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Pomegranate leaf attenuates lipid absorption in the small intestine in hyperlipidemic mice by inhibiting lipase activity

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Chinese Journal of Natural Medicines 2017年第10期15卷 732-739页

作者： YU Xuan WANG Xin-Pei LEI Fan JIANG Jing-Fei LI Jun XING Dong-Mang DU Li-Jun laboratory of Molecular Pharmacology and pharmaceutical Sciences School of Life Sciences Tsinghua University Beijing100084 China School of pharmaceutical Sciences Tsinghua University Beijing 100084 China state key laboratory of innovative drugs and efficient energy-saving pharmaceutical equipment Jiangxi University of Chinese Medicine Nancang 330006 China

Pomegranate leaf(PGL)has a definite role in regulating lipid ***,pharmacokinetic results show the main active ingredient,ellagic acid,in PGL has lower oral bioavailability,suggesting that the lipid-lowering effect of PGL may act through inhibiting lipid absorption in the small *** results demonstrated that pomegranate leaf and its main active ingredients(i.e.,ellagic acid,gallic acid,pyrogallic acid and tannic acid)were capable of inhibiting pancreatic lipase activity in *** computational molecular docking,the four ingredients had good affinity for pancreatic *** lipid overload experiments showed that a large dosage of PGL significantly reduced serum total cholesterol(TG)and triglycerides(TC)levels in addition to inhibiting intestinal lipase activity,which demonstrated that PGL could inhibit lipase activity and reduce the absorption of *** also found that PGL could reverse the reduced tight-junction protein expression due to intestinal lipid overload,promote Occludin and Claudin4 expression in the small intestine,and enhance the intestinal mucosal *** conclusion,we demonstrated that PGL can inhibit lipid absorption and reduce blood TG and TC by targeting pancreatic lipase,promoting tight-junction protein expression and thereby preventing intestinal mucosa damage from an overload of lipids in the intestine.

关键词： Pomegranate leaf Lipase activity Hyperlipidemia Ellagic acid Pyrogallic acid

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An efficient ionic liquid supported divergent assembly of 3,6-branched glucosamine-containing pentasaccharide

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Chinese Chemical Letters 2014年第12期25卷 1525-1530页

作者： Ze-Shen Gao Sheng Sun Wei Li Qing Ma Qing Li Zhong-Jun Li The state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical SciencesPeking University

We utilized the glycosyl acceptor tagging method with ionic liquid support for synthesis of the core segment of Clostridium botulinum C2 toxin ligand through a divergent synthetic strategy without chromatographic *** total yield was 57.1% and the reaction was completed in 10 *** efficient ionic liquid supported glycosylation and purification procedure was applied for the synthesis of branched glucosamine-containing oligosaccharides for the first time,which expanded the scope of ionic liquid supported synthesis of biologically important oligosaccharides.

关键词： Ionic liquid Oligosaccharide Rapid assembling

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Revealing the Distribution of Aggregation-Induced Emission Nanoparticles via Dual-Modality Imaging with Fluorescence and Mass Spectrometry

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Research 2021年第1期2021卷 826-834页

作者： Liucheng Mao Yuming Jiang Hui Ouyang Yulin Feng Ruoxin Li Xiaoyong Zhang Zongxiu Nie Yen Wei The key laboratory of Bioorganic Phosphorus Chemistry&Chemical Biology(Ministry of Education) Department of ChemistryTsinghua UniversityBeijing 100084China Beijing National laboratory for Molecular Sciences Key Laboratory of Analytical Chemistry for Living BiosystemsInstitute of ChemistryChinese Academy of SciencesBeijing 100190China state key laboratory of innovative Drug and efficient energy-saving pharmaceutical equipment Jiangxi University of Traditional Chinese MedicineNanchang 330006China Department of Chemistry Nanchang University999 Xuefu AvenueNanchang 330031China

