Phytochemistry最新文献_第10页

Insights into terpenes profiling and transcriptional analyses during flowering of different Cannabis sativa L. chemotypes 不同大麻化学型开花期间萜烯分析和转录分析的启示。

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-10-05 DOI: 10.1016/j.phytochem.2024.114294

Flavia Fulvio , Ylenia Pieracci , Roberta Ascrizzi , Laura Bassolino , Guido Flamini , Roberta Paris

Terpenes, volatile compounds known for their aromatic and therapeutic properties, play a pivotal role in shaping the overall chemical profile of Cannabis sativa L. Their biosynthesis in planta occurs in trichomes and involves the 2-C-methyl-D-erythritol 4-phosphate (MEP) and the mevalonic acid (MVA) pathways, responsible for producing the substrates utilized by a family of enzymes, the terpene synthases (TPS), for terpene production. In this work, a comprehensive approach combining chemical analyses of the volatile compounds characterizing the aroma of the inflorescences three C. sativa genotypes collected at three stages of maturity and the transcriptional analyses of key genes involved in the terpene biosynthesis was adopted to study this pathway. The results revealed different terpene profiles among genotypes, which were characterized by peculiar compounds belonging to the sesqui- (CINBOL and Fibrante) or monoterpene (Ermo) categories. Both structural and putative regulatory genes were analysed by RT-qPCR, revealing distinct transcriptional profiles of Terpene Synthases, contributing to the diversity of mono and sesquiterpenes synthesized. Furthermore, the research delved into potential regulatory genes associated with trichome formation, a crucial factor influencing terpene accumulation. This integrated approach highlighted complex mechanisms governing terpene accumulation in cannabis, while also offering potential regulators putatively involved in this pathway.

萜烯是一种挥发性化合物，以其芳香和治疗特性而闻名，在形成大麻（Cannabis sativa L）的整体化学特征方面发挥着关键作用。萜烯在植物体内的生物合成发生在毛状体中，涉及 2-C-甲基-D-赤藓糖醇 4-磷酸（MEP）和甲羟戊酸（MVA）途径，负责生产萜烯合成酶（TPS）家族利用的底物。在这项工作中，采用了一种综合方法来研究这一途径，该方法结合了在三个成熟阶段采集的三种 C. sativa 基因型花序香气特征的挥发性化合物的化学分析，以及参与萜烯生物合成的关键基因的转录分析。研究结果显示，不同基因型的萜烯含量不同，其特征是属于倍半萜（CINBOL 和 Fibrante）或单萜烯（Ermo）类别的特殊化合物。通过 RT-qPCR 分析了结构基因和假定的调控基因，发现萜烯合成酶的转录特征各不相同，从而导致了单萜和倍半萜合成的多样性。此外，该研究还深入研究了与毛状体形成相关的潜在调控基因，毛状体形成是影响萜烯积累的关键因素。这种综合方法强调了大麻中萜烯积累的复杂机制，同时也提供了可能参与这一途径的潜在调控因子。

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引用次数: 0

Chevalierlin: A spirocyclic alkaloid from a hydrothermal vent associated fungus Aspergillus chevalieri TW132-65 Chevalierlin：一种来自热液喷口伴生真菌 Aspergillus chevalieri TW132-65 的螺环生物碱。

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-10-03 DOI: 10.1016/j.phytochem.2024.114295

Jihua Wei , Xuexia Chen , Yihan Ma , Bin Wu

A previously undescribed spirodiketopiperazine-indole alkaloid, chevalierlin (1), two pairs of previously undescribed dihydroisocoumarin enantiomers eurotiumides H–I (2–3), as well as six related known compounds (4–9) were isolated from the culture of a hydrothermal vent associated fungus Aspergillus chevalieri TW132-65. Their structures were unambiguously determined by NMR, mass spectrometry, and ECD calculations. Chevalierlin (1) exhibits moderate cytotoxic activities with IC₅₀ values of 6.20 ± 0.05 μM and 7.68 ± 0.01 μM against Namalwa and Raji cell lines.

