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[Research progress in natural allopyranosides]. [天然别嘌醇苷的研究进展]。
Yaoxue Xuebao Pub Date : 2017-03-01
Ying-ying Wang, Lei-yu Tian, Yan Yang, Zhi-ying Sun, Wei Wang
{"title":"[Research progress in natural allopyranosides].","authors":"Ying-ying Wang,&nbsp;Lei-yu Tian,&nbsp;Yan Yang,&nbsp;Zhi-ying Sun,&nbsp;Wei Wang","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The pharmacological activities of natural glycosides are closely related to the polyfunctional\u0000sugar moieties. Modification of active natural products by glycosylation can change the stereochemical\u0000configuration, improve the solubility, tune up the activities and change pharmacokinetic properties for higher\u0000efficacy and better selectivity. Compared with the common D-glucose, D-allose, a C-3 epimer of D-glucose\u0000rarely exists in nature, but it plays an important role in food, health, medicine, and so on. It is not easily\u0000metabolized in the living organisms, but can be used as a safe and low-calorie sweetener. The natural\u0000allopyranosides are absolute conjugation forms which are same as other glucopyranosides and rhamnopyranosides\u0000with a broad array of biological activities. This article summarizes the major progresses made in\u0000phytochemistry and biological activity studies of these compounds. Structure-activity relationship analyses of\u0000partial anti-tumor and anti-diabetic allopyranosides were performed regarding the data reported in the literatures.\u0000These insights may provide a theoretical and experimental reference for the discovery of new drug and drug\u0000design based on allopyranosides.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[A new triterpenic acid from the roots of Rosa laevigata]. [从玫瑰根部提取的一种新的三萜酸]。
Yaoxue Xuebao Pub Date : 2017-03-01
Yu-lu Li, Hua-nian Dai, Guo-xu Ma, Wen Zhang, Tong-yu Wu, Yun-qing Wang, Jie-ming Zou, Xiao-qing Zhong, Yan-lin Zhou, Jing-quan Yuan, Xu-dong Xu, Wei Yi
{"title":"[A new triterpenic acid from the roots of Rosa laevigata].","authors":"Yu-lu Li,&nbsp;Hua-nian Dai,&nbsp;Guo-xu Ma,&nbsp;Wen Zhang,&nbsp;Tong-yu Wu,&nbsp;Yun-qing Wang,&nbsp;Jie-ming Zou,&nbsp;Xiao-qing Zhong,&nbsp;Yan-lin Zhou,&nbsp;Jing-quan Yuan,&nbsp;Xu-dong Xu,&nbsp;Wei Yi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This study was designed to investigate triterpenoids from the roots of Rosa laevigata Michx.\u0000The silica gel column chromatography was used to separate the chemical constituents from the roots of Rosa\u0000laevigata Michx. HPLC was used to analyze its purity and chemical constitution. Spectroscopy methods were\u0000used to determine their structures. Five constituents were isolated and identified as19α-OH-3β-E-feruloyl corosolic\u0000acid (1), 23-hydroxy-tormentic acid (2), 2α, 3β, 19α, 23- tetrahydroxy-12-en-28-oleanolic acid (3), 2α, 3α, 20β-\u0000trihydroxyurs-13 (18)-en-28-oic-acid (4), 2α, 3β, 20β-trihydroxyurs-13 (18)-en-28-oic-acid (5). Compound 1 was\u0000assigned as a new compound, compounds 4, 5 were obtained from the genus Rosa for the first time.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290617","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Quality control of human chorionic gonadotrophin subunit dissociation]. 人绒毛膜促性腺激素亚基解离的质量控制。
Yaoxue Xuebao Pub Date : 2017-03-01
Qin-pei Deng, Ran An, Tong-ze Xu, Li-xiu He, Meng-mei Sun, Jia-ming Yang, Yu-cai Peng
{"title":"[Quality control of human chorionic gonadotrophin subunit dissociation].","authors":"Qin-pei Deng,&nbsp;Ran An,&nbsp;Tong-ze Xu,&nbsp;Li-xiu He,&nbsp;Meng-mei Sun,&nbsp;Jia-ming Yang,&nbsp;Yu-cai Peng","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Human chorionic gonadotrophin (hCG), a glycohormone widely used in treatment of infertility,\u0000is a heterodimer composed of an alpha- and a beta-subunit. The heterodimer could be dissociated during\u0000production and storage with an impact on its bioactivity. A CE-SDS method for quantitative analysis of hCG\u0000subunit dissociation was established in this study by optimization of a variety of method conditions including\u0000sample preparation buffer compositions, incubation temperature, separation voltage, and capillary temperature.