Anti-cancer agents in medicinal chemistry最新文献

{"title":"Screening and <i>in vitro</i> Biological Evaluation of Novel Multiple Tyrosine Kinases Inhibitors as Promising Anticancer Agents.","authors":"Xiuying Li, Pinglang Ruan, Gang Jiang, Weidong Zhang","doi":"10.2174/1871520623666230403104816","DOIUrl":"10.2174/1871520623666230403104816","url":null,"abstract":"<p><strong>Background: </strong>Tyrosine kinases have emerged as key stimulatory drivers in several cancer-related pathways. This is particularly evident in non-small cell lung cancer with regulating cell growth and apoptosis and so on. Tyrosine kinase inhibitors (TKI) are one breakthrough option that could improve the life quality of cancer patients.</p><p><strong>Objective: </strong>This study aims to find more effective tyrosine kinase inhibitors.</p><p><strong>Methods: </strong>In this study, natural products from TargetMol that may be the potential TKI for lung cancer were screened through structure-based virtual screening and experimental validation. Moreover, the binding between the hit compounds and tyrosine kinase was explored.</p><p><strong>Results: </strong>From the study findings, Gramicidin and Tannic acid have strong interactions with the four tyrosine kinases (ALK, TRK, MET, and ABL), and this could significantly inhibit the viability of A549 cells in a concentrationdependent manner.</p><p><strong>Conclusion: </strong>These findings indicated that Gramicidin and Tannic acid might be potential multiple TKI and are promising anticancer agents that call for further study.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"555-562"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9254173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Updated Review on Dysregulated lncRNAs and their Contribution to the Various Molecular Types of Lung Carcinoma.","authors":"Narges Dastmalchi, Mohammad Reza Alipour, Reza Safaralizadeh, Khalil Hajiasgharzadeh","doi":"10.2174/0118715206336608241104065557","DOIUrl":"10.2174/0118715206336608241104065557","url":null,"abstract":"<p><p>Lung cancer is correlated with a high death rate, with approximately 1.8 million mortality cases reported worldwide in 2022. Despite development in the control of lung cancer, most cases are detected at higher stages with short survival rates. This reveals a need to recognize novel techniques to treat malignancy and decrease the burden of lung cancer. Long noncoding RNAs (lncRNAs) manage vital cellular and biochemical functions. lncRNAs play crucial roles in transcriptional and translational processes and signaling cascades. Recently, lncRNAs have been reported to be associated with malignancy where their expression is deregulated, leading to abnormal cellular activities and signaling pathways. In various malignancies, including lung cancer, lncRNA deregulation disrupts normal cellular function, promoting tumorigenesis and influencing patient outcomes and treatment responses. Studies have shown that lncRNAs can act as both oncogenes and tumor suppressors, depending on the lung cancer subtype, specifically in Non-small Cell Lung Cancer (NSCLC) and Small Cell Lung Cancer (SCLC). This dual role of lncRNAs as critical biomarkers might provide insights into lung cancer development and progression. lncRNAs have been discussed as key biomarkers in lung cancer. A comprehensive understanding of the biological activities of lncRNAs in NSCLC and SCLC may improve prognosis, diagnosis, and therapeutic methods. Researchers are increasingly interested in lncRNAs as potential diagnostic biomarkers and therapeutic targets in cancer treatment. As researchers continue to explore lncRNAs, their pivotal roles in lung cancer become increasingly evident. This review highlights the function of lncRNAs in lung carcinogenesis and discusses their molecular mechanisms of function.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"490-498"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142926263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pioneering a New Era in Oral Cancer Treatment with Electrospun Nanofibers: A Comprehensive Insight.","authors":"Devika Tripathi, Tanya Gupta, Awani Kumar Rai, Prashant Pandey","doi":"10.2174/0118715206348821241119100134","DOIUrl":"10.2174/0118715206348821241119100134","url":null,"abstract":"<p><p>Oral cancer, currently ranked 16th among the most prevalent malignancies worldwide according to GLOBOCAN, presents significant challenges to global oral health. Conventional treatment modalities such as surgery, radiation, and chemotherapy often have limitations, prompting the need for innovative therapeutic approaches. Tissue engineering has emerged as a promising solution aimed at developing biocompatible, functional, and biologically responsive tissue