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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
Two new cucurbitane-type triterpenoid saponins from the fruit of Citrullus colocynthis 从秋刀鱼果实中提取的两种新葫芦烷类三萜皂甙
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-04 DOI: 10.1080/10286020.2024.2364908
Two new cucurbitane-type triterpenoid saponins, 2,20β,22β-trihydroxy-16α,23(R)-epoxycucurbita-1,5,24-triene-3,11-dione 2-O-β-D-glucopyranoside (1), 2,20β,22α-trihydroxy-16α,23(S)-epoxycucurbita-1,5,11,24-tetraene-3-one 2-O-β-D-glucopyranoside (2) were isolated from the fruit of Citrullus colocynthis (L.) Schrad. Their structures were elucidated by mass spectrometry, IR, 1D, and 2D NMR spectroscopy, etc. Besides, both of the compounds showed significant hepatoprotective activities at 10 μM against paracetamol-induced HepG2 cell damage.
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引用次数: 0
Fuzheng Huayu recipe inhibits bleomycin-induced pulmonary fibrosis in rats by inhibiting M2 polarization of macrophages via the oxidative phosphorylation pathway. 扶正化瘀方通过氧化磷酸化途径抑制巨噬细胞的M2极化,从而抑制博莱霉素诱导的大鼠肺纤维化。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-03 DOI: 10.1080/10286020.2024.2371050
Xing-Hua Yuan, Su-Fang Zhang, Yu Hang, Yan-Hua Shen, Shan-Fang Zhang, Wei-Ling Huang, Jing-Yi Huang, Ye-Chang Qian, Xiu-Lian Zhang, Qiu-Hong Li, Li Li

Fuzheng Huayu recipe (FZHYR) is a Chinese patent medicine for the treatment of fibrosis. The effects of FZHYR on pulmonary fibrosis and macrophage polarization were investigated in vitro. FZHYR inhibited pulmonary inflammation and fibrosis and M2 polarization of macrophages in bleomycin-induced pulmonary fibrosis (BPF) of rat model. Differentially expressed genes were screened by high-throughput mRNA sequencing and GSEA showed that oxidative phosphorylation (OXPHOS) was correlated with BPF. FZHYR inhibited expressions of Ndufa2 and Ndufa6 in lung tissues of BPF rats. These findings suggest that OXPHOS pathway serves as a possible target for pulmonary fibrosis therapy by FZHYR.

扶正化瘀方(FZHYR)是一种治疗肺纤维化的中成药。研究人员在体外研究了扶正化瘀汤对肺纤维化和巨噬细胞极化的影响。在博莱霉素诱导的大鼠肺纤维化(BPF)模型中,FZHYR可抑制肺部炎症和纤维化以及巨噬细胞的M2极化。高通量 mRNA 测序筛选了差异表达基因,GSEA 显示氧化磷酸化(OXPHOS)与 BPF 相关。FZHYR 可抑制 BPF 大鼠肺组织中 Ndufa2 和 Ndufa6 的表达。这些研究结果表明,OXPHOS途径可能是FZHYR治疗肺纤维化的靶点。
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引用次数: 0
New cembranoid with potent anti-inflammatory effect isolated from Boswellia sacra by inactivating the NF-κB signaling pathway. 通过使 NF-κB 信号通路失活,从乳香中分离出具有强效抗炎作用的新型cembranoid。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-02 DOI: 10.1080/10286020.2024.2372390
Xiao-Rong Yin, Zhen Yuan, Wei-Feng Wang, Bing-Yang Zhang, Lu-Qiong Wang, Feng Qiu, Feng Zhao

Boswellia sacra has the properties of activating blood circulation, fixing pain, subduing swelling and promoting muscle growth. However, the anti-inflammatory active ingredients and molecular mechanisms of Boswellia sacra are still not clearly explored. Boswellia sacra was grounded and extracted using 95% ethanol, the extracts were separated by column chromatography preparation to give compounds. Spectral analysis and quantum calculations confirmed the structures of compounds and identified compound 1 as a new compound. Compounds 1-3 showed potent inhibitory activities and their effects on inflammatory mediator NO and inflammatory cytokines were examined by ELISA assay. Furthermore, their modulatory mechanism on inflammatory signal pathways was explored.

