Doxycycline
(Synonyms: 多西环素) 目录号 : GC63621
Doxycycline(多西环素DOX)是一种四环素衍生物的广谱抗生素,通过干扰细菌核糖体30S亚基A位点上活化的氨基酰基tRNA的结合来抑制蛋白质合成。
Cas No.:564-25-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- Datasheet
| Cell experiment [1]: | |
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Cell lines |
MCF-7 and MDA-MB-468 cells |
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Preparation Method |
Cells were seeded in 96-well plates at a density of 5000 cells/well. The cells were incubated with doxycycline at concentrations of 0-250 µM for 72 hours. |
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Reaction Conditions |
0-250 µM; 72h |
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Applications |
Doxycycline inhibits cell viability of breast cancer cells and mammospheres. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice |
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Preparation Method |
Mice were assigned to a sham, Traumatic brain injury (TBI), or TBI with doxycycline arm. A moderate TBI was induced utilizing a controlled cortical impactor. The TBI with doxycycline cohort received a dose of doxycycline (20 mg/kg) 2 hours after injury and every 12 hours until postoperative day (POD) 6. |
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Dosage form |
20 mg/kg; p.o ; 2 times |
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Applications |
Doxycycline treated following mice TBI improved behavioral and motor function. |
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References: [1]. Zhang L, Xu L, et,al. Doxycycline inhibits the cancer stem cell phenotype and epithelial-to-mesenchymal transition in breast cancer. Cell Cycle. 2017 Apr 18;16(8):737-745. doi: 10.1080/15384101.2016.1241929. Epub 2016 Oct 18. PMID: 27753527; PMCID: PMC5405729. |
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Doxycycline is a tetracycline-derivative wide-spectrum antibiotic, inhibit protein synthesis by interfering with the binding of activated aminoacyl-tRNAs on the A-site of the 30S subunit of bacterial ribosomes. It is used to treat a variety of infections caused by bacteria and protozoa. Doxycycline is also a nonspecific matrix metalloproteinase (MMP) inhibitor. Doxycycline exhibits anti-tumour and pro-apoptotic activity [1-4].
Doxycycline(0-250 µM; 72h) inhibits cell viability of breast cancer cells and mammospheres[5]. Doxycycline (100 ng/mL, 1 µg/mL; 24 h) reduces proliferation of human cell lines[6].
Doxycycline(20mg /kg; p.o.;2times) treated following mice TBI improved behavioral and motor function suggesting doxycycline's role in preserving murine BBB integrity[7]. Doxycycline(DOX in drinking water (6 mg/ml, 5 ml/day/mice) ; 36 days) significantly minimized the dystrophic phenotype of skeletal and cardiac muscles and improved forelimb muscle strength[8]. The FM(fecal microbiota) of female C57BL/6NCrl mice is significantly altered by administration of doxycycline(doxycycline in the drinking water at 2 mg/ml during weeks 1, 2, and 4) at a concentration of 2 mg/ml in the drinking water[9].
References:
[1]. Cunha BA, Sibley CM, et,al. Doxycycline. Ther Drug Monit. 1982;4(2):115-35. doi: 10.1097/00007691-198206000-00001. PMID: 7048645.
[2].Manchado E, Weissmueller S, et,al. A combinatorial strategy for treating KRAS-mutant lung cancer. Nature. 2016 Jun 30;534(7609):647-51. doi: 10.1038/nature18600. Epub 2016 Jun 22. PMID: 27338794; PMCID: PMC4939262.
[3].Luger AL, Sauer B, et,al. Doxycycline Impairs Mitochondrial Function and Protects Human Glioma Cells from Hypoxia-Induced Cell Death: Implications of Using Tet-Inducible Systems. Int J Mol Sci. 2018 May 17;19(5):1504. doi: 10.3390/ijms19051504. PMID: 29772845; PMCID: PMC5983704.
[4]. Duivenvoorden WC, Popović SV, et,al. Doxycycline decreases tumor burden in a bone metastasis model of human breast cancer. Cancer Res. 2002 Mar 15;62(6):1588-91. PMID: 11912125.
[5]. Zhang L, Xu L, et,al. Doxycycline inhibits the cancer stem cell phenotype and epithelial-to-mesenchymal transition in breast cancer. Cell Cycle. 2017 Apr 18;16(8):737-745. doi: 10.1080/15384101.2016.1241929. Epub 2016 Oct 18. PMID: 27753527; PMCID: PMC5405729.
[6]. Ahler E, Sullivan WJ, et,al. Doxycycline alters metabolism and proliferation of human cell lines. PLoS One. 2013 May 31;8(5):e64561. doi: 10.1371/journal.pone.0064561. PMID: 23741339; PMCID: PMC3669316.
[7]. Malek AJ, Robinson BD, et,al. Doxycycline improves traumatic brain injury outcomes in a murine survival model. J Trauma Acute Care Surg. 2020 Sep;89(3):435-440. doi: 10.1097/TA.0000000000002801. PMID: 32467458.
