A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（car...A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（carbamazepine）,quercetin-3’-O-glucoside was extracted from plasma samples by simple liquid-liquid extraction with ethyl acetate.The mass spectrometry detection was set in multiple reaction monitoring（MRM） mode via positive electrospray ionization（ESI）.The chromatographic run time was 3.5 min per sample.The calibration curves were linear（r^2 = 0.9992） with a lower limit of quantification（LLOQ） of 10.625 ng/mL,and the limit of detection（LOD） was 4.25 ng/mL.The intra-and inter-day precision and accuracy,in terms of relative standard deviation（RSD）,were all lower than 10.44%.The recovery rate of the analyte and internal standard were higher than 66.80%.After intravenous administration of 10 mg/kg quercetin-3’-O-glucoside,the t1/2 and AUC were（0.02±0.01） h and（1.22±0.28）×10^4 μg/L·h.The method is accurate,stable and sensitive,which is suitable for the pharmacokinetic study of quercetin-3’-O-glucoside in rats.展开更多
Dear Editor, The 2015-2016 outbreak of Zika virus （ZIKV） fever, first reported in Brazil during early 2015 （Zanluca et al., 2015）, has infected millions of people and is a global public health concern. ZIKV infect...Dear Editor, The 2015-2016 outbreak of Zika virus （ZIKV） fever, first reported in Brazil during early 2015 （Zanluca et al., 2015）, has infected millions of people and is a global public health concern. ZIKV infections are associated with fetal microcephaly, as well as neurological complications in humans. The virus can be shed in the semen and vaginal secretions of humans, leading to sexual transmission, and unexpectedly ZIKV infections cause severe damage to the male reproductive organs in male mice （Govero et al., 2016; Ma et al., 2016）.展开更多
Delonix elata L.is a Ceasalpinaceae species and is traditionally used in India for treatment of skin diseases,liver diseases and rheumatic problems.However,systematic evaluation of its wound healing activity is lackin...Delonix elata L.is a Ceasalpinaceae species and is traditionally used in India for treatment of skin diseases,liver diseases and rheumatic problems.However,systematic evaluation of its wound healing activity is lacking.Thus,in the present study,we aimed to assess the wound healing activity of D.elata stem bark extract(DSE)and its isolated constituent quercetin-3-rhamnopyranosyl-(1-6)glucopyranoside(QRPG)in rats.The formulations effects on wound healing were assessed by the wound contraction rate,epithelialization period,tensile strength,content of the hydroxyproline,hexosamine and uronic acid in granulation tissue,histopathological studies and Col 1α(I)expression level in wound tissue by reverse transcription polymerase chain reaction(RT-PCR)study.The topical application of DSE ointment caused faster epithelialization,significant wound contraction(100%),and better tensile strength(710.5±10.5 g/cm^(2)),while QRPG showed wound epithelialization with 98.2%contraction,better than that of the control group(78.18%).The biochemical analysis of granulation tissue revealed that DSE and QRPG significantly increased hydroxyproline,hexosamine and uronic acid content.A significant increase in the expression of Col 1α(I)was observed in the wound tissue of DSE and QRPG treated rats.DSE and QRPG were shown to enhance wound healing by increasing collagen synthesis through upregulation of Col 1α(I),thus validating ethnomedicinal uses.展开更多
Ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF/MS) and the MetabolynxTM software, combined with mass defect filtering, were applied to identity the metabolites of quercet...Ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF/MS) and the MetabolynxTM software, combined with mass defect filtering, were applied to identity the metabolites of quercetin-3-O-β-D-glucopyranosyl-(4→1)-α-L-rhamnoside(QGR) in rats after intravenous administration. MSE was used for simultaneous acquisition of precursor ion information and fragment ion data at high and low collision energy in one analytical run, which facilitated the rapid structural characterization of eight metabolites in rat plasma, urine and bile. The results indicated that methylation and glucuronidation were the major metabolic pathways of QGR in vivo. The present study provided important information about the metabolism of QGR which will be useful for fully understanding the mechanism of action of this compound. Furthermore, this work demonstrated the potential of the UPLC-Q-TOF/MS approach using Metabolynx for rapid and automated research of the metabolites of natural products.展开更多
The core of the natural product chemistry laboratory is isolation secondary metabolit</span><span style="font-family:Verdana;">e</span><span style="font-family:""><s...The core of the natural product chemistry laboratory is isolation secondary metabolit</span><span style="font-family:Verdana;">e</span><span style="font-family:""><span style="font-family:Verdana;">s. One of the potential secondary metabolites for isolation in the natural product chemistry laboratory is routine (quercetin-3-O-glycosides). Routine (Quercetin-3-O-glycoside) has been isolated from ethanol extract of rubber cassava leaves (</span><i><span style="font-family:Verdana;">Manihot glaziovii </span></i><span style="font-family:Verdana;">MA). Isolation was done by maceration and recrystallization. The isolation method used in this study is complemented by the isolation method published. The isolated (Quercetin-3-O-glycoside) routine using this method obtained a yield of 0.118% of the total dried leaf extract. The routine (Quercetin-3-O-glycoside) was identified using a standard routine. Routine can be further utilized in the world of medicine as an amplifier of capillary structure, reducing the permeability and fragility of blood vessels.展开更多
溃疡性结肠炎(ulcerative colitis,UC)是一种以结肠黏膜及黏膜下层炎症为主要特征的慢性非特异性炎症,其致病机制复杂,易反复发作,现代医学研究认为其涉及氧化应激、免疫失衡等多方面因素。信号转导和转录激活因子3(signal transducer a...溃疡性结肠炎(ulcerative colitis,UC)是一种以结肠黏膜及黏膜下层炎症为主要特征的慢性非特异性炎症,其致病机制复杂,易反复发作,现代医学研究认为其涉及氧化应激、免疫失衡等多方面因素。信号转导和转录激活因子3(signal transducer and activator of transcription,STAT3)是调节细胞生长、分化和存活的重要因子,可被相关细胞因子激活,从而介导炎症、氧化应激及免疫反应以影响UC病理进程,并与核因子κB(nuclear factor kappa-B,NF-κB)、NOD样受体热蛋白结构域相关蛋白3(NOD-like receptor thermal protein domain associated protein 3,NLRP3)、细胞因子信号传导抑制因子(suppressor of cytokine signaling,SOCSs)等信号通路存在串扰现象。STAT3作为近年来UC相关研究的热点之一,本文综述了中药通过调控STAT3信号通路防治UC的研究进展,深入探究了STAT3激活及介导UC病理过程的分子机制,以及中药成分如何通过多途径调控STAT3信号通路,发挥其潜在的作用机制。相关研究揭示了中药通过调节STAT3信号通路,不仅有效抑制炎症、氧化应激的发生,还能在调控免疫反应、维持肠道屏障功能及完整性等方面发挥重要作用,有望为治疗UC提供新思路。展开更多
背景:骨代谢紊乱会引起骨相关疾病的发生,而叉头框转录因子O3可以通过调节氧化应激、自噬水平等来影响骨组织细胞增殖、分化与凋亡,调控骨代谢过程。目的:系统性分析叉头框转录因子O3调控骨代谢及其在骨科疾病中作用机制的相关研究文献...背景:骨代谢紊乱会引起骨相关疾病的发生,而叉头框转录因子O3可以通过调节氧化应激、自噬水平等来影响骨组织细胞增殖、分化与凋亡,调控骨代谢过程。目的:系统性分析叉头框转录因子O3调控骨代谢及其在骨科疾病中作用机制的相关研究文献,为后续以叉头框转录因子O3为靶点治疗骨疾病的研究提供参考。方法:以“(SU=FoxO3a OR SU=Foxo3 OR SU=Forkhead box O3 OR SU=叉头框转录因子O3)AND SU=骨”为检索句在中国知网进行检索,以“主题:(“FoxO3a”)OR主题:(“Foxo3”)OR主题:(“Forkhead box O3”)OR主题:(“叉头框转录因子O3”)AND主题:(“骨”)”为检索句在万方医学数据库进行检索;以“((FoxO3a)OR(Foxo3)OR(Forkhead box O3))AND((bone)OR(Skeleton))”为检索句在PubMed数据库进行检索,排除陈旧、重复、质量较差以及不相关的文献,最终纳入56篇文献进行综述分析。结果与结论:①叉头框转录因子O3与骨髓间充质干细胞:叉头框转录因子O3能够促进成骨谱系的形成,还可通过激活自噬促进早期成骨分化。同时,叉头框转录因子O3在骨髓间充质干细胞中体现抗氧化特性,保护细胞免受氧化应激诱导的衰老。②叉头框转录因子O3与成骨细胞:叉头框转录因子O3在成骨细胞中能通过干扰Wnt/β-连环蛋白通路抑制成骨,同时能激活抗氧化酶保护成熟成骨细胞。叉头框转录因子O3能促进成骨祖细胞的增殖,并通过激活自噬促进成骨分化。③叉头框转录因子O3与破骨细胞:叉头框转录因子O3表达可抵抗氧化应激和激活自噬抑制破骨细胞生成。④叉头框转录因子O3与骨细胞:叉头框转录因子O3可通过抗氧化作用保护骨细胞,还可通过抑制p16和p53信号通路和抑制衰老相关分泌表型来减少骨流失。⑤叉头框转录因子O3与软骨细胞:叉头框转录因子O3在骨关节炎中对软骨细胞起到保护作用,抑制软骨细胞分解或凋亡,促进软骨细胞外基质合成,可抑制软骨细胞肥大;然而,叉头框转录因子O3与Runt相关转录因子1在软骨细胞中高度共表达却会促进软骨祖细胞的早期软骨形成和终末肥大。⑥叉头框转录因子O3通过参与氧化应激抵抗与调控自噬等过程影响骨代谢,参与多类骨相关疾病的病理进程。展开更多
基金National Natural Science Foundation of China (Grant No. 30960494)Jiangxi Province NSFC (Grant No. 2009 GZY0099)
