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SSRN 2023年

作者： Ke, Tongwei Zhang, Jing Guo, Mengyue Qin, Jia'an Ruan, Haonan Tian, Jiao He, Chunjiao Luo, Yawen Qin, Xuhua Luo, Jiaoyang Yang, Meihua School of Pharmacy Chengdu University of Traditional Chinese Medicine Sichuan Chengdu611137 China Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of Education Institute of Medicinal Plant Development Chinese Academy of Medical Sciences Peking Union Medical College Beijing100193 China

In this study, we developed a simple, cheap, and sensitive carbon nanoparticles (CNPs) based immunochromatographic method for the determination of thiamethoxam in honeysuckle. The CNPs based immunochromatography strip (CNP-ICS) was prepared based on the indirect immune competition principle. The preparation conditions of CNPs labeled monoclonal antibody, test strip and sample diluent were optimized. Compared with the traditional colloidal gold immunochromatography test strip, the developed method had higher sensitivity, better specificity and accuracy. The labeling concentration of antibody was optimized to be 3.6 μg, and the coating antigen concentration was 0.05 mg·mL-1. The sensitivity reached 0.1 ng·mL-1, the detection limit of thiamethoxam in honeysuckle was 2 ng·mL-1, and the IC50 was 0.450 ng·mL-1. The cross-reaction rates of thiamethoxam with nine structural analogs, such as nitenpyram, imidaclothiz and clothianidin, were all less than 0.2%. It was verified that the results of 26 batches of honeysuckle samples detected by the CNP-ICS method were consistent with those of LC-MS/MS. The immunochromatography test strip prepared in this study has the advantages of simple preparation, low cost, and high sensitivity, which can be used for rapid field screening and detection of thiamethoxam residues in honeysuckle with a complex matrix. © 2023, The Authors. All rights reserved.

关键词： Monoclonal antibodies

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Ganoderic acid a derivative induces apoptosis of cervical cancer cells by inhibiting JNK pathway

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Chinese Herbal Medicines 2024年

作者： Wang, Mengchen Han, Qin Zhang, Xuelian Dong, Xi Ran, Jiadong Wei, Fei Luo, Yun Sun, Xiaobo Institute of Medicinal Plant Development Peking Union Medical College and Chinese Academy of Medical Sciences Beijing 100193 China Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of Education Beijing 100193 China Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine Beijing 100193 China NMPA Key Laboratory for Research and Evaluation of Pharmacovigilance Beijing 100193 China

Objective: Ganoderic acid A can inhibit the proliferation and promotes the apoptosis of cancer cells. Surprisingly, the molecular mechanisms underlying the anti-cancer effects of ganoderic acid A still remain poorly defined. Ganoderic acid A derivative (GaAD19) is an effective ingredient obtained by structural modification of ganoderic acid A. The purpose of this study was to evaluate the anti-proliferation effect of GaAD19 on cervical cancer cells. Methods: Through the HeLa cervical cancer cell model, the drug target of GaAD19 was predicted using the SwissTargetPrediction database and molecular docking. Subsequently, computer analysis results were verified by a series of molecular biology experiments, such as flow cytometry, Western blot, immunocytochemical staining, terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL), quantitative real time polymerase chain reaction (qPCR), and so on. Then, pathway agonists and inhibitors were used to investigate the mechanism of GaAD19. Finally, the mouse model of cervical cancer was established to evaluate the inhibitory effect of GaAD19 on tumor growth in U14 cervical cancer mice. Results: GaAD19 induced apoptosis and inhibited the growth of tumors. It also blocked the transition from the G₁ to the S phase of the cell cycle. However, in the presence of a c-Jun N-terminal kinase (JNK)agonist, the effects of GaAD19 on the proliferation, apoptosis, and cell cycle transition of cancer cells were suppressed. Conclusions: This study showed that GaAD19 can play an anti-cervical cancer role by inhibiting the JNK signaling pathway. These results will be helpful in further exploring the mechanism of GaAD19 in the treatment of cervical cancer. © 2024 Tianjin Press of Chinese Herbal Medicines

