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Keywords = anti-cancer drugs

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19 pages, 2581 KiB  
Article
Design, Synthesis, and Evaluation of EA-Sulfonamides and Indazole-Sulfonamides as Promising Anticancer Agents: Molecular Docking, ADME Prediction, and Molecular Dynamics Simulations
by Nassima Saghdani, Nabil El Brahmi, Abdelmoula El Abbouchi, Rachid Haloui, Souad Elkhattabi, Gérald Guillaumet and Saïd El Kazzouli
Chemistry 2024, 6(6), 1396-1414; https://doi.org/10.3390/chemistry6060083 (registering DOI) - 9 Nov 2024
Abstract
New EA-sulfonamides and indazole-sulfonamides were synthesized, characterized, and evaluated for their anticancer activities. The target compound structures were elucidated using various spectroscopic techniques such as NMR-{1H and 13C}, infrared spectroscopy, and high-resolution mass spectrometry. The anticancer activities of the [...] Read more.
New EA-sulfonamides and indazole-sulfonamides were synthesized, characterized, and evaluated for their anticancer activities. The target compound structures were elucidated using various spectroscopic techniques such as NMR-{1H and 13C}, infrared spectroscopy, and high-resolution mass spectrometry. The anticancer activities of the novel compounds were evaluated against four human cancer cell lines, namely A-549, MCF-7, Hs-683, and SK-MEL-28 as well as the normal cell line HaCaT, using 5-fluorouracil and etoposide as reference drugs. Among the tested compounds, 9, 10, and 13 exhibited potent anticancer activities which are better than or similar to the reference compounds 5-fluorouracil and etoposide, against the A-549, MCF-7, and Hs-683 cancer cell lines, with IC50 values ranging from 0.1 to 1 μM. Molecular docking studies of compounds 9, 10, and 13 showed a strong binding with selected protein kinase targets, which are linked to the tested cancer types. Furthermore, the analysis of the molecular dynamics simulation results demonstrated that compound 9 exhibits significant stability when bound to both JAK3 and ROCK1 kinases. This new compound has the potential to be developed as a novel therapeutic agent against various cancers. Full article
(This article belongs to the Special Issue Cutting-Edge Studies of Computational Approaches in Drug Discovery)
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19 pages, 915 KiB  
Article
Optimized Liquid Medium Formulation for Sanghuangporus vaninii and Biological Activity of the Exopolysaccharides
by Haichen Huang, Xiaomin Li, Qi Lu, Hui Xu, Huijuan Sun, Junli Zhang, Xiaoping Wu and Junsheng Fu
Foods 2024, 13(22), 3574; https://doi.org/10.3390/foods13223574 (registering DOI) - 8 Nov 2024
Viewed by 271
Abstract
Aims: Sanghuangporus vaninii (S. vaninii) is a rare medicinal mushroom that is rich in polysaccharides, triterpenes, flavonoids, and other bioactive compounds. It has good potential development value. Methods and Results: We performed single factor experiments and Box-Behnken response surface methodology to [...] Read more.
