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Erratum to "Suppression of Lipopolysaccharide-induced Inflammatory and Oxidative Response by 5-Aminolevulinic Acid in RAW 264.7 Macrophages and Zebrafish Larvae" [Biomol Ther 29(6), 685-696 (2021)]. “5-氨基乙酰丙酸对巨噬细胞和斑马鱼幼体炎症和氧化反应的抑制作用”[j].生物医学工程学报,29(6),685-696(2021)。
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-05-01 DOI: 10.4062/biomolther.2025.002
Seon Yeong Ji, Hee-Jae Cha, Ilandarage Menu Neelaka Molagoda, Min Yeong Kim, So Young Kim, Hyun Hwangbo, Hyesook Lee, Gi-Young Kim, Do-Hyung Kim, Jin Won Hyun, Heui-Soo Kim, Suhkmann Kim, Cheng-Yun Jin, Yung Hyun Choi
{"title":"Erratum to \"Suppression of Lipopolysaccharide-induced Inflammatory and Oxidative Response by 5-Aminolevulinic Acid in RAW 264.7 Macrophages and Zebrafish Larvae\" [Biomol Ther 29(6), 685-696 (2021)].","authors":"Seon Yeong Ji, Hee-Jae Cha, Ilandarage Menu Neelaka Molagoda, Min Yeong Kim, So Young Kim, Hyun Hwangbo, Hyesook Lee, Gi-Young Kim, Do-Hyung Kim, Jin Won Hyun, Heui-Soo Kim, Suhkmann Kim, Cheng-Yun Jin, Yung Hyun Choi","doi":"10.4062/biomolther.2025.002","DOIUrl":"https://doi.org/10.4062/biomolther.2025.002","url":null,"abstract":"","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":"33 3","pages":"554"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12059357/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143972894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anti-Inflammatory Activity of Cell-Penetrating Peptide Nucleic Acids Targeting Indoleamine 2,3-Dioxygenase 1 in IFNγ-Treated Human Keratinocytes. 靶向吲哚胺2,3-双加氧酶1的细胞穿透肽核酸在ifn γ-处理的人角质形成细胞中的抗炎活性
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-05-01 Epub Date: 2025-04-30 DOI: 10.4062/biomolther.2024.207
Daram Jung, Sungjin Ahn, In Guk Park, Yeasel Jeon, Sangbong Lee, Minsoo Noh
{"title":"Anti-Inflammatory Activity of Cell-Penetrating Peptide Nucleic Acids Targeting Indoleamine 2,3-Dioxygenase 1 in IFNγ-Treated Human Keratinocytes.","authors":"Daram Jung, Sungjin Ahn, In Guk Park, Yeasel Jeon, Sangbong Lee, Minsoo Noh","doi":"10.4062/biomolther.2024.207","DOIUrl":"https://doi.org/10.4062/biomolther.2024.207","url":null,"abstract":"<p><p>Indoleamine 2,3-dioxygenase 1 (IDO1) is an enzyme that plays a pivotal role in immune regulation by metabolizing tryptophan into kynurenine, leading to T cell suppression and promoting immune tolerance. However, persistent activation of IDO1 can lead to prolonged immune stimulation in inflammatory conditions such as skin diseases and chronic inflammation. In this study, we developed modified peptide nucleic acids (PNAs) conjugated with cationic lipid chains to target IDO1 pre-mRNA and evaluated their anti-inflammatory effects in human keratinocytes. The modified PNAs demonstrated enhanced solubility, robust binding affinity, and effective penetration into keratinocytes. Quantitative PCR results showed significant downregulation of IDO1 and pro-inflammatory cytokines such as IL-6, IL-8, and PTGS2 in interferon γ (IFNγ)-treated keratinocytes. These findings suggest that cell-penetrating PNAs targeting IDO1 hold potential as a therapeutic approach for inflammatory skin disorders and chronic inflammation.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":"33 3","pages":"494-500"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12059366/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971427","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cynaropicrin Induces Reactive Oxygen Species-Dependent Paraptosis-Like Cell Death in Human Liver Cancer Cells. 西那匹克林诱导人肝癌细胞中活性氧依赖性跃迁样细胞死亡
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-05-01 Epub Date: 2025-04-04 DOI: 10.4062/biomolther.2025.011
