Ohne Titel
Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic,...
Ausführliche Beschreibung
Autor*in: |
Zhang, Keyi [verfasserIn] Gao, Min [verfasserIn] Xue, Beiru [verfasserIn] Kamau, Peter Muiruri [verfasserIn] Lai, Ren [verfasserIn] Luo, Lei [verfasserIn] |
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Format: |
E-Artikel |
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Sprache: |
Englisch |
Erschienen: |
2023 |
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Schlagwörter: |
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Übergeordnetes Werk: |
Enthalten in: Journal of ethnopharmacology - New York, NY [u.a.] : Elsevier, 1979, 320 |
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Übergeordnetes Werk: |
volume:320 |
DOI / URN: |
10.1016/j.jep.2023.117392 |
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Katalog-ID: |
ELV065980751 |
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520 | |a Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. | ||
650 | 4 | |a Osthenol | |
650 | 4 | |a Na | |
650 | 4 | |a Anti-nociceptive activity | |
650 | 4 | |a Lead molecule | |
700 | 1 | |a Gao, Min |e verfasserin |4 aut | |
700 | 1 | |a Xue, Beiru |e verfasserin |4 aut | |
700 | 1 | |a Kamau, Peter Muiruri |e verfasserin |4 aut | |
700 | 1 | |a Lai, Ren |e verfasserin |4 aut | |
700 | 1 | |a Luo, Lei |e verfasserin |0 (orcid)0000-0002-1327-6220 |4 aut | |
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10.1016/j.jep.2023.117392 doi (DE-627)ELV065980751 (ELSEVIER)S0378-8741(23)01262-X DE-627 ger DE-627 rda eng 610 390 VZ 15,3 ssgn PHARM DE-84 fid 44.41 bkl Zhang, Keyi verfasserin aut 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. Osthenol Na Anti-nociceptive activity Lead molecule Gao, Min verfasserin aut Xue, Beiru verfasserin aut Kamau, Peter Muiruri verfasserin aut Lai, Ren verfasserin aut Luo, Lei verfasserin (orcid)0000-0002-1327-6220 aut Enthalten in Journal of ethnopharmacology New York, NY [u.a.] : Elsevier, 1979 320 Online-Ressource (DE-627)302467696 (DE-600)1491279-X (DE-576)081952767 1872-7573 nnns volume:320 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_156 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.41 Pharmazeutische Biologie VZ AR 320 |
spelling |
10.1016/j.jep.2023.117392 doi (DE-627)ELV065980751 (ELSEVIER)S0378-8741(23)01262-X DE-627 ger DE-627 rda eng 610 390 VZ 15,3 ssgn PHARM DE-84 fid 44.41 bkl Zhang, Keyi verfasserin aut 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. Osthenol Na Anti-nociceptive activity Lead molecule Gao, Min verfasserin aut Xue, Beiru verfasserin aut Kamau, Peter Muiruri verfasserin aut Lai, Ren verfasserin aut Luo, Lei verfasserin (orcid)0000-0002-1327-6220 aut Enthalten in Journal of ethnopharmacology New York, NY [u.a.] : Elsevier, 1979 320 Online-Ressource (DE-627)302467696 (DE-600)1491279-X (DE-576)081952767 1872-7573 nnns volume:320 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_156 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.41 Pharmazeutische Biologie VZ AR 320 |
allfields_unstemmed |
10.1016/j.jep.2023.117392 doi (DE-627)ELV065980751 (ELSEVIER)S0378-8741(23)01262-X DE-627 ger DE-627 rda eng 610 390 VZ 15,3 ssgn PHARM DE-84 fid 44.41 bkl Zhang, Keyi verfasserin aut 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. Osthenol Na Anti-nociceptive activity Lead molecule Gao, Min verfasserin aut Xue, Beiru verfasserin aut Kamau, Peter Muiruri verfasserin aut Lai, Ren verfasserin aut Luo, Lei verfasserin (orcid)0000-0002-1327-6220 aut Enthalten in Journal of ethnopharmacology New York, NY [u.a.] : Elsevier, 1979 320 Online-Ressource (DE-627)302467696 (DE-600)1491279-X (DE-576)081952767 1872-7573 nnns volume:320 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_156 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.41 Pharmazeutische Biologie VZ AR 320 |
allfieldsGer |