从一种与热液喷口有关的真菌 Aspergillus chevalieri TW132-65 的培养物中分离出了一种以前未曾描述过的螺二酮哌嗪吲哚生物碱 chevalierlin (1)、两对以前未曾描述过的二氢异香豆素对映体 eurotiumides H-I (2-3) 以及六种相关的已知化合物 (4-9)。通过核磁共振、质谱和 ECD 计算，这些化合物的结构被明确确定。Chevalierlin (1) 对 Namalwa 和 Raji 细胞株具有中等程度的细胞毒性活性，IC50 值分别为 6.20 ± 0.05 μM 和 7.68 ± 0.01 μM。

引用次数: 0

LC–MS coupled with diagnostic ion strategy facilitated the discovery of 5-methylcoumarin meroterpenoids from Gerbera piloselloides 液相色谱-质谱联用诊断离子策略有助于从非洲菊中发现 5-甲基香豆素类萜物。

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-10-02 DOI: 10.1016/j.phytochem.2024.114296

Shi-lin Chen , Ha Gao , Chen-xu Zhao, Tao Zhang, Zhong-mei Zou

Plant-derived natural products remain crucial in drug development. However, the identification of undescribed natural products is becoming increasingly challenging. A comprehensive strategy combining LC–MS with diagnostic ions was proposed for the discovery of undescribed 5-methylcoumarin meroterpenoids. Thirteen undescribed 5-methylcoumarin meroterpenoids, including five pairs of enantiomers (1a/1b and 5a/5b–8a/8b), were isolated from the whole plant of Gerbera piloselloides. Their structures and absolute configurations were unambiguously determined based on their spectroscopic data, calculated and experimental ECD data and X-ray diffraction analysis. Bioassays conducted on scopolamine-induced injury PC12 cells revealed that compounds 5a/5b, 7a/7b and 8a/8b possessed mild protective effects. Additionally, compounds 2 and 8 showed notable IL-6 inhibition in lipopolysaccharide-induced BEAS-2B cells.

植物提取的天然产品在药物开发中仍然至关重要。然而，鉴定未被描述的天然产品正变得越来越具有挑战性。研究人员提出了一种将 LC-MS 与诊断离子相结合的综合策略，用于发现未被描述的 5-甲基香豆素类双萜类化合物。从非洲菊（Gerbera piloselloides）全株中分离出 13 个未被描述的 5-甲基香豆素类萜物，包括五对对映体（1a/1b 和 5a/5b-8a/8b ）。根据光谱数据、计算和实验 ECD 数据以及 X 射线衍射分析，明确确定了它们的结构和绝对构型。在东莨菪碱诱导损伤的 PC12 细胞上进行的生物测定显示，化合物 5a/5b、7a/7b 和 8a/8b 具有轻微的保护作用。此外，化合物 2 和 8 在脂多糖诱导的 BEAS-2B 细胞中显示出显著的 IL-6 抑制作用。

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引用次数: 0

Chemical constituents from marine medicinal brown alga-derived Scytalidium lignicola SC228 从海洋药用褐藻中提取的化学成分 Scytalidium lignicola SC228。

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-29 DOI: 10.1016/j.phytochem.2024.114289

Hsiao-Yang Hsi , George Hsiao , Shih-Wei Wang , Shu-Jung Huang , Tzong-Huei Lee

In this study, a marine medicinal brown alga Sargassum cristaefolium-derived fungal strain Scytalidium lignicola SC228 has been isolated and identified. Column chromatography of the extracts from liquid-fermented products of the fungal strain was carried out, and led to the purification of eight compounds. Their structures were characterized by spectroscopic analysis, and the absolute configurations were further established by single X-ray diffraction analysis and modified Mosher's method as four previously undescribed compounds, namely scytabenzofurans A–C (1–3), and (3S,4S)-5-chloro-3,4-dihydro-4,6,8-trihydroxy-3-methyl-1H-2-benzopyran-1-one (4), along with four known compounds 5–8. All the isolates were subjected to anti-inflammatory and anti-angiogenic assays. Compounds 1–4, 7, and 8 showed moderate nitric oxide production inhibitory activities in lipopolysaccharide-activated BV-2 microglial cells with IC₅₀ in the range of 19.6 ± 0.1 to 49.0 ± 1.2 μM in comparison with that of curcumin (IC₅₀ = 2.7 ± 0.3 μM). Compounds 5–7 exhibited moderate to potent inhibitory effects on EPCs growth with IC₅₀ in the range of 0.5 ± 0.1 to 42.7 ± 0.9 μM as compared to sorafenib (IC₅₀ = 5.50 ± 1.50 μM).

