CN111773202A - Medical application of dendrophenol and anti-propionibacterium acnes medicine - Google Patents
Medical application of dendrophenol and anti-propionibacterium acnes medicine Download PDFInfo
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- CN111773202A CN111773202A CN202010794889.0A CN202010794889A CN111773202A CN 111773202 A CN111773202 A CN 111773202A CN 202010794889 A CN202010794889 A CN 202010794889A CN 111773202 A CN111773202 A CN 111773202A
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- dendrophenol
- propionibacterium acnes
- medicine
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- YTRAYUIKLRABOQ-UHFFFAOYSA-N 4-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-2,6-dimethoxyphenol Chemical compound C1=C(O)C(OC)=CC(CCC=2C=C(OC)C(O)=C(OC)C=2)=C1 YTRAYUIKLRABOQ-UHFFFAOYSA-N 0.000 title claims abstract description 34
- NRPAEDCATWOFMY-UHFFFAOYSA-N dendrophenol Natural products COc1cc(CCc2ccc(O)c(O)c2)cc(OC)c1O NRPAEDCATWOFMY-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 239000003814 drug Substances 0.000 title claims abstract description 26
- 229940055019 propionibacterium acne Drugs 0.000 title claims abstract description 25
- 241000186427 Cutibacterium acnes Species 0.000 claims abstract description 21
- 238000002360 preparation method Methods 0.000 claims abstract description 3
- 241000588724 Escherichia coli Species 0.000 claims description 11
- 241000191967 Staphylococcus aureus Species 0.000 claims description 11
- 229940079593 drug Drugs 0.000 claims description 8
- 230000002401 inhibitory effect Effects 0.000 claims description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 3
- 239000000463 material Substances 0.000 claims description 3
- 229940124350 antibacterial drug Drugs 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 206010059866 Drug resistance Diseases 0.000 abstract description 3
- 230000003115 biocidal effect Effects 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 208000015181 infectious disease Diseases 0.000 abstract description 2
- 231100000331 toxic Toxicity 0.000 abstract description 2
- 230000002588 toxic effect Effects 0.000 abstract description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 12
- 241000894006 Bacteria Species 0.000 description 5
- 230000003385 bacteriostatic effect Effects 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 5
- 239000001963 growth medium Substances 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 206010000496 acne Diseases 0.000 description 4
- SDXKZPQOVUDXIY-UHFFFAOYSA-N 5-[2-(3-hydroxy-5-methoxyphenyl)ethyl]-2-methoxyphenol Chemical compound COC1=CC(O)=CC(CCC=2C=C(O)C(OC)=CC=2)=C1 SDXKZPQOVUDXIY-UHFFFAOYSA-N 0.000 description 3
- 208000002874 Acne Vulgaris Diseases 0.000 description 3
- 230000003255 anti-acne Effects 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 229920001817 Agar Polymers 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 241000186429 Propionibacterium Species 0.000 description 2
- 239000008272 agar Substances 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 238000009630 liquid culture Methods 0.000 description 2
- 239000012452 mother liquor Substances 0.000 description 2
- 235000013824 polyphenols Nutrition 0.000 description 2
- 210000003491 skin Anatomy 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- BMSPEISBKGSBTR-UHFFFAOYSA-N 3',4-Dihydroxy-3,5'-dimethoxybibenzyl Natural products COC1=CC(O)=CC(CCC=2C=C(OC)C(O)=CC=2)=C1 BMSPEISBKGSBTR-UHFFFAOYSA-N 0.000 description 1
- 229920000742 Cotton Polymers 0.000 description 1
- 206010011732 Cyst Diseases 0.000 description 1
- 241001523681 Dendrobium Species 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 102000009571 Macrophage Inflammatory Proteins Human genes 0.000 description 1
- 108010009474 Macrophage Inflammatory Proteins Proteins 0.000 description 1
- 102000003945 NF-kappa B Human genes 0.000 description 1
- 108010057466 NF-kappa B Proteins 0.000 description 1
- 206010033733 Papule Diseases 0.000 description 1
- 206010037888 Rash pustular Diseases 0.000 description 1
- 241000191940 Staphylococcus Species 0.000 description 1
- 208000031320 Teratogenesis Diseases 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 208000037887 cell injury Diseases 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 238000012258 culturing Methods 0.000 description 1
- 208000031513 cyst Diseases 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 238000013118 diabetic mouse model Methods 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000007865 diluting Methods 0.000 description 1
- 238000003113 dilution method Methods 0.000 description 1
- 238000007598 dipping method Methods 0.000 description 1