\u0000This method was validated for good sensitivity, linearity, precision, and accuracy for both α- and β-subunit.\u0000CE-SDS also showed much better precision and accuracy than SDS-PAGE. The method was successfully used\u0000in both recombinant hCG (r-hCG) produced by cell culture and hCG (u-hCG) derived from urine. The CE-SDS\u0000method was used in the study of hCG development and stability. Therefore, it is an useful tool for the quality\u0000control of hCG.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290619","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Effect of apigenin on dendritic cells maturation and function in murine splenocytes]. 芹菜素对小鼠脾细胞树突状细胞成熟和功能的影响。
Yaoxue Xuebao Pub Date : 2017-03-01
Yi-fei Liu, Xiao-xu Xue, Zheng-yi Li, Jun-peng Wang, Yi-jie Zhang
{"title":"[Effect of apigenin on dendritic cells maturation and function in murine splenocytes].","authors":"Yi-fei Liu,&nbsp;Xiao-xu Xue,&nbsp;Zheng-yi Li,&nbsp;Jun-peng Wang,&nbsp;Yi-jie Zhang","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This study was designed to explore the effect of apigenin (Api) on dendritic cell (DCs) maturation\u0000and function in murine spleen cells. The single spleen cell was isolated, and then cultured with lipopolysaccharide\u0000(LPS) in the present and absence of apigenin. After 24 h, the toxicity of Api and the T cell proliferation were\u0000determined by CCK8 kit. In addition, we collected the cell-free supernatants to measure cytokine production\u0000using ELISA, collected the cells to determine the DC maturation using flow cytometry. Finally, we purified\u0000Api and/or LPS-treated CD11c+ DCs which were pulsed with ovalbumin (OVA)323−339 and then were adoptive\u0000transferred into C57BL/6 mice to detect the OVA323−339-specific T cell proliferation and T helper (Th1) and Th2\u0000cell secreting IFN-γ and IL-4 production, respectively. We found that Api did not affect splenocyte viability, but\u0000inhibited the production of pro-inflammatory cytokine IL-1β, IL-6 and TNF-α, not anti-inflammatory cytokine\u0000IL-10. In addition, Api inhibited the expression of co-stimulatory CD80, CD86 and MHCII of CD11c + DCs.\u0000Finally, compared to LPS+OVA DCs group, DCs from Api and LPS co-treated splenocytes (Api+LPS+DCs)\u0000impaired OVA323−339-specific T cell proliferation and the production of IFN-γ and IL-4 in CD4+ T cells, which\u0000had the similar responses with OVA+DCs. These data suggest that Api exhibits anti-inflammatory properties\u0000via inhibiting DC activation and function, as a new immune-modulator, which may induce immune-tolerance\u0000with a benefit to those with chronic inflammation.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36288724","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Chromatographic fingerprint analysis of Toosendan Fructus by HPLC-CAD coupled with chemometrics methods]. [HPLC-CAD -化学计量学相结合的Toosendan Fructus色谱指纹图谱分析]。
Yaoxue Xuebao Pub Date : 2017-03-01
Chun-ni Zhang, Ying-zi Wang, Xin-guang Sun, Yang Zhao, Wei Zheng, Wen-hua Li, Zhen Long, Bai-ping Ma
{"title":"[Chromatographic fingerprint analysis of Toosendan Fructus by HPLC-CAD coupled with chemometrics methods].","authors":"Chun-ni Zhang,&nbsp;Ying-zi Wang,&nbsp;Xin-guang Sun,&nbsp;Yang Zhao,&nbsp;Wei Zheng,&nbsp;Wen-hua Li,&nbsp;Zhen Long,&nbsp;Bai-ping Ma","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A new method was developed for the chromatographic fingerprint analysis of Toosendan Fructus\u0000by HPLC coupled with the charged aerosol detector (CAD) in the present study. Samples were well separated\u0000on an Agilent ZOBAX SB C18 column (4.6 mm × 250 mm, 5 μm) by gradient elution using acetonitrile and water\u0000containing 0.1 % formic acid (v/v) at the flow rate of 1.0 mL·min−1. The column temperature was 30 ℃ and the\u0000injection volume was 5 μL. The nitrogen inlet pressure of the charged aerosol detector (CAD) was 35 psi, and\u0000the nebulizer chamber temperature was 35 ℃. In addition, the method of the chromatographic fingerprints\u0000combined with multivariate statistical analysis was effective and reasonable lead to an accurate classification of\u000020 batches of samples from different locations. The results showed that 28 common peaks were observed in the\u0000fingerprint and the samples were classified into three clusters. The established method was well validated, and\u0000showed high precision, good repeatability, and satisfactory stability. It may serve in the quality control and\u0000evaluation of Toosendan Fructus.