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Effect of Ilex hainanensis Merr. On HFD-induced nonalcoholic fatty liver disease and rebalance of gut microbiota and bile acids metabolism in mice Ilex hainanensis Merr.对高密度脂蛋白胆固醇诱导的非酒精性脂肪肝以及小鼠肠道微生物群和胆汁酸代谢的再平衡的影响
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-12 DOI: 10.1016/j.fitote.2024.106186

Nonalcoholic fatty liver disease (NAFLD) is a clinicopathological syndrome characterized by excessive intracellular fat deposition in the hepatocytes, and the development is exacerbated by gut microbiota and bile acids metabolism disorders. Ilex hainanensis Merr. is a traditional medicine of the Zhuang nationality, historically esteemed for its efficacy in lowering blood pressure and lipid levels. This study aimed to investigate the pharmacodynamic effects in NAFLD mice and impacts on gut microbiota and bile acids (BAs) metabolism of I. hainanensis extract (IHA). 16 compounds were identified from IHA by HPLC-DAD-MS analysis. IHA significantly reduced body weight indexs, alanine transaminase (ALT) and aspartate transaminase (AST) activities, improved dyslipidemia and insulin resistance (IR), and effectively ameliorated hepatic steatosis in HFD-induced NAFLD mice. IHA also altered gut microbiota composition, particularly enhancing the abundance of bacteria involved in BAs metabolism, as well as augmented BAs synthesis in the liver and increased fecal excretion. In conclusion, our findings suggest that IHA holds promise in improving NAFLD conditions and modulating gut microbiota and BAs metabolism. These insights contribute to a deeper understanding of the mechanisms underlying IHA-mediated alleviation of lipid accumulation in NAFLD.

非酒精性脂肪肝(NAFLD)是一种以肝细胞内脂肪过度沉积为特征的临床病理综合征,肠道微生物群和胆汁酸代谢紊乱会加剧该病的发展。Ilex hainanensis Merr.是壮族的传统药材,历来被推崇为降血压、降血脂的良药。本研究旨在探讨海南藤提取物(IHA)对非酒精性脂肪肝小鼠的药效学作用以及对肠道微生物群和胆汁酸代谢的影响。通过 HPLC-DAD-MS 分析,从 IHA 中鉴定出 16 种化合物。IHA能明显降低高氟酸膳食诱导的非酒精性脂肪肝小鼠的体重指数、丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)活性,改善血脂异常和胰岛素抵抗(IR),并有效改善肝脏脂肪变性。IHA 还改变了肠道微生物群的组成,特别是提高了参与 BAs 代谢的细菌的丰度,并促进了肝脏中 BAs 的合成和粪便排泄量的增加。总之,我们的研究结果表明,IHA 有望改善非酒精性脂肪肝的状况,调节肠道微生物群和 BAs 代谢。这些见解有助于加深对 IHA 介导的非酒精性脂肪肝脂质积累缓解机制的理解。
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引用次数: 0
[1–7-NαC]-Crocaorb A1 and A2, orbitides from the latex of Croton campanulatus [1-7-NαC]-Crocaorb A1 和 A2,从巴豆乳汁中提取的眶苷。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-12 DOI: 10.1016/j.fitote.2024.106183

Two new heptapeptides, [1–7-NαC]-crocaorbs A1 (1) and A2 (2), were isolated from the latex of Croton campanulatus. Their structures were determined using NMR spectroscopic techniques, ESI-HRMS data, Marfey's method, and further refined using molecular dynamics with simulated annealing (MD/SA). Molecular dynamics calculations of peptides 1 and 2 demonstrated greater stability in simulations using a biological solvent compared to those using DMSO. Compound 1, the most abundant peptide in latex, was assessed for NO production, antiplasmodial and cytotoxicity activities. The peptide significantly increased nitric oxide (NO) production at concentrations of 40, 20 or 10 μM (17.932 ± 1.1, 18.270 ± 0.9, 18.499 ± 0.7, respectively). Its antiplasmodial activity exhibited limited efficacy, with only 5% inhibition of Plasmodium falciparum 3D7 growth at a concentration of 50 μM. Also, it exhibited no cytotoxic effects in the J774A.1 murine macrophages cell line. This study represents the first report of a phytochemical investigation of the species C. campanulatus, which showed orbitides with distinctive sequences in contrast to other peptides described for the genus Croton and contributes to the study of structural diversity within this particular class of compounds.

