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Evaluation of the antibacterial and antifungal properties of oleuropein, olea Europea leaf extract, and thymus vulgaris oil. 评估油菜素、油菜叶提取物和胸腺油的抗菌和抗真菌特性。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-08-09 DOI: 10.1186/s12906-024-04596-x
Fuad Al-Rimawi, Mahmood Sbeih, Mousa Amayreh, Belal Rahhal, Samer Mudalal

Background: Although synthetic preservatives and antioxidants may have high antimicrobial and antioxidant activity, they are usually associated with adverse effects on human health. Currently, there is a growing interest in natural antimicrobial and antioxidant agents. This study aimed to evaluate the antimicrobial activity of two medicinal plant extracts and one active compound. Olive leaf extracts (0.2, 0.3, and 0.4% w/v), oleuropein (0.2, 0.4, and 0.6% w/v), thyme oil (0.1%), and oleuropein in combination with thyme oil (0.4% w/v and 0.1% v/v) were used against three bacterial strains (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus) and two fungal strains (Candida albicans and Aspergillus niger).

Results: The use of oleuropein resulted in complete antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. In this context, a reduction of 7 logs was achieved during the storage period (4 weeks). Oleuropein showed no fungal activity at low concentrations (0.2%), but Aspergillus niger was reduced by 2.35 logs at higher concentrations (0.6% w/v). Similar antibacterial and antifungal properties were observed for the olive leaf extracts. Oleuropein at a concentration of 0.4 w/v and a mixture of oleuropein and thyme at concentrations of 0.4 and 0.1 (v/v) showed strong antimicrobial activity against the studied microorganisms.

Conclusion: Olive leaf extract, thyme oil, and oleuropein have strong antibacterial and weak antifungal properties. There was a good synergistic effect between oleuropein and thymol.

背景:尽管合成防腐剂和抗氧化剂可能具有很高的抗菌和抗氧化活性,但它们通常会对人体健康产生不利影响。目前,人们对天然抗菌剂和抗氧化剂的兴趣与日俱增。本研究旨在评估两种药用植物提取物和一种活性化合物的抗菌活性。橄榄叶提取物(0.2%、0.3% 和 0.4% w/v)、油菜素(0.2%、0.4% 和 0.6% w/v)、百里香油(0.1%)以及油菜素与百里香油(0.4% w/v 和 0.1% v/v)来对抗三种细菌菌株(大肠杆菌、绿脓杆菌和金黄色葡萄球菌)和两种真菌菌株(白色念珠菌和黑曲霉):结果:使用油菜素对金黄色葡萄球菌、绿脓杆菌和大肠杆菌具有完全的抗菌活性。在这种情况下,贮藏期(4 周)内可减少 7 个对数值。油菜素在低浓度(0.2%)时没有真菌活性,但在较高浓度(0.6% w/v)时,黑曲霉的活性降低了 2.35 个对数值。橄榄叶提取物也具有类似的抗菌和抗真菌特性。浓度为 0.4 w/v 的油菜素以及浓度为 0.4 和 0.1(v/v)的油菜素和百里香混合物对所研究的微生物具有很强的抗菌活性:结论:橄榄叶提取物、百里香油和油菜素具有较强的抗菌性和较弱的抗真菌性。油菜素和百里酚之间有很好的协同作用。
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引用次数: 0
Extract of Phyllanthus emblica L. fruit stimulates basal glucose uptake and ameliorates palmitate-induced insulin resistance through AMPK activation in C2C12 myotubes. 刺五加果实提取物可通过激活 C2C12 肌细胞中的 AMPK 刺激基础葡萄糖摄取并改善棕榈酸酯诱导的胰岛素抵抗。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-08-02 DOI: 10.1186/s12906-024-04592-1
Hai-Yan Li, Chun-Fei Li, Chun-Hui Liu, Sun-Ce Chen, Yi-Fan Liu, Quan-He Lv, Wen Zhang

Background: The fruit of Phyllanthus emblica L., a traditional medicine in China and India, is used to treat diabetes mellitus. Its water extract (WEPE) has demonstrated hypoglycemic effects in diabetic rats, but its mechanisms on glucose utilization and insulin resistance in skeletal muscle remain unclear. Therefore, this study aims to investigate the effects and underlying mechanisms of WEPE on glucose utilization and insulin resistance using C2C12 myotubes.

Methods: Effects of WEPE on glucose uptake, GLUT4 translocation, and AMPK and AKT phosphorylation were investigated in C2C12 myotubes and palmitate-treated myotubes. An AMPK inhibitor and siRNA were used to explore the mechanisms of WEPE. Glucose uptake was determined using a 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-2-deoxyglucose (2-NBDG) uptake assay, and protein expression and GLUT4 translocation were assessed via western blotting.

Results: In normal myotubes, WEPE significantly stimulated glucose uptake and GLUT4 translocation to the plasma membrane at concentrations of 125 and 250 µg/mL. This was accompanied by an increase in the phosphorylation of AMPK and its downstream targets. However, both compound C and AMPK siRNA blocked the WEPE-induced GLUT4 translocation and glucose uptake. Moreover, pretreatment with STO-609, a calcium/calmodulin-dependent protein kinase kinase β (CaMKKβ) inhibitor, inhibited WEPE-induced AMPK phosphorylation and attenuated the WEPE-stimulated glucose uptake and GLUT4 translocation. In myotubes treated with palmitate, WEPE prevented palmitate-induced insulin resistance by enhancing insulin-mediated glucose uptake and AKT phosphorylation. It also restored the insulin-mediated translocation of GLUT4 from cytoplasm to membrane. However, these effects of WEPE on glucose uptake and GLUT4 translocation were blocked by pretreatment with compound C.

Conclusions: WEPE significantly stimulated basal glucose uptake though CaMKKβ/AMPK pathway and markedly ameliorated palmitate-induced insulin resistance by activating the AMPK pathway in C2C12 myotubes.

