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Chinese Journal of Structural Chemistry 2018年第7期37卷 1071-1077页

作者：李午戊郑敏燕李小博张尊听 College of Chemistry & Chemical Engineering Xianyang Normal University key laboratory of the Ministry of Education for Medicinal Resources and Natural pharmaceutical Chemistry National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China and School of Chemistry and Chemical Engineering Shaanxi Normal University

The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673（8）, b = 17.9938（15）, c = 21.2004（17） A, V = 3611.5（5） A3, Z = 8, μ = 0.6726 mm^（-1）, Dc = 1.795 g/cm3, F（000） = 2080, the final R = 0.0358 and wR = 0.0644 with I 2σ（I）. The results show that the addition reaction occurs at the carbon-carbon double bond（C2 and C3） of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells（K562）, human breast cancer cells（MCF-7） and human lung cancer cells（A549）. 1 exhibited potent antitumor activities against human leukemia cells（K562） with the IC50 values of 18.9 μmol/L.

关键词： 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one spectroscopic property crystal structure reaction mechanisms antitumor activity

A new linearly-combined bi-exponential model for kinetic analysis of the isometric relaxation process of Bufo gastrocnemius under electric stimulation in vitro

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2007年第12期8卷 867-874页

作者： GUO Rui LI Sheng-bing ZHAO Li-na ZHAO Yun-sheng LU Wei YUAN Pei DENG Ping LIAO Fei Unit of Biochemical Pharmacology and Protein Biotechnology Chongqing Key Laboratory of Biochemistry and Moleczdar Pharmacology College of Pharmaceutical Sciences Chongqing Medical University Chongqing 400016 China

There was a slow-relaxing tail of skeletal muscles in vitro upon the inhibition of Ca2+-pump by cyclopiazonic acid (CPA). Herein, a new linearly-combined bi-exponential model to resolve this slow-relaxing tail from the fast-relaxing phase was investigated for kinetic analysis of the isometric relaxation process of Bufo gastrocnemius in vitro, in comparison to the single exponential model and the classical bi-exponential model. During repetitive stimulations at a 2-s interval by square pulses of a 2-ms duration at 12 V direct currency (DC), the isometric tension of Bufo gastrocnemius was recorded at 100 Hz. The relaxation curve with tensions falling from 90% of the peak to the 15th datum before next stimulation was analyzed by three exponential models using a program in MATLAB 6.5. Both the goodness of fit and the distribution of the residuals for the best fitting sup- ported the comparable validity of this new bi-exponential model for kinetic analysis of the relaxation process of the control muscles. After CPA treatment, however, this new bi-exponential model showed an obvious statistical superiority for kinetic analysis of the muscle relaxation process, and it gave the estimated rest tension consistent to that by experimentation, whereas both the classical bi-exponential model and the single exponential model gave biased rest tensions. Moreover, after the treatment of muscles by CPA, both the single exponential model and the classical bi-exponential model yielded lowered relaxation rates, nevertheless, this new bi-exponential model had relaxation rates of negligible changes except much higher rest tensions. These results suggest that this novel linearly-combined bi-exponential model is desirable for kinetic analysis of the relaxation process of muscles with altered Ca2+-pumping activity.

关键词： Bufo gastrocnemius Ca^2+ -pump Cyclopiazonic acid (CPA) Linearly-combined bi-exponential model Muscle relaxation rate Residual distribution Rest tension

Solubility and pharmacokinetics determination of chlorogeninc acid

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中国药理学与毒理学杂志 2015年第S1期29卷 113-114页

作者： LiZHANG Wei-shengXU Su-boWANG Guan-huaDU YangLU Beijing city key laboratory of Polymorphic Drugs Research Centre of Polymorphic Drugs Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 China Beijing city key laboratory of Drug Target and Screening Research National Center for pharmaceutical Screening Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 China

