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Patrick Diel - One of the best experts on this subject based on the ideXlab platform.
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detection and quantitation of Ecdysterone in human serum by liquid chromatography coupled to tandem mass spectrometry
Steroids, 2020Co-Authors: Gabriella Ambrosio, Patrick Diel, Francesco Botrè, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Jan Felix Joseph, Maria Kristina ParrAbstract:Abstract The polyhydroxylated phytosteroid Ecdysterone is present in various plants (e.g. spinach). It is widely marketed as the active component of dietary supplements, due to its reported health and performance promoting effects. For evaluation of its actual bioavailability, a fast and sensitive method was developed, optimized and validated for human serum. Instrumental analysis was performed utilizing liquid chromatography-tandem mass spectrometry with positive electrospray ionization and acquisition in multiple reaction mode. Solid phase extraction and dilute-and-inject (following protein precipitation) were tested to isolate Ecdysterone from human serum. Both methods were compared in the light of the preset analytical target profile. The limit of detection (LOD) and quantitation (LOQ) for Ecdysterone in human serum after SPE extraction corresponded to 0.06 ng/mL and 0.14 ng/mL, respectively, meeting the requested sensitivity of the method. The assay was linear over the range of 0.10 ng/mL to 20.83 ng/mL. As expected, the sensitivity of the SPE method was better than that of the dilute-and-inject procedure, which did not allow for quantitation of all post administration serum samples. Accuracy (relative error; %) and precision (coefficient of variation; %), were both within acceptance criteria ( The developed method was successfully applied to a ten week intervention study conducted in young men performing regular resistance training. Different doses of supplements containing Ecdysterone from spinach extract have been administered during the study and the quantitation of Ecdysterone in serum samples has been successfully conducted. Ecdysterone could be quantified in all post-administration samples using solid phase extraction (SPE) for sample pretreatment.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2020Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Ecdysteroids as non-conventional anabolic agent: performance enhancement by Ecdysterone supplementation in humans
Archives of Toxicology, 2019Co-Authors: Eduard Isenmann, Francesco Botrè, Gabriella Ambrosio, Monica Mazzarino, Xavier De La Torre, Jan Felix Joseph, Philipp Zimmer, Rymantas Kazlauskas, Catrin Goebel, Patrick DielAbstract:Recent studies suggest that the anabolic effect of Ecdysterone, a naturally occurring steroid hormone claimed to enhance physical performance, is mediated by estrogen receptor (ER) binding. In comparison with the prohibited anabolic agents (e.g., metandienone and others), Ecdysterone revealed to be even more effective in a recent study performed in rats. However, scientific studies in humans are very rarely accessible. Thus, our project aimed at investigating the effects of Ecdysterone-containing products on human sport exercise. A 10-week intervention study of strength training of young men ( n = 46) was carried out. Different doses of Ecdysterone-containing supplements have been administered during the study to evaluate the performance-enhancing effect. Analysis of blood and urine samples for Ecdysterone and potential biomarkers of performance enhancement has been conducted. To ensure the specificity of the effects measured, a comprehensive screening for prohibited performance-enhancing substances was also carried out. Furthermore, the administered supplement has been tested for the absence of anabolic steroid contaminations prior to administration. Significantly higher increases in muscle mass were observed in those participants that were dosed with Ecdysterone. The same hypertrophic effects were also detected in vitro in C2C12 myotubes. Even more relevant with respect to sports performance, significantly more pronounced increases in one-repetition bench press performance were observed. No increase in biomarkers for liver or kidney toxicity was noticed. These data underline the effectivity of an Ecdysterone supplementation with respect to sports performance. Our results strongly suggest the inclusion of Ecdysterone in the list of prohibited substances and methods in sports in class S1.2 “other anabolic agents”.
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Targeting the Administration of Ecdysterone in Doping Control Samples
2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Abstract Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using GC-QTOF-MS and LC-QTOF-MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC-MS (after derivatization) and/or LC-MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC-MS(/MS) or SPE using Oasis HLB for GC-MS or LC-MS were found most suitable, while liquid-liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally desoxy-poststerone was tentatively assigned as minor metabolite, however further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than two days after the administration of a single dose of ~50 mg.
Gisela Tervooren - One of the best experts on this subject based on the ideXlab platform.
