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Yonarolide A, an unprecedented furanobutenolide-containing norcembranoid derivative formed by photoinduced intramolecular[2+2] cycloaddition

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Chinese Chemical Letters 2023年第2期34卷 420-424页

作者： Yeqing Du Ligong Yao Xuwen Li Yuewei Guo School of Chinese Materia Medica Nanjing University of Chinese MedicineNanjing 210023China State Key Laboratory of drug research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China drug discovery Shandong Laboratory Bohai Rim Advanced Research Institute for Drug DiscoveryYantai 264117China

Eight polycyclic furanobutenolide-containing norcembrane diterpenoids featuring C19 frameworks(1–8)were rapidly recognized and isolated from the Hainan soft coral Sinularia sp. by the HSQC-based small molecule accurate recognition technology. Yonarolide A(1a), featuring an unprecedented 5/6/4/4/7 pentacyclic ring skeleton, was surprisingly obtained as a transformed product by leaving compound 1 under indoor natural light, and was further proved to be a [2 + 2] cycloaddition product of 1 by photochemical reaction. The absolute stereochemistry of 1a and the three known norcembrane diterpenoids 1, 4, and7 were determined by using X-ray diffraction(XRD) analyses. Further, with the aid of XRD analysis, the structure of scabrolide B(2), which was previously reported of possessing 5/6/7 tricyclic skeleton, was firmly revised as 2a with the rare inelegane skeleton featured by the highly oxygenated 5/7/6 tricyclic carbocycle.

关键词： Soft coral Sinularia Norcembranoid Photocycloaddition SMART method

Determination of bioactive components in the fruits of Cercis chinensis Bunge by HPLC-MS/MS and quality evaluation by principal components and hierarchical cluster analyses

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Journal of Pharmaceutical Analysis 2021年第4期11卷 465-471页

作者： Yuan Hong Xiaoyan Liao Zilin Chen Key Laboratory of Combinatorial Biosynthesis and drug discovery Ministry of EducationHubei Province Engineering and Technology Research Center for Fluorinated PharmaceuticalsSchool of Pharmaceutical SciencesWuhan UniversityWuhan430071China State Key Laboratory of Transducer technology Chinese Academy of SciencesBeijing100080China

The fruits of leguminous plants Cercis Chinensis Bunge are still overlooked although they have been reported to be antioxidative because of the limited information on the phytochemicals of *** fruits.A simple,rapid and sensitive HPLC-MS/MS method was developed for the identification and quantitation of the major bioactive components in *** *** polyphenols were identified,which are first reported in *** ***,ten components were simultaneously *** validated quantitative method was proved to be sensitive,reproducible and ***,it was applied to analyze batches of *** fruits from different phytomorph and *** principal components analysis(PCA)realized visualization and reduction of data set dimension while the hierarchical cluster analysis(HCA)indicated that the content of phenolic acids or all ten components might be used to differentiate *** fruits of different phytomorph.

关键词： C.chinensis fruits HPLC-MS/MS Polyphenols Principal components analysis Hierarchical cluster analysis

Emerging nanomedicine-based therapeutics for hematogenous metastatic cascade inhibition:Interfering with the crosstalk between “seed and soil”

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Acta Pharmaceutica Sinica B 2021年第8期11卷 2286-2305页

作者： Junyu Wu Yang Long Man Li Qin He Key Laboratory of drug-Targeting and drug Delivery System of the Education Ministry Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial TechnologyWest China School of Pharmacy Sichuan UniversityChengdu 610064China

Despite considerable progresses in cancer treatment,tumor metastasis is still a thorny issue,which leads to majority of cancer-related *** hematogenous metastasis,the concept of"seed and soil"suggests that the crosstalk between cancer cells(seeds)and premetastatic niche(soil)facilitates tumor *** efforts have been dedicated to inhibit the tumor metastatic cascade,which is a highly complicated process involving various pathways and biological ***,satisfactory therapeutic outcomes are rarely observed,since it is a great challenge to thwart this multi-phase *** advances in nanotechnology-based drug delivery systems have shown great potential in the field of anti-metastasis,especially compared with conventional treatment methods,which are limited by serious side effects and poor *** this review,we summarized various factors involved in each phase of the metastatic cascade ranging from the metastasis initiation to *** we reviewed current approaches of targeting these factors to stifle the metastatic cascade,including modulating primary tumor microenvironment,targeting circulating tumor cells,regulating premetastatic niche and eliminating established ***,we highlighted the multiphase targeted drug delivery systems,which hold a better chance to inhibit ***,we demonstrated the limitation and future perspectives of nanomedicine-based anti-metastasis strategies.

