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Plumbagin Attenuates Ovalbumin-induced Allergic Asthma in Mice through Inhibition of Inflammatory Response 白桦素通过抑制炎症反应减轻卵清蛋白诱导的小鼠过敏性哮喘
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-11-03 DOI: 10.1177/09731296231184537
Dong Yiming, Abdullah R Alzahrani, Abubucker Peer Mohideen
Background Asthma is a prominent non-communicable inflammatory disease that affects both children and the elderly. Younger people are more prone to asthma, and most prescribed anti-asthmatic medicines relieve symptoms but do not cure the condition completely. We investigated the ability of a phytochemical plumbagin to alleviate ovalbumin (OVA)-induced asthma in BALB/c mice. Materials and Methods The allergic asthma-induced mice were treated with two different doses of 25 and 50 mg/kg bwt plumbagin, and to compare the efficacy of plumbagin, a standard drug dexamethasone treatment was given. OVA-specific IgE and eotaxin were quantified to determine the induction of asthma and the inhibitory role of plumbagin. Total leukocyte and differential count were done to assess the effect of plumbagin on inflammatory cells. Inflammatory cytokines inducing both atopic and non-atopic asthma were quantified to examine the efficacy of plumbagin against allergic and non-allergic-induced asthma. Nitric oxide (NO) and myeloperoxidase activity were measured to investigate the anti-asthmatic potential of plumbagin. The antioxidant potency of plumbagin was assessed by quantifying the levels of antioxidants and the oxidative stress marker malondialdehyde. Lung weight index and histopathological analysis of lung tissue were done to confirm the ameliorative potency of plumbagin against OVA allergen-induced asthma. Results Plumbagin treatment significantly decreased the status of OVA-specific IgE and eotaxin, thereby prevented the eosinophilic infiltration. It also inhibited the synthesis of both atopic and non-atopic inducing inflammatory cytokines. Plumbagin treatment also increased the levels of antioxidants and prevented the lung tissue damage, which was evidenced with our histopathology study of lung tissue. Conclusion Overall, our finding confirms that plumbagin is persuasively alleviated OVA allergen-induced asthma complications in mice model and may be an alternative for currently available anti-asthmatic drugs.
哮喘是一种影响儿童和老年人的非传染性炎症性疾病。年轻人更容易患哮喘,大多数处方的抗哮喘药物可以缓解症状,但不能完全治愈病情。我们研究了一种植物化学物质白桦素缓解BALB/c小鼠卵清蛋白(OVA)诱导的哮喘的能力。材料与方法分别给予25、50 mg/kg bwt不同剂量的白丹素治疗过敏性哮喘小鼠,并以标准药物地塞米松治疗白丹素,比较其疗效。测定ova特异性IgE和eotaxin对哮喘的诱导作用和白桦素的抑制作用。用白细胞总数和差异计数来评估白桦素对炎症细胞的影响。对诱导特应性和非特应性哮喘的炎症细胞因子进行量化,以检验白桦素对过敏性和非过敏性哮喘的疗效。通过测定一氧化氮(NO)和髓过氧化物酶活性来研究白桦素的抗哮喘作用。通过定量测定抗氧化剂和氧化应激标志物丙二醛的水平来评估白桦素的抗氧化能力。肺重指数和肺组织病理分析证实白桦素对OVA变应原诱导哮喘的改善作用。结果白桦素可显著降低ova特异性IgE和eotaxin水平,从而抑制嗜酸性粒细胞的浸润。它还抑制了特应性和非特应性诱导炎症细胞因子的合成。我们对肺组织的组织病理学研究证明,白桦苷处理还能提高抗氧化剂水平,防止肺组织损伤。综上所述,我们的研究结果证实了白桦白素有减轻OVA过敏原诱导的小鼠哮喘并发症的作用,可能是现有抗哮喘药物的替代方案。
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引用次数: 0
Rhapontigenin Improves Non-alcoholic Fatty Liver Disease by Inducing Lipophagy Through the ACOX1 and mTOR/ULK1 Pathways Rhapontigenin通过ACOX1和mTOR/ULK1途径诱导脂肪吞噬改善非酒精性脂肪性肝病
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-11-03 DOI: 10.1177/09731296231197299
Ying-Xiao Wang, Xin-Ge Ke, Chen Wang, Kang-Bo Peng, He-Zhen Wu, Yan-Fang Yang
Background Non-alcoholic fatty liver disease (NAFLD) is severely affecting the quality of people’s life. Rhapontigenin (RA) is a stilbene compound isolated from Rhubarb L., which has been reported to have an effect on cholesterol diet-induced hyperlipidemia in rats. This study aims to explore the pharmacodynamics and the mechanism of RA obtained from Rheum franzenbachii Munt. against NAFLD. RA was extracted from the roots of the Rheum L. (Polygonaceae) plant Rheum franzenbachii Munt. Materials and Methods RA was extracted by Sephadex-gel column and identified by high-performance liquid chromatography (HPLC)-UV and HR-ESI-MS. The pharmacodynamic indexes of L-02 cells and mice treated with RA were determined by histological staining and ELISA, while the expression of autophagy-related proteins was analyzed by Western blot. Results The results in vivo showed that the liver structure of RA-treatment mice was normal, and the organ coefficient was significantly decreased. It also showed that RA could significantly reduce the expression of reactive oxygen species (ROS) in the liver as well as inhibit oxidative stress and inflammatory response. Interestingly, the autophagy inhibitor 3-methyladenine (3-MA) could reverse the effect of RA on NAFLD, which further confirmed that RA plays an anti-NAFLD role through activating lipophagy. Conclusion It suggested that RA has an effect on NAFLD by down-regulating the expression of Acyl-CoA oxidase 1 (ACOX1), p-mTOR, and p-Unc-51-like kinase 1 (ULK1), then inhibiting Acetyl-CoA (A-CoA) production, and up-regulating the expression of autophagy protein 5 (Atg5) to promote the lipophagy of lipocytes.