背景:中国和印度的一种传统药物--白皮松果实可用于治疗糖尿病。其水提取物(WEPE)对糖尿病大鼠有降血糖作用,但其对骨骼肌葡萄糖利用和胰岛素抵抗的机制仍不清楚。因此,本研究旨在利用 C2C12 肌管研究 WEPE 对葡萄糖利用和胰岛素抵抗的影响及其内在机制:方法:研究了WEPE对C2C12肌管和棕榈酸盐处理肌管中葡萄糖摄取、GLUT4转位、AMPK和AKT磷酸化的影响。研究使用了 AMPK 抑制剂和 siRNA 来探索 WEPE 的作用机制。使用2-(N-(7-硝基苯并-2-氧杂-1,3-二唑-4-基)氨基)-2-脱氧葡萄糖(2-NBDG)摄取试验测定葡萄糖摄取量,并通过Western印迹法评估蛋白质表达和GLUT4转位:结果:在正常肌管中,当浓度为 125 和 250 µg/mL 时,西普能显著刺激葡萄糖摄取和 GLUT4 转位至质膜。随之而来的是 AMPK 及其下游靶标的磷酸化增加。然而,化合物 C 和 AMPK siRNA 都阻断了 WEPE 诱导的 GLUT4 转位和葡萄糖摄取。此外,使用钙/钙调蛋白依赖性蛋白激酶激酶 β(CaMKKβ)抑制剂 STO-609 预处理可抑制 WEPE 诱导的 AMPK 磷酸化,并减轻 WEPE 刺激的葡萄糖摄取和 GLUT4 转位。在用棕榈酸酯处理的肌管中,WEPE 通过增强胰岛素介导的葡萄糖摄取和 AKT 磷酸化,防止了棕榈酸酯诱导的胰岛素抵抗。它还能恢复胰岛素介导的 GLUT4 从细胞质到细胞膜的转位。然而,化合物 C 的预处理阻断了 WEPE 对葡萄糖摄取和 GLUT4 转位的这些作用:结论:通过激活C2C12肌管中的AMPK通路,WEPE可明显刺激CaMKKβ/AMPK通路的基础葡萄糖摄取,并明显改善棕榈酸酯诱导的胰岛素抵抗。
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引用次数: 0
A randomized controlled trial of acupuncture and receptive music therapy for sleep disorders in the elderly-ELAMUS: study protocol. 针灸和接受性音乐疗法治疗老年人睡眠障碍的随机对照试验--ELAMUS:研究方案。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-08-02 DOI: 10.1186/s12906-024-04581-4
C Klocke, K Rhein, H Cramer, B Kröger, A-J Wetzel, J Vagedes, H Mauch, F Beißner, S Joos, J Valentini

Background: Globally, the demographic shift towards an aging population leads to significant challenges in healthcare systems, specifically due to an increasing incidence of multimorbidity resulting in polypharmacy among the elderly. Simultaneously, sleep disorders are a common complaint for elderly people. A treatment with pharmacological therapies often leads to side effects causing a high potential for dependency. Within this context, there is a high need to explore non-pharmacological therapeutic approaches. The purpose of this study is to evaluate the effectiveness of acupuncture and music therapy, both individually and combined as a multimodal therapy, in the treatment of sleep disorders in individuals aged 70 years and older.

Methods: We conduct a confirmatory randomized controlled trial using a two-factorial study design. A total of n = 100 elderly people receive evidence-based standard care information for age-related sleep disorders. Beyond that, patients are randomly assigned into four groups of n = 25 each to receive acupuncture, receptive music therapy with a monochord, multimodal therapy with both acupuncture and music therapy, or no further therapy. The study's primary outcome measurement is the improvement in sleep quality as assessed by the Pittsburgh Sleep Quality Index (PSQI) (global score), at the end of intervention. Additionally, depression scores (Geriatric Depression Scale), health-related quality of life (Short-Form-Health Survey-12), neurovegetative activity measured via heart rate variability, and safety data are collected as secondary outcomes. Using a mixed-methods approach, a qualitative process evaluation will be conducted to complement the quantitative data.

Discussion: The study is ongoing and the last patient in is expected to be enrolled in April 2024. The results can provide valuable insights into the effectiveness of non-pharmacological interventions for sleep disorders among the elderly, contributing to a more personalized and holistic approach in geriatric healthcare.

Trial registration: German Clinical Trials Register (DRKS00031886).

背景:在全球范围内,人口向老龄化的转变给医疗保健系统带来了巨大的挑战,特别是由于多病症的发病率不断上升,导致老年人使用多种药物。同时,睡眠障碍也是老年人的常见病。使用药物治疗往往会产生副作用,造成很大的依赖性。在这种情况下,亟需探索非药物治疗方法。本研究的目的是评估针灸和音乐疗法作为一种多模式疗法单独或联合治疗 70 岁及以上老年人睡眠障碍的效果:我们采用双因素研究设计进行了一项确证性随机对照试验。共有 n = 100 名老年人接受以循证医学为基础的标准护理信息,以治疗与年龄相关的睡眠障碍。除此之外,患者会被随机分配到四组,每组 n = 25 人,分别接受针灸、单弦接受性音乐疗法、针灸和音乐疗法的多模式疗法,或不再接受其他疗法。研究的主要结果是在干预结束时,通过匹兹堡睡眠质量指数(PSQI)(总分)评估睡眠质量的改善情况。此外,还收集了抑郁评分(老年抑郁量表)、健康相关生活质量(短表格健康调查-12)、通过心率变异性测量的神经活力活动以及安全性数据,作为次要结果。将采用混合方法进行定性过程评估,以补充定量数据:该研究正在进行中,最后一名患者预计将于 2024 年 4 月入组。研究结果将为老年人睡眠障碍的非药物干预措施的有效性提供有价值的见解,有助于在老年医疗保健中采用更加个性化和全面的方法:德国临床试验注册(DRKS00031886)。
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引用次数: 0
The effect of salidroside in promoting endogenous neural regeneration after cerebral ischemia/reperfusion involves notch signaling pathway and neurotrophic factors. 水杨甙促进脑缺血/再灌注后内源性神经再生的作用涉及notch信号通路和神经营养因子。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-08-01 DOI: 10.1186/s12906-024-04597-w
Jiabing Zheng, Jizhou Zhang, Jing Han, Zhichang Zhao, Kan Lin

Background: Salidroside is the major bioactive and pharmacological active substance in Rhodiola rosea L. It has been reported to have neuroprotective effects on cerebral ischemia/reperfusion (I/R). However, whether salidroside can enhance neural regeneration after cerebral I/R is still unknown. This study investigated the effects of salidroside on the endogenous neural regeneration after cerebral I/R and the related mechanism.

