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Synthesis and Cytotoxicity of the First Arene Ruthenium Compound Containing Two Thiosemicarbazone Ligands

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chinese Journal of Structural Chemistry 2019年第9期38卷 1543-1548页

作者： SU Wei LUO Zhi-Jin CUI Hao TANG Zhao-Feng LI Pei-Yuan PENG Bing-Hua Key Laboratory of guangxi Key Laboratory of Natural Polymer Chemistry and Physics(Nanning Normal university) Nanning530001China College of Pharmacy Guangxi University of Chinese MedicineNanning530001China

A Ru-arene compound containing two thiosemicarbazone ligands [(η6-p-cymene)Ru(TSC)2 Cl]Cl(1, TSC = benzophenone 4-methylthiosemicarbazone) has been synthesized and characterized by 1 H NMR, elemental analysis and HR-ESI mass spectrometry analysis. The molecular structure was determined by single-crystal X-ray diffraction analysis. The in vitro anticancer activities of the complex have been evaluated against two human cancer cell lines(SGC-7901, BEL-7404), and the IC50 values are 32.5 and 57 μM, respectively.

关键词： ruthenium arene thiosemicarbazones X-ray crystal diffraction cytotoxicity running head arene ruthenium compound containing TSC

Synthesis,Crystal Structure and Its Application in Living Cells Imaging of Benz(c)acridine-1,2,3-triazole Derivatives

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chinese Journal of Structural Chemistry 2021年第10期40卷 1309-1316页

作者： YAN Zhen-Shuo KANG Yan-Hui CHEN Yang-Ling HUO Li-Ni guangxi university of chinese medicine Nanning 530001China Hebei university of Engineering Handan 056038China

A highly selective iron ions fluorescent probe based on the benz(c)acridine-1,2,3-triazole derivatives was produced by multi-step reactions. 1-(7-Benz[c]acridinyl)-4-(4-methylphenyl)-1,2,3-triazole(4 a), C_(26)H_(18)N_(4), was structurally determined by single-crystal X-ray diffraction. It crystallizes in the trigonal system, space group R-3 with a = 36.230(10), b = 36.230(10), c = 7.993(3)Å, β = 90°, V = 9086(6)Å^(3), Z = 18, D_(c)= 1.271 g/cm^(3), F(000) = 3636, μ = 0.602 mm^(-1), the final R = 0.0865 and wR = 0.1619 for 3951 observed reflections(I > 2σ(I)). X-ray analysis indicated that all four rings of benz(c)acridine are in the same plane, and the 1,2,3-triazole ring and the corresponding linked benzene(C(1)–C(6)–C(7)–C(8)–C(9)–N(1)) are approximately perpendicular with a dihedral angle of 106.5°. The crystal packing of the compound was stabilized by two weak interactions between C(11)–H(10)…N(4) and C(18)–H(18)…N(1). In fluorescence spectra studies, compound 4 c was exhibited good selectivity and sensitivity towards iron ions in DMSO: mops buffer solution. Furthermore, 4 c was successfully used for imaging iron ions in living He La cervical cancer cells.

关键词： benz(c)acridine-1 2 3-triazole crystal structure fluorescent probe iron ions

Intestinal OCTN2-and MCT1-targeted drug delivery to improve oral bioavailability

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Asian Journal of Pharmaceutical Sciences 2020年第2期15卷 158-172页

作者： Gang Wang Lichun Zhao Qikun jiang Yixin Sun Dongyang Zhao Mengchi Sun Zhonggui He Jin sun Yang Wang Zhuang Yao medicine Center of Engineering and Technology Guang Xi University of Chinese MedicineNanning 530200China School of Pharmacy Guang Xi University of Chinese MedicineNanning 530200China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

Various drug transporters are widely expressed throughout the intestine and play important roles in absorbing nutrients and drugs,thus providing high quality targets for the design of prodrugs or nanoparticles to facilitate oral drug *** particular,intestinal carnitine/organic cation transporter 2(OCTN2)and mono-carboxylate transporter protein 1(MCT1)possess high transport capacities and complementary ***,we outline recent developments in transporter-targeted oral drug delivery with regard to the OCTN2 and MCT1 proteins in this ***,basic information of the two transporters is reviewed,including their topological structures,characteristics and functions,expression and key features of their ***,progress in transporter-targeting prodrugs and nanoparticles to increase oral drug delivery is discussed,including improvements in the oral absorption of anti-inflammatory drugs,antiepileptic drugs and anticancer ***,the potential of a dual transporter-targeting strategy is discussed.

