Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie最新文献

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Corrigendum to "Lactobacillus rhamnosus GG coating with nanocomposite ameliorates intestinal inflammation" [Biomed. Pharmacother. 178 (2024) 117-197]. 鼠李糖乳杆菌 GG 涂覆纳米复合材料可改善肠道炎症》[Biomed. Pharmacother. 178 (2024) 117-197] 更正。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-10-01 Epub Date: 2024-09-10 DOI: 10.1016/j.biopha.2024.117434
Zihan Zhai, Xin Wang, Zhanyin Qian, Aili Wang, Wenjing Zhao, Jie Xiong, Jingyi Wang, Yinsong Wang, Hailong Cao
{"title":"Corrigendum to \"Lactobacillus rhamnosus GG coating with nanocomposite ameliorates intestinal inflammation\" [Biomed. Pharmacother. 178 (2024) 117-197].","authors":"Zihan Zhai, Xin Wang, Zhanyin Qian, Aili Wang, Wenjing Zhao, Jie Xiong, Jingyi Wang, Yinsong Wang, Hailong Cao","doi":"10.1016/j.biopha.2024.117434","DOIUrl":"10.1016/j.biopha.2024.117434","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117434"},"PeriodicalIF":0.0,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142303320","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Retraction notice to "Overexpression of macrophage stimulating 1 enhances the anti-tumor effects of IL-24 in esophageal cancer via inhibiting ERK-Mfn2 signaling-dependent mitophagy" [Biomed. Pharmacother. 114 (2019) 108844]. 关于 "Overexpression of macrophage stimulating 1 enhances the anti-tumor effects of IL-24 in esophageal cancer via inhibiting ERK-Mfn2 signaling-dependent mitophagy "的撤稿通知 [Biomed. Pharmacother. 114 (2019) 108844]。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-10-01 Epub Date: 2024-09-14 DOI: 10.1016/j.biopha.2024.117355
Jianpeng Zhang, Lin Sun, Weiqiang Li, Yanyu Wang, Xinzhen Li, Yang Liu
{"title":"Retraction notice to \"Overexpression of macrophage stimulating 1 enhances the anti-tumor effects of IL-24 in esophageal cancer via inhibiting ERK-Mfn2 signaling-dependent mitophagy\" [Biomed. Pharmacother. 114 (2019) 108844].","authors":"Jianpeng Zhang, Lin Sun, Weiqiang Li, Yanyu Wang, Xinzhen Li, Yang Liu","doi":"10.1016/j.biopha.2024.117355","DOIUrl":"10.1016/j.biopha.2024.117355","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117355"},"PeriodicalIF":0.0,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142303325","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Corrigendum to "3D printed PLGA scaffold with nano-hydroxyapatite carrying linezolid for treatment of infected bone defects" [Biomed. Pharmacother. 172 (2024) 116228]. 对 "含有纳米羟基磷灰石的三维打印 PLGA 支架用于治疗感染性骨缺损"[Biomed. Pharmacother.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-10-01 Epub Date: 2024-09-04 DOI: 10.1016/j.biopha.2024.117212
A Li Mu Ke Re Mu, Zhi Lin Liang, Linlin Chen, Ai Ke Bai Er Tu Xun, Mai Mai Ti Ai Li A Bu Li Ke Mu, Yuan Quan Wu
{"title":"Corrigendum to \"3D printed PLGA scaffold with nano-hydroxyapatite carrying linezolid for treatment of infected bone defects\" [Biomed. Pharmacother. 172 (2024) 116228].","authors":"A Li Mu Ke Re Mu, Zhi Lin Liang, Linlin Chen, Ai Ke Bai Er Tu Xun, Mai Mai Ti Ai Li A Bu Li Ke Mu, Yuan Quan Wu","doi":"10.1016/j.biopha.2024.117212","DOIUrl":"10.1016/j.biopha.2024.117212","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117212"},"PeriodicalIF":0.0,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142134759","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Astragalus polysaccharide enhances antitumoral effects of chimeric antigen receptor- engineered (CAR) T cells by increasing CD122+CXCR3+PD-1- memory T cells. 黄芪多糖通过增加 CD122+CXCR3+PD-1- 记忆 T 细胞,增强嵌合抗原受体工程(CAR)T 细胞的抗肿瘤效果。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-10-01 Epub Date: 2024-09-08 DOI: 10.1016/j.biopha.2024.117401
