The objective of this research was to assess the potential of phosphatidylcholineencapsulated resveratrol as a cosmetic ingredient.The hydrogen peroxide(H_(2)O_(2))and ultraviolet A(UVA)induced human skin fibroblasts(...The objective of this research was to assess the potential of phosphatidylcholineencapsulated resveratrol as a cosmetic ingredient.The hydrogen peroxide(H_(2)O_(2))and ultraviolet A(UVA)induced human skin fibroblasts(HSF)models of skin damage were established to compare the antioxidant and anti-wrinkle properties between phosphatidylcholine-encapsulated resveratrol and unencapsulated resveratrol.The findings reveal that encapsulating resveratrol with phosphatidylcholine not only enhances skin absorption but also significantly improves its antioxidant capabilities.In the H2O2-induced HSF injury model,phosphatidylcholine-encapsulated resveratrol demonstrates a superior ability to neutralize reactive oxygen species(ROS)generated by H2O2 compared to the resveratrol group.Further analysis indicates that this enhanced functionality is associated with increased enzymatic activities of superoxide dismutase(SOD),glutathione peroxidase(GSH-Px)and catalase(CAT)when treated with phosphatidylcholine-encapsulated resveratrol.Additionally,in UVA-irradiated HSF cells,phosphatidylcholine-encapsulated resveratrol effectively reduces the levels of matrix metalloproteinases-1 and-3(MMP-1 and MMP-3)and increased the contents of CollagenⅠand CollagenⅢ(Col-1 and Col-3),demonstrating significant anti-wrinkle effects.These findings provide critical evaluation criteria and application references for enhancing cosmetic ingredients through phosphatidylcholine encapsulation,thereby advancing skincare formulations.展开更多
OBJECTIVE To elucidate the structural-pharmacokinetic relationship and identify resveratrol analogs with favorable pharmacokinetic profiles for potential medicinal application. METHODS The pharmacokinetic data of resv...OBJECTIVE To elucidate the structural-pharmacokinetic relationship and identify resveratrol analogs with favorable pharmacokinetic profiles for potential medicinal application. METHODS The pharmacokinetic data of resveratrol(trans-3,5,4-trihydroxystilbene),pterostilbene(trans-3,5-dimethoxy-4-hydroxystilbene),resveratrol trimethyl ether(trans-3,5,4-trimethoxystilbene)and some other herbal resveratrol analogs were extracted from the authors′recent publications and compared.RESULTS Aqueous solubility,to different extent,has been identified as a barrier to oral absorption of resveratrol and its analogs.In addition,the para hydroxyl group(s)on the aromatic ring was less liable to metabolism compared to the meta-hydroxyl group(s).Pterostilbene and resveratrol trimethyl ether displayed more superior pharmacokinetic properties than resveratrol,i.e.much slower clearance and abundant plasma exposure.CONCLUSION Pterostilbene appears to be a favorable candidate for further development.Resveratrol analogs with meta-hydroxyl group(s)might have poor metabolic stability and suffer from rapid clearance and low oral bioavailability.展开更多
OBJECTIVE To investigate the therapeutic effects and related signaling pathways involved in the actions of resveratrol on experimental pneumoconiosis in vivo and in vitro.METHODS The pneumoconiosis animal model was in...OBJECTIVE To investigate the therapeutic effects and related signaling pathways involved in the actions of resveratrol on experimental pneumoconiosis in vivo and in vitro.METHODS The pneumoconiosis animal model was induced by exposing male SD rats to 15mg·m-3 silica aerosol in an inhalation chamber system for 6h·d-1,5d·week-1 for up to 8 weeks.The vehicle or resveratrol(10or 20mg·kg-1)was preventively or remedially administered to the rats during or after the 4-or 8-week silica exposure(SE)period,respectively.After 4-,8-,and up to 14-week treatment,in vivo near-infrared fluorescence imaging analysis and histological analysis were performed to evaluate the pathological changes in rat lung.Inflammatory cytokines level in bronchoalveolar lavage fluid(BALF)was measured by ELISA testing,and the deposition of fibrotic collagen proteins in lung parenchyma