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Online identification of chemical constituents in Mongolian medicine Zhachong-13 pills by UHPLC-Q-exactive Orbitrap MS. 超高效液相色谱-Q-反应式 Orbitrap MS 在线鉴定蒙药扎冲十三味丸中的化学成分
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-22 DOI: 10.1080/10286020.2024.2379981
Cai-Yun Tian, Qing-Rui Yang, Ling-Xuan Fan, Yu-Mei Yang, Bo-Wen Gao, Jian-Bo Yang

Zhachong-13 pills (ZC-13), as a traditional prescription of Mongolian medicine, are often used in the clinical practice of Mongolian hospitals for the treatment of stroke and rheumatic arthritis. In this experiment, UHPLC-Q-Exactive Orbitrap MS was used to explore the chemical composition of ZC-13. The results showed that 315 compounds were identified or inferred, including 56 alkaloids, 77 2-(2-phenylethyl)chromones, 61 flavonoids, 31 tannins, 8 coumarins, 16 lignans, 21 terpenoids, 5 amino acids, 19 organic acids, and 21 other components. In addition, the pharmacological activities related to anti-cerebral ischemia of these components were summarized. This result laid a foundation for further study on the pharmacodynamic material basis of ZC-13 and provided a scientific basis for the formulation of ZC-13 quality specifications.

扎冲十三味丸(ZC-13)是蒙医药的传统处方,在蒙医医院临床上经常用于治疗中风和风湿性关节炎。本实验采用超高效液相色谱-Q-Exactive Orbitrap MS对ZC-13的化学成分进行了研究。结果表明,共鉴定或推断出 315 种化合物,其中包括 56 种生物碱、77 种 2-(2-苯基乙基)色酮、61 种黄酮类、31 种鞣质、8 种香豆素、16 种木质素、21 种萜类、5 种氨基酸、19 种有机酸和 21 种其他成分。此外,还总结了这些成分在抗脑缺血方面的药理活性。这一结果为进一步研究 ZC-13 的药效物质基础奠定了基础,也为制定 ZC-13 质量标准提供了科学依据。
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引用次数: 0
Screening of GLP-1r agonists from natural products using affinity ultrafiltration screening coupled with UPLC-ESI-Orbitrap-MS technology: a case study of Panax ginseng. 利用 UPLC-ESI-Orbitrap-MS 技术进行亲和超滤筛选,从天然产品中筛选 GLP-1r 激动剂:三七案例研究。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-22 DOI: 10.1080/10286020.2024.2378821
Hong-Ping Wang, Zhao-Zhou Lin, Qiong Yin, Jing Du

In our study, a method based on affinity ultrafiltration screening coupled with UPLC-ESI-Orbitrap-MS technology was established to select Glucagon-like peptide-1 receptor (GLP-1R) agonists from natural products, and as an example, the GLP-1R agonists from Panax ginseng was selected using our established method. As a result, total five GLP-1R agonists were selected from Panax ginseng for the first time. Our results indicated that activating GLP-1R to promote insulin secretion probably was another important hypoglycemia mechanism for ginsenosides in Panax ginseng, which had great influence on the study of the anti-diabetes effect of ginsenosides.

我们的研究建立了一种基于亲和超滤筛选结合UPLC-ESI-Orbitrap-MS技术从天然产物中筛选胰高血糖素样肽-1受体(GLP-1R)激动剂的方法,并以我们建立的方法从三七中筛选出的GLP-1R激动剂为例。结果,首次从三七中筛选出了五种 GLP-1R 激动剂。我们的研究结果表明,激活GLP-1R促进胰岛素分泌可能是人参中人参皂苷的另一重要降血糖机制,这对研究人参皂苷的抗糖尿病作用具有重要影响。
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引用次数: 0
Harmine inhibits the proliferation and migration and promotes the apoptosis of colon cancer cells via inhibition of the FAK/AKT and ERK1/2/CREB signaling pathways. Harmine 通过抑制 FAK/AKT 和 ERK1/2/CREB 信号通路,抑制结肠癌细胞的增殖和迁移,并促进其凋亡。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-13 DOI: 10.1080/10286020.2024.2361767
Fu-Hong Liu, Xing-Cheng Lin, Yu-Wei Liu, Tian-Tian Zhang, Yang-Bo Zhang, Zhuo-Long Xie, Yuan Zhan, Ping Hu

Harmine is present in a variety of medicinal plants, and its effects on colon cancer cells remain unclear. Here, we found that harmine exhibited significant inhibitory effects on the proliferation of colon cancer cells by inhibiting the phosphorylation levels of the FAK/AKT and ERK1/2/CREB. Furthermore, harmine also inhibited the migration of colon cancer cells and suppressed the expression levels of MMP-2, MMP-9, and VEGF. Additionally, harmine-induced apoptosis in colon cancer cells by regulating the expression of Bcl-2 and Bax. In conclusion, our findings suggest that harmine exerts a significant inhibitory effect on the development of colon cancer cells.