Aggregation-induced emission nanoparticles(AIE NPs)are widely used in the biomedical ***,understanding the biological process of AIE NPs via fluorescence imaging is challenging because of the strong background and poor penetration ***,we present a novel dual-modality imaging strategy that combines fluorescence imaging and label-free laser desorption/ionization mass spectrometry imaging(LDI MSI)to map and quantify the biodistribution of AIE NPs(TPAFN-F127 NPs)by monitoring the intrinsic photoluminescence and mass spectrometry signal of the AIE *** discovered that TPAFN-F127 NPs were predominantly distributed in the liver and spleen,and most gradually excreted from the body after 5 *** accumulation and retention of TPAFN-F127 NPs in tumor sites were also confirmed in a tumor-bearing mouse *** a proof of concept,the suborgan distribution of TPAFN-F127 NPs in the spleen was visualized by LDI MSI,and the results revealed that TPAFN-F127 NPs were mainly distributed in the red pulp of the spleen with extremely high concentrations within the marginal *** in vivo toxicity test demonstrated that TPAFN-F127 NPs are nontoxic for a long-term *** dual-modality imaging strategy provides some insights into the fine distribution of AIE NPs and might also be extended to other polymeric NPs to evaluate their distribution and drug release behaviors in vivo.

关键词： spleen distribution retention

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Recent advances in the preparation of Fmoc-SPPS-based peptide thioester and its surrogates for NCL-type reactions

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Science China Chemistry 2017年第2期60卷 201-213页

作者： Hongxing Li Suwei Dong state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical Sciences Peking University Beijing 100191 China

Solid phase peptide synthesis(SPPS)based on Fmoc chemistry has become a commonly used technique in peptide chemistry,as it can be easily conducted using automated machine,and not requiring highly toxic HF in comparison to *** the fast development in the emerging field of protein chemical synthesis,many efforts have been endeavored aiming to find more efficient methods for preparing peptide fragments required in ligation *** review briefly summarizes recent advances in the engineering and modification of Fmoc-SPPS-derived peptides,which can be used as the N-terminal fragments in a native chemical ligation(NCL)or NCL-type ligation reactions.

关键词： native chemical ligation Fmoc-SPPS peptide thioester protein chemical synthesis

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A novel method for the synthesis of sulfur substituted-cyclopyrophosphate of cADPR analogs

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Chinese Chemical Letters 2014年第12期25卷 1583-1585页

作者： Ren-Min Wu Na Qi Yu-Wen Jia Zhu Guan Liang-Ren Zhang Li-He Zhang Zhen-Jun Yang state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical SciencesPeking University

A facile and efficient protocol for the synthesis of sulfur substituted-cyclopyrophosphate of cIDPRE（P_S^1-cIDPRE） was *** key step was the cyclization process which was completed by the sulfur substituted cyclizati... 详细信息

关键词： cADPR cIDPRE Phosphoramidite strategy Cyclopyrophosphate

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Synthesis of L-glucose and L-galactose derivatives from D-sugars

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Chinese Chemical Letters 2014年第9期25卷 1220-1224页

作者： Tian-Yu Xia Yang-Bing Li Zhao-Jun Yin Xiang-Bao Meng Shu-Chun Li Zhong-Jun Li The state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical SciencePeking University

An efficient route to prepare L-glucose and L-galactose is described. The L-sugars are achieved by using the strategy of switching the functional groups at C1 and C5 of D-glucose and D-mannose. The oxidation and reduction of the silyl enol ether at C1 and the lead（IV） tetraacetate mediated oxidative decarboxylation at C5 are the key steps. L-Glucose and L-galactose are prepared in a convenient and inexpensive way.

关键词： Carbohydrates L-Hexoses Head-to-tail inversions Oxidation Decarboxylation One-pot procedure

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A five-component one-pot synthesis of phosphatidylinositol pentamannoside(PIM_5)

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Chinese Chemical Letters 2018年第9期29卷 1340-1342页

作者： Dong Wang De-Cai Xiong Xin-Shan Ye state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical Sciences Peking University

A practical and efficient synthesis of phosphatidylinositol pentamannoside （PIM5） was achieved based on a five-component one-pot sequential glycosylation protocol with exclusive regio- and stereo-selectivity. Two regioselective sequential glycosylations on inositol and p-tolyl thioglycosides as the sole type of building blocks made this protocol to avoid the tedious protective group manipulations. This synthetic strategy provides access to other important glycolipids with similar structures.