关键词： Carnitine/organic cation transporter 2(OCTN2) Monocarboxylate transporter protein 1(MCT1) Transporter-targeting Nanoparticle Prodrug

Preparation and Methicillin-Resistant Staphylococcus aureus Biofilm Elimination Effect of Baicalein-Loaded Hyaluronic acid/β-Cyclodextrin grafted Chitosan Nanoparticles

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Biomedical and Environmental Sciences 2024年第10期37卷 1227-1231页

作者： Liting Lai Wenyou Ding Guoying Huang Mengke Wang Jinqing Chen Liuzhen Lai Xiuzhen Deng Ling Tang Xinyi Yu Ya Huang Thi Minh Hien Truong Zhongbin Zhang Wenya Ding Faculty of Pharmacy Guangxi University of Traditional Chinese Medicine Key Laboratory of Common Technology of Traditional Chinese Medicine PreparationGuangxi University of Traditional Chinese MedicineNanning 530200GuangxiChina College of Basic Courses Wuhan Donghu UniversityWuhan 430000HubeiChina guangxi Engineering Research Center for Advantageous chinese Patent medicine and Ethnic medicine Development Guangxi University of Traditional Chinese MedicineNanning 530200GuangxiChina

Methicillin-resistant Staphylococcus aureus(MRSA)is a common pathogen causing acquired *** are routinely employed for bacterial infection *** antibiotic use for bacterial infections heightens resistance,and MRSA resistance is being prevalent[1].MRSA exhibits substantial resistance to conventional antibiotics,which is associated with its biofilm-forming *** bacterial biofilm serves as a barrier,restricting nutrient access and slowing internal metabolism,increasing antibiotic *** bacterial biofilm forms a defensive layer,resisting antibiotic penetration while preventing nutrient entry,inducing a slow bacterial metabolism,and increasing bacterial resistance[2].Consequently,biofilm formation and the emergence of resistance to conventional antibiotics have become substantial challenges in the field of infectious *** development of agents to remove biofilm barriers is urgently required because biofilms are extremely hazardous.

关键词： metabolism routine remove

Application of nanoscale metal-organic frameworks in tumor immunotherapy

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Rare Metals 2024年第10期43卷 4867-4883页

作者： Xiao-Xuan Zeng Jing-Sheng Lu Dong-Wei Ma Yu-Ting Huang Ling Chen Gang Wang Qing Chen Ning Lin College of Pharmacy Guangxi Scientific Research Center of Traditional Chinese MedicineGuangxi University of Chinese MedicineNanning 530200China guangxi Zhuang Yao medicine Center of Engineering and Technology Nanning 530200China

Immunotherapy has attracted wide attention because it can not only kill tumor cells but also effectively prevent tumor ***,due to the poor efficacy of the monotherapy in tumor immunotherapy,combination therapies are needed to enhance their efficacy,such as chemodynamic therapy/immunotherapy,photodynamic therapy/immunotherapy,sonodynamic therapy/immunotherapy and so *** metal-organic frameworks(nMOFs)are widely used for drug delivery because of their rich and variable composition,high drug loading capacity and good *** with other conventional drug delivery systems(DDSs),nMOFs play more advantageous role in inducing immune cell death of tumor cells and combination *** article focuses on the application of n MOFs in tumor immunotherapy in terms of their use as gatekeepers,supplementary agents and drug carriers,respectively,with the aim of providing some ideas and references for the design of smart nanoscale DDS for tumor immunotherapy.