乳香具有活血、止痛、消肿和促进肌肉生长的功效。然而,乳香的抗炎活性成分和分子机制仍未得到明确的探索。将乳香磨碎并用 95% 的乙醇提取,提取物经柱层析分离得到化合物。光谱分析和量子计算证实了化合物的结构,并确定化合物 1 为新化合物。通过酶联免疫吸附试验检测了化合物 1-3 对炎症介质 NO 和炎症细胞因子的影响。此外,还探讨了它们对炎症信号通路的调节机制。
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引用次数: 0
Correction. 更正。
IF 1.7 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-07-01 Epub Date: 2024-03-28 DOI: 10.1080/10286020.2024.2334547
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引用次数: 0
A new cassane diterpenoid from the seed of Caesalpinia sappan. 从 Caesalpinia sappan 种子中提取的一种新的决明二萜。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-30 DOI: 10.1080/10286020.2024.2360640
Yue-Lin Zhao, Yue Jin, Zi-Ying Han, Wen-Han Song, Hui-Lin Zhu, Jian Zhang, Qian Wang, Miao Wang, Xiao-Wen Jiang, Hui-Yuan Gao

In this study, a previously undescribed cassane diterpenoid, named caesalpinin JF (1), along with two known cassane diterpenoids caesanine C (2) and tomocinol B (3), was isolated from 95% EtOH extract of the seeds of Caesalpinia sappan Linn. Additionally, three known compounds including pulcherrin R (4), syringaresinol-4'-O-β-D-glucopyranoside (5) and kaempferol (6) were also identified. The structures of the isolated compounds were elucidated by comprehensive 1D and 2D NMR spectroscopic analyses. Additionally, electronic circular dichroism (ECD) calculation was used to identify the absolute structure of compound 1. Among the isolated compounds, compound 1 displayed a potent anti-neuroinflammation with an IC50 value of 9.87 ± 1.71 μM.

在这项研究中,从红豆杉种子 95% 的 EtOH 提取物中分离出了一种之前未曾描述过的决明子二萜,命名为 Caesalpinin JF (1),以及两种已知的决明子二萜 caesanine C (2) 和 tomocinol B (3)。此外,还鉴定出三种已知化合物,包括 Pulcherrin R (4)、Syringaresinol-4'-O-β-D-吡喃葡萄糖苷 (5) 和山奈酚 (6)。通过全面的一维和二维核磁共振光谱分析,阐明了这些分离化合物的结构。在分离出的化合物中,化合物 1 具有很强的抗神经发炎作用,其 IC50 值为 9.87 ± 1.71 μM。
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引用次数: 0
Bis-piperidine alkaloids from the peels of Areca catechu. 从Areca catechu果皮中提取的双哌啶生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-30 DOI: 10.1080/10286020.2024.2372383
Xia Zhang, Fang-Xin Wang, Zi-Wei Li, Song Wang, Shi-Qing Zhang, Min Song, Xiao-Qi Zhang

Four new alkaloids, arecatines A-D (1-4), were isolated from the peels of Areca catechu. Compound 1 is an unusual piperidine-pyridine hybrid alkaloid, whereas compounds 2-4 feature bis-piperidine alkaloids. Their structures were elucidated by UV, IR, HRESIMS, and NMR spectra analysis. The molecular docking analysis indicated that compound 3 exhibited the best binding affinity with the GABAA receptor, indicating its potential anti-epilepsy activity.

从儿茶属植物的果皮中分离出了四种新的生物碱,即儿茶碱 A-D(1-4)。化合物 1 是一种不常见的哌啶-吡啶混合生物碱,而化合物 2-4 则是双哌啶生物碱。通过紫外光谱、红外光谱、HRESIMS 和核磁共振光谱分析阐明了它们的结构。分子对接分析表明,化合物 3 与 GABAA 受体的结合亲和力最佳,表明其具有潜在的抗癫痫活性。
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引用次数: 0
A new canthinone glycoside isolated from the root barks of Ailanthus altissima with NO inhibitory activity 从具有 NO 抑制活性的 Ailanthus altissima 根皮中分离出一种新的 canthinone 苷。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-28 DOI: 10.1080/10286020.2024.2360047

One new canthinone glycoside (1), together with six known compounds (27) including three lignans (24), two coumarins (56) and one phenol (7) was isolated from the root barks of Ailanthus altissima. The structure of new compound 1 was established by the interpretation of UV, IR, MS and NMR data, while its absolute configuration was determined by acid hydrolysis and GIAO NMR calculations with DP4+ probability analysis. The inhibitory effects of all compounds on Nitric oxide (NO) production were investigated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Results showed that compounds 2 and 5 displayed NO production inhibitory activity with IC50 values of 30.1 and 15.3 μM, respectively.