10.1016/j.jep.2023.117392 doi (DE-627)ELV065980751 (ELSEVIER)S0378-8741(23)01262-X DE-627 ger DE-627 rda eng 610 390 VZ 15,3 ssgn PHARM DE-84 fid 44.41 bkl Zhang, Keyi verfasserin aut 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. Osthenol Na Anti-nociceptive activity Lead molecule Gao, Min verfasserin aut Xue, Beiru verfasserin aut Kamau, Peter Muiruri verfasserin aut Lai, Ren verfasserin aut Luo, Lei verfasserin (orcid)0000-0002-1327-6220 aut Enthalten in Journal of ethnopharmacology New York, NY [u.a.] : Elsevier, 1979 320 Online-Ressource (DE-627)302467696 (DE-600)1491279-X (DE-576)081952767 1872-7573 nnns volume:320 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_156 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.41 Pharmazeutische Biologie VZ AR 320 |
allfieldsSound |
10.1016/j.jep.2023.117392 doi (DE-627)ELV065980751 (ELSEVIER)S0378-8741(23)01262-X DE-627 ger DE-627 rda eng 610 390 VZ 15,3 ssgn PHARM DE-84 fid 44.41 bkl Zhang, Keyi verfasserin aut 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. Osthenol Na Anti-nociceptive activity Lead molecule Gao, Min verfasserin aut Xue, Beiru verfasserin aut Kamau, Peter Muiruri verfasserin aut Lai, Ren verfasserin aut Luo, Lei verfasserin (orcid)0000-0002-1327-6220 aut Enthalten in Journal of ethnopharmacology New York, NY [u.a.] : Elsevier, 1979 320 Online-Ressource (DE-627)302467696 (DE-600)1491279-X (DE-576)081952767 1872-7573 nnns volume:320 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_156 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 44.41 Pharmazeutische Biologie VZ AR 320 |
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Zhang, Keyi @@aut@@ Gao, Min @@aut@@ Xue, Beiru @@aut@@ Kamau, Peter Muiruri @@aut@@ Lai, Ren @@aut@@ Luo, Lei @@aut@@ |
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abstract |
Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. |
abstractGer |
Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. |
abstract_unstemmed |
Ethnopharmacological relevance: Wikstroemia indica (L.) C. A. Mey. is traditionally used for the treatment of gastrointestinal disorders, respiratory illnesses, skin infections, and inflammatory conditions. Despite extensive evidence of its biological potential, including antipyretic, antimicrobial, antifungal, anti-inflammatory, and diuretic properties, there are currently no reports indicating its analgesic effects.Aim of the study: Crude extracts from W. indica stems were examined for anti-nociceptive activity. Additionally, an in-depth investigation was conducted to uncover the molecular basis for the possible analgesic phenomenon.Materials and methods: W. indica stems were subjected to ethanol extraction. To evaluate the in vivo analgesic activity, both chemical and physical-induced pain models were employed. Additionally, single-cell electrophysiological recordings were performed on human embryonic kidney 293T (HEK293T) cells expressing NaV1.7 channel.Results: Crude extracts derived from W. indica exhibited significant efficacy in mitigating the pain sensation, as evidenced by their substantial effects in both acetic acid-induced and heat-induced pain models. Further screening unveiled osthenol as a key bioactive compound responsible for mediating the analgesic properties of W. indica. Osthenol directly interacts with the pore domain of NaV1.7 channels, leading to channel inhibition. Importantly, this interaction is independent of any changes in the channel gating modifier domain.Conclusion: Both W. indica and osthenol demonstrate potential as effective anti-nociceptive agents in preclinical studies. Their analgesic effects are likely achieved by inhibiting the NaV1.7 channel, which is crucial in pain initiation, transmission, and modulation. These results elucidate the molecular basis of the W. indica as a pain-relieving medication. Additionally, osthenol holds great potential in advancing the development of anti-nociceptive drugs targeting the NaV1.7 channel. |
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