constructs. This approach involves the integration of cells, bioactive compounds, and scaffolds to enhance treatment efficacy. Electrospun nanofibers, mimicking the extracellular matrix, exhibit considerable potential in addressing complex oral health issues by influencing cellular behavior. The versatility of electrospinning technology allows for the fabrication of fiber scaffolds with high surface area, making them ideal for localized delivery of bioactive compounds or pharmaceuticals. Enhancing these electrospun scaffolds with growth factors, nanoparticles, and biologically active substances significantly increases their therapeutic appeal in oral cancer management. This review offers a comprehensive examination of the various applications of electrospun nanofibers in oral cancer therapy. Utilizing electronic databases such as PubMed, CrossREF, and Google Scholar, we conducted an extensive review of relevant literature concerning \"electrospun nanofibers\" and their therapeutic potential in oral cancer treatment. Key topics addressed include engineering methodologies, drug diffusion mechanisms, factors influencing nanofiber scaffold design, toxicity concerns, and clinical implications. The findings underscore the transformative potential of electrospun nanofibers in revolutionizing oral cancer therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"468-489"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142942920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioactive Products Targeting C-Met As Potential Antitumour Drugs.","authors":"Liying Zhao, Chunmei Qian, Xiaoqi Ma, Xiaoyu Wang","doi":"10.2174/0118715206346207241217064022","DOIUrl":"10.2174/0118715206346207241217064022","url":null,"abstract":"<p><p>Mesenchymal‒epithelial transition factor (c-Met), a receptortyrosine kinase (RTK), plays a vital role in cell proliferation, migration and invasion, and tumour metastasis.</p><p><strong>Objective: </strong>With increasing duration of treatment, many tumours gradually develop drug resistance. Therefore, novel antitumour drugs need to be developed to treat patients with tumours. Targeting c-met inhibitors may be an effective treatment strategy.</p><p><strong>Methods: </strong>Scientific databases such as ScienceDirect, PubMed, the Wiley Online Library, and Social Sciences Citation Index were used to collect information. All the relevant literature was reviewed, and the available literature was screened. The upstream and downstream pathways of c-Met and their relevance to antitumour effects were searched based on the articles' title, abstract, and full text. The c-Met-targeting drugs with antitumour effects are summarized below. A \"citation within a citation\" or snowballing approach was used in this screening process to identify additional papers that may have been missed in the initial literature screening process. High-quality studies published in peer-reviewed journals were summarized and prioritized for citation in the review.</p><p><strong>Results: </strong>In recent years, research on small-molecule targeted drugs has developed rapidly. Many results have also been achieved in the synthesis and isolation of c-Met inhibitors from natural compounds and traditional Chinese medicines.</p><p><strong>Conclusion: </strong>This article summarizes the developments in anti-c-Met drugs, which are synthesized and isolated from natural compounds and traditional Chinese medicine (TCM). This study provides primary resources for the development of c-Met inhibitors.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"688-696"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synergistic Anti-tumorigenic Effects of Cabazitaxel and Usnic Acid Combination on Metastatic Castration-Resistant Prostate Cancer Cells.","authors":"Ceyda Colakoglu Bergel, Isil Ezgi Eryilmaz, Ebrucan Bulut, Rumeysa Fatma Balaban, Unal Egeli, Gulsah Cecener","doi":"10.2174/0118715206336754241015062614","DOIUrl":"10.2174/0118715206336754241015062614","url":null,"abstract":"<p><strong>Background: </strong>Prostate cancer (PC) affects millions of men, causing high mortality rates. Despite the treatment approaches, the options for metastatic castration-resistant prostate cancer (mCRPC), a lethal form of advanced PC, are still limited. Cabazitaxel (Cbx) is the last taxane-derived chemotherapeutic approved for Docetaxel- resistant mCRPC patients. However, its effects are limited due to the activation of several pathways. Therefore, new approaches are needed to increase the efficacy of Cbx. Usnic acid (UA) is a natural product with wellknown anti-tumorigenic and synergistic effects with various chemotherapeutics. Although the cytotoxicity of UA and Cbx has been evaluated on mCRPC cells, the anti-tumorigenic effect of UA combination with any taxane has not been investigated yet. Thus, we aimed to evaluate the possible synergistic effect of Cbx+UA in mCRPC cells.