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Nat Biotech| 北京大学谢正伟课题组与合作者创建基于基因指纹和深度学习的药效预测系统(DLEPS)
原文链接:https://www.nature.com/articles/s41587-021-00946-z
北京大学谢正伟团队开发的基于人工智能和基因指纹的药效预测系统在Nature Biotechnology(IF 36.6)上线了,先讲了神经网络结构,然后对性能做了标定;然后展示了在减肥、降尿酸和非酒精性脂肪性肝炎中的应用。里面所有的中药化学对照品来自“成都德思特生物”。
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Journal of separation science-07 January 2020
Comparison of the active components of Aster tataricus from different regions and related processed products by ultra-high performance liquid chromatography with tandem mass spectrometry期刊名:Journal of separation science文献编号:DOI 10.1002/jssc.201900814文献地址:https://onlinelibrary.wiley.com/doi/abs/10.1002/jssc.201900814发表日期:07 January 2020AbstractWe investigated crude Aster tataricus, vinegar‐processed Aster tataricus, honey‐processed Aster tataricus, and steamed Aster tataricus as a case study and developed a comprehensive strategy integrating quantitative analysis and chemical pattern recognition methods for the evaluation and differentiation of Aster tataricus from different regions, as well as related processed products. In the study, 15 batches of raw Aster tataricus collected from seven provinces were analyzed. A sensitive and rapid ultra‐high performance liquid chromatography with tandem mass spectrometry method for simultaneous determination of 15 compounds was established to evaluate the quality of raw and processed Aster tataricus. Furthermore, multivariate statistical techniques were applied to compare the differences among Aster tataricus samples. As a result, the herbs collected from seven provinces were divided into two categories, and chlorogenic acid was the most important component distinguishing between the regions. Moreover, all of the raw and processed samples were classified by partial least squares discriminant analysis based on the 15 analyzed compounds. Results showed that raw Aster tataricus, vinegar‐processed Aster tataricus, honey‐processed Aster tataricus, and steamed Aster tataricus were clustered in four different areas. Shionone, chlorogenic acid and kaempferol were the significant constituents differentiating the raw and differently processed Aster tataricus samples.Luteolin, shionone, quercetin, scopoletin, kaempferol, kaempferol-7-O-β-D-glucopyranoside, isorhamnetin, 7-hydroxycoumarin, methyl caffeate, and protocatechuic acid (purity ≥ 98%) were purchased from Chengdu Desite Biological Technology Co. Ltd. (Sichuan, China)
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Chlorogenic acid ameliorates mice clinical endometritis ...
期刊名:Journal of Pharmacy and Pharmacology期刊网址:https://pubmed.ncbi.nlm.nih.gov/33734387/发表日期:18 March 2021bstract
Objectives Clinical endometritis is a common reproductive disorder in mammals that seriously
endangers animal health and causes economic losses worldwide. This study aims to use lipopoly
saccharide and Trueperella pyogenes exotoxin as modelling reagents (LC) to perfuse the mouse
uterus in order to establish a model of clinical endometritis and to investigate the anti-inflamma
tory and antioxidant effects of chlorogenic acid (CGA).
Methods In this study, five LC uterine perfusions were selected to model clinical endomet
ritis. The anti-inflammatory and antioxidant effects of CGA were clarified. Through HE staining,
proinflammatory cytokines, blood testing, NFκB and Keap1/Nrf2 signalling pathways and other
index changes to explore the protection mechanism of CGA.
Key findings After CGA treatment, the appearance, inflammatory damage and blood indicators of
the mouse uterus returned to normal. Simultaneously, CGA could inhibit the activation of NFκB
and reduce the release of inflammatory cytokines; CGA could also activate Keap1/Nrf2, promote
the dissociation of Keap1 and Nrf2 and significantly increase the expression of the downstream
genes HO-1 and NQO1.
CGA (purity >98.0%) was purchased from Desite Bio (Chengdu, China).
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Drug Metabolism and Disposition Fast Forward. Published
Icotinib induces mechanism-based inactivation of rhCYP3A4/5 possibly via heme destruction by ketene intermediate期刊名:Drug Metabolism and Disposition文献编号:DMD-AR-2021-000369R2文献地址: https://doi.org/10.1124/dmd.121.000369发表日期:July 26, 2021
Abstract
Icotinib (ICT) is an anti-tumor drug approved by China National Medical Products Administration and is found to be effective to conquer non-small cell lung cancer. The present study aimed at the interaction of ICT with CYP3A. ICT exhibited time-, concentration- and NADPH-dependent inhibitory effect on recombinant human CYP3A4/5 (rhCYP3A4/5). About 60% of CYP3A activity was suppressed by ICT at 50 μM after 30 min. The observed enzyme inhibition could not be recovered by dialysis. Nifedipine protected CYP3A from the inactivation by ICT. The inhibitory effects of ICT on CYP3A were neither influenced by GSH/NAL nor by SOD/catalase. Incubation of ICT with human hepatic microsomes produced a ketene reactive intermediate trapped by 4-bromobenzylamine. CYP3A4 dominated the metabolic activation of ICT to the ketene intermediate. Ethyl and vinyl analogs of ICT did not induce inactivation of rhCYP3A4/5, which indicates that acetylenic bioactivation of ICT contributed to the enzyme inactivation. Moreover, the metabolic activation of ICT resulted in heme destruction. In conclusion, this study demonstrated that ICT was a mechanism-based inactivator of rhCYP3A4/5, and heme destruction by the ketene metabolite may be responsible for the observed CYP3A inactivation.
6β-Hydroxytestosterone was purchased from Chengdu De-Si-Te Biological Technology Co., Ltd (Chengdu, China).