从 Ailanthus altissima 的根皮中分离出了一种新的 canthinone 苷(1),以及六种已知化合物(2-7),包括三种木脂素(2-4)、两种香豆素(5-6)和一种酚(7)。通过解读紫外、红外、质谱和核磁共振数据,确定了新化合物 1 的结构;通过酸水解和 DP4+ 概率分析的 GIAO 核磁共振计算,确定了其绝对构型。在脂多糖(LPS)诱导的 RAW 264.7 细胞中,研究了所有化合物对一氧化氮(NO)产生的抑制作用。结果表明,化合物 2 和 5 具有抑制一氧化氮产生的活性,其 IC50 值分别为 30.1 和 15.3 μM。
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引用次数: 0
Design, synthesis and biological activity of oxyevodiamine-based histone deacetylase 6 inhibitors 基于氧代乙二胺的组蛋白去乙酰化酶 6 抑制剂的设计、合成和生物活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-26 DOI: 10.1080/10286020.2024.2362383
Histone deacetylase 6 (HDAC6) was a potential target for Alzheimer’s disease (AD). In this study, a series of novel oxyevodiamine-based HDAC6 inhibitors with a variety of linker moieties were designed, synthesized and evaluated. Compound 12 with a benzyl linker was identified as a high potent and selective HDAC6 inhibitor. It inhibited HDAC6 with an IC50 value of 6.2 nM and was more than 200 fold selectivity over HDAC1. It also had lower cytotoxicity and higher anti-H2O2 activity in vitro comparing with other derivatives. Compound 12 might be a good lead as novel HDAC6 inhibitor for the treatment of AD.
组蛋白去乙酰化酶6(HDAC6)是阿尔茨海默病(AD)的潜在靶点。本研究设计、合成并评估了一系列新型氧代乙二胺基 HDAC6 抑制剂,这些抑制剂具有多种连接基团。带有苄基连接基的化合物 12 被鉴定为一种高效力、高选择性的 HDAC6 抑制剂。它抑制 HDAC6 的 IC50 值为 6.2 nM,比 HDAC1 的选择性高出 200 多倍。与其他衍生物相比,它还具有更低的细胞毒性和更高的体外抗 H2O2 活性。化合物 12 可能是治疗注意力缺失症的新型 HDAC6 抑制剂。
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引用次数: 0
Enhancement of aqueous solubility of hesperidin and naringenin utilizing hydrotropic solubilization technique: characterization and in vitro evaluation 利用水力增溶技术提高橙皮甙和柚皮甙的水溶性:特征描述和体外评估。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-26 DOI: 10.1080/10286020.2024.2358831

The therapeutic potential of two important flavonoids, i.e. hesperidin and naringenin, remains unutilized due to pharmacokinetics issues, especially poor aqueous solubility. Hydrotropic solid dispersions with different agents like sodium salicylate, niacinamide, benzoic acid, and urea etc. can change the solubility profile of poorly soluble drugs. The current study investigated the potential of different hydrotropic agents in improving the solubility of both natural bioactives. The hydrotropic solid dispersion in 1:3 w/w drug: sodium salicylate ratio showed maximum solubility and dissolution amongst all the tested hydrotropes. This novel and economical approach could be explored for other poorly soluble pharmaceuticals.

由于药代动力学问题,尤其是水溶性差,橙皮甙和柚皮甙这两种重要黄酮类化合物的治疗潜力仍未得到充分利用。添加了水杨酸钠、烟酰胺、苯甲酸和尿素等不同药剂的水合固体分散体可以改变溶解性差的药物的溶解度曲线。目前的研究调查了不同的亲水剂在改善两种天然生物活性物质溶解度方面的潜力。在所有测试的水促剂中,药物与水杨酸钠重量比为 1:3 的水促剂固体分散体显示出最大的溶解度和溶解度。这种新颖而经济的方法可用于其他溶解性较差的药物。
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引用次数: 0
期刊
Journal of Asian Natural Products Research
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