AIM:To investigate the anti-inflammatory effects of the sesquiterpenesα-humulene andβ-caryophyllene on pterygium fibroblasts.METHODS:Primary cultures of pterygium fibroblasts were established.Third passage pterygium...AIM:To investigate the anti-inflammatory effects of the sesquiterpenesα-humulene andβ-caryophyllene on pterygium fibroblasts.METHODS:Primary cultures of pterygium fibroblasts were established.Third passage pterygium fibroblasts were exposed toα-humulene andβ-caryophyllene separately and together.The cell viability was assessed by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide(MTT)assay at 12,24,48,and 72h after exposure.The levels of the inflammatory cytokines interleukin(IL)-1β,IL-6,IL-8,tumor necrosis factor(TNF)-αand IL-10 in the conditioned culture medium were assessed by enzymelinked immunosorbent assay(ELISA)at 12,24 and 48h after exposure.Data were statistically analyzed using Friedman repeated measures analysis of variances on ranks.RESULTS:The 25μmol/Lβ-caryophyllene induced significant decrease in the IL-6 production by pterygium fibroblasts 48h after the exposure(P=0.041).The levels of IL-1β,IL-8,IL-10,and TNF-αwere very low and had no statistically significant variations af ter exposure toα-humulene,β-caryophyllene,or both compounds together.CONCLUSION:The exposure to 25μmol/L ofβ-caryophyllene significantly reduce the production of IL-6 by pterygium fibroblasts after 48h.This sesquiterpene may be a potential alternative adjuvant agent for the treatment of pterygium.展开更多
Numerous pathological states of the nervous system involve alterations in neuronal excitability and synaptic dysfunction,which depend on the function of ion channels.Due to their critical involvement in health and dis...Numerous pathological states of the nervous system involve alterations in neuronal excitability and synaptic dysfunction,which depend on the function of ion channels.Due to their critical involvement in health and disease,the search for new compounds that modulate these proteins is still relevant.Traditional medicine has long been a rich source of neuroactive compounds.For example,the indigenous Mapuche people have used the leaves and bark of the Drimys winteri tree for centuries to treat various diseases.Consequently,several studies have investigated the biological effects of compounds in Drimys winteri,highlighting sesquiterpenes such asα-humulene,drimenin,polygodial,andα-,β-,γ-eudesmol.However,there is currently no literature review focusing on the ability of these sesquiterpenes to modulate ion channels.This review summarizes the current knowledge about neuroactive compounds found in Drimys winteri,with special emphasis on their direct actions on neuronal ion channels.Several Drimys winteri sesquiterpenes modulate a diverse array of neuronal ion channels,including transient receptor potential channels,gamma-aminobutyric acid A receptors,nicotinic acetylcholine receptors,and voltage-dependent Ca^(2+)and Na^(+)channels.Interestingly,the modulation of these molecular targets by Drimys winteri sesquiterpenes correlates with their therapeutic actions.The promiscuous pharmacological profile of Drimys winteri sesquiterpenes suggests they modulate multiple protein targets in vivo,making them potentially useful for treating complex,multifactorial diseases.Further studies at the molecular level may aid in developing multitargeted drugs with enhanced therapeutic effects.展开更多
The study of the volatile components of the leaves, stems and flowers of Vernonanthura patens is discussed. A micro solid-phase extraction at constant temperature with a dimethylsiloxane fiber of 100 μm was performed...The study of the volatile components of the leaves, stems and flowers of Vernonanthura patens is discussed. A micro solid-phase extraction at constant temperature with a dimethylsiloxane fiber of 100 μm was performed. The compounds extracted were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). 7 monoterpenes structures were assigned to leaves, and three to stems, these compounds were not detected in the flowers with the configuration of the system used. 17 sesquiterpenes were identified in the leaves;6 in stems and 2 in flowers, finding coincidence in some of them. The major components were α-humulene in leaves, bergamotene in stems and caryophyllene in flowers.展开更多