Min Yeong Kim, Hee-Jae Cha, Su Hyun Hong, Sung-Kwon Moon, Taeg Kyu Kwon, Young-Chae Chang, Gi Young Kim, Jin Won Hyun, A-Young Nam, Jung-Hyun Shim, Yung Hyun Choi
{"title":"Cynaropicrin Induces Reactive Oxygen Species-Dependent Paraptosis-Like Cell Death in Human Liver Cancer Cells.","authors":"Min Yeong Kim, Hee-Jae Cha, Su Hyun Hong, Sung-Kwon Moon, Taeg Kyu Kwon, Young-Chae Chang, Gi Young Kim, Jin Won Hyun, A-Young Nam, Jung-Hyun Shim, Yung Hyun Choi","doi":"10.4062/biomolther.2025.011","DOIUrl":"10.4062/biomolther.2025.011","url":null,"abstract":"<p><p>Cynaropicrin, a sesquiterpene lactone found in artichoke leaves exerts diverse pharmacological effects. This study investigated whether cynaropicrin has a paraptosis-like cell death effect in human hepatocellular carcinoma Hep3B cells in addition to the apoptotic effects reported in several cancer cell lines. Cynaropicrin-induced cytotoxicity and cytoplasmic vacuolation, a key characteristic of paraptosis, were not ameliorated by inhibitors of necroptosis, autophagy, or pan caspase inhibitors in Hep3B cells. Our study showed that cynaropicrin-induced cytotoxicity was accompanied by mitochondrial dysfunction and endoplasmic reticulum stress along with increased cellular calcium ion levels. These effects were significantly mitigated by endoplasmic reticulum stress inhibitor or protein synthesis inhibitor. Moreover, cynaropicrin treatment in Hep3B cells increased reactive oxygen species generation and downregulated apoptosis-linked gene 2-interacting protein X (Alix), a protein that inhibits paraptosis. The addition of the reactive oxygen species scavenger <i>N</i>-acetyl-L-cysteine (NAC) neutralized cynaropicrin-induced changes in Alix expression and endoplasmic reticulum stress marker proteins counteracting endoplasmic reticulum stress and mitochondrial impairment. This demonstrates a close relationship between endoplasmic reticulum stress and reactive oxygen species generation. Additionally, cynaropicrin activated p38 mitogen activated protein kinase and a selective p38 mitogen activated protein kinase blocker alleviated the biological phenomena induced by cynaropicrin. NAC pretreatment showed the best reversal of cynaropicrin induced vacuolation and cellular inactivity. Our findings suggest that cynaropicrin induced oxidative stress in Hep3B cells contributes to paraptotic events including endoplasmic reticulum stress and mitochondrial damage.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"470-482"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12059367/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143778894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dual Disruption of DNA Repair by a Novel CHK2 Inhibitor, ART-446, and Olaparib is a Promising Strategy for Triple-Negative Breast Cancer Therapy. 一种新的CHK2抑制剂ART-446和奥拉帕尼对DNA修复的双重破坏是三阴性乳腺癌治疗的一种有希望的策略。
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-05-01 Epub Date: 2025-04-08 DOI: 10.4062/biomolther.2025.029
Hong-Jun Kang, Young-Woo Kang, Ha-Young Lee, Sojung Ha, Jong Oh Kim, Woo-Young Kim, Taegon Baik
{"title":"Dual Disruption of DNA Repair by a Novel CHK2 Inhibitor, ART-446, and Olaparib is a Promising Strategy for Triple-Negative Breast Cancer Therapy.","authors":"Hong-Jun Kang, Young-Woo Kang, Ha-Young Lee, Sojung Ha, Jong Oh Kim, Woo-Young Kim, Taegon Baik","doi":"10.4062/biomolther.2025.029","DOIUrl":"10.4062/biomolther.2025.029","url":null,"abstract":"<p><p>Triple-negative breast cancer (TNBC) is an aggressive cancer subtype lacking targeted therapies and is characterized by high recurrence rates and poor prognosis. Recent advances in targeting DNA damage response (DDR) pathways using poly (ADP‒ribose) polymerase (PARP) inhibitors offer promising therapeutic