Methods: Focal cerebral I/R was induced in rats by transient middle cerebral artery occlusion/reperfusion (MCAO/R). The rats were intraperitoneally treated salidroside once daily for 7 consecutive days. Neurobehavioral assessments were performed at 3 days and 7 days after the injury. TTC staining was performed to assess cerebral infarct volume. To evaluate the survival of neurons, immunohistochemical staining of Neuronal Nuclei (NeuN) in the ischemic hemisphere were conducted. Also, immunofluorescence double or triple staining of the biomarkers of proliferating neural progenitor cells in Subventricular Zone (SVZ) and striatum of the ischemia hemisphere were performed to investigate the neurogenesis. Furthermore, reverse transcription-polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay (ELISA) were used to detect the expression of neurotrophic factors (NTFs) brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF). Expression of Notch1 and its target molecular Hes1 were also analyzed by western-blotting and RT-PCR.

Results: Salidroside treatment ameliorated I/R induced neurobehavioral impairment, and reduced infarct volume. Salidroside also restored NeuN positive cells loss after I/R injury. Cerebral I/R injury significantly increased the expression of 5-Bromo-2'-Deoxyuridine (BrdU) and doublecotin (DCX), elevated the number of BrdU/Nestin/DCX triple-labeled cells in SVZ, and BrdU/Nestin/glial fibrillary acidic protein (GFAP) triple-labeled cells in striatum. Salidroside treatment further promoted the proliferation of BrdU/DCX labeled neuroblasts and BrdU/Nestin/GFAP labeled reactive astrocytes. Furthermore, salidroside elevated the mRNA expression and protein concentration of BDNF and NGF in ischemia periphery area, as well. Mechanistically, salidroside elevated Notch1/Hes1 mRNA expression in SVZ. The protein levels of them were also increased after salidroside administration.

Conclusions: Salidroside enhances the endogenous neural regeneration after cerebral I/R. The mechanism of the effect may involve the regulation of BDNF/NGF and Notch signaling pathway.

背景:据报道,它对脑缺血/再灌注(I/R)具有神经保护作用。然而,丹皮酚苷能否促进脑缺血再灌注后的神经再生仍是未知数。本研究探讨了水杨甙对脑缺血再灌注后内源性神经再生的影响及其相关机制:方法:通过一过性大脑中动脉闭塞/再灌注(MCAO/R)诱导大鼠局灶性大脑 I/R。大鼠腹腔注射柳氮磺吡啶,每天一次,连续7天。分别在损伤后3天和7天进行神经行为评估。TTC染色用于评估脑梗塞体积。为了评估神经元的存活情况,对缺血半球的神经元核(NeuN)进行了免疫组化染色。此外,还对缺血半球室下区(SVZ)和纹状体中增殖的神经祖细胞的生物标志物进行了免疫荧光双重或三重染色,以研究神经发生。此外,还采用反转录聚合酶链反应(RT-PCR)和酶联免疫吸附试验(ELISA)检测神经营养因子(NTFs)脑源性神经营养因子(BDNF)和神经生长因子(NGF)的表达。此外,还通过 Western-blotting 和 RT-PCR 分析了 Notch1 及其靶分子 Hes1 的表达:结果:水杨甙治疗可改善I/R诱导的神经行为损伤,并缩小梗死体积。水杨甙还能修复I/R损伤后丢失的NeuN阳性细胞。脑I/R损伤明显增加了5-溴-2'-脱氧尿苷(BrdU)和双胞素(DCX)的表达,增加了SVZ中BrdU/Nestin/DCX三重标记细胞的数量,以及纹状体中BrdU/Nestin/胶质纤维酸性蛋白(GFAP)三重标记细胞的数量。柳氮磺胺可进一步促进BrdU/DCX标记的神经母细胞和BrdU/Nestin/GFAP标记的反应性星形胶质细胞的增殖。此外,柳氮磺吡啶还能提高缺血周边区域 BDNF 和 NGF 的 mRNA 表达和蛋白浓度。从机制上讲,水杨甙可提高 SVZ 中 Notch1/Hes1 mRNA 的表达。结论:结论:水杨甙能增强脑I/R后的内源性神经再生。其作用机制可能涉及 BDNF/NGF 和 Notch 信号通路的调节。
{"title":"The effect of salidroside in promoting endogenous neural regeneration after cerebral ischemia/reperfusion involves notch signaling pathway and neurotrophic factors.","authors":"Jiabing Zheng, Jizhou Zhang, Jing Han, Zhichang Zhao, Kan Lin","doi":"10.1186/s12906-024-04597-w","DOIUrl":"10.1186/s12906-024-04597-w","url":null,"abstract":"<p><strong>Background: </strong>Salidroside is the major bioactive and pharmacological active substance in Rhodiola rosea L. It has been reported to have neuroprotective effects on cerebral ischemia/reperfusion (I/R). However, whether salidroside can enhance neural regeneration after cerebral I/R is still unknown. This study investigated the effects of salidroside on the endogenous neural regeneration after cerebral I/R and the related mechanism.</p><p><strong>Methods: </strong>Focal cerebral I/R was induced in rats by transient middle cerebral artery occlusion/reperfusion (MCAO/R). The rats were intraperitoneally treated salidroside once daily for 7 consecutive days. Neurobehavioral assessments were performed at 3 days and 7 days after the injury. TTC staining was performed to assess cerebral infarct volume. To evaluate the survival of neurons, immunohistochemical staining of Neuronal Nuclei (NeuN) in the ischemic hemisphere were conducted. Also, immunofluorescence double or triple staining of the biomarkers of proliferating neural progenitor cells in Subventricular Zone (SVZ) and striatum of the ischemia hemisphere were performed to investigate the neurogenesis. Furthermore, reverse transcription-polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay (ELISA) were used to detect the expression of neurotrophic factors (NTFs) brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF). Expression of Notch1 and its target molecular Hes1 were also analyzed by western-blotting and RT-PCR.</p><p><strong>Results: </strong>Salidroside treatment ameliorated I/R induced neurobehavioral impairment, and reduced infarct volume. Salidroside also restored NeuN positive cells loss after I/R injury. Cerebral I/R injury significantly increased the expression of 5-Bromo-2'-Deoxyuridine (BrdU) and doublecotin (DCX), elevated the number of BrdU/Nestin/DCX triple-labeled cells in SVZ, and BrdU/Nestin/glial fibrillary acidic protein (GFAP) triple-labeled cells in striatum. Salidroside treatment further promoted the proliferation of BrdU/DCX labeled neuroblasts and BrdU/Nestin/GFAP labeled reactive astrocytes. Furthermore, salidroside elevated the mRNA expression and protein concentration of BDNF and NGF in ischemia periphery area, as well. Mechanistically, salidroside elevated Notch1/Hes1 mRNA expression in SVZ. The protein levels of them were also increased after salidroside administration.</p><p><strong>Conclusions: </strong>Salidroside enhances the endogenous neural regeneration after cerebral I/R. The mechanism of the effect may involve the regulation of BDNF/NGF and Notch signaling pathway.</p>","PeriodicalId":9128,"journal":{"name":"BMC Complementary Medicine and Therapies","volume":null,"pages":null},"PeriodicalIF":3.3,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11295647/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141874088","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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
Phytochemical and biological investigation of Astragalus Caprinus L. 黄芪的植物化学和生物学研究
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-08-01 DOI: 10.1186/s12906-024-04484-4
Walid E Abdallah, Khaled A Abdelshafeek, Wael M Elsayed, Mona M AbdelMohsen, Neven A Salah, Heba D Hassanein