关键词： anti-cancer apoptosis cervical cancer ganoderic acid A derivative JNK pathway

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Identifying Qingkailing(清开灵)ingredients-dependent mesenchymal-epithelial transition factor-axiation“π”structuring module with angiogenesis and neurogenesis effects

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Journal of Traditional Chinese Medicine 2024年第1期44卷 35-43页

作者： CHENG Kunming YUAN Jianan LIU Jun ZHANG Shengpeng XU Qixiang XIE Yong ZHAO Jingfeng ZHANG Xiaoxu TANG Xudong ZHENG Yongqiu WANG Zhong Provincial Engineering Laboratory for Screening and Re-evaluation of Active Compounds of Herbal Medicines in Southern Anhui Teaching and Research Section of Traditional Chinese MedicineSchool of PharmacyWannan Medical CollegeWuhu 241000China Institute of Basic Research in Clinical Medicine China Academy of Chinese Medical SciencesBeijing 100700China Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of EducationDepartment of Medicinal Plant DevelopmentChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100193China Department of Gastroenterology Xiyuan HospitalChina Academy of Chinese Medical SciencesBeijing 100091China

OBJECTIVE:To explore the functional role of the drugdependent mesenchymal-epithelial transition(Met)-axiation"π"structural module of neurogenesis after processing by three components of Qingkailing injection in neurogenesis and angiogenesis in cerebral ***:We used a Glutathione S-transferase(GST)-pull down assay,isothermal titration calorimetry assay,and other related methods to identify the relationships among Met,inositol polyphosphate phosphatase like 1(Inppl1),and death associated protein kinase 3(Dapk3)in this allosteric *** biological effects of the modules of neurons generation composed of Met,Inppl1,and Dapk3 were measured through Western blot,apoptosis analysis,and double immunofluorescence ***:The GST-pull down assay revealed that proline-serine-threonine rich domain of Met binds to the Src homology domain of Inppl1 to form a protein-protein complex;Dapk3 with a C-terminal domain interacts weakly with the protein kinase C domain of Met in the intracellular ***,we obtained a“π”structuring module considered a neural regeneration *** biological effects of angiogenesis and neurogenesis modules composed of Met,Inppl1,and Dapk3 were also ***:The study suggested that understanding the functional modules that contribute to pharmaceutics might provide novel signatures that can be used as endpoints to define disease processes under stroke or cerebral ischemia conditions.

关键词： brain ischemia stroke neurogenesis angiogenesis modular pharmacology Met-axiation allosteric module

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A new strategy of enhancing absorptivity and safety for evodiamine: polyamidoamine derivatives modified by polyethylene glycol chain

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Traditional Medicine Research 2021年第2期6卷 100-110页

作者： Yao-Chun Gao Yuan-Sheng Lao Meng-Xue Zhang Nan Li Chen-Yang Wu Zheng-Qi Dong Institute of Medicinal Plant Development Chinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100193China Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of EducationChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100094China Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription Beijing 100700China

Background:Traditional Chinese medicine involves complex ingredients and mixtures of ingredients that often exhibit low bioavailability,and excipients are often lacking to increase the absorption-enhancing *** study modified the generation 4 polyamidoamine dendrimer with polyethylene glycol of different molecular weights(5000,2000,1000)to form a series of polyamidoamine-co-polyethylene glycol(PAMAM-co-PEG)as a novel class of oral absorption ***,the major alkaloid found in the traditional Chinese medicine Wu Zhu Yu(Fructus Evodiae),was used as a model drug to verify the absorption-enhancing effects and the safety of this ***:This study utilized the solubility determination method documented in the Pharmacopoeia of the People’s Republic of China(2015 edition)and the D0 values recommended in the US FDA guidelines to comprehensively evaluate the solubility of *** permeability of evodiamine was assessed using the apparent permeability coefficient in experiments based on in vitro cell *** aspects of the biological safety of PAMAM-co-PEG were explored using the MTT assay,LDH assay,and total protein release of the rat intestinal ***,the absorption-enhancing effects of PAMAM-co-PEG at different molecular weights on evodiamine were verified via the use of in vitro cell models and in vivo intestinal loop circulation experiments with ***:Evodiamine exhibited low solubility and permeability and was classified into class IV compounds using the biopharmaceutical classification ***-co-PEG 2000 demonstrated improvement in the biosafety and absorption-enhancement effect of evodiamine at a specific *** study showed that 0.05%(w/v)of PAMAM-co-PEG 2000 increased the cumulative penetration of evodiamine via cell transport by 1.32 times,and 0.10%(w/v)of PAMAM-co-PEG 2000 increased the area under curve value of evodiamine by 1.31 ***:Evodiamine possesses low solubility and