strategies, especially for TNBC patients with BRCA1/2 mutations. This study reports the development and characterization of ART-446, a novel and selective CHK2 inhibitor. ART-446 showed potent activity against TNBC, regardless of BRCA deficiency, and it also reversed PARP inhibitor resistance. ART-446 potently inhibited CHK2 (IC<sub>50</sub>: 9.06 nM) with high selectivity over other kinases; it synergized with the PARP inhibitor olaparib, enhancing DNA damage, inducing G2/M cell cycle arrest, and promoting apoptosis in both BRCA-mutant and wild-type TNBC cells. Mechanistic analyses revealed that ART-446 sensitized BRCA mutant and WT cells to PARP inhibitors by impairing DNA repair and increasing the accumulation of DNA damage. Importantly, ART-446 disrupted both homologous recombination and nonhomologous end-joining repair pathways, addressing a key limitation of PARP inhibitor monotherapy-resistance in BRCA-proficient cancers. <i>In vivo</i>, the combination of ART-446 and olaparib significantly reduced tumor growth in TNBC xenograft models without noticeable toxicity. The combined treatment increased DNA damage signaling, as evidenced by elevated γH2AX levels, and enhanced the sensitivity of BRCA2-deficient cells to ART-446. These findings underscore the potential of ART-446 to exploit DNA repair deficiencies and overcome resistance mechanisms associated with PARP inhibitors. By addressing the limitations of current treatments and expanding the utility of PARP inhibitors, ART-446 represents a promising candidate for DDR-targeted therapies, offering a novel approach to improve the outcomes of patients with TNBC.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"458-469"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12059358/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143802282","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
1,3,5-Tricaffeoylquinic Acid from Ipomoea batatas Vines Induced Ovarian Cancer Cell Apoptosis and Inhibited Endothelial Tube Formation. 1,3,5-三咖啡酰奎宁酸诱导卵巢癌细胞凋亡及抑制内皮管形成
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-05-01 Epub Date: 2025-04-08 DOI: 10.4062/biomolther.2024.239
Dahae Lee, Jaekyoung Kim, Soyoon Baek, Jin Woo Lee, Changyeol Lee, Ki Sung Kang, Sang Hee Shim
{"title":"1,3,5-Tricaffeoylquinic Acid from <i>Ipomoea batatas</i> Vines Induced Ovarian Cancer Cell Apoptosis and Inhibited Endothelial Tube Formation.","authors":"Dahae Lee, Jaekyoung Kim, Soyoon Baek, Jin Woo Lee, Changyeol Lee, Ki Sung Kang, Sang Hee Shim","doi":"10.4062/biomolther.2024.239","DOIUrl":"10.4062/biomolther.2024.239","url":null,"abstract":"<p><p>Ovarian cancer usually metastasizes from the ovary to adjacent organs through direct invasion with blood vessels formed by endothelial cells. Targeting apoptosis of ovarian cancer and angiogenesis is promising for anticancer therapy. Leaves of <i>Ipomoea</i> sp. have reportedly shown promise in treating ovarian cancer. Here, we investigated the apoptosis-inducing and anti-angiogenic effects of compounds isolated from <i>Ipomoea batatas</i> vines (IBV). Phytochemical examination of IBV led to the isolation and verification of eight compounds (<b>1-8</b>): chlorogenic acid (<b>1</b>), 3,4-dicaffeoylquinic acid (<b>2</b>), 3,5-dicaffeoylquinic acid (<b>3</b>), 4,5-dicaffeoylquinic acid (<b>4</b>), 1,3,5-tricaffeoylquinic acid (<b>5</b>), <i>N-trans</i>-feruloyltyramine (<b>6</b>), scopoletin (<b>7</b>), and esculetin (<b>8</b>). Of these, 1,3,5-tricaffeoylquinic acid (5) showed the highest cytotoxicity in A2780 human ovarian cancer cells, inducing apoptotic death in more than 37% cells and decreasing viability to less than 25% at 100 μM. Compound <b>5</b> increased the levels of cleaved caspase-8, Bax, cleaved PARP, and caspase-3/9, and decreased the levels of cleaved Bcl-2. Further, <b>5</b> inhibited tubule formation in HUVECs. VEGFR2, ERK, PI3K, Akt, and mTOR protein expression was also suppressed by <b>5</b>. Then, a simple, rapid, and reliable LC-MS/ MS method was developed to determine the contents of the isolated compounds from IBV. Overall, <b>5</b> has potential for treating ovarian cancer as it induces apoptosis in ovarian cancer cells and inhibits tube formation.