Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples
Background. Local anesthetics (LAs) have potent anti-inflammatory properties. Inflammatory down-regulation is crucial in diseases with overactive immune reactions, such as acute respiratory distress syndrome (ARDS) and chronic inflammation. We investigated the influence of four LAs, procaine, lidoca...
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| Format: | Article |
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MDPI AG
2022-03-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/23/6/3283 |
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| author | Stefan Weinschenk Carsten Weiss Justus Benrath Volker von Baehr Thomas Strowitzki Manuel Feißt |
| author_facet | Stefan Weinschenk Carsten Weiss Justus Benrath Volker von Baehr Thomas Strowitzki Manuel Feißt |
| author_sort | Stefan Weinschenk |
| collection | DOAJ |
| description | Background. Local anesthetics (LAs) have potent anti-inflammatory properties. Inflammatory down-regulation is crucial in diseases with overactive immune reactions, such as acute respiratory distress syndrome (ARDS) and chronic inflammation. We investigated the influence of four LAs, procaine, lidocaine, mepivacaine, and bupivacaine, on the reduction of tumor necrosis factor-alpha (TNF-α) secretion in lipopolysaccharide (LPS)-activated human leucocytes. Methods. Blood samples of 28 individuals were stimulated with LPS. The reduction of TNF-α production by each of the four LAs added (0.5 mg/mL) was measured and correlated with biometric variables. A response was defined as reduction to <85% of initial levels. Results. All four LAs down-regulated the TNF-α secretion in 44–61%: Bupivacaine (44.4%), lidocaine (61.5%), mepivacaine (44.4%), and procaine (50% of the individuals, “responders”). The TNF-α secretion was reduced to 67.4, 68.0, 63.6, and 67.1% of the initial values in responders. The effects in both patients and healthy persons were the same. Interindividual responses to LAs were not correlated with the duration or type of complaints, basal TNF-α serum level, sex, BMI, or age of responders. Conclusions. Four clinically relevant LAs (amid-LA and ester-LA) attenuate the inflammatory response provoked by LPS. They are potential candidates for drug repositioning in treating overactive immune reactions and chronic inflammation. |
| first_indexed | 2024-03-09T19:41:08Z |
| format | Article |
| id | doaj.art-2881ed3f99a149419bd5ebda31710b7b |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T19:41:08Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-2881ed3f99a149419bd5ebda31710b7b2023-11-24T01:36:30ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-03-01236328310.3390/ijms23063283Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood SamplesStefan Weinschenk0Carsten Weiss1Justus Benrath2Volker von Baehr3Thomas Strowitzki4Manuel Feißt5Department of Gynecological Endocrinology and Fertility Disorders, Women’s Hospital, University of Heidelberg, D-69120 Heidelberg, GermanyInstitute of Biological and Chemical Systems, Biological Information Processing, Karlsruhe Institute of Technology (KIT), Campus North, D-76133 Karlsruhe, GermanyPain Clinic, Mannheim University Hospital, Faculty of Heidelberg University, D-68167 Mannheim, GermanyInstitute of Medical Diagnostics, Nicolaistraße 22, D-12247 Berlin, GermanyDepartment of Gynecological Endocrinology and Fertility Disorders, Women’s Hospital, University of Heidelberg, D-69120 Heidelberg, GermanyInstitute of Medical Biometry (IMBI), Heidelberg University, Im Neuenheimer Feld 130.3, D-69120 Heidelberg, GermanyBackground. Local anesthetics (LAs) have potent anti-inflammatory properties. Inflammatory down-regulation is crucial in diseases with overactive immune reactions, such as acute respiratory distress syndrome (ARDS) and chronic inflammation. We investigated the influence of four LAs, procaine, lidocaine, mepivacaine, and bupivacaine, on the reduction of tumor necrosis factor-alpha (TNF-α) secretion in lipopolysaccharide (LPS)-activated human leucocytes. Methods. Blood samples of 28 individuals were stimulated with LPS. The reduction of TNF-α production by each of the four LAs added (0.5 mg/mL) was measured and correlated with biometric variables. A response was defined as reduction to <85% of initial levels. Results. All four LAs down-regulated the TNF-α secretion in 44–61%: Bupivacaine (44.4%), lidocaine (61.5%), mepivacaine (44.4%), and procaine (50% of the individuals, “responders”). The TNF-α secretion was reduced to 67.4, 68.0, 63.6, and 67.1% of the initial values in responders. The effects in both patients and healthy persons were the same. Interindividual responses to LAs were not correlated with the duration or type of complaints, basal TNF-α serum level, sex, BMI, or age of responders. Conclusions. Four clinically relevant LAs (amid-LA and ester-LA) attenuate the inflammatory response provoked by LPS. They are potential candidates for drug repositioning in treating overactive immune reactions and chronic inflammation.https://www.mdpi.com/1422-0067/23/6/3283clinical studycytokineslocal anestheticsLPSneural therapytumor necrosis factor-alpha |
| spellingShingle | Stefan Weinschenk Carsten Weiss Justus Benrath Volker von Baehr Thomas Strowitzki Manuel Feißt Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples International Journal of Molecular Sciences clinical study cytokines local anesthetics LPS neural therapy tumor necrosis factor-alpha |
| title | Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples |
| title_full | Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples |
| title_fullStr | Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples |
| title_full_unstemmed | Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples |
| title_short | Anti-Inflammatory Characteristics of Local Anesthetics: Inhibition of TNF-α Secretion of Lipopolysaccharide-Stimulated Leucocytes in Human Blood Samples |
| title_sort | anti inflammatory characteristics of local anesthetics inhibition of tnf α secretion of lipopolysaccharide stimulated leucocytes in human blood samples |
| topic | clinical study cytokines local anesthetics LPS neural therapy tumor necrosis factor-alpha |
| url | https://www.mdpi.com/1422-0067/23/6/3283 |
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