- 210000002889 endothelial cell Anatomy 0.000 description 1
- 239000002158 endotoxin Substances 0.000 description 1
- 235000021588 free fatty acids Nutrition 0.000 description 1
- 210000003780 hair follicle Anatomy 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 229920006008 lipopolysaccharide Polymers 0.000 description 1
- 210000003584 mesangial cell Anatomy 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000004925 microvascular endothelial cell Anatomy 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 150000008442 polyphenolic compounds Chemical class 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 208000029561 pustule Diseases 0.000 description 1
- 239000003642 reactive oxygen metabolite Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000002207 retinal effect Effects 0.000 description 1
- 150000004508 retinoic acid derivatives Chemical class 0.000 description 1
- 235000003441 saturated fatty acids Nutrition 0.000 description 1
- 150000004671 saturated fatty acids Chemical class 0.000 description 1
- 231100000241 scar Toxicity 0.000 description 1
- 210000001732 sebaceous gland Anatomy 0.000 description 1
- 210000002374 sebum Anatomy 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000000451 tissue damage Effects 0.000 description 1
- 231100000827 tissue damage Toxicity 0.000 description 1
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Classifications
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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
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a medicinal application of dendrophenol and a medicine for resisting propionibacterium acnes, wherein the dendrophenol is applied to the preparation of the medicine for resisting propionibacterium acnes, has no toxic or side effect on a human body, can be used as a conventional antibiotic medicine which is easy to relapse infection and generate drug resistance after replacement treatment in some aspects to become a clinically preferred medicine for resisting propionibacterium acnes, and has great application prospect.
Description
Technical Field
The invention relates to a medical application of dendrophenol and a medicine for resisting propionibacterium acnes, belonging to the technical field of medical biology.
Background
Currently, dendrophenol (Gigantol, CAS: 67884-30-4), a bibenzyl phenolic substance, is extracted from the root of dendrobe and is one of the medicinal effective components of dendrobe. The dendrophenol can inhibit the release of macrophage inflammatory factors of mice induced by bacterial lipopolysaccharide through a nuclear transcription factor NF-kB approach, and reduce the apoptosis of glomerular mesangial cells of the mice induced by high glucose. In a high-glucose-induced human retinal microvascular endothelial cell injury model, dendrophenol is found to reduce intracellular reactive oxygen species levels to protect injured endothelial cells. In a diabetic mouse model, the dendrobium polyphenol extract can play a role in resisting diabetes and complications by regulating the abundance of intestinal flora.
Acne is a common chronic inflammatory disease of hair follicles and sebaceous glands caused by various factors, and clinically appears as comedo, papule, pustule, nodule, cyst, scar and the like. Propionibacterium acnes is an anaerobic gram-positive bacterium that is considered to be the major pathogenic bacterium of acne. When sebum secretion is excessive or pores are blocked due to various reasons, propionibacterium acnes rapidly proliferate, which can decompose saturated fatty acids to produce a large amount of free fatty acids, thereby causing skin stress reactions, and bacteria such as staphylococcus can further aggravate skin tissue damage. The existing external medicine for treating acne comprises antibiotics and vitamin A acids, wherein the former has the problem of easy generation of drug resistance and the like, and the latter has certain irritation and potential teratogenesis risk, so that the exploration of external anti-acne medicines which have good safety and are difficult to resist drugs is particularly urgent.
Disclosure of Invention
The invention aims to overcome the defects of the prior art and provides the medical application of the dendrophenol, which is applied to the preparation of the anti-propionibacterium acnes medicine, has no toxic or side effect on a human body, can be used as a conventional antibiotic medicine for replacing easily relapsing infection and easily generating drug resistance after treatment to become a clinically preferred anti-propionibacterium acnes medicine in some aspects, and has great application prospect.
