Fitoterapia最新文献

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An updated overview of Gypsophila species: Phytochemical and pharmacological investigations 关于 Gypsophila 种类的最新概述：植物化学和药理学研究

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106230

Medicinal plants and their consituents play a crucial role in disease prevention and treatment. The genus Gypsophila (Caryophyllaceae family), comprising approximately 150 species of flowering plants, holds significant value in both ornamental and therapeutic fields. Traditional uses in various cultures highlight their potential in treating a range of conditions, such as liver disorders, diabetes, and kidney stones. These resilient plants, known for their delicate blooms and adaptability to diverse environments, are rich in chemical compounds, including non-volatile constituents such as phenolic compounds (e.g., flavonoids), terpenoids, saponins, cyclopeptides, and alkaloids. Additionally, monoterpenes and sesquiterpenes, the primary volatile constituents, exhibit significant insecticidal properties. Gypsophila species show a broad spectrum of pharmacological effects, including hepatoprotective, cytotoxic, anti-diabetic, antioxidant, cytotoxic, anti-inflammatory, diuretic, neuroprotective, and anti-obesity properties. This review underscores the promising therapeutic potential of Gypsophila and advocates for further research, particularly clinical trials, to thoroughly assess their efficacy and safety. By consolidating existing knowledge, it sheds light on the potential of Gypsophila species as valuable resources for human health and underscores the need for continued exploration to uncover novel treatments and interventions.

药用植物及其成分在预防和治疗疾病方面发挥着至关重要的作用。石竹属（石竹科）包括约 150 种开花植物，在观赏和治疗领域都具有重要价值。各种文化中的传统用法都强调了它们在治疗肝脏疾病、糖尿病和肾结石等一系列疾病方面的潜力。这些生命力顽强的植物以其娇艳的花朵和对不同环境的适应能力而闻名，含有丰富的化合物，包括酚类化合物（如类黄酮）、萜类化合物、皂甙、环肽和生物碱等非挥发性成分。此外，主要挥发性成分单萜和倍半萜具有显著的杀虫特性。石膏蕨类植物具有广泛的药理作用，包括保肝、细胞毒性、抗糖尿病、抗氧化、细胞毒性、抗炎、利尿、神经保护和抗肥胖等特性。这篇综述强调了石膏花的巨大治疗潜力，并主张进一步开展研究，特别是临床试验，以全面评估其疗效和安全性。通过整合现有知识，该综述揭示了石膏草物种作为人类健康宝贵资源的潜力，并强调了继续探索以发现新型治疗方法和干预措施的必要性。

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引用次数: 0

Antileishmanial, antitrypanosomal and anti-coronavirus activities of benzophenanthridine alkaloids and other specialized metabolites isolated from the root bark of Zanthoxylum zanthoxyloides (Lam.) B.Zepernick & Timler 从 Zanthoxylum zanthoxyloides (Lam.) B.Zepernick & Timler 的根皮中分离的苯并菲啶生物碱及其他特殊代谢物的抗利什曼病、抗锥虫和抗冠状病毒活性。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106232

Strong antileishmanial and antitrypanosomal activities were highlighted for the crude methanolic extract (IC₅₀ = 0.61 and 2.15 μg/mL, respectively) of Zanthoxylum zanthoxyloides (Lam.) B.Zepernick & Timler root bark, as well as for its apolar partitions (cyclohexane: IC₅₀ = 0.66 and 5.17 μg/mL, respectively and dichloromethane: IC₅₀ = 0.07 and 0.22 μg/mL, respectively), with a good selectivity index (SI) towards WI-38 cells. In addition, cyclohexane and dichloromethane extracts exhibited a dose-dependent inhibition of human coronavirus HCoV-229E infection in hepatoma Huh-7 cells expressing or not the cellular protease TMPRSS2 (IC₅₀ values of 5.29 μg/mL and 4.87 μg/mL, respectively). Fractionation of these active extracts led to the isolation of a new racemic benzophenanthridine alkaloid named zanthoxyloithrine (1), together with 13 known compounds. Their structures were elucidated by spectroscopic techniques including IR, UV, HR-MS, 1D and 2D NMR and electronic circular dichroism. In parallel, HR-ESI-MS/MS based dereplication and molecular networking analysis were performed to identify unpurified compounds in cyclohexane and dichloromethane extracts. Zanthoxyloithrine (1) showed strong antileishmanial (IC₅₀ = 0.14 μM, SI = 52.0) and antitrypanosomal (IC₅₀ = 0.36 μM, SI = 20.8) activities. In addition, compound (1) demonstrated a high antiviral activity against HCoV-229E with IC₅₀ value of 6.70 μM in presence of TMPRRS2 and without significant toxicity on Huh-7 cells. Other purified benzo[c]phenanthridine alkaloids also showed anti-coronavirus and antiparasitic activities.