关键词： Tumor metastasis drug delivery systems Nanomedicine Metastatic cascade Seed and soil Tumor microenvironment Circulating tumor cells Premetastatic niche

Targeted delivery of hyaluronic acid nanomicelles to hepatic stellate cells in hepatic fibrosis rats

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Acta Pharmaceutica Sinica B 2020年第4期10卷 693-710页

作者： Wenhao Li Chuchu Zhou Yao Fu Tijia Chen Xing Liu Zhirong Zhang Tao Gong Key Laboratory of drug-Targeting and drug Delivery System of the Education Ministry Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial TechnologyWest China School of PharmacySichuan UniversityChengdu 610064China

Hepatic fibrosis is one kind of liver diseases with a high mortality rate and *** activation and proliferation of hepatic stellate cells(HSCs)is the most fundamental reason of hepatic *** are no specific and effective drug delivery carriers for the treatment of hepatic fibrosis at *** found that when hepatic fibrosis occurs,the expression of CD44 receptors on the surface of HSCs is significantly *** on this finding,we designed silibinin-loaded hyaluronic acid(SLB-HA)micelles to achieve the treatment of hepatic ***,we constructed liver fibrosis rat model using Sprague-Dawley *** demonstrated that HA micelles had specific uptake to HSCs in vitro while avoiding the distribution in normal liver cells and the phagocytosis of ***,HA micelles showed a significant liver targeting effect in vivo,especially in fibrotic liver which highly expressed CD44 *** addition,SLB-HA micelles could selectively kill activated HSCs,having an excellent anti-hepatic fibrosis effect in vivo and a significant sustained release effect,and also had a good biological safety and ***,HA micelles represented a novel nanomicelle system which showed great potentiality in anti-hepatic fibrosis drugs delivery.

关键词： Nanomicelles Hyaluronic acid Hepatic stellate cells Hepatic fibrosis Silibinin

APOBEC3B and IL-6 form a positive feedback loop in hepatocellular carcinoma cells

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Science China(Life Sciences) 2017年第6期60卷 617-626页

作者： Shuran Li Xueyang Bao Duowei Wang Linjun You Xianjing Li Hongbao Yang Jinsong Bian Yun Wang Yong Yang State Key Laboratory of Natural Medicines Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease Center for New Drug Safety Evaluation and Research China Pharmaceutical University Department of Pharmacology Yong Loo Lin School of Medicine National University of Singapore

APOBEC3 protein families, a DNA cytidine deaminase, were up-regulated in multiple tumors. However, the relationship between Hepatocellular carcinoma(HCC) and APOBEC3B(A3B) remains unknown. It has been confirmed that interleukin-6(IL-6)has significant impacts on oncogenesis of HCC. Here, we reported that the expression of IL-6 was substantially up-regulated by A3 B in HepG2 cells. A3 B induced IL-6 expression through relocating HuR to enhance the IL-6 mRNA stability. Further analysis indicated that IL-6 also increased the expression of A3 B through JAK1/STAT3 signaling pathway, which formed a positive feedback to maintain the continuous expression of A3 B and IL-6, and thereby promoted the prolonged non-resolving inflammation. Collectively, these findings suggest that A3 B is essential for oncogenesis of HCC, and is a potential target for preventive intervention.

关键词： APOBEC3B interleukin-6 hepatitis hepatocellular carcinoma HuR

Development of the novel ACLY inhibitor 326E as a promising treatment for hypercholesterolemia

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Acta Pharmaceutica Sinica B 2023年第2期13卷 739-753页

作者： Zhifu Xie Mei Zhang Qian Song Long Cheng Xinwen Zhang Gaolei Song Xinyu Sun Min Gu Chendong Zhou Yangming Zhang Kexin Zhu Jianpeng Yin Xiaoyan Chen Jingya Li Fajun Nan State Key Laboratory of drug research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China Burgeon Therapeutics Co. Ltd.Shanghai 201203China drug discovery Shandong Laboratory Bohai Rim Advanced Research Institute for Drug DiscoveryYantai 264117China

Hepatic cholesterol accumulation is an important contributor to hypercholesterolemia,which results in atherosclerosis and cardiovascular disease(CVD).ATP-citrate lyase(ACLY)is a key lipogenic enzyme that converts cytosolic citrate derived from tricarboxylic acid cycle(TCA cycle)to acetyl-CoA in the ***,ACLY represents a link between mitochondria oxidative phosphorylation and cytosolic de novo *** this study,we developed the small molecule 326E with an enedioic acid structural moiety as a novel ACLY inhibitor,and its CoA-conjugated form 326E-CoA inhibited ACLY activity with an IC_(50)=5.31±1.2μmol/L in vitro.326E treatment reduced de novo lipogenesis,and increased cholesterol efflux in vitro and in vivo.326E was rapidly absorbed after oral administration,exhibited a higher blood exposure than that of the approved ACLY inhibitor bempedoic acid(BA)used for *** 326E treatment in hamsters and rhesus monkeys resulted in remarkable improvement of *** daily oral administration of 326E for 24 weeks prevented the occurrence of atherosclerosis in ApoE^(-/-)mice to a greater extent than that of BA *** together,our data suggest that inhibition of ACLY by 326E represents a promising strategy for the treatment of hypercholesterolemia.