Aims: Sanghuangporus vaninii (S. vaninii) is a rare medicinal mushroom that is rich in polysaccharides, triterpenes, flavonoids, and other bioactive compounds. It has good potential development value. Methods and Results: We performed single factor experiments and Box-Behnken response surface methodology to optimize the liquid fermentation medium formulation for S. vaninii with mycelial biomass as the indicator. The in vitro antioxidant and anti-cancer capacity of the exopolysaccharides of S. vaninii were estimated. The optimal liquid fermentation media composition for the MS-4, MS-6, and MS-8 strains of Sanghuangporus vaninii consisted of 25.86 ± 0.068 g/L maltose, 7.3 ± 0.043 g/L yeast extract, and 0.71 ± 0.005 g/L dandelion powder. The average mycelial biomass of S. vaninii under optimal conditions was 12.61 g/L. The mycelial biomass of the Sanghuangporus vaninii strains in the optimized formulation was 109–191% higher than that obtained with the basic potato dextrose broth (PDB). The exopolysaccharides of Sanghuangporus vaninii exhibited an ABTS radical scavenging activity with an EC50 of 0.021 ± 0.017 mg/mL and a DPPH radical scavenging activity with an EC50 of 0.076 ± 0.043 mg/mL. In anti-cancer assays, these exopolysaccharides demonstrated an IC50 value of 1.98 ± 0.36 mg/mL against PC-3 human prostate cancer cells, indicating significant bioactivity, highlighting their potential as functional food ingredients. Conclusions: In this study, the formula of liquid fermentation of S. vaninii strains was optimized, which lays a theoretical foundation for increasing the yield of S. vaninii and its application in industry. Moreover, our data showed the clinical potential of the S. vaninii exopolysaccharides as antioxidants and anti-cancer drugs. Full article
(This article belongs to the Section Food Physics and (Bio)Chemistry)
13 pages, 2737 KiB  
Article
Genomic Comparisons Revealed the Key Genotypes of Streptomyces sp. CB03234-GS26 to Optimize Its Growth and Relevant Production of Tiancimycins
by Huiming Liu, Jing Lin, Yong Huang, Yanwen Duan and Xiangcheng Zhu
Bioengineering 2024, 11(11), 1128; https://doi.org/10.3390/bioengineering11111128 - 8 Nov 2024
Viewed by 230
Abstract
Strain robustness and titer improvement are major challenges faced in the industrial development of natural products from Streptomyces. Tiancimycins (TNMs) produced by Streptomyces sp. CB03234 are promising anticancer payloads for antibody-drug conjugates, but further development is severely limited by the low titer [...] Read more.
Strain robustness and titer improvement are major challenges faced in the industrial development of natural products from Streptomyces. Tiancimycins (TNMs) produced by Streptomyces sp. CB03234 are promising anticancer payloads for antibody-drug conjugates, but further development is severely limited by the low titer of TNMs. Despite many efforts to generate various TNMs overproducers, the mechanisms underlying high TNMs production remain to be explored. Herein, genome resequencing and genomic comparisons of different TNMs overproducers were conducted to explore the unique genotypes in CB03234-GS26. Four target genes were selected for further bioinformatic analyses and genetic validations. The results indicated that the inactivation of histidine ammonia-lyase (HAL) showed the most significant effect by blocking the intracellular degradation of histidine to facilitate relevant enzymatic catalysis and thus improve the production of TNMs. Additionally, the potassium/proton antiporter (P/PA) was crucial for intracellular pH homeostasis, and its deficiency severely impaired the alkaline tolerance of the cells. Subsequent pan-genomic analysis suggested that HAL and P/PA are core enzymes that are highly conserved in Streptomyces. Therefore, HAL and P/PA represented novel targets to regulate secondary metabolism and enhance strain robustness and could become potential synthetic biological modules to facilitate development of natural products and strain improvement in Streptomyces. Full article
(This article belongs to the Special Issue Synthetic Biology and Bioprocess Engineering for High-Value Compounds)
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14 pages, 3464 KiB  
Article
Effects of Flavanone Derivatives on Adipocyte Differentiation and Lipid Accumulation in 3T3-L1 Cells
by Yasuhito Nobushi, Taira Wada, Motofumi Miura, Rikuto Onoda, Ryuta Ishiwata, Naoki Oikawa, Karin Shigematsu, Toshinori Nakakita, Masaharu Toriyama, Shigeki Shimba and Yukinaga Kishikawa
Life 2024, 14(11), 1446; https://doi.org/10.3390/life14111446 - 7 Nov 2024
Viewed by 410
Abstract
Flavanones, a class of flavonoids, are abundant in fruits, vegetables, and herbs. They are known to have several biological activities, such as anti-inflammatory and anti-cancer activities, but their effects on obesity remain unclear. Obesity is closely associated with adipocyte differentiation and lipid accumulation [...] Read more.