背景非酒精性脂肪性肝病(NAFLD)严重影响着人们的生活质量。Rhapontigenin (RA)是一种从大黄中分离出来的二苯乙烯类化合物,据报道对胆固醇饮食诱导的大鼠高脂血症有影响。本研究旨在探讨大黄类风湿性关节炎的药效学及作用机制。对非酒精性脂肪肝。RA是从蓼科植物大黄(Rheum L.)的根中提取的。材料与方法采用Sephadex-gel柱提取RA,并采用高效液相色谱(HPLC)-UV和HR-ESI-MS进行鉴定。采用组织学染色和酶联免疫吸附法检测L-02细胞及RA小鼠的药效学指标,Western blot检测自噬相关蛋白的表达。结果体内实验结果显示,ra处理小鼠肝脏结构正常,脏器系数明显降低。RA能显著降低肝脏活性氧(ROS)的表达,抑制氧化应激和炎症反应。有趣的是,自噬抑制剂3-甲基腺嘌呤(3-MA)可以逆转RA对NAFLD的作用,进一步证实RA通过激活脂噬发挥抗NAFLD作用。结论RA通过下调Acyl-CoA氧化酶1 (ACOX1)、p-mTOR和p- unc -51样激酶1 (ULK1)的表达,抑制乙酰辅酶a (A-CoA)的产生,上调自噬蛋白5 (Atg5)的表达,促进脂肪细胞的脂噬,从而对NAFLD产生影响。
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引用次数: 0
Comparative Chemical Profiling of a Polyherbal Formulation with Respect to its Ingredient Plants Using Spectrophotometric and High-performance Thin-layer Chromatographic Techniques 用分光光度法和高效薄层色谱技术比较复方成分的化学谱图
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-11-02 DOI: 10.1177/09731296231200365
Cheruthazhakkat Sulaiman, Thankayathil Shafna, Geetha Raguthaman Advaya, Poovathusseri Raghava Varier Ramesh, Kamalakshan Pillai Mahesh, Mooriath Praveen, Erayur Mana Anandan, Indira Balachandran
Background Guggulutiktam Kashayam (GTK) is a water decoction used in Ayurveda for the treatment of various diseases like skin diseases, ulcers, anemia, thyroid problems, stress, liver disease, and leucorrhoea. It is a polyherbal formulation prepared from specific parts of 28 medicinal plants. Objectives The study aimed at a comparative phytochemical evaluation of an important polyherbal formulation with its ingredient plants. Materials and Methods Chemical profiling of GTK has been carried out in comparison with its ingredient plants. Spectrophotometric estimation of major class compounds and high-performance thin-layer chromatography (HPTLC) profiling were done using a standardized protocol. Results The results of the study showed that the phytochemical contents of the finished formulation are different from those of the ingredient plants, which might be due to the numerous synergistic and antagonistic interactions of numerous chemical components extracted from different ingredient drugs. HPTLC-based comparative chromatograms showed the differences and similarities in certain compounds that are specific to some of the plant ingredients. Conclusion The study established the cumulative chemical interactions of various phytochemicals during the preparation of an important polyherbal formula used in Ayurveda.
Guggulutiktam Kashayam (GTK)是阿育吠陀中用于治疗各种疾病的水汤剂,如皮肤病,溃疡,贫血,甲状腺问题,压力,肝脏疾病和白带。它是由28种药用植物的特定部分制成的多草药制剂。目的对一种重要的中药复方及其成分植物进行比较化学评价。材料与方法对GTK进行了化学分析,并与其主要成分植物进行了比较。主要类化合物的分光光度估计和高效薄层色谱(HPTLC)分析采用标准化的方案。结果研究结果表明,制剂中植物化学成分的含量与原料药不同,这可能是由于从不同原料药中提取的多种化学成分存在多种增效和拮抗作用所致。基于hptlc的比较色谱显示了某些植物成分特有的某些化合物的差异和相似性。结论本研究建立了阿育吠陀重要复方制备过程中各种植物化学物质的累积化学相互作用。
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引用次数: 0
Metabolic and Pharmacokinetic Investigation of Ilexsaponin A1 in Normal and Antibiotic-treated Rats 异外皂苷A1在正常及抗生素治疗大鼠体内代谢及药代动力学研究
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-31 DOI: 10.1177/09731296231198608
Di Cao, Zhengjiao Wang, Xiuting Shen, Xiaojun Song, Zhongxiang Zhao
Background Ilexsaponin A 1 (IA 1 ) is a bioactive triterpene saponin derived from natural medicinal plants. IA 1 exhibits anti-inflammatory and proangiogenic activities and improves intestinal barrier function. It has been reported that IA 1 could be metabolized into a dominant metabolite, ilexgenin A (IA) by β-glucosidase enzymes in intestinal microflora. Materials and Methods Herein, an accurate, sensitive, and selective method based on ultra-performance liquid chromatography coupled with mass spectrometry was established to simultaneously profile the metabolism and pharmacokinetic behaviors of IA 1 in normal and antibiotic-treated rat plasma after intragastric administration of IA 1 . The precursor-to-product ion pairs of IA and IA 1 were m/ z 501.32↓439.32 and m/ z 663.38↓501.32, respectively. For method validation, the specificity, matrix effect, accuracy, precision, and stability of the pharmacokinetic study were measured, and a calibration curve was created. The collaborative pharmacological target pathways of IA 1 and its metabolite IA were