Zanthoxylum zanthoxyloides (Lam.) B. Zepernick & Timler根皮的粗甲醇提取物（IC50分别为0.61和2.15微克/毫升）以及其无极分馏物（环己烷：IC50分别为0.66和5.17微克/毫升）具有很强的抗利什曼病和抗锥虫活性。Zepernick & Timler 的根皮提取物，以及其极性分区（环己烷：IC50 分别为 0.66 和 5.17 微克/毫升，二氯甲烷：IC50 分别为 0.07 和 0.22 微克/毫升），对 WI-38 细胞具有良好的选择性指数（SI）。此外，环己烷和二氯甲烷提取物对表达或不表达细胞蛋白酶 TMPRSS2 的肝癌 Huh-7 细胞感染人类冠状病毒 HCoV-229E 有剂量依赖性抑制作用（IC50 值分别为 5.29 μg/mL 和 4.87 μg/mL）。对这些活性提取物进行分馏后，分离出了一种新的外消旋苯并菲啶生物碱，名为 zanthoxyloithrine（1），以及 13 种已知化合物。通过红外光谱、紫外光谱、HR-MS、一维和二维核磁共振以及电子圆二色性等光谱技术，阐明了这些化合物的结构。同时，还进行了基于 HR-ESI-MS/MS 的去复制和分子网络分析，以确定环己烷和二氯甲烷提取物中未纯化的化合物。Zanthoxyloithrine (1) 具有很强的抗利什曼病（IC50 = 0.14 μM，SI = 52.0）和抗锥虫（IC50 = 0.36 μM，SI = 20.8）活性。此外，化合物（1）对 HCoV-229E 具有很高的抗病毒活性，在 TMPRRS2 存在下，IC50 值为 6.70 μM，且对 Huh-7 细胞无明显毒性。其他纯化的苯并[c]菲啶生物碱也显示出抗冠状病毒和抗寄生虫活性。

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引用次数: 0

Sesquiterpenes from the seeds of Cichorium glandulosum and their anti- neuroinflammation activities 刺五加种子中的倍半萜及其抗神经发炎活性。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106239

Three previously undescribed sesquiterpenes, along with three known ones were isolated from the seeds of Cichorium glandulosum. The structures of them were elucidated by the analysis of spectroscopic data. The isolated compounds were tested for their neuroprotective effects against LPS-induced neuroinflammation in BV-2 cells. Santamarine (5) exhibited inhibitory activity on LPS-induced NO production in BV-2 cells with IC₅₀ of 0.89 ± 0.12 μM. The mechanism of the compound 5 was related to activating the NF-κB, MAPK and cGAS/STING pathways.

从 Cichorium glandulosum 的种子中分离出了三种以前未曾描述过的倍半萜内酯以及三种已知的倍半萜内酯。通过分析光谱数据，阐明了它们的结构。在 BV-2 细胞中测试了分离出的化合物对 LPS 诱导的神经炎症的神经保护作用。山豆根碱（5）对 LPS 诱导的 BV-2 细胞 NO 生成具有抑制作用，IC50 为 0.89 ± 0.12 μM。化合物 5 的作用机制与激活 NF-κB、MAPK 和 cGAS/STING 通路有关。

引用次数: 0

Identification of isoquinoline alkaloids from Corydalis mucronifera and their acetylcholinesterase inhibitory effects 从堇菜中鉴定异喹啉生物碱及其乙酰胆碱酯酶抑制作用。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106220