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"483-493"},"PeriodicalIF":3.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12059361/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143802280","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Artesunate Inhibits the Proliferation and Migration of Cutaneous Squamous Cell Carcinoma by Regulating the SLC7A11-GPX4 Pathway via the p300-p53 Axis. 青蒿琥酯通过p300-p53轴调控SLC7A11-GPX4通路抑制皮肤鳞状细胞癌的增殖和迁移
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-03-01 Epub Date: 2025-02-24 DOI: 10.4062/biomolther.2024.156
Xinyan Huang, Wenxi Wang, Songzhao Zhang, Lili Li, Jihui Huang
{"title":"Artesunate Inhibits the Proliferation and Migration of Cutaneous Squamous Cell Carcinoma by Regulating the SLC7A11-GPX4 Pathway via the p300-p53 Axis.","authors":"Xinyan Huang, Wenxi Wang, Songzhao Zhang, Lili Li, Jihui Huang","doi":"10.4062/biomolther.2024.156","DOIUrl":"10.4062/biomolther.2024.156","url":null,"abstract":"<p><p>The incidence of cutaneous squamous cell carcinoma (CSCC) is increasing rapidly. This study discussed the effects of artesunate (ART) on CSCC cell proliferation and migration via the solute carrier family 7 member 11 (SLC7A11)-glutathione peroxidase 4 (GPX4) pathway. MTT assessed cell viability and analyzed the IC<sub>50</sub> value (69.26 μM). Accordingly, human CSCC cells (A431) were cultured <i>in vitro</i>, and treated with 70 μM ART, Ferrostatin-1, oe-SLC7A11, and C646, with cell biological behavior assessed. The potential targets of ART were predicted. p53 acetylation and protein stability and ART-p300 binding were examined. Thymusless nude mice were subcutaneously inoculated with A431 cells, and treated with ART and C646. ART-treated A431 cells showed weakened proliferation, migration, lactate dehydrogenase levels, oxidized glutathione/glutathione ratio, reactive oxygen species, malondialdehyde, and active Fe<sup>2+</sup> levels, which could be reversed by suppressing ferroptosis. ART promoted p53 acetylation and protein stability and curbed the SLC7A11-GPX4 pathway by targeting p300. ART stimulated ferroptosis via the SLC7A11-GPX4 pathway, thereby repressing CSCC cell proliferation and migration, which were counteracted by p300 inhibition. ART regulated the SLC7A11-GPX4 pathway by up-regulating the p300-p53 axis, thereby hindering tumor growth <i>in vivo</i>. Collectively, ART inhibits CSCC proliferation and migration by modulating the SLC7A11-GPX4 pathway through the p300-p53 axis.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"365-377"},"PeriodicalIF":3.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11893488/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143482122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Resveratrol from Peanut Sprout Extract Promotes NK Cell Activation and Antitumor Activity. 花生芽提取物中的白藜芦醇促进NK细胞活化和抗肿瘤活性。
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-03-01 Epub Date: 2025-02-20 DOI: 10.4062/biomolther.2024.133
Hyunmin Chung, Seong Ho Bak, Eunju Shin, Taeho Park, Jinwoo Kim, Hanseul Jeong, Haiyoung Jung, Suk Ran Yoon, Ji-Yoon Noh