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die wirkung von rohpressaften und rohextrakten aus ajuga arten auf frasaktivitat und metamorphose von epilachna varivestis muls
Journal of Applied Entomology, 2009Co-Authors: H. Schmutterer, Gisela TervoorenAbstract:The effect of squeezed juices and crude extracts of Ajuga species on feeding activity and metamorphosis of Epilachna varivestis (Col., Coccinellidae) The effect of fresh, squeezed plant juices and that of crude extracts from dried parts of Ajuga reptans and A. remota on the feeding activity and metamorphosis of Epilachna varivestis was investigated by means of various testing methods. Squeezed plant juices and crude plant extracts cause a strong antifeedant effect. The causal agents are most probably ajugarins, at least in case of A. remota. Furthermore, the metamorphosis is strongly influenced by the extracts, leading to high larval and pupal mortalities, the appearance of pupal-adult specimens and of beetles showing more or less deformed wings. The growth-regulating effect is presumedly caused by ecdysoids, primarily Ecdysterone. Zusammenfassung Die Wirkung von Pressaften aus frischen und von Rohextrakten aus getrockneten Teilen von Ajuga reptans und A. remota auf die Frasaktivitat und Metamorphose von Epilachna varivestis wurde mit Hilfe verschiedener Testmethoden untersucht. Pressafte und Rohextrakte bewirken eine deutliche Frashemmung, die zumindest bei A. remota wahrscheinlich auf Ajugarine zuruckgefuhrt werden konnen. Auserdem wird die Metamorphose stark beeinflust, was zu hoher Larven- und Puppenmortalitat sowie zur Entstehung sog. pupal-adulter Tiere und zu Kafern mit mehr oder weniger stark deformierten Flugeln fuhrt. Die metamorphosestorende Wirkung ist mit groser Wahrscheinlichkeit auf die in den Ajuga-Arten enthaltenen Ecdysoide, insbesondere das Ecdysteron zuruckzufuhren.
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Die Wirkung von Rohpreßsäften und Rohextrakten aus Ajuga‐Arten auf Fraßaktivität und Metamorphose von Epilachna varivestis Muls
Journal of Applied Entomology, 2009Co-Authors: H. Schmutterer, Gisela TervoorenAbstract:The effect of squeezed juices and crude extracts of Ajuga species on feeding activity and metamorphosis of Epilachna varivestis (Col., Coccinellidae) The effect of fresh, squeezed plant juices and that of crude extracts from dried parts of Ajuga reptans and A. remota on the feeding activity and metamorphosis of Epilachna varivestis was investigated by means of various testing methods. Squeezed plant juices and crude plant extracts cause a strong antifeedant effect. The causal agents are most probably ajugarins, at least in case of A. remota. Furthermore, the metamorphosis is strongly influenced by the extracts, leading to high larval and pupal mortalities, the appearance of pupal-adult specimens and of beetles showing more or less deformed wings. The growth-regulating effect is presumedly caused by ecdysoids, primarily Ecdysterone. Zusammenfassung Die Wirkung von Pressaften aus frischen und von Rohextrakten aus getrockneten Teilen von Ajuga reptans und A. remota auf die Frasaktivitat und Metamorphose von Epilachna varivestis wurde mit Hilfe verschiedener Testmethoden untersucht. Pressafte und Rohextrakte bewirken eine deutliche Frashemmung, die zumindest bei A. remota wahrscheinlich auf Ajugarine zuruckgefuhrt werden konnen. Auserdem wird die Metamorphose stark beeinflust, was zu hoher Larven- und Puppenmortalitat sowie zur Entstehung sog. pupal-adulter Tiere und zu Kafern mit mehr oder weniger stark deformierten Flugeln fuhrt. Die metamorphosestorende Wirkung ist mit groser Wahrscheinlichkeit auf die in den Ajuga-Arten enthaltenen Ecdysoide, insbesondere das Ecdysteron zuruckzufuhren.
Francesco Botrè - One of the best experts on this subject based on the ideXlab platform.