Four new spirobenzylisoquinoline mucroniferanines N − Q (1–4) and a rare chlorinated isoquinoline mucroniferanine R (5) were isolated from Corydalis mucronifera Maxim. Their structures were elucidated based on extensive spectroscopic data analysis of HRESIMS, 1D and 2D NMR, and their absolute configurations were confirmed by ECD data. The isolated compounds were evaluated for acetylcholinesterase (AChE) inhibitory activities. Mucroniferanine R showed significant activities with IC₅₀ values of 0.78 μM compared to galanthamine (1.34 μM). The AChE inhibitory activity was further supported by the molecular docking analysis that exhibited the accommodation of mucroniferanine R in the active site of human AChE.

从 Corydalis mucronifera Maxim 中分离出了四种新的螺苄基异喹啉短叶木犀草素 N - Q（1-4）和一种罕见的氯化异喹啉短叶木犀草素 R（5）。根据 HRESIMS、1D 和 2D NMR 的大量光谱数据分析，阐明了它们的结构，并通过 ECD 数据确认了它们的绝对构型。对分离出的化合物进行了乙酰胆碱酯酶（AChE）抑制活性评估。与加兰他敏（1.34 μM）相比，Mucroniferanine R 显示出显著的活性，其 IC50 值为 0.78 μM。分子对接分析表明，木犀草素 R 与人 AChE 的活性位点相容，从而进一步证实了其 AChE 抑制活性。

引用次数: 0

Discovery of metabolite from the insect-derived endophytic Penicillium chrysogenum and their COX-2 inhibitory activity 从昆虫内生青霉中发现代谢物及其 COX-2 抑制活性

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106238

Three new N-alkylated amino acid derivatives, penichrysoamides A-C (1–3), along with a new citric acid derivative, penichrysoacid A (4), a new chromanone lactone penichrysoacid B (5), and a new amide derivative, penichrysoamide D (6), as well as seven known benzamide derivatives (7–13), were isolated from the endophytic fungus Penicillium chrysogenum derived from the insect Periplaneta americana. The structures of these compounds, including their absolute configurations, were elucidated using spectroscopic and computational techniques. Biological evaluation revealed that compounds 8–13 exhibited significant COX-2 inhibitory activity, with IC₅₀ values ranging from 275 nM to 1350 nM.

从源自昆虫 Periplaneta americana 的内生真菌 Penicillium chrysogenum 中分离出了三种新的 N-烷基化氨基酸衍生物 Penichrysoamides A-C (1-3)、一种新的柠檬酸衍生物 Penichrysoacid A (4)、一种新的色酮内酯 Penichrysoacid B (5)、一种新的酰胺衍生物 Penichrysoamide D (6)，以及七种已知的苯甲酰胺衍生物 (7-13)。利用光谱和计算技术阐明了这些化合物的结构，包括它们的绝对构型。生物学评价显示，化合物 8-13 具有显著的 COX-2 抑制活性，IC50 值从 275 nM 到 1350 nM 不等。

引用次数: 0

Polygala japonica Houtt.: A comprehensive review on its botany, traditional uses, phytochemistry, pharmacology, and pharmacokinetics 日本远志关于其植物学、传统用途、植物化学、药理学和药代动力学的全面综述

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106233

Polygala japonica Houtt. (P. japonica), a member of the Polygala genus in the Polygalaceae family, has been historically utilized in traditional folk medicine as an expectorant, anti-inflammatory, anti-bacterial, and anti-depressant agent. This paper systematically reviews the latest research in botany, traditional uses, phytochemistry, pharmacology, and pharmacokinetics, aiming to provide a scientific foundation for the future development and application of P. japonica and to explore its potential value comprehensively. Approximately 86 compounds have been isolated from P. japonica, with triterpenoid saponins being the most prevalent and bioactive components. Extensive pharmacological activities of P. japonica extracts or compounds have been confirmed in vivo and in vitro, including anti-inflammatory, anti-depressant, neuroprotective, anti-obesity, anti-apoptotic, and skin-protective effects. Additionally, P. japonica has demonstrated significant curative effects and relatively clear pharmacological mechanisms in treating inflammatory and nervous system diseases. Specific components of its primary triterpenoid saponins are rapidly absorbed in the body. This review advocates for deeper scientific research on P. japonica, noting that most current research remains in its early stages and many reported biological activities require further clinical validation. Despite this, the traditional medical use of P. japonica across various cultures attests to its broad application value. Presently, the pharmacological activities of P. japonica extracts and compounds provide a scientific basis for its traditional uses. Future research must ensure the safety and effectiveness of P. japonica through in-depth pharmacokinetic studies, and the establishment of a refined and standardized quality evaluation system is essential for its clinical development and application.