从巴豆的乳汁中分离出了两种新的七肽--[1-7-NαC]-crocaorbs A1 (1) 和 A2 (2)。利用核磁共振光谱技术、ESI-HRMS 数据和 Marfey 方法确定了它们的结构,并利用模拟退火(MD/SA)分子动力学进一步完善了它们的结构。肽 1 和肽 2 的分子动力学计算表明,与使用 DMSO 的模拟相比,使用生物溶剂的模拟具有更高的稳定性。化合物 1 是乳胶中含量最高的多肽,对其进行了氮氧化物生成、抗痉挛和细胞毒性活性评估。在浓度为 40、20 或 10 μM 时,该肽能明显增加一氧化氮(NO)的产生(分别为 17.932 ± 1.1、18.270 ± 0.9、18.499 ± 0.7)。其抗疟原虫活性的效力有限,在浓度为 50 μM 时,对恶性疟原虫 3D7 生长的抑制率仅为 5%。此外,它对 J774A.1 小鼠巨噬细胞系也没有细胞毒性作用。这项研究是对 C. campanulatus 这一物种进行植物化学调查的首次报告,与 Croton 属的其他肽相比,该物种的眶苷具有独特的序列,有助于研究这一类特殊化合物的结构多样性。
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引用次数: 0
Unveiling the hidden potential: Above-ground parts of Paris yunnanensis Franch. Is promise as an anti-acne therapeutic beyond traditional medicinal sites 揭开隐藏潜力的面纱:云南帕里斯(Paris yunnanensis Franch.作为一种抗痤疮疗法,它的前景超出了传统的药用范围。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-10 DOI: 10.1016/j.fitote.2024.106179

The dried rhizomes of Paris yunnanensis Franch. have been extensively utilized in traditional Chinese medicine as hemostatic, antitumor, and antimicrobial agents. An examination of classical texts and renowned Chinese medical formulations showcased its efficacy in acne treatment. Presently, there is a significant scarcity of Paris resources. Consider directing attention towards the non-medicinal parts of Paris to mitigate the strain on medicinal resources within this realm. To address these resource limitations, this study investigated the bioactivity and pharmacodynamics of the above-ground parts of Paris (AGPP). A synergistic approach integrating network pharmacology, molecular docking (in silico validation), and animal experimentation (in vivo validation) was employed to elucidate the potential mechanisms underlying the efficacy of AGPP against acne vulgaris in this study. The active constituents in AGPP extracts were identified via UHPLC-Q-Orbitrap HRMS analysis, with their targets extracted for network pharmacological analysis. KEGG pathway analysis unveiled potential therapeutic mechanisms, validated through molecular docking and rat auricular acne model experiments. Comprehensive chemical characterization revealed fifty constituents, including steroidal saponins, flavonoids, amino acids, organic acids, phytohormones, phenolic acids, and alkaloids. Diosgenin, Quercetin, Kaempferol, Ecdysone, and α-linolenic acid were identified as main constituents with acne-treating potential. Core targets included SRC, MAPK3, and MAPK1, with key signaling pathways implicated. Histologically, AGPP mitigated acne-induced follicular dilatation and inflammation, inhibiting inflammatory cytokine production (IL-6, IL-1β, TNF-α). This study offers insight into AGPP's mechanism for acne treatment, laying groundwork for Paris development and drug discovery.