关键词： Metal–organic frameworks Tumor Immunotherapy Drug delivery system

Zinc-based metal-organic frameworks as efficient carriers for anticancer drug to reduce toxicity and increase efficacy

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Rare Metals 2024年第10期43卷 5152-5163页

作者： Dong-Wei Ma Jing-Sheng Lu Xiang-Xin Cao Yan-Wei Cheng Gang Wang Zi-Qian Zhang Bo-Cheng Chen Ning Lin Qing Chen College of Pharmacy Guangxi Scientific Research Center of Traditional Chinese MedicineGuangxi University of Chinese MedicineNanning 530200China guangxi Zhuang Yao medicine Center of Engineering and Technology Nanning 530200China

The rational design of a specific co-drug delivery platform that can address the unavoidable resistance,toxic side effects and low targeting efficiency of traditional cancer treatments is of great ***,Zn-based MOF-zeolitic imidazole framework-90(ZIF-90)was selected as the drug delivery carrier,with the cancer therapeutic drug mercaptopurine(6-MP)and glucose oxidase(GOD)as the drug models,hyaluronic acid(HA)was used for protection and targeted delivery,which designed and fabricated an intelligent drug delivery platform(6-MP@ZIF-90@GOD@HA).This platform aims to reduce the toxic side effects of 6-MP and enhance its efficacy while improving the targeting ability of GOD,thereby further enhancing the treatment ***,results from both in vitro and in vivo experiments demonstrate that the targeted synergistic chemo/reactive oxygen species(ROS)-mediated/starvation therapy inhibited the cancer cell growth while reducing the chemotherapy toxicity,which provides new possibilities for the development of more precise and effective treatment strategies.

关键词： Metal-organic framework Cancer treatment Combination therapy Drug delivery Reduced toxicity

Rejuvenation of BMSCs senescence by pharmacological enhancement of TFEB-mediated autophagy alleviates aged-related bone loss and extends lifespan in middle aged mice

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Bone Research 2024年第3期12卷 661-674页

作者： Ziwei Luo Wanyi Wei Dawei Qiu Zixia Su Liangpu Liu Honghai Zhou Hao Cui Li Yang College of Orthopedics Guangxi University of Chinese MedicineNanning 530200 GuangxiChina Faculty of chinese medicine Science Guangxi University of Chinese MedicineNanning 530200 GuangxiChina Department of Physical Education Guangxi University of Chinese MedicineNanning 530200 GuangxiChina guangxi Key Laboratory of Efficacy Study on chinese Materia Medica Guangxi University of Chinese MedicineNanning 530200 GuangxiChina College of Pharmacy Guangxi University of Chinese MedicineNanning 530200 GuangxiChina Key Laboratory of Biorheological Science and Technology Ministry of EducationBioengineering CollegeChongqing UniversityChongqing 400030China

Bone marrow stromal/stem cells(BMSCs)are generally considered as common progenitors for both osteoblasts and adipocytes in the bone marrow,but show preferential differentiation into adipocytes rather than osteoblasts under aging,thus leading to senile *** evidences indicate that rejuvenation of BMSCs by autophagic enhancement delays bone aging.

关键词： senile osteoporosis progenitor

Effect of Rheum palmatum *** NF-κ B signaling pathway of mice with acute liver failure

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Asian Pacific Journal of Tropical medicine 2015年第10期8卷 823-829页

作者： Rong-Zhen Zhang Hua Qiu Na Wang Fu-Li Long De-Wen Mao First Affiliated Hospital of guangxi university of TCM