Flavanones, a class of flavonoids, are abundant in fruits, vegetables, and herbs. They are known to have several biological activities, such as anti-inflammatory and anti-cancer activities, but their effects on obesity remain unclear. Obesity is closely associated with adipocyte differentiation and lipid accumulation in adipose tissue. Therefore, in this study, we examined the effects of flavanone derivatives on adipocyte differentiation and lipid accumulation by using 3T3-L1 cells. Among the 15 flavanone derivatives studied, 4′-phenylflavanone (4PF), with a biphenyl structure, significantly inhibited adipocyte differentiation-related lipid accumulation in 3T3-L1 cells; this inhibition of lipid accumulation was dose-dependent. Gene expression analysis showed that 4PF suppressed the expression of adipogenic marker genes. Although the induction of peroxisome proliferator activator γ2 (Pparγ2), a master regulator of adipocyte differentiation, and its target genes during adipocyte differentiation was attenuated in 4PF-treated cells, 4PF did not directly regulate Pparγ2 gene expression and its activation. In contrast, 4PF suppressed mitotic clonal expansion (MCE), which is associated with changes in the expression of proliferation-related genes at the early stages of adipocyte differentiation. Taken together, these results suggest that 4PF inhibits lipid accumulation because it suppresses MCE during adipocyte differentiation. Thus, our findings may help in the development of anti-obesity drugs. Full article
(This article belongs to the Special Issue New Updates in Adipocytes and Adipose Tissue: 2nd Edition)
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15 pages, 7584 KiB  
Article
5-Fluorouracil Inhibits Bacterial Growth and Reduces Biofilm in Addition to Having Synergetic Effects with Gentamicin Against Pseudomonas aeruginosa
by Amani A. Niazy, May M. Alrashed, Rhodanne Nicole A. Lambarte and Abdurahman A. Niazy
Microorganisms 2024, 12(11), 2257; https://doi.org/10.3390/microorganisms12112257 - 7 Nov 2024
Viewed by 341
Abstract
Pseudomonas aeruginosa is a multidrug-resistant pathogen known for chronic infections, mainly due to biofilm formation. This study aimed to explore the potential repurposing of 5-fluorouracil (5-FU), an anticancer drug, to treat P. aeruginosa infections. Firstly, we investigated the inhibitory effects of 5-FU on [...] Read more.
Pseudomonas aeruginosa is a multidrug-resistant pathogen known for chronic infections, mainly due to biofilm formation. This study aimed to explore the potential repurposing of 5-fluorouracil (5-FU), an anticancer drug, to treat P. aeruginosa infections. Firstly, we investigated the inhibitory effects of 5-FU on bacterial growth using the microdilution method. Secondly, the impact of 5-FU on biofilm formation and disassembly was assessed via biofilm biomass measurements with the crystal violet staining method and confocal microscopy analyses. Lastly, the potential synergy between 5-FU and the antibiotics gentamicin and meropenem was evaluated using a checkerboard assay. Results revealed that 5-FU inhibited bacterial growth in a dose-dependent manner, with 100% inhibition observed at concentrations of 25 µg/mL and higher. Also, 70% and 100% reductions in biofilm biomass were demonstrated at concentrations of 12 and 100 µg/mL, respectively. Controversy, these higher concentrations unexpectedly increased biofilm biomass in pre-formed biofilms. Synergistic interactions were observed between 5-FU and gentamicin in both growth inhibition (FICI 0.31) and biofilm inhibition (ZIP 14.1), while no synergy was found with meropenem. These findings highlight the potential of 5-FU as an adjunctive therapy for P. aeruginosa infections, especially in combination with gentamicin. However, further research is required to address 5-FU limitations against mature biofilms. Full article
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24 pages, 3304 KiB  
Review
Tungsten Disulfide-Based Materials and Their Conjugates for Cancer Photothermal Therapy
by Ana Rita Lopes, Fernão D. Magalhães, Joana A. Loureiro and Artur M. Pinto
J. Compos. Sci. 2024, 8(11), 460; https://doi.org/10.3390/jcs8110460 - 7 Nov 2024
Viewed by 233
Abstract
Cancer remains one of the most critical global health issues. Conventional treatments, such as radiotherapy, surgery, or chemotherapy, have limitations, especially concerning side effects, resistance, and recurrence. Consequently, new innovative treatments to overcome these problems are needed. Photothermal therapy (PTT) is a promising [...] Read more.