</p><p><strong>Methods: </strong>Cell viability and apoptosis were analyzed using WST-1 and Annexin-V. Morphological changes were visualized by fluorescent staining. Finally, cell cycle, mitochondrial health, and ROS levels were determined.</p><p><strong>Results: </strong>Based on WST-1 results, 25 μM UA exhibited significant additive and synergistic effects with the use of Cbx. Annexin V and cell cycle results showed that UA significantly enhanced the Cbx efficacy at increasing doses compared to using only Cbx (**p<0.01). Moreover, combined treatment significantly increased ROS levels and mitochondrial membrane depolarization compared with Cbx alone (**p<0.01).</p><p><strong>Conclusions: </strong>Thus, the results suggest that UA increased the anti-tumorigenic effects of Cbx on mCRPC cells by increasing apoptosis, causing an increase in intracellular ROS and disrupting mitochondrial health. Consequently, combining UA and Cbx offers a new combined therapeutic strategy for mCRPC treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"610-619"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Evaluation of 5-oxo-1,2,4-triazole-3-carboxamide Compounds as Promising Anticancer Agents: Synthesis, Characterization, <i>In vitro</i> Cytotoxicity and Molecular Docking Studies.","authors":"Rajitha Balavanthapu, Girija Sastry Vedula","doi":"10.2174/0118715206315373241014101856","DOIUrl":"10.2174/0118715206315373241014101856","url":null,"abstract":"<p><strong>Background: </strong>Cancer presents a significant global health challenge, necessitating effective treatment strategies. While chemotherapy is widely employed, its non-specific nature can induce adverse effects on normal cells, prompting the exploration of targeted therapies. The 1,2,4-triazole scaffold has emerged as a promising element in anticancer drug development due to its structural diversity and potential to target cancer cells.</p><p><strong>Objective: </strong>This study aims to synthesize and evaluate novel derivatives derived from the 1,2,4-triazole scaffold for their potential as anticancer agents. Molecular docking techniques are employed to investigate the interactions between the designed derivatives and specific cancer-related targets, providing insights into potential underlying mechanisms.</p><p><strong>Methods: </strong>The synthesis involves a three-step process to produce 5-oxo-1,2,4-triazole-3-carboxamide derivatives. Various analytical techniques, including NMR and HRMS, validate the successful synthesis. Molecular docking studies utilize X-ray crystal structures of EGFR and CDK-4 obtained from the Protein Data Bank, employing the Schrödinger suite for ligand preparation and Glide's extra-precision docking modes for scoring.</p><p><strong>Results: </strong>The synthesis yields compounds with moderate to good yields, supported by detailed characterization. Molecular docking scores for the derivatives against EGFR and CDK-4 revealed diverse affinities influenced by distinct substituents. Compounds with hydroxyl, and halogen, substitutions exhibited notable binding affinities, while alkyl and amino substitutions showed varying effects. The 1,2,4-triazole derivatives demonstrated potential for targeted cancer therapy.</p><p><strong>Conclusion: </strong>The study highlights the successful synthesis of 5-oxo-1,2,4-triazole-3-carboxamides and their diverse interactions with cancer-related targets. The findings emphasized the potential of these derivatives as candidates for further development as anticancer agents, offering insights into structure-activity relationships. The 1,2,4-triazole scaffold stands out as a promising platform for advancing cancer treatment with enhanced precision and efficacy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"765-773"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142942894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Unveiling the Potential of S4 on Non-small Cell Lung Cancer Cells: Impact on Proliferation, Apoptosis, Senescence, and Metabolome Profile.","authors":"Turan Demircan, Mervenur Yavuz, Aydın Boluk","doi":"10.2174/0118715206350735241224073200","DOIUrl":"10.2174/0118715206350735241224073200","url":null,"abstract":"<p><strong>Background: </strong>Lung cancer is a highly aggressive tumor with limited therapeutic options. The misregulation of Androgen Receptor (AR) signaling has been observed in lung cancer. Therefore, inhibiting AR signaling is a promising strategy for treating lung cancer.</p><p><strong>Objective: </strong>Selective Androgen Receptor Modulators (SARMs) are small molecule drugs with a high affinity for the AR. S4, a member of SARMs was potentially positioned as a promising therapeutic agent in A549 lung cancer cells owing to its high bioavailability, lesser side effects, and novelty in cancer.