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Keywords = UGI cancer

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23 pages, 3384 KiB  
Article
Derivatization of Abietane Acids by Peptide-like Substituents Leads to Submicromolar Cytotoxicity at NCI-60 Panel
by Elena Tretyakova, Anna Smirnova, Denis Babkov and Oxana Kazakova
Molecules 2024, 29(15), 3532; https://doi.org/10.3390/molecules29153532 - 27 Jul 2024
Cited by 1 | Viewed by 1530
Abstract
Natural compounds, including diterpenoids, play a critical role in various biological processes and are recognized as valuable components in cancer treatment. Isocyanides multicomponent reactions (IsMCRs) are one of the effective methods to obtain adducts at the carboxyl group with a peptide-like substituent. In [...] Read more.
Natural compounds, including diterpenoids, play a critical role in various biological processes and are recognized as valuable components in cancer treatment. Isocyanides multicomponent reactions (IsMCRs) are one of the effective methods to obtain adducts at the carboxyl group with a peptide-like substituent. In this study, dehydroabietic acid and levopimaric acid diene adducts as the starting scaffolds were modified by the multicomponent Passerini (P-3CR) and Ugi (U-4CR) reactions to afford α-acyloxycarboxamides and α-acylaminocarboxamides. A group of twenty novel diterpene hybrids was subjected to NCI in vitro assessment, and a consistent structure–activity relationship was established. Eleven of the synthesized derivatives inhibited the growth of cancer cells of 4 to 39 cell lines in one dose assay, and the most active were derivatives 3d, 9d, and 10d holding a fragment of 1a,4a-dehydroquinopimaric acid. They were selected for a five-dose analysis and demonstrated a significant antiproliferative effect towards human cancer cell lines. The outstanding cytotoxic activity was observed for the P-3CR product 3d with growth inhibitory at submicromolar and micromolar concentrations (GI50 = 0.42–3 μM) against the most sensitive cell lines. The U-4CR products 9d and 10d showed selective activity against all leukemia cell lines with GI50 in the range of 1–17 µM and selectivity indexes of 5.49 and 4.72, respectively. Matrix COMPARE analysis using the GI50 vector showed a moderate positive correlation of compound 3d with standard anticancer agents that can influence kinase receptors and epidermal growth factor receptors (EGFRs). The ADMET analysis acknowledges the favorable prognosis using compounds as potential anticancer agents. The obtained results indicate that these new hybrids could be useful for the further development of anticancer drugs, and 1a,4a-dehydroquinopimaric acid derivatives could be recommended for in-depth studies and the synthesis of new antitumor analogs on their basis. Full article
(This article belongs to the Special Issue Lead Compounds Discovery and Antitumor Drug Design)
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12 pages, 2602 KiB  
Communication
A Facile Ugi/Ullmann Cascade Reaction to Access Fused Indazolo-Quinoxaline Derivatives with Potent Anticancer Activity
by Yong Li, Liujun He, Hongxia Qin, Yao Liu, Binxin Yang, Zhigang Xu and Donglin Yang
Molecules 2024, 29(2), 464; https://doi.org/10.3390/molecules29020464 - 17 Jan 2024
Cited by 3 | Viewed by 1750
Abstract
A facile methodology for the construction of a complex heterocycle indazolo-fused quinoxalinone has been developed via an Ugi four-component reaction (U-4CR) followed by an intramolecular Ullmann reaction. The expeditious process features an operationally simple approach, time efficiency, and a broad substrate scope. Biological [...] Read more.