was determined by western blotting and immunohistochemistry analysis.Microarray analysis was performed to screen the signaling pathways involved in the actions of resveratrol on pneumoconiosis in vitro models.Anti-inflammation action and signaling of resveratrol was evaluated on silica-stimulated rat alveolar macrophage,which is one of the crucial effector cells for silica-induced inflammatory response;anti-fibrosis action and signaling of resveratrol was evaluated on TGF-β-induced human lung fibroblast,which acts as a promoter in the later fibrotic process of pneumoconiosis.RESULTS Silica aerosol exposure significantly increased macrophage infiltration and matrix metalloproteinases activity in lung tissue concomitant with the increased levels of inflammatory mediators in BALF.Preventive treatment with resveratrol(20mg·kg-1·d-1)reversed all these biochemical indices as well as histopathological alterations induced by silica exposure.Post-SE resveratrol treatment mildly reduced silica-induced inflammatory response in rat lung with no statistical significance.In vitro study revealed that resveratrol could inhibit alveolar macrophage cell death and decrease the levels of IL-1β and TNF-αinduced by silica particle exposure to cultured alveolar macrophages.Resveratrol was further shown to inhibit the nuclear transition of NF-κB and formation of cleaved caspase-1.Encouragingly,resveratrol preventively attenuated the lung fibrosis,evidenced by less fibrotic nodules formation and collagen proteins expression.No significant improvement on lung fibrosis was observed with post-SE resveratrol treatment.Invitrostudy further demonstrated that resveratrol suppressed TGF-β-induced lung fibroblast proliferation and collagen deposition,concomitant with the depressed activity of TGF-β/Smad signaling in lung fibroblast.CONCLUSION Resveratrol shows the anti-inflammation and anti-fibrosis actions on experimental pneumoconiosis in vivo and in vitro models.The depression of NF-κB,NALP3-inflammasome,and TGF-β/Smad signaling pathways may be involved in the anti-inflammation and anti-fibrosis actions of resveratrol,respectively.Resveratrol could be a potential therapeutic agent for the intervention of pneumoconiosis.展开更多
OBJECTIVE To evaluate the protective effects of resveratrol nanosuspensions loaded in situ hydrogel on Alzheimer disease model mice after intranasal administration. METHODS Resveratrol nanosuspensions were fabricated ...OBJECTIVE To evaluate the protective effects of resveratrol nanosuspensions loaded in situ hydrogel on Alzheimer disease model mice after intranasal administration. METHODS Resveratrol nanosuspensions were fabricated by antisolvent nano-precipitation method,and then dispersed into0.5% gellan gum to form resveratrol nanosuspenisons loaded ionic sensitive in situ hydrogel. The Alzheimer′s disease models were induced by lateral ventricle injection of Aβ_(25~35)and the protection and treatment effects of resveratrol nanosuspensions loaded in situ hydrogel on study and memory capability were performed after intranasal administration in water maze experiments. The analyses of the changes of cholinergic neurotransmitters in the brain were also determined according to the contents of acetylcholine(ACh),choline acetyltransferase(ChAT) and acetylcholinesterase(AChE). RESULTS Behavior assessment disclosed that in position navigation,escape latency test,each of experimental animals showed a decreased trend with swim training days increase,indicating that in the training process they had the ability of learning and memory in looking for the platform. Compared with the control group,average latency of model group significantly increased. While compared with the model group,treatment group′s average latency was significantly shorter. Space exploration experiment results showed that the times of model group across target quadrant of the platform is less than that of control group. But the crossing times of treatment group with resveratrol increased compared with the model group. As for the changes of cholinergic neurotransmitters,in AD mice brain ACh content decreased; the Ch AT activity decreased,while the activity of ACh E with the ability to hydrolysis acetylcholine increased. The administration of resveratrol can decrease the activity of ACh enzymes but increase Ch AT activity and the levels of acetylcholine. CONCLUSION Resveratrol nanosuspension loaded in situ gel can ameliorate the declining ability of learning and memory of AD model mice after intranasal administration. As a promising approach for the treatment of central nervous system(CNS) disease,intranasal administration route can effectively deliver to the brain and thus enhance the therapeutic effect.展开更多
