏倒数第1段-右栏第1段 * |
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