本研究分离并鉴定了一种海洋药用褐藻马尾藻（Sargassum cristaefolium）衍生真菌菌株Scytalidium lignicola SC228。研究人员对该真菌菌株液体发酵产物的提取物进行了柱层析，最终纯化出 8 种化合物。通过光谱分析确定了它们的结构特征，并通过单 X 射线衍射分析和改进的莫舍尔法进一步确定了它们的绝对构型，即四种以前未曾描述过的化合物，即鞘氨醇 A-C （1-3）和 (3S,4S)-5-氯-3,4-二氢-4,6,8-三羟基-3-甲基-1H-2-苯并吡喃-1-酮（4），以及四种已知化合物 5-8。所有分离物都进行了抗炎和抗血管生成试验。与姜黄素（IC50 = 2.7 ± 0.3 μM）相比，化合物 1-4、7 和 8 在脂多糖激活的 BV-2 微神经胶质细胞中显示出中等程度的一氧化氮生成抑制活性，IC50 在 19.6 ± 0.1 到 49.0 ± 1.2 μM之间。与索拉非尼（IC50 = 5.50 ± 1.50 μM）相比，化合物 5-7 对 EPCs 的生长具有中度到强效的抑制作用，IC50 在 0.5 ± 0.1 到 42.7 ± 0.9 μM之间。

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引用次数: 0

Targeted isolation of lignans from the roots of Anthriscus sylvestris (L.) Hoffm. by small molecule accurate recognition technology 利用小分子精确识别技术，有针对性地从西洋蒽（L. Hoffm.）根中分离木质素。

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-28 DOI: 10.1016/j.phytochem.2024.114293

Yan-ling Liu , Yan-gang Cao , Ya-juan Zheng , Ying Niu , Lan Chen , Xu Chen , Xin-yi Ma , Xiang-da Li , Xiao-ke Zheng , Wei-sheng Feng

Five undescribed lignans (1–5), along with sixteen known lignans (6–21), were isolated from the roots of Anthriscus sylvestris using small molecule accurate recognition technology (SMART). The structures of the isolated compounds were determined by comprehensive spectroscopic analyses, and the absolute configurations of compounds 3–5 were elucidated by comparison of their calculated and experimental ECD spectra. Compounds 5, 14−15, 19, and 21 exhibited significantly inhibitory effects against hypoxia-stimulated abnormal proliferation of pulmonary arterial smooth muscle cells (PASMCs). Moreover, compounds 5, 14−15, 19, and 21 can significantly restore expression of expression of PASMCs proliferation-related protein, including α-SMA, PCNA, P27, and CyclinD3, which are closely related to cell proliferation.

利用小分子精确识别技术（SMART）从芒柄蜡草（Anthriscus sylvestris）根部分离出了五种未被描述的木质素（1-5）和十六种已知的木质素（6-21）。通过全面的光谱分析确定了分离化合物的结构，并通过比较计算和实验 ECD 光谱阐明了化合物 3-5 的绝对构型。化合物 5、14-15、19 和 21 对缺氧刺激的肺动脉平滑肌细胞（PASMCs）的异常增殖有明显的抑制作用。此外，化合物 5、14-15、19 和 21 还能明显恢复 PASMCs 增殖相关蛋白的表达，包括与细胞增殖密切相关的 α-SMA、PCNA、P27 和 CyclinD3。

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引用次数: 0

Structurally diversified sesquiterpenoids from Chloranthus henryi and their neuroprotective activities on H2O2 damaged PC12 cells 来自 Chloranthus henryi 的结构多样的倍半萜类化合物及其对 H2O2 损伤的 PC12 细胞的神经保护活性

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-26 DOI: 10.1016/j.phytochem.2024.114292

Meng-Li He , Lian-Lian Xu , Yang Liu , Yan-Ping Gao , Yong-Ming Luo , Rong-Cai Yue , Fang-You Chen

Fifteen undescribed sesquiterpenoid monomers, including six pairs of sesquiterpenoid enantiomers (1a/1b–3a/3b and 5a/5b–7a/7b) and three analogues (4, 8, and 9), together with two known sesquiterpenoid dimers (10 and 11) were isolated from the whole plant of Chloranthus henryi Hemsl. Their structures were characterized by spectroscopic data analysis, ECD calculations, and single crystal X-Ray diffractions. Compounds 1a and 1b were highly aromatic cadinane-type sesquiterpenoids. At a concentration of 10 μM, compounds 8, 10, and 11 exhibited potent neuroprotective activity against H₂O₂-induced PC12 cell damage. Compounds 10 and 11 significantly decreased the level of ROS. In addition, compound 11 increased the levels of p-AMPK, p-SIRT1, and SIRT3 in the H₂O₂-induced PC12 cell damage via activated the AMPK/SIRT signaling pathway.