该研究探究了日粮中添加白藜芦醇对牛肌纤维类型和丝氨酸-苏氨酸蛋白激酶(serine-threonine protein kinase,Akt)/叉头盒蛋白O(forkhead box protein O,FoxO)通路信号分子的影响,并进一步以牛肌管细胞为研究对象,验证其分子机制。结果表...该研究探究了日粮中添加白藜芦醇对牛肌纤维类型和丝氨酸-苏氨酸蛋白激酶(serine-threonine protein kinase,Akt)/叉头盒蛋白O(forkhead box protein O,FoxO)通路信号分子的影响,并进一步以牛肌管细胞为研究对象,验证其分子机制。结果表明,肉牛日粮添加450 mg/kg白藜芦醇显著提高了背最长肌和腰大肌Ⅰ型纤维基因表达(P<0.05),降低了Ⅱ型纤维基因表达(P<0.05)。进一步分析其分子机制,发现,白藜芦醇显著上调肉牛背最长肌中磷酸酰肌醇3-激酶(phosphatidylinositol3-kinase,PI3K)和Akt的基因表达水平(P<0.05),显著下调FoxO 3基因表达水平(P<0.05),显著上调了PI3K、p-Akt/Akt和p-FoxO1/FoxO1蛋白表达(P<0.05);显著上调肉牛腰大肌PI 3 K和Akt的基因表达水平(P<0.05),显著下调FoxO 1和FoxO3基因表达水平(P<0.05),显著下调了FoxO1和FoxO3的蛋白表达水平(P<0.05),显著上调了PI3K、p-Akt、p-FoxO1/FoxO1和p-FoxO3/FoxO3蛋白表达(P<0.05),表明肉牛日粮添加白藜芦醇激活了Akt/FoxO通路。添加PI3K抑制剂渥曼青霉素(wortmannin)阻断Akt/FoxO信号通路后,白藜芦醇对牛肌管细胞中肌纤维类型的转化作用和对Akt/FoxO信号通路的激活作用被减弱。研究表明,白藜芦醇可通过激活Akt/FoxO通路促进牛肌纤维类型从Ⅱ型到Ⅰ型的转化。展开更多
文摘The objective of this research was to assess the potential of phosphatidylcholineencapsulated resveratrol as a cosmetic ingredient.The hydrogen peroxide(H_(2)O_(2))and ultraviolet A(UVA)induced human skin fibroblasts(HSF)models of skin damage were established to compare the antioxidant and anti-wrinkle properties between phosphatidylcholine-encapsulated resveratrol and unencapsulated resveratrol.The findings reveal that encapsulating resveratrol with phosphatidylcholine not only enhances skin absorption but also significantly improves its antioxidant capabilities.In the H2O2-induced HSF injury model,phosphatidylcholine-encapsulated resveratrol demonstrates a superior ability to neutralize reactive oxygen species(ROS)generated by H2O2 compared to the resveratrol group.Further analysis indicates that this enhanced functionality is associated with increased enzymatic activities of superoxide dismutase(SOD),glutathione peroxidase(GSH-Px)and catalase(CAT)when treated with phosphatidylcholine-encapsulated resveratrol.Additionally,in UVA-irradiated HSF cells,phosphatidylcholine-encapsulated resveratrol effectively reduces the levels of matrix metalloproteinases-1 and-3(MMP-1 and MMP-3)and increased the contents of CollagenⅠand CollagenⅢ(Col-1 and Col-3),demonstrating significant anti-wrinkle effects.These findings provide critical evaluation criteria and application references for enhancing cosmetic ingredients through phosphatidylcholine encapsulation,thereby advancing skincare formulations.
基金The project supported by a start-up grant from the National University of Singapore(R148000174133)
文摘OBJECTIVE To elucidate the structural-pharmacokinetic relationship and identify resveratrol analogs with favorable pharmacokinetic profiles for potential medicinal application. METHODS The pharmacokinetic data of resveratrol(trans-3,5,4-trihydroxystilbene),pterostilbene(trans-3,5-dimethoxy-4-hydroxystilbene),resveratrol trimethyl ether(trans-3,5,4-trimethoxystilbene)and some other herbal resveratrol analogs were extracted from the authors′recent publications and compared.RESULTS Aqueous solubility,to different extent,has been identified as a barrier to oral absorption of resveratrol and its analogs.In addition,the para hydroxyl group(s)on the aromatic ring was less liable to metabolism compared to the meta-hydroxyl group(s).Pterostilbene and resveratrol trimethyl ether displayed more superior pharmacokinetic properties than resveratrol,i.e.much slower clearance and abundant plasma exposure.CONCLUSION Pterostilbene appears to be a favorable candidate for further development.Resveratrol analogs with meta-hydroxyl group(s)might have poor metabolic stability and suffer from rapid clearance and low oral bioavailability.
