196,015 research outputs found
Investigation of a Radio-Iodinated Alpha-Mangostin for Targeting Estrogen Receptor Alpha (ERα) in Breast Cancer: In Silico Design, Synthesis, and Biological Evaluation
Muchtaridi Muchtaridi,1,2 Wiwit Nurhidayah,1 Taufik Muhammad Fakih,1,3 Kento Kannaka,4 Hiroyuki Suzuki,4 Toto Subroto,5 Tomoya Uehara4 1Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, 45363, Indonesia; 2Research Collaboration Centre for Radiopharmaceuticals Theranostic, National Research and Innovation Agency (BRIN), Sumedang, 45363, Indonesia; 3Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Islam Bandung, Bandung, 40116, Indonesia; 4Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, 260-8675, Japan; 5Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Sumedang, 45363, IndonesiaCorrespondence: Tomoya Uehara; Muchtaridi Muchtaridi, Email [email protected]; [email protected]: Alpha-mangostin (AM), the most representative xanthone derivative isolated from the rind of the Purple Mangosteen (Garcinia mangostana Linn), has been reported pharmacologically to be associated with breast cancer in silico, in vitro, and in vivo. Although the pharmacological effects of AM are believed to involve the estrogen receptor alpha (ERα), there are no reports available in the literature describing the binding of AM to ERα.Methods: In this study, iodine-125 (125I)-labeled AM ([125I]I-AM) was prepared, and its binding to ERα was investigated in vitro using MCF-7 cell lines. To investigate the applicability of radioiodine-labeled AM as a radiopharmaceutical for breast cancer, [125I]I-AM was injected into nude mice bearing MCF-7.Results: The results obtained showed that the uptake of [125I]I-AM into MCF-7 cells was found to be inhibited by AM and tamoxifen, suggesting that its uptake is partially mediated by ERα. In addition, the biodistribution studies using MCF-7 bearing nude mice showed that [125I]I-AM accumulated in tumor tissues, although deiodination did occur, reducing the concentration of iodine-125 (125I) in the targeted cells.Conclusion: These results suggested that AM would be a useful platform for the development of a new radiopharmaceutical targeting ERα. Further studies are, however, required to reduce deiodination of [125I]I-AM in vivo.Keywords: alpha-mangostin (AM), estrogen receptor alpha (ERα), breast cancer, radiopharmaceutical, iodine-125 (125I
Complexation of α-Mangostin with γ-Cyclodextrin and Its Application in Alginate/Chitosan Hydrogel Mucoadhesive Film for Treatment of Recurrent Aphthous Stomatitis
Ine Suharyani,1,2 Ahmed Fouad Abdelwahab Mohammed,3 Muchtaridi Muchtaridi,4 Ali El-Rayyes,5 Marline Abdassah,1 Cecep Suhandi,1 Nasrul Wathoni1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, 45363, Indonesia; 2Faculty of Pharmacy, Universitas Muhammadiyah Ahmad Dahlan Cirebon, Cirebon, West Java, 45153, Indonesia; 3Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, 61517, Egypt; 4Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, 45363, Indonesia; 5Center for Scientific Research and Entrepreneurship, Northern Border University, Arar, 73213, Saudi ArabiaCorrespondence: Nasrul Wathoni, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, 45363, Indonesia, Tel\Fax +6222 842 888888, Email [email protected]: α-Mangostin (α-M), one of the xanthon compound isolated from Garcinia mangostana rind, demonstrates the efficacy in the treatment of recurrent aphthous stomatitis (RAS). The lack of solubility of α-mangostin in water limited its pharmacological application.Purpose: The lack of solubility of α-mangostin in water limited its formulation and pharmacological application. This study was done to enhance the solubility of α-M by complexation with γ-cyclodextrin (γ-CD) and its application in Alginate/Chitosan Hydrogel Mucoadhesive Film (HMF) for RAS treatment.Methods: This complex was made by dissolved α-M and γ-CD in separated solution. α-M solution gradualy added into γ-CD to formed α-M/γ-CD complex (α-M/γ-CD CX). This complex then evaporated to yield the dry complex powder. The complex was successfully formulated into hydrogel mucoadhesive film (HMF) preparations based on characterization using Scanning Electron Microscope (SEM), Fourier Transform Infra-Red (FTIR), and X-Ray Diffractometry (XRD). The complex was formulated in hydrogel mucoadhesive film, followed by in-vitro drug release and the study of recurrent aphthous stomatitis (RAS) activity in rats.Results: The α-M/γ-CD CX HMF film has a higher mucoadhesive force and mucoadhesive time than other HMFs resulting in a prolonged retention time in the oral mucosa. The drug release of α-M/γ-CD CX HMF followed the Korsmeyer-Peppas Model with a total amount of drug released 80.34+0.32%. The inclusion complex of α-M/γ-CD CX HMF exhibited increased anti-RAS activity compared to HMF base, α-M HMF, and α-M/γ-CD PM HMF. This was evidenced by a significant decrease in wound area of approximately 79.05± 3.30%, an increase in epithelial thickness of about 1.24± 0.09 μm, and a decrease in neutrophil score 1.10± 0.26. These findings highlight the potential use of α-M/γ-CD CX as an effective RAS agent in HMF.Conclusion: The complex of α-M/γ-CD CX has improved solubility of α-M, resulting in the transparent and homogenous film. The film containing this complex has the better physical characteristic, increasing the release and RAS activity. Keywords: α-Mangostin, γ-cyclodextrin, inclusion complex, solubility, hydrogel mucoadhesive film, recurrent aphthous stomatiti
