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Genome mining for ribosomally synthesized and post-translationally modified peptides (RiPPs) in Streptomyces bacteria 链霉菌中核糖体合成和翻译后修饰肽（RiPPs）的基因组挖掘。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED
Journal of Asian Natural Products Research
Pub Date : 2024-08-13 DOI: 10.1080/10286020.2024.2390510
Abdullah Al Mamun , Khorshed Alam , Farjana Akter Koly , Farjana Showline Chaity , Jannatul Ferdous , Saiful Islam
Ribosomally synthesized post-translationally modified peptides (RiPPs) are a novel category of bioactive natural products (NPs). Streptomyces bacteria are a potential source of many bioactive NPs. Limited opportunities are available to characterize all the bioactive NP gene clusters. In this study, 410 sequences of Streptomyces were analyzed for RiPPs through genome mining using the National Center for Biotechnology Information (NCBI), by combining BAGEL and anti-SMASH. A total of 4098 RiPPs were found; including both classified (lanthipeptide, RiPP-like, bacteriocin, LAPs, lassopeptide, thiopeptides) and nonclassified RiPPs. Soil was identified as a rich habitat for RiPPs. These data may offer alternative future remedies for various health issues.
核糖体合成的翻译后修饰肽（RiPPs）是一类新型生物活性天然产物（NPs）。链霉菌是许多生物活性 NPs 的潜在来源。对所有生物活性 NP 基因簇进行表征的机会有限。本研究利用美国国家生物技术信息中心（NCBI）的基因组挖掘技术，结合 BAGEL 和 anti-SMASH，对 410 个链霉菌序列进行了 RiPPs 分析。总共发现了 4098 个 RiPPs；包括分类（lanthipeptide、RiPP-like、bacteriocin、LAPs、lassopeptide、thiopeptides）和非分类 RiPPs。土壤被确定为 RiPPs 的丰富栖息地。这些数据可为未来解决各种健康问题提供替代性疗法。
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引用次数: 0
Integrated ceRNAs regulating relationship and bioinformatics analysis to study the molecular mechanisms of the inhibition of puerarin on bladder cancer cell 综合ceRNAs调控关系和生物信息学分析，研究葛根素抑制膀胱癌细胞的分子机制。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED
Journal of Asian Natural Products Research
Pub Date : 2024-08-12 DOI: 10.1080/10286020.2024.2390508
Yu-Yang Ma , Wen Gao , Hao Wang , Hao Xu , Deng Pan , Jing-Kai Wang , Peng Xu , Hai-Luo Wang , Kun Pang
Based on previous experiments, we demonstrated puerarin inhibited the proliferation of BC T24 cells. To further explore the molecular mechanisms, whole transcriptome sequencing combined with bioinformatics analysis was performed. The results showed puerarin significantly inhibited T24 proliferation and pathway enrichment analysis of differentially expressed RNAs were mainly enriched in Cell cycle, PI3K/AKT, Ras family chromatin remodeling. lncRNAs and circRNAs may regulate miRNAs, thereby regulating the expression of ITGA1, PAK2 and UTRN. The predicted upstream transcription factor ERG and puerarin were well docked, which may be one of the underlying mechanisms by which puerarin inhibiting BC cells.
基于之前的实验，我们证实葛根素能抑制 BC T24 细胞的增殖。为了进一步探讨其分子机制，我们进行了全转录组测序和生物信息学分析。结果表明，葛根素能明显抑制T24细胞的增殖，其差异表达RNA的通路富集分析主要富集于细胞周期、PI3K/AKT、Ras家族染色质重塑。预测的上游转录因子ERG与葛根素有很好的对接，这可能是葛根素抑制BC细胞的潜在机制之一。
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引用次数: 0
Kaempferol inhibited invasion and metastasis of gastric cancer cells by targeting AKT/GSK3β pathway based on network pharmacology and molecular docking 基于网络药理学和分子对接的山奈酚通过靶向AKT/GSK3β通路抑制胃癌细胞的侵袭和转移
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED
Journal of Asian Natural Products Research
Pub Date : 2024-08-10 DOI: 10.1080/10286020.2024.2387756
Xia-Qing Gao , Hai-Long Li , Meng Wang , Chun-Ting Yang , Rong Su , Li-Hua Shao
This study aims to explore the mechanisms of the inhibitory effect of kaempferol on the invasion and metastasis of gastric cancer (GC) cells through network pharmacology prediction and experimental verification. It identifies core targets via PPI network analysis and finds that kaempferol binds to these targets well. In vitro experiments showed that kaempferol could inhibit the proliferation, colony formation, migration and invasion of GC cells. Western blotting indicated kaempferol may reduce AKT and GSK3β phosphorylation, leading to lower expression of invasion-related genes SRC, MMP9, CXCR4, KDR, and MMP2. Overall, kaempferol may prevent migration and invasion of GC cells via the AKT/GSK3β signaling pathway.
本研究旨在通过网络药理学预测和实验验证，探索山奈酚抑制胃癌细胞侵袭和转移的作用机制。该研究通过PPI网络分析确定了核心靶点，并发现山奈酚能很好地与这些靶点结合。体外实验表明，山奈酚能抑制胃癌细胞的增殖、集落形成、迁移和侵袭。Western 印迹显示山奈酚可降低 AKT 和 GSK3β 的磷酸化，从而降低与侵袭相关的基因 SRC、MMP9、CXCR4、KDR 和 MMP2 的表达。总之，山奈酚可通过 AKT/GSK3β 信号通路阻止 GC 细胞的迁移和侵袭。
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引用次数: 0
Four new lycoctonine-type C19-diterpenoid alkaloids from the whole plants of Delphinium kamaonense. 从Delphinium kamaonense全株中提取的四种新的莱克多宁型C19-二萜生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED
Journal of Asian Natural Products Research
Pub Date : 2024-07-31 DOI: 10.1080/10286020.2024.2385370
Xing-Yao Li, Rui-Sheng Chen, Guo-Chang Li, Kai-Cheng Du, Lan-Tao Lai, Yu-Meng Wang, Da-Li Meng

