anti-cancer activities

抗癌活性
  • 文章类型: Journal Article
    在弥漫性大B细胞淋巴瘤(DLBCL)患者中,原癌基因MYC经常失调,并在疾病进展中起关键作用。改善DLBCL患者的临床预后,制定针对MYC的战略至关重要。使用药用植物开发抗癌药物由于其不同的作用机制而引起了相当大的关注。在这项研究中,筛选了100种来自大韩民国的植物提取物,以寻找具有抗DLBCL作用的新型药物。其中,Ajaniapacifica(Nakai)K.Bremer和Humphries提取物(APKH)有效抑制DLBCL细胞的存活,同时对正常小鼠骨髓细胞毒性最小。APKH抑制抗凋亡BCL2家族成员的表达,导致促凋亡和抗凋亡BCL2成员之间的不平衡。这种破坏的线粒体膜电位,细胞色素c释放,和pro-caspase-3激活并最终导致DLBCL细胞死亡。重要的是,MYC表达被APKH显著下调,MYC在DLBCL细胞中的异位表达消除了APKH的促凋亡作用。这些结果证明APKH通过抑制MYC表达发挥抗DLBCL作用。此外,当与阿霉素联合使用时,CHOP方案的重要组成部分(环磷酰胺,阿霉素,长春新碱,和泼尼松),APKH协同增强阿霉素的治疗效果。这表明APKH可以克服耐药性,这在难治性/复发性DLBCL患者中很常见。为了鉴定APKH中具有抗DLBCL活性的化合物,使用UPLC-QTOF/MSe分析进行APKH的化学谱分析并评估其抗癌活性。基于UPLC-QTOF/MSe化学剖析,可以想象,APKH可能是靶向MYC并使耐药DLBCL细胞对CHOP化疗敏感的新型药物.有必要进一步研究阐明APKH中的化合物如何在DLBCL中发挥肿瘤抑制作用。
    The proto-oncogene MYC is frequently dysregulated in patients with diffuse large B-cell lymphoma (DLBCL) and plays a critical role in disease progression. To improve the clinical outcomes of patients with DLBCL, the development of strategies to target MYC is crucial. The use of medicinal plants for developing anticancer drugs has garnered considerable attention owing to their diverse mechanisms of action. In this study, 100 plant extracts of flora from the Republic of Korea were screened to search for novel agents with anti-DLBCL effects. Among them, Ajania pacifica (Nakai) K. Bremer and Humphries extract (APKH) efficiently suppressed the survival of DLBCL cells, while showing minimal toxicity toward normal murine bone marrow cells. APKH suppressed the expression of anti-apoptotic BCL2 family members, causing an imbalance between the pro-apoptotic and anti-apoptotic BCL2 members. This disrupted mitochondrial membrane potential, cytochrome c release, and pro-caspase-3 activation and eventually led to DLBCL cell death. Importantly, MYC expression was markedly downregulated by APKH and ectopic expression of MYC in DLBCL cells abolished the pro-apoptotic effects of APKH. These results demonstrate that APKH exerts anti-DLBCL effects by inhibiting MYC expression. Moreover, when combined with doxorubicin, an essential component of the CHOP regimen (cyclophosphamide, doxorubicin, vincristine, and prednisone), APKH synergistically enhanced the therapeutic effect of doxorubicin. This indicates that APKH may overcome drug resistance, which is common in patients with refractory/relapsed DLBCL. To identify compounds with anti-DLBCL activities in APKH, the chemical profile analysis of APKH was performed using UPLC-QTOF/MSe analysis and assessed for its anticancer activity. Based on the UPLC-QTOF/MSe chemical profiling, it is conceivable that APKH may serve as a novel agent targeting MYC and sensitizing drug-resistant DLBCL cells to CHOP chemotherapy. Further studies to elucidate how the compounds in APKH exert tumor-suppressive role in DLBCL are warranted.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    一品红是一品红科的一个大属。在化学和药理学上研究了大约250种大品藻属;从这些物种中分离出不同的化合物,尤其是二萜和三萜.一些报告显示,几种物种具有抗炎活性,这可以归因于二萜的存在,例如abietanes,ingenanes,和lathyranes。此外,发现从不同一品红种分离的一些二萜具有抗癌活性。在这次审查中,我们纳入了从2018年至2023年9月发表的具有抗炎或细胞毒性作用的一品红属物种中分离出的化合物.这篇综述使用的数据库是科学直接,Scopus,PubMed,Springer,和谷歌学者,使用具有抗炎或细胞毒性活性的关键字Euphorbia。在这次审查中,收集并分析了68项研究,这些研究涉及从36种大猩猩属物种获得的264种化合物的抗炎和抗癌活性。本综述中包括的化合物是萜烯(95%),其中68%是二萜,尤其是ingenanes的类型,abietanes,和三萜(约15%)。