A facile methodology for the construction of a complex heterocycle indazolo-fused quinoxalinone has been developed via an Ugi four-component reaction (U-4CR) followed by an intramolecular Ullmann reaction. The expeditious process features an operationally simple approach, time efficiency, and a broad substrate scope. Biological activity was evaluated and demonstrated that compound 6e inhibits human colon cancer cell HCT116 proliferation with an IC50 of 2.1 μM, suggesting potential applications for developing a drug lead in medicinal chemistry. Full article
(This article belongs to the Special Issue Synthesis and Properties of Heterocyclic Compounds: Recent Advances)
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29 pages, 5815 KiB  
Article
Synthesis of Pyrrolo[3,4-b]pyridin-5-ones via Ugi–Zhu Reaction and In Vitro–In Silico Studies against Breast Carcinoma
by Ivette Morales-Salazar, Carlos E. Garduño-Albino, Flora P. Montes-Enríquez, Dania A. Nava-Tapia, Napoleón Navarro-Tito, Leonardo David Herrera-Zúñiga, Eduardo González-Zamora and Alejandro Islas-Jácome
Pharmaceuticals 2023, 16(11), 1562; https://doi.org/10.3390/ph16111562 - 6 Nov 2023
Cited by 9 | Viewed by 3222
Abstract
An Ugi–Zhu three-component reaction (UZ-3CR) coupled in a one-pot manner to a cascade process (N-acylation/aza Diels–Alder cycloaddition/decarboxylation/dehydration) was performed to synthesize a series of pyrrolo[3,4-b]pyridin-5-ones in 20% to 92% overall yields using ytterbium triflate as a catalyst, toluene [...] Read more.
An Ugi–Zhu three-component reaction (UZ-3CR) coupled in a one-pot manner to a cascade process (N-acylation/aza Diels–Alder cycloaddition/decarboxylation/dehydration) was performed to synthesize a series of pyrrolo[3,4-b]pyridin-5-ones in 20% to 92% overall yields using ytterbium triflate as a catalyst, toluene as a solvent, and microwaves as a heat source. The synthesized molecules were evaluated in vitro against breast cancer cell lines MDA-MB-231 and MCF-7, finding that compound 1f, at a concentration of 6.25 μM, exhibited a potential cytotoxic effect. Then, to understand the interactions between synthesized compounds and the main proteins related to the cancer cell lines, docking studies were performed on the serine/threonine kinase 1 (AKT1) and Orexetine type 2 receptor (Ox2R), finding moderate to strong binding energies, which matched accurately with the in vitro results. Additionally, molecular dynamics were performed between proteins related to the studied cell lines and the three best ligands. Full article
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22 pages, 14729 KiB  
Article
Rational Design and Multicomponent Synthesis of Lipid–Peptoid Nanocomposites towards a Customized Drug Delivery System Assembly
by Thaissa Pasquali F. Rosalba, Guilherme D. R. Matos, Carlos Eduardo M. Salvador and Carlos Kleber Z. Andrade
Molecules 2023, 28(15), 5725; https://doi.org/10.3390/molecules28155725 - 28 Jul 2023
Cited by 4 | Viewed by 1681
Abstract
Nanotechnology has assumed a significant role over the last decade in the development of various technologies applied to health sciences. This becomes even more evident with its application in controlled drug delivery systems. In this context, peptoids are a promising class of compounds [...] Read more.
Nanotechnology has assumed a significant role over the last decade in the development of various technologies applied to health sciences. This becomes even more evident with its application in controlled drug delivery systems. In this context, peptoids are a promising class of compounds for application as nanocarriers in drug delivery systems. These compounds can be obtained efficiently and with highly functionalized structural diversity via the Ugi 4-component reaction (U-4CR). Herein, we report the design of the process control strategy for the future development of lipid–peptoid-based customized drug delivery system assemblies. Over 20 lipid–peptoid nanocomposites were synthesized via the U-4CR in good to excellent yields. These products were successfully submitted to the nanoparticle formation by the emulsification–evaporation process from lipophilic solution and analyzed via Dynamic Light Scattering (DLS). Several molecules generated nanoparticles with a size ≤200 nm, making them good candidates for drug delivery systems, such as in cancer treatment. Full article
(This article belongs to the Special Issue Organic Nanomaterials: Synthesis and Applications)
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12 pages, 1267 KiB  
Article
Healthy Diet, Polygenic Risk Score, and Upper Gastrointestinal Cancer Risk: A Prospective Study from UK Biobank
by Wenmin Liu, Tianpei Wang, Meng Zhu and Guangfu Jin
Nutrients 2023, 15(6), 1344; https://doi.org/10.3390/nu15061344 - 10 Mar 2023
Cited by 15 | Viewed by 4574
Abstract
Dietary and genetic factors are considered to be associated with UGI cancer risk. However, examinations of the effect of healthy diet on UGI cancer risk and the extent to which healthy diet modifies the impact of genetic susceptibility on UGI cancer remains limited. [...] Read more.