Qunfang Zhang, Chunzhao Su, Yini Luo, Fang Zheng, Chun-Ling Liang, Yuchao Chen, Huazhen Liu, Feifei Qiu, Yunshan Liu, Wenxuan Feng, Zhenhua Dai
{"title":"Astragalus polysaccharide enhances antitumoral effects of chimeric antigen receptor- engineered (CAR) T cells by increasing CD122<sup>+</sup>CXCR3<sup>+</sup>PD-1<sup>-</sup> memory T cells.","authors":"Qunfang Zhang, Chunzhao Su, Yini Luo, Fang Zheng, Chun-Ling Liang, Yuchao Chen, Huazhen Liu, Feifei Qiu, Yunshan Liu, Wenxuan Feng, Zhenhua Dai","doi":"10.1016/j.biopha.2024.117401","DOIUrl":"10.1016/j.biopha.2024.117401","url":null,"abstract":"<p><p>Chimeric antigen receptor-engineered T (CAR-T) cell therapy of cancer has been a hotspot and promising. However, due to rapid exhaustion, CAR-T cells are less effective in solid tumors than in hematological ones. CD122<sup>+</sup>CXCR3<sup>+</sup> memory T cells are characterized with longevity, self-renewal and great antitumoral capacity. Thus, it's compelling to induce memory CAR-T cells to enhance their efficacy on solid tumors. Astragalus polysaccharide (APS) has reportedly exhibited antitumoral effects. However, it's unclear if APS has an impact on CD8<sup>+</sup> memory T cell generation or persistence. Using two human cancer cell lines, here we found that APS significantly improved the persistence of GPC3-targeted CAR-T cells and enhanced their suppression of tumor growth in both Huh7 and HepG2 xenograft models of hepatocellular carcinoma. APS increased CD122<sup>+</sup>/CXCR3<sup>+</sup> memory T cells, but decreased their PD-1<sup>+</sup> subset within CD8<sup>+</sup> CAR-T cells in tumor-bearing mice, while these effects of APS were also confirmed with in vitro experiments. Moreover, APS augmented the expression of chemokines CXCL9/CXCL10 by the tumor in vivo and in vitro. It also enhanced the proliferation and chemotaxis/migration of CAR-T cells in vitro. Finally, APS promoted the phosphorylation of STAT5 in CD8<sup>+</sup> CAR-T cells, whereas inhibition of STAT5 activation reversed these in vitro effects of APS. Therefore, APS enhanced the antitumoral effects of CD8<sup>+</sup> CAR-T cells by promoting formation/persistence of CD122<sup>+</sup>/CXCR3<sup>+</sup>/PD-1<sup>-</sup> memory T cells and their migration to the tumor.</p>","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":"179 ","pages":"117401"},"PeriodicalIF":0.0,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142147087","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Retraction notice to "Hispidulin inhibits hepatocellular carcinoma growth and metastasis through AMPK and ERK signaling mediated activation of PPARγ" [Biomed. Pharmacother. 103 (2018) 272-283]. Hispidulin inhibits hepatocellular carcinoma growth and metastasis through AMPK and ERK signaling mediated activation of PPARγ" [Biomed. Pharmacother. 103 (2018) 272-283] 的撤稿通知。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-10-01 Epub Date: 2024-09-14 DOI: 10.1016/j.biopha.2024.117354
Mei Han, Hui Gao, Ping Ju, Ming-Quan Gao, Yin-Ping Yuan, Xue-Hong Chen, Kai-Li Liu, Yan-Tao Han, Zhi-Wu Han