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detection and quantitation of Ecdysterone in human serum by liquid chromatography coupled to tandem mass spectrometry
Steroids, 2020Co-Authors: Gabriella Ambrosio, Patrick Diel, Francesco Botrè, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Jan Felix Joseph, Maria Kristina ParrAbstract:Abstract The polyhydroxylated phytosteroid Ecdysterone is present in various plants (e.g. spinach). It is widely marketed as the active component of dietary supplements, due to its reported health and performance promoting effects. For evaluation of its actual bioavailability, a fast and sensitive method was developed, optimized and validated for human serum. Instrumental analysis was performed utilizing liquid chromatography-tandem mass spectrometry with positive electrospray ionization and acquisition in multiple reaction mode. Solid phase extraction and dilute-and-inject (following protein precipitation) were tested to isolate Ecdysterone from human serum. Both methods were compared in the light of the preset analytical target profile. The limit of detection (LOD) and quantitation (LOQ) for Ecdysterone in human serum after SPE extraction corresponded to 0.06 ng/mL and 0.14 ng/mL, respectively, meeting the requested sensitivity of the method. The assay was linear over the range of 0.10 ng/mL to 20.83 ng/mL. As expected, the sensitivity of the SPE method was better than that of the dilute-and-inject procedure, which did not allow for quantitation of all post administration serum samples. Accuracy (relative error; %) and precision (coefficient of variation; %), were both within acceptance criteria ( The developed method was successfully applied to a ten week intervention study conducted in young men performing regular resistance training. Different doses of supplements containing Ecdysterone from spinach extract have been administered during the study and the quantitation of Ecdysterone in serum samples has been successfully conducted. Ecdysterone could be quantified in all post-administration samples using solid phase extraction (SPE) for sample pretreatment.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2020Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Ecdysteroids as non-conventional anabolic agent: performance enhancement by Ecdysterone supplementation in humans
Archives of Toxicology, 2019Co-Authors: Eduard Isenmann, Francesco Botrè, Gabriella Ambrosio, Monica Mazzarino, Xavier De La Torre, Jan Felix Joseph, Philipp Zimmer, Rymantas Kazlauskas, Catrin Goebel, Patrick DielAbstract:Recent studies suggest that the anabolic effect of Ecdysterone, a naturally occurring steroid hormone claimed to enhance physical performance, is mediated by estrogen receptor (ER) binding. In comparison with the prohibited anabolic agents (e.g., metandienone and others), Ecdysterone revealed to be even more effective in a recent study performed in rats. However, scientific studies in humans are very rarely accessible. Thus, our project aimed at investigating the effects of Ecdysterone-containing products on human sport exercise. A 10-week intervention study of strength training of young men ( n = 46) was carried out. Different doses of Ecdysterone-containing supplements have been administered during the study to evaluate the performance-enhancing effect. Analysis of blood and urine samples for Ecdysterone and potential biomarkers of performance enhancement has been conducted. To ensure the specificity of the effects measured, a comprehensive screening for prohibited performance-enhancing substances was also carried out. Furthermore, the administered supplement has been tested for the absence of anabolic steroid contaminations prior to administration. Significantly higher increases in muscle mass were observed in those participants that were dosed with Ecdysterone. The same hypertrophic effects were also detected in vitro in C2C12 myotubes. Even more relevant with respect to sports performance, significantly more pronounced increases in one-repetition bench press performance were observed. No increase in biomarkers for liver or kidney toxicity was noticed. These data underline the effectivity of an Ecdysterone supplementation with respect to sports performance. Our results strongly suggest the inclusion of Ecdysterone in the list of prohibited substances and methods in sports in class S1.2 “other anabolic agents”.
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Targeting the Administration of Ecdysterone in Doping Control Samples
2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Abstract Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using GC-QTOF-MS and LC-QTOF-MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC-MS (after derivatization) and/or LC-MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC-MS(/MS) or SPE using Oasis HLB for GC-MS or LC-MS were found most suitable, while liquid-liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally desoxy-poststerone was tentatively assigned as minor metabolite, however further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than two days after the administration of a single dose of ~50 mg.
Maria Kristina Parr - One of the best experts on this subject based on the ideXlab platform.