胭脂虫碱存在于多种药用植物中,它对结肠癌细胞的影响尚不清楚。在这里,我们发现鹤顶红通过抑制FAK/AKT和ERK1/2/CREB的磷酸化水平,对结肠癌细胞的增殖有明显的抑制作用。此外,鹤顶红还能抑制结肠癌细胞的迁移,并抑制MMP-2、MMP-9和血管内皮生长因子的表达水平。此外,加害碱还能通过调节 Bcl-2 和 Bax 的表达诱导结肠癌细胞凋亡。总之,我们的研究结果表明,鹤顶红对结肠癌细胞的发展具有显著的抑制作用。
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引用次数: 0
Diterpenoid alkaloids from Delphinium sherriffii. Delphinium sherriffii 的二萜生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-12 DOI: 10.1080/10286020.2024.2376244
Guo-Qing Sun, Cheng-En Fu, Yang Yang, Xiao-Jian Li, Jia-Yi Ma, Shuai Huang, Xian-Li Zhou, Lin Chen

Three new diterpenoid alkaloids (1, 2, 3) and seventeen known (4-20) compounds were isolated from the whole plant of Delphinium sherriffii Munz (Ranunculaceae). Their structures were elucidated by various spectroscopic analyses, including IR, HR-ESI-MS, 1D and 2D NMR spectra. All compounds were evaluated for the inhibitory activity of Sf9 cells and compound 5 exhibited the strongest cytotoxicity (IC50 = 8.97 μM) against Sf9 cell line.

从 Delphinium sherriffii Munz(毛茛科)全株中分离出三个新的二萜生物碱(1、2、3)和 17 个已知化合物(4-20)。通过各种光谱分析,包括红外光谱、HR-ESI-MS、一维和二维核磁共振光谱,阐明了这些化合物的结构。评估了所有化合物对 Sf9 细胞的抑制活性,其中化合物 5 对 Sf9 细胞株的细胞毒性最强(IC50 = 8.97 μM)。
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引用次数: 0
Schisandrin A can promote the anti-tumor effect of 5-Fu by reversing the immunosuppressive state of the body in rat. 五味子甲素可以通过逆转大鼠体内的免疫抑制状态来促进 5-Fu 的抗肿瘤作用。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-09 DOI: 10.1080/10286020.2024.2375291
Xiao-Hui Wang, Peng-Fei Dong, Feng Wang, Lin Zhou

In this study, based on Walker 256 in vitro experiments, CCK-8 assay, clone formation assay, wound healing assay, and flow cytometry were used to detect cell apoptosis and cell cycle. It was found that schisandrin may have significant anti-tumor effects in vitro by inhibiting TGF-β/Smad signaling pathway. In addition, in vivo experiments, immunohistochemistry was used to observe the expression of HIF-1α, VEGF and VEGFR-2 in tumor tissues. It was found that schisandrin could significantly improve the immunosuppression induced by 5-Fu and enhance the antitumor effect of 5-Fu. The mechanism may be related to the inhibition of Wnt-1/β-catenin signaling pathway.

本研究以 Walker 256 体外实验为基础,采用 CCK-8 试验、克隆形成试验、伤口愈合试验和流式细胞术检测细胞凋亡和细胞周期。结果发现,五味子甲素可通过抑制 TGF-β/Smad 信号通路在体外发挥显著的抗肿瘤作用。此外,在体内实验中,免疫组化法观察了肿瘤组织中 HIF-1α、VEGF 和 VEGFR-2 的表达。结果发现,五味子素能明显改善5-Fu诱导的免疫抑制,增强5-Fu的抗肿瘤作用。其机制可能与抑制Wnt-1/β-catenin信号通路有关。
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引用次数: 0
Chromomycins from soil-derived Streptomyces sp. inhibit the growth of human non-small cell lung cancer cells by targeting c-FLIP. 源自土壤的链霉菌的色霉素通过靶向 c-FLIP 抑制人类非小细胞肺癌细胞的生长。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-08 DOI: 10.1080/10286020.2024.2375288
Gao-Jie Li, Chen Wang, Wen-Die Wang, Yue Shang, Chao-Yang Zeng, Ai-Min Wang, Jing-Lin Bai, Jing Su, Ling Su, Shu-Yi Si, Li-Yan Yu, Mao-Luo Gan, Shu-Zhen Chen