{"title":"Retraction notice to \"Hispidulin inhibits hepatocellular carcinoma growth and metastasis through AMPK and ERK signaling mediated activation of PPARγ\" [Biomed. Pharmacother. 103 (2018) 272-283].","authors":"Mei Han, Hui Gao, Ping Ju, Ming-Quan Gao, Yin-Ping Yuan, Xue-Hong Chen, Kai-Li Liu, Yan-Tao Han, Zhi-Wu Han","doi":"10.1016/j.biopha.2024.117354","DOIUrl":"10.1016/j.biopha.2024.117354","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117354"},"PeriodicalIF":0.0,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142303324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Scent of relief: Mastic resin scent recovers salivation in chronic dry mouth patients. 缓解的香味松香树脂的香味能恢复慢性口干症患者的唾液分泌。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-09-01 Epub Date: 2024-08-06 DOI: 10.1016/j.biopha.2024.117245
Mouri R J Faruque, Wiktoria Potocka, Kamran Nazmi, Antoon J Ligtenberg, Floris J Bikker, Marja L Laine
{"title":"Scent of relief: Mastic resin scent recovers salivation in chronic dry mouth patients.","authors":"Mouri R J Faruque, Wiktoria Potocka, Kamran Nazmi, Antoon J Ligtenberg, Floris J Bikker, Marja L Laine","doi":"10.1016/j.biopha.2024.117245","DOIUrl":"10.1016/j.biopha.2024.117245","url":null,"abstract":"<p><strong>Background: </strong>Olfactory stimulation with mastic resin, derived from the Pistacia lentiscus tree, demonstrated a bona fide sialagogic effect in healthy volunteers [1]. Its main volatile compound, α-pinene, also showed this effect. The current study aimed to validate the effect of mastic resin volatiles in chronic dry mouth patients with confirmed decreased saliva secretion.</p><p><strong>Methods: </strong>41 chronic dry mouth patients with decreased unstimulated saliva secretion (<0.25 mL/min) were exposed to mastic resin volatiles as part of the diagnostic routine at the Saliva Clinic of Academic Centre for Dentistry Amsterdam. During their visit, dry-mouth questionnaires were conducted and samples of unstimulated whole saliva, chew-stimulated saliva, acid-stimulated saliva and mastic resin stimulated saliva were collected. Saliva flow rate, spinnbarkeit, pH, ion composition, MUC5B and MUC7 levels in all samples were analyzed.</p><p><strong>Results: </strong>Salivary flow rates increased by all stimuli when compared to the baseline unstimulated saliva (P<0.001). During olfactory mastic resin stimulation, the salivary spinnbarkeit (P<0.001) and sodium concentration (P<0.01) were increased compared to unstimulated saliva. MUC5B and MUC7 levels were increased during olfactory mastic resin stimulation compared to chew-stimulated saliva (P=0.016 and P<0.001, respectively). Spinnbarkeit correlated positively with MUC5B (R=0.399, P=0.002) and MUC7 levels (R=0.375, P=0.004). Results of dry-mouth questionnaires indicated reduced posterior palate dryness shortly after olfactory mastic resin stimulation (P=0.04).</p><p><strong>Conclusions: </strong>Olfactory mastic resin stimulation increased mucous saliva secretion and reduced posterior palate dryness in a group of chronic dry mouth patients. These findings, validated in patients, underscore mastic resin scent as a beneficial and non-invasive sialagogic treatment for clinical applications.</p>","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":"178 ","pages":"117245"},"PeriodicalIF":0.0,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141903956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
PTX-RPPR, a conjugate of paclitaxel and NRP-1 peptide inhibitor to prevent tumor growth and metastasis. PTX-RPPR,一种紫杉醇和 NRP-1 肽抑制剂的共轭物,用于防止肿瘤生长和转移。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-09-01 Epub Date: 2024-08-14 DOI: 10.1016/j.biopha.2024.117264
Yuanyuan Li, Qiqi Feng, Qi Gao, Yaonan Wang, Shurui Zhao, Xiaoyi Zhang, Ming Zhao