文摘A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（carbamazepine）,quercetin-3’-O-glucoside was extracted from plasma samples by simple liquid-liquid extraction with ethyl acetate.The mass spectrometry detection was set in multiple reaction monitoring（MRM） mode via positive electrospray ionization（ESI）.The chromatographic run time was 3.5 min per sample.The calibration curves were linear（r^2 = 0.9992） with a lower limit of quantification（LLOQ） of 10.625 ng/mL,and the limit of detection（LOD） was 4.25 ng/mL.The intra-and inter-day precision and accuracy,in terms of relative standard deviation（RSD）,were all lower than 10.44%.The recovery rate of the analyte and internal standard were higher than 66.80%.After intravenous administration of 10 mg/kg quercetin-3’-O-glucoside,the t1/2 and AUC were（0.02±0.01） h and（1.22±0.28）×10^4 μg/L·h.The method is accurate,stable and sensitive,which is suitable for the pharmacokinetic study of quercetin-3’-O-glucoside in rats.
文摘Dear Editor, The 2015-2016 outbreak of Zika virus （ZIKV） fever, first reported in Brazil during early 2015 （Zanluca et al., 2015）, has infected millions of people and is a global public health concern. ZIKV infections are associated with fetal microcephaly, as well as neurological complications in humans. The virus can be shed in the semen and vaginal secretions of humans, leading to sexual transmission, and unexpectedly ZIKV infections cause severe damage to the male reproductive organs in male mice （Govero et al., 2016; Ma et al., 2016）.
基金partially supported by the Department of Biotechnology,New Delhi,India(Grant no.BT/PR11505/SPD/24/337/2008BT/PR9128/INF/22/190/2013)
文摘Delonix elata L.is a Ceasalpinaceae species and is traditionally used in India for treatment of skin diseases,liver diseases and rheumatic problems.However,systematic evaluation of its wound healing activity is lacking.Thus,in the present study,we aimed to assess the wound healing activity of D.elata stem bark extract(DSE)and its isolated constituent quercetin-3-rhamnopyranosyl-(1-6)glucopyranoside(QRPG)in rats.The formulations effects on wound healing were assessed by the wound contraction rate,epithelialization period,tensile strength,content of the hydroxyproline,hexosamine and uronic acid in granulation tissue,histopathological studies and Col 1α(I)expression level in wound tissue by reverse transcription polymerase chain reaction(RT-PCR)study.The topical application of DSE ointment caused faster epithelialization,significant wound contraction(100%),and better tensile strength(710.5±10.5 g/cm^(2)),while QRPG showed wound epithelialization with 98.2%contraction,better than that of the control group(78.18%).The biochemical analysis of granulation tissue revealed that DSE and QRPG significantly increased hydroxyproline,hexosamine and uronic acid content.A significant increase in the expression of Col 1α(I)was observed in the wound tissue of DSE and QRPG treated rats.DSE and QRPG were shown to enhance wound healing by increasing collagen synthesis through upregulation of Col 1α(I),thus validating ethnomedicinal uses.
基金supported by the National Science and Technology Support Program of China(No.2011 BAI04B03)
文摘Ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF/MS) and the MetabolynxTM software, combined with mass defect filtering, were applied to identity the metabolites of quercetin-3-O-β-D-glucopyranosyl-(4→1)-α-L-rhamnoside(QGR) in rats after intravenous administration. MSE was used for simultaneous acquisition of precursor ion information and fragment ion data at high and low collision energy in one analytical run, which facilitated the rapid structural characterization of eight metabolites in rat plasma, urine and bile. The results indicated that methylation and glucuronidation were the major metabolic pathways of QGR in vivo. The present study provided important information about the metabolism of QGR which will be useful for fully understanding the mechanism of action of this compound. Furthermore, this work demonstrated the potential of the UPLC-Q-TOF/MS approach using Metabolynx for rapid and automated research of the metabolites of natural products.