investigated using network pharmacology tools. Results The validated analytical method was successfully utilized to investigate the pharmacokinetics of IA 1 in normal and antibiotic-treated rats. The bioavailability of IA 1 and conversion from IA 1 to IA were significantly inhibited by antibiotic-treated rats after oral administration of IA 1 . Fragment ions at m/z 483.3155, 455.3159, 439.3233, 421.3136, 395.3362, 152.9952, 113.0256, and 71.0531 were characteristic of the IA 1 moiety. IA 1 was metabolized in rat plasma by biotransformation routes involving deglycosylation, decarboxylation, isomerization, hydrogenation, dehydrogenation, and oxidation. Considering database analysis, IA and IA 1 play synergistic role in common pharmacological pathways, such as hypertrophic cardiomyopathy and dilated cardiomyopathy. Conclusion The experiments illustrated that β-glucosidase activity inhibited by antibiotics suppressed the hydrolysis reaction of IA 1 in the intestinal tract. IA 1 and IA play a synergistic role in exerting effects.
Ilexsaponin a1 (ia1)是从天然药用植物中提取的具有生物活性的三萜皂苷。IA 1具有抗炎和促血管生成活性,改善肠道屏障功能。据报道,肠道菌群中的β-葡萄糖苷酶可将ia1代谢为优势代谢物ilexgenin a (IA)。材料与方法本研究建立了一种基于超高效液相色谱-质谱联用的准确、灵敏、选择性的方法,用于同时测定正常和抗生素治疗大鼠灌胃IA 1后血浆中IA 1的代谢和药代动力学行为。IA和IA 1的前驱物-产物离子对分别为m/ z 501.32↓439.32和m/ z 663.38↓501.32。为验证方法,测定了药代动力学研究的特异性、基质效应、准确度、精密度和稳定性,并建立了校准曲线。利用网络药理学工具研究了IA 1及其代谢物IA的协同药理靶点通路。结果本方法可用于正常大鼠和抗生素治疗大鼠体内IA - 1的药动学研究。经抗生素处理的大鼠口服IA 1后,IA 1的生物利用度和IA 1向IA的转化明显受到抑制。在m/z 483.3155、455.3159、439.3233、421.3136、395.3362、152.9952、113.0256和71.0531处的碎片离子是IA 1片段的特征离子。IA 1在大鼠血浆中通过生物转化途径代谢,包括去糖基化、脱羧化、异构化、氢化、脱氢和氧化。结合数据库分析,IA和IA 1在肥厚型心肌病、扩张型心肌病等常见药理通路中发挥协同作用。结论抗生素抑制β-葡萄糖苷酶活性可抑制肠道IA 1的水解反应。IA 1与IA协同发挥作用。
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引用次数: 0
A Novel Tumor Glycolysis Inhibitor: 4-Methylumbelliferone 一种新的肿瘤糖酵解抑制剂:4- methylumbellliferone
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-31 DOI: 10.1177/09731296231206300
Zi-Yao Li, Qin Yang, Xiao-Ge Cheng, Yan-Li Zhou, Xiang-Ling Piao, Li Qiu, Bo-Jun Zhou, Song-Tao Wu
Background and Objectives 4-Methylumbelliferone (4-MU) is a coumarin compound that can be extracted from the medicinal plant with anti-cancer properties, Smilax china L. In recent years, studies have revealed its potential as an anti-tumor and anti-metastasis drug with promising effects in cancer treatment. Despite an increase in research on the metabolic patterns of tumor cells, no prior research has suggested that 4-MU inhibits tumor proliferation by blocking glycolysis. This thesis presents evidence that 4-MU binds to proteins involved in glycolysis, thus mediating its anti-tumor effects. Materials and Methods Network pharmacology, transcriptomics, and molecular docking were utilized to forecast the potential targets and probable pathways of 4-MU’s anti-cancer activity, and the affinity of 4-MU towards potential targets was discovered using microscale thermophoresis (MST) detection. Results The results of transcriptome analysis brought to light that the genes with differential expressions were primarily enriched in metabolic pathways, including glycolysis-related proteins. Using network pharmacology and molecular docking, our study identified Heat Shock Protein 90 Alpha Family Class A Member 1 (Hsp90AA1), mitochondria, phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2), and glucose-6-phosphate isomerase (GPI) as potential targets of 4-MU. The strong binding affinity between 4-MU and these proteins was confirmed by the MST assay. Conclusion The findings indicate that 4-MU can hinder glycolysis by binding to glycolysis-associated proteins such as Hsp90AA1, PGK2, GPD2, and GPI. This results in the prevention of the energy supply to the tumor tissue, which ultimately curbs tumor growth, thereby demonstrating its anti-tumor properties. These results conclude that 4-MU has the capacity to be a novel glycolysis inhibitor for cancer treatment. Moreover, the identification of these glycolysis-associated proteins as possible targets for cancer therapy offers new avenues for research in the field of cancer treatment, thus providing further valuable evidence for the anti-cancer mechanism of 4-MU.
