Article
Chemistry, Applied
Yiqi Zhou, Jidong Zhang, Xianheng Wang, Caoyuan Wu, Changkuo Zhao
Summary: A study synthesized 42 novel anticancer drug molecules, some of which exhibited high cytotoxicity against liver cancer and colon cancer cells, while showing lower toxicity to normal cells. One of the compounds was also found to induce a specific type of macrophages to polarize into another type.
NATURAL PRODUCT RESEARCH
(2022)
Article
Chemistry, Medicinal
Filippo Basagni, Jose A. Ortega, Sine M. Bertozzi, Andrea Armirotti, Maria Summa, Rosalia Bertorelli, Manuela Bartolini, Ian R. Mellor, Martina Bedeschi, Giovanni Bottegoni, Vittorio Lembo, Anna Minarini, Andrea Cavalli, Michela Rosini
Summary: Neurodegenerative processes in Alzheimer's disease are associated with impaired cholinergic and glutamatergic neurotransmitter systems. The standard treatment for AD involves the use of acetylcholinesterase inhibitors and NMDAR antagonists. Researchers have developed new hybrids with improved biological profiles, including increased cholinesterase inhibitory potency and selective antagonism towards specific NMDAR subunits. These hybrids also showed increased brain uptake, indicating potential for further chemical optimizations.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Ala' Salem, Alexandra Hagymasi, Barbara Voros-Horvath, Tatjana Safarik, Tomislav Balic, Peter Szabo, Fruzsina Gosi, Sandor Nagy, Szilard Pal, Sandor Kunsagi-Mate, Aleksandar Szechenyi
Summary: Polymorphism of crystalline active pharmaceutical ingredients (APIs) is common, but there are limited reports on polymorphic co-crystals; controlling polymorph generation is crucial due to its impact on API properties. Different solvents can control polymorph nucleation to obtain desired crystal polymorphs; selecting solvents based on HSPs can affect co-crystallization by interacting differently with APIs. The study successfully obtained a new polymorph of 4-aminosalicylic acid-sulfamethazine co-crystals through manipulation of solvent parameters based on HSPs.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Zhongyu Li, Jiwen Li, Mei Sun, Lei Men, Enhua Wang, Yiran Zhao, Keke Li, Xiaojie Gong
Summary: In vivo, drug metabolism plays a crucial role in altering drug composition and determining the pharmacological properties of oral drugs. However, existing in vitro models lack the ability to replicate the complexity of drug metabolism, resulting in poor predictive power. The development of organs-on-chip-based microfluidics system offers a new in vitro drug screening platform that can mimic the metabolic process and pharmacological activity of natural products. This study utilized an improved microfluidic device to establish an in vitro co-culture model, which successfully examined the metabolism of ginsenosides and their effectiveness against tumors. The results demonstrated the validity and controllability of this model, highlighting the essential role of hepatic metabolism in determining ginsenosides efficacy.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Ting Chen, Haitang Liu, Sheng Qiang, Jie Li, Jing Liu, Beibei Chen, Lin Chen, Fufeng Liu, Rui Liu, Xue Jiang, Xiaoyuan Liao
Summary: In this study, a novel polysaccharide-based preservative named carboxymethyl hemicellulose p-hydroxybenzoate (P-CMHC) was synthesized by modifying hemicellulose extracted from eucalyptus waste liquor. P-CMHC showed excellent antioxidant activity, hygroscopic and moisturizing properties, and negligible cytotoxicity, suggesting its potential as a safe and healthy preservative.
