Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit ...Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.展开更多
Background:Polygonum multiflorum-induced liver injury(PM-DILI)has significantly hindered its clinical application and development.Methods:This study investigates the variation in content and toxicity of dian-thrones,t...Background:Polygonum multiflorum-induced liver injury(PM-DILI)has significantly hindered its clinical application and development.Methods:This study investigates the variation in content and toxicity of dian-thrones,the toxic components of P.multiflorum,during different processing cycles.We employed the ultra-high-performance liquid chromatography triple quadrupole mass spectrometry method to quantify six dianthrones in raw P.multiflorum and formulations processed with a method called nine cycles of steaming and sunning.Additionally,toxicity assessments were conducted using human normal liver cell line L02 and zebrafish embryos.Results:Results indicate a gradual reduction in dianthrones content with increasing processing cycles.Processed formulations exhibited significantly reduced cytotoxic-ity in L02 cells and hepatotoxicity in zebrafish embryos.Conclusions:Our findings elucidate the relationship between processing cycles and P.multiflorum toxicity,providing theoretical support for its safe use.展开更多
The chlorophyll fluorescence parameters of Kobresia humilis Serg. and Polygonum viviparum L. grown at two different altitudes (3?200 m, 3?980 m) were measured and the ultrastructure of chloroplasts were observ...The chlorophyll fluorescence parameters of Kobresia humilis Serg. and Polygonum viviparum L. grown at two different altitudes (3?200 m, 3?980 m) were measured and the ultrastructure of chloroplasts were observed for studying the photosynthetic adaptability of plants to the influences of stress conditions in alpine environment. Rfd _values, the vitality index, in leaves of K. humilis and P.viviparum grown at 3?980 m were higher than those at 3?200 m. The higher ratio of F v/F o and F v/F m in leaves of K. humilis and P.viviparum indicated that the rate of photosynthetic conversion of light energy increased at higher altitude. Ratios of F v/F o and F v/F m and Rfd _values in K.humilis were higher than that in P.viviparum grown at the same altitude. There were more irregular chloroplasts in leaves of both species grown at higher altitude. Many irregular chloroplasts such as swollen thylakoid, deformed chloroplast envelope, were observed in P.viviparum grown at 3?980 m, but few in K. humilis . These results were discussed in relation to the photosynthetic adaptability of alpine plants and the different adaptive competence between K.humilis and P.viviparum .展开更多
Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respec...Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respectively. Results A qualitative TLC method and a quantitative HPLC method with piceid as the reference substance were established, respectively. With piceid as the reference substance and ethyl acetate-methanol-formic acid-water ( 19:3:0.5:1) as the mobile phase, a TLC method for the identification of Huzhang from the commonly used crude drugs of the same family was also set up. Conclusion The established TLC method can reasonably appraise the quality of the drug and easily distinguish Huzhang from the other commonly used crude drugs of the same family. The HPLC method for determining piceid is simple, reproducible, accurate, and feasible.展开更多