关键词： Polyamidoamine dendrimers Polyethylene glycol Intestinal absorption enhancer Bioavailability Evodiamine Fructus Evodiae

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Effects of diarylbutane lignans from Schisandra chinensis fruit on SARS-CoV-2 3CL^pro and PL^pro and their in vitro anti-inflammatory properties

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Phytomedicine Plus 2023年第2期3卷 100432-100432页

作者： Li, Bin Qiao, Liansheng Xiao, Qi Zhang, Jianuo Liu, Jiushi Zhang, Bengang Liu, Haitao Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of Education Institute of Medicinal Plant Development Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100193 China School of Chinese Materia Medica Beijing University of Chinese Medicine Beijing 100029 China

Background: Schisandra chinensis fruit is a well-known traditional Chinese medicine (TCM), whose extract has a potent inhibitory effect on the severe acute respiratory syndrome-coronavirus-2 (SARS‑CoV‑2) 3-chymotrypsin-like protease (3CL^pro) and papain-like protease (PL^pro). Purpose: This work aims to find the active components from the fruit of S. chinensis against SARS‑CoV‑2 3CL^pro and PL^pro. Materials and methods: The chemical constituents of the fruit of S. chinensis were retrieved based on the electronic databases, such as Web of Science, PubMed, Medline Plus, and CNKI. Molecular docking was used to screen the active components against SARS‑CoV‑2 3CL^pro and PL^pro. Potential hit compounds were further evaluated by enzymatic activity assay. Furthermore, the anti-inflammatory activities of the active compounds were further explored using the phorbol-12-myristate-13-acetate (PMA)-induced THP1 cells model. Results: In this work, we retrieved 75 components of S. chinensis fruit, including 62 dibenzocyclooctadiene-type lignans, 3 diarylbutane-type lignans, 2 tetrahydrofuran-type lignans, and 8 nortriterpenoids. Combining molecular docking study and in vitro experiments, we found that pregomisin (63), meso‑dihydroguaiaretic acid (64), and nordihydroguaiaretic acid (65) could potently inhibit 3CL^pro with IC₅₀ values of 3.07 ± 0.38, 4.12 ± 0.38, and 6.06 ± 0.62 μM, respectively, and inhibit PL^pro with IC₅₀ values of 5.23 ± 0.33, 4.24 ± 0.46, and 16.28 ± 0.54 μM, respectively. Interestingly, compounds 63, 64, and 65 also have potent activities of regulating the inflammatory response in vitro. Conclusion: Our results suggest that compounds 63, 64, and 65 may be promising SARS-CoV-2 3CL^pro and PL^pro inhibitors and anti-inflammatory. © 2023

关键词： 3-Chymotrypsin-like protease Diarylbutane lignans Inflammation Papain-like protease SARS-CoV-2 Schisandra chinensis fruit

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Cembranoid Diterpenes from the South China Sea Soft Coral Sarcophyton Crassocaule

SSRN

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SSRN 2024年

作者： Peng, Han-Yang Zeng, Yan-Bo Yang, Li Wu, Fei Gai, Cui-Juan Yuan, Jing-Zhe Chang, Wen-Jun Dai, Hao-Fu Wang, Xia-Chang Zhang, Rui Jiangsu Key Laboratory for Functional Substances of Chinese Medicine Nanjing University of Chinese Medicine Nanjing210023 China Hainan Provincial Key Laboratory for Functional Components Research Utilization of Marine Bio-resources National Key Laboratory for Tropical Crop Breeding Institute of Tropical Bioscience and Biotechnology Chinese Academy of Tropical Agricultural Sciences Haikou571101 China Zhanjiang Experimental Station of Chinese Academy of Tropical Agricultural Sciences Zhanjiang524013 China