背景与目的4- methylumbellliferone (4-MU)是一种从具有抗癌作用的药用植物菝葜中提取的香豆素类化合物,近年来研究表明其具有抗肿瘤和抗转移的潜力,在癌症治疗中具有良好的效果。尽管对肿瘤细胞代谢模式的研究越来越多,但之前没有研究表明4-MU通过阻断糖酵解来抑制肿瘤增殖。本文提出证据表明,4-MU与参与糖酵解的蛋白质结合,从而介导其抗肿瘤作用。材料与方法利用网络药理学、转录组学、分子对接等方法预测4-MU抗癌活性的潜在靶点和可能通路,并利用微尺度热泳术(MST)检测发现4-MU对潜在靶点的亲和力。结果转录组分析结果表明,差异表达基因主要富集于代谢途径,包括糖酵解相关蛋白。通过网络药理学和分子对接,我们的研究确定了热休克蛋白90 α家族A类成员1 (Hsp90AA1)、线粒体、磷酸甘油酸激酶2 (PGK2)、甘油-3-磷酸脱氢酶(GPD2)和葡萄糖-6-磷酸异构酶(GPI)是4-MU的潜在靶点。MST实验证实了4-MU与这些蛋白之间的强结合亲和力。结论4-MU通过与糖酵解相关蛋白Hsp90AA1、PGK2、GPD2和GPI结合而抑制糖酵解。这导致阻止肿瘤组织的能量供应,最终抑制肿瘤生长,从而显示其抗肿瘤特性。这些结果表明,4-MU有能力成为一种新的糖酵解抑制剂,用于癌症的治疗。此外,这些糖酵解相关蛋白作为癌症治疗的可能靶点,为癌症治疗领域的研究提供了新的途径,从而为4-MU的抗癌机制提供了进一步有价值的证据。
{"title":"A Novel Tumor Glycolysis Inhibitor: 4-Methylumbelliferone","authors":"Zi-Yao Li, Qin Yang, Xiao-Ge Cheng, Yan-Li Zhou, Xiang-Ling Piao, Li Qiu, Bo-Jun Zhou, Song-Tao Wu","doi":"10.1177/09731296231206300","DOIUrl":"https://doi.org/10.1177/09731296231206300","url":null,"abstract":"Background and Objectives 4-Methylumbelliferone (4-MU) is a coumarin compound that can be extracted from the medicinal plant with anti-cancer properties, Smilax china L. In recent years, studies have revealed its potential as an anti-tumor and anti-metastasis drug with promising effects in cancer treatment. Despite an increase in research on the metabolic patterns of tumor cells, no prior research has suggested that 4-MU inhibits tumor proliferation by blocking glycolysis. This thesis presents evidence that 4-MU binds to proteins involved in glycolysis, thus mediating its anti-tumor effects. Materials and Methods Network pharmacology, transcriptomics, and molecular docking were utilized to forecast the potential targets and probable pathways of 4-MU’s anti-cancer activity, and the affinity of 4-MU towards potential targets was discovered using microscale thermophoresis (MST) detection. Results The results of transcriptome analysis brought to light that the genes with differential expressions were primarily enriched in metabolic pathways, including glycolysis-related proteins. Using network pharmacology and molecular docking, our study identified Heat Shock Protein 90 Alpha Family Class A Member 1 (Hsp90AA1), mitochondria, phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2), and glucose-6-phosphate isomerase (GPI) as potential targets of 4-MU. The strong binding affinity between 4-MU and these proteins was confirmed by the MST assay. Conclusion The findings indicate that 4-MU can hinder glycolysis by binding to glycolysis-associated proteins such as Hsp90AA1, PGK2, GPD2, and GPI. This results in the prevention of the energy supply to the tumor tissue, which ultimately curbs tumor growth, thereby demonstrating its anti-tumor properties. These results conclude that 4-MU has the capacity to be a novel glycolysis inhibitor for cancer treatment. Moreover, the identification of these glycolysis-associated proteins as possible targets for cancer therapy offers new avenues for research in the field of cancer treatment, thus providing further valuable evidence for the anti-cancer mechanism of 4-MU.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"213 ","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135872448","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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 Composition, Bioavailability and Pharmacokinetics of Scorzonera undulata Methanolic Extracts: Antioxidant, Anticancer, and Apoptotic Effects on MCF7 Cells 山葵甲醇提取物的植物化学成分、生物利用度和药代动力学:对MCF7细胞的抗氧化、抗癌和凋亡作用
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-29 DOI: 10.1177/09731296231207231
Imen Bédoui, Hmed Ben Nasr, Kamilia Ksouda, Wajdi Ayadi, Nour Louati, Mohamed Chamkha, Sirine Choura, Jalel Gargouri, Serria Hammami, Hanen Affes, Walid S. Hamadou, Nourhene Zammel, Subuhi Sherwani, Khaled Zeghal, Riadh Badraoui
Background Finding new effective substances to develop drugs against cancer or to prevent it remains a big challenge facing scientists and clinicians. Objectives In such an issue, we tested the anti-tumoral effect of Scorzonera undulata extracts on MCF7 cells. Materials and Methods Methanolic extracts of S. undulata roots (RSU) and aerial parts (ASU) from the Ha’il region were analyzed by HPLC. Their DPPH scavenging, ferric-reducing antioxidant power (FRAP) and total antioxidant potentials were evaluated. The MTT test was used to determine their cytotoxic effects on MCF7 cells using different concentrations, and their potential to induce apoptosis was determined by measuring the mitochondrial transmembrane loss of potential by flow cytometry using the JC-1 fluorescent marker. Results S. undulata was found to be rich in flavonoids, tannins, and polyphenols. ASU contains great amounts of apigenin and gallic acid, whereas RSU contains luteolin and chlorogenic acid as major components. The potential to scavenge DPPH and the total antioxidant activity of ASU were twofold greater than those of RSU. MCF7 cell viability was reduced by 50% at concentrations of 4.22 ± 0.06 and 5.89 ± 0.08 mg.mL −1 , respectively, for ASU and RSU at 24 h. In addition, S. undulata extracts induced MCF7 cells’ death through cell lysis and apoptosis. Conclusion As an edible vegetable, S. undulata is worth further exploration in alternative and complementary medication as it possesses significant antioxidant and anticancer potentials.
