OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detect...OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.展开更多
目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R...目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R3软件对2000-2021年雷公藤与类风湿性关机炎相关的英文文献进行文献计量学分析,从机构发文量、作者发文量、关键词以及发展趋势等研究方面进行可视化分析。结果:研究纳入252篇英文文献,2017-2021年发文量占比35.3%,主要集中在亚洲国家及地区,包括中国、日本和中国台湾,而《民族药理学杂志》是发文量最多的英文期刊,发文量最多的作者是以Aiping Lu、Cheng Lu、Cheng Xiao等为代表的团队,研究内容是雷公藤治疗类风湿性关节炎的基础研究及临床应用,共计发文26篇,发文机构主要集中在国内高校,其中中国中医研究院是发文量最多的研究机构,多达42篇,并形成以中国中医科学院、中国药科大学和北京中医药大学为中心的主要发文研究机构。关键词可视化分析显示研究方向主要集中在甲氨蝶呤联合用药、活化作用、定量分析等方面,而未来研究热点主要集中在信号通路、机制研究等方面。结论:雷公藤和类风湿性关节炎相关英文文献发文量逐年上升,预测未来研究热点和发展方向主要集中于调控信号通路和挖掘治疗疾病的基础机制研究方面。目前,雷公藤治疗类风湿性关节炎的研究仍处在发展深入阶段,而相关研究团队应该进一步加强国际间的合作,促进后续该领域研究的发展,并提供参考依据。展开更多
In this study a reliable protocol was developed for the establishment of commercial in vitro cultures of Tripterygium wilfordii Hook f.. Juvenile shoots from one-year-old elite plants were used as the source of explan...In this study a reliable protocol was developed for the establishment of commercial in vitro cultures of Tripterygium wilfordii Hook f.. Juvenile shoots from one-year-old elite plants were used as the source of explants. New axillary shoots were obtained after 30 days of culture on a MS medium supplemented with BAP （2.0 mg.L^-1） and NAA （0.1 mg.L^-1）. The optimal multiplication medium was a modified MS medium supplemented with BAP （1.0 mg.L^-1） and NAA （0.1 mg.L^-1）. This yielded a multiplication rate of 2.4 for each subculture. Slightly more than 92% of shoots rooted when cultured on a modified MS medium containing IBA （0.2 mg.L^-1） and activated charcoal （0.5 mg.L^-1）. Activated charcoal promoted both a strong and a high rooting rate during the rooting phase. Plantlets were transferred to pots for a short acclimatization stage in a greenhouse where 95% of the plantlets survived. This highly reproducible procedure can be adopted for large-scale propagation of T. wilfordii.展开更多
Triptolide is an important active component of Tripterygium wilfordii Hook F (TWHF) and possesses anti-inflammatory, immunosuppressive, male anti-fertility, and anticancer properties. A new method combining different ...Triptolide is an important active component of Tripterygium wilfordii Hook F (TWHF) and possesses anti-inflammatory, immunosuppressive, male anti-fertility, and anticancer properties. A new method combining different techniques, including solid-liquid extraction, liquid-liquid partition, column chromatography and high-speed counter-current chromatography (HSCCC) but avoiding the use of chloroform, was developed for the isolation and purification of triptolide from the leaves of TWHF. 48 mg of triptolide at 96.5% purity was obtained from 1 kg of air-dried leaves of TWHF.展开更多
Purpose:Toexamine the effect of Tii treatment of cornea graft survival in a rab-bit model.Methods:Tii was administrated orally after eccentrical corneal transplantation.Survival times were determined by biomicroscopy....Purpose:Toexamine the effect of Tii treatment of cornea graft survival in a rab-bit model.Methods:Tii was administrated orally after eccentrical corneal transplantation.Survival times were determined by biomicroscopy.Cytotoxic T lymphocytes(CTL)and delayed-type hypersensitivity(DTH)responses to donor alloantigens were assessed at ady 16after heterotopic corneal grafts.Results:Administration of Tii reduced the incidence and prologed the graft sur-vival time.Both CTLand DTH responses to donor alloantigens were severely ed-pressed in hosts treated with Tii.However,combination of Tii and cyclosporine further enhanced the immunosuppressive effects described above.Conclusions:Tii is a potent immunosuppressant with the ability to prolong allo-graft survival in the rabbit penetrating keratoplasty model and may have coordi-native effects with CsA through different mechanisms.Further studies are neces-sary to define any potentially coordinative role in the prevention of allograft rejec-tion in human keratoplasty.Eye Science 1995;11:168-172.展开更多
A new diterpenoid was isolated from the ethanolic extract of the dried root bark of Tripterygium wilfordii Hook.f. It is the first example of abietane diterpenoid glycoside isolated from Tripterygium wilfordii Hook.f...A new diterpenoid was isolated from the ethanolic extract of the dried root bark of Tripterygium wilfordii Hook.f. It is the first example of abietane diterpenoid glycoside isolated from Tripterygium wilfordii Hook.f. Its structure was identified to be 11-O-b-D-glucopyranosyl- neotriptophenolide based on spectral methods.展开更多
文摘OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.