Role of Radioiodine in Cancer Therapy: A Review of the Design and Challenges in Selecting Radioligands from Natural Sources
Taufik Muhammad Fakih,1,2 Dhania Novitasari,3,4 Mukh Syaifudin,4,5 Edy Meiyanto,6 Okid Parama Astirin,7 Amirah Mohd Gazzali,8 Muchtaridi Muchtaridi3,4 1Doctoral Program of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, West Java, Indonesia; 2Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Islam Bandung, Bandung, West Java, Indonesia; 3Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, West Java, Indonesia; 4Research Collaboration Centre for Theranostic Radiopharmaceuticals, National Research and Innovation Agency (BRIN), Sumedang, West Java, Indonesia; 5Research Center for Radioisotope, Radiopharmaceutical and Biodosimetry Technology, Research Organization for Nuclear Energy, National Research and Innovation Agency (BRIN), Tangerang Selatan, Banten, Indonesia; 6Laboratory of Macromolecular Engineering, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Gadjah Mada, Sleman, Yogyakarta, Indonesia; 7Department of Biology, Faculty of Mathematics and Natural Science, Universitas Sebelas Maret, Surakarta, Central Java, Indonesia; 8School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, MalaysiaCorrespondence: Muchtaridi Muchtaridi, Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, West Java, 45363, Indonesia, Email [email protected]: The use of radioactive isotopes in cancer treatment has marked a pivotal shift in modern medicine, where precise diagnosis and targeted therapy now blend to offer patients more effective care with minimized side effects. Despite significant advancements, the exploration of iodine-labeled radioligands from natural sources remains underdeveloped, and comprehensive evaluations of their design, pharmacokinetics, and clinical relevance are still lacking. This gap has created a pressing need for systematic studies that bridge natural product chemistry with radiopharmaceutical applications. Since the initial application of iodine-131 in thyroid treatments, radioisotopes such as iodine-125 and iodine-131 have gained prominence in oncology due to their dual functionality: they enable accurate imaging while delivering therapeutic radiation directly to tumor cells, reducing harm to surrounding healthy tissues. Recent advancements in radiopharmaceuticals, particularly iodine-labeled compounds, aim to further improve this balance by enhancing cancer treatment efficacy and safety. This review synthesizes findings from clinical and experimental studies that explore a range of iodine-labeled compounds, including natural agents like hypericin, curcumin, and piperine, as well as various synthetic analogs. Key methodologies for incorporating iodine, such as the Iodogen method and other stable-labeling techniques, are evaluated for their impact on the compounds’ pharmacokinetics, stability, and therapeutic performance. Furthermore, in silico methods are highlighted for their contribution to optimize the molecular structures, binding affinities, and specificity, streamlining the selection of high-potential candidates for radiopharmaceutical applications. Findings reveal that iodine-labeled compounds effectively concentrate in tumor cells, enhancing selectivity and reducing radiation exposure to non-cancerous tissues. Notably, these compounds demonstrate stability in biological environments, making them viable options for integrated diagnostic and therapeutic purposes. Moving forward, the ongoing refinement of compound stability and targeted biodistribution is crucial in ensuring these therapies can meet the demands of precision oncology and improve clinical outcomes across various cancer types.Keywords: radioiodine isotopes, natural radiopharmaceuticals, cancer treatment, diagnostic imaging, future radioactive desig
Dr. Duane M. Jackson, Morehouse College, July 2011
This video is a conversation with Dr. Duane M. Jackson. Dr. Jackson talks about his paper, "Recall and the Serial Position Effect: The Role of Primacy and Recency on Accounting Students' Performance." Jackie Daniel, AUC Woodruff Library, is the interviewer
"Reflections on the subject of Emigration from Europe with a view to Settlement in the United States" By M. Carey.
