Day 1 :
Keynote Forum
Gabor Patonay
Georgia State University, USA
Keynote: Fluorescent Dye Copolymerized Silica Nanoparticles for Analytical Applications
Time : 10:00
Biography:
Dr. Gabor Patonay is Professor of Analytical Chemistry at Department of Chemistry, Georgia State University, Atlanta, GA 30303, USA. He obtained his M.S. and Ph.D. degrees from the Technical University of Budapest, Hungary. In 1982 he joined Professor Isiah Warner’s group at Emory University, Atlanta, GA, USA. He joined the faculty of GSU in 1987, where he is currently Professor. He spent his years at GSU focusing on NIR fluorescence and developing new bioanalytical and biomedical applications using NIR probes and labels. His recent research interests include bioanalytical and biological applications of fluorescent silica nanoparticles. Dr. Patonay has published over 200 papers. He is the Editor-in-Chief for Analytical Chemistry Insights.
Abstract:
Recent trend for fluorescence detected analytical applications is the use of longer wavelength fluorophores and encapsulation of fluorophores by utilizing nanoparticles. Many applications can be cited such as separations, antibody detection, biomolecule charachterizations, etc. Long wavelength fluorescence in analytical chemistry has several advantages such as lower background interference especially in biological matrices. While many different types of nanoparticles have been utilized for, silica nanoparticles have significant advantages in biological system. Silica nanoparticle synthesis for copolymerization of fluorescent dyes an easily controllable process by using modified TEOS reactive analogues. The fluorescence of silica nanoparticles can significantly be increased by enclosing a large number of dye molecules. For high dye concentrations in the silica nanoparticle self quenching can be significant but it can be minimized by synthesizing large Stokes’ shift dyes or resonance energy transfer. Using NIR dyes excellent sensitivity can be achieved but one major disadvantage is that most biological fluorescence instruments are designed for shorter excitation wavelengths frequently matching the optical properties of fluorescein, a widely used fluorophore. One approach to make these new fluorescent silica nanoparticles more compatible with widely used excitation wavelengths is the development of fluorescent silica nanoparticles containing dyes that are good candidates for fluorescence energy transfer. This presentation discusses the facile synthesis and analytical applications of such silica nanoparticles containing copolymerized multiple fluorophores. The surface properties of fluorescence silica nanoparticles were modified by adding hydrophobic or hydrophilic molecules on the surface to achieve biocompatibility. Biocompatibility was evaluated by hemolytic experiments. Typical applications of these particles are for immunochemistry, flow cytometry, CE, forensic applications, etc. They are also suitable for biomolecule characterization utilizing their specific binding characteristics to biomolecules. Modifying surface properties of silica nanoparticles enhances their analytical utility. Examples will be given for applications of modulated surface hydrophobicity and chirality.
Keynote Forum
Joseph Kipronoh Rugutt
Missouri State University, USA
Keynote: USA-Kenya collaboration in guided-inquiry green nanoscience drug discovery research
Time : 10:40-11:10
Biography:
Abstract:
The Department of Chemistry at Missouri State University-West Plains (MSU-WP) is internationalizing the existing research activities by initiating a collaborative USA-Kenya drug discovery project. Professors Rugutt (MSU-WP) and Kiplimo (University of Kabianga (UoK), Kenya) are indebted to the Carnegie African Diaspora Fellowship (CADF) program for a three-month award that supported the project. Undergraduate, graduate, and high school students played an integral part in implementation of all research and educational activities. The overarching goal of the project is to establish synergistic relationships between different research groups and academic institutions in Kenya and MSU-WP. We chose natural products as the centerpiece of our collaboration because many medicinal Kenyan plants represent an important and underexploited reservoir of potentially new pharmaceutical drugs. Our preliminary results on bioassay-directed fractionation and screening of representative plants afforded several compounds that exhibited various bioactivities including anticancer, antimalarial, anti-HIV, antimicrobial, antimycobaterial, and antifungal. After identifying the most active natural products (sesquiterpene lactones, flavonoids, binaphthyls, steroids, etc.), we conducted a hypothesis-driven green nanosynthetic modifications in order to pinpoint the essential structural features necessary for bioactivity. Novel compounds were prepared based on the world’s best