文摘The core of the natural product chemistry laboratory is isolation secondary metabolit</span><span style="font-family:Verdana;">e</span><span style="font-family:""><span style="font-family:Verdana;">s. One of the potential secondary metabolites for isolation in the natural product chemistry laboratory is routine (quercetin-3-O-glycosides). Routine (Quercetin-3-O-glycoside) has been isolated from ethanol extract of rubber cassava leaves (</span><i><span style="font-family:Verdana;">Manihot glaziovii </span></i><span style="font-family:Verdana;">MA). Isolation was done by maceration and recrystallization. The isolation method used in this study is complemented by the isolation method published. The isolated (Quercetin-3-O-glycoside) routine using this method obtained a yield of 0.118% of the total dried leaf extract. The routine (Quercetin-3-O-glycoside) was identified using a standard routine. Routine can be further utilized in the world of medicine as an amplifier of capillary structure, reducing the permeability and fragility of blood vessels.
文摘溃疡性结肠炎(ulcerative colitis,UC)是一种以结肠黏膜及黏膜下层炎症为主要特征的慢性非特异性炎症,其致病机制复杂,易反复发作,现代医学研究认为其涉及氧化应激、免疫失衡等多方面因素。信号转导和转录激活因子3(signal transducer and activator of transcription,STAT3)是调节细胞生长、分化和存活的重要因子,可被相关细胞因子激活,从而介导炎症、氧化应激及免疫反应以影响UC病理进程,并与核因子κB(nuclear factor kappa-B,NF-κB)、NOD样受体热蛋白结构域相关蛋白3(NOD-like receptor thermal protein domain associated protein 3,NLRP3)、细胞因子信号传导抑制因子(suppressor of cytokine signaling,SOCSs)等信号通路存在串扰现象。STAT3作为近年来UC相关研究的热点之一,本文综述了中药通过调控STAT3信号通路防治UC的研究进展,深入探究了STAT3激活及介导UC病理过程的分子机制,以及中药成分如何通过多途径调控STAT3信号通路,发挥其潜在的作用机制。相关研究揭示了中药通过调节STAT3信号通路,不仅有效抑制炎症、氧化应激的发生,还能在调控免疫反应、维持肠道屏障功能及完整性等方面发挥重要作用,有望为治疗UC提供新思路。
文摘背景:骨代谢紊乱会引起骨相关疾病的发生,而叉头框转录因子O3可以通过调节氧化应激、自噬水平等来影响骨组织细胞增殖、分化与凋亡,调控骨代谢过程。目的:系统性分析叉头框转录因子O3调控骨代谢及其在骨科疾病中作用机制的相关研究文献,为后续以叉头框转录因子O3为靶点治疗骨疾病的研究提供参考。方法:以“(SU=FoxO3a OR SU=Foxo3 OR SU=Forkhead box O3 OR SU=叉头框转录因子O3)AND SU=骨”为检索句在中国知网进行检索,以“主题:(“FoxO3a”)OR主题:(“Foxo3”)OR主题:(“Forkhead box O3”)OR主题:(“叉头框转录因子O3”)AND主题:(“骨”)”为检索句在万方医学数据库进行检索;以“((FoxO3a)OR(Foxo3)OR(Forkhead box O3))AND((bone)OR(Skeleton))”为检索句在PubMed数据库进行检索,排除陈旧、重复、质量较差以及不相关的文献,最终纳入56篇文献进行综述分析。结果与结论:①叉头框转录因子O3与骨髓间充质干细胞:叉头框转录因子O3能够促进成骨谱系的形成,还可通过激活自噬促进早期成骨分化。同时,叉头框转录因子O3在骨髓间充质干细胞中体现抗氧化特性,保护细胞免受氧化应激诱导的衰老。②叉头框转录因子O3与成骨细胞:叉头框转录因子O3在成骨细胞中能通过干扰Wnt/β-连环蛋白通路抑制成骨,同时能激活抗氧化酶保护成熟成骨细胞。叉头框转录因子O3能促进成骨祖细胞的增殖,并通过激活自噬促进成骨分化。③叉头框转录因子O3与破骨细胞:叉头框转录因子O3表达可抵抗氧化应激和激活自噬抑制破骨细胞生成。④叉头框转录因子O3与骨细胞:叉头框转录因子O3可通过抗氧化作用保护骨细胞,还可通过抑制p16和p53信号通路和抑制衰老相关分泌表型来减少骨流失。⑤叉头框转录因子O3与软骨细胞:叉头框转录因子O3在骨关节炎中对软骨细胞起到保护作用,抑制软骨细胞分解或凋亡,促进软骨细胞外基质合成,可抑制软骨细胞肥大;然而,叉头框转录因子O3与Runt相关转录因子1在软骨细胞中高度共表达却会促进软骨祖细胞的早期软骨形成和终末肥大。⑥叉头框转录因子O3通过参与氧化应激抵抗与调控自噬等过程影响骨代谢,参与多类骨相关疾病的病理进程。
