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Corrigendum to “Anti-diabetic compounds from the seeds of Psoralea corylifolia” [Fitoterapia 139 (2019) 104373] “补骨脂种子抗糖尿病化合物”的勘误表[Fitoterapia 139(2019) 104373]。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.107036
Gaohui Zhu, Yanhong Luo, Xuejiao Xu, Huijiao Zhang, Min Zhu
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引用次数: 0
Corrigendum to “Pharmacodynamic effects and mechanism of Pueraria lobata-Schisandra chinensis combination in the treatment of alcoholic liver disease” [Fitoterapia 187 (2025) 106873] “葛根-五味子联合治疗酒精性肝病的药效学作用及机制”的勘误表[Fitoterapia 187(2025) 106873]。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.106991
Shihao Zhang , Ding Liu , Dongyan Guo , Chongbo Zhao , Yajun Shi , Junbo Zou , Huanxian Shi , Jiangxue Cheng , Jing Sun , Xiaofei Zhang
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引用次数: 0
Corrigendum to “Isolation and characterization of xuetonlignans L-P, previously undescribed spirobenzofuranoid dibenzocyclooctadiene lignans from the fruits of Kadsura heteroclita” [Fitoterapia 185 (2025) 106726] “从Kadsura heteroclita果实中分离和表征雪桐木脂素L-P,先前描述的螺苯并呋喃二苯并环二烯木脂素”的更正[Fitoterapia 185(2025) 106726]。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.107037
Wei Su , Hanwen Yuan , Muhammad Aamer , Xudong Zhou , Kang Zhou , Ling Li , Yupei Yang , Qingling Xie , Shiqi Liu , Gang Fu , Yu Mao , Bin Li , Wei Wang
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引用次数: 0
Corrigendum to “Chemical profiling of Lycium shawii via RP-HPLC-QTOF-MS and MS/MS: Unveiling its in-vivo wound-healing potential supported by molecular docking investigations” [Fitoterapia 185 (2025) 106749] “通过RP-HPLC-QTOF-MS和MS/MS分析枸杞的化学特征:揭示其体内伤口愈合潜力的分子对接研究”的更正[Fitoterapia 185(2025) 106749]。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.106953
Mahmoud Moustafa , Walaa S. Aboelmaaty , Weaam Ebrahim , Reham Hassan Mekky , Mohamed A. Tammam , Amr El-Demerdash , Ahmed M. Zaghloul
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引用次数: 0
Corrigendum to “Bushen Yinao pill improves cognitive function in Alzheimer's disease rats by regulating PI3K/Akt pathway and intestinal microbiota” [Fitoterapia 188 (2026) 106999] 补肾益脑丸通过调节PI3K/Akt通路和肠道菌群改善阿尔茨海默病大鼠认知功能[Fitoterapia 188(2026) 106999]的更正。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.107019
Shunfeng Lan , Fan Gao , Rong Ji, Zixuan Wang, Zhikun Zang, Yuxin Wei, Haixue Kuang, Zhibin Wang
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引用次数: 0
Gardenia jasminoides Ellis polysaccharides improve gut microbiota disorder and glucose homeostasis in type 2 diabetic mice 栀子多糖改善2型糖尿病小鼠肠道菌群紊乱和葡萄糖稳态。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 DOI: 10.1016/j.fitote.2025.107080
Wenye Lu , Wanjun Ju , Ningning Niu , Yuanyuan Li , Tianming Wang , Yu Feng , Yueming Ma , Jiasheng Wu
Type 2 diabetes mellitus (T2DM) is the most prevalent metabolic disorder. Gardenia jasminoides Ellis is a traditional herbal medicine used in metabolic disease treatment; however, the effects of Gardenia jasminoides Ellis polysaccharides (GPS) on T2DM remain unknown. This study aimed to investigate the antidiabetic effect of GPS in a T2DM mouse model induced by high-fat diet (HFD) and streptozotocin administration, and to elucidate the potential molecular mechanism. Treatment with low and high doses (200 and 400 mg/kg) of GPS significantly reduced the fasting blood glucose level of T2DM mice by 44.8 % and 33.0 %, respectively. In T2DM mice, oral glucose tolerance test outcomes and insulin tolerance were significantly improved by GPS intervention (p < 0.05), and the pancreatic tissue damage was ameliorated compared with control mice. Moreover, GPS intervention upregulated the liver expression of peroxisome proliferator-activated receptor gamma (PPARγ) by 1.7 fold, improved insulin resistance, and increased glycogen synthesis in T2DM mice compared with in untreated control mice (p < 0.05). More importantly, GPS intervention significantly improved gut microbiota dysbiosis, increased the abundance of short chain fatty acids producing Lactobacillus and Dubosiella by 6.6- and 16.5-fold, respectively, and elevated the serum level of butyric acid in T2DM mice. Furthermore, in vitro experiments confirmed that butyric acid can induce PPARγ expression. In conclusion, these findings suggest that GPS may alleviate T2DM by reshaping the gut microbiota and regulating intestinal metabolites. Therefore, GPS may be a potential prebiotic for modulating T2DM-associated metabolic disorders.