Four new lycoctonine-type C19-diterpenoid alkaloids kamaonensines H-K (1-4) have been isolated from the whole plants of Delphinium kamaonense, together with 12 known compounds (5-16). Interestingly, kamaonensines 1-3 contained a rare nitrone (immine N-oxide) moiety, respectively. Their structures were established by spectroscopic analyses. The active evaluation of compounds (1-16) by LPS induced RAW 264.7 macrophages showed that compounds 4 and 8 displayed strong anti-inflammatory activities. While compounds 11 and 12 also showed strong cytotoxicities by the RAW 264.7 cell viability assay.

从 Delphinium kamaonense 的整株植物中分离出了四种新的莱菔子碱型 C19-二萜生物碱 kamaonensines H-K（1-4），以及 12 种已知化合物（5-16）。有趣的是，Kamaonensines 1-3 分别含有一个罕见的腈酮（亚胺 N-氧化物）分子。通过光谱分析确定了它们的结构。通过 LPS 诱导的 RAW 264.7 巨噬细胞对化合物（1-16）的活性评估表明，化合物 4 和 8 具有很强的抗炎活性。而化合物 11 和 12 在 RAW 264.7 细胞活力测定中也显示出很强的细胞毒性。
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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
Journal of Asian Natural Products Research
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
Correction. 更正。
IF 1.7 3区 医学 Q3 CHEMISTRY, APPLIED
Journal of Asian Natural Products Research
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
Journal of Asian Natural Products Research
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
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
Journal of Asian Natural Products Research
Pub Date : 2024-06-28 DOI: 10.1080/10286020.2024.2360047

One new canthinone glycoside (1), together with six known compounds (2–7) including three lignans (2–4), two coumarins (5–6) 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
Journal of Asian Natural Products Research
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
Journal of Asian Natural Products Research
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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