    Euphorbia is a large genus of the Euphorbiaceae family. Around 250 species of the Euphorbia genus have been studied chemically and pharmacologically; different compounds have been isolated from these species, especially diterpenes and triterpenes. Several reports show that several species have anti-inflammatory activity, which can be attributed to the presence of diterpenes, such as abietanes, ingenanes, and lathyranes. In addition, it was found that some diterpenes isolated from different Euphorbia species have anti-cancer activity. In this review, we included compounds isolated from species of the Euphorbia genus with anti-inflammatory or cytotoxic effects published from 2018 to September 2023. The databases used for this review were Science Direct, Scopus, PubMed, Springer, and Google Scholar, using the keywords Euphorbia with anti-inflammatory or cytotoxic activity. In this review, 68 studies were collected and analyzed regarding the anti-inflammatory and anti-cancer activities of 264 compounds obtained from 36 species of the Euphorbia genus. The compounds included in this review are terpenes (95%), of which 68% are diterpenes, especially of the types ingenanes, abietanes, and triterpenes (approximately 15%).
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    Aralia continentalis has been used in Korea as a folk remedy for arthralgia, rheumatism, and inflammation. However, its anti-lymphoma effect remains uncharacterized. Here, we demonstrate that A. continentalis extract and its three diterpenes efficiently kill B-lymphoma cells. Our in vitro and in vivo results suggest that the cytotoxic activities of continentalic acid, a major diterpene from A. continentalis extract, are specific towards cancer cells while leaving normal murine cells and tissues unharmed. Mechanistically, continentalic acid represses the expression of pro-survival Bcl-2 family members, such as Mcl-1 and Bcl-xL. It dissociates the mitochondrial membrane potential, leading to the stimulation of effector caspase 3/7 activities and, ultimately, cell death. Intriguingly, this agent therapeutically synergizes with roflumilast, a pan-PDE4 inhibitor that has been successfully repurposed for the treatment of aggressive B-cell malignancies in recent clinical tests. Our findings unveiled that A. continentalis extract and three of the plant\'s diterpenes exhibit anti-cancer activities. We also demonstrate the synergistic inhibitory effect of continentalic acid on the survival of B-lymphoma cells when combined with roflumilast. Taken in conjunction, continentalic acid may hold significant potential for the treatment of B-cell lymphoma.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    藤黄酸(GA),藤黄树分泌的一种干树脂,是一种具有多种生物活性的天然活性成分,比如抗癌,抗炎,抗氧化剂,抗菌作用,等。越来越多的证据表明,GA通过各种分子机制具有明显的抗癌作用,包括细胞凋亡的诱导,自噬,细胞周期停滞和入侵的抑制,转移,血管生成。为了提高癌症治疗的疗效,纳米药物递送系统已被用于负载GA并形成胶束,纳米粒子,纳米纤维,等等。在这次审查中,我们的目标是提供化学结构和性质的总结,抗癌活动,药物递送系统和GA的联合治疗,为促进GA的发展和临床应用提供参考。
    Gambogic acid (GA), a kind of dry resin secreted by the Garcinia hanburyi tree, is a natural active ingredient with various biological activities, such as anti-cancer, anti-inflammatory, antioxidant, anti-bacterial effects, etc. An increasing amount of evidence indicates that GA has obvious anti-cancer effects via various molecular mechanisms, including the induction of apoptosis, autophagy, cell cycle arrest and the inhibition of invasion, metastasis, angiogenesis. In order to improve the efficacy in cancer treatment, nanometer drug delivery systems have been employed to load GA and form micelles, nanoparticles, nanofibers, and so on. In this review, we aim to offer a summary of chemical structure and properties, anti-cancer activities, drug delivery systems and combination therapy of GA, which might provide a reference to promote the development and clinical application of GA.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