OBJECTIVE To enhance the quality and efficiency of chlorogeninc acid by investigating the differences among the chlorogeninc acid polymorphs in bioavailability and *** Determinative method was used to analyze the solubility of chlorogeninc acid polymorphs;solid chlorogeninc acid in different forms were orally administered to the rats,and a HPLC method was established to determinate plasma lever of metabolite-acyclovir and the bioavailability was *** The indirect pharmacokinetic parameters of Chlorogeninc acid,as the metabolites of the form Ⅰ,Ⅱ,Ⅲ,were as follows:cmaxwas 0.37,0.34 and 0.44mg·L-1,respectively;AUC0→twas 0.71,0.76 and 0.79mg·L-1·h,*** The solubility of form Ⅲ was larger than the other forms′.The solubility of Chlorogeninc acid polymorphs:form Ⅰ,form Ⅱ,form Ⅲ were merely the same,there was no statistically significant difference in pharmacokinetic parameters among these three forms.

关键词： chlorogeninc acid polymorphs solubility pharmacoki

AstragalosideⅣameliorates insulin induced insulin resistance in HepG2 cells through reactive oxygen species mediated c-Jun N-terminal kinase pathway

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Journal of Traditional Chinese Medicine 2023年第1期43卷 60-67页

作者： YE Xiaomei XING Xiaowei YUAN Kangrui WANG Dongming WU Dudu CHEN Zhi YU Zhiqiang School of Pharmacy Guangdong Medical UniversityDongguan 523808China Department of Clinical Pharmacy SSL Central Hospital of Dongguan City(the Third People's Hospital of Dongguan City)Dongguan 523326China Department of Pharmacy Central People's Hospital of ZhanjiangGuangzhou 510515China School of pharmaceutical Sciences Guangdong Provincial Key Laboratory of New Drug ScreeningSouthern Medical UniversityZhanjiang 524037China

OBJECTIVE:To investigate the effects and elucidate the mechanism of Astragaloside IV(AS-IV)for insulin resistance(IR)and type 2 diabet es mellitus(T2DM).METHODS:CCK8 kit was used to detect cell viability,glucose detection kit was used to detect the concentration of glucose in cell supernatant,reactive oxygen species(ROS)detection kit and Western blot were used to explore the mechanism of Astragaloside IV(AS-IV)in improving IR.A diabetic rat model was also established by feeding high sugar and fat diet and streptozotocin(STZ)*** treatment with AS-IV,rosiglitazone(ROZ),or normal saline,the fasting blood glucose(FBG),C peptide(C-P),tumor necrosis factor-α(TNF-α),interleukin-6(IL-6)and the glucose tolerance were ***:AS-IV could effectively reduce the content of ROS and increase the glucose uptake in high insulintreated IR-type HepG 2 *** results of molecular mechanisms indicated that AS-IV could improve insulin resistance by reducing JNK phosphorylation and regulating c-Jun N-terminal kinase(JNK)downstream protein ***,AS-IV could significantly reduce the levels of FBG,TNF-α,IL-6 and the glucose tolerance in diabetic rats(P<0.05 or<0.01).The high and medium dose groups of AS-IV could significantly increase the C-P levels in diabetic rats(P<0.05 or<0.01).CONCLUSIONS:Our results indicated that AS-IV improve liver IR through the JNK pathway and ROS,which meant a new molecular target for the treatment of *** AS-IV also helped to prevent and improved the insulin resistance of rats.

关键词： AstragalosideⅣ Insulin resistance Glucose consumption ROS JNK HepG2 cells

The transcriptional regulators of virulence for Pseudomonas aeruginosa:Therapeutic opportunity and preventive potential of its clinical infections

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Genes & Diseases 2023年第5期10卷 2049-2063页

作者： Xiaolong Shao Chunyan Yao Yiqing Ding Haiyan Hu Guoliang Qian Mingliang He Xin Deng College of Plant Protection Laboratory of Plant ImmunityKey Laboratory of Integrated Management of Crop Diseases and PestsNanjing Agricultural UniversityNanjingJiangsu 210095China Department of Biomedical Sciences City University of Hong KongKowloon TongHong Kong SARChina School of pharmaceutical Sciences Sun Yat-Sen UniversityUniversity TownGuangzhouGuangdong 510006China Tung Biomedical Sciences Centre City University of Hong KongKowloon TongHong Kong SARChina Shenzhen Research Institute City University of Hong KongShenzhenGuangdong 518057China