In order to solve the technical problems, the technical scheme of the invention is as follows: a medicinal application of dendrophenol in preparing medicine for resisting Propionibacterium acnes is disclosed.
Further, it is used for inhibiting Staphylococcus aureus.
Further, it is used for inhibiting Escherichia coli.
The invention also provides a medicine for resisting the propionibacterium acnes, which comprises dendrophenol.
Furthermore, the anti-acne propionibacterium medicine is a dosage form prepared from dendrophenol and pharmaceutically acceptable auxiliary materials or excipients.
Furthermore, the anti-acne propionibacterium drug is a dosage form prepared by taking dendrophenol as an effective component and adding a bacteria inhibiting drug component and pharmaceutically acceptable auxiliary materials or excipients.
After the technical scheme is adopted, the dendrophenol has obvious antibacterial and bacteriostatic effects on propionibacterium acnes, staphylococcus aureus and escherichia coli, and can be used for preparing corresponding antibacterial drugs.
Drawings
FIG. 1 is a graph showing the results of the control group and the dendrobe phenol group for the respective bacteriostatic ring radii of Propionibacterium acnes, Staphylococcus aureus, or Escherichia coli; wherein,* P<0.05 compared to control group;
FIG. 2: dendrophenol Minimum Inhibitory Concentration (MIC) determination result graph.
Detailed Description
In order that the present invention may be more readily and clearly understood, a more particular description of the invention briefly described above will be rendered by reference to specific embodiments that are illustrated in the appended drawings.
Example 1: and (5) bacteriostatic ring experiment.
Preparing the medicine: dissolving dendrophenol by DMSO to prepare mother liquor with the concentration of 160 mg/mL. In the experiment, the dendrophenol mother liquor is diluted by 4 times of a sterile liquid culture medium to prepare the dendrophenol experiment concentration (40 mg/mL).
The experimental method comprises the following steps: measuring by agar diffusion method, taking a plate with diameter of 12 cm, adding 10 mL of culture medium, condensing, respectively dipping different bacteria solutions (Propionibacterium acnes, Staphylococcus aureus or Escherichia coli) with sterile cotton swab, uniformly coating on the surface of the culture medium, and standing at room temperature for 3-5 min. Sterile Oxford cups with a diameter of 6 mm were placed on an agar plate, 50. mu.L of dendrophenol at a concentration of 40 mg/mL was added to the cups, and DMSO (25%) was used as control wells, 3 controls were repeated for each condition. The diameter of the zone of inhibition was measured after 24h incubation at 37 ℃.
The experimental results are as follows: as shown in figure 1, dendrophenol significantly increased the bacteriostatic ring radius of Propionibacterium acnes, Staphylococcus aureus, or Escherichia coli (DMSO) compared to control group (DMSO) ((P<0.05). The dendrophenol can obviously inhibit the in vitro growth of propionibacterium acnes, staphylococcus aureus or escherichia coli, and has obvious antibacterial activity.
Example 2: minimum Inhibitory Concentration (MIC) assay.
The experimental method comprises the following steps: the liquid dilution method is used for measuring, and a culture medium control hole, a bacteria liquid control hole (propionibacterium acnes, staphylococcus aureus or escherichia coli) and a dendrophenol liquid medicine control hole are arranged in a 96-hole cell culture plate. Diluting dendrophenol (with concentration of 40 mg/mL-1.25 mg/mL) with liquid culture medium at equal times, adding 100 μ L of diluted dendrophenol liquid and 10 μ L of test bacterial liquid (Propionibacterium acnes, Staphylococcus aureus or Escherichia coli) into each well, culturing at 37 deg.C for 24h, and detecting absorbance (OD) value of 600 nm wavelength of each well by MTT method. The critical drug concentration before the sudden increase of the OD value is taken as the Minimum Inhibitory Concentration (MIC) of the drug.