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Journal of Ethnopharmacology
Contents lists available at ScienceDirect
https://doi.org/10.1016/j.jep.2021.114336
Received 25 January 2021; Received in revised form 2 June 2021; Accepted 11 June 2021
ABSTRACT
Ethnopharmacological relevance: Viticis fructus (VF) has been widely used in alleviating the swelling and pain, owning to its pharmacologically active components including agnuside,10-O-vanilloylaucubin, luteolin and casticin.Aim of the study: The pharmacokinetic profiles of the absorbed components from aqueous and ethanolic ex-tracts of VF in rat plasma were performed, and explored the molecular mechanisms of absorbed components via network pharmacology.
Materials and methods: Ultra-performance liquid chromatography-tandem mass spectroscopy (UHPLC-MS/MS)was employed to identify the absorbed components from rat plasma. Liquid-liquid extraction with ethyl acetate was used to purify the plasma samples. Plasma pharmacokinetics parameters of the components absorbed were analyzed after oral administration of both extracts. Network pharmacology was used to predict the biological functions and potential signaling pathways of VF. The anti-cancer effects of VF extract and absorbed components have been confirmed by in vitro experiments.
Results: The method was very sensitive with lower limit of quantification (LLOQ) of 1.0, 2.5, 0.2 and 0.5 ng/mL for agnuside, 10-O-vanilloylaucubin, luteolin and casticin, respectively. With the exception of 10-O-vanil-loylaucubin which was not detected in the ethanolic extract of VF, all other components were detected in both extracts in plasma. The pharmacokinetic parameters of the four components from rat plasma were significantly different between the two extracts. According to the results of network pharmacology, the absorption compo-nents of VF are enriched in 32 key pathways, and 15 pathways are related to cancer. Ultimately, the anti-cancer effects, as well as the signaling pathways of VF ethanolic extract and absorbed components were veri-fied by in vitro experiments.
Conclusion: The optimized, sensitive and validated UHPLC-MS/MS method was successfully applied for the plasma pharmacokinetics comparison analysis of the two VF extracts. The combination of network pharma-cology and pharmacokinetics provides a useful method to elucidate the biological effects and molecular mechanism of the absorbed components of VF.
laboratory. Agnuside, luteolin, casticin, formononetin and geniposide (purity on HPLC> 98%) were supplied by Chengdu Desite Bio-Technology (Chengdu, China).
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Journal of Ethnopharmacology (Volume 260, 5 October 2020, 113044)
https://doi.org/10.1016/j.jep.2020.113044Received 16 March 2020; Received in revised form 11 May 2020; Accepted 28 May 2020Available online 11 June 2020
Abstract
Ethnopharmacological relevance: San-Ye-Tang-Zhi-Qing formula (SYTZQ) is an effffective prescription for the treatment of pre-diabetes disorders of glycolipid metabolism in type 2 diabetes mellitus (T2DM). It consists of five Chinese herbs including Mori Folium, Nelumbinis Folium, Crataegi Folium, Salviae Miltiorrhizae Radix et Rhizoma and Paeoniae Radix Rubra.
Aim of the study: This study was aimed to reveal the pharmacological mechanism of pharmacokinetic target components of SYTZQ for the treatment of T2DM.
Materials and methods: A rapid, precise and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed to quantify simultaneously nuciferin, vitexin-4″-O-glu-coside, vitexin-2″-O-rhamnoside, paeoniflflorin and rosmarinic acid in rat plasma after oral administration of SYTZQ. The network pharmacology was used to analyze the effffect of the compounds absorbed into the blood of SYTZQ on T2DM. The effffects of paeoniflflorin, nuciferine and rosmarinic acid on adipogenic difffferentiation werevalidated in vitro experiments.
Results: The separation was performed on an ACQUITY UHPLC HSS T3 column (2.1 mm × 100 mm, 1.7 μm) using acetonitrile and 0.1% (v/v) formic acid in water as the mobile phase in gradient elution. The calibration curves of fifive analytes showed good linearity (r ≥ 0.9991) with the lower limits of quantifification (LLOQ) between 0.3 and 5.0 ng/mL. The recoveries and matrix effffects of fifive analytes ranged from 81.1% to 113%. The RSDs of inter-day and intra-day precision were all within 13.7%. The validated method was successfully appliedto the pharmacokinetic study of fifive ingredients after oral administration of SYTZQ to rat. 39 major targets and22 candidate pathways of fifive compounds absorbed into the blood of rats after administration of SYTZQ were identifified and successfully constructed a compound-target-disease-pathway network. It was confifirmed that paeniforin, nuciferine and rosmarinic acid could decrease the adipogenicity difffferentiation in vitro experiments. Conclusions: The pharmacokinetic parameters indicated that the fifive components (nuciferin, vitexin-4″-O-glu-coside, vitexin-2″-O-rhamnoside, paeoniflflorin and rosmarinic acid) were absorbed and eliminated quickly in vivo. These fifive absorbed components were associated with 22 pathways, including insulin resistance, regulation of lipolysis in adipocytes, PI3k/AKT-, TNF-, cAMP- and cGMP-PKG-signaling pathway. Paeoniflflorin, nuciferine and rosmarinic acid have the effffect of inhibiting adipocyte difffferentiation. This study could provide more re-ference for quality control, and provide a fifirm basis for evaluating the clinical effiffifficiency of SYTZQ.
Nuciferin, vitexin-4″-O-glucoside, vitexin-2″-O-rhamnoside, paeoni-flflorin, rosmarinic acid, genipin (IS1), berberine (IS2) and baicalein (IS3) were purchased from Chengdu Desite Biotechnology Co., Ltd.(Chengdu, China). All purity of these ingredients was more than 98%.The chemical structures of those ingredients were presented in Fig. 1.
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