寻找新的有效物质来开发抗癌或预防癌症的药物仍然是科学家和临床医生面临的一个巨大挑战。目的在本课题中,我们检测了蛇尾草提取物对MCF7细胞的抗肿瘤作用。材料与方法采用高效液相色谱法对哈伊勒地区山地莲根(RSU)和地皮(ASU)的甲醇提取物进行分析。对其DPPH清除能力、铁还原抗氧化能力(FRAP)和总抗氧化电位进行了评价。采用MTT法检测不同浓度下其对MCF7细胞的细胞毒作用,采用JC-1荧光标记物流式细胞术检测线粒体跨膜电位损失,测定其诱导凋亡的潜力。结果山参中含有丰富的黄酮类、单宁类和多酚类物质。ASU含有大量的芹菜素和没食子酸,而RSU含有木犀草素和绿原酸作为主要成分。ASU对DPPH的清除能力和总抗氧化活性是RSU的2倍。在浓度为4.22±0.06和5.89±0.08 mg时,MCF7细胞活力降低50%。24 h时,ASU和RSU分别为mL−1。此外,波曲参提取物通过细胞裂解和凋亡诱导MCF7细胞死亡。结论波纹草具有显著的抗氧化和抗癌作用,值得进一步开发作为一种可食用蔬菜的替代和补充药物。
{"title":"Phytochemical Composition, Bioavailability and Pharmacokinetics of <i>Scorzonera undulata</i> Methanolic Extracts: Antioxidant, Anticancer, and Apoptotic Effects on MCF7 Cells","authors":"Imen Bédoui, Hmed Ben Nasr, Kamilia Ksouda, Wajdi Ayadi, Nour Louati, Mohamed Chamkha, Sirine Choura, Jalel Gargouri, Serria Hammami, Hanen Affes, Walid S. Hamadou, Nourhene Zammel, Subuhi Sherwani, Khaled Zeghal, Riadh Badraoui","doi":"10.1177/09731296231207231","DOIUrl":"https://doi.org/10.1177/09731296231207231","url":null,"abstract":"Background Finding new effective substances to develop drugs against cancer or to prevent it remains a big challenge facing scientists and clinicians. Objectives In such an issue, we tested the anti-tumoral effect of Scorzonera undulata extracts on MCF7 cells. Materials and Methods Methanolic extracts of S. undulata roots (RSU) and aerial parts (ASU) from the Ha’il region were analyzed by HPLC. Their DPPH scavenging, ferric-reducing antioxidant power (FRAP) and total antioxidant potentials were evaluated. The MTT test was used to determine their cytotoxic effects on MCF7 cells using different concentrations, and their potential to induce apoptosis was determined by measuring the mitochondrial transmembrane loss of potential by flow cytometry using the JC-1 fluorescent marker. Results S. undulata was found to be rich in flavonoids, tannins, and polyphenols. ASU contains great amounts of apigenin and gallic acid, whereas RSU contains luteolin and chlorogenic acid as major components. The potential to scavenge DPPH and the total antioxidant activity of ASU were twofold greater than those of RSU. MCF7 cell viability was reduced by 50% at concentrations of 4.22 ± 0.06 and 5.89 ± 0.08 mg.mL −1 , respectively, for ASU and RSU at 24 h. In addition, S. undulata extracts induced MCF7 cells’ death through cell lysis and apoptosis. Conclusion As an edible vegetable, S. undulata is worth further exploration in alternative and complementary medication as it possesses significant antioxidant and anticancer potentials.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"77 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136135604","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Mutagenic, Anti-mutagenic, and Cytotoxic Activities of Methanol, Hexane, and Ethyl Acetate Extracts of Zingiber zerumbet (L.) Smith 生姜甲醇、己烷和乙酸乙酯提取物的致突变性、抗突变性和细胞毒活性史密斯
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-29 DOI: 10.1177/09731296231207226
Farah Syahibah Mohd Hariri, Asmah Hamid, Nor Fadilah Rajab
Background Zingiber zerumbet (L.) Smith (lempoyang) has a traditional application in the treatment of indigestion, worm infestation, loss of appetite, and postpartum conditions. Objectives Extracts of Z. zerumbet (methanol, hexane, and ethyl acetate) were utilized to investigate the mutagenic, anti-mutagenic, and cytotoxic properties. Materials and Methods Initially, a mutagenicity test (Ames test) was conducted, followed by an anti-mutagenicity test, to assess the potential of Z. zerumbet extracts in inhibiting mutagenicity induced by sodium azide and 9-aminoacridine. Furthermore, the cytotoxic ability of the extracts was evaluated using the methyl thiazolyl tetrazolium (MTT) assay. Results The mutagenicity assessment revealed that the methanol extract of Z. zerumbet exhibited a twofold increase in the number of revertants in Salmonella typhimurium strain TA 1537. Similar results were observed for the hexane extract, except at a concentration of 6.25 mg/mL, where no significant increase in revertants was observed. On the other hand, the ethyl acetate extract demonstrated a twofold increase in revertants in S. typhimurium strain TA 1535. Notably, the ethyl acetate extract displayed remarkable anti-mutagenic activity against 9-aminoacridine, while the hexane extract exhibited strong anti-mutagenic activity against sodium azide. Regarding cytotoxicity assessment using the MTT assay, the methanol extract of Z. zerumbet exhibited the highest cytotoxicity with an IC 50 value estimated at 388.50 ± 135.75 µg/mL. The hexane and ethyl acetate extracts showed IC 50 values of 514.17 ± 135.75 and 589.67 ± 241.67 µg/mL, respectively. Conclusion The extracts displayed both mutagenic and cytotoxic activities. However, they also exhibited promising anti-mutagenic potential, which could be harnessed for cancer prevention purposes.