基金The project is supported by Pneumoconiosis Compensation Fund Board(6903114),HKSAR Government,Hong Kong
文摘OBJECTIVE To investigate the therapeutic effects and related signaling pathways involved in the actions of resveratrol on experimental pneumoconiosis in vivo and in vitro.METHODS The pneumoconiosis animal model was induced by exposing male SD rats to 15mg·m-3 silica aerosol in an inhalation chamber system for 6h·d-1,5d·week-1 for up to 8 weeks.The vehicle or resveratrol(10or 20mg·kg-1)was preventively or remedially administered to the rats during or after the 4-or 8-week silica exposure(SE)period,respectively.After 4-,8-,and up to 14-week treatment,in vivo near-infrared fluorescence imaging analysis and histological analysis were performed to evaluate the pathological changes in rat lung.Inflammatory cytokines level in bronchoalveolar lavage fluid(BALF)was measured by ELISA testing,and the deposition of fibrotic collagen proteins in lung parenchyma was determined by western blotting and immunohistochemistry analysis.Microarray analysis was performed to screen the signaling pathways involved in the actions of resveratrol on pneumoconiosis in vitro models.Anti-inflammation action and signaling of resveratrol was evaluated on silica-stimulated rat alveolar macrophage,which is one of the crucial effector cells for silica-induced inflammatory response;anti-fibrosis action and signaling of resveratrol was evaluated on TGF-β-induced human lung fibroblast,which acts as a promoter in the later fibrotic process of pneumoconiosis.RESULTS Silica aerosol exposure significantly increased macrophage infiltration and matrix metalloproteinases activity in lung tissue concomitant with the increased levels of inflammatory mediators in BALF.Preventive treatment with resveratrol(20mg·kg-1·d-1)reversed all these biochemical indices as well as histopathological alterations induced by silica exposure.Post-SE resveratrol treatment mildly reduced silica-induced inflammatory response in rat lung with no statistical significance.In vitro study revealed that resveratrol could inhibit alveolar macrophage cell death and decrease the levels of IL-1β and TNF-αinduced by silica particle exposure to cultured alveolar macrophages.Resveratrol was further shown to inhibit the nuclear transition of NF-κB and formation of cleaved caspase-1.Encouragingly,resveratrol preventively attenuated the lung fibrosis,evidenced by less fibrotic nodules formation and collagen proteins expression.No significant improvement on lung fibrosis was observed with post-SE resveratrol treatment.Invitrostudy further demonstrated that resveratrol suppressed TGF-β-induced lung fibroblast proliferation and collagen deposition,concomitant with the depressed activity of TGF-β/Smad signaling in lung fibroblast.CONCLUSION Resveratrol shows the anti-inflammation and anti-fibrosis actions on experimental pneumoconiosis in vivo and in vitro models.The depression of NF-κB,NALP3-inflammasome,and TGF-β/Smad signaling pathways may be involved in the anti-inflammation and anti-fibrosis actions of resveratrol,respectively.Resveratrol could be a potential therapeutic agent for the intervention of pneumoconiosis.
基金The project supported by the National Training Program of Innovation and Entrepreneurship for Undergraduates(201610439108)
文摘OBJECTIVE To evaluate the protective effects of resveratrol nanosuspensions loaded in situ hydrogel on Alzheimer disease model mice after intranasal administration. METHODS Resveratrol nanosuspensions were fabricated by antisolvent nano-precipitation method,and then dispersed into0.5% gellan gum to form resveratrol nanosuspenisons loaded ionic sensitive in situ hydrogel. The Alzheimer′s disease models were induced by lateral ventricle injection of Aβ_(25~35)and the protection and treatment effects of resveratrol nanosuspensions loaded in situ hydrogel on study and memory capability were performed after intranasal administration in water maze experiments. The analyses of the changes of cholinergic neurotransmitters in the brain were also determined according to the contents of acetylcholine(ACh),choline acetyltransferase(ChAT) and acetylcholinesterase(AChE). RESULTS Behavior assessment disclosed that in position navigation,escape latency test,each of experimental animals showed a decreased trend with swim training days increase,indicating that in the training process they had the ability of learning and memory in looking for the platform. Compared with the control group,average latency of model group significantly increased. While compared with the model group,treatment group′s average latency was significantly shorter. Space exploration experiment results showed that the times of model group across target quadrant of the platform is less than that of control group. But the crossing times of treatment group with resveratrol increased compared with the model group. As for the changes of cholinergic neurotransmitters,in AD mice brain ACh content decreased; the Ch AT activity decreased,while the activity of ACh E with the ability to hydrolysis acetylcholine increased. The administration of resveratrol can decrease the activity of ACh enzymes but increase Ch AT activity and the levels of acetylcholine. CONCLUSION Resveratrol nanosuspension loaded in situ gel can ameliorate the declining ability of learning and memory of AD model mice after intranasal administration. As a promising approach for the treatment of central nervous system(CNS) disease,intranasal administration route can effectively deliver to the brain and thus enhance the therapeutic effect.