A sensitive and specific reversed-phase high performance liquid chromatography （RP-HPLC） method was established for the simultaneous quantitative determination of eight active components, two stilbenes （resveratrol...A sensitive and specific reversed-phase high performance liquid chromatography （RP-HPLC） method was established for the simultaneous quantitative determination of eight active components, two stilbenes （resveratrol, polydatin） and six flavonoids （rutin, quercilrin, quercetin, luteotin, isoorientin, kaempferol）, in Polygonum multiflorum Thunb. The chromatographic separation was performed on a Kromasil C18 column （250 mm^4.6 mm, 5 ~tm）, and gradient elution was carried out with water-methanol as the mobile phase at a flow rate of 1 mL/min. Stilbenes and flavonoids were respectively detected at 320 nm and 350 nm with DAD. The correlation coefficients of all the calibration curves were found to be higher than 0.9995. The average recoveries were ranged from 96.8% to 102.5% with RSD less than 4.8% for these components. RP-HPLC was validated to be a robust method for the quantitative determination of active components in Polygonum multiflorum Thunb, and it could be used in the quality control of this traditional medicine.展开更多
Two new stilbene glycosides (1 and 2), together with nine known compounds (3-11), were isolated from the water extract of Polygonum multiflorum Thunb. The structures of the new compounds were elucidated by their c...Two new stilbene glycosides (1 and 2), together with nine known compounds (3-11), were isolated from the water extract of Polygonum multiflorum Thunb. The structures of the new compounds were elucidated by their chemical properties and spectroscopic analyses, including extensive 2D NMR experiments. Compound 2 showed strong DNA cleavage activity, and compounds 1, 2 and 10 (2, 3, 4′, 5_tetrahydroxy_ trans _stilbene_2_O_β_ D _glucopyranoside) exhibited significant inhibition of lipid peroxidation.展开更多
[Objective] The aim was to study the variation of leaf characters from different provenance sources of Polygonum multiflorum Thunb,as well as to carry out cluster analysis on P.multiflorum from different provenance so...[Objective] The aim was to study the variation of leaf characters from different provenance sources of Polygonum multiflorum Thunb,as well as to carry out cluster analysis on P.multiflorum from different provenance sources to provide basis for the classification,identification,breeding and improved variety selection of P.multiflorum.[Method] Leaf shape characters of 31 copies of germplasm resources in the major distribution region of the whole country were determined,and the genetic variation of P.multiflorum leaves from different producing areas was analyzed.[Result] The leaf characters of single plant of the same experimental provenance source of P.multiflorum were relatively stable,the variation was mainly found on the single leaf area,1/2 leaf width,leaf width and other indicators;the variation of each leaf character among different provenance sources was obvious,and the variation was mainly found on the single leaf weight,leaf area,1/2 leaf width,leaf length and other indicators.The correlation analysis of each leaf character in P.multiflorum suggested that the single leaf area and single leaf weight showed extremely significant positive correlation with leaf length,1/2 leaf width,leaf width,leaf thickness and leaf stem length,while the single leaf area and single leaf weight showed significant negative correlation with WWR（leaf width/1/2 leaf width）and LWR（leaf length/1/2 leaf length）,in addition,several macroscopic leaf characters such as leaf length,1/2 leaf width,leaf width,leaf stem length showed extremely positive correlation.The main component analysis result suggested that the contribution rate of accumulation variance of the front three main components was up to 97.4%,which could better reflect the comprehensive performance of leaf characters of different provenance sources of P.multiflorum.The cluster analysis showed that the experimental 31 copies of P.multiflorum provenance sources should be divided into three classes,the first class was distributed in the Middle,Western of Guizhou,northwestern of Guangxi and western areas with higher altitude;the second class was distributed in Hunan,Hubei,Sichuan,Guangdong and the most area of Guangxi;the third class was distributed in Anhui,Jiangsu and Henan and Shandong.