Five new cembranoid diterpenes, meijicrassolins A–E (1–5), were isolated from the soft coral Sarcophyton crassocaule, along with five previously reported analogs (6–10). The structures and absolute configuration for new compounds 1–5 were assigned by extensive spectroscopic analysis, single-crystal X-ray crystallography, quantum mechanical nuclear magnetic resonance (QM-NMR) and time-dependent density functional theory/electronic circular dichroism (TDDFT/ECD) calculations. Compounds 2, 3 and 9 showed moderate inhibition of nitric oxide generation in lipopolysaccharide (LPS) stimulated RAW264.7 cells. © 2024, The Authors. All rights reserved.

关键词： Spectroscopic analysis

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Mycorrhizal fungal community composition in seven orchid species inhabiting Song Mountain, Beijing, China

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Science China(Life Sciences) 2019年第6期62卷 838-847页

作者： Yanhong Chen Yue Gao Linli Song Zeyu Zhao Shunxing Guo Xiaoke Xing Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of Education Institute of Medicinal Plant Development Chinese Academy of Medical Sciences and Peking Union Medical College

Mycorrhizal fungi play an important role in the germination and growth of orchids essentially influencing their survival,abundance, and spatial distribution. In this study, we investigated the composition of the mycorrhizal fungal community in seven terrestrial orchid species inhabiting Song Mountain, Beijing, China, using Illumina MiSeq high-throughput sequencing. The mycorrhizal communities in the seven orchids were mainly composed of members of the Ceratobasidiaceae, Sebacinales, and Tulasnellaceae, while a number of ectomycorrhizal fungi belonging to the Russulaceae, Tricholomataceae, Thelephoraceae, and Cortinariaceae were occasionally observed. However, the dominant fungal associates and mycorrhizal community differed significantly among the orchid species as well as subhabitats. These findings confirm the previous observation that sympatric orchid species show different preferences for mycorrhizal fungi, which may drive niche partitioning and contribute to their cooccurrence.

关键词： orchid mycorrhiza fungal community terrestrial orchids fungal diversity

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L-NRB alleviates amyotrophic lateral sclerosis by regulating P11-Htr4 signaling pathway

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Biomedicine and Pharmacotherapy 2024年 180卷 117588-117588页

作者： Pan, Yunfeng Sun, Xiao Tian, Yu Yu, Miao Luo, Yun Sun, Xiaobo Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of Education Institute of Medicinal Plant Development Chinese Academy of Medical Sciences & Peking Union Medical College Beijing China Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine Institute of Medicinal Plant Development Peking Union Medical College and Chinese Academy of Medical Sciences Beijing China Key Laboratory of new drug discovery based on Classic Chinese medicine prescription Chinese Academy of Medical Sciences Beijing China

Introduction: L-NRB is a compound formed as a ring cleavage product of butylphthalide and borneol in a molar ratio 1:2. This study aimed to explore the therapeutic effect of L-NRB on amyotrophic lateral sclerosis (ALS) and its possible mechanism. Methods: SOD1-G93A mice were used as an ALS model. Behavioral tests, histopathological staining, Nissl staining, immunohistochemistry, enzyme-linked immunosorbent assays, and Western blotting were used to analyze the therapeutic effect. The underlying mechanism of L-NRB in treating ALS was investigated using transcriptomic analyses. Results: It was found that L-NRB alleviated motor dysfunction, pathological changes in the gastrocnemius muscle, and motor neuron injuries. The results indicated that L-NRB had a neuroprotective function associated with the inhibition of neuroinflammation. The anti-apoptotic effect of L-NRB was found to be related to the regulation of the P11-Htr4 signaling pathway. Conclusion: In summary, the results demonstrated the therapeutic effect of L-NRB on ALS and suggest a promising new therapeutic candidate for ALS. © 2024 The Authors