"Reflections on the subject of Emigration from Europe with a view to Settlement in the United States: containing bried sketches of the moral and political character of those states.
By M. Carey, member of the American philosophical, and of the American Antiquarian Society, and author of The Olive Branch, Cindiciae Hibernicae, essays on banking, on political economy, and on internal improvement.
To which are now added the English editor's comments on the subject; together with Important Advice to Emigrants, and Cautions Against Impositions Practiced in the Outports
Dispelling the Myths Behind First-author Citation Counts
We conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
Dr. Glendon Swarthout
Hosted by Roger M. Busfield, MSU Assistant Professor of Speech and Theater, Meet the Author is designed to introduce a general audience to a contemporary author and their work through in-depth interviews. This episode features a conversation between Dr. Glendon Swarthout, prolific author and English professor at MSU, and assistant professors Sam S. Baskett and Theodore B. Strandness
Simulation of thermal plant optimization and hydraulic aspects of thermal distribution loops for large campuses
Following an introduction, the author describes Texas A&M University and its utilities system. After that, the author presents how to construct simulation models for chilled water and heating hot water distribution systems. The simulation model was used in a $2.3 million Ross Street chilled water pipe replacement project at Texas A&M University. A second project conducted at the University of Texas at San Antonio was used as an example to demonstrate how to identify and design an optimal distribution system by using a simulation model. The author found that the minor losses of these closed loop thermal distribution systems are significantly higher than potable water distribution systems. In the second part of the report, the author presents the latest development of software called the Plant Optimization Program, which can simulate cogeneration plant operation, estimate its operation cost and provide optimized operation suggestions. The author also developed detailed simulation models for a gas turbine and heat recovery steam generator and identified significant potential savings. Finally, the author also used a steam turbine as an example to present a multi-regression method on constructing simulation models by using basic statistics and optimization algorithms. This report presents a survey of the author??s working experience at the Energy Systems Laboratory (ESL) at Texas A&M University during the period of January 2002 through March 2004. The purpose of the above work was to allow the author to become familiar with the practice of engineering. The result is that the author knows how to complete a project from start to finish and understands how both technical and nontechnical aspects of a project need to be considered in order to ensure a quality deliverable and bring a project to successful completion. This report concludes that the objectives of the internship were successfully accomplished and that the requirements for the degree of Degree of Engineering have been satisfied
Intern experience at CH���M Hill, Inc.: an internship report
Includes author's vita"Submitted to the College of Engineering of Texas A&M University in partial
fulfillment of the requirement for the degree of Doctor of Engineering."Includes bibliographical referencesA review of the author's internship experience with CH���M HILL, Inc.
during the period September 1975 through May 1976 is presented. During this nine month
internship the author worked as an Engineer II in the Industrial Processes discipline of this
large consulting engineering firm... The author's prime responsibility was as one of three
lead design engineers on the design of a large wastewater treatment facility for a pulp mill
in Hoquiam, Washington owned by ITT Rayonier Inc. The work generally consisted of the design
of individual treatment units and associated piping and pumping. The purpose of the project
was to provide wastewater treatment capabilities that would satisfy the effluent limitations
(standards) imposed upon the mill by the State of Washington Department of Ecology and the
U.S. Environmental Protection Agency. The author's assignment also entailed necessary
interaction with the project manager and other CH���M HILL design engineers and support staff
members, the client's representatives, and representatives of two other consulting engineering
firms working on the project. Thus, the internship position at CH���M HILL provided considerable
experience coordinating the author's work with the work of other engineers, guiding the design
and administrative efforts of a support staff, and interacting regularly with the client and
other consulting firms. This broad exposure to a variety of engineering and organizational
problems provided a valuable educational experience
Transition to turbulence in a qblique shock-wave/boundary-layer interaction at M=15
Direct numerical simulations are carried out for different forcing techniques to trigger transition during the interaction between an oblique shock-wave and a laminar boundary-layer at M = 1.5. Three forcing methods are used: a) forcing of oblique unstable modes, whose shape and behaviour are determined by the local linear stability theory, b) broadband free-stream acoustic disturbances, and c) a cold plasma flow control device. While the oblique-mode breakdown is dominant for low-amplitude forcing, long streaky structures drive the transition process in a high-amplitude disturbance environment. LES are also performed on the experimental setup by the Institute of Theoretical and Applied Mechanics (ITAM) from Novosibirsk State University with cold plasma actuation. As well as the disturbance type, the effect of Reynolds number and forcing amplitude will be investigated
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