PICsome, which is composed of nano-sized unilamellar polyion complex (PIC) membrane with semipermeability, have been utilized for biomedical applications in recent years. This property makes it to be a carrier for protein delivery and a container for enzymes as a nanoreactor. However, due to lack of ability to concentrate dispersed proteins into the vesicle, the loading efficiency is relatively low in previous studies. To enhance the loading efficiency of proteins, we tried development of a novel yolk-shell PIC, which consists of a protein-enriched core and PIC shell. We assume that yolk-shell PICs can be formed by vesicle-induction from protein enriched PIC aggregates, consisting of anionic protein and homo-polycation. PIC vesicle might generate from the PIC aggregates in a way of nucleation-growth phase separation. Specifically, we used an anionic enzyme diamine oxidase (DAO; M.W. = 170 kDa, pI 5.2) labelled with FITC. Then, DAO-FITC was mixed with 10 mM phosphate buffer solutions of polyions, PEGylated poly(α,β-aspartic acid) (PEG-PAsp; DP of PEG = 49, DP of PAsp = 69) as a polyanion and poly-L-lysine (PLL; DP = 108) as a polycation in an anion/cation ratio of 1:1.5. Dynamic light scattering results revealed that an average size of the resulting PIC was ~500 nm, and the loading efficiency obtained from ICP-AES was approximately 60%. In addition, we confirmed that enzymatic activity of encapsulated DAO was still maintained in the PIC. The structure of the PIC was carefully studied by cross-sectional TEM observation. Detailed structure will be discussed in the presentation.
Yiwei Liu has complete his bachelor's degree in China Agricultural University, China. He is a PhD student in Kyushu University, Japan.
Enhanced permeability and retention (EPR) effect discovered by Matsumura and Maeda is the phenomenon that nano-sized particles are spontaneously accumulated into tumor, which is widely used for passive targeting of nanomedicine including polyethyleneglycol-modified liposome (LP). Even though the drugs encapsulated by nanomedicine are more accumulated into tumor than free drugs due to this EPR effect, enhanement of EPR effect is still a critical issue for further development of nanomedicines. To improve the accumulation of nanomedicine by the increase in the blood flow to tumor, we have focused on nitric oxide (NO), which is known for one of endogenous vasodilators, then developed NO donor-encapsulated liposome (NO-LP), which boosted EPR effect without systemic toxicity. Herein, we investigated the potency of NO-LP as an EPR booster for co-administrated nanomedicine. NO-LP was injected to the mice inoculated with CT-26 either with the injection of fluorophore (DiR)-labeled empty LP (DiR-LP) or with the injection of DiR-LP 6 hours later, then fluorescent intensity was quantified by in vivo imager IVIS. The slightly enhanced accumulation of nanomedicine was observed in the NO-LP co-injection group, but statistically both groups showed the similar accumulations with only DiR-LP injection group. These results can be taken into account for formulating the nanomedicine using NO as EPR booster system
Takuma Yoshikawa got his barchelor degree in the department of materials science and engineering at Kyushu University, and master degree in the department of materials physics and chemistry at graduate school of engineering, Kyushu University. Currently he is a PhD candidate at the same department. He joined in the Program for Leading graduate schools, Advanced graduate course on molecular system for devices when he enrolled in the graduate school.
Pseudo peptide can mimic the biological or structural properties of natural peptides. They has become an increasing attention in medicinal chemistry because of their interesting advantages like more bioavailability and less biodegradation than compare to the physiologically active native peptides which increases their therapeutic applications .Many biologically active compounds contains urea as functional groups and they have improved pharmacokinetic properties because of their bioavailability and metabolic stability .Recently we have reported a single-step synthesis of sulfonyl urea and sulfonyltriuret from sulfonyl chloride and sodium cyanate  according to scheme 1. In the present work we mainly focused on the selective synthesis of sulfonyltriuret using tetrabutylammonium cyanate and sulfonyl chloride. The distinctive architecture of these molecules in the form of their pseudo-peptide backbone offers promise as a potential pharmacophore. The synthesized molecules have been screened on trypsin enzyme and we observed that these molecules are the efficient activator of trypsin enzyme.
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Reaction of 1-[4-(1,2-dihydro-1,5-dimethyl-2-phenyl-3-oxo-3H-pyrazol-4-yl)-2-phenyl sulfonyl-1-ethanone (1) with phenyl isothiocyanate, in DMF/ followed by treatment with dilute hydrochloric acid afforded the corresponding 4-(3-mercapto-3-(phenylamino)-2-(phenylsulfonyl)acryloyl)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one (2). Treatment of compound 2 with hydrazonoyl chlorides 3a-h afforded the corresponding1,3,4-thiadiazole derivatives 5a–h. Cyclocondensation reaction of compound 2 with the appropriate α-halo-compounds 6, 8, 10, 12a,b or 14 (ethyl 2-chloroacetate, chloroacetonitrile, 1-chloropropan-2-one, 2-bromo-1-phenylethanone, 2-bromo-1-p-tolylethanone and 2-bromoacetyl-3H-benzo[f]chromen-3-one, afforded the corresponding 1,3-thiazole 7, 9, 11, 13a,b and 15,respectively. Coupling of the ketosulphone1 withthe appropriate diazotized heterocyclic amines , namely, 4H-1,2,4-triazol-3-amine(16)or2-aminobenzimidazole (19)afforded the corresponding 1,5-dimethyl-2-phenyl-4-(4-(phenylsulfonyl)-[1,2,4]triazolo[5,1-c][1,2,4]triazin-3-yl)-1H-pyrazol-3(2H)-one (18). 1,5-Dimethyl-2-phenyl-4-(4-(phenylsulfonyl)benzo[4,5]imidazo[2,1-c][1,2,4]triazin-3-yl)-1H-pyrazol-3(2H)-one (21), respectively. The synthesized compounds were confirmed on the basis of their elemental analysis and spectral data and evaluated as potential anticancer agents.
