With the support by the National Natural Science Foundation of China,a study led by Prof.Lu Boxun(鲁伯埙)from Fudan University demonstrates that a toxic mutant HTT species is resistant to selective autophagy,revealing...With the support by the National Natural Science Foundation of China,a study led by Prof.Lu Boxun(鲁伯埙)from Fudan University demonstrates that a toxic mutant HTT species is resistant to selective autophagy,revealing the fundamental mechanism of Huntington’s Disease.The study was published展开更多
Overlook of chiral consideration in transdermal drug delivery increases administrated dose and risk of side effects,decreasing therapeutical effects.To improve the transdermal delivery efficiency of eutomer,this work ...Overlook of chiral consideration in transdermal drug delivery increases administrated dose and risk of side effects,decreasing therapeutical effects.To improve the transdermal delivery efficiency of eutomer,this work focused on investigating the law and mechanism of enantioselective enhancing effects of chiral permeation enhancers on drug enantiomers.Chiral nonsteroidal anti-inflammatory drugs and terpene permeation enhancers were selected as model drug and enhancers.The results indicated that the L-isomer of permeation enhancers increased the skin absorption of S-enantiomer of drug and D-isomer improve the permeation of R-enantiomer,in which the enhancement effect(ER)of Lmenthol on S-enantiomer(ER=3.23)was higher than that on R-enantiomer(ER=1.49).According to the pharmacokinetics results,L-menthol tended to enhance the permeation of S-enantiomer better than R-enantiomer(2.56 fold),and showed excellent in vitro/in vivo correlations.The mechanism study showed that L-isomer of permeation enhancers improved the permeation of S-enantiomer by increasing the retention,but the D-isomer by improving partition for better permeation.Enantioselective mechanism indicated that the weaker chiral H-bond interaction between drug-chiral enhancers was caused by the enantiomeric conformation.Additionally,stronger chiral enhancers-skin interaction between L-isomer and S-conformation of ceramide produced better enhancing effects.In conclusion,enantioselective interaction of chiral drug-chiral enhancers and chiral enhancers-chiral skin played a critical role in transdermal drug delivery,rational utilization of which contributed to improving the uptake of eutomer and inhibiting distomers to decrease a half of dose and side effects,increasing transdermal therapeutical efficiency.展开更多
Achieving color-tunable room-temperature phosphorescence(RTP),especially including blue RTP from a single-component polymer still faces a formidable challenge.Herein,we wisely choose conformation-dependent phenothiazi...Achieving color-tunable room-temperature phosphorescence(RTP),especially including blue RTP from a single-component polymer still faces a formidable challenge.Herein,we wisely choose conformation-dependent phenothiazine with trifluoromethyl substituent as the side group of the phosphor monomer(Cz PT)and then copolymerize it with N-isopropylacrylamide(NIPAM)through photopolymerization to obtain polymers PPCz PTs.Time-dependent color-tunable phosphorescence from unusual quasi-equatorial(eq)to quasi-axial(ax)conformers are obtained,and the RTP color changes from orange(550 nm)to blue(470 nm)with phosphorescence lifetime up to 0.96 s.The theoretical calculations confirm that the quasi-axial conformer is the preferred structure that facilitates the formation of intramolecular hydrogen bonds on the trifluoromethyl group.The EPR spectra illustrate that the persistent UV irradiation generates radical cations to induce the conformational transitions first,followed by photopolymerization immobilizing the ax conformation in PPCz PTs.Applications of data encryption and anti-counterfeiting are fabricated to show prompt and delayed multicolor information.This work affords a simple and feasible avenue for two-dimensional color tunable room temperature phosphorescence from a single-component polymer.展开更多
文摘With the support by the National Natural Science Foundation of China,a study led by Prof.Lu Boxun(鲁伯埙)from Fudan University demonstrates that a toxic mutant HTT species is resistant to selective autophagy,revealing the fundamental mechanism of Huntington’s Disease.The study was published
基金supported by the National Natural Science Foundation of China(Grant No.82273879)
文摘Overlook of chiral consideration in transdermal drug delivery increases administrated dose and risk of side effects,decreasing therapeutical effects.To improve the transdermal delivery efficiency of eutomer,this work focused on investigating the law and mechanism of enantioselective enhancing effects of chiral permeation enhancers on drug enantiomers.Chiral nonsteroidal anti-inflammatory drugs and terpene permeation enhancers were selected as model drug and enhancers.The results indicated that the L-isomer of permeation enhancers increased the skin absorption of S-enantiomer of drug and D-isomer improve the permeation of R-enantiomer,in which the enhancement effect(ER)of Lmenthol on S-enantiomer(ER=3.23)was higher than that on R-enantiomer(ER=1.49).According to the pharmacokinetics results,L-menthol tended to enhance the permeation of S-enantiomer better than R-enantiomer(2.56 fold),and showed excellent in vitro/in vivo correlations.The mechanism study showed that L-isomer of permeation enhancers improved the permeation of S-enantiomer by increasing the retention,but the D-isomer by improving partition for better permeation.Enantioselective mechanism indicated that the weaker chiral H-bond interaction between drug-chiral enhancers was caused by the enantiomeric conformation.Additionally,stronger chiral enhancers-skin interaction between L-isomer and S-conformation of ceramide produced better enhancing effects.In conclusion,enantioselective interaction of chiral drug-chiral enhancers and chiral enhancers-chiral skin played a critical role in transdermal drug delivery,rational utilization of which contributed to improving the uptake of eutomer and inhibiting distomers to decrease a half of dose and side effects,increasing transdermal therapeutical efficiency.
基金supported by the National Natural Science Foundation of China (22175149)the Natural Science Foundation of Hunan Province (NSFH 2021JJ30661)。
文摘Achieving color-tunable room-temperature phosphorescence(RTP),especially including blue RTP from a single-component polymer still faces a formidable challenge.Herein,we wisely choose conformation-dependent phenothiazine with trifluoromethyl substituent as the side group of the phosphor monomer(Cz PT)and then copolymerize it with N-isopropylacrylamide(NIPAM)through photopolymerization to obtain polymers PPCz PTs.Time-dependent color-tunable phosphorescence from unusual quasi-equatorial(eq)to quasi-axial(ax)conformers are obtained,and the RTP color changes from orange(550 nm)to blue(470 nm)with phosphorescence lifetime up to 0.96 s.The theoretical calculations confirm that the quasi-axial conformer is the preferred structure that facilitates the formation of intramolecular hydrogen bonds on the trifluoromethyl group.The EPR spectra illustrate that the persistent UV irradiation generates radical cations to induce the conformational transitions first,followed by photopolymerization immobilizing the ax conformation in PPCz PTs.Applications of data encryption and anti-counterfeiting are fabricated to show prompt and delayed multicolor information.This work affords a simple and feasible avenue for two-dimensional color tunable room temperature phosphorescence from a single-component polymer.