{"title":"PTX-RPPR, a conjugate of paclitaxel and NRP-1 peptide inhibitor to prevent tumor growth and metastasis.","authors":"Yuanyuan Li, Qiqi Feng, Qi Gao, Yaonan Wang, Shurui Zhao, Xiaoyi Zhang, Ming Zhao","doi":"10.1016/j.biopha.2024.117264","DOIUrl":"10.1016/j.biopha.2024.117264","url":null,"abstract":"<p><p>Paclitaxel, a potent anti-tumor drug widely recognized for its therapeutic efficacy, has faced limitations in clinical application due to its poor solubility. The use of Cremophor EL (CrEL) as a cosolvent in paclitaxel injections has been associated with hypersensitivity reactions in some patients. To overcome these challenges, we have developed a novel conjugate by linking a neuropilin-1 targeting peptide, RPPR, to paclitaxel, resulting in PTX-RPPR. This innovative approach has significantly enhanced the solubility of paclitaxel, achieving a 3.8 mg/mL concentration, a remarkable 90-fold increase over the native drug. PTX-RPPR has shown potent anti-tumor activity, inhibiting tumor cell proliferation with an IC<sub>50</sub> ranging from 0.26 to 1.64 μM and effectively suppressing migration, invasion, and angiogenesis at a concentration of 75 nM. Notably, in a 4T1 mammary carcinoma model, PTX-RPPR administered at a dose of 0.7 μmol/kg exhibited tumor growth inhibition comparable to that of paclitaxel at a higher dose of 3.5 μmol/kg, with superior efficacy in preventing lung metastasis. Furthermore, PTX-RPPR effectively reduced NRP-1 expression in both tumors and lungs post-treatment. In contrast to paclitaxel formulated with CrEL, PTX-RPPR did not induce IL-6 expression, suggesting a safer profile in terms of immunological response. Characterized by a particle size of 200 nm and a zeta potential of +30 mV, the nano-formulation of PTX-RPPR demonstrated remarkable stability over seven days. This study introduced PTX-RPPR as a promising peptide-drug conjugate that addresses the solubility and hypersensitivity issues associated with paclitaxel, offering a safer therapeutic strategy for cancer treatment.</p>","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":"178 ","pages":"117264"},"PeriodicalIF":0.0,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141989771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Retraction notice to 'MiR-370 functions as oncogene in melanoma by direct targeting pyruvate dehydrogenase B' [Biomedicine & Pharmacotherapy, Volume 90 (2017) Pages 278-286]. MiR-370通过直接靶向丙酮酸脱氢酶B在黑色素瘤中发挥癌基因功能》的撤稿通知[《生物医学与药物治疗》,第90卷(2017),第278-286页]。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-09-01 Epub Date: 2024-07-21 DOI: 10.1016/j.biopha.2024.117168
Shufang Wei, Weiyuan Ma
{"title":"Retraction notice to 'MiR-370 functions as oncogene in melanoma by direct targeting pyruvate dehydrogenase B' [Biomedicine & Pharmacotherapy, Volume 90 (2017) Pages 278-286].","authors":"Shufang Wei, Weiyuan Ma","doi":"10.1016/j.biopha.2024.117168","DOIUrl":"10.1016/j.biopha.2024.117168","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117168"},"PeriodicalIF":0.0,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141749962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Corrigendum to "Berberine mitigates cognitive decline in an Alzheimer's Disease Mouse Model by targeting both tau hyperphosphorylation and autophagic clearance" [Biomed. Pharmacother. 121 (2020) 109670]. 小檗碱通过靶向 tau 过度磷酸化和自噬清除减轻阿尔茨海默病小鼠模型的认知能力下降》[Biomed. Pharmacother. 121 (2020) 109670]的更正。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-09-01 Epub Date: 2024-08-03 DOI: 10.1016/j.biopha.2024.117250
Ying Chen, Yuling Chen, Yubin Liang, Hongda Chen, Xiaoying Ji, Min Huang