Dietary and genetic factors are considered to be associated with UGI cancer risk. However, examinations of the effect of healthy diet on UGI cancer risk and the extent to which healthy diet modifies the impact of genetic susceptibility on UGI cancer remains limited. Associations were analyzed through Cox regression of the UK Biobank data (n = 415,589). Healthy diet, based on “healthy diet score,” was determined according to fruit, vegetables, grains, fish, and meat consumption. We compared adherence to healthy diet and the risk of UGI cancer. We also constructed a UGI polygenic risk score (UGI-PRS) to assess the combined effect of genetic risk and healthy diet. For the results high adherence to healthy diet reduced 24% UGI cancer risk (HR high-quality diet: 0.76 (0.62–0.93), p = 0.009). A combined effect of high genetic risk and unhealthy diet on UGI cancer risk was observed, with HR reaching 1.60 (1.20–2.13, p = 0.001). Among participants with high genetic risk, the absolute five-year incidence risk of UGI cancer was significantly reduced, from 0.16% to 0.10%, by having a healthy diet. In summary, healthy diet decreased UGI cancer risk, and individuals with high genetic risk can attenuate UGI cancer risk by adopting a healthy diet. Full article
(This article belongs to the Special Issue Dietary Patterns and Nutritional Value in Non-communicable Diseases)
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23 pages, 4355 KiB  
Article
3D-Printing of Capsule Devices as Compartmentalization Tools for Supported Reagents in the Search of Antiproliferative Isatins
by Camilla Malatini, Carlos Carbajales, Mariángel Luna, Osvaldo Beltrán, Manuel Amorín, Christian F. Masaguer, José M. Blanco, Silvia Barbosa, Pablo Taboada and Alberto Coelho
Pharmaceuticals 2023, 16(2), 310; https://doi.org/10.3390/ph16020310 - 16 Feb 2023
Cited by 4 | Viewed by 3118
Abstract
The application of high throughput synthesis methodologies in the generation of active pharmaceutical ingredients (APIs) currently requires the use of automated and easily scalable systems, easy dispensing of supported reagents in solution phase organic synthesis (SPOS), and elimination of purification and extraction steps. [...] Read more.
The application of high throughput synthesis methodologies in the generation of active pharmaceutical ingredients (APIs) currently requires the use of automated and easily scalable systems, easy dispensing of supported reagents in solution phase organic synthesis (SPOS), and elimination of purification and extraction steps. The recyclability and recoverability of supported reagents and/or catalysts in a rapid and individualized manner is a challenge in the pharmaceutical industry. This objective can be achieved through a suitable compartmentalization of these pulverulent reagents in suitable devices for it. This work deals with the use of customized polypropylene permeable-capsule devices manufactured by 3D printing, using the fused deposition modeling (FDM) technique, adaptable to any type of flask or reactor. The capsules fabricated in this work were easily loaded “in one step” with polymeric reagents for use as scavengers of isocyanides in the work-up process of Ugi multicomponent reactions or as compartmentalized and reusable catalysts in copper-catalyzed cycloadditions (CuAAC) or Heck palladium catalyzed cross-coupling reactions (PCCCRs). The reaction products are different series of diversely substituted isatins, which were tested in cancerous cervical HeLa and murine 3T3 Balb fibroblast cells, obtaining potent antiproliferative activity. This work demonstrates the applicability of 3D printing in chemical processes to obtain anticancer APIs. Full article
(This article belongs to the Special Issue 3D Printing of Drug Formulations)
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9 pages, 534 KiB  
Article
Evaluation of Tumor Necrosis Factor-Alpha Gene (−308 G/A, −238 G/A and −857 C/T) Polymorphisms and the Risk of Gastric Cancer in Eastern Indian Population
by Kanishka Uthansingh, Girish Kumar Pati, Prasanta Kumar Parida, Jimmy Narayan, Subhasis Pradhan, Manoj Kumar Sahu and Rabindra Nath Padhy
Gastroenterol. Insights 2022, 13(4), 340-348; https://doi.org/10.3390/gastroent13040034 - 10 Oct 2022
Cited by 4 | Viewed by 2826
Abstract
Introduction: Gastric cancer (GC) is one of the leading causes of cancer-related decimations worldwide. The gastric infection at both the stomach and duodenum with Helicobacter pylori causes inflammation by the tumor necrosis factor-alpha (TNF-α). The aim of the study was to associate and [...] Read more.