2型糖尿病(T2DM)是最常见的代谢紊乱。栀子是治疗代谢性疾病的传统中草药;然而,栀子多糖(GPS)对T2DM的影响尚不清楚。本研究旨在探讨GPS在高脂饮食(HFD)和链脲佐菌素诱导的T2DM小鼠模型中的降糖作用,并探讨其可能的分子机制。低剂量和高剂量(100和200 mg/kg)的GPS治疗可使T2DM小鼠的空腹血糖水平分别降低44.8% %和33.0% %。在T2DM小鼠中,GPS干预显著改善了口服糖耐量试验结果和胰岛素耐量(p
{"title":"Gardenia jasminoides Ellis polysaccharides improve gut microbiota disorder and glucose homeostasis in type 2 diabetic mice","authors":"Wenye Lu ,&nbsp;Wanjun Ju ,&nbsp;Ningning Niu ,&nbsp;Yuanyuan Li ,&nbsp;Tianming Wang ,&nbsp;Yu Feng ,&nbsp;Yueming Ma ,&nbsp;Jiasheng Wu","doi":"10.1016/j.fitote.2025.107080","DOIUrl":"10.1016/j.fitote.2025.107080","url":null,"abstract":"<div><div>Type 2 diabetes mellitus (T2DM) is the most prevalent metabolic disorder. <em>Gardenia jasminoides</em> Ellis is a traditional herbal medicine used in metabolic disease treatment; however, the effects of <em>Gardenia jasminoides</em> Ellis polysaccharides (GPS) on T2DM remain unknown. This study aimed to investigate the antidiabetic effect of GPS in a T2DM mouse model induced by high-fat diet (HFD) and streptozotocin administration, and to elucidate the potential molecular mechanism. Treatment with low and high doses (200 and 400 mg/kg) of GPS significantly reduced the fasting blood glucose level of T2DM mice by 44.8 % and 33.0 %, respectively. In T2DM mice, oral glucose tolerance test outcomes and insulin tolerance were significantly improved by GPS intervention (<em>p</em> &lt; 0.05), and the pancreatic tissue damage was ameliorated compared with control mice. Moreover, GPS intervention upregulated the liver expression of peroxisome proliferator-activated receptor gamma (PPARγ) by 1.7 fold, improved insulin resistance, and increased glycogen synthesis in T2DM mice compared with in untreated control mice (<em>p</em> &lt; 0.05). More importantly, GPS intervention significantly improved gut microbiota dysbiosis, increased the abundance of short chain fatty acids producing <em>Lactobacillus</em> and <em>Dubosiella</em> by 6.6- and 16.5-fold, respectively, and elevated the serum level of butyric acid in T2DM mice. Furthermore, in vitro experiments confirmed that butyric acid can induce PPARγ expression. In conclusion, these findings suggest that GPS may alleviate T2DM by reshaping the gut microbiota and regulating intestinal metabolites. Therefore, GPS may be a potential prebiotic for modulating T2DM-associated metabolic disorders.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107080"},"PeriodicalIF":2.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145896384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phytochemical constituents and toxicological, anti-inflammatory, and antinociceptive assessment of Baliospermum effusum Pax et Hoffm. 积液巴利ospermum effusum Pax et Hoffm.植物化学成分及毒理学、抗炎和抗伤性评价。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-12-31 DOI: 10.1016/j.fitote.2025.107078
Qing-Ying Hong, Zu-Hui Wang, Yi-Hang Ba, Yi-Huan Li, De-Xin Li, Hong-Ping He, Rui Yang, Hua-Yi Jiang