Cancer remains one of the most critical global health issues. Conventional treatments, such as radiotherapy, surgery, or chemotherapy, have limitations, especially concerning side effects, resistance, and recurrence. Consequently, new innovative treatments to overcome these problems are needed. Photothermal therapy (PTT) is a promising alternative that uses photothermal agents that convert near-infrared light (NIR) into heat to kill cancer cells. Nanoparticles can be used as photothermal agents and also as drug delivery platforms, improving the drugs’ stability, allowing for targeted delivery, and reducing toxicity. Due to its broad absorption band, high surface area, and versatility for surface functionalization, tungsten disulfide (WS2) has high potential in this context. This paper presents the state-of-the-art on the use of WS2-based materials to achieve effective and biocompatible new anticancer treatment strategies. Full article
(This article belongs to the Special Issue Feature Papers in Journal of Composites Science in 2024)
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17 pages, 4738 KiB  
Article
Evaluation of Anticancer and Immunomodulatory Effects of Microwave-Extracted Polysaccharide from Ruditapes philippinarum
by Mengyue Liu, Fei Li, Shuang Feng, Jiamin Guo, Jia Yu, Shengcan Zou, Xiang Gao and Yuxi Wei
Foods 2024, 13(22), 3552; https://doi.org/10.3390/foods13223552 - 7 Nov 2024
Viewed by 353
Abstract
In recent years, research on active polysaccharides has progressed significantly, particularly regarding their anticancer and immunomodulatory properties. Among these, clam polysaccharides, a type of marine-derived polysaccharide, exhibit notable biological activities, including both anticancer effects and immune modulation. The aims of this study are [...] Read more.
In recent years, research on active polysaccharides has progressed significantly, particularly regarding their anticancer and immunomodulatory properties. Among these, clam polysaccharides, a type of marine-derived polysaccharide, exhibit notable biological activities, including both anticancer effects and immune modulation. The aims of this study are to investigate the anticancer and immunomodulatory effects of microwave-extracted clam polysaccharide (MCP) in vitro. Cell experiments demonstrated that MCP significantly inhibited both colony formation and migration of HT-29 cells. Furthermore, treatment with MCP led to the downregulation of Bcl-2 gene expression, a reduction in mitochondrial membrane potential, activation of cytochrome C gene and caspase-3 gene, and, finally, the induction of apoptosis in HT-29 cells, implying the involvement of the mitochondrial pathway. Additionally, MCP was found to prompt a phenotypic shift in macrophages from M2 to M1 subtype and from M0 to M1 subtype. MCP also decreased reactive oxygen species (ROS) levels within the cancer cells, thereby augmenting anticancer efficacy through a dual mechanism of immune activation and antioxidant enhancement. These findings suggest that MCPs present significant potential as natural antitumor agents and immunomodulators, especially in the development of functional foods or drugs. Full article
(This article belongs to the Section Nutraceuticals, Functional Foods, and Novel Foods)
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13 pages, 2151 KiB  
Article
In Silico and In Vitro Investigation of Cytotoxicity and Apoptosis of Acridine/Sulfonamide Hybrids Targeting Topoisomerases I and II
by Mohamed Badr, Elshaymaa I. Elmongy, Doaa Elkhateeb, Yasmine S. Moemen, Ashraf Khalil, Hadeer Ali, Reem Binsuwaidan, Feby Awadallah and Ibrahim El Tantawy El Sayed
Pharmaceuticals 2024, 17(11), 1487; https://doi.org/10.3390/ph17111487 - 6 Nov 2024
Viewed by 297
Abstract
Background: Sulfonamide acridine derivatives have garnered significant attention from medicinal chemists due to their diverse range of biological activities. Methods: In this study, eleven compounds were synthesized according to the literature, and their impact on cell growth inhibition, induction of apoptosis, and cell [...] Read more.