Background: cultivated and wild plants are used to treat different ailments. The Astragalus genus is found in temperate and dry climates; thus, it is found in Egypt and the arab world. Astragalus caprinus has a good amount of bioactive chemicals, which may help explain its therapeutic effects in reducing the risk of consequences from disease.

Method: The phytochemical investigation of the herb and roots of Astragalus caprinus L. included the analytical characterization for the petroleum ether components by GC/MS, unsaponifiable matter (unsap. fraction), and fatty acids (FAME) investigation by GLC analysis. Main flavonoids were chromatographically isolated from ethyl acetate and n-butanol extracts. In vitro antimicrobial activity has been tested against the Gram-positive bacteria Staphylococcus aureus and Streptococcus mutans for different plant extracts, the Gram-negative bacteria Pseudomonas aeruginosa and Klebsiella pneumonia, the fungus Candida albicans and Aspergillus niger, and the Escherichia coli bacterium. Metabolite cytotoxicity was examined using the MTT assay against HepG-2 (human liver carcinoma) and MCF-7 (breast carcinoma).

Results: Identifying the important components of the herb and root petroleum ether extracts was achieved. Using column chromatography, luteolin, cosmosiin (apigenin-7-O-glucoside), and cynaroside (luteolin-7-O-glucoside) were separated and identified using UV, NMR, and Mass Spectroscopy. Root extracts displayed potential antimicrobial activity against most of the tested pathogens. Both extracts (herb and roots) were active against the MCF-7 cell line and HepG-2 cell line with IC50 62.5 ± 0.64 and 72.4 ± 2.3 µg/ml, and 75.9 ± 2.5 and 96.8 ± 4.2 µg/ml, respectively.

Conclusion: Astragalus caprinus seems to be a promising source of bioactive compounds that could potentially aid in preventing disease complications and address common health issues in developing countries. Moreover, the various parts of this plant could be utilized as natural raw materials for producing health-boosting products that could address common health issues in developing countries.

背景:栽培和野生植物被用来治疗不同的疾病。黄芪属植物生长在温带和干燥的气候条件下,因此在埃及和阿拉伯世界都有分布。黄芪含有大量生物活性化学物质,这可能有助于解释其在降低疾病后果风险方面的治疗效果:对黄芪草本和根部的植物化学研究包括通过气相色谱/质谱分析石油醚成分、不皂化物(unsap.从乙酸乙酯和正丁醇提取物中色谱分离出了主要的黄酮类化合物。针对不同植物提取物的革兰氏阳性菌金黄色葡萄球菌和变异链球菌、革兰氏阴性菌铜绿假单胞菌和肺炎克雷伯氏菌、真菌白色念珠菌和黑曲霉以及大肠杆菌进行了体外抗菌活性测试。代谢物的细胞毒性采用 MTT 法对 HepG-2(人肝癌)和 MCF-7(乳腺癌)进行检测:结果:确定了草药和根石油醚提取物的重要成分。通过柱层析法,分离出了叶黄素、波斯菊苷(芹菜素-7-O-葡萄糖苷)和胭脂虫苷(叶黄素-7-O-葡萄糖苷),并利用紫外光谱、核磁共振和质谱进行了鉴定。根提取物对大多数测试病原体具有潜在的抗菌活性。两种提取物(草本和根茎)对 MCF-7 细胞系和 HepG-2 细胞系均有活性,IC50 分别为 62.5 ± 0.64 和 72.4 ± 2.3 µg/ml 以及 75.9 ± 2.5 和 96.8 ± 4.2 µg/ml:黄芪似乎是一种很有前景的生物活性化合物来源,有可能有助于预防疾病并发症和解决发展中国家的常见健康问题。此外,这种植物的各个部分可作为天然原料用于生产促进健康的产品,从而解决发展中国家常见的健康问题。
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引用次数: 0
Exploring the pharmacological potential of Lepionurus sylvestris blume: from folklore medicinal usage to modern drug development strategies using in vitro and in silico analyses. 利用体外和硅学分析探索鳞茎叶的药理潜力:从民间药用到现代药物开发战略。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-07-30 DOI: 10.1186/s12906-024-04567-2
Laldinfeli Ralte, Hmingremhlua Sailo, Nachimathu Senthil Kumar, Y Tunginba Singh

Background: Lepionurus sylvestris Blume has a long history of folklore medicinal usage against various ailments. However, studies on these plants were neglected particularly their pharmacological potential.

Methods: The crude extract was identified using LC-MS analysis. In vitro assays were carried out to determine the properties of antioxidant, anti-microbial, and anti-cancer. Further, network pharmacology was proposed to evaluate the potential targets of the compounds against breast cancer and type II diabetes. Molecular docking and molecular dynamic simulation were used to determine the potential compounds for the drug formulation of diabetes.

