Gold nanomaterials are immerging candidates in medical diagnosis and treatment.Among them,gold nanorods(Au NRs)are widely used for cancer treatment.Tiopronin as a novel thiol drug was used to stabilize Au NRs in this work.Doxorubicin(DOX),a chemotherapeutic drug which works by interacting with DNA to arrest the cell cycle and induce apoptosis,was linked to Au NRs through electrostatic reaction with tiopronin,to obtain Au-TIOP-DOX NRs.Au NRs are also regarded as hyperthermia agents for photothermal cancer treatment.This delivery system(Au-TIOP-DOX NRs)was designed for passively targeting tumor cells in cancer therapy.More importantly,the carboxyl groups of tiopronin can be modified with some biological molecules(DNA/RNA,peptides,or drugs)to make Au NRs as a novel drug-delivery system for cancer treatment.
HUO ShuaiDongJIN ShuBinZHENG KaiYuanHE ShengTaiWANG DongLiangLIANG XingJie
Based on the structure of the integrase core domain and pharmacophore perception, the authors picked out the hit quinolone derivative 1 as the lead compound via virtual screen in ACD, MDDIL NCI and Chinese Herb three-dimensional database with the aid of DOCK4.0 program and synthesized a series of analogues of compound 1. Their primary anti-HIV properties against integrase reveal that 6-position methyl group on the benzene ring of quinolone plays a more important role than chlorine, 7-position methyl group or no substituted group. But the title compounds exhibit little difference When the substituted group was phenyl or thienyl on the pyridine ring of quinoline.
LUO Zai-gangZENG Cheng-chuWANG FangHE Hong-qiuWANG Cun-xinDUHong-guangHU Li-ming
As unique nanoparticles,fullerenes have attracted much attention due to their unparalleled physical,chemical and biological properties.Various functionalized fullerenes with OH,NH2,COOH,and peptide modifications were developed.It summarized the biological activities of fullerenes derivatives in cancer therapy with high efficiency and low toxicity,as reactive oxygen species scavenger and lipid peroxidation inhibitor,to inhibit human immunodeficiency virus and to suppress bacteria and microbial at low concentration.In addition,the mechanism for fullerene to enter cells and biodistribution of fullerene in vivo was also discussed.This research focuses on the current understanding of fullerenes-based nanomaterials in the potential clinical application as well as biological mechanism of fullerenes and its derivatives in disease therapy.
MA HuiLi & LIANG Xing-Jie Chinese Academy of Sciences Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety
利用紫外-可见光谱（UV-vis）、X衍射（X-ray Diffraction,XRD）和透射电子显微镜（Transmission Electron Microscope,TEM）等研究小尺寸水溶性金纳米粒子的可控制备.在乙酸和甲醇（体积比为1：6）的混合系统中,通过NaBH4对三水氯金酸还原,将硫普罗宁分子包覆到金纳米粒子表面,得到尺寸可控、稳定的硫普罗宁包覆的金纳米粒子水溶胶.通过控制金与硫普罗宁的摩尔比（Au/S比）,金纳米粒子的尺寸能够在2~8nm范围内得到有效控制.本文中,当Au/S比分别为1：3,1：1和3：1时,所合成的金纳米粒子的尺寸分别为（2.8±0.3）,（4.0±0.3）,（6.1±0.4）nm.
HIV-1整合酶是HIV-1生命周期中必不可少的酶之一,已成为目前最具潜力的抗HIV药物设计的靶点之一。2007年,Merk公司研发的MK-5108作为首个整合酶抑制剂药物被美国食品药物管理局批准上市,标志着整合酶抑制剂研究的重大突破,也激发了抗HIV-1整合酶抑制剂研究的新一轮高潮。计算机辅助药物设计(computer-aided drug design,CADD)具有效率高、成本低等特点,基于计算机辅助手段合理药物设计已取得了很大的进展。文章综述了近几年来计算机辅助设计抗HIV整合酶抑制剂及耐药机理方面的研究进展。