CARBOHYDRATE RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Sheng Zhao, Zhi-Peng Wang, Zihua Lin, Guoxing Wei, Xumei Wen, Siyu Li, Xiaohong Yang, Qun Zhang, Chunmei Jing, Yuanwei Dai, Jian Guo, Yun He
Summary: Drug repurposing is a promising strategy to combat antimicrobial resistance, and the conjugation of Mtx with a siderophore can lead to the development of new antibacterials with higher activity against bacteria and lower cytotoxicity to humans.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Medicinal
Daria Elzbieta Nawrot, Ghada Bouz, Ondrsi Jandourek, Klara Konecna, Pavla Paterova, Pavel Barta, Martin Novak, Radim Kucera, Julia Zemanova, Martin Forbak, Jana Kordulakova, Oto Pavlis, Pavla Kubickova, Martin Dolezal, Jan Zitko
Summary: Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the leading cause of death among infectious diseases caused by a single microbe. With the emergence of antimicrobial resistance, the success rate of treating this infection is decreasing, and there is an urgent need for novel treatments. In this study, a novel series of compounds inspired by combining fragments from first-line and second-line agents for tuberculosis were synthesized and evaluated. Compound 10c from the second series showed selective and potent antimycobacterial activity against both drug-sensitive and drug-resistant Mtb strains, with no cytotoxicity. The compound targeted methionine metabolism rather than the folate pathway and had a long half-life, overcoming the limitations of current drugs for tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Pooja V. D. Hegde, Michael D. Howe, Matthew Zimmerman, Helena L. M. Boshoff, Sachin Sharma, Brianna Remache, Ziyi D. Jia, Yan Pan, Anthony C. Baughn, Veronique Dartois, Courtney Aldrich
Summary: Tuberculosis is a deadly infectious disease with limited treatment options. Researchers have developed prodrugs and modified the structure of para-Aminosalicylic acid (PAS) to improve its oral bioavailability and reduce rapid clearance. These innovations have the potential to enhance the therapeutic effectiveness of PAS.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Polymer Science
Muhammad Suhail, Yu-Fang Shao, Quoc Lam Vu, Pao-Chu Wu
Summary: pH-sensitive hydrogels were prepared for targeted drug delivery to the colon. The hydrogels showed high thermal stability, swelling capacity, and drug release in both acidic and basic environments.
Article
Thermodynamics
J. G. Pontes-Neto, T. R. F. Silva, F. O. S. Ribeiro, D. A. Silva, M. F. R. Soares, J. L. Soares-Sobrinho
Summary: Layered double hydroxides can be used as drug delivery systems to improve the dissolution rate of poorly water-soluble drugs, with the reconstitution method proving to be an effective way to intercalate drugs. The interaction between LDH and 5ASA was confirmed through various characterization techniques, showing a 25.5% drug load and indicating the efficiency of the method in drug intercalation.
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY
(2022)
Article
Biochemistry & Molecular Biology
Goran Poje, Marina Marinovic, Kristina Pavic, Marija Mioc, Marijeta Kralj, Lais Pessanha de Carvalho, Jana Held, Ivana Perkovic, Zrinka Rajic
Summary: This study presents the design, synthesis, and evaluation of harmicens, a new class of hybrids with structural diversity. The harmicens showed moderate antiplasmodial activity against malaria and significant and selective antiproliferative activity against cancer cell lines. Cell localization and cycle analysis revealed different mechanisms of action.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Nanoscience & Nanotechnology
Bin Ren, Zhong-Chao Cai, Xue-Jie Zhao, Lin-Song Li, Mei-Xia Zhao
Summary: This study developed a targeted AuNPs drug delivery system with good apoptotic induction effects on folate-receptor overexpressing cancer cells. Experimental results confirmed its excellent anti-tumor activity and demonstrated the mechanism of apoptosis induction by intracellular ROS production through effective internalization of AuNPs.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Chemistry, Multidisciplinary
Houzong Yao, Zhigang Wang, Na Wang, Zhiqin Deng, Gongyuan Liu, Jianghong Zhou, Shu Chen, Jiahai Shi, Guangyu Zhu
Summary: This study presents a rational design of a platinum(IV) anticancer prodrug that can bind to erythrocytes, greatly extending its circulatory half-life and enhancing tumor accumulation. The prodrug demonstrates significantly enhanced antitumor activity and reduced side effects compared to carboplatin.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Oncology
Min Yuen Teo, Jonathan E. Rosenberg
Summary: Nectin-4 serves as the target for enfortumab vedotin, with its gene expression varying significantly across different molecular subtypes and playing a crucial role in the efficacy of enfortumab vedotin.