“named reactions” such as those developed by Nobel Laureates (Diels-Alder, Grubbs, etc.). Our integration of research and education was anchored on the fact that natural products research cuts across many STEM (Science, Technology, Engineering, and Mathematics) disciplines such as medicinal, organic, analytical, and inorganic chemistry. To strengthen preparation of students for STEM careers, chemistry faculty at MSU-WP and UoK are revamping their research and laboratory courses by incorporating current “hot” and inspirational topics in guided-inquiry green chemistry, nanoscience, and natural products. The new courses will provide students with opportunities to learn innovative experimental techniques (chromatography, spectroscopy, bioassays, etc.). Bioassay data from structure-bioactivity relationship studies will be discussed. Also, reports summarizing professional development activities will be disseminated
- Track 2:Analytical Chemistry | Track 4:Environmental Chemistry |Track 7:Physical Chemistry|Track 14:Medicinal Chemistry |Track 17:Organic and Inorganic Chemistry
Session Introduction
Keiichi Kaneto
Osaka Institute of Technology, Japan
Title: High power lemon Juice biofuel cells using conducting Polymer catalyst
Biography:
Keiichi Kaneto Completed his Ph.D in 1977 from Department of Electrical Engineering, Osaka University, Osaka, Japan and also worked as an Research Associate, Faculty of Engineering, Osaka University, Osaka, Japan1981 Postdoctoral Researcher, c/o Prof. Alan G. MacDiarmid, University of Pennsylvania, USA, In 1988 Professor, Department of Computer Science and Systems, Kyushu Institute of Technology, Japan. 2017 Professor, Department of Biomedical Engineering, Osaka Institute of Technology, Japan. In 2007 Award of 1st European Scientific Network for Artificial Muscle, by European Science Foundation
Abstract:
Biofuel cells, which generate electric power from biomaterials such as glucose, alcohol, organic acids, are interested as a potential candidate for sustainable energy sources. The key material for biofuel cells is catalyst, which enhances chemical reaction and conversion efficiency to electric power. However, expensive rare metals like Pt are commonly used for the catalyst. We have been studying biofuel cells to explore the possibility to replace rare metals with functional materials. It was found that conducting polymers exhibited excellent performance as the anode catalyst.
In this talk, fabrication of biofuel cells, measurement and characterization of the electrical output using conducting polymer, poly(3,4-ethylenedioxythiophene) polystyrene sulfonate (PEDOT*PSS) as the anode catalyst are presented. The biofuels were ascorbic acid (AsA; known as vitamin C), citric acid (CitA), and lemon juice. The output powers based on these biofuels were compared.
The cells consisted of biofuel/current collector/PEDOT*PSS /Nafion® (N117)/Pt-B (black) cathode catalyst/current collector/air. For the current collector a low resistance CuNi-coated polymer cloth was used. The cell was a direct and passive type. Figure 1 shows cell performances of electromotive force (E0), maximum power (Pmax) and cell voltage (Emax) at the power maximum. The highest performance was obtained in the lemon juice cell having the Pmax about 4 mW/cm2 using PEDOT*PSS anode catalyst. Taking the fact that lemon juice contains approximately 0.03 M AsA and 0.3 M CitA, the Pmax of lemon juice cell is consistent with the sum of them. It is also noted that the cell performances of PEDOT*PSS was better than that of Pt-B for anode catalysts and 0.5 M AsA. The mechanism of high power CuNi/PEDOT*PSS anode cell will be discussed.
Manju Kumari Saroj
University of Delhi, India
Title: An experimental and theoretical Investigation of inclusion complexes of Indole Chalcones in ï¢-Cyclodextrin
Biography:
Dr Manju K Saroj has her expertise in working experimentally and theoretically on photophysical properties of the biologically active molecules like isatine chalcone, indole chalcones and thymol based shiffs bases. She has done extensive study related to specific and non-specific interaction of various probe in heterogeneous and homogenous media by considering their absorption and fluorescence spectral profile. In the present work, she has justified the ability of IC derivatives to depict the changes in the microenvironment of β-CD, which suggest its potential application as a probe of this medium.