</p><p><strong>Methods: </strong>We employed several techniques to investigate the potential anti-carcinogenic effect of S4 on A549 cells at cellular level. The cytotoxicity of S4 was investigated thorough MTT, and the IC₅₀ value was identified as 0.22 mM. Then, the anchorage-dependent and -independent colonization of cells were assessed by colony formation and soft agar assays, respectively. Additionally, migration capacity, apoptosis, proliferation, senescene, cell-cycle progression of cells was examined thoroughly. In addition, gene expression profile and metabolome signature were explored via qRT-PCR and metabolomics, respectively to provide molecular links for S4 mode of action.</p><p><strong>Results: </strong>Our findings demonstrate that S4 inhibited growth, migration, and proliferation while inducing apoptosis. S4 significantly upregulated the <i>BAX, CDKN1A, PUMA,</i> and <i>GADD45A</i> genes while downregulating <i>MKI67, BIRC5,</i> and <i>PCNA</i> expression. S4 treatment drastically altered the metabolome signature, and enrichment of cancer related pathways by altered metabolites was noteworthy.</p><p><strong>Conclusion: </strong>We report the first study evaluating the potential anti-carcinogenic effects of S4 on lung cancer invitro which would bridge the gap on the utility of SARMs as inhibitors of lung cancer. Our results suggest that S4 could be considered as a promising drug candidate to test further for lung cancer treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"785-799"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143021761","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, Synthesis, and Molecular Docking Studies of Indolo[3,2-c]Quinolines as Topoisomerase Inhibitors.","authors":"Mohamed Badr, Elshaymaa I Elmongy, Ibrahim El Tantawy El Sayed, Yasmine S Moemen, Ashraf Khalil, Doaa Elkhateeb, Reem Binsuwaidan, Hadeer Ali","doi":"10.2174/0118715206360700241219065917","DOIUrl":"10.2174/0118715206360700241219065917","url":null,"abstract":"<p><strong>Background: </strong>The tetracyclic indoloquinoline ring system has attracted considerable interest in the recent past due to its broad spectrum of biological activities and its binding to various types of nucleic acids.</p><p><strong>Objective: </strong>This study aims to elucidate their interactions with DNA and their effects on topoisomerases (TOPO) I and II.</p><p><strong>Methods: </strong>Several compounds derived from 6-amino-11H-indolo[3,2-c]quinoline with diverse groups on the quinoline ring have been successfully synthesized according to a previously established protocol where all the synthesized indolo[3,2-c]quinoline derivatives were evaluated <i>in vitro</i> against A549, HCT-116, BALB/3T3, and MV4-11 cell lines using MTT (3-[4,5- dimethylthiazol-2-yl]-2,5-diphenyl- tetrazolium bromide) assay. These derivatives were then screened for their topo I and II inhibitory activities.</p><p><strong>Results: </strong>The tested compounds were more effective at killing MV4-11 leukemia cells than the standard cancer drug cisplatin, as shown by the fact that their IC₅₀ values were less than 0.9 μM. On the other hand, cisplatin revealed an IC₅₀ value of 2.36 μM. Moreover, they exhibited inhibitory activity against both Topoisomerase (Topo) I and II. The most potent compound, 5g, demonstrated a suppressive impact on topoisomerase I, with an IC₅₀ value of 2.9 μM compared to the positive control Camptothecin (IC₅₀ 1.64 μM) and compound 8 displayed remarkable topoisomerase II inhibitory activity with an IC₅₀ of 6.82 μM compared to the positive control Doxorubicin (IC₅₀ 6.49 μM). The cell cycle study for compounds 5g and 8 revealed that cell cycle arrest occurred at the G1/S and S phases, respectively. Compounds 5g and 8 showed a high selectivity index, which suggests that they could be used to develop low-toxicity chemotherapeutic agents.</p><p><strong>Conclusion: </strong>The results of this study demonstrate that compounds 5g and 8 can be considered promising candidates for further anti-cancer drug development, which might be related to inhibiting TOPO I and TOPO II activities.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"1029-1040"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143121983","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Utilizing Indigenous Flora in East Africa for Breast Cancer Treatment: An Overview.","authors":"Esther Ugo Alum, Tabussam Tufail, Daniel Ejim Uti, Patrick Maduabuchi Aja, Christian Emeka Offor, Udu Ama Ibiam, Chris U A Ukaidi, Benedict Nnachi Alum","doi":"10.2174/0118715206338557240909081833","DOIUrl":"10.2174/0118715206338557240909081833","url":null,"abstract":"<p><strong>Background: </strong>Breast cancer is a significant global health challenge, contributing substantially to cancer- related deaths. Conventional treatment methods, including hormone therapy, chemotherapy, surgical interventions, and radiation, have long been utilized. However, these traditional treatments are often associated with serious side effects and drug resistance, limiting their efficacy.