       PDF(Pubmed)

  • 文章类型: Journal Article
    优化了车前草毛状根的诱导,以利用转化的根培养物。最高的转化频率是使用叶外植体实现的,A4菌株,外植体的预培养,150μM乙酰丁香酮,接种5分钟,半强度Murashige和Skoog基础培养基作为共培养,和半强度Gamborg的基础培养基作为含有3%蔗糖的选择性培养基。在所研究的包含没食子酸的化合物中,catalpol和芹菜素,在24小时时,只有20mgL-1AgNO3和100mgL-1壳聚糖会影响毛状根中没食子酸的产生,其含量增加了7.63、4.76倍,分别。20mgL-1AgNO3引起的毛状根甲醇提取物对肺炎克雷伯菌具有抗菌活性(MIC和MBC=25mgmL-1),普通变形杆菌和伤寒沙门氏菌以及未引起的杉木毛状根的抗菌潜力(MIC=25mgmL-1和MBC=35mgmL-1)对肺炎克雷伯菌和普通P。比其他细菌。与IC50=5263.65±4.6µg的人胚肾(HEK-293)相比,杉木毛状根的甲醇提取物对结直肠癌细胞系(SW-480)表现出明显的细胞毒性活性。μgmL-1。车前草毛状根显示出重要的生物活性,解释了其在传统医学中的作用。
    Hairy root induction in Plantago lanceolata was optimized to take advantage of transformed root cultures. The highest frequency of transformation was achieved using leaf explant, A4 strain, pre-cultivation of explant, 150 µM Acetosyringone, 5 min inoculation, half-strength Murashige and Skoog basal medium as co-cultivation, and half-strength Gamborg\'s basal medium as a selective medium with 3% sucrose. Among the studied compound encompassing gallic acid, catalpol and apigenin, only the production of gallic acid in hairy roots was affected by 20 mg L-1 AgNO3 and 100 mg L-1 chitosan at 24 hr which yielded 7.63, 4.76-fold increase in its content, respectively. The methanolic extracts of hairy roots elicited by 20 mg L-1 AgNO3 exhibited anti-bacterial activity (MIC and MBC = 25 mg mL-1) against Klebsiella pneumoniae, Proteus vulgaris and Salmonella typhi and anti-bacterial potential of non-elicited hairy roots of P. lanceolata (MIC = 25 mg mL-1 and MBC = 35 mg mL-1) were more active against Klebsiella pneumoniae and P. vulgaris than other bacteria. The methanolic extracts of the P. lanceolata hairy roots demonstrated significant cytotoxic activity on colorectal carcinoma cell line (SW-480) with IC50 = 250.65 ± 6.8 µg mL-1 in comparison to human embryonic kidney (HEK-293) with IC50 = 5263.65 ± 4.6 µg mL-1. Plantago lanceolata hairy roots showed important biological activity explaining its role in traditional medicine.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

  • 文章类型: Journal Article
    人类微生物群由数万亿个微生物组成,这些微生物已经与它们的人类宿主一起进化并继续生活在它们的人类宿主上/内。不同的环境因素和饮食对人类微生物群有很大的影响。这些微生物与它们的宿主协同生活,并且以许多不同的方式有益于宿主。许多微生物有助于对抗人类疾病。癌症是一种这样的疾病,其影响大量人群,通常导致死亡。癌症也是最致命的人类疾病之一,每年在全世界杀死数百万人。虽然许多治疗程序是可用的,但没有一个是100%有效的治疗癌症。在这次审查中,我们试图了解人类微生物群在癌症治疗中的作用。由不同微生物产生的脂肽(LP)可以作为抗癌的有效药物。LP是低分子量的脂蛋白,其也因其抗癌活性而已知。由于人类微生物群属于宿主体内的环境,使用这些微生物制备的药物很容易被人体接受。这种使用人类微生物群产生的LP的新方法可以被认为是癌症治疗中急需的变化。因此,建议研究应集中在宿主-微生物相互作用上,这可能为理解这些微生物在癌症治疗中的作用铺平道路。
    Human microbiota comprises of trillions of microbes which have evolved with and continued to live on/ within their human hosts. Different environmental factors and diet have a large impact upon human microbiota population. These microorganisms live in synergy with their hosts and are beneficial to the host in many different ways. Many microorganisms help to fight against human diseases. Cancer is one such diseases which effects a large human population often leading to death. Cancer is also one of the most fatal human diseases killing millions of people world-wide every year. Though many treatment procedures are available but none is 100 % effective in curing cancer. In this review, we seek to understand the role of human microbiota in cancer treatment. Lipopeptide(s) (LPs) produced by different microorganisms can act as efficient drug(s) against cancer. LPs are low molecular weight lipo-proteins that are also known for their anti-cancer activities. As human microbiota belongs to an environment within the host body, a drug prepared using these microorganisms will be easily accepted by the body. This novel approach of using LPs produced by human microbiota can be considered for the much needed change in cancer treatment. Therefore, it is proposed that research should focus on the host-microbe interaction which could pave the way in understanding role played by these microorganisms in cancer treatment.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