Objective:To explore the regulation effect of Rheum palmatum(***) *** NF-κ.B signaling pathway of ALF ***:The intraperitoneal injection of D-GalN/LPS was employed for the model *** in the treatment group and positive control group were given the R,palmatum *** bifendate before the model *** in the normal group were given the intraperitoneal injection of equivalent normal saline for continuously *** 16 h of model building,the blood was collected from eyeballs of mice and then mice were *** measurement was performed on the content of ALT,AST,NO and 11-1βin the serum of mice in eaeh group,as well as the activity of Caspase 3 and Caspase 8 in the liver *** staining was employed to detect the pathological morphology of liver;and the western blot was used to detect the expression of iNOS,COX-2,Bax,Bcl-2,PCNA,NF-κ B p65 and I κ.***:The content of ALT,AST,NO and I1-1β in the serum and the activity of Caspase 3 and Caspase 8 in the liver tissue were increased in the mice of ALF model ***,the expression of iNOS,COX-2 and Bax was increased,the expression of Bcl-2 and PCNA was decreased,the phosphorylation of NF-κ B p65 and 1κ B was significant and the treatment group of *** *** inhibit such ***:Through NF-κB signaling pathway,the *** *** reduce the content of enzyme of liver function and inflammation factor in the serum of ALF mice,regulate the expression of cell apoptosisrelated protein and improve the symptoms of ALF mice.

关键词： Rheum officinale Acute liver failure Inflammation

Hydrolyzed seawater pearl tablet modulates the immunity via attenuating Th1/Th2 imbalance in an immunosuppressed mouse model

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Journal of Traditional chinese medicine 2021年第3期41卷 397-405页

作者： LAN Taijin LUO Xuefei MO Mingyue CHEN Zhenxing LUO Fei HAN Siyin LIU Peng LIANG Zhongxiu ZHANG Ting LI Tianyi YAN Qiangqiang LIN Yong LIN Jiang School of Basic Medical Science Guangxi University of Chinese MedicineNanning 530200China Ruikang Hospital Affiliated to guangxi university of chinese medicine Nanning 530011China Beihai Baozhulin Marine Technology Co.Ltd. Beihai 536000China

OBJECTIVE: To investigate whether Hydrolyzed Seawater Pearl tablet(HSPT) could modulate the Th1/Th2 imbalance in an immunosuppressed mouse model with Th1 to Th2 shift induced by Cyclosporine A(Cs A) which can be used in the clinical treatment of Th2 to Th1 shift diseases, and explore the possible mechanism for the adjuvant therapeutic efficacy of HSPT on recurrent respiratory infections(RRI) and acquired immune deficiency syndrome(AIDS).METHODS: The mice were randomly divided into six groups of five animals each, namely normal group, model group, lentinan polysaccharide tablet(LPT) group and three HPST treated groups. HPST treated groups were administered with HPST(0.51,1.02, 2.04 g/kg) via intragastric gavage(i.g) for 30 consecutive days. LPT used as reference drug for positive control, LPT group was administered with LPT(8.2 mg/kg) for 30 consecutive days. Normal group and model group were received distilled water. The animals in model group, LPT group and HPST treated groups were injected intraperitoneally with Cs A(50 mg/kg) to establish the immunosuppressed mice model with Th1 to Th2 shift on the20 th, 22 nd and 24 th day, one hour after the administration of the respective treatment. Animals were sacrificed one hour after the last administration to collect blood and splenic tissue. The proportion of T cells including CD8+ and CD4+ T cells, Th1 and Th2 in peripheral blood of experimental mice were measured by flow cytometric. The protein level in serum and m RNA level in splenic tissue of experimental mice for interleukin(IL)-2, IL-12, interferon-γ(IFN-γ), IL-4, IL-6, IL-10 and IL-13 were measured by enzyme linked immunosorbent assay and fluorescence quantitative polymerase chain reaction ***: HSPT elevated the proportion of T cells including both CD8+ and CD4+ T cells, in which the proportion of Th1 and Th2 cells increased, while the ratio of Th1/Th2 cells decreased in peripheral blood of the immunosuppressed mouse model with Th1 to Th2 shift

关键词： respiratory tract infections acquired immunodeficiency syndrome Th1-Th2 balance interleukins interferon-gamma Hydrolyzed Seawater Pearl tablet