Introduction: Gastric cancer (GC) is one of the leading causes of cancer-related decimations worldwide. The gastric infection at both the stomach and duodenum with Helicobacter pylori causes inflammation by the tumor necrosis factor-alpha (TNF-α). The aim of the study was to associate and evaluate the three TNF-α gene polymorphisms at positions −308 G/A, −238 G/A, and −857 C/T with the risk of GC. Methods: A total of 156 individuals (consecutively diagnosed 95 GC patients and 61 controls) above the age of 18 years were enrolled in the study. Healthy individuals with normal upper gastrointestinal endoscopy (UGIE) irrespective of their family history of GC or peptic ulcer were included as controls. The cited three TNF-α gene polymorphisms were evaluated using polymerase chain reaction-restriction fragment length polymorphism (RFLP). Results: There was no significant difference in the distribution of gene polymorphisms as genetic factors, TNF-α−308 GA/AA (22.1% vs. 14.8%, p = 0.2), TNF-α−238 GA/AA (21% vs. 19.6%, p = 0.8), and TNF-α−857 CT/TT (8.4% vs. 11.5%, p = 0.5), between GC cases and healthy controls. A subgroup analysis of H. pylori-positive patients showed that there was no significant difference in the distribution of GA/AA polymorphisms in TNF-α−308 (15(45.5%) vs. 3(23%); p = 0.17) and −238 (12(36.3%) vs. 2(15.4%); p = 0.17), and the distribution of TT/CT −857 CT/TT (13(39.4%) vs. 2(15.4%); p = 0.13), among the GC cases and controls. Conclusion: The statistical comparisons of GA/AA vs. GG genotypes at −308 (with OR = 1.6, 95% CI: 0.6–3.8), −238 (OR = 1.09, 95% CI: 0.4–2.4) and TT/CT vs. CC genotypes at −857 (OR = 0.7, 95% CI: 0.2–2.1) did not suggest any association of TNF-α with GC in the population herein. Hence, the TNF-α (−308 G/A, −238 G/A and −857 C/T) may not be the associating factor for GC incidence determined by the PCR–RFLP method. Full article
(This article belongs to the Collection Advances in Gastrointestinal Cancer)
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11 pages, 2695 KiB  
Article
Comparative Study of Helicobacter pylori-Infected Gastritis in Okinawa and Tokyo Based on the Kyoto Classification of Gastritis
by Shotaro Oki, Tsutomu Takeda, Mariko Hojo, Ryota Uchida, Nobuyuki Suzuki, Daiki Abe, Atsushi Ikeda, Yoichi Akazawa, Hiroya Ueyama, Shuko Nojiri, Shinichi Hoshino, Hayashi Shokita and Akihito Nagahara
J. Clin. Med. 2022, 11(19), 5739; https://doi.org/10.3390/jcm11195739 - 28 Sep 2022
Cited by 3 | Viewed by 3048
Abstract
The incidence of gastric cancer in Okinawa Prefecture is the lowest in Japan, which is attributed to differences in strains of Helicobacter pylori in Okinawa and other prefectures in Japan. Our aim was to compare the endoscopic findings of H. pylori-infected gastric [...] Read more.