Results: Various bioactive compounds were identfied using LC-MS and Galiposin, Fujikinetin, Boeravinone B, 4-Deoxybryaquinone, and Norbaeocystin were described for the first time from the plant. Determination of antioxidant potential showed that the IC50 value of ABTS, DPPH, and phosphomolybdate was 24.33 µg/ml, 37.81 µg/ml, 60.35 µg/ml, and reducing power assays 1.185. The antibacterial activity against Streptococcus pyogenes, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli was determined, and the minimum inhibition concentration (MIC) was found to be 5.3 mg/ml, 3.47 mg/ml, 3.33 mg/ml, and 2.7 mg/ml respectively, revealing the extracts as effective antibacterial agents. The IC50 values for the plant extract were determined to be 26 µg/ml, 30.52 µg/ml, and 24.39 µg/ml for HeLa, MCF-7, and K-562 cells, respectively, and the increasing concentration of the plant extract increased LDH release. Furthermore, the in silico network pharmacology, molecular docking which had the highest docking score for GAPDH and HIF-1 target proteins of -9.3 kcal/mol, and - 11.3 kcal/mol binding affinities, and molecular dynamic simulation analysis revealed the bioactive compound Boeravinone B present in the plant was significant for the treatment of various ailments.

Conclusion: Based on our findings, plant extracts could be a promising option for developing new drug formulations.

背景介绍Lepionurus sylvestris Blume 有着悠久的民间药用历史,可用于治疗各种疾病。然而,对这些植物的研究却被忽视了,尤其是对其药理潜力的研究:方法:使用 LC-MS 分析鉴定粗提取物。方法:采用 LC-MS 分析法对粗提取物进行鉴定,并进行体外试验以确定其抗氧化、抗微生物和抗癌特性。此外,还提出了网络药理学,以评估化合物对乳腺癌和 II 型糖尿病的潜在靶点。分子对接和分子动态模拟被用来确定糖尿病药物制剂的潜在化合物:利用 LC-MS 鉴定了多种生物活性化合物,首次从该植物中发现了 Galiposin、Fujikinetin、Boeravinone B、4-Deoxybryaquinone 和 Norbaeocystin。抗氧化潜力测定显示,ABTS、DPPH 和磷钼酸盐的 IC50 值分别为 24.33 µg/ml、37.81 µg/ml、60.35 µg/ml,还原力测定为 1.185。测定了植物提取物对化脓性链球菌、金黄色葡萄球菌、绿脓杆菌和大肠杆菌的抗菌活性,发现最低抑菌浓度(MIC)分别为 5.3 毫克/毫升、3.47 毫克/毫升、3.33 毫克/毫升和 2.7 毫克/毫升,表明这些提取物是有效的抗菌剂。经测定,植物提取物对 HeLa、MCF-7 和 K-562 细胞的 IC50 值分别为 26 微克/毫升、30.52 微克/毫升和 24.39 微克/毫升,并且随着植物提取物浓度的增加,LDH 释放量也增加。此外,硅学网络药理学、分子对接(对 GAPDH 和 HIF-1 靶蛋白的对接得分最高,分别为 -9.3 kcal/mol 和 -11.3 kcal/mol 结合亲和力)和分子动态模拟分析表明,该植物中的生物活性化合物 Boeravinone B 对治疗各种疾病有显著效果:根据我们的研究结果,植物提取物是开发新药物制剂的一个很有前景的选择。
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引用次数: 0
Efficacy of Traditional Chinese Medicine Combined Online Group Psychotherapy (TCM-eRhab) on improving quality of life and relieving psychological burden for colorectal cancer survivors: a study protocol for a phase-II randomized controlled trial. 中医药联合在线团体心理治疗(TCM-eRhab)对提高结直肠癌幸存者生活质量和减轻心理负担的疗效:II期随机对照试验的研究方案。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-07-30 DOI: 10.1186/s12906-024-04533-y
Yunzi Yan, Jiaxi Liu, Ying Pang, Zixu Wang, Rongyan Peng, Demei Jiang, Yufei Yang, Lili Tang, Lingyun Sun

Background: More than 50% of colorectal cancer(CRC) patients experience cancer-related psychological burden after radical surgery, which can seriously affect their physical wellness, quality of life and even survival outcomes. Our research team developed a six-week Traditional Chinese Medicine Combined Online Group Psychotherapy (TCM-eRhab) and proved its efficacy on relieving cancer-related anxiety, depression and fear of cancer recurrence though phase I single arm clinical trial (n = 40). Large sample size randomized controlled clinical trial(RCT) is necessary to further evaluate TCM-eRhab's role on improving quality of life and survival outcomes among this population.

Methods: We design a phase II RCT study, in which 210 CRC patients who have received radical surgery (stage I-III) will be recruited. Eligible patients will be randomly assigned to TCM-eRhab group or usual care group by 2:1 ratio. Patients in the intervention group will receive the structured TCM-eRhab program for six weeks, while patients in control group will receive usual care only. The primary outcomes are quality of life, severity of anxiety, depression and fear of cancer recurrence. Cancer recurrence rate will also be calculated according to long term follow-up data.

Discussion: As one of the first RCTs to evaluate the impacts of TCM combined psychological therapy to improve CRC patients' quality of life after surgery, the results from this study will provide innovative knowledge and evidence on integrating TCM into CRC survivorship care and mind-body intervention model.