云南白药(Paris yunnanensis Franch.)的干燥根茎在传统中药中被广泛用作止血、抗肿瘤和抗菌剂。对古典文献和著名中药配方的研究表明,它对治疗痤疮有很好的疗效。目前,巴黎资源十分匮乏。可考虑将注意力转向巴黎的非药用部分,以减轻该领域药用资源的压力。针对这些资源限制,本研究调查了巴黎地上部分(AGPP)的生物活性和药效学。本研究采用了网络药理学、分子对接(硅学验证)和动物实验(体内验证)相结合的协同方法,以阐明 AGPP 对寻常痤疮具有疗效的潜在机制。通过超高效液相色谱-Q-Orbitrap HRMS分析鉴定了AGPP提取物中的活性成分,并提取其靶标进行网络药理学分析。KEGG 通路分析揭示了潜在的治疗机制,并通过分子对接和大鼠耳廓痤疮模型实验进行了验证。综合化学特性分析揭示了 50 种成分,包括甾体皂苷、黄酮类、氨基酸、有机酸、植物激素、酚酸和生物碱。经鉴定,薯蓣皂苷、槲皮素、山柰酚、蜕皮激素和α-亚麻酸是具有治疗痤疮潜力的主要成分。其核心靶标包括 SRC、MAPK3 和 MAPK1,并涉及关键的信号传导途径。从组织学角度看,AGPP 可减轻痤疮引起的毛囊扩张和炎症,抑制炎症细胞因子(IL-6、IL-1β、TNF-α)的产生。这项研究深入揭示了 AGPP 治疗痤疮的机制,为巴黎研发和药物发现奠定了基础。
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引用次数: 0
Effect of ultrasonic and conventional extraction on bioactive components, glucosinolate content and antidiabetic activity of Crambe tataria 超声波萃取和传统萃取对蝙蝠葛生物活性成分、葡萄糖苷酸含量和抗糖尿病活性的影响
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106177

This study was conducted to determine and compare the phenolic compounds, glucosinolate contents and antidiabetic effects of the extracts obtained by ultrasonic and conventional extraction method of the leaves and flowers of the Crambe tataria. The highest antioxidant activity (12.95 mg/mL IC50 value) and total phenolic content (1313.57 mg GAE/100 g fw) were detected in the ultrasonic flower extract. In total flavonoid results, extracts obtained from the flower part of C. tataria had higher values than that of extracts obtained from the leaf part. The most abundant phenolic component in the flower extract was catechin. The highest catechin content in all samples was detected in the ultrasonic flower extract with a value of 374.37 mg/kg. Rutin was the dominant phenolic component in the leaf extract. Rutin values were 654.38 mg/kg and 757.30 mg/kg for conventional and ultrasonic extraction, respectively. In glucosinolate analysis, the highest glucoraphanin content was obtained in flower samples and by conventional extraction method (3466.84 mg/kg). The highest contents of sinigrin (689.97 mg/kg), glucotropaeolin (420.89 mg/kg), glucoerucin (357.27 mg/kg), glucoraphasatin (181.11 mg/kg) and gluconasturtin (66.07 mg/kg) were detected in ultrasonic flower extracts. The highest α-amylase and α-glucosidase enzyme inhibition effects belonged to the ultrasonic flower extract with values of 3.70 mg/mL and 4.89 mg/mL, respectively. As a result, this study determined for the first time that ultrasonic extraction of C. tataria flowers has much higher bioactive components and antidiabetic effects, revealing the potential use of this plant in the fields of medicine, pharmacology and chemistry.