Zingiber zerumbet (L.)史密斯(lempoyang)传统上用于治疗消化不良,蠕虫感染,食欲不振和产后状况。目的采用甲醇、己烷和乙酸乙酯三种提取物,研究其致突变性、抗突变性和细胞毒性。材料与方法首先进行诱变性试验(Ames试验),然后进行抗诱变性试验,评估泽兰提取物对叠氮化钠和9-氨基吖啶诱导的诱变性的抑制潜力。此外,采用甲基噻唑四氮唑(MTT)测定法评估了提取物的细胞毒能力。结果对鼠伤寒沙门菌TA 1537的致突变性进行了评价,结果表明,采珠草甲醇提取物对鼠伤寒沙门菌TA 1537的致突变性增加了2倍。在己烷提取物中也观察到类似的结果,除了浓度为6.25 mg/mL时,没有观察到明显的还原物增加。另一方面,乙酸乙酯提取物在鼠伤寒沙门氏菌ta1535中显示出两倍的反复性。乙酸乙酯提取物对9-氨基吖啶具有显著的抗诱变活性,己烷提取物对叠氮化钠具有较强的抗诱变活性。关于MTT法的细胞毒性评估,zz . zerumbet甲醇提取物显示出最高的细胞毒性,ic50值估计为388.50±135.75µg/mL。正己烷和乙酸乙酯提取物的IC 50值分别为514.17±135.75和589.67±241.67µg/mL。结论黄芪提取物具有致突变性和细胞毒活性。然而,它们也显示出有希望的抗诱变潜力,这可以用于癌症预防目的。
{"title":"Mutagenic, Anti-mutagenic, and Cytotoxic Activities of Methanol, Hexane, and Ethyl Acetate Extracts of <i>Zingiber zerumbet</i> (L.) Smith","authors":"Farah Syahibah Mohd Hariri, Asmah Hamid, Nor Fadilah Rajab","doi":"10.1177/09731296231207226","DOIUrl":"https://doi.org/10.1177/09731296231207226","url":null,"abstract":"Background Zingiber zerumbet (L.) Smith (lempoyang) has a traditional application in the treatment of indigestion, worm infestation, loss of appetite, and postpartum conditions. Objectives Extracts of Z. zerumbet (methanol, hexane, and ethyl acetate) were utilized to investigate the mutagenic, anti-mutagenic, and cytotoxic properties. Materials and Methods Initially, a mutagenicity test (Ames test) was conducted, followed by an anti-mutagenicity test, to assess the potential of Z. zerumbet extracts in inhibiting mutagenicity induced by sodium azide and 9-aminoacridine. Furthermore, the cytotoxic ability of the extracts was evaluated using the methyl thiazolyl tetrazolium (MTT) assay. Results The mutagenicity assessment revealed that the methanol extract of Z. zerumbet exhibited a twofold increase in the number of revertants in Salmonella typhimurium strain TA 1537. Similar results were observed for the hexane extract, except at a concentration of 6.25 mg/mL, where no significant increase in revertants was observed. On the other hand, the ethyl acetate extract demonstrated a twofold increase in revertants in S. typhimurium strain TA 1535. Notably, the ethyl acetate extract displayed remarkable anti-mutagenic activity against 9-aminoacridine, while the hexane extract exhibited strong anti-mutagenic activity against sodium azide. Regarding cytotoxicity assessment using the MTT assay, the methanol extract of Z. zerumbet exhibited the highest cytotoxicity with an IC 50 value estimated at 388.50 ± 135.75 µg/mL. The hexane and ethyl acetate extracts showed IC 50 values of 514.17 ± 135.75 and 589.67 ± 241.67 µg/mL, respectively. Conclusion The extracts displayed both mutagenic and cytotoxic activities. However, they also exhibited promising anti-mutagenic potential, which could be harnessed for cancer prevention purposes.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"45 7","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136135683","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Research Advancements in Pharmacological Activities and Mechanisms of Matrine 苦参碱的药理活性及其作用机制研究进展
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-27 DOI: 10.1177/09731296231203458
Xiaohui Chen, Panpan Liu, Yanni Mao, Guiqin Wang
Matrine possesses a broad spectrum of pharmacological activities as one of the primary components of Chinese herbal medicine Sophora flavescens extract, along with fewer side effects and low toxicity. Matrine possesses anti-inflammatory, anti-cancer, anti-virus, antibiosis, and anti-oxidative properties and protects the central nervous and cardiovascular systems, immunosuppression, intestinal flora balance regulation, and broad-spectrum insecticidal activities. We reviewed the recent progress in matrine research in terms of the pharmacological activities and associated mechanisms to provide a reference for the wide and safe application of matrine.