Three chromomycin derivatives, chromomycins A3 (1, CA3), A5 (2, CA5), and monodeacetylchromomycin A3 (3, MDA-CA3), were identified from the soil-derived Streptomyces sp. CGMCC 26516. A reinvestigation of the structure of CA5 is reported, of which the absolute configuration was unambiguously determined for the first time to be identical with that of CA3 based on nuclear magnetic resonance (NMR) data analysis as well as NMR and electronic circular dichroism calculations. Compounds 1-3 showed potent cytotoxicity against the non-small-cell lung cancer (NSCLC) cells (A549, H460, H157-c-FLIP, and H157-LacZ) and down-regulated the protein expression of c-FLIP in A549 cells. The IC50 values of chromomycins in H157-c-FLIP were higher than that in H157-LacZ. Furthermore, si-c-FLIP promoted anti-proliferation effect of chromomycins in NSCLC cells. In nude mice xenograft model, 1 and 2 both showed more potent inhibition on the growth of H157-lacZ xenografts than that of H157-c-FLIP xenografts. These results verify that c-FLIP mediates the anticancer effects of chromomycins in NSCLC.

从源于土壤的链霉菌 CGMCC 26516 中鉴定出三种铬霉素衍生物,即铬霉素 A3(1,CA3)、A5(2,CA5)和单去乙酰铬霉素 A3(3,MDA-CA3)。报告对 CA5 的结构进行了重新研究,根据核磁共振数据分析以及核磁共振和电子圆二色性计算,首次明确确定其绝对构型与 CA3 相同。化合物1-3对非小细胞肺癌(NSCLC)细胞(A549、H460、H157-c-FLIP和H157-LacZ)具有很强的细胞毒性,并能下调A549细胞中c-FLIP的蛋白表达。铬霉素在H157-c-FLIP中的IC50值高于在H157-LacZ中的IC50值。此外,si-c-FLIP还能促进铬霉素在NSCLC细胞中的抗增殖作用。在裸鼠异种移植模型中,1和2对H157-lacZ异种移植细胞生长的抑制作用均强于H157-c-FLIP异种移植细胞。这些结果验证了c-FLIP介导了铬霉素在NSCLC中的抗癌作用。
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引用次数: 0
Two new diterpenoid alkaloids from the roots of Aconitum nagarum and their cytotoxic activity. 从 Aconitum nagarum 的根中提取的两种新的二萜生物碱及其细胞毒性活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-08 DOI: 10.1080/10286020.2024.2373326
Jiang Hu, Ren Ji, Guang-Rong Yang, Tao Lv, Qiang Li, Feng Gao

A chemical investigation on the roots of Aconitum nagarum afforded two undescribed C19-diterpenoid alkaloids nagarumines D and E (1 and 2). The structures of the new compounds were elucidated by spectral methods such as 1D and 2D (1H-1H COSY, HMQC, and HMBC) NMR spectroscopy, as well as HR-ESI-MS. The two isolated alkaloids were tested in vitro for cytotoxic activity against five gastric tumor cell lines. Consequently, compound 2 exhibited some cytotoxicities against several human cancer cell lines with IC50 value less than 20.0 μM.

通过对 Aconitum nagarum 的根部进行化学研究,发现了两种未曾描述过的 C19-二萜生物碱 nagarumines D 和 E(1 和 2)。通过一维和二维(1H-1H COSY、HMQC 和 HMBC)核磁共振光谱以及 HR-ESI-MS 等光谱方法阐明了新化合物的结构。在体外测试了这两种分离出的生物碱对五种胃肿瘤细胞系的细胞毒性活性。结果表明,化合物 2 对几种人类癌细胞株具有一定的细胞毒性,其 IC50 值小于 20.0 μM。
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引用次数: 0
Mechanisms and therapeutic potential of chinonin in nervous system diseases. 奇诺宁在神经系统疾病中的作用机制和治疗潜力。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-08 DOI: 10.1080/10286020.2024.2371040
Zhang Hui, Wang Lai-Fa, Wang Xue-Qin, Deng Ling, He Bin-Sheng, Jian-Ming Li

The flavonoid compound chinonin is one of the main active components of Rhizoma anemarrhena with multiple activities, including anti-inflammatory and antioxidant properties, protection of mitochondrial function and regulation of immunity. In this paper, we reviewed recent research progress on the protective effect of chinonin on brain injury in neurological diseases. "Chinonin" OR "Mangiferin" AND "Nervous system diseases" OR "Neuroprotection" was used as the terms for search in PumMed. After discarding duplicated and irrelevant articles, a total of 23 articles relevant to chinonin published between 2012 and 2023 were identified in our study.