[Conclusion] Cluster analysis of leaf characters indicated that the kinds of provenance sources which the geographical position was closer could be got together.The study had provided a certain basis for the classification of P.multiflorum.展开更多
[Objective] The research aimed to study the response and accumulation characteristics of Cd in Polygonum pubescens Bl.[Method] Taking Hoagland nutritional solution as the culture substrate,eight kinds of Cd concentrat...[Objective] The research aimed to study the response and accumulation characteristics of Cd in Polygonum pubescens Bl.[Method] Taking Hoagland nutritional solution as the culture substrate,eight kinds of Cd concentrations （0,25,50,100,200,500,800,1 000 mg/L） were set up.[Result] Under low concentrations of Cd （25 and 50 mg/L）,the biomass of P.pubescens had no significant difference with CK （P0.05）.Under all the test concentrations of Cd,Cd content in the roots and shoots of P.pubescens exceeded 100 mg/kg and the enrichment coefficients of Cd were over 1.With the increasing of Cd concentration,Cd content and Cd accumulation amount in P.pubescens increased significantly.When Cd concentration exceeded 50 mg/L,translocation capacity coefficient was greater than 1.[Conclusion] Polygonum pubescens has high tolerance and accumulation capacity of Cd,and it may has some potential on the phytoremediation of Cd-contaminated soil.展开更多
由于虎杖根茎离散元模型缺乏准确的物料特性参数,对其机械化收获过程的理论研究和相关收获机具设计与优化造成很大困难。为此,以虎杖根茎为研究对象,结合试验方法测定了其物理参数、关键接触参数和弯曲断裂力学参数,对其离散元模型接触...由于虎杖根茎离散元模型缺乏准确的物料特性参数,对其机械化收获过程的理论研究和相关收获机具设计与优化造成很大困难。为此,以虎杖根茎为研究对象,结合试验方法测定了其物理参数、关键接触参数和弯曲断裂力学参数,对其离散元模型接触参数进行了标定。分别采用Hertz-Mindlin(no slip)模型和Hertz-Mindlin with Bonding V2模型建立虎杖根茎堆积角仿真模型和弯曲仿真模型,通过设计响应面试验完成对虎杖根茎离散元仿真模型接触参数和粘结参数的标定。通过碰撞弹跳试验测得虎杖根茎与作业设备间的碰撞恢复系数为0.665;通过响应面试验得到虎杖根茎之间滚动摩擦因数、碰撞恢复系数、静摩擦因数的最优参数组合为0.027、0.650、0.414,虎杖根茎与作业设备间的滚动摩擦因数、静摩擦因数分别为0.035、0.400,虎杖根茎法向接触刚度、切向接触刚度、临界法向应力、临界切向应力的最优值分别为2.02×10^(11)N/m、1.56×10^(11)N/m、1.49×10^(7)Pa、1.33×10^(7)Pa。结果表明:堆积角仿真试验和弯曲仿真试验结果与实际试验结果的相对误差分别为2.59%、1.50%,仿真与试验一致性较好,为虎杖根茎基于离散元方法的数值仿真奠定了理论基础。展开更多
目的建立定量测定大鼠血浆中顺式二苯乙烯苷[cis-2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(TSG)]与反式二苯乙烯苷(trans-TSG)血药浓度的UPLC-MS/MS方法,系统探究2种异构体在大鼠体内的药动学差异。方法将40只雄性SD大鼠随机分为...目的建立定量测定大鼠血浆中顺式二苯乙烯苷[cis-2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(TSG)]与反式二苯乙烯苷(trans-TSG)血药浓度的UPLC-MS/MS方法,系统探究2种异构体在大鼠体内的药动学差异。方法将40只雄性SD大鼠随机分为4组(每组10只),即cis-TSG ig给药组、cis-TSG尾iv给药组、trans-TSG ig给药组、transTSG尾iv给药组。ig组给药剂量为100 mg·kg^(-1),尾iv组给药剂量为10 mg·kg^(-1);于给药前(0 h)及给药后0.030、0.083、0.160、0.250、0.330、0.500、1.000、2.000、4.000、6.000、8.000、10.000、12.000、24.000 h,通过眼静脉丛采集血样。以虎杖苷为内标,测定上述2个成分在不同时间点的血药浓度;利用DAS 1.0软件计算药动学参数,分析其药动学行为差异。结果所建立的UPLC-MS/MS方法在专属性、稳定性、准确度与精密度方面均符合体内药物浓度测定的技术要求,且无明显基质效应、提取回收率稳定。药动学结果显示:①给药途径对暴露水平影响显著:2种成分经iv给药后的血药浓度-时间曲线下面积(AUC)、达峰浓度(C_(max))均显著高于ig给药,且达峰时间(t_(max))更短,提示iv给药可使药物直接、快速进入体循环;②异构体间暴露差异显著:无论是iv还是ig给药,cis-TSG的AUC、C_(max)均显著高于trans-TSG(P<0.05),cis-TSG的消除半衰期(t_(1/2))长于trans-TSG[iv(7.03 h vs 2.63 h)、ig(16.90 h vs 8.46 h)],提示2种异构体在吸收、代谢或分布过程中存在本质差异;③口服生物利用度较低:cis-TSG与trans-TSG的口服绝对生物利用度分别为28.46%、27.35%。结论cis-TSG与trans-TSG在大鼠体内的药动学行为存在显著差异,主要体现为cis-TSG的体内暴露水平更高、消除更缓慢;且2种成分的口服生物利用度均较低。展开更多
基金supported by grants from Zhejiang Chinese Medicine University affiliated hospital research project(2023FSYYZZ18)scientific research item(2022FH001),School of Life Sciences,Zhejiang Chinese Medicine University.