{"title":"Resveratrol from Peanut Sprout Extract Promotes NK Cell Activation and Antitumor Activity.","authors":"Hyunmin Chung, Seong Ho Bak, Eunju Shin, Taeho Park, Jinwoo Kim, Hanseul Jeong, Haiyoung Jung, Suk Ran Yoon, Ji-Yoon Noh","doi":"10.4062/biomolther.2024.133","DOIUrl":"10.4062/biomolther.2024.133","url":null,"abstract":"<p><p>Natural killer (NK) cells are innate immune cells that are crucial for anticancer activity and have been developed as an immune cell therapy for leukemia. However, their limited effectiveness against solid tumors has prompted research into methods to enhance NK cell activity through combination therapies. Health supplements capable of boosting immune surveillance against tumor cells are gaining attention owing to their potential benefits. Resveratrol, a stilbenoid produced by several plants including peanuts and grapes, reportedly exerts anticancer effects and can activate immune cells. The peanut sprout extract cultivated with fermented sawdust medium (PSEFS) is rich in resveratrol, leveraging its health benefits in terms of the dry weight of herbal products, thus maximizing the utilization of resveratrol's beneficial properties. Our study compared the efficacy of resveratrol and PSEFS and revealed that PSEFS significantly enhanced NK cell activation compared with an equivalent dose of resveratrol. We investigated the ability of PSEFS to potentiate NK cell anticancer activity, focusing on NK cell survival, tumor cell lysis, and NK cell activation in PSEFS-administered mice. Our findings suggest that PSEFS could be a potential NK cell booster for cancer immunotherapy.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"355-364"},"PeriodicalIF":3.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11893499/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143456616","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Piperine Regulates Melanogenesis through ERK Activation and Proteasomal Degradation of MITF. 胡椒碱通过ERK激活和蛋白酶体降解MITF调节黑色素生成
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-03-01 Epub Date: 2025-02-12 DOI: 10.4062/biomolther.2024.065
Jun Hyeong Lee, Jieun Lee, Sukanya Dej-Adisai, Jae Sung Hwang
{"title":"Piperine Regulates Melanogenesis through ERK Activation and Proteasomal Degradation of MITF.","authors":"Jun Hyeong Lee, Jieun Lee, Sukanya Dej-Adisai, Jae Sung Hwang","doi":"10.4062/biomolther.2024.065","DOIUrl":"10.4062/biomolther.2024.065","url":null,"abstract":"<p><p>Melanin is a bio-pigment molecule synthesized by melanocytes. Its role is to shield the skin from ultraviolet radiation. Nonetheless, aberrant melanin production, whether excessive or deficient, can lead to conditions such as vitiligo, freckles, melanocytic nevi, and even melanoma. The biosynthetic pathway of melanin is known as melanogenesis, which is regulated by various transcription factors and enzymatic processes. Piperine (PPN), an alkaloid compound extracted from Piper retrofractum Vahl., was investigated for its potential anti-fungal and anti-inflammatory effects. Our hypothesis centered on the inhibition of melanin biosynthesis in response to PPN treatment. Subsequently, it was observed that PPN treatment resulted in a dose-dependent reduction in melanin production, accompanied by a decrease in tyrosinase activity. Furthermore, PPN was found to downregulate the protein levels of key melanogenesis-related genes. Additionally, PPN was observed to elevate the phosphorylation levels of ERK. To assess the role of ERK signaling in PPN-induced melanogenesis regulation, PD98059, an ERK inhibitor, was used. When Melan-A cells were treated with PD98059, the reduced expression level of MITF and melanin content induced by piperine were restored. Additionally, phosphorylation of ERK increased the phosphorylation of MITF at Ser73. This phosphorylated MITF leads to ubiquitination, and ultimately, the protein level of MITF decreases through proteasomal degradation. Likewise, when Melan-A cells were treated with MG132, a proteasomal inhibitor, the reduced expression level of MITF and melanin content induced by piperine were restored. Consequently, PPN can be a potential candidate for application as a skin whitening agent or in formulations to mitigate hyperpigmentation.