黄酮类化合物chinonin是金莲花的主要活性成分之一,具有多种活性,包括抗炎、抗氧化、保护线粒体功能和调节免疫力。在本文中,我们综述了近期有关奇诺宁对神经系统疾病中脑损伤的保护作用的研究进展。在 PumMed 中使用 "奇诺宁 "或 "芒果苷 "和 "神经系统疾病 "或 "神经保护 "作为检索词。在剔除重复和不相关的文章后,我们的研究共发现了 23 篇 2012 年至 2023 年间发表的与芒果苷相关的文章。
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引用次数: 0
Discovery of sesquiterpene lactones with anti-inflammatory effect from Youngia japonica. 从莬丝子中发现具有抗炎作用的倍半萜内酯
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-04 DOI: 10.1080/10286020.2024.2370401
Xian-Sheng Ye, Kuan Lin, Chang-Long Leng, Yu-Ran Gui, Shu-Xiu Zhu, Hui-Ying Liu, Yi-Yuan Xia, Bin-Lian Sun, Wei Liu, Xi-Ji Shu

The preliminary study revealed that the ethyl acetate eluate of Youngia japonica (YJ-E) could inhibit the expression of key proteins of p-p65, p-IκBα, p-IKKα/β, and p-AKT in LPS stimulated BV2 cell. Further phytochemical study led to the isolation of eight compounds from YJ-E, including one new sesquiterpene lactone. Their structures were elucidated by several spectroscopic data, and comparing the NMR data of known compound. In addition, all of the isolates were evaluated for the anti-inflammatory effect. As a result, compounds 3 and 4 distinctly attenuated the expressions of p-IκBα, p-p65, and p-AKT in LPS stimulated BV2 cell, respectively.

初步研究发现,莬丝子乙酸乙酯洗脱液(YJ-E)可抑制 LPS 刺激的 BV2 细胞中 p-p65、p-IκBα、p-IKKα/β 和 p-AKT 等关键蛋白的表达。通过进一步的植物化学研究,从 YJ-E 中分离出了八种化合物,其中包括一种新的倍半萜内酯。通过一些光谱数据以及与已知化合物核磁共振数据的比较,阐明了这些化合物的结构。此外,还对所有分离物的抗炎效果进行了评估。结果表明,化合物 3 和 4 分别明显减轻了 LPS 刺激的 BV2 细胞中 p-IκBα、p-p65 和 p-AKT 的表达。
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引用次数: 0
Five new glycosides from the culms of Phyllostachys nigra var. henonis. 从黑木耳变种秆中提取的五种新苷。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-04 DOI: 10.1080/10286020.2024.2366450
Bao Zhang, Hai-Hua Yuan, Jia Sun, Hang Xun, Jie Wang, Feng Qiu, Jian-Jun Wang, Xi Yao, Jin Wang, Wei Fan, Feng Tang

Five new glycosides, namely methyl 3-methoxybenzoate-4,5-di-O-β-D-glucopyranoside (1), (1aS,3aS,3R)-3-(4'-O-β-D-glucopyranosyl-3'-methoxyphenyl)-5,6-dioxa-bicyclo[3.3.0]octane-1-one (2), quinolin-4(1H)-one-3-O-β-D-glucopyranoside (3), 3-methoxy-propiophenone 4-O-(6'-β-D-xylopyranosyl)-β-D-glucopyranoside (4), methyl 3-methoxybenzoate 4-O-(6'-β-D-xylopyranosyl)-β-D-glucopyranoside (5), and one known compound, bambulignan B (6) were isolated from the culms of Phyllostachys nigra var. henonis. Their structures were determined using spectroscopic analysis. All compounds were evaluated for their DPPH radical scavenging activity. Compound 6 exhibited antioxidant activity with IC50 value of 59.5 μM (positive control, L-ascorbic acid, IC50 = 12.4 μM; 2,6-ditertbutyl-4-methyl phenol, IC50 = 11.8 μM).

五种新苷,即 3-甲氧基苯甲酸甲酯-4,5-二-O-β-D-吡喃葡萄糖苷 (1)、(1aS,3aS,3R)-3-(4'-O-β-D-吡喃葡萄糖基-3'-甲氧基苯基)-5,6-二氧杂双环[3.3.0]辛烷-1-酮(2)、喹啉-4(1H)-酮-3-O-β-D-吡喃葡萄糖苷(3)、3-甲氧基苯丙酮 4-O-(6'-β-D-吡喃木糖基)-β-D-吡喃葡萄糖苷(4)、从 Phyllostachys nigra var. henonis 的秆中分离出了 3-甲氧基苯甲酸甲酯 4-O-(6'-β-D-xylopyranosyl)-β-D-吡喃葡萄糖苷(5)和一种已知化合物--班布利酮 B(6)。秆中分离出来。通过光谱分析确定了它们的结构。对所有化合物的 DPPH 自由基清除活性进行了评估。化合物 6 具有抗氧化活性,其 IC50 值为 59.5 μM(阳性对照 L-抗坏血酸,IC50 = 12.4 μM;2,6-二叔丁基-4-甲基苯酚,IC50 = 11.8 μM)。
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引用次数: 0
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Journal of Asian Natural Products Research
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