Taha Mohamed Abdalla Eldebss has completed his Ph. D. Organic Chemistry, Cairo University, Giza, Egypt, M. Sc. Organic Chemistry, Cairo University, Cairo, Egypt (1997).B. Sc. Chemistry, Cairo University, Giza, Egypt ( Distinction Honor) (1997). Also, Teaching of Practical Organic Chemistry(1st Year students, 2nd Year students, 3rd Year students, 4th Year students of different Departments, Faculty of Science, Cairo University, Pre-Dental students, Pre-Veterinary students and Pre-Pharmacy students ) and Practical Analytical Chemistry(1st Year students of different Departments, Faculty of Science, Cairo University, Pre-Dental students, Pre-Veterinary students and Pre-Pharmacy students , in addition to participation in the preparation of notes.His research Interests includes Organic and Heterocyclic Chemistry, Synthesis and biological evaluation of several heterocyclic ring systems, in addition to, their industrial and pharmacological applications.
Starch/Chitosan films have drawn keen attention due to their widespread applications in a diversity of fields such as food canning industries, wound dressings (artificial skin), tissue engineering, antibacterial agents and carriers in drug delivery/drug release systems, especially, anticancer drugs. In the present work, we are introducing for the first time, Starch/Chitosan/Gelatin thin films using Glycerol as a plasticizer. The current study gives a detailed comparison between three different concentrations of Starch/Chitosan/Gelatin blends blend I (15:15:20), blend II (12.5:12.5:25), and blend III (10:10:30) while using Glycerol as a plasticizer in all the blends. The characterization of the prepared thin films has been performed using X-Ray Diffraction (XRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FTIR). In addition, mechanical properties measurements (tensile strength, elastic modulus and the elongation at break %) were estimated. The results of the present study indicated that blend III (10:10:30) showed significant increases in the tensile strength, elastic modulus, and the elongation at break% relative to the 2 other blends. These results pointed to the better mechanical properties of blend III. XRD demonstrated the amorphous structure in the prepared thin films. In addition, FTIR showed that the three materials used (Chitosan, Starch and Gelatin) were well cross linked together which resulted in a homogeneous mixture.The DSC thermograms of all the prepared blends showed high decomposition temperature. Finally, as a conclusion, the present study presented a flexible blend (blend III) made of Starch/Chitosan/Gelatin with the ratios (10:10:30) with enhanced mechanical properties that can be used in various applications. Further studies are needed to test the engineered thin films created in the present work in diverse applications such as canned food, skin grafts…. etc.. Keywords:Chitosan, Starch, Gelatin, Thin films, Glycerol, Blends.
Amena Sayed El-Feky , 21 years old, student at faculty of science, Cairo University, biophysics department. Since my childhood I used to learn myself and read about new inventions. I started my research journey by learning nanotechnology. In fact, the power of nanoscale sized materials caught my mind and how we can get benefit from it in various fields. Searching and self-learning provide me a wide area of thinking which helped me when I read about green chemistry for the first time, then I have decided to focus in my research on cooperation between nanotechnology and green chemistry to use the advantages of green chemistry in producing nanomaterials. The resulted product could add up benefits of both fields for people interest.
Advances in the field of cellular technologies have led to the possibility of developing a new direction of targeted therapy in regenerative medicine - "Strategy of Pharmacological Regulation of Intracellular Signal Transduction in Regenerator-competent Cells". The role of NF-кB, IKK, PKC, PKB, PI3K, ERK ½, p38, adenylate cyclase, PKA, JAKs, STAT3, JNK, p53 in the realization of functioning progenitor elements of different classes and cells of tissue microenvironment was studied in vitro by means of cultural, immunological and other methods. On the models of posthypoxic encephalopathy, skin wound and cytostatic myelosuppression in experimental animals the therapeutic effects and mechanisms of action of modifiers of signal molecules activity were studied. The specificity of the involvement of a number of signaling molecules in the regulation of cell cycle and development of progenitor cells of various classes, as well as in the production of humoral factors by microenvironment cells was revealed. The neuroregenerative effects of JNK inhibitors associated with activation of neural stem cells of brain were shown on the model of encephalopathy. An algorithm and approaches for estimating the potential efficiency and many-sided selectivity of the modifiers of signaling molecules activity as targeted hemostimulators were developed. The effectiveness of various targeted pharmacological agents determined by the selective effect on different types of regenerative-competent cells was demonstrated on the models of cytostatic myelosuppression of various genesis. The perspective of using intracellular signaling molecules in regenerative-competent cells as targets of drugs for regenerative medicine was shown.
Gleb N. Zyuz`kov now is a Scientist Secretary of Institute, Head of the laboratory of pathology and experimental therapy (Goldberg Research Institute of Pharmacology and Regenerative Medicine), Tomsk National Research Medical Center. Ph.D (2003), Doctor of Medicine (2006), Professor of Russian Academy of Sciences (2016). Author of 53 patents. The European Scientific Society and the European Academy of Natural Sciences (Germany) International Award of Elsevier`s "SciVal/Scopus Award Russia» (2012). Dr. Zyuz′kov G.N. is: auditor of the Tomsk branch of National society for regenerative medicine (Russia), a member of Russian scientific society of Pharmacology and Tomsk Professors Society.