从 Chloranthus henryi Hemsl 的全草中分离出了 15 种未曾描述过的倍半萜单体，包括六对倍半萜对映体（1a/1b-3a/3b 和 5a/5b-7a/7b）和三种类似物（4、8 和 9），以及两种已知的倍半萜二聚体（10 和 11）。通过光谱数据分析、ECD 计算和单晶 X 射线衍射，对它们的结构进行了表征。化合物 1a 和 1b 是高度芳香的卡迪那类倍半萜化合物。在 10 μM 的浓度下，化合物 8、10 和 11 对 H2O2 诱导的 PC12 细胞损伤有很强的神经保护活性。化合物 10 和 11 能明显降低 ROS 的水平。此外，在 H2O2- 诱导的 PC12 细胞损伤中，化合物 11 通过激活 AMPK/SIRT 信号通路，提高了 p-AMPK、p-SIRT1 和 SIRT3 的水平。

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引用次数: 0

Chemical constituents with their alpha-glucosidase inhibitory activity from the whole plant of Ceratophyllum demersum 叶枯素全草中的化学成分及其α-葡萄糖苷酶抑制活性

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-25 DOI: 10.1016/j.phytochem.2024.114290

Thuc-Huy Duong , Thammarat Aree , Thi-Kim-Dung Le , Van-Son Dang , Ngoc-Hong Nguyen , Jirapast Sichaem

From Ceratophyllum demersum growing in Vietnam, twelve compounds were isolated and structurally elucidated, including six previously undescribed compounds, demersones A-D (1–4), acetylvelutins A and B (8 and 9), together with six known compounds, (+)-cyclocolorenone (5), 1-hydroxycyclocolorenone (6), 10-hydroxycyclocolorenone (7), retusin (10), betulinic acid (11), and lupeol (12). The chemical structures and stereochemistry of 1–12 were identified through analysis of spectroscopic data (1D and 2D NMR and HRESIMS), ECD data, and DFT calculation. Notably, this is the first time that humulene-type (1 and 2), guaiane-type (3), and aromadendrane-type (4–7) sesquiterpenoids have been reported in this genus. Compounds 8 and 9 are the first examples of 8-acetoxyflavones found in nature. Upon evaluation of the alpha-glucosidase of 1–3 and 5–12, it was found that 12 exhibited the highest potential with an IC₅₀ value of 15.4 ± 1.1 μM. The molecular docking of 3 and 8 was further studied.

从生长在越南的 Ceratophyllum demersum 中分离并阐明了 12 种化合物的结构，其中包括 6 种以前未曾描述过的化合物 demersones A-D (1-4)、乙酰绒毛素 A 和 B (8 和 9)，以及 6 种已知化合物 (+)-cyclocolorenone (5)、1-hydroxycyclocolorenone (6)、10-hydroxycyclocolorenone (7)、retusin (10)、betulinic acid (11) 和 lupeol (12)。通过分析光谱数据（1D 和 2D NMR 以及 HRESIMS）、ECD 数据和 DFT 计算，确定了 1-12 的化学结构和立体化学性质。值得注意的是，这是该属首次报道胡芦巴烯型（1 和 2）、愈创木烯型（3）和芳香丹烯型（4-7）倍半萜化合物。化合物 8 和 9 是自然界中首次发现的 8-乙酰氧基黄酮类化合物。在对 1-3 和 5-12 的α-葡萄糖苷酶进行评估后发现，12 表现出最高的潜力，其 IC50 值为 15.4 ± 1.1 μM。对 3 和 8 的分子对接进行了进一步研究。