本研究旨在测定和比较用超声波提取法和传统提取法萃取的蝙蝠葛叶和花的酚类化合物、葡萄糖苷酸含量和抗糖尿病作用。超声波花提取物的抗氧化活性(12.95 mg/mL IC50 值)和总酚含量(1313.57 mg GAE/100 g fw)最高。在总黄酮的结果中,从 C. tataria 花部提取物的值高于从叶部提取物的值。花提取物中含量最高的酚类成分是儿茶素。所有样品中儿茶素含量最高的是超声波花提取物,含量为 374.37 毫克/千克。芦丁是叶提取物中最主要的酚类成分。传统提取和超声波提取的芦丁值分别为 654.38 毫克/千克和 757.30 毫克/千克。在葡萄糖苷酸分析中,花朵样品和传统提取法得到的葡萄糖苷酸含量最高(3466.84 毫克/千克)。在超声波花提取物中检测到的西尼格林(689.97 毫克/千克)、葡萄糖苷(420.89 毫克/千克)、葡萄糖醛酸(357.27 毫克/千克)、葡萄糖苷(181.11 毫克/千克)和葡萄糖酸(66.07 毫克/千克)含量最高。超声花提取物对α-淀粉酶和α-葡萄糖苷酶的抑制效果最高,分别为 3.70 毫克/毫升和 4.89 毫克/毫升。因此,本研究首次确定了超声波萃取 C. tataria 花具有更高的生物活性成分和抗糖尿病作用,揭示了该植物在医学、药理学和化学领域的潜在用途。
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引用次数: 0
Triterpenoid saponins from the roots of Panax notoginseng with protective effects against APAP-induced liver injury 三七根中的三萜类皂甙对 APAP 引起的肝损伤具有保护作用
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106159

Five previously undescribed protopanaxatriol-type saponins, notoginsenosides Ta-Te (15), together with eighteen known triterpenoid saponins (623) were isolated from the roots of Panax notoginseng. The structures of new compounds were determined by HRESIMS and NMR spectroscopic analyses and chemical methods. Compounds 1 and 2 were the first examples of ginsenosides featuring a 6-deoxy-β-d-glucose moiety from Panax species. Compounds 14, 7, 10, 12, 2122 showed protective effects on L02 cells against the injury of acetaminophen (APAP). Among them, notoginsenoside R1 (12), ginsenoside Rg1 (21), and ginsenoside Re (22) were the most potent ones, with cell viabilities >80%. Moreover, compounds 12 and 22 remarkably alleviated APAP-induced liver injury in mice. These saponins are potential hepatoprotective agents.

从三七根部分离出了五种以前未曾描述过的原三七皂苷类皂甙--三七皂苷 Ta-Te(1-5),以及十八种已知的三萜类皂甙(6-23)。新化合物的结构是通过 HRESIMS 和 NMR 光谱分析以及化学方法确定的。化合物 1 和 2 是首次从三七中分离出具有 6-脱氧-β-d-葡萄糖分子的人参皂甙。化合物 1-4、7、10、12、21-22 对 L02 细胞具有对乙酰氨基酚(APAP)损伤的保护作用。其中,人参皂苷 R1(12)、人参皂苷 Rg1(21)和人参皂苷 Re(22)的作用最强,细胞存活率大于 80%。此外,化合物 12 和 22 还能显著减轻 APAP 引起的小鼠肝损伤。这些皂甙是潜在的肝脏保护剂。
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引用次数: 0
Targeted discovery of clerodane diterpenoids from Tinospora sinensis as immunomodulatory agents 从天竺葵中发现可作为免疫调节剂的蛤蜊烷二萜类化合物。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106174

Under the guidance of MS/MS-based molecular networking, five new clerodane diterpenoid glucosides, tinosinesides R-V (15), along with 15 known diterpenoids (6–20), were isolated from the stems of Tinospora sinensis. Compound 1 represents the first example of diterpenoid bearing a thio sugar and compound 5 is the first 18,19-dinor-clerodane with cis-fused A/B ring. The structures of the new compounds were elucidated by spectroscopic means, and their absolute configurations were established on the basis of time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation and chemical methods. Selected compounds were evaluated for their immunomodulatory effect and several compounds could enhance the proliferation of B lymphocytes. Preliminary mechanistic studies disclosed that 3 could promote B cell generation and inhibit B cell differentiation.