[8]. Pereira JA, Taniguti AP, et,al. Doxycycline ameliorates the dystrophic phenotype of skeletal and cardiac muscles in mdx mice. Muscle Nerve. 2012 Sep;46(3):400-6. doi: 10.1002/mus.23331. PMID: 22907231.
[9]. Boynton FDD, Ericsson AC, et,al. Doxycycline induces dysbiosis in female C57BL/6NCrl mice. BMC Res Notes. 2017 Nov 29;10(1):644. doi: 10.1186/s13104-017-2960-7. PMID: 29187243; PMCID: PMC5708113.
Doxycycline(多西环素DOX)是一种四环素衍生物的广谱抗生素,通过干扰细菌核糖体30S亚基A位点上活化的氨基酰基tRNA的结合来抑制蛋白质合成。它被用来治疗由细菌和原生动物引起的各种感染。Doxycycline也是一种非特异性基质金属蛋白酶(MMP)抑制剂。Doxycycline具有抗肿瘤和促细胞凋亡活性[1-4]。
Doxycycline (0 - 250µM;72h)抑制乳腺癌细胞和乳腺球细胞活力[5]。Doxycycline (100 ng/mL, 1µg/mL;24 h)降低人细胞系的增殖[6]。Doxycycline (100 ng/mL, 1 µg/mL; 24 h)减少人类细胞系的增殖[7]。
Doxycycline (20mg /kg; p.o.;2times) 在小鼠脑外伤后改善了行为和运动功能,Doxycycline在保护小鼠血脑屏障完整性方面有效[8]。Doxycycline (DOX in drinking water (6 mg/ml, 5 ml/day/mice) ; 36 days)显著减少了骨骼肌和心肌的营养不良表型,并改善了前肢肌肉力量[9]。雌性C57BL/6NCrl小鼠的FM(粪便微生物群)在给予Doxycycline (doxycycline in the drinking water at 2 mg/ml during weeks 1, 2, and 4)后显著改变[10]。
| Cas No. | 564-25-0 | SDF | |
| 别名 | 多西环素 | ||
| 分子式 | C22H24N2O8 | 分子量 | 444.43 |
| 溶解度 | DMSO : 125 mg/mL (281.26 mM; Need ultrasonic) | 储存条件 | Store at 4°C, protect from light, stored under argon |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2501 mL | 11.2504 mL | 22.5007 mL |
| 5 mM | 0.45 mL | 2.2501 mL | 4.5001 mL |
| 10 mM | 0.225 mL | 1.125 mL | 2.2501 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Minocycline and Doxycycline: More Than Antibiotics
Curr Mol Pharmacol 2021;14(6):1046-1065.PMID:33568043DOI:10.2174/1874467214666210210122628.
Minocycline and Doxycycline both are second-generation tetracycline antibiotics with similar chemical structures and comparable antibacterial spectrum. Minocycline has also emerged as the tetracycline of choice for multidrug-resistant Acinetobacter baumannii infections, although Doxycycline has also shown the activity. Minocycline showed promising results in experimental neurology, which was due to its highly lipophilic nature. It is clinically safe and effective adjunct to antipsychotic medications. The objective of the current review is to provide clinical and preclinical, non-antibiotic uses of minocycline as well as Doxycycline. Relevant literature covers antibiotic actions but is more specifically concerned with the non-antibiotic biological aspect of tetracyclines. Non-antibiotic biological effects for both the antibiotics were identified through searching relevant databases including: PubMed, Scopus, and Web of Science up to 2020, using the keywords 'minocycline and Doxycycline'. Anti-inflammatory, anti-oxidant, anti-apoptotic neuroprotective, immunomodulatory and the number of other non-antibiotic effects were compiled for minocycline and Doxycycline.
Doxycycline
Ther Drug Monit 1982;4(2):115-35.PMID:7048645DOI:10.1097/00007691-198206000-00001.
The chemistry, mode of action, antimicrobial activity, pharmacokinetics, and therapeutic efficacy of Doxycycline are reviewed. Doxycycline displays excellent activity against gram-positive and gram-negative aerobic and anaerobic pathogens. The oral absorption of Doxycycline is rapid and virtually complete and is not significantly decreased by food. Moreover, serum concentrations of Doxycycline following oral and intravenous (i.v.) administration are comparable. Because of the prolonged half-life of Doxycycline, once daily administration is possible. Tissue penetration of Doxycycline is excellent. Levels within the therapeutic range have been found in most organs and tissues, including kidney, lung, gallbladder, prostate, intestinal tract, myocardium, sinus secretions, tonsil, aqueous humor, and female reproductive tissue. Doxycycline does not accumulate in patients with renal insufficiency and is not removed from the blood to any great extent during hemodialysis. Extensive clinical investigation has shown Doxycycline to be highly effective in infections of the respiratory tract, including atypical pneumonias; skin and soft tissue; genitourinary infection including gonorrhea, syphilis, nonspecific urethritis, and prostatitis; intraabdominal infection due to trauma, sepsis, or surgery; and cholera. Evidence also suggests that Doxycycline will prove effective in the treatment of Legionnaires' disease. In addition, placebo-controlled clinical trials suggest Doxycycline is effective in the prevention of traveler's diarrhea.