文摘目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R3软件对2000-2021年雷公藤与类风湿性关机炎相关的英文文献进行文献计量学分析,从机构发文量、作者发文量、关键词以及发展趋势等研究方面进行可视化分析。结果:研究纳入252篇英文文献,2017-2021年发文量占比35.3%,主要集中在亚洲国家及地区,包括中国、日本和中国台湾,而《民族药理学杂志》是发文量最多的英文期刊,发文量最多的作者是以Aiping Lu、Cheng Lu、Cheng Xiao等为代表的团队,研究内容是雷公藤治疗类风湿性关节炎的基础研究及临床应用,共计发文26篇,发文机构主要集中在国内高校,其中中国中医研究院是发文量最多的研究机构,多达42篇,并形成以中国中医科学院、中国药科大学和北京中医药大学为中心的主要发文研究机构。关键词可视化分析显示研究方向主要集中在甲氨蝶呤联合用药、活化作用、定量分析等方面,而未来研究热点主要集中在信号通路、机制研究等方面。结论:雷公藤和类风湿性关节炎相关英文文献发文量逐年上升,预测未来研究热点和发展方向主要集中于调控信号通路和挖掘治疗疾病的基础机制研究方面。目前,雷公藤治疗类风湿性关节炎的研究仍处在发展深入阶段,而相关研究团队应该进一步加强国际间的合作,促进后续该领域研究的发展,并提供参考依据。
基金supported by the Youth Talent Project of Science and Technology Department, Fujian Province (No. 2007F3017)the Research Project of the Forestry Department, Fujian Province (Minlin 2004 Kehan No. 8)
文摘In this study a reliable protocol was developed for the establishment of commercial in vitro cultures of Tripterygium wilfordii Hook f.. Juvenile shoots from one-year-old elite plants were used as the source of explants. New axillary shoots were obtained after 30 days of culture on a MS medium supplemented with BAP （2.0 mg.L^-1） and NAA （0.1 mg.L^-1）. The optimal multiplication medium was a modified MS medium supplemented with BAP （1.0 mg.L^-1） and NAA （0.1 mg.L^-1）. This yielded a multiplication rate of 2.4 for each subculture. Slightly more than 92% of shoots rooted when cultured on a modified MS medium containing IBA （0.2 mg.L^-1） and activated charcoal （0.5 mg.L^-1）. Activated charcoal promoted both a strong and a high rooting rate during the rooting phase. Plantlets were transferred to pots for a short acclimatization stage in a greenhouse where 95% of the plantlets survived. This highly reproducible procedure can be adopted for large-scale propagation of T. wilfordii.
基金Supported by the National Natural Science Foundation of China （20576113） Zhejiang Provincial Natural Science Foundation of China （R4090358）
文摘Triptolide is an important active component of Tripterygium wilfordii Hook F (TWHF) and possesses anti-inflammatory, immunosuppressive, male anti-fertility, and anticancer properties. A new method combining different techniques, including solid-liquid extraction, liquid-liquid partition, column chromatography and high-speed counter-current chromatography (HSCCC) but avoiding the use of chloroform, was developed for the isolation and purification of triptolide from the leaves of TWHF. 48 mg of triptolide at 96.5% purity was obtained from 1 kg of air-dried leaves of TWHF.
基金National Natural Science Foundation of China grantNatural Science Foundation of Guangdong Province grant
文摘Purpose:Toexamine the effect of Tii treatment of cornea graft survival in a rab-bit model.Methods:Tii was administrated orally after eccentrical corneal transplantation.Survival times were determined by biomicroscopy.Cytotoxic T lymphocytes(CTL)and delayed-type hypersensitivity(DTH)responses to donor alloantigens were assessed at ady 16after heterotopic corneal grafts.Results:Administration of Tii reduced the incidence and prologed the graft sur-vival time.Both CTLand DTH responses to donor alloantigens were severely ed-pressed in hosts treated with Tii.However,combination of Tii and cyclosporine further enhanced the immunosuppressive effects described above.Conclusions:Tii is a potent immunosuppressant with the ability to prolong allo-graft survival in the rabbit penetrating keratoplasty model and may have coordi-native effects with CsA through different mechanisms.Further studies are neces-sary to define any potentially coordinative role in the prevention of allograft rejec-tion in human keratoplasty.Eye Science 1995;11:168-172.
文摘A new diterpenoid was isolated from the ethanolic extract of the dried root bark of Tripterygium wilfordii Hook.f. It is the first example of abietane diterpenoid glycoside isolated from Tripterygium wilfordii Hook.f. Its structure was identified to be 11-O-b-D-glucopyranosyl- neotriptophenolide based on spectral methods.