Baliospermum effusum Pax et Hoffm., a shrub known as “Baodongdian” in Dai folk medicine, has been traditionally employed for treating traumatic injuries, rheumatism, and jaundice. The present study investigated the acute toxicity, anti-inflammatory and antinociceptive properties, and phytochemical constituents of the 95 % ethanolic extract of B. effusum (EEBe). The toxicity assessment revealed that EEBe (2000 mg/kg) induced no adverse effects in behavior, mortality, body/organ weights, histopathology, or biochemical parameters over 14 d. Pharmacological assays on EEBe (150, 300, and 600 mg/kg) revealed that it effectively inhibited carrageenan-induced paw edema (n = 10), xylene-stimulated ear edema (n = 8), and acetic acid-triggered writhes (n = 8), while showing no significant antinociceptive activity in the hot-plate test (n = 8). ELISA (n = 8) showed that EEBe modulated serum IL-1β, IL-6, and IL-10 levels, while qRT-PCR (n = 5) demonstrated the downregulation of IL-1β and IL-6 mRNA expression. Furthermore, eight compounds including 4-hydroxy-2,3-dimethyl-2-nonen-4-olide (1), 22-dehydroclerosterol (2), β-sitosterol (3), vanillin (4), 1-linolenoylglycerol (5), 1-O-stearoyl-glycerol (6), bis(2,3-dihydroxypropyl)nonanedioate (7), and (3S,5S)-diverniciaoid A (8) were isolated from EEBe, with compounds 5 and 7 suppressing NO production in LPS-induced RAW 264.7 macrophages. These data revealed that EEBe was non-toxic at 2000 mg/kg and exhibited anti-inflammatory and antinociceptive properties, and that 5 and 7, reported for the first time from this species, showed anti-inflammatory activity in vitro, collectively supporting the folk use of B. effusum for inflammatory and pain-related disorders. To our knowledge, this is the first report on the in vivo pharmacological activities and toxicity of B. effusum.
Pax et Hoffm。在傣族民间医学中,这种灌木被称为“宝洞店”,传统上被用来治疗外伤、风湿病和黄疸。本文研究了95 %乙醇提取物的急性毒性、抗炎、抗伤性和植物化学成分。毒性评估显示,EEBe(2000 毫克/公斤)诱导行为,没有不利影响死亡率,阀体/器官重量、组织病理学、或生化参数超过14 d。药理分析EEBe(150、300和600 毫克/公斤)透露,它有效地抑制carrageenan-induced爪子水肿(n = 10),xylene-stimulated耳朵水肿(n = 8)和醋酸acid-triggered扭动(n = 8),而没有显著的抗antinociceptive活动(n = 8)。ELISA (n = 8)结果显示,EEBe可调节血清IL-1β、IL-6、IL-10水平,qRT-PCR (n = 5)结果显示,ebe可下调血清IL-1β、IL-6 mRNA表达。此外,从EEBe中分离到8个化合物,包括4-羟基-2,3-二甲基-2-壬烯-4-olide(1)、22- dehydroclero甾醇(2)、β-谷甾醇(3)、香兰素(4)、1-亚麻烯酰甘油(5)、1- o -硬脂酰甘油(6)、双(2,3-二羟丙基)壬烯二酸酯(7)和(3S,5S)-diverniciaoid A(8),其中化合物5和7抑制lps诱导的RAW 264.7巨噬细胞NO的产生。这些数据表明,EEBe在2000 mg/kg时无毒,具有抗炎和抗伤性,并且首次从该物种中报道的5和7在体外显示出抗炎活性,共同支持民间将积液芽孢杆菌用于炎症和疼痛相关疾病。据我们所知,这是第一个关于积液芽孢杆菌体内药理活性和毒性的报道。
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引用次数: 0
Bee bread as a natural shield against genetic damage: Investigation of antigenotoxic and antimutagenic potential 蜜蜂面包作为抗基因损伤的天然屏障:抗基因毒性和抗诱变潜力的研究。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-12-27 DOI: 10.1016/j.fitote.2025.107077
Karolina Matejczuk , Piotr M. Kuś , Piotr Szweda
Bee bread (BB), a fermented bee product rich in bioactive compounds, such as aminoacids and peptides, vitamins and polyphenols, has garnered attention for its potential health benefits, particularly high antioxidant potential. However, its role in protecting genetic material from damage (antigenotoxic and antimutagenic activity) remains largely unexplored. This study provides the first comprehensive evaluation of both antigenotoxic and antimutagenic activities of Polish bee bread extracts in human HEK293 cells, integrating functional assays with advanced chemical profiling.