Doxycycline, salinomycin, monensin and ivermectin repositioned as cancer drugs
Bioorg Med Chem Lett 2019 Jul 1;29(13):1549-1554.PMID:31054863DOI:10.1016/j.bmcl.2019.04.045.
Chemotherapy is one of the standard methods for the treatment of malignant tumors. It aims to cause lethal damage to cellular structures, mainly DNA. Noteworthy, in recent years discoveries of novel anticancer agents from well-known antibiotics have opened up new treatment pathways for several cancer diseases. The aim of this review article is to describe new applications for the following antibiotics: Doxycycline (DOX), salinomycin (SAL), monensin (MON) and ivermectin (IVR) as they are known to show anti-tumor activity, but have not yet been introduced into standard oncological therapy. To date, these agents have been used for the treatment of a broad-spectrum of bacterial and parasitic infectious diseases and are widely available, which is why they were selected. The data presented here clearly show that the antibiotics mentioned above should be recognised in the near future as novel agents able to eradicate cancer cells and cancer stem cells (CSCs) across several cancer types.
[Doxycycline]
Ann Dermatol Venereol 2002 Jun-Jul;129(6-7):874-82.PMID:12218915doi
Doxycyclin is a semi-synthetic structural isomer of the tetracycline family. It exhibits good intra-cellular penetration, with bacteriostatic activity on many bacteria. Different types or bacterial resistance are known. Acquired resistance has a ribosomal or a plasmidic mechanism. Resistance of Propionibacterium acnes is secondary to a mutation of ARNr. Doxycyclin also has an anti-inflammatory activity, via numerous pathways. Doxycyclin is rapidly and almost completely absorbed by the digestive tract. Food has no incidence on the absorption. It has a high but labile affinity for proteins with 90 p. 100 of the molecule linked. It rapidly diffuses in the extravascular compartment and in most of the tissues. Bile excretion is the main excretion route. It occurs more slowly by the kidney with tubular reabsorption. The main dermatological indication is acne with daily dose varing between 50 mg and 100 mg. Although good assays are lacking, a large professional consensus has validated its use. It is also active at the same dosage in rosacea. Chlamydial and mycoplasma urethritis may be treated by doxycyclin, and this antibiotic is presently used as second choice. Many other diseases may be treated as a primary or secondary choice, such as treponematoses, brucellosis, pasteurellosis, borreliosis, rickettsioses and cholera. Some non infectious diseases have been occasionally treated by Doxycycline. Digestive side effects are the more frequent. Esophageal toxicity has been reduced with tablets and sufficient concomitant water ingestion. Phototoxicity is dose-dependent. Various cutaneous side effects have been described, some of them severe. Systemic toxicity is rare. Pregnancy is a contra-indication, and as other tetracyclines, it should not be given to children and during lactation. Doxycycline is commercialized as tablets. No reduction of the dose is necessary in renal failure. Association with retinoids is not recommended. Anticoagulants are potentialized. Didanosin, iron, and mineral salts lower its activity.
Doxycycline: An option in the treatment of ulcerated oral lesions?
J Clin Pharm Ther 2019 Dec;44(6):838-843.PMID:31400293DOI:10.1111/jcpt.13022.
What is known and objectives: In addition to its antimicrobial effect, Doxycycline has potent anti-inflammatory activity. In view of these pharmacological characteristics, its use in the management of inflammatory, autoimmune and granulomatous diseases has been proposed. The objective of this study was to investigate, through a systematic literature review, the effect of Doxycycline on pain and healing of ulcerated lesions of the mouth. Methods: An electronic search was performed in accordance with PRISMA guidelines in PubMed, Cochrane Central Register, Web of Science, Bireme/LILACS and Scopus databases. Controlled, randomized clinical trials were selected. The concentration of Doxycycline, frequency of application, pain relief and clinical remission of the lesions were analysed. Results and discussion: According to the inclusion criteria, five articles were selected. In four of these studies, Doxycycline was used in the treatment of aphthous stomatitis, and in one study, it was used in the treatment of herpes labialis. In all studies, the drug was used topically, both as a hydrogel and as a crushed tablet (along with a prosthetic adhesive). The groups treated with Doxycycline showed faster healing of lesions and lower pain scores compared to placebo. What is new and conclusion: The present study suggests that topical Doxycycline has a positive effect on the treatment of recurrent aphthous ulceration and herpes labialis. Experimental animal studies and double-blind randomized clinical trials should be performed on other oral lesions, such as traumatic ulcers and mucositis.