基金Supported by Sao Paulo State Research Foundation(Fundacao de AmparoàPesquisa do Estado de S?o Paulo–FAPESPNo.2012/10032-4)supported by a fellowship by Coordination for the Improvement of Higher Level Education Personnel(CAPES),Ministry of Education,Brazil(No.06460/2013)。
文摘AIM:To investigate the anti-inflammatory effects of the sesquiterpenesα-humulene andβ-caryophyllene on pterygium fibroblasts.METHODS:Primary cultures of pterygium fibroblasts were established.Third passage pterygium fibroblasts were exposed toα-humulene andβ-caryophyllene separately and together.The cell viability was assessed by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide(MTT)assay at 12,24,48,and 72h after exposure.The levels of the inflammatory cytokines interleukin(IL)-1β,IL-6,IL-8,tumor necrosis factor(TNF)-αand IL-10 in the conditioned culture medium were assessed by enzymelinked immunosorbent assay(ELISA)at 12,24 and 48h after exposure.Data were statistically analyzed using Friedman repeated measures analysis of variances on ranks.RESULTS:The 25μmol/Lβ-caryophyllene induced significant decrease in the IL-6 production by pterygium fibroblasts 48h after the exposure(P=0.041).The levels of IL-1β,IL-8,IL-10,and TNF-αwere very low and had no statistically significant variations af ter exposure toα-humulene,β-caryophyllene,or both compounds together.CONCLUSION:The exposure to 25μmol/L ofβ-caryophyllene significantly reduce the production of IL-6 by pterygium fibroblasts after 48h.This sesquiterpene may be a potential alternative adjuvant agent for the treatment of pterygium.
基金supported by ANID-FONDECYT 1200908(to JF),ANID-FONDECYT 1211082 and 1250856(to GEY)by the Millennium Nucleus for the Study of Pain NCN19_038(Mi Nu SPain)(to GEY)funded by the ANID scholarship 21201176。
文摘Numerous pathological states of the nervous system involve alterations in neuronal excitability and synaptic dysfunction,which depend on the function of ion channels.Due to their critical involvement in health and disease,the search for new compounds that modulate these proteins is still relevant.Traditional medicine has long been a rich source of neuroactive compounds.For example,the indigenous Mapuche people have used the leaves and bark of the Drimys winteri tree for centuries to treat various diseases.Consequently,several studies have investigated the biological effects of compounds in Drimys winteri,highlighting sesquiterpenes such asα-humulene,drimenin,polygodial,andα-,β-,γ-eudesmol.However,there is currently no literature review focusing on the ability of these sesquiterpenes to modulate ion channels.This review summarizes the current knowledge about neuroactive compounds found in Drimys winteri,with special emphasis on their direct actions on neuronal ion channels.Several Drimys winteri sesquiterpenes modulate a diverse array of neuronal ion channels,including transient receptor potential channels,gamma-aminobutyric acid A receptors,nicotinic acetylcholine receptors,and voltage-dependent Ca^(2+)and Na^(+)channels.Interestingly,the modulation of these molecular targets by Drimys winteri sesquiterpenes correlates with their therapeutic actions.The promiscuous pharmacological profile of Drimys winteri sesquiterpenes suggests they modulate multiple protein targets in vivo,making them potentially useful for treating complex,multifactorial diseases.Further studies at the molecular level may aid in developing multitargeted drugs with enhanced therapeutic effects.
文摘The study of the volatile components of the leaves, stems and flowers of Vernonanthura patens is discussed. A micro solid-phase extraction at constant temperature with a dimethylsiloxane fiber of 100 μm was performed. The compounds extracted were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). 7 monoterpenes structures were assigned to leaves, and three to stems, these compounds were not detected in the flowers with the configuration of the system used. 17 sesquiterpenes were identified in the leaves;6 in stems and 2 in flowers, finding coincidence in some of them. The major components were α-humulene in leaves, bergamotene in stems and caryophyllene in flowers.