The incidence of gastric cancer in Okinawa Prefecture is the lowest in Japan, which is attributed to differences in strains of Helicobacter pylori in Okinawa and other prefectures in Japan. Our aim was to compare the endoscopic findings of H. pylori-infected gastric mucosa in Okinawa and Tokyo. Patients who underwent upper gastrointestinal endoscopy (UGI) at Northern Okinawa Medical Center (Okinawa group) and Juntendo University Hospital (Tokyo group) from April 2019 to March 2020 were included. Patients diagnosed with H. pylori-infected gastric mucosa were retrospectively compared between the Okinawa and Tokyo groups according to the Kyoto Classification of Gastritis. The numbers of subjects (Okinawa/Tokyo) were 435/352, male/female ratio was 247:188/181:171, and age was 53.3 ± 14.7/64.6 ± 14.3 (mean ± standard deviation) years. Regarding the Kyoto Classification of Gastritis, the prevalence (Okinawa/Tokyo) of the closed type of atrophic gastritis was 73%/37% (p < 0.001), diffuse redness 80%/84% (p = 0.145), mucosal swelling 46%/46% (p = 0.991), enlarged fold 26%/32% (p = 0.048), spotty redness 77%/68% (p = 0.002), sticky mucus 17%/36% (p < 0.001), and intestinal metaplasia 32%/42% (p < 0.001). Age analysis also revealed that closed-type atrophy and spotty redness were more frequent in the Okinawa group than in the Tokyo group. There may be regional differences in endoscopic findings of H. pylori-infected gastric mucosa between Okinawa and Tokyo. Full article
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14 pages, 1194 KiB  
Article
Synthesis of Novel Lipophilic Polyamines via Ugi Reaction and Evaluation of Their Anticancer Activity
by Artemiy Nichugovskiy, Varvara Maksimova, Ekaterina Trapeznikova, Elizaveta Eshtukova-Shcheglova, Igor Ivanov, Marianna Yakubovskaya, Kirill Kirsanov, Dmitry Cheshkov, Gian Cesare Tron and Mikhail Maslov
Molecules 2022, 27(19), 6218; https://doi.org/10.3390/molecules27196218 - 21 Sep 2022
Cited by 6 | Viewed by 2997
Abstract
Natural polyamines (PAs) are involved in the processes of proliferation and differentiation of cancer cells. Lipophilic synthetic polyamines (LPAs) induce the cell death of various cancer cell lines. In the current paper, we have demonstrated a new method for synthesis of LPAs via [...] Read more.
Natural polyamines (PAs) are involved in the processes of proliferation and differentiation of cancer cells. Lipophilic synthetic polyamines (LPAs) induce the cell death of various cancer cell lines. In the current paper, we have demonstrated a new method for synthesis of LPAs via the multicomponent Ugi reaction and subsequent reduction of amide groups by PhSiH3. The anticancer activity of the obtained compounds was evaluated in the A-549, MCF7, and HCT116 cancer cell lines. For the first time, it was shown that the anticancer activity of LPAs with piperazine fragments is comparable with that of aliphatic LPAs. The presence of a diglyceride fragment in the structure of LPAs appears to be a key factor for the manifestation of high anticancer activity. The findings of the study strongly support further research in the field of LPAs and their derivatives. Full article
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation III)
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26 pages, 2337 KiB  
Review
Artificial Intelligence for Upper Gastrointestinal Endoscopy: A Roadmap from Technology Development to Clinical Practice
by Francesco Renna, Miguel Martins, Alexandre Neto, António Cunha, Diogo Libânio, Mário Dinis-Ribeiro and Miguel Coimbra
Diagnostics 2022, 12(5), 1278; https://doi.org/10.3390/diagnostics12051278 - 21 May 2022
Cited by 25 | Viewed by 9764
Abstract
Stomach cancer is the third deadliest type of cancer in the world (0.86 million deaths in 2017). In 2035, a 20% increase will be observed both in incidence and mortality due to demographic effects if no interventions are foreseen. Upper GI endoscopy (UGIE) [...] Read more.