Twenty Polish BB samples were analyzed for antioxidant activity using DPPH Radical Scavenging Assay and Cellular Antioxidant Activity assays, revealing significant radical scavenging and intracellular ROS reduction capacities. UHPLC-DAD-QqTOF-MS profiling identified 71 compounds, predominantly flavonoids and phenolamides, known for their cytoprotective roles.
Importantly, comet assay results demonstrated that BB extracts significantly reduced methyl methanesulfonate (MMS)-induced DNA strand breaks, while cytokinesis-block micronucleus assay confirmed up to 91 % reduction in mutagenicity without intrinsic genotoxicity. Unlike previous studies that focused primarily on antioxidant activity, our work establishes bee bread as a natural chemoprotective agent against DNA damage and chromosomal instability, highlighting its potential in disease prevention. These findings expand the current understanding of bee bread bioactivity and position it as a promising candidate for functional food and nutraceutical applications.
蜜蜂面包(BB)是一种富含生物活性化合物的发酵蜂产品,如氨基酸和多肽、维生素和多酚,因其潜在的健康益处,特别是高抗氧化潜力而受到关注。然而,它在保护遗传物质免受损害(抗基因毒性和抗诱变活性)方面的作用在很大程度上仍未被探索。该研究首次综合评价了波兰蜜蜂面包提取物对人HEK293细胞的抗基因毒性和抗诱变活性,将功能分析与先进的化学分析相结合。使用DPPH自由基清除实验和细胞抗氧化活性实验分析了20个波兰BB样品的抗氧化活性,揭示了显著的自由基清除和细胞内ROS还原能力。UHPLC-DAD-QqTOF-MS分析鉴定了71种化合物,主要是类黄酮和酚酰胺,已知具有细胞保护作用。重要的是,彗星试验结果表明,BB提取物显著降低了甲基甲烷磺酸盐(MMS)诱导的DNA链断裂,而细胞分裂阻断微核试验证实,在没有内在遗传毒性的情况下,致突变性降低了91% %。与以往主要关注抗氧化活性的研究不同,我们的工作确定了蜜蜂面包是一种天然的化学保护剂,可以防止DNA损伤和染色体不稳定,突出了它在疾病预防方面的潜力。这些发现扩大了目前对蜜蜂面包生物活性的理解,并将其定位为功能性食品和营养保健应用的有希望的候选者。
{"title":"Bee bread as a natural shield against genetic damage: Investigation of antigenotoxic and antimutagenic potential","authors":"Karolina Matejczuk ,&nbsp;Piotr M. Kuś ,&nbsp;Piotr Szweda","doi":"10.1016/j.fitote.2025.107077","DOIUrl":"10.1016/j.fitote.2025.107077","url":null,"abstract":"<div><div>Bee bread (BB), a fermented bee product rich in bioactive compounds, such as aminoacids and peptides, vitamins and polyphenols, has garnered attention for its potential health benefits, particularly high antioxidant potential. However, its role in protecting genetic material from damage (antigenotoxic and antimutagenic activity) remains largely unexplored. This study provides the first comprehensive evaluation of both antigenotoxic and antimutagenic activities of Polish bee bread extracts in human HEK293 cells, integrating functional assays with advanced chemical profiling.</div><div>Twenty Polish BB samples were analyzed for antioxidant activity using DPPH Radical Scavenging Assay and Cellular Antioxidant Activity assays, revealing significant radical scavenging and intracellular ROS reduction capacities. UHPLC-DAD-QqTOF-MS profiling identified 71 compounds, predominantly flavonoids and phenolamides, known for their cytoprotective roles.</div><div>Importantly, comet assay results demonstrated that BB extracts significantly reduced methyl methanesulfonate (MMS)-induced DNA strand breaks, while cytokinesis-block micronucleus assay confirmed up to 91 % reduction in mutagenicity without intrinsic genotoxicity. Unlike previous studies that focused primarily on antioxidant activity, our work establishes bee bread as a natural chemoprotective agent against DNA damage and chromosomal instability, highlighting its potential in disease prevention. These findings expand the current understanding of bee bread bioactivity and position it as a promising candidate for functional food and nutraceutical applications.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107077"},"PeriodicalIF":2.6,"publicationDate":"2025-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145855107","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Progress of anti-tumor research on natural products combined with doxorubicin 天然产物联合阿霉素抗肿瘤研究进展。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-12-27 DOI: 10.1016/j.fitote.2025.107076
Yanqing Wu, Jianguo Gao, Yuwei Zhao, Yingzhi Lu, Xiaoqing Cai
Cancer represents a major global public health challenge, with its incidence and mortality rates increasing annually. Doxorubicin (DOX) is a commonly used chemotherapeutic agent. Despite its marked antitumor efficacy, the clinical application of DOX is limited by drug resistance and cumulative toxicity. Numerous natural products have garnered significant attention owing to their favorable antitumor, antioxidant, anti-inflammatory, and anti-apoptotic properties, and are increasingly being developed as adjuvant agents in combination therapy with DOX. The co-administration of natural products with DOX has emerged as a promising strategy to enhance therapeutic outcomes while mitigating adverse effects. However, this combination approach is constrained by poor drug solubility and disparate pharmacokinetic profiles. The advent of multifunctional nanodelivery systems has improved drug bioavailability and tumor targeting, thereby laying the groundwork for synergistic interactions between natural products and DOX. This review systematically summarizes the antitumor mechanisms and toxic side effects of DOX, elucidates the mechanisms of action and structure-activity relationships of certain natural products serving as DOX sensitizers and protective agents, and highlights recent advances in nano-platform-based co-delivery strategies, offering valuable insights for future cancer therapeutics.