苦参碱是中药苦参提取物的主要成分之一,具有广泛的药理活性,副作用少,毒性低。苦参碱具有抗炎、抗癌、抗病毒、抗菌、抗氧化等作用,具有保护中枢神经和心血管系统、免疫抑制、调节肠道菌群平衡、广谱杀虫等作用。本文从苦参碱的药理活性及其作用机制等方面综述了近年来苦参碱的研究进展,以期为苦参碱的广泛、安全应用提供参考。
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引用次数: 0
Phytochemical Profiling and Assessment of Habbe Musaffe Khoon Against Cervical Cancer Habbe Musaffe Khoon抗宫颈癌的植物化学分析及评价
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-26 DOI: 10.1177/09731296231204132
Nidhi Sharma, Prerna Raina, Ghazalla Mulla, Anand Shindikar, Prajakta Patil, Supriya Bhalerao, Ruchika Kaul-Ghanekar
Background In India, cancer of the cervix is the second most common cancer in women. Nowadays, various traditional herbal formulations can be used as adjuncts during conventional cancer therapies due to their anticancer activity. Habbe Musaffi Khoon (HMK), a Unani compound formulation, is traditionally used as a blood purifier and thus used to treat boils, scabies, acne, and pimples. It is also indicated in skin diseases, Habis-ud-Dam (styptic), and therapeutically used in Nafz-ud-Dam (hemorrhagic). Objectives The main purpose of this work was to phytochemically characterize HMK aqueous extract (HMKaq) and determine its activity against cervical cancer cells. Materials and Methods HMKaq was subjected to liquid chromatography-mass spectrometry (LC-MS) and evaluated for the presence of phytocompounds. HMKaq was evaluated for its effect on the viability of cervical cancer cells (HeLa, SiHa, and C33A) and was determined by MTT assay. Trypan blue dye exclusion was used to determine the outcome of HMKaq on the growth kinetics of cervical cancer cells. The role of HMK in regulating the cell cycle was analyzed by FACS and its effect on apoptosis was evaluated by checking mitochondrial membrane potential readings of JC-1 aggregates on a microplate reader and on the mRNA expression of caspase-3 and cytochrome c was evaluated by PCR. Results LC-MS analysis revealed 3845 compounds, out of which 58 were the major compounds. These included phenolics, esters, fatty acids, furans, quinones, tannins, flavonoids, and terpenes. HMKaq reduced the viability and growth of the cells. It induced arrest in the cell cycle of HeLa and apoptosis in SiHa and C33A by depolarizing the membrane potential of the mitochondria and upregulation of mRNA expression of Cas3 and Cyt C. Conclusion HMK exhibited anticancer activity against cervical cancer cells, thereby signifying its therapeutic potential.
在印度,子宫颈癌是女性中第二常见的癌症。目前,各种传统草药制剂由于具有抗癌活性,可作为常规癌症治疗的辅助药物。Habbe Musaffi Khoon (HMK)是一种Unani复方制剂,传统上被用作血液净化剂,因此用于治疗疖子、疥疮、痤疮和丘疹。它也适用于皮肤病,Habis-ud-Dam(闭合性)和Nafz-ud-Dam(出血性)的治疗。目的研究HMK水提物(HMKaq)的植物化学性质,并测定其抗宫颈癌细胞活性。材料与方法采用液相色谱-质谱联用技术(LC-MS)鉴定HMKaq中是否含有植物化合物。评估HMKaq对宫颈癌细胞(HeLa、SiHa和C33A)活力的影响,并采用MTT法测定。台盼蓝染色排除法测定HMKaq对宫颈癌细胞生长动力学的影响。FACS分析HMK对细胞周期的调控作用,PCR检测JC-1聚集体的线粒体膜电位,检测其对细胞凋亡的影响。结果LC-MS共鉴定出3845个化合物,其中58个为主要化合物。这些物质包括酚类、酯类、脂肪酸、呋喃类、醌类、单宁类、黄酮类和萜烯类。HMKaq降低了细胞的活力和生长。HMK通过使线粒体膜电位去极化,上调Cas3和Cyt c的mRNA表达,诱导HeLa细胞周期阻滞和SiHa、C33A细胞凋亡。结论HMK对宫颈癌细胞具有抗癌活性,具有一定的治疗潜力。
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引用次数: 0
Bee Pollen and Doxorubicin by Synergistic Effects Inhibit the Proliferation of Breast Tumors in 4T1 Tumor-bearing BALB/c Mice: A Biochemical, Immunohistochemical,and Molecular Approach 蜂花粉和阿霉素协同作用抑制4T1荷瘤BALB/c小鼠乳腺肿瘤的增殖:生化、免疫组织化学和分子方法
4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-10-26 DOI: 10.1177/09731296231203809
Jinwen Li