CLINICAL CANCER RESEARCH
(2021)
Article
Cell Biology
Jing Li, Ruiqin Wu, Mingo M. H. Yung, Jing Sun, Zhuqing Li, Hai Yang, Yi Zhang, Stephanie S. Liu, Annie N. Y. Cheung, Hextan Y. S. Ngan, John C. Braisted, Wei Zheng, Huiqiang Wei, Yingtang Gao, Peter Nemes, Huadong Pei, David W. Chan, Yiliang Li, Wenge Zhu
Summary: The JAK2/STAT pathway is hyperactivated in many cancers, leading to poor clinical prognosis and drug resistance. The protease SENP1 interacts with and deSUMOylates JAK2, promoting JAK2 accumulation in the cytoplasm for activation, which is critical for platinum-resistance in ovarian cancer.
CELL DEATH & DISEASE
(2021)
Article
Materials Science, Biomaterials
Elie Hembe Mukaya, Robyn van Zyl, Natasha Jansen van Vuuren, Xavier Yangkou Mbianda
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2018)
Article
Materials Science, Biomaterials
Kayembe Jacques Diainabo, E. W. Neuse, Chien-Teng Chen, Robyn Lynne Van Zyl
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2019)
Article
Materials Science, Biomaterials
Kayembe Jacques Diainabo, E. W. Neuse, Chien-Teng Chen, Robyn Lynne Van Zyl
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2019)
Correction
Materials Science, Biomaterials
Kayembe Diainabo, E. W. Neuse, Chien-Teng Chen, Robyn Lynne Van Zyl
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2019)
Article
Materials Science, Biomaterials
Hembe E. Mukaya, Robyn L. Van Zyl, Natasha C. Jansen van Vuuren, Chien-Teng Chen, Xavier Y. Mbianda
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2019)
Review
Energy & Fuels
Masego Molefe, Diakanua Nkazi, Hembe Elie Mukaya
Article
Energy & Fuels
Madinoge Bridgiliah Mampuru, Diakanua Bavon Nkazi, Hembe Elie Mukaya
ENERGY SOURCES PART A-RECOVERY UTILIZATION AND ENVIRONMENTAL EFFECTS
(2020)
Article
Materials Science, Multidisciplinary
Aime Victoire Abega, Horace Manga Ngomo, Isaac Nongwe, Hembe Elie Mukaya, Paul-Michel Adolphe Kouoh Sone, Xavier Yangkou Mbianda
Article
Biochemistry & Molecular Biology
Bakolise Mathebula, Kamogelo Rosinah Butsi, Robyn Lynne van Zyl, Natasha Colleen Jansen van Vuuren, Heinrich Carl Hoppe, Joseph Philip Michael, Charles Bernard de Koning, Amanda Louise Rousseau
CHEMICAL BIOLOGY & DRUG DESIGN
(2019)
Review
Education, Scientific Disciplines
Ntsako Portia Chauke, Hembe Elie Mukaya, Diakanua Bavon Nkazi
Article
Materials Science, Biomaterials
N. Dlamini, H. E. Mukaya, R. L. Van Zyl, C. T. Chen, R. J. Zeevaart, X. Y. Mbianda
MATERIALS SCIENCE AND ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
(2019)
Review
Chemistry, Medicinal
Elie Hembe Mukaya, Xavier Yangkou Mbianda
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2020)
Meeting Abstract
Public, Environmental & Occupational Health
Miles B. Markus, Lizette L. Koekemoer, Robyn L. van Zyl
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE
(2019)