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引用次数: 0

Maeruines A−E, elusive indole alkaloids from stems of Maerua siamensis and their inhibitory effects on cyclooxygenases and HT-29 colorectal cancer cell proliferation 茜草茎中难以捉摸的吲哚生物碱 Maeruines A-E 及其对环氧化酶和 HT-29 大肠癌细胞增殖的抑制作用

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-24 DOI: 10.1016/j.phytochem.2024.114291

Sasiwimon Nukulkit , Nonthaneth Nalinratana , Thammarat Aree , Utid Suriya , Rutt Suttisri , Nitra Nuengchamnong , Hsun-Shuo Chang , Chaisak Chansriniyom

Five previously undescribed indole alkaloids, maeruines A−E (1−5), bearing imino-2H-thieno[2,3-b]indol-3(8H)-one skeleton, were obtained from the stems of Maerua siamensis. Their chemical structures were elucidated using spectroscopic techniques [NMR, MS, IR, and UV], and single-crystal X-ray diffraction. Maeruine D (4) displayed selective cyclooxygenase-2 (COX-2) inhibitory activity in vitro with an IC₅₀ of 29.72 ± 6.36 μM. Molecular dynamics simulations revealed that maeruine D could form a stable complex with human COX-2, predominantly driven by hydrophobic interactions. In addition, five amino-acid residues including Val349, Leu352, Leu384, Val523, and Ala527 were identified as hot-spot ones, which may lead to high binding affinity and selectivity. Furthermore, it exhibited cytotoxicity against HT-29 colorectal cancer cells with an IC₅₀ of 29.32 ± 4.76 μM, and, at 0.1−10 μM, significantly inhibited their proliferation, induced by the proinflammatory cytokine interleukin-1β (IL-1β), in a dose-dependent manner.

从暹罗缅菊的茎中获得了五种以前未曾描述过的吲哚生物碱--缅菊碱 A-E（1-5），它们具有亚氨基-2H-噻吩并[2,3-b]吲哚-3(8H)-酮骨架。利用光谱技术[核磁共振、质谱、红外光谱和紫外光谱]和单晶 X 射线衍射法阐明了它们的化学结构。Maeruine D（4）在体外显示出选择性环氧化酶-2（COX-2）抑制活性，其 IC50 为 29.72 ± 6.36 μM。分子动力学模拟显示，maeruine D 能与人 COX-2 形成稳定的复合物，主要是由疏水相互作用驱动的。此外，包括 Val349、Leu352、Leu384、Val523 和 Ala527 在内的五个氨基酸残基被确定为热点残基，这可能会导致高结合亲和力和选择性。此外，它对 HT-29 大肠癌细胞具有细胞毒性，IC50 为 29.32 ± 4.76 μM，并且在 0.1-10 μM 的剂量下，能显著抑制由促炎细胞因子白细胞介素-1β（IL-1β）诱导的细胞增殖，且呈剂量依赖性。

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引用次数: 0

Non-alkaloid components with inhibitory activity against LPS induced NO production in RAW 264.7 cells isolated from the roots of Sophora flavescens 从槐树根中分离出的具有抑制 LPS 诱导 RAW 264.7 细胞产生 NO 活性的非生物碱成分

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-19 DOI: 10.1016/j.phytochem.2024.114288

Yang Xu , Jinxia Chen , Yuxia Li , Dejuan Sun , Hua Li , Lixia Chen

Sophora flavescens Aiton is a plant in the Leguminosae family. As a traditional Chinese medicine, it is used to treat eczema, bloody stool, skin pruritus, and so on. By studying non-alkaloid components in the roots of S. flavescens, we obtained a total of 49 compounds (1–49), including three undescribed flavonoids (13, 15 and 18), five undescribed isopentenyl flavonoids (32, 34, 38, 39 and 48), two known coumarins (1–2), three phenolic acids (3–5), one known isopentenyl flavonoids (19–31, 33, 35–37, 40–47 and 49). On the basis of chemical evidences and spectral data analysis (UV, ECD, Optical rotation data, 1D/2D-NMR and HR-ESI-MS), the structures of undescribed compounds were elucidated. The inhibitory effect of compounds 1–49 on LPS induced NO production in RAW 264.7 cells was detected. Compounds 11, 19, 21–24, and 28–30 showed significant inhibitory effects, and the IC₅₀ values of compounds 11 and 22 even reached 4.58 ± 0.66 and 4.53 ± 0.66 μM. This study suggests that flavonoids may be the main component that exerts anti-inflammatory effects in the non-alkaloid extraction layer of the extract from the roots of S. flavescens.