背景50%以上的结直肠癌(CRC)患者在根治术后会出现与癌症相关的心理负担,这会严重影响他们的身体健康、生活质量甚至生存结果。我们的研究团队开发了一种为期六周的中医药联合在线团体心理疗法(TCM-eRhab),并通过一期单臂临床试验(n = 40)证明了其在缓解癌症相关焦虑、抑郁和癌症复发恐惧方面的疗效。有必要进行大样本量随机对照临床试验(RCT),以进一步评估中医康复疗法在改善该人群生活质量和生存结果方面的作用:我们设计了一项 II 期 RCT 研究,将招募 210 名接受过根治性手术(I-III 期)的 CRC 患者。符合条件的患者将按 2:1 的比例随机分配到中医康复治疗组或常规护理组。干预组患者将接受为期六周的结构化中医康复治疗,而对照组患者则只接受常规护理。主要结果包括生活质量、焦虑、抑郁的严重程度以及对癌症复发的恐惧。癌症复发率也将根据长期随访数据进行计算:作为首批评估中医结合心理疗法对改善 CRC 患者术后生活质量影响的 RCT 研究之一,本研究的结果将为将中医融入 CRC 幸存者护理和身心干预模式提供创新性的知识和证据。
{"title":"Efficacy of Traditional Chinese Medicine Combined Online Group Psychotherapy (TCM-eRhab) on improving quality of life and relieving psychological burden for colorectal cancer survivors: a study protocol for a phase-II randomized controlled trial.","authors":"Yunzi Yan, Jiaxi Liu, Ying Pang, Zixu Wang, Rongyan Peng, Demei Jiang, Yufei Yang, Lili Tang, Lingyun Sun","doi":"10.1186/s12906-024-04533-y","DOIUrl":"10.1186/s12906-024-04533-y","url":null,"abstract":"<p><strong>Background: </strong>More than 50% of colorectal cancer(CRC) patients experience cancer-related psychological burden after radical surgery, which can seriously affect their physical wellness, quality of life and even survival outcomes. Our research team developed a six-week Traditional Chinese Medicine Combined Online Group Psychotherapy (TCM-eRhab) and proved its efficacy on relieving cancer-related anxiety, depression and fear of cancer recurrence though phase I single arm clinical trial (n = 40). Large sample size randomized controlled clinical trial(RCT) is necessary to further evaluate TCM-eRhab's role on improving quality of life and survival outcomes among this population.</p><p><strong>Methods: </strong>We design a phase II RCT study, in which 210 CRC patients who have received radical surgery (stage I-III) will be recruited. Eligible patients will be randomly assigned to TCM-eRhab group or usual care group by 2:1 ratio. Patients in the intervention group will receive the structured TCM-eRhab program for six weeks, while patients in control group will receive usual care only. The primary outcomes are quality of life, severity of anxiety, depression and fear of cancer recurrence. Cancer recurrence rate will also be calculated according to long term follow-up data.</p><p><strong>Discussion: </strong>As one of the first RCTs to evaluate the impacts of TCM combined psychological therapy to improve CRC patients' quality of life after surgery, the results from this study will provide innovative knowledge and evidence on integrating TCM into CRC survivorship care and mind-body intervention model.</p>","PeriodicalId":9128,"journal":{"name":"BMC Complementary Medicine and Therapies","volume":null,"pages":null},"PeriodicalIF":3.3,"publicationDate":"2024-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11290286/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141854782","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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
Traditional Chinese medicine for sjögren's syndrome: a national survey of attitudes and perceptions among Chinese patients and rheumatologists. 中药治疗sjögren's综合征:对中国患者和风湿病医生的态度和看法的全国性调查。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-07-30 DOI: 10.1186/s12906-024-04591-2
Ruihua Liu, Zilin Guo, Haodong Xu, Jing He, Bei Wang, Yuebo Jin, Ziying Zhao, Xiaopo Tang, Xinyao Zhou

Background: This study explored similarities and differences among Chinese patients and rheumatologists in their attitudes towards and perceptions of traditional Chinese medicine (TCM) for Sjögren's syndrome (SS), including analyzing factors that influenced their decision making.

Methods: An anonymous questionnaire was used to conduct a multicenter survey among patients with SS at three tertiary care medical centers in Beijing and among rheumatology clinicians at several hospitals across China. Results were analyzed using descriptive statistics.

Results: There were 942 valid questionnaires from patients from 31 provinces and cities in China, with a male-to-female ratio of approximately 1:14, a mean age of 48.81 years, and a median disease duration of 7 (4, 10) years. There were 320 valid questionnaires from rheumatologists, covering 30 provinces and cities in China, with a male-to-female ratio of approximately 0.87:1, a mean age of 48 years, and a median work duration of 10.5 (6, 15) years. The rheumatologists treated a median of 15 (11, 50) SS cases per month, and the median proportion of SS to all rheumatic diseases was 6.66% (6-10%). Many patients believed TCM could cure the root of the disease, and the most expected TCM therapies were TCM patent prescriptions and medicinal teas. Conversely, rheumatologists placed high value on the efficacy of TCM, and most commonly prescribed Chinese herbal decoctions. Most doctor-patient groups were positive about TCM treatment, citing the low side effects as the major advantage. Regression analysis showed that for patients over 40 years old with a course of disease > 4 years, the probability of using TCM has increased by 1-6 times; the probability of recommending TCM in clinical work of doctors who have worked for more than 15 years, TCM and integrated traditional Chinese and western medicine has increased 1-2 times.

Conclusions: TCM has become widely accepted and earned attention from doctor-patient groups, especially among older patients and experienced rheumatologists. However, negative prejudices and absence of accurate information about TCM treatments and SS itself require improvement. The contradiction between TCM dosage form and efficacy is a major problem, and patient demand for convenient and efficient TCM patent preparations suggests future work should focus on developing TCM patent preparations with clear compositions and mechanisms.