文摘Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.
基金National Natural Science Foundation of China,Grant/Award Number:81973476Chinese Society of Toxicology,Grant/Award Number:CST2021CT101。
文摘Background:Polygonum multiflorum-induced liver injury(PM-DILI)has significantly hindered its clinical application and development.Methods:This study investigates the variation in content and toxicity of dian-thrones,the toxic components of P.multiflorum,during different processing cycles.We employed the ultra-high-performance liquid chromatography triple quadrupole mass spectrometry method to quantify six dianthrones in raw P.multiflorum and formulations processed with a method called nine cycles of steaming and sunning.Additionally,toxicity assessments were conducted using human normal liver cell line L02 and zebrafish embryos.Results:Results indicate a gradual reduction in dianthrones content with increasing processing cycles.Processed formulations exhibited significantly reduced cytotoxic-ity in L02 cells and hepatotoxicity in zebrafish embryos.Conclusions:Our findings elucidate the relationship between processing cycles and P.multiflorum toxicity,providing theoretical support for its safe use.
文摘The chlorophyll fluorescence parameters of Kobresia humilis Serg. and Polygonum viviparum L. grown at two different altitudes (3?200 m, 3?980 m) were measured and the ultrastructure of chloroplasts were observed for studying the photosynthetic adaptability of plants to the influences of stress conditions in alpine environment. Rfd _values, the vitality index, in leaves of K. humilis and P.viviparum grown at 3?980 m were higher than those at 3?200 m. The higher ratio of F v/F o and F v/F m in leaves of K. humilis and P.viviparum indicated that the rate of photosynthetic conversion of light energy increased at higher altitude. Ratios of F v/F o and F v/F m and Rfd _values in K.humilis were higher than that in P.viviparum grown at the same altitude. There were more irregular chloroplasts in leaves of both species grown at higher altitude. Many irregular chloroplasts such as swollen thylakoid, deformed chloroplast envelope, were observed in P.viviparum grown at 3?980 m, but few in K. humilis . These results were discussed in relation to the photosynthetic adaptability of alpine plants and the different adaptive competence between K.humilis and P.viviparum .
基金TheNinth Five yearNationalKeyScientificandTech nicalProgramofChinaNo.99 92 9 0 1 3 1
文摘Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respectively. Results A qualitative TLC method and a quantitative HPLC method with piceid as the reference substance were established, respectively. With piceid as the reference substance and ethyl acetate-methanol-formic acid-water ( 19:3:0.5:1) as the mobile phase, a TLC method for the identification of Huzhang from the commonly used crude drugs of the same family was also set up. Conclusion The established TLC method can reasonably appraise the quality of the drug and easily distinguish Huzhang from the other commonly used crude drugs of the same family. The HPLC method for determining piceid is simple, reproducible, accurate, and feasible.