Background: Sulfonamide acridine derivatives have garnered significant attention from medicinal chemists due to their diverse range of biological activities. Methods: In this study, eleven compounds were synthesized according to the literature, and their impact on cell growth inhibition, induction of apoptosis, and cell cycle distribution were assessed in three different cell lines. Their inhibitory effects on the topoisomerase (Topo) I and II were investigated in vitro. Molecular docking studies were conducted to predict the binding affinities of these compounds for crystallized downloaded topoisomerases. Results: The compounds were examined in vitro for their anticancer activity against human hepatic (HepG2) colon (HCT-8) and breast (MCF-7) carcinoma cell lines. Compound 8b was the most active against HepG2, HCT-116, and MCF-7 with IC50 14.51, 9.39, and 8.83 µM, respectively, compared to Doxorubicin as reference. In addition, it demonstrated the highest potency among the tested compounds against Topo-I, with an IC50 value of 3.41 µg/mL compared to the control camptothecin (IC50 of 1.46 μM). Compound 7c displayed a significant inhibitory effect on Topo-II, with an IC50 of 7.33 μM, compared to an IC50 value of 6.49 μM via Doxorubicin, the control. Compounds 7c and 8b were assessed against topoisomerases showing induction of apoptosis and a reduction in the S phase of the cell cycle. Molecular docking demonstrated interaction with the active site as with those exhibited by the co-crystallized ligands of the crystallized proteins in both topoisomerases. Conclusion: Compounds 7c and 8b hold promise as potential anticancer drugs due to their anti-proliferative and proapoptotic effects, which are mediated by their action on the topoisomerase enzyme, particularly Topo II. Full article
(This article belongs to the Special Issue Topoisomerases as Targets for Novel Drug Discovery)
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21 pages, 2568 KiB  
Review
Exploring COX-Independent Pathways: A Novel Approach for Meloxicam and Other NSAIDs in Cancer and Cardiovascular Disease Treatment
by Lixia Cheng, Zhenghui Hu, Jiawei Gu, Qian Li, Jiahao Liu, Meiling Liu, Jie Li and Xiaowen Bi
Pharmaceuticals 2024, 17(11), 1488; https://doi.org/10.3390/ph17111488 - 6 Nov 2024
Viewed by 316
Abstract
As a fundamental process of innate immunity, inflammation is associated with the pathologic process of various diseases and constitutes a prevalent risk factor for both cancer and cardiovascular disease (CVD). Studies have indicated that several non-steroidal anti-inflammatory drugs (NSAIDs), including Meloxicam, may prevent [...] Read more.
As a fundamental process of innate immunity, inflammation is associated with the pathologic process of various diseases and constitutes a prevalent risk factor for both cancer and cardiovascular disease (CVD). Studies have indicated that several non-steroidal anti-inflammatory drugs (NSAIDs), including Meloxicam, may prevent tumorigenesis, reduce the risk of carcinogenesis, improve the efficacy of anticancer therapies, and reduce the risk of CVD, in addition to controlling the body’s inflammatory imbalances. Traditionally, most NSAIDs work by inhibiting cyclooxygenase (COX) activity, thereby blocking the synthesis of prostaglandins (PGs), which play a role in inflammation, cancer, and various cardiovascular conditions. However, long-term COX inhibition and reduced PGs synthesis can result in serious side effects. Recent studies have increasingly shown that some selective COX-2 inhibitors and NSAIDs, such as Meloxicam, may exert effects beyond COX inhibition. This emerging understanding prompts a re-evaluation of the mechanisms by which NSAIDs operate, suggesting that their benefits in cancer and CVD treatment may not solely depend on COX targeting. In this review, we will explore the potential COX-independent mechanisms of Meloxicam and other NSAIDs in addressing oncology and cardiovascular health. Full article
(This article belongs to the Section Pharmacology)
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23 pages, 7747 KiB  
Article
Supercomputer-Based Virtual Screening for Deoxyribonucleic Acid Methyltransferase 1 Inhibitors as Novel Anticancer Agents
by Lara Johanna Friedrich, Axel Guthart, Min Zhou, Paola B. Arimondo, Thomas Efferth and Mona Dawood
Int. J. Mol. Sci. 2024, 25(22), 11870; https://doi.org/10.3390/ijms252211870 - 5 Nov 2024
Viewed by 320
Abstract
Targeting epigenetics is a new strategy to treat cancer and develop novel epigenetic drugs with anti-tumor activity. DNA methyltransferases transfer the methyl group from S-adenosyl-L-methionine (SAM) to the cytosine residue in a CpG island, leading to the transcription silencing of the gene. [...] Read more.