远志（Polygala japonica Houtt.(远志（P. japonica）是远志科远志属植物，在传统民间医药中一直被用作祛痰、消炎、抗菌和抗抑郁药物。本文系统地综述了植物学、传统用途、植物化学、药理学和药代动力学等方面的最新研究成果，旨在为日后的开发和应用提供科学依据，并全面发掘其潜在价值。目前已从白花蛇舌草中分离出约 86 种化合物，其中三萜类皂苷是最常见的生物活性成分。已在体内和体外证实了 P. japonica 提取物或化合物的广泛药理活性，包括抗炎、抗抑郁、神经保护、抗肥胖、抗细胞凋亡和皮肤保护作用。此外，P. japonica 在治疗炎症和神经系统疾病方面具有显著疗效和相对明确的药理机制。其主要三萜类皂苷的特定成分可被人体快速吸收。这篇综述提倡对白花蛇舌草进行更深入的科学研究，并指出目前的大多数研究仍处于早期阶段，许多已报道的生物活性还需要进一步的临床验证。尽管如此，不同文化背景下的传统医学使用证明了白花蛇舌草的广泛应用价值。目前，P. japonica 提取物和化合物的药理活性为其传统用途提供了科学依据。未来的研究必须通过深入的药代动力学研究来确保白花蛇舌草的安全性和有效性，而建立完善和标准化的质量评价体系对于白花蛇舌草的临床开发和应用至关重要。

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引用次数: 0

Glucopyranosyloxybenzyl succinates and their biological activities 吡喃葡萄糖基氧基苄基琥珀酸盐及其生物活性。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-24 DOI: 10.1016/j.fitote.2024.106231

Over the past decades, great efforts have been made to explore the glucopyranosyloxybenzyl succinates from Orchidaceae. At the same time, some of those compounds with new structures have led to new findings of their biological functions. The structures, classifications, distributions and bioactivities of glucopyranosyloxybenzyl succinates have been summarized in this review.

过去几十年来，人们一直在努力探索兰科植物中的葡萄糖吡喃氧基苄基琥珀酸盐。与此同时，其中一些具有新结构的化合物的生物功能也有了新的发现。本综述总结了葡萄糖吡喃氧基苄基琥珀酸酯的结构、分类、分布和生物活性。

引用次数: 0

Cuparene-type sesquiterpenes with neuroprotective activities from the edible mushroom Flammulina filiformis 食用菌丝状蘑菇中具有神经保护活性的杯烯类倍半萜化合物

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106235

Four new cuparene-type sesquiterpenes, flammuterpenols A − D (1–4), along with one known congener (5) were isolated from the solid culture of edible mushroom Flammulina filiformis. Their structures with a benzoxabicyclo[3.2.1]octane core were elucidated by integrated multiple spectroscopic techniques, electronic circular dichroism, and single crystal X-ray diffraction analysis. Biologically, compounds 1–5 were evaluated in vitro for their neuroprotective effects against 6-hydroxydopamine induced cell death in human neuroblastoma SH-SY5Y cells. All of them exhibited remarkable neuroprotective effects possessing the EC₅₀ values ranging from 0.93 ± 0.02 to 10.28 ± 0.10 μM. These findings not only enrich the structural diversity of cuparene-type sesquiterpenes, but also provide potential candidates for the further development of the neuroprotective agents.