文摘A sensitive and specific reversed-phase high performance liquid chromatography （RP-HPLC） method was established for the simultaneous quantitative determination of eight active components, two stilbenes （resveratrol, polydatin） and six flavonoids （rutin, quercilrin, quercetin, luteotin, isoorientin, kaempferol）, in Polygonum multiflorum Thunb. The chromatographic separation was performed on a Kromasil C18 column （250 mm^4.6 mm, 5 ~tm）, and gradient elution was carried out with water-methanol as the mobile phase at a flow rate of 1 mL/min. Stilbenes and flavonoids were respectively detected at 320 nm and 350 nm with DAD. The correlation coefficients of all the calibration curves were found to be higher than 0.9995. The average recoveries were ranged from 96.8% to 102.5% with RSD less than 4.8% for these components. RP-HPLC was validated to be a robust method for the quantitative determination of active components in Polygonum multiflorum Thunb, and it could be used in the quality control of this traditional medicine.
文摘Two new stilbene glycosides (1 and 2), together with nine known compounds (3-11), were isolated from the water extract of Polygonum multiflorum Thunb. The structures of the new compounds were elucidated by their chemical properties and spectroscopic analyses, including extensive 2D NMR experiments. Compound 2 showed strong DNA cleavage activity, and compounds 1, 2 and 10 (2, 3, 4′, 5_tetrahydroxy_ trans _stilbene_2_O_β_ D _glucopyranoside) exhibited significant inhibition of lipid peroxidation.
基金Supported by High-tech Research Project of Jiangsu Province(BG2004314)~~
文摘[Objective] The aim was to study the variation of leaf characters from different provenance sources of Polygonum multiflorum Thunb,as well as to carry out cluster analysis on P.multiflorum from different provenance sources to provide basis for the classification,identification,breeding and improved variety selection of P.multiflorum.[Method] Leaf shape characters of 31 copies of germplasm resources in the major distribution region of the whole country were determined,and the genetic variation of P.multiflorum leaves from different producing areas was analyzed.[Result] The leaf characters of single plant of the same experimental provenance source of P.multiflorum were relatively stable,the variation was mainly found on the single leaf area,1/2 leaf width,leaf width and other indicators;the variation of each leaf character among different provenance sources was obvious,and the variation was mainly found on the single leaf weight,leaf area,1/2 leaf width,leaf length and other indicators.The correlation analysis of each leaf character in P.multiflorum suggested that the single leaf area and single leaf weight showed extremely significant positive correlation with leaf length,1/2 leaf width,leaf width,leaf thickness and leaf stem length,while the single leaf area and single leaf weight showed significant negative correlation with WWR（leaf width/1/2 leaf width）and LWR（leaf length/1/2 leaf length）,in addition,several macroscopic leaf characters such as leaf length,1/2 leaf width,leaf width,leaf stem length showed extremely positive correlation.The main component analysis result suggested that the contribution rate of accumulation variance of the front three main components was up to 97.4%,which could better reflect the comprehensive performance of leaf characters of different provenance sources of P.multiflorum.The cluster analysis showed that the experimental 31 copies of P.multiflorum provenance sources should be divided into three classes,the first class was distributed in the Middle,Western of Guizhou,northwestern of Guangxi and western areas with higher altitude;the second class was distributed in Hunan,Hubei,Sichuan,Guangdong and the most area of Guangxi;the third class was distributed in Anhui,Jiangsu and Henan and Shandong.[Conclusion] Cluster analysis of leaf characters indicated that the kinds of provenance sources which the geographical position was closer could be got together.The study had provided a certain basis for the classification of P.multiflorum.
基金Supported by National Science Foundation of China(30560032)Guangxi Key Laboratory Foundation (0702k023)~~
文摘[Objective] The research aimed to study the response and accumulation characteristics of Cd in Polygonum pubescens Bl.[Method] Taking Hoagland nutritional solution as the culture substrate,eight kinds of Cd concentrations （0,25,50,100,200,500,800,1 000 mg/L） were set up.[Result] Under low concentrations of Cd （25 and 50 mg/L）,the biomass of P.pubescens had no significant difference with CK （P0.05）.Under all the test concentrations of Cd,Cd content in the roots and shoots of P.pubescens exceeded 100 mg/kg and the enrichment coefficients of Cd were over 1.With the increasing of Cd concentration,Cd content and Cd accumulation amount in P.pubescens increased significantly.When Cd concentration exceeded 50 mg/L,translocation capacity coefficient was greater than 1.[Conclusion] Polygonum pubescens has high tolerance and accumulation capacity of Cd,and it may has some potential on the phytoremediation of Cd-contaminated soil.
