Structure of Colistin sulfate
CAS No.: 1264-72-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Colistin sulfate is a polymyxin antibiotic, a mixture of cyclic polypeptides colistin A and B, effective against most Gram-negative bacilli.
Synonyms: Polymyxin E sulfate; Polymixin E Sulfate
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| CAS No. : | 1264-72-8 |
| SMILES Code : | NONE |
| Synonyms : |
Polymyxin E sulfate; Polymixin E Sulfate
|
| MDL No. : | MFCD00146495 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H302-H315-H319-H335 |
| Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| Acinetobacter baumannii AB5075 | 1.22 μg/mL | 12 h | To evaluate the potentiating effect of kaempferol on colistin activity, results showed complete inhibition of bacterial growth when 0.375 mM kaempferol was combined with sub-MIC colistin | Commun Biol. 2023 Sep 13;6(1):937. |
| P. aeruginosa 41782/98 | 1 μg/mL | 24 h | Tested susceptibility of Colistin-resistant strain to combination therapy, revealing Colistin's role in disrupting outer membrane for Rifampicin penetration. | Antimicrob Agents Chemother. 2023 Apr 18;67(4):e0164122. |
| P. aeruginosa 19848/85 | 0.25 μg/mL | 24 h | Evaluated killing kinetics of Colistin on clinical isolates, demonstrating synergistic bactericidal activity with Rifampicin. | Antimicrob Agents Chemother. 2023 Apr 18;67(4):e0164122. |
| P. aeruginosa PAO1 | 0.25 μg/mL | 24 h | Investigated bactericidal effects of Colistin alone and combined with Rifampicin on planktonic P. aeruginosa, showing complete eradication of susceptible strains with combination therapy. | Antimicrob Agents Chemother. 2023 Apr 18;67(4):e0164122. |
| E. cloacae D01 | 2 μg/ml | 24 h | Evaluate the synergistic bactericidal effect of Colistin with PFK-158, results showed continuous bacterial elimination within 24 h | Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00271-19. |
| K. pneumoniae H04 | 2 μg/ml | 24 h | Evaluate the synergistic bactericidal effect of Colistin with PFK-158, results showed continuous bacterial elimination within 24 h | Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00271-19. |
| E. coli 13-43 | 2 μg/ml | 24 h | Evaluate the synergistic bactericidal effect of Colistin with PFK-158, results showed continuous bacterial elimination within 24 h | Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00271-19. |
| Vero cells (monkey kidney epithelial cells) | 1 mg/ml | 24 h | Evaluate cytotoxicity of Colistin, found that combination with Nisin A (2 mg/ml) abolished toxicity | Antimicrob Agents Chemother. 2013 Jun;57(6):2719-25. |
| human peripheral blood leukocytes (PBLs) | 550 ng/ml | 1 h | Assess DNA damage caused by Colistin, observed tail extensions of about 69.29μm | Antimicrob Agents Chemother. 2013 Jun;57(6):2719-25. |
| Klebsiella pneumoniae FADDI-KP035 | 5 mg/L | 72 h | Evaluate the bactericidal effect of Colistin monotherapy against K. pneumoniae FADDI-KP035. Results showed no efficacy against the resistant strain. | Antimicrob Agents Chemother. 2012 Oct;56(10):5103-12. |
| Klebsiella pneumoniae FADDI-KP032 | 0.5, 2, 5 mg/L | 72 h | Evaluate the bactericidal effect and resistance development of Colistin monotherapy against K. pneumoniae FADDI-KP032. Results showed rapid bacterial killing at low inoculum but poor efficacy at high inoculum with emergence of resistant subpopulations. | Antimicrob Agents Chemother. 2012 Oct;56(10):5103-12. |
| Klebsiella pneumoniae FADDI-KP033 | 0.5, 2, 5 mg/L | 72 h | Evaluate the bactericidal effect and resistance development of Colistin monotherapy against K. pneumoniae FADDI-KP033. Results showed rapid bacterial killing at low inoculum but poor efficacy at high inoculum with emergence of resistant subpopulations. | Antimicrob Agents Chemother. 2012 Oct;56(10):5103-12. |
| Klebsiella pneumoniae ATCC 13883 | 0.5, 2, 5 mg/L | 72 h | Evaluate the bactericidal effect and resistance development of Colistin monotherapy against K. pneumoniae. Results showed rapid bacterial killing at low inoculum (10^6 CFU/ml) but poor efficacy at high inoculum (10^8 CFU/ml) with emergence of resistant subpopulations. | Antimicrob Agents Chemother. 2012 Oct;56(10):5103-12. |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| NIH mice | Sepsis model | Intraperitoneal injection | 8 mg/kg | Every 12 hours for 48 hours | Evaluate the synergistic antimicrobial effect of Ob with Colistin in vivo against resistant strains, showing the combination successfully rescued 80% of the animals. | Commun Biol. 2022 Jun 21;5(1):613 |
| Galleria mellonella | Infection model | Injection | 0.08 µg/larva | Single dose, observed for 32 hours | To evaluate the in vivo efficacy of kaempferol-colistin combination therapy, results showed significant increase in larval survival | Commun Biol. 2023 Sep 13;6(1):937. |
| ICR mice | Systemic infection model | Intravenous injection | 1.3 mg/kg | Single dose at 1 hour postinfection | Evaluate the in vivo synergistic effect of Colistin with PFK-158, results showed significant improvement in mouse survival rates | Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00271-19. |
| ICR male mice | Subcutaneous biofilm infection model | Intraperitoneal injection | 20 mg/kg | Every 12 hours (COL) or 24 hours (LEV/AMI) for 5 days | Evaluate the efficacy of COL alone and in combination with other antibiotics on PAO1 and CRPAO1 biofilm infections, results showed that COL combined with amikacin significantly shortened biofilm eradication time, superior to monotherapy | Microbiol Spectr. 2022 Oct 26;10(5):e0146822 |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT00826670 | Enterobacteriaceae Infections | Phase 4 | Completed | - | Switzerland ... More >> Geneva Universits Hospitals Geneva, Switzerland, 1211 Less << |