Objectives This study investigated the effects of BP and doxorubicin (DOX) on 4T1 tumor cells in a mouse model. Materials and Methods After inducing breast tumors, 70 4T1-tumor-bearing BALB/c mice were divided into seven groups ( n = 10/group). The groups were treated with DOX and BP for 35 days. On the 36th day, blood was taken from the heart, and serum was separated to measure levels of cytokines, estrogen, progesterone, testosterone, and nitric oxide. Antioxidant enzyme activities, as well as tissue ferric-reducing antioxidant power (FRAP) and malondialdehyde (MDA) levels, were evaluated. The expression of apoptotic genes and metastasis was measured using real-time polymerase chain reaction (PCR), while the expression of apoptotic proteins was evaluated using Western blotting. Finally, Ki-67 and p-53 were examined using immunohistochemistry to determine apoptosis. Results The study found that BP, with its synergistic effects with DOX, reduced the volume of tumors and increased the expression of apoptotic genes and proteins. In a dose-dependent manner, groups receiving BP and DOX with their synergistic effects reduced the level of estrogen and nitric oxide and also reduced the level of pro-inflammatory cytokines. BP along with DOX increased serum interferon-γ (IFN-γ) levels. Tumor tissue FRAP and thiobarbituric acid reactive substances (TBARS) levels increased in BP-treated groups. Ki-67 and Bcl-2 proliferation markers levels decreased, and p53 levels increased in 4T1-breast tumors. Conclusion The study concluded that BP with its synergistic effects along with DOX has the ability to suppress the growth of tumors and can also inhibit the oxidative damage of DOX.
目的探讨BP和多柔比星(DOX)对小鼠4T1肿瘤细胞的影响。材料与方法将70只乳腺肿瘤诱导后的4t1荷瘤BALB/c小鼠分为7组(n = 10/组)。各组均给予DOX和BP治疗,疗程35 d。第36天,取心脏血,分离血清,测定细胞因子、雌激素、孕酮、睾酮和一氧化氮的水平。测定抗氧化酶活性、组织铁还原抗氧化能力(FRAP)和丙二醛(MDA)水平。采用实时聚合酶链反应(real-time polymerase chain reaction, PCR)检测凋亡基因的表达和转移情况,Western blotting检测凋亡蛋白的表达情况。最后用免疫组化法检测Ki-67和p-53的凋亡情况。结果研究发现,BP通过与DOX的协同作用,使肿瘤体积减小,凋亡基因和蛋白表达增加。以剂量依赖的方式,接受BP和DOX协同作用的组降低了雌激素和一氧化氮水平,也降低了促炎细胞因子水平。BP与DOX一起增加血清干扰素-γ (IFN-γ)水平。bp治疗组肿瘤组织FRAP和硫代巴比妥酸活性物质(TBARS)水平升高。4t1期乳腺肿瘤中Ki-67、Bcl-2增殖标志物水平降低,p53水平升高。结论BP与DOX具有协同作用,具有抑制肿瘤生长的能力,并能抑制DOX的氧化损伤。
{"title":"Bee Pollen and Doxorubicin by Synergistic Effects Inhibit the Proliferation of Breast Tumors in 4T1 Tumor-bearing BALB/c Mice: A Biochemical, Immunohistochemical,and Molecular Approach","authors":"Jinwen Li","doi":"10.1177/09731296231203809","DOIUrl":"https://doi.org/10.1177/09731296231203809","url":null,"abstract":"Objectives This study investigated the effects of BP and doxorubicin (DOX) on 4T1 tumor cells in a mouse model. Materials and Methods After inducing breast tumors, 70 4T1-tumor-bearing BALB/c mice were divided into seven groups ( n = 10/group). The groups were treated with DOX and BP for 35 days. On the 36th day, blood was taken from the heart, and serum was separated to measure levels of cytokines, estrogen, progesterone, testosterone, and nitric oxide. Antioxidant enzyme activities, as well as tissue ferric-reducing antioxidant power (FRAP) and malondialdehyde (MDA) levels, were evaluated. The expression of apoptotic genes and metastasis was measured using real-time polymerase chain reaction (PCR), while the expression of apoptotic proteins was evaluated using Western blotting. Finally, Ki-67 and p-53 were examined using immunohistochemistry to determine apoptosis. Results The study found that BP, with its synergistic effects with DOX, reduced the volume of tumors and increased the expression of apoptotic genes and proteins. In a dose-dependent manner, groups receiving BP and DOX with their synergistic effects reduced the level of estrogen and nitric oxide and also reduced the level of pro-inflammatory cytokines. BP along with DOX increased serum interferon-γ (IFN-γ) levels. Tumor tissue FRAP and thiobarbituric acid reactive substances (TBARS) levels increased in BP-treated groups. Ki-67 and Bcl-2 proliferation markers levels decreased, and p53 levels increased in 4T1-breast tumors. Conclusion The study concluded that BP with its synergistic effects along with DOX has the ability to suppress the growth of tumors and can also inhibit the oxidative damage of DOX.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136382228","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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Pharmacognosy Magazine
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