{"title":"魔芋通过调节PI3K/AKT细胞信号通路抑制雌激素受体+ (ER+)乳腺癌进展的药理作用","authors":"Hailong Li, Qinghong Yu, Jiaqing Song, Haining Ding, Yian Chen, Ying Jin, Hongting Wu, Liaqat Hussain, Xiufei Gao","doi":"10.2174/0115680096360994250106082347","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>Breast Cancer (BC) is one of the most prevalent malignant tumors in women. The incidence of estrogen receptor-positive (ER+) breast cancer is as high as 70%, and it is increasing. Amorphophalli rhizoma (APR) has the potential to be used in breast cancer.</p><p><strong>Aims: </strong>The objectives of the present study were to explore the impact of different APR extracts on the proliferation, migration, and invasion of ER+BC and to investigate their possible mechanism at the molecular level.</p><p><strong>Methods: </strong>Various extracts of APR were prepared in different solvents, such as petroleum ether, ethyl acetate, n-butanol, and water. ER+ T47D breast cancer cell lines were acquired and uti-lized to assess the effect of APR extracts on ER+ BC. Cell viability was assessed using the cell counting kit8 (CCk8) method, while anti-invasive and migratory effects were examined by transwell and wound healing assay. All the extracts were initially screened, and the ethyl acetate fraction (APR-EA) was found to be the most effective. Ultra High-Performance Liquid Chro-matography (UHPLC) of APR-EAE extract revealed the presence of various phytochemicals, such as succinic acid, 2-methoxy resorcinol, penicillic acid, morphine, salicylic acid, α-linolenic acid, and linolenic acid. Flow cytometry, western blot, and immunohistochemistry were used to explore molecular mechanisms.</p><p><strong>Results: </strong>APR-EA demonstrated anti-proliferative, anti-migratory, and anti-invasive effects on the ER+ T47D cell line. Thus, APR-EAE might inhibit the expression of P-PI3K/PI3K and P-Akt/Akt proteins, which subsequently represses the expression of ERα. This inhibition affects the downstream expression of the proteins CDK4 and Bcl-2, which are linked to cell growth and apoptosis.</p><p><strong>Conclusion: </strong>Additionally, APR-EA might increase the expression of P21 and Bax proteins, which are associated with cell cycle arrest and apoptosis. Overall, these effects contribute to the anti-ER+ breast cancer properties of APR-EA.</p>","PeriodicalId":10816,"journal":{"name":"Current cancer drug targets","volume":" ","pages":""},"PeriodicalIF":2.3000,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Pharmacological Evaluation of Amorphophalli rhizoma to Inhibit the Progression of Estrogen Receptor+ (ER+) Breast Cancer by Modulating the PI3K/AKT Cell Signaling Pathway.\",\"authors\":\"Hailong Li, Qinghong Yu, Jiaqing Song, Haining Ding, Yian Chen, Ying Jin, Hongting Wu, Liaqat Hussain, Xiufei Gao\",\"doi\":\"10.2174/0115680096360994250106082347\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>Breast Cancer (BC) is one of the most prevalent malignant tumors in women. The incidence of estrogen receptor-positive (ER+) breast cancer is as high as 70%, and it is increasing. Amorphophalli rhizoma (APR) has the potential to be used in breast cancer.</p><p><strong>Aims: </strong>The objectives of the present study were to explore the impact of different APR extracts on the proliferation, migration, and invasion of ER+BC and to investigate their possible mechanism at the molecular level.</p><p><strong>Methods: </strong>Various extracts of APR were prepared in different solvents, such as petroleum ether, ethyl acetate, n-butanol, and water. ER+ T47D breast cancer cell lines were acquired and uti-lized to assess the effect of APR extracts on ER+ BC. Cell viability was assessed using the cell counting kit8 (CCk8) method, while anti-invasive and migratory effects were examined by transwell and wound healing assay. All the extracts were initially screened, and the ethyl acetate fraction (APR-EA) was found to be the most effective. Ultra High-Performance Liquid Chro-matography (UHPLC) of APR-EAE extract revealed the presence of various phytochemicals, such as succinic acid, 2-methoxy resorcinol, penicillic acid, morphine, salicylic acid, α-linolenic acid, and linolenic acid. Flow cytometry, western blot, and immunohistochemistry were used to explore molecular mechanisms.