In Pseudomonas aeruginosa(***),transcription factors(TFs)are important mediators in the genetic regulation of adaptability and pathogenicity to respond to multiple environmental stresses and host *** *** genome harbours 371 putative TFs;of these,about 70 have been shown to regulate virulence-associated phenotypes by binding to the promoters of their target *** the past three decades,several techniques have been applied to identify TF binding sites on the *** genome,and an atlas of TF binding patterns has been *** virulence-associated regulons of TFs show complex crosstalk in ***'s regulatory *** this review,we summarise the recent literature on TF regulatory networks involved in the quorum-sensing system,biofilm formation,pyocyanin synthesis,motility,the type III secretion system,the type VI secretion system,and oxidative stress *** discuss future perspectives that could provide insights and targets for preventing clinical infections caused by *** based on the global regulatory network of transcriptional regulators.

关键词： Crosstalk Pseudomonas aeruginosa Regulatory network Transcriptional regulators Virulence

Differentiation of Belamcandae Rhizoma and Iridis Tectori Rhizoma by Thin-Layer Chromatography and High-Performance Liquid Chromatography

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World Journal of Traditional Chinese Medicine 2021年第1期7卷 63-70页

作者： Lu-Lu Xu Yang Zhang Yue Chai Kuan Chen Hai-Dong Wang Chun-Guo Yang Min Ye Xue Qiao State key laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijingChina Shandong Medicinal Materials Co.LTD 28 Gongqingtuan RoadShizhong DistrictJinan CityShandong 250000China

Objective:Belamcandae Rhizoma and Iridis Tectori Rhizoma are easily confused with each *** main objective of this study is to distinguish them using chemical *** and Methods:Thin-layer chromatography(TLC)and high-performance liquid chromatography(HPLC)fingerprint methods were established to compare the chemical profile,while HPLC quantitation was used to determine the contents of three isoflavones in thirty batches of Belamcandae Rhizoma and Iridis Tectori Rhizoma ***:The two herbs could be distinguished by TLC using acetic acid-n hexane-ethyl acetate(1:90:80 v/v/v)as the mobile phase,according to the fluorescent band under 366 nm at R_(f) *** total,12 compounds were identified in the 24-min HPLC *** similarity coefficient between the two herbs was 0.54±***(1),tectoridin(2),iridin(3),irigenin(5),irisflorentin(6),and iristectorin A(9)were the main peaks in Belamcandae Rhizoma,while tectoridin(2)and tectorigenin(4)were the major peaks in Iridis Tectori *** contents of 2 in Iridis Tectori Rhizoma(2.50±0.20%)were 8.93 times higher than that of Belamcandae Rhizoma(0.28±0.08%),while the ones of 5 and 6 were slightly lower in Iridis Tectori ***:The study established fast and effective methods to distinguish Belamcandae Rhizoma from Iridis Tectori Rhizoma.

关键词： Belamcandae Rhizoma high-performance liquid chromatography fingerprint high-performance liquid chromatography quantitative analysis Iridis Tectori Rhizoma thin-layer chromatography

3, 4-seco-Labdane diterpenoids from the leaves of Callicarpa nudiflora with anti-inflammatory effects

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Chinese Journal of Natural Medicines 2019年第9期17卷 707-712页

作者： WANG Hong-Gang LUO Fu-Kang LEI Xiang YAO Yun-Da LIAO Guo-Chao LIU Zhong-Qiu JIANG Zhi-Hong ZHOU Hua WU Peng Joint laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of China International Institute for Translational Chinese MedicineGuangzhou University of Chinese MedicineGuangzhou 510006China School of Translational Chinese Medicine Guangdong Pharmaceutical UniversityGuangzhou 510006China State key laboratory of Quality Research in Chinese Medicine Macao University of Science and TechnologyMacao 999078China

Four new 3,4-seco-labdane diterpenoids,nudiflopenes J-M,were isolated from the leaves of Callicarpa nudiflora along with six known *** structures of these diterpenoids were determined by comprehensive spectroscopic *** the isolated compounds were evaluated for their inhibitory effects on NO production in LPS-stimulated RPMs and RAW264.7 *** results suggest that nudiflopenes J-M and other four known compounds showed significant inhibitory effects against NO production comparable to the positive control dexamethasone.