Abstract:
Indole chalcone (IC) derivatives form an important group of chalcones with biological activities such as anti-inflammatory, neuro-protective, anti-amoebic, anti-cancer etc. In addition, various chalcones are also recognized for their wide antimicrobial activity, and they can be employed as efficient drugs for the treatment of several diseases, like malaria or tuberculosis. Despite a variety of potential applications of chalcones in medicinal chemistry, these compounds generally have limited pharmacological uses because of low dissolution rate and bioavailability. There are multiple techniques designed to increase the solubility of a drug, including the use of micelles, liposomes, nanoparticles and nanodispersions. Among the existing techniques, the formation of inclusion complexes with encapsulating agents such as
β-cyclodextrin (b-CD), is frequently employed.
The present study focuses on the formation of inclusion complexes of IC derivatives with b-CD, which involves absorption and steady state fluorescence spectroscopies. The stoichiometries and binding constants (Kin) of these complexes have been investigated by monitoring their absorbance and fluorescence spectral profiles. The data are analyzed by Benesi-Hildebrand plots as well as Job’s method, which indicate 1:1 stoichiometry of IC:b-CD complexes. Fluorescence measurements are also used to investigate the effect of temperature on the stability of inclusion complexes. Stability of IC:b-CD complexes is significantly affected with variation in substituents on the phenyl ring and temperature. The stability of the inclusion complex observed to decreases with increase in temperature. All the experimental results and the geometrical data obtained using PM3 semiempirical method illustrate the partial inclusion of IC derivatives from the phenyl ring side in β-CD cavity. The binding process of IC derivatives with b-CD is found to be exothermic in nature and seems to be controlled by electrostatic and hydrophobic forces.
Yong Zhang
Southeast University, China
Title: Development of a novel and efficient route to the Tropomyosin-related Kinase (Trk) Inhibitor Larotrectinib (LOXO-101)
Biography:
Yong Zhang, School of Biological Science & Medical Engineering, Southeast University, Si Pai Lou 2#, Nanjing, 210096, PR China. His expertise in design, synthesis, and biological evaluation of novel compound to certain disease
Abstract:
Larotrectinib (LOXO-101) is a small-molecule ATP-competitive oral inhibitor of the tropomyosin-related kinase (Trk) family of receptor kinases, including Trk-A, Trk-B and Trk-C kinases. Herein, a novel and efficient route for the synthesis of Larotrectinib using starting materials that are commercially available has been achieved. The procedure employed mild reaction conditions and avoided the use of expensive reagents compared to the original synthetic route reported by Array BioPharma. More importantly, gram scale synthesis was accomplished and this protocol could be valid in the synthesis of similar drugs.
Wang Xue-jie
Zhejiang International Studies University, China
Title: Thermal decomposition mechanism and kinetics of tenoxicam
Biography:
Xuejie Wang graduated and received B.Sc. degree from Fudan University in 1982, and then received his M.Sc. and Ph.D. degrees from Zhejiang University. He joined Zhejiang Educational Institute (The predecessor of Zhejiang International Studies University) in 1988 and was appointed as Professor in 2000. He serviced as dean of the school of science and technology from 2004 to 2014. He is good at chromatographic, spectral, thermal, and electrochemical analysis. His current research projects include the molecular structure and thermal stability of drugs and materials. He has published more than 100 papers.
Abstract:
Tenoxicam (TNX) is a non-steroidal anti-inflammatory drug. Its thermal decomposition processes were studied with thermogravimetry and differential scanning calorimetry. The produced gaseous products and residues during decomposition were detected and characterized using Fourier transform infrared spectroscopy. Combining with the molecular bond order distribution obtained from the quantum chemistry calculation, the thermal decomposition mechanism of TNX has been speculated. The kinetic parameters for thermal decomposition, such as activation energy Eα and the pre-exponential factor A, were obtained using the ATSM E1641 method. The prospective lifetime of TNX was estimated using the ATSM E1877 method. The results indicated that the thermal decomposition of TNX is a three-stage process. During the first stage of thermal decomposition, the main part of the molecule, including sulfamide, thiophene and amide, decompose simultaneously, and to form gasifiable small molecules and carbonized residues. The initial decomposition temperature in either nitrogen or air is about 204 °C. For decomposition in nitrogen, the Eα and A for the initial thermal decomposition are 174.8 kJ mol-1 and 2.512 × 1017 min-1, respectively. For decomposition in air, the corresponding Eα and A are 179.4 kJ mol-1 and 7.943 × 1017 min-1, respectively. The TNX has good thermal stability under routine temperature.