在基于 MS/MS 的分子网络的指导下,从中华天南星茎中分离出了五种新的萜类二萜糖苷--天南星苷 R-V(1-5),以及 15 种已知的二萜类化合物(6-20)。化合物 1 代表了第一个带有硫糖的二萜类化合物,化合物 5 则是第一个带有顺式融合 A/B 环的 18,19 二甲基-氯丹。这些新化合物的结构是通过光谱手段阐明的,其绝对构型是根据基于时间相关密度泛函理论(TD-DFT)的电子圆二色性(ECD)计算和化学方法确定的。对所选化合物的免疫调节作用进行了评估,其中一些化合物可以促进 B 淋巴细胞的增殖。初步机理研究发现,3 能促进 B 细胞生成并抑制 B 细胞分化。
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引用次数: 0
Antiproliferative metabolites against glioma cells from the marine-associated actinomycete Streptomyces sp. ZZ735 海洋放线菌链霉菌 ZZ735 对胶质瘤细胞的抗增殖代谢物。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-08 DOI: 10.1016/j.fitote.2024.106176

Metabolites produced by the genus Streptomyces are the most important resource for discovering bioactive compounds. In this study, chemical investigation on the metabolites produced by the marine-derived Streptomyces sp. ZZ735 in rice solid medium led to the isolation of eighteen compounds (118). Chemical structures of the isolated compounds were determined based on their HRESIMS data and the extensive NMR spectral analyses. Streptonaphthothiazines A (1), B (2), 2-(2-hydroxy-2-methylpropanoylamino)-benzoic acid (7), and streptomycinoic acids A (17), B (18) are characterized as five previously undescribed compounds. The structural backbones of streptonaphthothiazines A (1), B (2) and streptomycinoic acids A (17), B (18) are found from a natural resource for the first time. It is also the first report of 2-(2-methylpropanoylamino)-benzoic acid (3), 2-(2-methylpropanoylamino)-benzamide (4), methyl 2-(3-hydroxypropanoylamino)-benzoate (5), 2-propionylaminobenzamide (6), and (2E)-3-(3-hydroxy-4,5-dimethoxyphenyl)-2-propenoic acid (15) as natural products. Streptonaphthothiazines A (1), B (2) and streptomycinoic acids A (17), B (18) have antiproliferative activity against human glioma U87MG or U251 cells with IC50 values ranging from 31.8 to 37.9 μM.

链霉菌属产生的代谢物是发现生物活性化合物的最重要资源。本研究对海洋链霉菌 ZZ735 在水稻固体培养基中产生的代谢物进行了化学研究,分离出 18 种化合物(1-18)。根据 HRESIMS 数据和大量核磁共振光谱分析,确定了分离化合物的化学结构。链萘噻嗪 A (1)、B (2)、2-(2-羟基-2-甲基丙酰氨基)-苯甲酸 (7) 和链霉素 A (17)、B (18) 是以前未曾描述过的五个化合物。首次从天然资源中发现了链萘噻嗪 A (1)、B (2)和链霉素酸 A (17)、B (18)的结构骨架。这也是首次报道 2-(2-甲基丙酰氨基)-苯甲酸 (3)、2-(2-甲基丙酰氨基)-苯甲酰胺 (4)、2-(3-羟基丙酰氨基)-苯甲酸甲酯 (5)、2-丙酰氨基苯甲酰胺 (6) 和 (2E)-3-(3- 羟基-4,5-二甲氧基苯基)-2-丙烯酸 (15) 的天然产物。链萘噻嗪 A (1)、B (2) 和链霉素 A (17)、B (18) 对人类胶质瘤 U87MG 或 U251 细胞具有抗增殖活性,其 IC50 值介于 31.8 至 37.9 μM 之间。
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引用次数: 0
Gentiana decoction inhibits liver fibrosis and the activation of hepatic stellate cells via upregulating the expression of Parkin 龙胆草煎剂通过上调 Parkin 的表达,抑制肝纤维化和肝星状细胞的活化。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-07 DOI: 10.1016/j.fitote.2024.106170