关键词： Callicarpa nudiflora Verbenaceae 3,4-seco-Labdane diterpenoid Anti-inflammatory RPMs RAW264.7

Mechanistic engineering of celastrol liposomes induces ferroptosis and apoptosis by directly targeting VDAC2 in hepatocellular carcinoma

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Asian Journal of pharmaceutical Sciences 2023年第6期18卷 157-174页

作者： Piao Luo Qian Zhang Shuo Shen Yehai An Lixia Yuan Yin-Kwan Wong Sizhe Huang Shaohui Huang Jingnan Huang Guangqing Cheng Jiahang Tian Yu Chena Xiaoyong Zhang Weiguang Li Songqi He Jigang Wang Qingfeng Du School of Traditional Chinese Medicine and School of pharmaceutical Sciences Southern Medical UniversityGuangzhou 510515China State key laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs Artemisinin Research Centerand Institute of Chinese Materia MedicaChina Academy of Chinese Medical SciencesBeijing 100700China Department of Biological Sciences National University of SingaporeSingapore 117543Singapore Department of Nephrology Shenzhen key Laboratory of Kidney Diseasesand Shenzhen Clinical Research Centre for GeriatricsShenzhen People’s HospitalThe First Affiliated HospitalSouthern University of Science and TechnologyShenzhen 518020China Department of Health technology and Informatics The Hong Kong Polytechnic UniversityHong Kong 100872China Department of Oncology the Affiliated Hospital of Southwest Medical UniversityLuzhou 646000China National pharmaceutical Engineering Center for Solid Preparation of Chinese Herbal Medicine Jiangxi University of Chinese MedicineNanchang 330006China

Hepatocellular carcinoma(HCC)is one of most common and deadliest ***(Cel),a natural product derived from the Tripterygium wilfordii plant,has been extensively researched for its potential effectiveness in fighting ***,its clinical application has been hindered by the unclear mechanism of ***,we used chemical proteomics to identify the direct targets of Cel and enhanced its targetability and antitumor capacity by developing a Cel-based liposomes in *** demonstrated that Cel selectively targets the voltage-dependent anion channel 2(VDAC2).Cel directly binds to the cysteine residues of VDAC2,and induces cytochrome C release via dysregulating VDAC2-mediated mitochondrial permeability transition pore(mPTP)*** further found that Cel induces ROS-mediated ferroptosis and apoptosis in HCC ***,coencapsulation of Cel into alkyl glucoside-modified liposomes(AGCL)improved its antitumor efficacy and minimized its side *** has been shown to effectively suppress the proliferation of tumor *** a xenograft nude mice experiment,AGCL significantly inhibited tumor growth and promoted *** findings reveal that Cel directly targets VDAC2 to induce mitochondria-dependent cell death,while the Cel liposomes enhance its targetability and reduces side ***,Cel shows promise as a therapeutic agent for HCC.

关键词： Celastrol VDAC2 Ferroptosis Apoptosis Hepatocellular carcinoma Liposomes

Size engineering of 2D MOF nanosheets for enhanced photodynamic antimicrobial therapy

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Chinese Chemical Letters 2023年第9期34卷 219-224页

作者： Baoli Xue Xiwen Geng Haohao Cui Huiying Chen Zhikang Wu Hong Chen Hai Li Zhan Zhou Meiting Zhao Chaoliang Tan Jingguo Li Henan Provincial People’s Hospital People’s Hospital of Zhengzhou UniversityZhengzhou 450003China College of Chemistry and Chemical Engineering Henan Key Laboratory of Function-Oriented Porous MaterialsLuoyang Normal UniversityLuoyang 471934China Luoyang key laboratory of Organic Functional Molecules College of Food and DrugLuoyang Normal UniversityLuoyang 471934China Institute of Advanced Materials(IAM)and key laboratory of Flexible Electronics(KLoFE) Nanjing Tech University(NanjingTech)Nanjing 211816China Department of Chemistry Institute of Molecular Aggregation ScienceTianjin Key Laboratory of Molecular Optoelectronic SciencesTianjin UniversityTianjin 300072China Department of Chemistry and Center of Super-Diamond and Advanced Films(COSDAF) City University of Hong KongHong Kong 999077China Shenzhen Research Institute City University of Hong KongShenzhen 518057China pharmaceutical Sciences laboratory Abo Akademi UniversityTurku 20520Finland