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"408-414"},"PeriodicalIF":3.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11893493/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143397995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Daurisoline Inhibits Progression of Triple-Negative Breast Cancer by Regulating the γ-Secretase/Notch Axis. Daurisoline通过调节γ-分泌酶/Notch轴抑制三阴性乳腺癌的进展。
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-03-01 Epub Date: 2025-02-12 DOI: 10.4062/biomolther.2024.131
Xiangyi Zhan, Xiaoyong Chen, Mei Feng, Kuo Yao, Kefan Yang, Hui Jia
{"title":"Daurisoline Inhibits Progression of Triple-Negative Breast Cancer by Regulating the γ-Secretase/Notch Axis.","authors":"Xiangyi Zhan, Xiaoyong Chen, Mei Feng, Kuo Yao, Kefan Yang, Hui Jia","doi":"10.4062/biomolther.2024.131","DOIUrl":"10.4062/biomolther.2024.131","url":null,"abstract":"<p><p>Triple-negative breast cancer (TNBC) is a subtype of breast cancer that is challenging to treat and lacks targeted therapeutic drugs in the clinic. Natural active ingredients provide promising opportunities for discovering and developing targeted therapies for TNBC. This study investigated the effects of daurisoline on TNBC and elucidated its potential mechanisms. Using network pharmacology, a correlation was identified between daurisoline, derived from <i>Menispermum dauricum</i>, and breast cancer, particularly involving the Notch signaling pathway. The effects of daurisoline on the proliferation, migration, and apoptosis of MDA-MB-231 and MDA-MB-468 cells were evaluated <i>in vitro</i>. Additionally, the impact of daurisoline on the growth of MDA-MB-231 xenograft tumors in nude mice was assessed through <i>in vivo</i> experiments. Expression levels of Notch signaling pathway-related proteins, including Notch-1, NICD, PSEN-1, Bax, and Bcl-2, were examined using molecular docking and Western blotting to explore the underlying mechanisms of daurisoline's anti-breast cancer effects. It was revealed that daurisoline could effectively inhibit the proliferation and migration of MDA-MB-231 and MDA-MB-468 cells and promote apoptosis. Furthermore, it significantly reduced the growth of subcutaneous tumors in nude mice. Notably, daurisoline could reduce the hydrolytic activity of γ-secretase by binding to the catalytic core PSEN-1, thereby inhibiting activation of the γ-secretase/Notch axis and contributing to its anti-TNBC effects. This study supported the development of naturally targeted drugs for TNBC and provided insights into the research on dibenzylisoquinoline alkaloids, such as daurisoline.</p>","PeriodicalId":8949,"journal":{"name":"Biomolecules & Therapeutics","volume":" ","pages":"331-343"},"PeriodicalIF":3.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11893495/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143397973","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Erratum to "Potential Role of Dietary Salmon Nasal Cartilage Proteoglycan on UVB-Induced Photoaged Skin" [Biomol Ther 32(2), 249-260 (2024)]. “膳食中三文鱼鼻软骨蛋白多糖对uvb诱导的光老化皮肤的潜在作用”[生物学报]32(2),249-260(2024)。
IF 3 3区 医学
Biomolecules & Therapeutics Pub Date : 2025-03-01 DOI: 10.4062/biomolther.2025.001
Hae Ran Lee, Seong-Min Hong, Kyohee Cho, Seon Hyeok Kim, Eunji Ko, Eunyoo Lee, Hyun Jin Kim, Se Yeong Jeon, Seon Gil Do, Sun Yeou Kim
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