Stomach cancer is the third deadliest type of cancer in the world (0.86 million deaths in 2017). In 2035, a 20% increase will be observed both in incidence and mortality due to demographic effects if no interventions are foreseen. Upper GI endoscopy (UGIE) plays a paramount role in early diagnosis and, therefore, improved survival rates. On the other hand, human and technical factors can contribute to misdiagnosis while performing UGIE. In this scenario, artificial intelligence (AI) has recently shown its potential in compensating for the pitfalls of UGIE, by leveraging deep learning architectures able to efficiently recognize endoscopic patterns from UGIE video data. This work presents a review of the current state-of-the-art algorithms in the application of AI to gastroscopy. It focuses specifically on the threefold tasks of assuring exam completeness (i.e., detecting the presence of blind spots) and assisting in the detection and characterization of clinical findings, both gastric precancerous conditions and neoplastic lesion changes. Early and promising results have already been obtained using well-known deep learning architectures for computer vision, but many algorithmic challenges remain in achieving the vision of AI-assisted UGIE. Future challenges in the roadmap for the effective integration of AI tools within the UGIE clinical practice are discussed, namely the adoption of more robust deep learning architectures and methods able to embed domain knowledge into image/video classifiers as well as the availability of large, annotated datasets. Full article
(This article belongs to the Special Issue Advances in the Detection and Screening of Gastric Cancer)
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18 pages, 1956 KiB  
Article
Greener Synthesis of Antiproliferative Furoxans via Multicomponent Reactions
by Mariana Ingold, Victoria de la Sovera, Rosina Dapueto, Paola Hernández, Williams Porcal and Gloria V. López
Molecules 2022, 27(6), 1756; https://doi.org/10.3390/molecules27061756 - 8 Mar 2022
Cited by 3 | Viewed by 2424
Abstract
Prostate and bladder cancers are commonly diagnosed malignancies in men. Several nitric oxide donor compounds with strong antitumor activity have been reported. Thus, continuing with our efforts to explore the chemical space around bioactive furoxan moiety, multicomponent reactions were employed for the rapid [...] Read more.
Prostate and bladder cancers are commonly diagnosed malignancies in men. Several nitric oxide donor compounds with strong antitumor activity have been reported. Thus, continuing with our efforts to explore the chemical space around bioactive furoxan moiety, multicomponent reactions were employed for the rapid generation of molecular diversity and complexity. We herein report the use of Ugi and Groebke–Blackburn–Bienaymé multicomponent reactions under efficient, safe, and environmentally friendly conditions to synthesize a small collection of nitric-oxide-releasing molecules. The in vitro antiproliferative activity of the synthesized compounds was measured against two different human cancer cell lines, LNCaP (prostate) and T24 (bladder). Almost all compounds displayed antiproliferative activity against both cancer cell lines, providing lead compounds with nanomolar GI50 values against the cancer bladder cell line with selectivity indices higher than 10. Full article
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22 pages, 5913 KiB  
Review
Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
by Artemiy Nichugovskiy, Gian Cesare Tron and Mikhail Maslov
Molecules 2021, 26(21), 6579; https://doi.org/10.3390/molecules26216579 - 30 Oct 2021
Cited by 13 | Viewed by 6139
Abstract
Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ [...] Read more.
Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in their structure, have demonstrated high antitumor activity and are involved in clinical trials. The chemical synthesis of PAs and their conjugates require the correct choice of synthetic pathways—methods for constructing conjugates and the orthogonal protection of amino groups. The most common methods of synthesis of PA conjugates are acylation of regioselectively protected PAs or their alkylation under the conditions of the Fukuyama reaction. One of the most promising methods of PA synthesis is the use of a multicomponent Ugi reaction, which allows various PAs to be obtained in high yields. In this review, we describe and analyze various approaches that are used in the synthesis of polyamines and their conjugates. Full article
(This article belongs to the Special Issue Polyamine Drug Discovery)
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14 pages, 2259 KiB  
Article
A One-Pot Six-Component Reaction for the Synthesis of 1,5-Disubstituted Tetrazol-1,2,3-Triazole Hybrids and Their Cytotoxic Activity against the MCF-7 Cell Line
by Cesia M. Aguilar-Morales, Jorge Gustavo Araujo-Huitrado, Yamilé López-Hernández, Claudia Contreras-Celedón, Alejandro Islas-Jácome, Angelica Judith Granados-López, Cesar R. Solorio-Alvarado, Jesús Adrián López, Luis Chacón-García and Carlos J. Cortés-García
Molecules 2021, 26(20), 6104; https://doi.org/10.3390/molecules26206104 - 10 Oct 2021
Cited by 13 | Viewed by 3494
Abstract
A high-order multicomponent reaction involving a six-component reaction to obtain the novel linked 1,5-disubstituted tetrazole-1,2,3-triazole hybrids in low to moderate yield is described. This one-pot reaction is carried out under a cascade process consisting of three sequential reactions: Ugi-azide, bimolecular nucleophilic substitution (S [...] Read more.