The experimental results are as follows: as shown in figure 2, the MICs of dendrophenol to Propionibacterium acnes and Escherichia coli were both 10 mg/mL, and the MICs of dendrophenol to Staphylococcus aureus were both 20 mg/mL. The results show that the dendrophenol has obvious antibacterial and bacteriostatic effects on propionibacterium acnes, staphylococcus aureus and escherichia coli.
The above embodiments are described in further detail to solve the technical problems, technical solutions and advantages of the present invention, and it should be understood that the above embodiments are only examples of the present invention and are not intended to limit the present invention, and any modifications, equivalent substitutions, improvements and the like made within the spirit and principle of the present invention should be included in the protection scope of the present invention.
Claims (6)
1. The medical application of dendrophenol is characterized in that dendrophenol is applied to preparation of a medicine for resisting propionibacterium acnes.
2. The pharmaceutical use of dendrophenol according to claim 1, for inhibiting staphylococcus aureus.
3. The pharmaceutical use of dendrophenol of claim 1, in inhibiting escherichia coli.
4. A medicine for resisting propionibacterium acnes is characterized by comprising dendrophenol.
5. The drug against propionibacterium acnes according to claim 4, which is a formulation prepared from dendrophenol and pharmaceutically acceptable adjuvants or excipients.
6. The drug for resisting propionibacterium acnes according to claim 4, which is a dosage form prepared by adding an antibacterial drug component and pharmaceutically acceptable auxiliary materials or excipients into dendrophenol serving as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010794889.0A CN111773202B (en) | 2020-08-10 | 2020-08-10 | Medical application of dendrophenol and anti-propionibacterium acnes medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010794889.0A CN111773202B (en) | 2020-08-10 | 2020-08-10 | Medical application of dendrophenol and anti-propionibacterium acnes medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111773202A true CN111773202A (en) | 2020-10-16 |
| CN111773202B CN111773202B (en) | 2022-06-17 |
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| CN202010794889.0A Active CN111773202B (en) | 2020-08-10 | 2020-08-10 | Medical application of dendrophenol and anti-propionibacterium acnes medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114903907A (en) * | 2022-05-31 | 2022-08-16 | 合肥师范学院 | Application of arenobufagin and derivatives thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140288186A1 (en) * | 2013-03-19 | 2014-09-25 | Tunghai University | Method for lowering blood glucose and method for treating hepatic disease, obesity and diabetes |
| CN107308141A (en) * | 2017-05-31 | 2017-11-03 | 合肥师范学院 | Application of the dendrophnol and combinations thereof in prevention and treatment atherosclerosis medicine is prepared |
| CN110302080A (en) * | 2019-07-24 | 2019-10-08 | 汉义生物科技（北京）有限公司 | Hemp compounds Herba Dendrobii extract and its preparation method and application |
-
2020
- 2020-08-10 CN CN202010794889.0A patent/CN111773202B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140288186A1 (en) * | 2013-03-19 | 2014-09-25 | Tunghai University | Method for lowering blood glucose and method for treating hepatic disease, obesity and diabetes |
| CN107308141A (en) * | 2017-05-31 | 2017-11-03 | 合肥师范学院 | Application of the dendrophnol and combinations thereof in prevention and treatment atherosclerosis medicine is prepared |
| CN110302080A (en) * | 2019-07-24 | 2019-10-08 | 汉义生物科技（北京）有限公司 | Hemp compounds Herba Dendrobii extract and its preparation method and application |
Non-Patent Citations (3)
| Title |
|---|
| CHEN M ET AL: "Gigantol has Protective Effects against High Glucose-Evoked Nephrotoxicity in Mouse Glomerulus Mesangial Cells by Suppressing ROS/MAPK/NF-κB Signaling Pathways", 《MOLECULES》 * |
| 张帮磊 等: "铁皮石斛化学成分及其药理功效研究进展", 《临床医药文献电子杂志》 * |
| 张薇薇 等: "叠鞘石斛水提取物对小肠结肠炎耶尔森菌的抗菌活性及机制研究", 《现代预防医学》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114903907A (en) * | 2022-05-31 | 2022-08-16 | 合肥师范学院 | Application of arenobufagin and derivatives thereof |
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| CN111773202B (en) | 2022-06-17 |
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