</p><p><strong>Results: </strong>APR-EA demonstrated anti-proliferative, anti-migratory, and anti-invasive effects on the ER+ T47D cell line. Thus, APR-EAE might inhibit the expression of P-PI3K/PI3K and P-Akt/Akt proteins, which subsequently represses the expression of ERα. This inhibition affects the downstream expression of the proteins CDK4 and Bcl-2, which are linked to cell growth and apoptosis.</p><p><strong>Conclusion: </strong>Additionally, APR-EA might increase the expression of P21 and Bax proteins, which are associated with cell cycle arrest and apoptosis. Overall, these effects contribute to the anti-ER+ breast cancer properties of APR-EA.</p>\",\"PeriodicalId\":10816,\"journal\":{\"name\":\"Current cancer drug targets\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":2.3000,\"publicationDate\":\"2025-03-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current cancer drug targets\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/0115680096360994250106082347\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"ONCOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current cancer drug targets","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115680096360994250106082347","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"ONCOLOGY","Score":null,"Total":0}
Pharmacological Evaluation of Amorphophalli rhizoma to Inhibit the Progression of Estrogen Receptor+ (ER+) Breast Cancer by Modulating the PI3K/AKT Cell Signaling Pathway.
Introduction: Breast Cancer (BC) is one of the most prevalent malignant tumors in women. The incidence of estrogen receptor-positive (ER+) breast cancer is as high as 70%, and it is increasing. Amorphophalli rhizoma (APR) has the potential to be used in breast cancer.
Aims: The objectives of the present study were to explore the impact of different APR extracts on the proliferation, migration, and invasion of ER+BC and to investigate their possible mechanism at the molecular level.
Methods: Various extracts of APR were prepared in different solvents, such as petroleum ether, ethyl acetate, n-butanol, and water. ER+ T47D breast cancer cell lines were acquired and uti-lized to assess the effect of APR extracts on ER+ BC. Cell viability was assessed using the cell counting kit8 (CCk8) method, while anti-invasive and migratory effects were examined by transwell and wound healing assay. All the extracts were initially screened, and the ethyl acetate fraction (APR-EA) was found to be the most effective. Ultra High-Performance Liquid Chro-matography (UHPLC) of APR-EAE extract revealed the presence of various phytochemicals, such as succinic acid, 2-methoxy resorcinol, penicillic acid, morphine, salicylic acid, α-linolenic acid, and linolenic acid. Flow cytometry, western blot, and immunohistochemistry were used to explore molecular mechanisms.
Results: APR-EA demonstrated anti-proliferative, anti-migratory, and anti-invasive effects on the ER+ T47D cell line. Thus, APR-EAE might inhibit the expression of P-PI3K/PI3K and P-Akt/Akt proteins, which subsequently represses the expression of ERα. This inhibition affects the downstream expression of the proteins CDK4 and Bcl-2, which are linked to cell growth and apoptosis.
Conclusion: Additionally, APR-EA might increase the expression of P21 and Bax proteins, which are associated with cell cycle arrest and apoptosis. Overall, these effects contribute to the anti-ER+ breast cancer properties of APR-EA.
期刊介绍：
Current Cancer Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular drug targets involved in cancer, e.g. disease specific proteins, receptors, enzymes and genes.
Current Cancer Drug Targets publishes original research articles, letters, reviews / mini-reviews, drug clinical trial studies and guest edited thematic issues written by leaders in the field covering a range of current topics on drug targets involved in cancer.
As the discovery, identification, characterization and validation of novel human drug targets for anti-cancer drug discovery continues to grow; this journal has become essential reading for all pharmaceutical scientists involved in drug discovery and development.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