Targeting epigenetics is a new strategy to treat cancer and develop novel epigenetic drugs with anti-tumor activity. DNA methyltransferases transfer the methyl group from S-adenosyl-L-methionine (SAM) to the cytosine residue in a CpG island, leading to the transcription silencing of the gene. Hypermethylation can frequently be observed in several tumor types. Hence, the inhibition of DNMT1 has become a novel approach to cure cancer. In this study, virtual screening and molecular docking were performed for more than 11,000 ligands from the ZINC15 database to discover new hypomethylation agents. Four candidate compounds were further tested for their effects on DNMT1 in silico and in vitro. Compounds 2 and 4 showed the best DNMT1 inhibitory activity, but only compound 4 was able to inhibit the growth of several cancer cell lines. The hypomethylation of the luciferase gene by compound 4 was verified by a CMV- luciferase assay using KG-1 cells. Additionally, compound 4 suppressed cell migration in a dose- and time-dependent manner in the wound healing assay. Moreover, cell cycle analyses demonstrated that compound 4 arrested CCRF-CEM cells and MDA-MB-468 cells in the G0/G1 phase. Also, compound 4 significantly induced early and late apoptosis in a dose-dependent manner. In conclusion, we introduce compound 4 as a novel DNMT1 inhibitor with anticancer activity. Full article
(This article belongs to the Special Issue Small Molecule Drug Design and Research: 3rd Edition)
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24 pages, 3599 KiB  
Article
Complementary Treatment of Breast Cancer Cells with Different Metastatic Potential with Iscador Qu in the Presence of Clinically Approved Anticancer Drugs
by Ivan Iliev, Iana Tsoneva, Aleksandrina Nesheva, Galya Staneva, Bozhil Robev, Albena Momchilova and Biliana Nikolova
Curr. Issues Mol. Biol. 2024, 46(11), 12457-12480; https://doi.org/10.3390/cimb46110740 - 5 Nov 2024
Viewed by 472
Abstract
European mistletoe extract (Iscador Qu) has been studied for decades, but it has not ceased to arouse scientific interest. The purpose was to investigate the impact of Iscador Qu on the antiproliferative potential of 11 standard chemotherapeutic agents on two breast cancer cell [...] Read more.
European mistletoe extract (Iscador Qu) has been studied for decades, but it has not ceased to arouse scientific interest. The purpose was to investigate the impact of Iscador Qu on the antiproliferative potential of 11 standard chemotherapeutic agents on two breast cancer cell lines: MCF-7 low-metastatic and MDA-MB-231 high-metastatic and control cell lines (MCF-10A). MTT-dye reduction assay, FACS analysis, and PI staining were utilized. The most promising combinations acting against the MDA-MB-231 cell line were observed upon the simultaneous application of Iscador Qu (80 µg/mL) and Docetaxel, with 4-fold reduction in IC50. An antagonistic effect was found under treatment with Cisplatin and Iscador Qu (1.5-fold increase in IC50). The response of the low-metastatic breast cancer cell line MCF-7 to the tested combinations was different compared to the high-metastatic one. The most pronounced cytotoxic effect was found for the combination of Oxaliplatin and Iscador Qu (20 µg/mL) (5.2-fold IC50 reduction). An antagonistic effect for MCF-7 line was also observed when combinations with Olaparib and Tamoxifen were applied. This in vitro study offers new combinations between Iscador Qu and standard chemotherapeutic agents that hold great promise in establishing breast cancer therapeutic protocols compared to traditional monotherapies. Full article
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7 pages, 1051 KiB  
Case Report
Anti-Cancer Drug-Induced Lyell’s Syndrome: A Series of Two Patients
by Julie Coussirou, Magali Ravoire, Alma Stancu and Léa Vazquez
Curr. Oncol. 2024, 31(11), 6891-6897; https://doi.org/10.3390/curroncol31110509 - 4 Nov 2024
Viewed by 275
Abstract
Lyell’s syndrome or Toxic Epidermal Necrolysis (TEN) is a rare and life-threatening dermatological disease. Most commonly, this syndrome is drug-induced, and is a result of an immune-allergic reaction to medications. Anti-cancer drugs were not the most frequent groups of therapeutic agents related to [...] Read more.