关键词： Hypercholesterolemia Atherosclerosis Liver ATP-Citrate lyase(ACLY) Lipogenesis Cholesterol efflux ACLY inhibitor

Rational Design of Organelle-Targeted Fluorescent Probes:Insights from Artificial Intelligence

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research 2023年第3期2023卷 769-779页

作者： Jie Dong Jie Qian Kunqian Yu Shuai Huang Xiang Cheng Fei Chen Hualiang Jiang Wenbin Zeng Xiangya School of Pharmaceutical Sciences Central South UniversityChangsha 410083P.R.China National Engineering research center of Rice and Byproduct Deep Processing School of Food Science and EngineeringCentral South University of Forestry and TechnologyChangsha 410004P.R.China State Key Laboratory of drug research Drug Discovery and Design CenterShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203P.R.China

Monitoring the physiological changes of organelles is essential for understanding the local biological information of cells and for improving the diagnosis and therapy of ***,fluorescent probes are considered as the most powerful tools for imaging and have been widely applied in biomedical ***,the expected targeting effects of these probes are often inconsistent with the real *** design of fluorescent probes mainly depends on the empirical knowledge of researchers,which was inhibited by limited chemical space and low ***,we proposed a novel multilevel framework for the prediction of organelle-targeted fluorescent probes by employing advanced artificial intelligence *** this way,not only the targeting mechanism could be interpreted beyond intuitions but also a quick evaluation method could be established for the rational ***,the targeting and imaging powers of the optimized and synthesized probes based on this methodology were verified by quantitative calculation and experiments.

关键词： inhibited diagnosis Probe

Novel strategies for the treatment of osteoarthritis based on biomaterials and critical molecular signaling

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Journal of Materials Science & technology 2023年第18期149卷 42-55页

作者： Xingyun Huang Zhiyong Wang Huaiyu Wang Di Chen Liping Tong research center for Computer-aided drug discovery Shenzhen Institute of Advanced TechnologyChinese Academy of SciencesShenzhen 518055China Faculty of Pharmaceutical Sciences Shenzhen Institute of Advanced TechnologyChinese Academy of SciencesShenzhen 518055China University of Chinese Academy of Sciences Beijing 100049China center for Human Tissues and Organs Degeneration Shenzhen Institute of Advanced TechnologyChinese Academy of SciencesShenzhen 518055China

Osteoarthritis(OA)is a degenerative disease involving entire *** is often initiated from the low-grade inflammation in synovial tissue and then affects articular cartilage and subchondral *** risk factors,such as aging,mechanical overloading,trauma,overuse,*** involved in OA *** approaches have been utilized to repair cartilage *** them,biomaterials-based mes-enchymal stromal cell(MSCs)therapy is considered as the most promising *** burgeoning material science and manufacturing technologies,such as 3D printing,allow us to mimic native articu-lar cartilage and regulate the artificial cartilage development,regeneration and functional *** this review article,we will summarize the recent progress of biomaterials combined with MSCs or chon-drocytes in repairing cartilage damage induced by *** typical natural and synthetic biomaterials,such as collagen,alginate,hyaluronic acid and poly(ethylene glycol),polylactide acid,polyurethane,*** cartilage repairing will be ***,critical signaling pathways associated with the pro-gression of OA,as well as the targeted pharmacologic,genetic therapies and tissue engineering scaffolds for OA and cartilage repairing are *** will also provide our prospects for future directions in this active research area.

关键词： Osteoarthritis Cartilage Repairing Biomaterials 3D printing Signaling pathways

Regulatory role of peroxynitrite in advanced glycation end products mediated diabetic cardiovascular complications

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World Journal of Diabetes 2024年第3期15卷 572-574页

作者： Asis Bala Pharmacology and drug discovery research Laboratory Division of Life SciencesInstitute of Advanced Study in Science and TechnologyGuwahati 781035AssamIndia

The Advanced Glycation End Products(AGE)binding with its receptor can increase reactive oxygen species(ROS)generation through specific signaling *** effect of superoxide(O2-)and O2-mediated ROS and reactive nitrogen species depends on their concentration and location of *** oxide(NO)has anti-inflammatory and anticoagulant properties and a vasodilation effect,but NO can be deactivated by reacting with O_(2)^(-).This reaction between NO and O2-produces the potent oxidant ONOO−.Therefore,ONOO-'s regulatory role in AGEs in diabetic cardiovascular complications must considered as a regulator of cardiovascular complications in diabetes.

关键词： Diabetes Cardiovascular complication Advanced glycation end products Reactive oxygen species Reactive nitrogen species Peroxynitrite