| NCT03397914 | Gram-Negative Bacterial Infect... More >>ions Pediatric Cancer Colistin Colistin Adverse Reaction MIC Less << | Phase 4 | Recruiting | June 2019 | Egypt ... More >> Iman Sidhom Recruiting Cairo, Cairo Governorate, Egypt Contact: Yosr Samia Abou Sedira, BCS 201227531255 yosrsamia@gmail.com Contact: Iman Sidhom, professor imansidhom@yahoo.com Less << |
| NCT02472600 | Intestinal Colonization With M... More >>ultidrug-resistant Bacteria Less << | Phase 2 | Active, not recruiting | March 2018 | France ... More >> Assistance Publique-Hôpitaux de Paris, Hôpital Beaujon Clichy, France, 92110 Israel Sourasky Medical Center Tel Aviv, Israel Netherlands Universitair Medisch Centrum Utrecht, Utrecht, Netherlands Switzerland Geneva University Hospitals Geneva, Switzerland Less << |
| NCT01740947 | Colorectal Cancer | Phase 4 | Terminated(Superiority was no ... More >>longer attainable) Less << | - | Netherlands ... More >> Slotervaart Ziekenhuis Amsterdam, Netherlands VU University Medical Center Amsterdam, Netherlands Kennemer Gasthuis Haarlem, Netherlands Spaarne Ziekenhuis Hoofddorp, Netherlands WestFries Gasthuis Hoorn, Netherlands Less << |
| NCT01798537 | Bacteremia Associated With Int... More >>ravascular Line Ventilator Associated Pneumonia Bacteremia Less << | Phase 2 Phase 3 | Unknown | July 2015 | Israel ... More >> Rambam Health Care Campus Not yet recruiting Haifa, Israel, 31096 Contact: Yaron P Bar-Lavie, M.D. ++972-50-206-2027 y_barlavie@rambam.health.gov.il Contact: Mical Paul, Prof. ++972-50-206-2140 m_paul@rambam.health.gov.il Principal Investigator: Yaron P Bar-Lavie, M.D. Principal Investigator: Mical Paul, Prof. Less << |
| NCT01863719 | Pathogen Resistance ... More >> Pneumococcal Infection Pneumonia Less << | Phase 1 | Terminated(Completion of cohor... More >>t 3, safety concerns) Less << | - | United States, Maryland ... More >> Johns Hopkins Bayview Medical Center - Infectious Diseases Baltimore, Maryland, United States, 21224-2735 United States, Ohio Case Western Reserve University - Case Medical Center - Infectious Disease & HIV Medicine Cleveland, Ohio, United States, 44106-1716 Less << |
Tags: Colistin | Polymyxin E | Colistin sulfate | Polymyxin E sulfate | polymyxin antibiotic | Gram-negative bacteria | lipopolysaccharides | multidrug-resistant infections | antibiotic resistance | nephrotoxicity | neurotoxicity | Bacterial | Autophagy | Antibiotic | 1264-72-8
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Response | |
| Code | Phrase |
| P301 | IF SWALLOWED: |
| P304 | IF INHALED: |
| P305 | IF IN EYES: |
| P306 | IF ON CLOTHING: |
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| P378 | |
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| P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
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| P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
| P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
| P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
| P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
| P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
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| P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
| P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
| P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
| P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
| P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
| P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
| P370 + P376 | In case of fire: Stop leak if safe to Do so. |
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| H200 | Unstable explosive |
| H201 | Explosive; mass explosion hazard |
| H202 | Explosive; severe projection hazard |
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Health hazards | |
| Code | Phrase |
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| H302 | Harmful if swallowed |
| H303 | May be harmful if swallowed |
| H304 | May be fatal if swallowed and enters airways |
| H305 | May be harmful if swallowed and enters airways |
| H310 | Fatal in contact with skin |
| H311 | Toxic in contact with skin |
| H312 | Harmful in contact with skin |
| H313 | May be harmful in contact with skin |
| H314 | Causes severe skin burns and eye damage |
| H315 | Causes skin irritation |
| H316 | Causes mild skin irritation |
| H317 | May cause an allergic skin reaction |
| H318 | Causes serious eye damage |
| H319 | Causes serious eye irritation |
| H320 | Causes eye irritation |
| H330 | Fatal if inhaled |
| H331 | Toxic if inhaled |
| H332 | Harmful if inhaled |
| H333 | May be harmful if inhaled |
| H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
| H335 | May cause respiratory irritation |
| H336 | May cause drowsiness or dizziness |
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| H341 | Suspected of causing genetic defects |
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| H361d | Suspected of damaging the unborn child |
| H362 | May cause harm to breast-fed children |
| H370 | Causes damage to organs |
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| H372 | Causes damage to organs through prolonged or repeated exposure |
| H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
| Code | Phrase |
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| H401 | Toxic to aquatic life |
| H402 | Harmful to aquatic life |
| H410 | Very toxic to aquatic life with long-lasting effects |
| H411 | Toxic to aquatic life with long-lasting effects |
| H412 | Harmful to aquatic life with long-lasting effects |
| H413 | May cause long-lasting harmful effects to aquatic life |
| H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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