Although porphyrin-based metal-organic frameworks(MOFs)have been widely explored as photosensitizers for photodynamic therapy,how the size will affect the light-induced catalytic activity for generation of reactive oxygen species(ROS)still remain ***,we first report the size-controlled synthesis of two-dimensional(2D)porphyrin-based PCN-134 MOF nanosheets by a two-step solvothermal method to explore the size effect on its PDT performance,thus yielding enhanced photodynamic antimicrobial *** simply controlling the reaction temperature in the synthesis process,the bulk PCN-134 crystal,large PCN-134(L-PCN-134)nanosheets with a lateral size of 2–3μm and thickness of 33.2–37.5 nm and small PCN-134 nanosheets(S-PCN-134)with a lateral size of 160–180 nm and thickness of 9.1–9.7 nm were successfully ***,the S-PCN-134 nanosheets exhibit much higher photodynamic activity for ROS generation than that of the bulk 3D PCN-134 crystal and L-PCN-134 nanosheets under a660 nm laser irradiation,suggesting that the photodynamic activity of PCN-134 MOF increases when the size ***,the S-PCN-134 nanosheets show much enhanced performance when used as a photosensitizer for photodynamic antimicrobial activity and wound healing.

关键词： 2D nanosheets PCN-134 MOFs Size effect Photodynamic therapy Antibacterial

A novel inhibitor of N^(6)-methyladenosine demethylase FTO induces m RNA methylation and shows anti-cancer activities

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Acta Pharmaceutica Sinica B 2022年第2期12卷 853-866页

作者： Guoyou Xie Xu-Nian Wu Yuyi Ling Yalan Rui Deyan Wu Jiawang Zhou Jiexin Li Shuibin Lin Qin Peng Zigang Li Hongsheng Wang Hai-Bin Luo School of pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou 510006China key laboratory of Tropical Biological Resources of Ministry of Education School of Life and Pharmaceutical SciencesHainan UniversityHaikou 570228China Center for Translational Medicine the First Affiliated HospitalSun Yat-sen UniversityGuangzhou 510080China Institute of Systems and Physical Biology Shenzhen Bay LaboratoryShenzhen 518067China

N^(6)-methyladenosine(m^(6)A)modification is critical for m RNA splicing,nuclear export,stability and *** mass and obesity-associated protein(FTO),the first identified m^(6)A demethylase,is critical for cancer ***,we developed small-molecule inhibitors of FTO by virtual screening,structural optimization,and *** a result,two FTO inhibitors namely 18077 and 18097 were identified,which can selectively inhibit demethylase activity of ***,18097 bound to the active site of FTO and then inhibited cell cycle process and migration of cancer *** addition,18097 reprogrammed the epi-transcriptome of breast cancer cells,particularly for genes related to P53 pathway.18097 increased the abundance of m^(6)A modification of suppressor of cytokine signaling1(SOCS1)m RNA,which recruited IGF2 BP1 to increase m RNA stability of SOCS1 and subsequently activated the P53 signaling ***,18097 suppressed cellular lipogenesis via downregulation of peroxisome proliferator-activated receptor gamma(PPARγ),CCAAT/enhancer-binding protein alpha(C/EBPa),and C/EBPβ.Animal studies confirmed that 18097 can significantly suppress in vivo growth and lung colonization of breast cancer ***,we identified that FTO can work as a potential drug target and the small-molecule inhibitor 18097 can serve as a potential agent against breast cancer.

关键词： m6A FTO inhibitors Cancer cell Lipogenesis SOCS1