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detection and quantitation of Ecdysterone in human serum by liquid chromatography coupled to tandem mass spectrometry
Steroids, 2020Co-Authors: Gabriella Ambrosio, Patrick Diel, Francesco Botrè, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Jan Felix Joseph, Maria Kristina ParrAbstract:Abstract The polyhydroxylated phytosteroid Ecdysterone is present in various plants (e.g. spinach). It is widely marketed as the active component of dietary supplements, due to its reported health and performance promoting effects. For evaluation of its actual bioavailability, a fast and sensitive method was developed, optimized and validated for human serum. Instrumental analysis was performed utilizing liquid chromatography-tandem mass spectrometry with positive electrospray ionization and acquisition in multiple reaction mode. Solid phase extraction and dilute-and-inject (following protein precipitation) were tested to isolate Ecdysterone from human serum. Both methods were compared in the light of the preset analytical target profile. The limit of detection (LOD) and quantitation (LOQ) for Ecdysterone in human serum after SPE extraction corresponded to 0.06 ng/mL and 0.14 ng/mL, respectively, meeting the requested sensitivity of the method. The assay was linear over the range of 0.10 ng/mL to 20.83 ng/mL. As expected, the sensitivity of the SPE method was better than that of the dilute-and-inject procedure, which did not allow for quantitation of all post administration serum samples. Accuracy (relative error; %) and precision (coefficient of variation; %), were both within acceptance criteria ( The developed method was successfully applied to a ten week intervention study conducted in young men performing regular resistance training. Different doses of supplements containing Ecdysterone from spinach extract have been administered during the study and the quantitation of Ecdysterone in serum samples has been successfully conducted. Ecdysterone could be quantified in all post-administration samples using solid phase extraction (SPE) for sample pretreatment.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2020Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Targeting the administration of Ecdysterone in doping control samples
Forensic Toxicology, 2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples, analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Analytical properties of Ecdysterone were evaluated using gas chromatography-quadrupole/time-of-flight-mass spectrometry (GC–QTOF–MS) and liquid chromatography (LC)–QTOF–MS. Its metabolism and elimination in human were studied using urines collected after administration. The detectability of Ecdysterone by GC–MS (after derivatization) and/or LC–MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC–MS(/MS) or solid phase extraction using Oasis HLB for GC–MS or LC–MS were found most suitable, while liquid–liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally, desoxy-poststerone was tentatively assigned as minor metabolite, however, further investigations are needed. An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than 2 days after the administration of a single dose of ~ 50 mg.
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Targeting the Administration of Ecdysterone in Doping Control Samples
2019Co-Authors: Maria Kristina Parr, Patrick Diel, Gabriella Ambrosio, Bernhard Wuest, Monica Mazzarino, Xavier De La Torre, Francesca Sibilia, Jan Felix Joseph, Francesco BotrèAbstract:Abstract Purpose The phytosteroid Ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of Ecdysterone from urine samples analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. Methods Analytical properties of Ecdysterone were evaluated using GC-QTOF-MS and LC-QTOF-MS. Its metabolism and elimination in human were studied using urines collected after administration. Results The detectability of Ecdysterone by GC-MS (after derivatization) and/or LC-MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC-MS(/MS) or SPE using Oasis HLB for GC-MS or LC-MS were found most suitable, while liquid-liquid extraction was hampered by the high polarity of ecdysteroids. Most abundantly, Ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-Ecdysterone. Additionally desoxy-poststerone was tentatively assigned as minor metabolite, however further investigations are needed. Conclusion An administration of Ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-Ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than two days after the administration of a single dose of ~50 mg.
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Ecdysteroids: A novel class of anabolic agents?
Biology of Sport, 2015Co-Authors: Maria Kristina Parr, Patrick Diel, Francesco Botrè, Alexandra Naß, Jonas Hengevoss, Gerhard WolberAbstract:Increasing numbers of dietary supplements with ecdysteroids are marketed as "natural anabolic agents". Results of recent studies suggested that their anabolic effect is mediated by estrogen receptor (ER) binding. Within this study the anabolic potency of Ecdysterone was compared to well characterized anabolic substances. Effects on the fiber sizes of the soleus muscle in rats as well the diameter of C2C12 derived myotubes were used as biological readouts. Ecdysterone exhibited a strong hypertrophic effect on the fiber size of rat soleus muscle that was found even stronger compared to the test compounds metandienone (dianabol), estradienedione (trenbolox), and SARM S 1, all administered in the same dose (5 mg/kg body weight, for 21 days). In C2C12 myotubes Ecdysterone (1 µM) induced a significant increase of the diameter comparable to dihydrotestosterone (1 µM) and IGF 1 (1.3 nM). Molecular docking experiments supported the ERβ mediated action of Ecdysterone. To clarify its status in sports, Ecdysterone should be considered to be included in the class "S1.2 Other Anabolic Agents" of the list of prohibited substances of the World Anti-Doping Agency.