Lyell’s syndrome or Toxic Epidermal Necrolysis (TEN) is a rare and life-threatening dermatological disease. Most commonly, this syndrome is drug-induced, and is a result of an immune-allergic reaction to medications. Anti-cancer drugs were not the most frequent groups of therapeutic agents related to Lyell’s syndrome, but the emergence of new therapeutic classes, particularly targeted therapy and immunotherapy, is changing current data. We present two cases of Lyell’s syndrome induced by anticancer drugs. (1) TEN in a man treated for metastatic urothelial carcinoma with Enfortumab Vedotin. (2) TEN in a man with metastatic melanoma treated with Nivolumab and Ipilimumab. Despite quick medical treatment and transfer to a severe burn unit, both patients died of TEN. Full article
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22 pages, 3765 KiB  
Article
A Novel Delivery System for the Combined Use of Natural Ingredients: The Preparation of Berberine Hydrochloride–Matrine Liposomes and Preliminary Exploration of Their Anti-Tumor Activity
by Min Xu, Zhangkai Ye, JunJing Liu, Shunpeng Zhu, Yuchen Chen, Jia Cai, Yangxi Chen, Long Wang, Liang Zhang and Qiang Ye
Molecules 2024, 29(21), 5210; https://doi.org/10.3390/molecules29215210 - 4 Nov 2024
Viewed by 616
Abstract
Berberine hydrochloride (BH) extracted from Coptis chinensis (CC) and Matrine (MT) separated from Sophora flavescens (SF) are alkaloids with potent anti-bacterial, anti-inflammatory, and anti-tumor effects. Motivated by the clinical practice of using CC and SF together, we aimed to demonstrate that the synergistic [...] Read more.
Berberine hydrochloride (BH) extracted from Coptis chinensis (CC) and Matrine (MT) separated from Sophora flavescens (SF) are alkaloids with potent anti-bacterial, anti-inflammatory, and anti-tumor effects. Motivated by the clinical practice of using CC and SF together, we aimed to demonstrate that the synergistic application of the natural compounds BH and MT could enhance therapeutic effects and minimize side effects. Two types of liposomes, liposomes containing only BH (BH-LP) and liposomes containing both BH and MT (BH-MT-LP), were successfully prepared via the reverse evaporation method. The liposome preparation process was optimized by single-factor screening and the Box–Behnken experimental design method. The results showed that the liposomes had particle sizes in the range of 222.7 to 235.4 nm, polydispersity indicated in the range of 11.8% to 23.3%, and zeta potentials in the range of −35.9 to −31.1 mv. BH-MT-LP showed superior anti-tumor activity against MDA-MB-231, HepG-2, and HGC-27 cells in vitro. The incorporation of MT effectively promoted the anti-tumor effect of BH, while the controlled release from liposomes further enhanced the therapeutic efficacy of BH. Furthermore, based on the flow cytometry results, we speculated that BH-MT-LP might promote apoptosis by blocking the G1 phase of cells and inducing cell death. In conclusion, BH-MT-LP provides evidence for the combined use of natural compounds as a stable, safe, and practical drug delivery system for the treatment of potential cancers. Meanwhile, the successful preparation for BH-MT-LP also provides a new approach to the combined use of traditional Chinese medicine ingredients. Full article
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24 pages, 7219 KiB  
Article
Enhancing Anti-PD-1 Immunotherapy by Targeting MDSCs via Hepatic Arterial Infusion in Breast Cancer Liver Metastases
by Minhyung Kim, Colin A. Powers, Daniel T. Fisher, Amy W. Ku, Nickolay Neznanov, Alfiya F. Safina, Jianmin Wang, Avishekh Gautam, Siddharth Balachandran, Anuradha Krishnamurthy, Katerina V. Gurova, Sharon S. Evans, Andrei V. Gudkov and Joseph J. Skitzki
Cancers 2024, 16(21), 3711; https://doi.org/10.3390/cancers16213711 - 3 Nov 2024
Viewed by 690
Abstract
Background: Surgery, chemotherapy, and radiation often have limited utility for advanced metastatic disease in the liver, and despite its promising activity in select cancers, PD-1 blockade therapy similarly has minimal benefit in this setting. Curaxin, CBL0137, is an experimental anti-cancer drug that disrupts [...] Read more.