文摘由于虎杖根茎离散元模型缺乏准确的物料特性参数,对其机械化收获过程的理论研究和相关收获机具设计与优化造成很大困难。为此,以虎杖根茎为研究对象,结合试验方法测定了其物理参数、关键接触参数和弯曲断裂力学参数,对其离散元模型接触参数进行了标定。分别采用Hertz-Mindlin(no slip)模型和Hertz-Mindlin with Bonding V2模型建立虎杖根茎堆积角仿真模型和弯曲仿真模型,通过设计响应面试验完成对虎杖根茎离散元仿真模型接触参数和粘结参数的标定。通过碰撞弹跳试验测得虎杖根茎与作业设备间的碰撞恢复系数为0.665;通过响应面试验得到虎杖根茎之间滚动摩擦因数、碰撞恢复系数、静摩擦因数的最优参数组合为0.027、0.650、0.414,虎杖根茎与作业设备间的滚动摩擦因数、静摩擦因数分别为0.035、0.400,虎杖根茎法向接触刚度、切向接触刚度、临界法向应力、临界切向应力的最优值分别为2.02×10^(11)N/m、1.56×10^(11)N/m、1.49×10^(7)Pa、1.33×10^(7)Pa。结果表明:堆积角仿真试验和弯曲仿真试验结果与实际试验结果的相对误差分别为2.59%、1.50%,仿真与试验一致性较好,为虎杖根茎基于离散元方法的数值仿真奠定了理论基础。
文摘目的建立定量测定大鼠血浆中顺式二苯乙烯苷[cis-2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(TSG)]与反式二苯乙烯苷(trans-TSG)血药浓度的UPLC-MS/MS方法,系统探究2种异构体在大鼠体内的药动学差异。方法将40只雄性SD大鼠随机分为4组(每组10只),即cis-TSG ig给药组、cis-TSG尾iv给药组、trans-TSG ig给药组、transTSG尾iv给药组。ig组给药剂量为100 mg·kg^(-1),尾iv组给药剂量为10 mg·kg^(-1);于给药前(0 h)及给药后0.030、0.083、0.160、0.250、0.330、0.500、1.000、2.000、4.000、6.000、8.000、10.000、12.000、24.000 h,通过眼静脉丛采集血样。以虎杖苷为内标,测定上述2个成分在不同时间点的血药浓度;利用DAS 1.0软件计算药动学参数,分析其药动学行为差异。结果所建立的UPLC-MS/MS方法在专属性、稳定性、准确度与精密度方面均符合体内药物浓度测定的技术要求,且无明显基质效应、提取回收率稳定。药动学结果显示:①给药途径对暴露水平影响显著:2种成分经iv给药后的血药浓度-时间曲线下面积(AUC)、达峰浓度(C_(max))均显著高于ig给药,且达峰时间(t_(max))更短,提示iv给药可使药物直接、快速进入体循环;②异构体间暴露差异显著:无论是iv还是ig给药,cis-TSG的AUC、C_(max)均显著高于trans-TSG(P<0.05),cis-TSG的消除半衰期(t_(1/2))长于trans-TSG[iv(7.03 h vs 2.63 h)、ig(16.90 h vs 8.46 h)],提示2种异构体在吸收、代谢或分布过程中存在本质差异;③口服生物利用度较低:cis-TSG与trans-TSG的口服绝对生物利用度分别为28.46%、27.35%。结论cis-TSG与trans-TSG在大鼠体内的药动学行为存在显著差异,主要体现为cis-TSG的体内暴露水平更高、消除更缓慢;且2种成分的口服生物利用度均较低。