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290576","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Screening of small molecule inhibitors for PLK1 PBD and evaluation of antitumor activities]. [筛选 PLK1 PBD 小分子抑制剂并评估其抗肿瘤活性]。
Yaoxue Xuebao Pub Date : 2017-03-01
Yu-huan Jiang, Jing Zhang, Yun-yu Chen, Yan-hong Wang, Shu-yi Si
{"title":"[Screening of small molecule inhibitors for PLK1 PBD and evaluation of antitumor activities].","authors":"Yu-huan Jiang, Jing Zhang, Yun-yu Chen, Yan-hong Wang, Shu-yi Si","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>With the method of fluorescence polarization (FP), we screened small molecule inhibitors for\u0000PLK1 PBD to identify the lead compounds for antitumor drugs. FP led to the identification of a potent hit,\u0000F083-0063, whose inhibition rate was (99.7 ± 0.4) % at 10 μg·mL−1. The IC50 was calculated to be 1.9 ± 0.1\u0000μmol·L−1 using Graphpad Prism 5. The effect of the compound on cells' multiplication was measured by MTT\u0000assay which showed that F083-0063 inhibited the proliferation of many tumor cell lines. Flow cytometry\u0000analysis indicated that the F083-0063 promoted cell apoptosis and induced cell G2/M arrest. Migration abilities\u0000of cells, evaluated using scratch test, increased significantly in the presence of F083-0063 with the migration rate\u0000as low as (37.6 ± 0.7) % at 20 μmol·L−1. Molecular linkage technique found F083-0063 had good affinity with\u0000PLK1 PBD. The results of Western blotting showed that the expression of cyclin-dependent proteins was\u0000increased after treatment with F083-0063. In summary, F083-0063 has an antitumor activity and is expected\u0000to be an antitumor lead compound targeting PLK1 PBD.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290608","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Simultaneous determination of donafenib and its N-oxide metabolite in human plasma by liquid chromatography-tandem mass spectrometry]. 液相色谱-串联质谱法同时测定人血浆中多那非尼及其n -氧化物代谢物
Yaoxue Xuebao Pub Date : 2017-03-01
Jing Wang, Bin-hua Lü, Xiao-jian Dai, Yi-fan Zhang, Xiao-yan Chen, Da-fang Zhong
{"title":"[Simultaneous determination of donafenib and its N-oxide metabolite in human plasma by liquid chromatography-tandem mass spectrometry].","authors":"Jing Wang,&nbsp;Bin-hua Lü,&nbsp;Xiao-jian Dai,&nbsp;Yi-fan Zhang,&nbsp;Xiao-yan Chen,&nbsp;Da-fang Zhong","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Donafenib is the deuterium derivative of sorafenib, and is an anti-tumor drug in clinical trials. An accurate and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of donafenib and its N-oxide metabolite in human plasma. The analytes and internal standards (sorafenib and sorafenib N-oxide) were extracted from plasma by protein precipitation with acetonitrile, and separated on a Gemini C18 (50 mm × 2.0 mm, 5 μm) column using a gradient elution procedure. The mobile phase consisted of acetonitrile and 5 mmol ·L−1 ammonium acetate (0.2% formic acid) at a flow rate of 0.7 mL·min−1. The total run time was 5.0 min. Positive electrospray ionization was performed using multiple reaction monitoring (MRM) with transitions of m/z 468.2 → 273.2 for donafenib and m/z 465.2 → 270.2 for its internal standard sorafenib, m/z 484.2 → 289.2 for donafenib N-oxide and m/z 481.2 → 286.2 for its internal standard sorafenib N-oxide. The standard curves were linear in the range of 5.00−5 000 ng·mL−1 for donafenib, and 1.00−1 000 ng·mL−1 for donafenib N-oxide. The method was validated and successfully applied to the pharmacokinetics study of donafenib tosylate tablets in volunteers.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290616","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Advances in the study of the rat model of aging induced by D-galactose] 【d -半乳糖致衰老大鼠模型的研究进展】