A high-order multicomponent reaction involving a six-component reaction to obtain the novel linked 1,5-disubstituted tetrazole-1,2,3-triazole hybrids in low to moderate yield is described. This one-pot reaction is carried out under a cascade process consisting of three sequential reactions: Ugi-azide, bimolecular nucleophilic substitution (SN2), and copper-catalyzed alkyne–azide reaction (CuAAC), with high atom and step-economy due the formation of six new bonds (one C-C, four C-N, and one N-N). Thus, the protocol developed offers operational simplicity, mild reaction conditions, and structural diversity. Finally, to evaluate the antitumoral potential of the synthetized molecules, a proliferation study was performed in the breast cancer (BC) derived cell line MCF-7. The hybrid compounds showed several degrees of cell proliferation inhibition with a remarkable effect in those compounds with cyclohexane and halogens in their structures. These compounds represent potential drug candidates for breast cancer treatment. However, additionally assays are needed to elucidate their complete effect over the cellular hallmarks of cancer. Full article
(This article belongs to the Special Issue New Approach in Multicomponent Reactions)
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17 pages, 724 KiB  
Article
Assessment of Nutritional Status and Nutrition Impact Symptoms in Patients Undergoing Resection for Upper Gastrointestinal Cancer: Results from the Multi-Centre NOURISH Point Prevalence Study
by Irene Deftereos, Justin M. C. Yeung, Janan Arslan, Vanessa M. Carter, Elizabeth Isenring, Nicole Kiss and on behalf of The NOURISH Point Prevalence Study Group
Nutrients 2021, 13(10), 3349; https://doi.org/10.3390/nu13103349 - 24 Sep 2021
Cited by 37 | Viewed by 5147
Abstract
Background: Identification and treatment of malnutrition are essential in upper gastrointestinal (UGI) cancer. However, there is limited understanding of the nutritional status of UGI cancer patients at the time of curative surgery. This prospective point prevalence study involving 27 Australian tertiary hospitals investigated [...] Read more.