H. Schmutterer - One of the best experts on this subject based on the ideXlab platform.
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die wirkung von rohpressaften und rohextrakten aus ajuga arten auf frasaktivitat und metamorphose von epilachna varivestis muls
Journal of Applied Entomology, 2009Co-Authors: H. Schmutterer, Gisela TervoorenAbstract:The effect of squeezed juices and crude extracts of Ajuga species on feeding activity and metamorphosis of Epilachna varivestis (Col., Coccinellidae) The effect of fresh, squeezed plant juices and that of crude extracts from dried parts of Ajuga reptans and A. remota on the feeding activity and metamorphosis of Epilachna varivestis was investigated by means of various testing methods. Squeezed plant juices and crude plant extracts cause a strong antifeedant effect. The causal agents are most probably ajugarins, at least in case of A. remota. Furthermore, the metamorphosis is strongly influenced by the extracts, leading to high larval and pupal mortalities, the appearance of pupal-adult specimens and of beetles showing more or less deformed wings. The growth-regulating effect is presumedly caused by ecdysoids, primarily Ecdysterone. Zusammenfassung Die Wirkung von Pressaften aus frischen und von Rohextrakten aus getrockneten Teilen von Ajuga reptans und A. remota auf die Frasaktivitat und Metamorphose von Epilachna varivestis wurde mit Hilfe verschiedener Testmethoden untersucht. Pressafte und Rohextrakte bewirken eine deutliche Frashemmung, die zumindest bei A. remota wahrscheinlich auf Ajugarine zuruckgefuhrt werden konnen. Auserdem wird die Metamorphose stark beeinflust, was zu hoher Larven- und Puppenmortalitat sowie zur Entstehung sog. pupal-adulter Tiere und zu Kafern mit mehr oder weniger stark deformierten Flugeln fuhrt. Die metamorphosestorende Wirkung ist mit groser Wahrscheinlichkeit auf die in den Ajuga-Arten enthaltenen Ecdysoide, insbesondere das Ecdysteron zuruckzufuhren.
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Die Wirkung von Rohpreßsäften und Rohextrakten aus Ajuga‐Arten auf Fraßaktivität und Metamorphose von Epilachna varivestis Muls
Journal of Applied Entomology, 2009Co-Authors: H. Schmutterer, Gisela TervoorenAbstract:The effect of squeezed juices and crude extracts of Ajuga species on feeding activity and metamorphosis of Epilachna varivestis (Col., Coccinellidae) The effect of fresh, squeezed plant juices and that of crude extracts from dried parts of Ajuga reptans and A. remota on the feeding activity and metamorphosis of Epilachna varivestis was investigated by means of various testing methods. Squeezed plant juices and crude plant extracts cause a strong antifeedant effect. The causal agents are most probably ajugarins, at least in case of A. remota. Furthermore, the metamorphosis is strongly influenced by the extracts, leading to high larval and pupal mortalities, the appearance of pupal-adult specimens and of beetles showing more or less deformed wings. The growth-regulating effect is presumedly caused by ecdysoids, primarily Ecdysterone. Zusammenfassung Die Wirkung von Pressaften aus frischen und von Rohextrakten aus getrockneten Teilen von Ajuga reptans und A. remota auf die Frasaktivitat und Metamorphose von Epilachna varivestis wurde mit Hilfe verschiedener Testmethoden untersucht. Pressafte und Rohextrakte bewirken eine deutliche Frashemmung, die zumindest bei A. remota wahrscheinlich auf Ajugarine zuruckgefuhrt werden konnen. Auserdem wird die Metamorphose stark beeinflust, was zu hoher Larven- und Puppenmortalitat sowie zur Entstehung sog. pupal-adulter Tiere und zu Kafern mit mehr oder weniger stark deformierten Flugeln fuhrt. Die metamorphosestorende Wirkung ist mit groser Wahrscheinlichkeit auf die in den Ajuga-Arten enthaltenen Ecdysoide, insbesondere das Ecdysteron zuruckzufuhren.