  • 文章类型: Journal Article
    Phytochemical investigation of the ethyl acetate fraction of Lycopodium complanatum led to eight new serratane triterpenoids (lycomplanatums A-H, 1-8), along with five known analogues (9-13). Their structures were elucidated by extensive spectroscopic methods, including 1D/2D NMR, HRESIMS, and DFT GIAO 13C NMR calculation. Among them, compounds 2 and 13 showed moderate antiproliferative effects against seven human cancer cell lines, especially for MCF-7 with IC50 values of 13.8-44.7 μM. Additionally, the compounds were screened for anti-inflammatory effects based on their inhibitory activities of nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 cells, and compounds 2 and 13 diminished NO production more potently than others in a concentration-dependent manner.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

  • 文章类型: Journal Article
    Multifloside(4),与10-羟基油苷11-甲酯(1)一起,10-羟基油苷二甲酯(2),和10-羟基桂皮苷(3),都是类环烯醚萜类,它们是天然存在的化合物,具有广泛的生物和药理活性。然而,1-4的抗癌活性尚未评估。这项工作的目的是研究1-4在人表皮样癌细胞系A431和人非小细胞肺癌(NSCLC)细胞系A549中的抗癌活性。结果表明,1-4在抑制人A431和A549细胞增殖的能力方面的效力不同,和多花苷(4)对A431细胞表现出最高的抑制活性。结构-活性关系表明邻-羟基-对-羟基-苯基乙基基团可能有助于抗A431细胞的抗癌活性。还可以抑制细胞集落的形成,将细胞周期阻滞在S期,增加活性氧(ROS)的水平,和线粒体膜电位(MMP),但在低浓度下并不显著诱导细胞凋亡。研究结果表明,多花苷(4)具有在A431细胞中显示选择性抗癌作用的趋势,同时抑制菌落形成,诱导S细胞周期阻滞,ROS生产,增加MMP。
    Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1-4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1-4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1-4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

       PDF(Pubmed)

  • 文章类型: Journal Article
    The whole seed (W), endosperm (E) and hull (H) of five cultivars of Job\'s tears (Coix lachryma-jobi Linn. var. ma-yuen Stapf) including Thai Black Phayao, Thai Black Loei, Laos Black Loei, Laos White Loei and Laos Black Luang Phra Bang were processed before solvent extraction by non-cooking, roasting, boiling and steaming Each part of the Job\'s tears was extracted by the cold and hot process by refluxing with methanol and hexane. The total of 330 extracts included 150 methanol extracts and 180 hexane extracts were investigated for anti-proliferative activity on human colon adenocarcinoma cell line (HT-29) by the sulforhodamine B (SRB) assay. The extracts which gave high anti-proliferative activity were tested for apoptotic activity by acridine orange and ethidium bromide double staining and anti-oxidative activities including free radical scavenging and lipid peroxidation inhibition activities. The extract from the hull of Thai Black Loei roasted before extracting by hot methanol (M-HTBL-R2) showed the highest anti-proliferative activity on HT-29 with the IC50 values of 11.61 ± 0.95 μg/ml, while the extract from the non-cooked hull of Thai Black Loei by cold methanol extraction (M-HTBL-N1) gave the highest apoptosis (8.17 ± 1.18%) with no necrosis. In addition, M-HTBL-R2 and M-HTBL-N1 indicated free radical scavenging activity at the SC50 values of 0.48 ± 0.12 and 2.47 ± 1.15 mg/ml, respectively. This study has demonstrated the anti-colorectal cancer potential of the M-HTBL-R2 and M-HTBL-N1 extracts.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

  • 文章类型: Journal Article
    In this study, a series of bis(4-hydroxy)benzophenone oxime ether derivatives such as 12c, 12e and 12h were identified as novel estrogen receptor (ER) agonists that have additional and complementary anti-proliferative activities via ER-independent mechanism in cancer cells. These compounds are expected to overcome the therapeutic limitation of existing ER agonists such as estradiol and tamoxifen, which have been known to induce the proliferation of cancer cells.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Sci-hub)

公众号