Background: Identification and treatment of malnutrition are essential in upper gastrointestinal (UGI) cancer. However, there is limited understanding of the nutritional status of UGI cancer patients at the time of curative surgery. This prospective point prevalence study involving 27 Australian tertiary hospitals investigated nutritional status at the time of curative UGI cancer resection, as well as presence of preoperative nutrition impact symptoms, and associations with length of stay (LOS) and surgical complications. Methods: Subjective global assessment, hand grip strength (HGS) and weight were performed within 7 days of admission. Data on preoperative weight changes, nutrition impact symptoms, and dietary intake were collected using a purpose-built data collection tool. Surgical LOS and complications were also recorded. Multivariate regression models were developed for nutritional status, unintentional weight loss, LOS and complications. Results: This study included 200 patients undergoing oesophageal, gastric and pancreatic surgery. Malnutrition prevalence was 42% (95% confidence interval (CI) 35%, 49%), 49% lost ≥5% weight in 6 months, and 47% of those who completed HGS assessment had low muscle strength with no differences between surgical procedures (p = 0.864, p = 0.943, p = 0.075, respectively). The overall prevalence of reporting at least one preoperative nutrition impact symptom was 55%, with poor appetite (37%) and early satiety (23%) the most frequently reported. Age (odds ratio (OR) 4.1, 95% CI 1.5, 11.5, p = 0.008), unintentional weight loss of ≥5% in 6 months (OR 28.7, 95% CI 10.5, 78.6, p < 0.001), vomiting (OR 17.1, 95% CI 1.4, 207.8, 0.025), reduced food intake lasting 2–4 weeks (OR 7.4, 95% CI 1.3, 43.5, p = 0.026) and ≥1 month (OR 7.7, 95% CI 2.7, 22.0, p < 0.001) were independently associated with preoperative malnutrition. Factors independently associated with unintentional weight loss were poor appetite (OR 3.7, 95% CI 1.6, 8.4, p = 0.002) and degree of solid food reduction of <75% (OR 3.3, 95% CI 1.2, 9.2, p = 0.02) and <50% (OR 4.9, 95% CI 1.5, 15.6, p = 0.008) of usual intake. Malnutrition (regression coefficient 3.6, 95% CI 0.1, 7.2, p = 0.048) and unintentional weight loss (regression coefficient 4.1, 95% CI 0.5, 7.6, p = 0.026) were independently associated with LOS, but no associations were found for complications. Conclusions: Despite increasing recognition of the importance of preoperative nutritional intervention, a high proportion of patients present with malnutrition or clinically significant weight loss, which are associated with increased LOS. Factors associated with malnutrition and weight loss should be incorporated into routine preoperative screening. Further investigation is required of current practice for dietetics interventions received prior to UGI surgery and if this mitigates the impact on clinical outcomes. Full article
(This article belongs to the Section Nutrition Methodology & Assessment)
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15 pages, 4189 KiB  
Article
Antioxidant Activity of Bioactive Peptide Fractions from Germinated Soybeans Conjugated to Fe3O4 Nanoparticles by the Ugi Multicomponent Reaction
by Yarelys Elena Augusto-Jimenez, Marcela González-Montoya, Dany Naranjo-Feliciano, Daniel Uribe-Ramírez, Eliseo Cristiani-Urbina, Carlos Díaz-Águila, Hernani Yee-Madeira and Rosalva Mora-Escobedo
Molecules 2021, 26(19), 5726; https://doi.org/10.3390/molecules26195726 - 22 Sep 2021
Cited by 10 | Viewed by 3182
Abstract
The conjugation of biomolecules to magnetic nanoparticles has emerged as promising approach in biomedicine as the treatment of several diseases, such as cancer. In this study, conjugation of bioactive peptide fractions from germinated soybeans to magnetite nanoparticles was achieved. Different fractions of germinated [...] Read more.
The conjugation of biomolecules to magnetic nanoparticles has emerged as promising approach in biomedicine as the treatment of several diseases, such as cancer. In this study, conjugation of bioactive peptide fractions from germinated soybeans to magnetite nanoparticles was achieved. Different fractions of germinated soybean peptides (>10 kDa and 5–10 kDa) were for the first time conjugated to previously coated magnetite nanoparticles (with 3-aminopropyltriethoxysilane (APTES) and sodium citrate) by the Ugi four-component reaction. The crystallinity of the nanoparticles was corroborated by X-ray diffraction, while the particle size was determined by scanning transmission electron microscopy. The analyses were carried out using infrared and ultraviolet–visible spectroscopy, dynamic light scattering, and thermogravimetry, which confirmed the coating and functionalization of the magnetite nanoparticles and conjugation of different peptide fractions on their surfaces. The antioxidant activity of the conjugates was determined by the reducing power and hydroxyl radical scavenging activity. The nanoparticles synthesized represent promising materials, as they have found applications in bionanotechnology for enhanced treatment of diseases, such as cancer, due to a higher antioxidant capacity than that of fractions without conjugation. The highest antioxidant capacity was observed for a >10 kDa peptide fraction conjugated to the magnetite nanoparticles coated with APTES. Full article
(This article belongs to the Special Issue Redox Active Molecules in Cancer Treatments)
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