Background: Surgery, chemotherapy, and radiation often have limited utility for advanced metastatic disease in the liver, and despite its promising activity in select cancers, PD-1 blockade therapy similarly has minimal benefit in this setting. Curaxin, CBL0137, is an experimental anti-cancer drug that disrupts the binding of DNA to histones, destabilizes chromatin, and induces Z-DNA formation which may stimulate anti-tumor immune responses. Methods: Murine cell lines of colon (CT26) and breast (4T1) cancer were interrogated for survival and CBL0137-associated DNA changes in vitro. Immunocompetent models of liver metastases followed by CBL0137 hepatic arterial infusion (HAI) were used to examine in vivo tumor cell DNA alterations, treatment responses, and the immune contexture associated with CBL0137, both alone and in combination with anti-PD-1 therapy. Results: CBL0137 induced immediate changes to favor tumor cell death in vitro and in vivo with an efficient tumor uptake via the HAI route. Toxicity to CBL0137 was minimal and anti-tumor treatment effects were more efficient with HAI compared to intravenous delivery. Immune effects were pronounced with CBL0137 HAI with concurrent depletion of a specific population of myeloid-derived suppressor cells and maintenance of effector T cell populations. Conclusions: Combination of CBL0137 HAI with PD-1 blockade improved survival in 4T1 tumors but not in CT26 tumors, and therapeutic efficacy relies on the finding of simultaneous and targeted depletion of myeloid-derived suppressor cells and skewing of T cell populations to produce synergy with PD-1 blockade therapy. Full article
(This article belongs to the Special Issue Cancer Immunotherapy in Clinical and Translational Research)
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14 pages, 3813 KiB  
Article
An Electrochemical Biosensor Analysis of the Interaction of a Two-Vector Phospholipid Composition of Doxorubicin with dsDNA and Breast Cancer Cell Models In Vitro
by Lyubov V. Kostryukova, Anastasia S. Serdyukova, Veronica V. Pronina, Victoria V. Shumyantseva and Yulia A. Tereshkina
Pharmaceutics 2024, 16(11), 1412; https://doi.org/10.3390/pharmaceutics16111412 - 2 Nov 2024
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Abstract
Objectives: The main aim of our experiments was to demonstrate the suitability of cell-based biosensors for searching for new anticancer medicinal preparations. Methods: The effect of the substance doxorubicin, doxorubicin embedded in phospholipid nanoparticles, and doxorubicin with phospholipid nanoparticles modified by targeting vectors [...] Read more.
Objectives: The main aim of our experiments was to demonstrate the suitability of cell-based biosensors for searching for new anticancer medicinal preparations. Methods: The effect of the substance doxorubicin, doxorubicin embedded in phospholipid nanoparticles, and doxorubicin with phospholipid nanoparticles modified by targeting vectors (cRGD and folic acid) on dsDNA and breast cancer cell lines (MCF-7, MDA-MB-231) was studied. Results: In the obtained doxorubicin nanoforms, the particle size was less than 60 nm. Our study of the percentage of doxorubicin inclusion showed the almost complete embeddability of the substance into nanoparticles for all samples, with an average of 95.4 ± 4.6%. The calculation of the toxicity index of the studied doxorubicin samples showed that all substances were moderately toxic drugs in terms of adenine and guanine. The biosensor analysis using electrodes modified with carbon nanotubes showed an intercalation interaction between doxorubicin and its derivatives and dsDNA, except for the composition of doxorubicin with folic acid with a linker length of 2000 (NPh-Dox-Fol(2.0)). The results of the electroanalysis were normalized to the total cell protein (mg) and cell concentration. The highest intensity of the electrochemical signals was observed in intact control cells of the MCF-7 and MDA-MB-231 cell lines. Conclusions: The proposed electrochemical approach is useful for the analysis of cell line responses to the medicinal preparations. Full article
(This article belongs to the Special Issue Nanomedicines in Cancer Therapy)
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