Vishnu K Tandon
Lucknow University, India
Title: Recent developments on Anti-infective quinone derivatives
Biography:
Vishnu K Tandon has completed his Ph.D. at the age of 26 years from Central Drug Research Institute, Lucknow and Postdoctoral studies from Robert Robinson Laboratories, University of Liverpool, U.K. He is an E-Scientist at a premier Technology Institute at Lucknow. He has published more than 100 papers in reputed national and international journals and serving as an associate editorial board member of journal of repute.
Abstract:
One of the most significant achievements of the 20th Century has been the discovery and development of a large number of therapeutic agents that provide now reliable and effective treatment for many infectious diseases that had earlier caused extensive mortality and morbidity. A large number of antibacterial agents often possess quinone moiety which is of paramount significance in several biochemical processes including oxidative phosphorylation and electron transport. The biological activity imparted by 1,4-benzoquinone, 1,4-naphthoquinone and anthraquinones in most cases relies upon their ability to accept one and/ or two electrons to form radical anion or dianion species. The nature of substituents in benzoquinones, naphthoquinones and anthraquinones modulates the generation of radical anion and the redox property which is further responsible for compounds to generate oxidative radicals such as hydrogen peroxide and superoxides which damage the cells. The diverse biological effects caused by incorporation of nitrogen or sulfur atoms in the side chain or in five or six membered heterocyclic rings retaining the core quinone chromophore has been one of the main stay of structural and chemical modifications of this class of compounds. This has led us in successful development of lead antibacterial agents for future drug developments.
Joseph Kipronoh Rugutt
Missouri State University-West Plains, USA
Title: USA-Kenya Collaboration in Guided-Inquiry Green Nanoscience Drug Discovery Research
Biography:
Abstract:
The Department of Chemistry at Missouri State University-West Plains (MSU-WP) is internationalizing the existing research activities by initiating a collaborative USA-Kenya drug discovery project. Professors Rugutt (MSU-WP) and Kiplimo (University of Kabianga (UoK), Kenya) are indebted to the Carnegie African Diaspora Fellowship (CADF) program for a three-month award that supported the project. Undergraduate, graduate, and high school students played an integral part in implementation of all research and educational activities. The overarching goal of the project is to establish synergistic relationships between different research groups and academic institutions in Kenya and MSU-WP. We chose natural products as the centerpiece of our collaboration because many medicinal Kenyan plants represent an important and underexploited reservoir of potentially new pharmaceutical drugs. Our preliminary results on bioassay-directed fractionation and screening of representative plants afforded several compounds that exhibited various bioactivities including anticancer, antimalarial, anti-HIV, antimicrobial, antimycobaterial, and antifungal. After identifying the most active natural products (sesquiterpene lactones, flavonoids, binaphthyls, steroids, etc.), we conducted a hypothesis-driven green nanosynthetic modifications in order to pinpoint the essential structural features necessary for bioactivity. Novel compounds were prepared based on the world’s best
“named reactions” such as those developed by Nobel Laureates (Diels-Alder, Grubbs, etc.). Our integration of research and education was anchored on the fact that natural products research cuts across many STEM (Science, Technology, Engineering, and Mathematics) disciplines such as medicinal, organic, analytical, and inorganic chemistry. To strengthen preparation of students for STEM careers, chemistry faculty at MSU-WP and UoK are revamping their research and laboratory courses by incorporating current “hot” and inspirational topics in guided-inquiry green chemistry, nanoscience, and natural products. The new courses will provide students with opportunities to learn innovative experimental techniques (chromatography, spectroscopy, bioassays, etc.). Bioassay data from structure-bioactivity relationship studies will be discussed. Also, reports summarizing professional development activities will be disseminated.