Liver fibrosis is a wound-healing process. It can be induced by various chronic liver diseases. Liver fibrosis is characterized by the activation of hepatic stellate cells (HSCs), a key event. However, no effective treatment strategies to cure or alleviate liver fibrosis-induced pathologic changes have yet been developed. Traditional Chinese medicine (TCM) exhibits a good anti-fibrosis action, with few side effects. Gentiana decoction, a TCM also called Longdan Xiegan Tang (LXT), is used for purging the liver in clinical settings. However, the role of LXT in preventing liver fibrosis and the underlying regulatory mechanism have not yet been investigated. This study demonstrates that LXT treatment can protect the liver from the injuries resulting from CCl4-induced liver fibrosis in mice and suppress the activation of HSCs. The mice in the LXT group exhibit litter collagen I and HSC activation marker α-smooth muscle actin (α-SMA) expression. Transcriptome sequencing of the mouse liver tissue reveals that the level of Parkin, a mitophagy marker, decreased in CCl4-induced liver fibrosis. Further study shows that the injection of Parkin-overexpression adeno-associated virus (Parkin–AAV) via the tail vein can reduce CCl4-induced liver fibrogenesis in mice. We conducted a mechanistic study also, which suggests that LXT treatment suppresses the activation of HSCs by upregulating the expression of Parkin. Hence, it can be suggested that LXT inhibits liver fibrosis by activating the Parkin signaling pathway.

肝纤维化是一个伤口愈合的过程。各种慢性肝病都可能诱发肝纤维化。肝纤维化的特征是肝星状细胞(HSCs)的活化,这是一个关键事件。然而,目前尚未开发出有效的治疗策略来治愈或缓解肝纤维化引起的病理变化。中药具有良好的抗肝纤维化作用,且副作用小。龙胆草煎剂是一种中药,又称龙胆泻肝汤,在临床上用于清肝。然而,龙胆泻肝汤在预防肝纤维化方面的作用及其潜在的调节机制尚未得到研究。本研究表明,LXT 治疗可保护肝脏免受 CCl4 诱导的小鼠肝纤维化的损伤,并抑制造血干细胞的活化。LXT组小鼠的胶原蛋白I和造血干细胞活化标志物α-平滑肌肌动蛋白(α-SMA)的表达较低。小鼠肝脏组织的转录组测序显示,在 CCl4 诱导的肝纤维化中,有丝分裂标记物 Parkin 的水平下降。进一步的研究表明,通过尾静脉注射Parkin表达过高的腺相关病毒(Parkin-AAV)可以减少CCl4诱导的小鼠肝纤维化。我们还进行了一项机理研究,结果表明 LXT 可通过上调 Parkin 的表达来抑制造血干细胞的活化。因此,可以认为LXT通过激活Parkin信号通路来抑制肝纤维化。
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引用次数: 0
Limonin (LM) and its derivatives: Unveiling the neuroprotective and anti-inflammatory potential of LM and V-A-4 in the management of Alzheimer's disease and Parkinson's disease 柠檬素(LM)及其衍生物:揭示 LM 和 V-A-4 在治疗阿尔茨海默病和帕金森病中的神经保护和抗炎潜力。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-06 DOI: 10.1016/j.fitote.2024.106173

Neuroinflammation and neuronal apoptosis are central pathogenic consequences associated with Alzheimer's Disease (AD) and Parkinson's Disease (PD). Limonin (LM), a tetracyclic triterpenoid available in citrus fruits, has anti-tumor, antioxidant, anti-inflammatory, hepatoprotective, and neuroprotective actions. LM derivative, V-A-4 emerged as a potential neuroprotective drug due to their ability to target multiple molecular pathways intertwined with neuroinflammation and neuronal apoptosis. To date, the treatment of AD and PD is not successful even though the understanding of the mechanism of neuroinflammation and neuronal apoptosis is vast in the literature. Thus, there is an urgent need to identify novel neuroprotective drugs that could target the multiple molecular pathways associated with neuroinflammation and neuronal apoptosis. The various online databases (Google scholar, Pubmed, Scopus) were searched via keywords: limonin, limonin derivatives and neuroprotection. This review highlights the multifunctional nature of LM and derivatives in combating neuroinflammation and neuronal apoptosis by stimulating PI3K/AKT and downregulating TLR4/NF-κB critical pathways. By intervening in the secretion of NO and TNF-α from glial cells, V-A-4 attenuates the damaging cascade of neuroinflammation by suppressing IKK-α and IKK-β. Furthermore, V-A-4 demonstrates its versatility by suppressing the manifestation of miR-146a and miR-155, both intimately linked to neuroinflammation, this review summarized the activities of LM and its derivatives against AD and PD, with a special focus on V-A-4 as an effective neuroprotective drug. V-A-4's ability to stimulate PI3K/AKT signaling further underscores its neuroprotective effect in combating AD and PD. More in-vitro cell line studies are needed to develop V-A-4 as an upcoming neuroprotective compound.