Sophora flavescens Aiton 是豆科植物。作为一种传统中药，它可用于治疗湿疹、便血、皮肤瘙痒症等。通过研究 S. flavescens 根中的非生物碱成分，我们共获得了 49 个化合物（1-49），其中包括 3 个未被描述的黄酮类化合物（13、15 和 18）、5 个未被描述的异戊烯基黄酮类化合物（32、34、38、39 和 48）、2 个已知的香豆素类化合物（1-2）、3 个酚酸类化合物（3-5）、1 个已知的异戊烯基黄酮类化合物（19-31、33、35-37、40-47 和 49）。根据化学证据和光谱数据分析（紫外光谱、电子衍射光谱、光学旋转数据、1D/2D-NMR 和 HR-ESI-MS），阐明了未描述化合物的结构。检测了化合物 1-49 对 RAW 264.7 细胞中 LPS 诱导的 NO 生成的抑制作用。化合物 11、19、21-24 和 28-30 具有显著的抑制作用，化合物 11 和 22 的 IC50 值甚至达到了 4.58 ± 0.66 和 4.53 ± 0.66 μM。这项研究表明，黄酮类化合物可能是银莲花根提取物非生物碱提取层中发挥抗炎作用的主要成分。

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引用次数: 0

Steroidal constituents in the whole plants of Helleborus niger and their cytotoxic activity in vitro 黑僵菌全株中的类固醇成分及其体外细胞毒性活性

IF 3.2 2区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Phytochemistry

Pub Date : 2024-09-12 DOI: 10.1016/j.phytochem.2024.114272

Yuka Yoshizawa, Akihito Yokosuka, Mina Inomata, Tomoki Iguchi, Yoshihiro Mimaki

Phytochemical investigation of the whole plants of Helleborus niger L. (Ranunculaceae) resulted in the isolation of five undescribed compounds, including one bufadienolide (1), two bufadienolide rhamnosides (2 and 3), and two ecdysteroids (12 and 13), along with eight known compounds (4–11). The chemical structures of 1–3, 12, and 13 were determined by spectroscopic studies, including 2D NMR, and chromatographic and spectroscopic analyses of the hydrolyzed products. Compounds 1–13 were evaluated for their cytotoxic activity against HL-60 human leukemia cells, A549 human lung adenocarcinoma cells, SBC-3 human small-cell lung cancer cells, and TIG-3 human normal diploid lung cells. Compounds 1–12 showed cytotoxic activity against HL-60, A549, and SBC-3 cells, with IC₅₀ values ranging from 0.0016 to 6.1 μM. Bufadienolide rhamnoside 2 exhibited potent cell proliferation inhibitory activity against SBC-3 cells after 24–48 h of treatment and apoptosis-inducing activity in SBC-3 cells via an intrinsic pathway after 72 h of treatment. The JFCR39 panel screening of 2 suggests that the molecular target of 2 is Na⁺,K⁺-ATPase.

通过对黑毛笔（Ranunculaceae）全株进行植物化学研究，分离出了五种未曾描述过的化合物，包括一种布法迪内酯（1）、两种布法迪内酯鼠李糖苷（2 和 3）、两种蜕皮甾苷（12 和 13），以及八种已知化合物（4-11）。通过光谱研究（包括二维核磁共振）以及水解产物的色谱和光谱分析，确定了 1-3、12 和 13 的化学结构。评估了化合物 1-13 对 HL-60 人类白血病细胞、A549 人类肺腺癌细胞、SBC-3 人类小细胞肺癌细胞和 TIG-3 人类正常二倍体肺细胞的细胞毒活性。化合物 1-12 对 HL-60、A549 和 SBC-3 细胞具有细胞毒性活性，IC50 值从 0.0016 到 6.1 μM。处理 24-48 小时后，Bufadienolide 鼠李糖苷 2 对 SBC-3 细胞具有强效的细胞增殖抑制活性；处理 72 小时后，Bufadienolide 鼠李糖苷 2 通过内在途径诱导 SBC-3 细胞凋亡。对 2 的 JFCR39 小组筛选表明，2 的分子靶点是 Na+，K+-ATPase。

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引用次数: 0