关键词： Phosphatidylinositol pentamannoside Glycosylation Preactivation One-pot synthesis Thioglycoside

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Copper-catalyzed enantioselective cyanation of benzylic C–H bonds via radical relay

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Science China Chemistry 2017年第1期60卷 105-106页

作者： Yujie Liang Ning Jiao state key laboratory of Natural and Biomimetic drugs School of Pharmaceutical Sciences Peking University Beijing 100191 China

Direct methods that enable stereoselective functionalization of C（sp^3）–H bonds could facilitate efficient preparation of therapeutics and agrochemicals,and shall have a major effect on the discovery and development of new *** the transformations through C（sp^2）–H bond cleavage have been significantly developed in the past decades,the direct C（sp^3）–H functionalization,especially the asymmetric transformation is still a big challenge.

关键词： Carbon Copper Cyanides Drug products

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The ethyl acetate extraction of Pileostegia tomentella(ZLTE) exerts anti-cancer effects on H1299 cells via ROS-induced canonical apoptosis

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Chinese Journal of Natural Medicines 2020年第7期18卷 508-516页

作者： FAN Qiu-Mei ZHAO Wen-Tong YUAN Renyikun WANG Qin-Qin ZHANG Li-Feng GAO Hong-Wei LENG Jing YANG Shi-Lin College of Pharmacy Guangxi University of Chinese MedicineNanning 530000China Guangxi Engineering Technology Research Center of Advantage Chinese Patent Drug and Ethnic Drug Development Nanning 530200China state key laboratory of innovative Drug and efficient energy-saving pharmaceutical equipment Jiangxi University of Traditional Chinese MedicineNanchang 330004China Guangxi key laboratory of Translational Medicine fo r Treating High-Incidence Infectious Diseases with Integrative Medicine NanningGuangxi 530200China Guangxi key laboratory of Efficacy Study on Chinese Materia Medica Nanning 530200China

Lung cancer is the leading cause of cancer death and the most common malignant tumor, the long-term survival of which has stagnated in the past several *** tomentella *** is a traditional Chinese medicine called "Zhongliuteng"(ZLT) in the pharmacopeia, which has been proved to possess a potent anti-tumor effect on various *** this study, the effects of ZLT N-butanol extraction(ZLTN) and ZLT ethyl acetate extraction(ZLTE) on the viability of non-small cell lung cancer cell(NSCLC) lines H1299 and A549 were ***, we firstly reported that ZLTE significantly inhibited H1299 cells growth without affecting the release of lactate dehydrogenase(LDH).In addition, ZLTE induced caspase-dependent apoptosis in a concentration-dependent manner and increased the expression cleaved-PARP and decreased pro-caspase-3, pro-caspase-7, pro-caspase-8, and ***, ZLTE increased the level of cellular reactive oxygen species(ROS) in H1299 cells to lead to apoptosis,which was reversed by N-acetyl-cysteine(NAC).Taken together, our results revealed that ZLTE induced caspase-dependent apoptosis via ROS generation, suggesting that ZLTE is a promising herbal medicine for the treatment of NSCLC.

关键词： Pileostegia tomentella Lung cancer Apoptosis ROS

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CsOH catalyzed aerobic oxidative synthesis of p-quinols from multi-alkyl phenols under mild conditions

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Science China Chemistry 2015年第8期58卷 1334-1339页

作者： Yu-Feng Liang Kai Wu Zhiqing Liu Xiaoyang Wang Yujie Liang Chenjiang Liu Ning Jiao state key laboratory of Natural and Biomimetic drugs School of pharmaceutical Sciences Peking University The key laboratory of Oil and Gas Fine Chemicals Ministry of Education & Xinjiang Uygur Autonomous Region Xinjiang University

p-Quinols are ubiquitous structural motifs of various natural products and pharmaceutical compounds,and versatile building blocks in synthetic *** reported methods for the synthesis of p-quinol require stoichiometric amounts of *** oxygen is considered as an ideal oxidant due to its natural,inexpensive,and environmentally friendly *** the ongoing research of C–H bond hydroxylation,we found that multi-alkyl phenols could react with molecular oxygen under mild ***,we describe an efficient oxidative de-aromatization of multi-alkyl phenols to p-quinols.1 atm of molecular oxygen was used as the *** multi-alkyl phenols could react smoothly at room *** labeling experiment was also performed,and the result proved that the oxygen atom in the produced hydroxyl group is from molecular oxygen.

关键词： p-quinol molecular oxygen de-aromatization carbanion cesium hydroxide

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