</p><p><strong>Aim: </strong>This review aims to explore the potential of medicinal plants used in breast cancer management in East Africa, focusing on their bioactive compounds and anticancer properties.</p><p><strong>Methods: </strong>A comprehensive literature search was conducted to examine the effectiveness of medicinal plants in treating breast cancer across Kenya, Ethiopia, Uganda, Tanzania, and Rwanda. Relevant studies published between 2003 and 2023 were identified using keywords related to breast cancer and medicinal plants. The search was performed across multiple databases, including Google Scholar, PubMed, Scopus, Web of Science Core Collection, and Science Direct.</p><p><strong>Results: </strong>Numerous natural compounds found in East African medicinal plants including <i>Cymbopogon citratus (Lemongrass,)</i> Tabebuia avellanedae, <i>Prunus africana</i> (African Cherry), <i>Euclea divinorum, Berberis holstii, Withania somnifera</i> (Ashwagandha, <i>Curcuma longa</i> (Turmeric), <i>Garcinia mangostana</i> (Mangosteen, <i>Vitis vinifera</i> (Grapevine), <i>Eugenia jambolana</i> (Java Plum), <i>Moringa oleifera</i> (Drumstick Tree), <i>Camellia sinensis</i> (Tea), <i>Glycine max</i> (Soybean), <i>Catharanthus roseus</i>, Madagascar Periwinkle), <i>Rhus vulgaris</i> (Wild Currant) exhibit significant anticancer properties. These compounds have demonstrated the ability to reduce breast cancer aggressiveness, inhibit cancer cell proliferation, and modulate cancer-related pathways. Current research focuses on these natural and dietary compounds to develop more effective strategies for treating breast cancer.</p><p><strong>Conclusion: </strong>The findings suggested that East African medicinal plants hold promise as complementary treatments for breast cancer, offering potential benefits such as affordability, cultural appropriateness, and sustainability. Further research into these plants and their bioactive compounds could revolutionize breast cancer treatment, improving survival rates and addressing the rising incidence of breast cancer-related fatalities. Other: The review underscores the importance of continued research, conservation, and the integration of ancient healing methods to fully harness the potential of East African flora in breast cancer management.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"99-113"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142279369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Doramectin Induces Apoptosis in B16 Melanoma Cells.","authors":"Megan S Crotts, Jena C Jacobs, Robert W Baer, James L Cox","doi":"10.2174/0118715206325844240909144543","DOIUrl":"10.2174/0118715206325844240909144543","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Metastatic melanoma resists current pharmacological regimens that act through apoptosis. This indicates that therapies acting via non-apoptotic cell-death pathways could be pursued. Doramectin has shown promising results in another cancer of neural crest origin, neuroblastoma, through the inhibition of growth via autophagy. Our research hypothesis is that doramectin induces autophagy in B16F10 melanoma cells.</p><p><strong>Methods: </strong>Cells were treated with doramectin (15 uM) or a combination of both doramectin and a cell-death inhibitor, compared to untreated control cells (media), and then analyzed with MTT analysis. Likewise, MDC analysis was completed to detect autophagy involvement with doramectin treatment. Flow cytometry and TUNEL Assay were conducted to observe cell death-related effects.</p><p><strong>Results: </strong>MTT analysis of doramectin-treated cells displayed a decrease in cell growth compared to control. Apoptotic morphology was prominent in melanoma cells treated with doramectin. Increased autophagy was not detected by fluorometric microscopic analysis. Flow cytometry analysis of doramectin-treated cells showed apoptosis as a major mode of cell death with some necrosis.</p><p><strong>Conclusion: </strong>Doramectin induces a novel cell-death mechanism in melanoma compared to other forms of cancer and should be studied as an effective anti-cancer agent for melanoma treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"244-256"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142456331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}