{"title":"Corrigendum to \"Berberine mitigates cognitive decline in an Alzheimer's Disease Mouse Model by targeting both tau hyperphosphorylation and autophagic clearance\" [Biomed. Pharmacother. 121 (2020) 109670].","authors":"Ying Chen, Yuling Chen, Yubin Liang, Hongda Chen, Xiaoying Ji, Min Huang","doi":"10.1016/j.biopha.2024.117250","DOIUrl":"10.1016/j.biopha.2024.117250","url":null,"abstract":"","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":" ","pages":"117250"},"PeriodicalIF":0.0,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141891257","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and biological evaluation of imidazolium conjugated with dimethylcardamonin (DMC) as a novel potential agent against MDA-MB-231 triple-negative breast cancer cells. 咪唑鎓与二甲基卡达莫宁(DMC)共轭物的合成与生物学评价,作为一种新型潜在制剂抗击 MDA-MB-231 三阴性乳腺癌细胞。
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie Pub Date : 2024-09-01 Epub Date: 2024-08-06 DOI: 10.1016/j.biopha.2024.117249
Pornthip Chawapun, Nopawit Khamto, Kraikrit Utama, Sadanon Siriphong, Nathupakorn Dechsupa, Jiraporn Kantapan, Jomkhwan Meerak, Puttinan Meepowpan, Padchanee Sangthong
{"title":"Synthesis and biological evaluation of imidazolium conjugated with dimethylcardamonin (DMC) as a novel potential agent against MDA-MB-231 triple-negative breast cancer cells.","authors":"Pornthip Chawapun, Nopawit Khamto, Kraikrit Utama, Sadanon Siriphong, Nathupakorn Dechsupa, Jiraporn Kantapan, Jomkhwan Meerak, Puttinan Meepowpan, Padchanee Sangthong","doi":"10.1016/j.biopha.2024.117249","DOIUrl":"10.1016/j.biopha.2024.117249","url":null,"abstract":"<p><p>A new imidazolium ionic liquid (IL) halide conjugated with dimethylcardamonin (DMC, 1), namely [Bbim]Br-DMC (3), was synthesised to improve the biological activity of the natural chalcone. DMC was isolated from seeds of Syzygium nervosum A. Cunn. ex DC. which was an effective anti-breast cancer agent. The compound 1 and 3 showed anticancer activity in MDA-MB-231 cells with IC<sub>50</sub> values of 14.54 ± 0.99 μM and 7.40 ± 0.15 μM, respectively. MTT assay showed that compound 3 had cytotoxic effect at least two-fold greater than compound 1 but was low toxic to normal cells of Hs 578Bst. After 48 h, compound 3 at concentration of IC<sub>50</sub> value inhibited the proliferation and induced morphological changes of MDA-MB-231 cells in a time-dependent manner. The cell cycle profile also showed that compound 3 exerted anti-proliferation activity with the cell cycle arrest at G0/G1 phase and compound 3 also induced apoptosis and reduced mitochondrial membrane potential in MDA-MB-231 cells in a dose-dependent manner. In gene expression assay, compound 3 up-regulated pro-apoptotic genes such as Bax and p53 and suppressed anti-apoptotic Bcl-2 whereas there was no effect on DNA repair gene such as PARP1. The Bax/Bcl-2 ratio was significantly increased after treated with compound 3. In the molecular docking study, the interactions between compound 3 and B-DNA structure in the minor groove region via hydrogen bonds was reported. In conclusion, [Bbim]Br-DMC or compound 3 is a potential candidate to induce apoptosis and inhibits proliferation via cell cycle arrest and decreases mitochondrial membrane of triple-negative breast cancer MDA-MB-231 cells.</p>","PeriodicalId":93904,"journal":{"name":"Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie","volume":"178 ","pages":"117249"},"PeriodicalIF":0.0,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141903958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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