神经炎症和神经细胞凋亡是阿尔茨海默病(AD)和帕金森病(PD)的主要致病后果。柠檬素(LM)是柑橘类水果中的一种四环三萜类化合物,具有抗肿瘤、抗氧化、抗炎、保肝和保护神经的作用。LM 衍生物 V-A-4 是一种潜在的神经保护药物,因为它们能够靶向与神经炎症和神经元凋亡交织在一起的多种分子通路。迄今为止,尽管文献中对神经炎症和神经细胞凋亡的机制有了大量的了解,但对注意力缺失症和帕金森病的治疗仍不成功。因此,我们急需找到能够靶向与神经炎症和神经元凋亡相关的多种分子通路的新型神经保护药物。本文通过关键词 "柠檬素、柠檬素衍生物和神经保护 "对各种在线数据库(Google scholar、Pubmed、Scopus)进行了搜索。这篇综述强调了柠檬素及其衍生物通过刺激 PI3K/AKT 和下调 TLR4/NF-κB 关键通路来对抗神经炎症和神经元凋亡的多功能性。通过干预神经胶质细胞 NO 和 TNF-α 的分泌,V-A-4 可抑制 IKK-α 和 IKK-β,从而减轻神经炎症的破坏性级联反应。此外,V-A-4还能抑制与神经炎症密切相关的miR-146a和miR-155的表达,从而显示出其多功能性。本综述总结了LM及其衍生物对AD和PD的活性,并特别关注V-A-4这种有效的神经保护药物。V-A-4能够刺激PI3K/AKT信号转导,这进一步强调了它在对抗AD和PD方面的神经保护作用。要将 V-A-4 开发成一种新的神经保护化合物,还需要进行更多的体外细胞系研究。
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引用次数: 0
Design, synthesis and biological activity of α-nitrile substituted guaiazulene-based chalcone derivatives α-腈取代愈创木酚基查耳酮衍生物的设计、合成和生物活性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-06 DOI: 10.1016/j.fitote.2024.106151

In present study, seventeen α-nitrile substituted guaiazulene-based chalcone derivatives including twelve new were designed, synthesized, and assayed for antiviral, cytotoxicity and signal pathway activities. All derivatives showed potential antiviral activity towards influenza virus or herpes simplex virus (HSV), 7 g with the substitution of nitro group showed strong effects towards H1N1 virus at 30 μM with inhibitory rate of 66.0%, 7o with thiophene exhibited potent anti HSV-1 activities with inhibitory rate of 65.8%. Moreover, several compounds exhibited inhibitory effects on tumor cells and hypoxia-inducible factor-1 (HIF1) signaling pathways. These results showed that α-nitrile substituted guaiazulene-based chalcones offered a promising framework for the further development of new highly efficient drugs.

本研究设计、合成了 17 种α-硝基取代的瓜氮基查尔酮衍生物,其中包括 12 种新衍生物,并对其进行了抗病毒、细胞毒性和信号通路活性测定。所有衍生物都显示出了对流感病毒或单纯疱疹病毒(HSV)的潜在抗病毒活性,其中取代了硝基的 7 g 衍生物在 30 μM 时对 H1N1 病毒有很强的抑制作用,抑制率为 66.0%;含有噻吩的 7o 衍生物显示出了强效的抗 HSV-1 活性,抑制率为 65.8%。此外,几种化合物对肿瘤细胞和缺氧诱导因子-1(HIF1)信号通路也有抑制作用。这些结果表明,α-腈取代的瓜氮烯类查耳酮化合物为进一步开发新型高效药物提供了一个前景广阔的框架。
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