Yaoxue Xuebao Pub Date : 2017-03-01
Fan-fan Zhao, Yu-zhi Zhou, Li Gao, Xue-mei Qin, Guan-hua Du
{"title":"[Advances in the study of the rat model of aging induced by D-galactose]","authors":"Fan-fan Zhao,&nbsp;Yu-zhi Zhou,&nbsp;Li Gao,&nbsp;Xue-mei Qin,&nbsp;Guan-hua Du","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>D-galactose (D-gal)-induced aging model is widely used in the study of the pharmacodynamics of\u0000antiaging drugs. The model has a shorter life-span, disorders in learning and memory, reduced immune function\u0000and other aging characteristics. Regular and quantitative injection of D-gal solution to rats can produce\u0000symptoms of natural aging models that are used in screening of antiaging drugs, and their pharmacological\u0000activities. This paper provides a summary of the mechanism of rat model induced with D-gal solution. The\u0000methods of building and evaluation of the aging models are provided. The theoretical basis is included to\u0000facilitate the subsequent research and experiment in the mechanism study of aging and antiaging medicines.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290159","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Endocytosis pathway and intracellular distribution of heparosan]. [内吞途径和肝磷脂在细胞内的分布]。
Yaoxue Xuebao Pub Date : 2017-03-01
Huan-huan Peng, Ying Li, Jia-yi Yuan, Jing-xiao Chen, Jing-hua Chen
{"title":"[Endocytosis pathway and intracellular distribution of heparosan].","authors":"Huan-huan Peng,&nbsp;Ying Li,&nbsp;Jia-yi Yuan,&nbsp;Jing-xiao Chen,&nbsp;Jing-hua Chen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In this study, the endocytosis pathway of heparosan and its intracellular distribution were\u0000investigated in MCF-7 tumor cells and COS7 normal cells. The endocytosis inhibition and cellular probe\u0000location experiments showed that MCF-7 tumor cells took heparosan more efficiently and selectively than COS7\u0000cells. The cellular uptake of heparosan was energy-dependent in both MCF-7 tumor cells and COS7 normal\u0000cells. Moreover, the major endocytosis pathway of heparosan into MCF-7 tumor cells was caveolin-mediated\u0000endocytosis and macropinocytosis. The internalized heparosan was mainly located in lysosomes of the cells.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290508","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Population pharmacokinetics and its application in new drug research]. 群体药代动力学及其在新药研究中的应用
Yaoxue Xuebao Pub Date : 2017-03-01
Wen-jun Chen, Tian-yan Zhou, Wei Lu
{"title":"[Population pharmacokinetics and its application in new drug research].","authors":"Wen-jun Chen,&nbsp;Tian-yan Zhou,&nbsp;Wei Lu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Population pharmacokinetics is an emerging discipline developed from the combination of\u0000classical pharmacokinetic compartment model and statistics principles, which has been received more and more\u0000attention in recent years. Population pharmacokinetics plays important roles in all stages of new drug research.\u0000In the early preclinical phase, population pharmacokinetic analysis can help to achieve the preliminary prediction\u0000of parameters from animal to human, optimize clinical trial designs, and shorten the time required for new\u0000drugs from laboratory to clinical trials. In clinical trials and applications stage, population pharmacokinetic\u0000research can help researchers investigate the related covariates that affecting pharmacokinetic behavior of\u0000patients comprehensively, and find potential drug-drug interactions in clinical. In addition, population\u0000pharmacokinetics has a unique advantage in pediatric drug development due to its strong analysis ability of\u0000sparse data. This paper provides a summary on the history and methods of population pharmacokinetics,\u0000and the application in new drug discovery and development.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36290547","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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