关键词： amyotrophic lateral sclerosis apoptosis L-NRB neuroinflammation P11-Htr4 signal pathway

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Genome sizes of four important medicinal species in Kadsura by flow cytometry

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Chinese Herbal Medicines 2021年第3期13卷 416-420页

作者： Jing Xu Xue-ping Wei Jiu-shi Liu Yao-dong Qi Ben-gang Zhang Hai-tao Liu Pei-gen Xiao Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of EducationInstitute of Medicinal Plant DevelopmentChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100193China Engineering Research Center of Tradition Chinese Medicine Resource Ministry of EducationInstitute of Medicinal Plant DevelopmentChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100193China

Objective:Dianjixueteng is a geoherb in Yunnan Province,the source plant of which is Kadsura ***,the formation of this geoherb is not clear in genetic mechanism,in which genome size is the first step that should be known on the genomic *** this study we aimed to estimate the genome sizes of source plants of *** and three related herbs ***,***,and *** by flow cytometry(FCM)and make a ***:The genome sizes of ***,***,*** and ***,i.e.,the source plants of Dianjixueteng and its relative medicinal materials,were estimated by *** nuclei of *** were isolated using modified LB01 buffer,for the rest species,by the Galbraith’s ***:The genome sizes of ***,***,***,and *** were 7.36,7.12,7.01,and 5.15 pg/1 C,*** size of *** had no significant variation with those of *** and ***(P=0.296),which was significantly larger than that of ***:Genome size can not distinguish *** from *** and ***,but could distinguish them from ***,which lays the foundation for future studies on genetic mechanism of the geoherb formation.

关键词： Dianjixueteng Flow cytometry Genome size Kadsura interior A.C.Smith

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Highland barley improves lipid metabolism, liver injury, antioxidant capacities and liver functions in high-fat/cholesterol diet mice based on gut microbiota and LC-MS metabonomics

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Food Bioscience 2022年第6期50卷 982-1003页

作者： Xiang Li Yan Du Zhaoxin Tu Chengping Zhang Li Wang The Key Laboratory of Industrial Biotechnology Ministry of EducationJiangnan UniversityLihu Road 1800Wuxi214122China National Engineering Research Center for Cereal Fermentation and Food Biomanufacturing Jiangnan UniversityLihu Road 1800Wuxi214122China Jiangsu Provincial Engineering Research Center for Bioactive Product Processing Jiangnan UniversityLihu Road 1800Wuxi214122China Qinghai Huashi Technology Investment Management Co. Ltd(Qinghai Engineering Technology Research Institute for Comprehensive Utilization of Highland Barley Resources)XiningQinghai810016China

Highland barley (HB) possesses a series of properties such as regulating lipid metabolism and attenuating liver injury. Our study aimed to investigate the effect of HB, highland barley bran (HBB), whole grain highland barley (WGHB) on lipid metabolism, liver inflammation, gut microbiota and metabolite profiles in high-fat/cholesterol (HFCD) diet mice. 5 treatment groups were fed a normal control diet or a HFCD with or without HB supplementation for 10 weeks. The results showed that HB especially HBB significantly improved lipid parameters, liver function and injury and blood glucose indexes related to hyperlipidemia compared with HFCD group. In addition, HBB recovered the disorder of gut microbiota by increasing Bacteroidetes /Firmicutes ratio and Lactobacillus and Allobaculum abundances, and decreasing Proteobacteria abundance related to lipid metabolism bacteria. HBB enhanced the levels of 6 short chain fatty acids induced by HFCD. Fecal metabolomics analysis showed that the important differential metabolites between HBB group and HFCD group were deoxycholic acid, myclobutanil and cis -4-Hydroxy-D-proline, and the important differential metabolic pathways were arachidonic acid metabolism, tyrosine metabolism and bile secretion. Results suggested that HBB was an effective dietary intervention candidate to ameliorate hyperlipidemia.

关键词： Highland barley Lipid metabolism High-fat/cholesterol diet Gut microbiota Metabolomics

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