背景:本研究探讨了中国患者和风湿免疫科医生对中药治疗斯约格伦综合征(SS)的态度和认识的异同,包括分析影响其决策的因素:方法:采用匿名问卷对北京三家三级医疗中心的 Sjögren's 综合征患者和全国多家医院的风湿病临床医生进行了一次多中心调查。调查结果采用描述性统计方法进行分析:来自全国 31 个省市的 942 份有效问卷,男女比例约为 1:14,平均年龄为 48.81 岁,中位病程为 7(4,10)年。风湿免疫科医生的有效问卷有 320 份,覆盖中国 30 个省市,男女比例约为 0.87:1,平均年龄为 48 岁,中位病程为 10.5(6-15)年。风湿免疫科医生每月治疗的 SS 病例中位数为 15(11,50)例,SS 在所有风湿病中所占比例中位数为 6.66%(6-10%)。许多患者认为中医可以根治疾病,最期待的中医疗法是中成药方和药茶。相反,风湿免疫科医生非常重视中医药的疗效,最常开的处方是中药煎剂。大多数医患群体对中医治疗持肯定态度,认为副作用小是中医治疗的主要优势。回归分析表明,40 岁以上、病程大于 4 年的患者使用中医药的概率增加了 1-6 倍;工作 15 年以上的医生在临床工作中推荐中医药、中医药和中西医结合治疗的概率增加了 1-2 倍:结论:中医药已被广泛接受,并赢得了医患群体的关注,尤其是老年患者和经验丰富的风湿免疫科医生。结论:中医药已被医患群体广泛接受并受到重视,尤其是在老年患者和有经验的风湿病医生中。中药剂型与疗效之间的矛盾是一个主要问题,患者对方便、高效的中成药制剂的需求表明,今后的工作重点应放在开发成分和机理明确的中成药制剂上。
{"title":"Traditional Chinese medicine for sjögren's syndrome: a national survey of attitudes and perceptions among Chinese patients and rheumatologists.","authors":"Ruihua Liu, Zilin Guo, Haodong Xu, Jing He, Bei Wang, Yuebo Jin, Ziying Zhao, Xiaopo Tang, Xinyao Zhou","doi":"10.1186/s12906-024-04591-2","DOIUrl":"10.1186/s12906-024-04591-2","url":null,"abstract":"<p><strong>Background: </strong>This study explored similarities and differences among Chinese patients and rheumatologists in their attitudes towards and perceptions of traditional Chinese medicine (TCM) for Sjögren's syndrome (SS), including analyzing factors that influenced their decision making.</p><p><strong>Methods: </strong>An anonymous questionnaire was used to conduct a multicenter survey among patients with SS at three tertiary care medical centers in Beijing and among rheumatology clinicians at several hospitals across China. Results were analyzed using descriptive statistics.</p><p><strong>Results: </strong>There were 942 valid questionnaires from patients from 31 provinces and cities in China, with a male-to-female ratio of approximately 1:14, a mean age of 48.81 years, and a median disease duration of 7 (4, 10) years. There were 320 valid questionnaires from rheumatologists, covering 30 provinces and cities in China, with a male-to-female ratio of approximately 0.87:1, a mean age of 48 years, and a median work duration of 10.5 (6, 15) years. The rheumatologists treated a median of 15 (11, 50) SS cases per month, and the median proportion of SS to all rheumatic diseases was 6.66% (6-10%). Many patients believed TCM could cure the root of the disease, and the most expected TCM therapies were TCM patent prescriptions and medicinal teas. Conversely, rheumatologists placed high value on the efficacy of TCM, and most commonly prescribed Chinese herbal decoctions. Most doctor-patient groups were positive about TCM treatment, citing the low side effects as the major advantage. Regression analysis showed that for patients over 40 years old with a course of disease > 4 years, the probability of using TCM has increased by 1-6 times; the probability of recommending TCM in clinical work of doctors who have worked for more than 15 years, TCM and integrated traditional Chinese and western medicine has increased 1-2 times.</p><p><strong>Conclusions: </strong>TCM has become widely accepted and earned attention from doctor-patient groups, especially among older patients and experienced rheumatologists. However, negative prejudices and absence of accurate information about TCM treatments and SS itself require improvement. The contradiction between TCM dosage form and efficacy is a major problem, and patient demand for convenient and efficient TCM patent preparations suggests future work should focus on developing TCM patent preparations with clear compositions and mechanisms.</p>","PeriodicalId":9128,"journal":{"name":"BMC Complementary Medicine and Therapies","volume":null,"pages":null},"PeriodicalIF":3.3,"publicationDate":"2024-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11290160/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141854784","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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
Efficacy and safety of transcutaneous auricular vagus nerve stimulation for frequent premature ventricular complexes: rationale and design of the TASC-V trial. 经皮耳廓迷走神经刺激治疗频发室性早搏的有效性和安全性:TASC-V 试验的原理和设计。
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-07-29 DOI: 10.1186/s12906-024-04568-1
Yu Liu, Xinyao Wei, Lixin Wang, Yanling Yang, Liya Xu, Tianheng Sun, Li Yang, Song Cai, Xiaojie Liu, Zongshi Qin, Lulu Bin, Shaoxin Sun, Yao Lu, Jiaming Cui, Zhishun Liu, Jiani Wu

Background: Premature Ventricular Complexes (PVCs) are very common in clinical practice, with frequent PVCs (more than 30 beats per hour) or polymorphic PVCs significantly increasing the risk of mortality. Previous studies have shown that vagus nerve stimulation improves ventricular arrhythmias. Stimulation of the auricular distribution of the vagus nerve has proven to be a simple, safe, and effective method to activate the vagus nerve. Transcutaneous au ricular vagus nerve stimulation (taVNS) has shown promise in both clinical and experimental setting for PVCs; however, high-quality clinical studies are lacking, resulting in insufficient evidence of efficacy.

Methods: The study is a prospective, randomized, parallel-controlled trial with a 1:1 ratio between the two groups. Patients will be randomized to either the treatment group (taVNS) or the control group (Sham-taVNS) with a 6-week treatment and a subsequent 12-week follow-up period. The primary outcome is the proportion of patients with a ≥ 50% reduction in the number of PVCs monitored by 24-hour Holter. Secondary outcomes include the proportion of patients with a ≥ 75% reduction in PVCs, as well as the changes in premature ventricular beats, total heartbeats, and supraventricular premature beats recorded by 24-hour Holter. Additional assessments compared score changes in PVCs-related symptoms, as well as the score change of self-rating anxiety scale (SAS), self-rating depression scale (SDS), and 36-item short form health survey (SF-36).

Discussion: The TASC-V trial will help to reveal the efficacy and safety of taVNS for frequent PVCs, offering new clinical evidence for the clinical practice.

Trial registration: Clinicaltrials.gov: NCT04415203 (Registration Date: May 30, 2020).

