Inflammatory stimulation plays a significant role in the development and worsening of insulin-resistant diabetes.Therefore,it is crucial to identify therapeutic agents that can alleviate insulin resistance by targetin...Inflammatory stimulation plays a significant role in the development and worsening of insulin-resistant diabetes.Therefore,it is crucial to identify therapeutic agents that can alleviate insulin resistance by targeting inflammation.Here,we present evidence that Bakuchiol(BL),a monoterpene phenolic compound first discovered from Psoralea corylifolia L.as traditional Chinese medicine,can effectively improve insulin resistance in diabetic mice through anti-inflammation.Our findings demonstrate that BL alleviates inflammation by inhibiting the toll-like receptor 4/nuclear factorκB/mitogen-activated protein kinase axis,consequently enhancing insulin receptor signaling through the c-Jun N-terminal kinase/suppressors of cytokine signaling 3/insulin receptor substrate1 pathway and improving glucolipid homeostasis.Furthermore,the insulin recovery achieved with BL(60 mg/kg)was comparable to that of metformin(200 mg/kg).These results provide further support for considering BL as a potential treatment option for insulin-resistant diabetes mellitus.展开更多
Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of ...Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of bakuchiol through complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The bakuchiol/HP-β-CD inclusion complex's behavior and characterization were investigated by ultraviolet-visible(UV-vis)spectroscopy,Fourier transform infrared spectroscopy(FT-IR),thermogravimetric analysis(TGA),X-ray diffraction(XRD),1H nuclear magnetic resonance(NMR),and two-dimensional(2D)NMR.The obtained results indicated the formation of 1∶1 inclusion complex for bakuchiol with HP-β-CD.Water solubility of bakuchiol was significantly improved by complexation with HP-β-CD as demonstrated by phase solubility studies.The encapsulation of bakuchiol was confirmed by UV-vis,FT-IR,and XRD.The thermal stability was effectively enhanced by TGA and derivative thermogravimetry(DTG)analysis.In vitro antioxidant activity showed that bakuchiol/HP-β-CD inclusion complex had a little higher antioxidant ability than free bakuchiol.Moreover,we got the possible inclusion mode for the bakuchiol/HP-β-CD inclusion complex through NMR analysis.These results suggest that the inclusion complex can be a potentially useful approach in the design of novel formulations of bakuchiol for medical applications.展开更多
A face serum composed of a combination of biologically active compounds was evaluated for safety and efficacy <em>in vitro</em>, in a repeat insult patch test and in a human clinical efficacy trial. The se...A face serum composed of a combination of biologically active compounds was evaluated for safety and efficacy <em>in vitro</em>, in a repeat insult patch test and in a human clinical efficacy trial. The serum inhibited tyrosinase activity modestly, decreased collagenase activity and exhibited notable free radical scavenging activity <em>in vitro</em>. It is gentle to the skin, as the serum did not irritate the skin or produce symptoms of allergic contact dermatitis in the 55 healthy adults that participated in the repeat insult patch test. In the efficacy trial, daily application of the face serum for 30 days significantly increased skin hydration, with all 35 volunteers experiencing improvement. Substantial improvements in skin elasticity, roughness (fine lines and wrinkles), and brightness also occurred during the trial. Dermatological examination also revealed a trend for reduced comedone count with use of the serum. Self-assessment responses revealed that all volunteers experienced improvements in multiple skin quality parameters and that participant perceptions are consistent with the results of the instrumental analyses. These findings indicated that the measured improvements in skin quality are not only statistically significant but are also clinically relevant as they were great enough for users of the face serum to feel and recognize.展开更多
Background:Mining new whitening ingredients from plants is an effective way to develop new cosmetic products.Bakuchiol,as one of the main active ingredients from the seeds of Psoralea corylifolia L,displays whitening,...Background:Mining new whitening ingredients from plants is an effective way to develop new cosmetic products.Bakuchiol,as one of the main active ingredients from the seeds of Psoralea corylifolia L,displays whitening,antioxidant,antiaging,and free radical-scavenging activities and attracts wide attention especially in the cosmetics industry.However,environmentally friendly extraction technologies with high efficiency and high product purity remain to be developed for the scale production of bakuchiol.Objective:In this study,a new approach(acetic acid–steaming–assisted technique)was developed to improve the extraction efficiency of bakuchiol.Methods:The factors influencing the extraction efficiency of bakuchiol,including seed powder granularity,acetic acid volume,temperature,and time,were optimized based on single-factor experiments.Results:The extraction conditions were optimized as steaming the seed powder(100 g)of 40–100meshes with acetic acid(50 mL)for 10 minutes,from which a crude extract(25.1 g)containing bakuchiol was obtained.High purity(99.1)of bakuchiol(6.02 g)was then prepared by silica gel column chromatography in a one-step process.The method established in this study had higher extraction rate than other methods.The antioxidant potential of bakuchiol was evaluated based on the ABTS free radical scavenging activity and ferric reducing antioxidant power.Furthermore,bakuchiol demonstrated stronger tyrosinase inhibitory activity than the positive control(arbutin).Conclusions:Compared with the available methods,the method established in this study has increased extraction rate of bakuchiol and is environmentally friendly and economical,demonstrating the potential for industrial production.展开更多
基金supported by National Key R&D Program of China(2022YFF1100300)the Central Guidance on Local Science and Technology Development Found of Shenzhen,China(2021Szvup030).