癌症是一项重大的全球公共卫生挑战,其发病率和死亡率每年都在上升。阿霉素(DOX)是一种常用的化疗药物。尽管DOX具有显著的抗肿瘤疗效,但其耐药和累积毒性限制了其临床应用。许多天然产物因其良好的抗肿瘤、抗氧化、抗炎和抗凋亡特性而受到广泛关注,并越来越多地被开发为与DOX联合治疗的佐剂。天然产物与DOX联合给药已成为一种有希望的策略,可以提高治疗效果,同时减轻不良反应。然而,这种联合方法受到药物溶解度差和不同药代动力学特征的限制。多功能纳米递送系统的出现改善了药物的生物利用度和肿瘤靶向性,从而为天然产物和DOX之间的协同相互作用奠定了基础。本文系统总结了DOX的抗肿瘤机制和毒副作用,阐明了某些天然产物作为DOX致敏剂和保护剂的作用机制和构效关系,并重点介绍了基于纳米平台的共给药策略的最新进展,为未来的癌症治疗提供了有价值的见解。
{"title":"Progress of anti-tumor research on natural products combined with doxorubicin","authors":"Yanqing Wu,&nbsp;Jianguo Gao,&nbsp;Yuwei Zhao,&nbsp;Yingzhi Lu,&nbsp;Xiaoqing Cai","doi":"10.1016/j.fitote.2025.107076","DOIUrl":"10.1016/j.fitote.2025.107076","url":null,"abstract":"<div><div>Cancer represents a major global public health challenge, with its incidence and mortality rates increasing annually. Doxorubicin (DOX) is a commonly used chemotherapeutic agent. Despite its marked antitumor efficacy, the clinical application of DOX is limited by drug resistance and cumulative toxicity. Numerous natural products have garnered significant attention owing to their favorable antitumor, antioxidant, anti-inflammatory, and anti-apoptotic properties, and are increasingly being developed as adjuvant agents in combination therapy with DOX. The co-administration of natural products with DOX has emerged as a promising strategy to enhance therapeutic outcomes while mitigating adverse effects. However, this combination approach is constrained by poor drug solubility and disparate pharmacokinetic profiles. The advent of multifunctional nanodelivery systems has improved drug bioavailability and tumor targeting, thereby laying the groundwork for synergistic interactions between natural products and DOX. This review systematically summarizes the antitumor mechanisms and toxic side effects of DOX, elucidates the mechanisms of action and structure-activity relationships of certain natural products serving as DOX sensitizers and protective agents, and highlights recent advances in nano-platform-based co-delivery strategies, offering valuable insights for future cancer therapeutics.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107076"},"PeriodicalIF":2.6,"publicationDate":"2025-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145855128","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of sapogenin isolated from the defatted seeds of Camellia oleifera and its derivative as anti-breast cancer agents 油茶籽皂苷元及其衍生物抗乳腺癌作用的评价。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-12-27 DOI: 10.1016/j.fitote.2025.107075
Lu Li , Chuanqing Huang , Yunong Tian , Ying Wen , Meng Zhang , Yulin Liu , Shuhong Lin , Xianchun Hu , Yong Ye
The defatted seeds of Camellia oleifera are an underutilized resource that leads to poor economy. Saponins extracted from these seeds exhibit anti-breast cancer effects. To augment their anticancer efficacy, the saponins were structurally modified by the incorporation of a thiosemicarbazone moiety to yield the Camellia sapogenin thiosemicarbazone (CST). CST was subsequently complexed with zinc to form Zn-CST. This zinc complex demonstrated markedly enhanced antiproliferative and cytotoxic activity in ER+ / PR+ MCF-7 cells (IC₅₀ = 3.21 ± 0.44 μM) and HER2- T47D cells (IC₅₀ = 9.80 ± 1.31 μM), demonstrating greater potency than erlotinib. In MCF-7 cells, Zn-CST induced cell cycle arrest at the G₀ / G₁ phase and resulted in a 27-fold increase in apoptosis. Additionally, Zn-CST exhibited more potent inhibitory activity against EGFR kinase, with an IC₅₀ value of 0.25 ± 0.02 μM, compared to erlotinib. Molecular docking analysis confirmed Zn-CST's superior binding affinity for EGFR with a binding energy of −102.7 kcal/mol, predominantly due to a strong electrostatic interaction with Asp831. Collectively, these findings suggest that Zn-CST could be developed as anti ER+ / PR+ breast cancer candidate.