背景:室性早搏(PVC)在临床上非常常见,频繁的室性早搏(每小时超过 30 次)或多形性室性早搏会显著增加死亡风险。以往的研究表明,刺激迷走神经可改善室性心律失常。事实证明,刺激迷走神经的耳廓分布是一种简单、安全、有效的迷走神经激活方法。经皮耳廓迷走神经刺激(taVNS)在临床和实验中都显示出治疗 PVC 的前景,但目前缺乏高质量的临床研究,因此疗效证据不足:本研究是一项前瞻性、随机、平行对照试验,两组比例为 1:1。患者将被随机分配到治疗组(taVNS)或对照组(Sham-taVNS),治疗为期 6 周,随后进行为期 12 周的随访。主要结果是 24 小时 Holter 监测到的 PVCs 数量减少≥50% 的患者比例。次要结果包括 PVC 减少≥ 75% 的患者比例,以及 24 小时 Holter 记录的室性早搏、总心跳和室上性早搏的变化。其他评估还比较了PVC相关症状的评分变化,以及焦虑自评量表(SAS)、抑郁自评量表(SDS)和36项简表健康调查(SF-36)的评分变化:讨论:TASC-V试验将有助于揭示taVNS治疗频繁PVC的有效性和安全性,为临床实践提供新的临床证据:试验注册:Clinicaltrials.gov:试验注册:Clinicaltrials.gov:NCT04415203(注册日期:2020年5月30日)。
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引用次数: 0
Chemopreventive effect of modified zeng-sheng-ping on oral squamous cell carcinoma by regulating tumor associated macrophages through targeting tnf alpha induced protein 6. 改良增生平通过靶向 tnf alpha 诱导蛋白 6 调节肿瘤相关巨噬细胞对口腔鳞状细胞癌的化学预防作用
IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2024-07-27 DOI: 10.1186/s12906-024-04593-0
Jiaqi Wang, Feiran Lin, Yongxiang Zhou, Yuyi Cong, Sen Yang, Sujuan Wang, Xiaobing Guan

Background: Oral squamous cell carcinoma (OSCC) is the most common malignancy of the head and neck. Zeng-Sheng-Ping, composed of Sophora tonkinensis Gagnep., Bistorta officinalis Delarbre, Sonchus arvensis L., Prunella vulgaris L., Dioscorea bulbifera L., and Dictamnus dasycarpus Turcz., was regarded as an anti-cancer drug with significant clinical efficacy, but was discontinued due to liver toxicity. Our research group developed a modified Zeng-Sheng-Ping (ZSP-M) based on original Zeng-Sheng-Ping that exhibited high efficiency and low toxicity in preliminary investigations, although its pharmacodynamic mechanism is still unclear. Here, we aimed to elucidate the pharmacodynamic material basis of ZSP-M and investigate its chemopreventive effect on OSCC by modulating tumor associated macrophages (TAMs).

Methods: Components of ZSP-M were characterized using ultra-performance liquid chromatography-mass spectrometry. Chemopreventive effect induced by ZSP-M against experimental oral cancer was investigated using the 4-nitroquinoline N-oxide precancerous lesion mouse model. RNA sequencing analysis was used to gain a global transcriptional view of the effect of ZSP-M treatment. A cell co-culture model was used to study the targeted effect of ZSP-M on TAMs and the biological properties of OSCC cells and to detect changes in TAM phenotypes. The binding of ZSP-M active compounds to TNF alpha induced protein 6 (TNFAIP6) protein was analyzed by molecular docking and dynamic simulation.

Results: Forty main components of ZSP-M were identified, the most abundant of which were flavonoids. ZSP-M inhibited the degree of epithelial dysplasia in precancerous lesions by inhibiting the expression of the TNFAIP6 and CD163 proteins in the precancerous lesions of the tongue. ZSP-M inhibited proliferation, colony formation, migration and invasion of SCC7 cells by targeting TAMs. ZSP-M reduced the expression of CD163+ cells, inhibited the expression of TNFAIP6 protein, Arg1 mRNA and Il10 mRNA in TAMs, and reduced IL-10 cytokine release in the co-culture environment. This effect was maintained after the addition of recombinant TNFAIP6 protein. Computer simulations showed that trifolirhizin and maackiain are well-connected to TNFAIP6.

Conclusions: ZSP-M counteracts the immunosuppressive action of TAMs by specific targeting of TNFAIP6, thereby exerting chemopreventive activity of OSCC.

背景:口腔鳞状细胞癌(OSCC口腔鳞状细胞癌(OSCC)是头颈部最常见的恶性肿瘤。曾生平(Sophora tonkinensis Gagnep.、Bistorta officinalis Delarbre.、Sonchus arvensis L.、Prunella vulgaris L.、Dioscorea bulbifera L.、Dictamnus dasycarpus Turcz.)被认为是一种临床疗效显著的抗癌药物,但因肝毒性而停用。我们的研究小组在原增生平的基础上开发了一种改良增生平(ZSP-M),在初步研究中表现出高效、低毒的特点,但其药效学机制仍不清楚。在此,我们旨在阐明ZSP-M的药效学物质基础,并研究其通过调节肿瘤相关巨噬细胞(TAMs)对OSCC的化学预防作用:方法:采用超高效液相色谱-质谱法对ZSP-M的成分进行表征。采用4-硝基喹啉N-氧化物癌前病变小鼠模型研究了ZSP-M对实验性口腔癌的化学预防作用。利用 RNA 测序分析获得了 ZSP-M 治疗效果的全局转录视图。利用细胞共培养模型研究了ZSP-M对TAMs的靶向效应和OSCC细胞的生物特性,并检测了TAM表型的变化。通过分子对接和动态模拟分析了ZSP-M活性化合物与TNFα诱导蛋白6(TNFAIP6)蛋白的结合:结果:鉴定出ZSP-M的40种主要成分,其中含量最高的是黄酮类化合物。ZSP-M通过抑制TNFAIP6和CD163蛋白在舌癌前病变中的表达,抑制了癌前病变的上皮发育不良程度。ZSP-M 通过靶向 TAMs 抑制了 SCC7 细胞的增殖、集落形成、迁移和侵袭。ZSP-M 降低了 CD163+ 细胞的表达,抑制了 TAMs 中 TNFAIP6 蛋白、Arg1 mRNA 和 Il10 mRNA 的表达,并减少了共培养环境中 IL-10 细胞因子的释放。加入重组 TNFAIP6 蛋白后,这种效果仍能保持。计算机模拟显示,三唑醇和马钱子碱与 TNFAIP6 关系密切:结论:ZSP-M通过特异性靶向TNFAIP6来对抗TAMs的免疫抑制作用,从而发挥对OSCC的化学预防活性。
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BMC Complementary Medicine and Therapies
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