文摘Inflammatory stimulation plays a significant role in the development and worsening of insulin-resistant diabetes.Therefore,it is crucial to identify therapeutic agents that can alleviate insulin resistance by targeting inflammation.Here,we present evidence that Bakuchiol(BL),a monoterpene phenolic compound first discovered from Psoralea corylifolia L.as traditional Chinese medicine,can effectively improve insulin resistance in diabetic mice through anti-inflammation.Our findings demonstrate that BL alleviates inflammation by inhibiting the toll-like receptor 4/nuclear factorκB/mitogen-activated protein kinase axis,consequently enhancing insulin receptor signaling through the c-Jun N-terminal kinase/suppressors of cytokine signaling 3/insulin receptor substrate1 pathway and improving glucolipid homeostasis.Furthermore,the insulin recovery achieved with BL(60 mg/kg)was comparable to that of metformin(200 mg/kg).These results provide further support for considering BL as a potential treatment option for insulin-resistant diabetes mellitus.
基金Fundamental Research Funds for the Central Universities(No.2232018D3-40)National Natural Science Foundation of China(No.81671508)。
文摘Bakuchiol isolated from Psoralea corylifolia is a naturally occurring prenylated phenolic monoterpene with a variety of bioactivities.The aim of this study was to improve the water solubility and thermal stability of bakuchiol through complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The bakuchiol/HP-β-CD inclusion complex's behavior and characterization were investigated by ultraviolet-visible(UV-vis)spectroscopy,Fourier transform infrared spectroscopy(FT-IR),thermogravimetric analysis(TGA),X-ray diffraction(XRD),1H nuclear magnetic resonance(NMR),and two-dimensional(2D)NMR.The obtained results indicated the formation of 1∶1 inclusion complex for bakuchiol with HP-β-CD.Water solubility of bakuchiol was significantly improved by complexation with HP-β-CD as demonstrated by phase solubility studies.The encapsulation of bakuchiol was confirmed by UV-vis,FT-IR,and XRD.The thermal stability was effectively enhanced by TGA and derivative thermogravimetry(DTG)analysis.In vitro antioxidant activity showed that bakuchiol/HP-β-CD inclusion complex had a little higher antioxidant ability than free bakuchiol.Moreover,we got the possible inclusion mode for the bakuchiol/HP-β-CD inclusion complex through NMR analysis.These results suggest that the inclusion complex can be a potentially useful approach in the design of novel formulations of bakuchiol for medical applications.
文摘A face serum composed of a combination of biologically active compounds was evaluated for safety and efficacy <em>in vitro</em>, in a repeat insult patch test and in a human clinical efficacy trial. The serum inhibited tyrosinase activity modestly, decreased collagenase activity and exhibited notable free radical scavenging activity <em>in vitro</em>. It is gentle to the skin, as the serum did not irritate the skin or produce symptoms of allergic contact dermatitis in the 55 healthy adults that participated in the repeat insult patch test. In the efficacy trial, daily application of the face serum for 30 days significantly increased skin hydration, with all 35 volunteers experiencing improvement. Substantial improvements in skin elasticity, roughness (fine lines and wrinkles), and brightness also occurred during the trial. Dermatological examination also revealed a trend for reduced comedone count with use of the serum. Self-assessment responses revealed that all volunteers experienced improvements in multiple skin quality parameters and that participant perceptions are consistent with the results of the instrumental analyses. These findings indicated that the measured improvements in skin quality are not only statistically significant but are also clinically relevant as they were great enough for users of the face serum to feel and recognize.
文摘Background:Mining new whitening ingredients from plants is an effective way to develop new cosmetic products.Bakuchiol,as one of the main active ingredients from the seeds of Psoralea corylifolia L,displays whitening,antioxidant,antiaging,and free radical-scavenging activities and attracts wide attention especially in the cosmetics industry.However,environmentally friendly extraction technologies with high efficiency and high product purity remain to be developed for the scale production of bakuchiol.Objective:In this study,a new approach(acetic acid–steaming–assisted technique)was developed to improve the extraction efficiency of bakuchiol.Methods:The factors influencing the extraction efficiency of bakuchiol,including seed powder granularity,acetic acid volume,temperature,and time,were optimized based on single-factor experiments.Results:The extraction conditions were optimized as steaming the seed powder(100 g)of 40–100meshes with acetic acid(50 mL)for 10 minutes,from which a crude extract(25.1 g)containing bakuchiol was obtained.High purity(99.1)of bakuchiol(6.02 g)was then prepared by silica gel column chromatography in a one-step process.The method established in this study had higher extraction rate than other methods.The antioxidant potential of bakuchiol was evaluated based on the ABTS free radical scavenging activity and ferric reducing antioxidant power.Furthermore,bakuchiol demonstrated stronger tyrosinase inhibitory activity than the positive control(arbutin).Conclusions:Compared with the available methods,the method established in this study has increased extraction rate of bakuchiol and is environmentally friendly and economical,demonstrating the potential for industrial production.