油茶的脱脂种子是一种未充分利用的资源,导致经济状况不佳。从这些种子中提取的皂苷具有抗乳腺癌的作用。为了增强其抗癌作用,我们对这些皂苷进行了结构修饰,加入了硫代氨基脲部分,得到了山茶皂苷基硫代氨基脲(CST)。CST随后与锌络合形成Zn-CST。这锌复杂了明显增强的抗增殖和细胞毒性活动ER + / PR + MCF-7细胞(IC₅₀ = 3.21 ±0.44  μM)和HER2 - T47D细胞(IC₅₀ = 9.80 ±1.31  μM),证明比埃罗替尼更大的力量。在MCF-7细胞中,Zn-CST诱导细胞周期阻滞在G 0 / G 1期,导致细胞凋亡增加27倍。此外,与厄洛替尼相比,Zn-CST对EGFR激酶表现出更强的抑制活性,IC₅₀值为0.25 ± 0.02 μM。分子对接分析证实,Zn-CST对EGFR具有较强的结合亲和力,结合能为-102.7 kcal/mol,这主要是由于与Asp831的强静电相互作用。总之,这些发现表明Zn-CST可以作为抗ER+ / PR+乳腺癌的候选药物。
{"title":"Evaluation of sapogenin isolated from the defatted seeds of Camellia oleifera and its derivative as anti-breast cancer agents","authors":"Lu Li ,&nbsp;Chuanqing Huang ,&nbsp;Yunong Tian ,&nbsp;Ying Wen ,&nbsp;Meng Zhang ,&nbsp;Yulin Liu ,&nbsp;Shuhong Lin ,&nbsp;Xianchun Hu ,&nbsp;Yong Ye","doi":"10.1016/j.fitote.2025.107075","DOIUrl":"10.1016/j.fitote.2025.107075","url":null,"abstract":"<div><div>The defatted seeds of <em>Camellia oleifera</em> are an underutilized resource that leads to poor economy. Saponins extracted from these seeds exhibit anti-breast cancer effects. To augment their anticancer efficacy, the saponins were structurally modified by the incorporation of a thiosemicarbazone moiety to yield the <em>Camellia</em> sapogenin thiosemicarbazone (CST). CST was subsequently complexed with zinc to form Zn-CST. This zinc complex demonstrated markedly enhanced antiproliferative and cytotoxic activity in ER+ / PR+ MCF-7 cells (IC₅₀ = 3.21 ± 0.44 μM) and HER2- T47D cells (IC₅₀ = 9.80 ± 1.31 μM), demonstrating greater potency than erlotinib. In MCF-7 cells, Zn-CST induced cell cycle arrest at the G₀ / G₁ phase and resulted in a 27-fold increase in apoptosis. Additionally, Zn-CST exhibited more potent inhibitory activity against EGFR kinase, with an IC₅₀ value of 0.25 ± 0.02 μM, compared to erlotinib. Molecular docking analysis confirmed Zn-CST's superior binding affinity for EGFR with a binding energy of −102.7 kcal/mol, predominantly due to a strong electrostatic interaction with Asp831. Collectively, these findings suggest that Zn-CST could be developed as anti ER+ / PR+ breast cancer candidate.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107075"},"PeriodicalIF":2.6,"publicationDate":"2025-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145855052","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","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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