从食用菌丝状蘑菇（Flammulina filiformis）的固体培养物中分离出了四种新的杯烯类倍半萜，即 Flammuterpenols A - D（1-4），以及一种已知的同系物（5）。通过综合多种光谱技术、电子圆二色性和单晶 X 射线衍射分析，阐明了它们以苯并氧杂双环[3.2.1]辛烷为核心的结构。化合物 1-5 在体外对 6-羟基多巴胺诱导的人神经母细胞瘤 SH-SY5Y 细胞死亡的神经保护作用进行了生物学评估。所有化合物都表现出了显著的神经保护作用，其 EC50 值从 0.93 ± 0.02 到 10.28 ± 0.10 μM。这些发现不仅丰富了杯烯类倍半萜的结构多样性，而且为进一步开发神经保护剂提供了潜在的候选物质。

引用次数: 0

Evaluation of the Antihyperglycemic efficacy of the roots of Ferula orientalis L.: An in vitro to in vivo assessment 东方阿魏根的降血糖功效评估：从体外到体内的评估

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106225

Decoctions of Ferula orientalis L. (Apiaceae), have been traditionally used to lower blood glucose levels (BGLs). After in vitro enzyme inhibition tests on the dichloromethane extracts of the roots (FOD) and the methanol extract of the roots (FOM), isolation studies were carried out on the FOD extract. The anti-hyperglycemic effects of the FOD extract and the pure compounds were studied in mice using the Oral Glucose Tolerance Test (OGTT) and streptozotocin (STZ)-induced diabetes mellitus (DM) models. Molecular docking studies were performed on potent compounds in the binding pockets of enzymes α-glucosidase and α-amylase. The isolations of 11 compounds were isolated from the FOD extract, which comprised teferidine (1), ferutinin (FT) (2), teferin (3), epoxy-jaeschkeanadiol-p-hydroxybenzoate (4), epoxy-jaeschkeanadiol-6-vanillate (5), tovarol-8-angelate (6), leucoferin (7), tovarol-8-p-hydroxybenzoate (8), tovarol-8-vanillate (9), 6-β-p-hydroxybenzoyloxy-germacra-1(10),4-diene (10), and chimgin (11). Compounds 2 and 8–11 exhibited a higher inhibitory activity on α-glucosidase. In the OGTT, pretreatment with the FOD extract or compound 2 did not alter the BGLs after administration of the glucose solution compared to the control. In the STZ-induced diabetic mice model, no significant difference in the BGLs was observed with the FOD extract (200 mg/kg) or compound 2 (100 mg/kg)-treated diabetic mice compared to the diabetic control mice. The experimental studies all showed that the F. orientalis extract had significant effects on the enzyme systems involved in DM, and it would be appropriate to plan further studies on possible problems of bioavailability of the compound FT and the FOD extract, inadequate dose, and duration of administration.

东方阿魏（Apiaceae）的煎剂传统上用于降低血糖水平（BGLs）。在对根部二氯甲烷提取物（FOD）和根部甲醇提取物（FOM）进行体外酶抑制试验后，对 FOD 提取物进行了分离研究。利用口服葡萄糖耐量试验（OGTT）和链脲佐菌素（STZ）诱导的糖尿病（DM）模型，研究了 FOD 提取物和纯化合物对小鼠的抗高血糖作用。对α-葡萄糖苷酶和α-淀粉酶结合口袋中的强效化合物进行了分子对接研究。从 FOD 提取物中分离出了 11 种化合物，包括铁线蕨苷（1）、铁线蕨素（FT）（2）、铁线蕨素（3）、环氧-马齿苋二醇-对羟基苯甲酸酯（4）、环氧-马齿苋二醇-对羟基苯甲酸酯（5）、环氧-马齿苋二醇-对羟基苯甲酸酯（6）和环氧-马齿苋二醇-对羟基苯甲酸酯（7）、环氧-香豆素-6-香兰酸酯（5）、香豆素-8-angelate（6）、leucoferin（7）、香豆素-8-对羟基苯甲酸酯（8）、香豆素-8-香兰酸酯（9）、6-β-对羟基苯甲酰氧基-germacra-1(10),4-二烯（10）和 chimgin（11）。化合物 2 和 8-11 对α-葡萄糖苷酶具有较高的抑制活性。在 OGTT 试验中，与对照组相比，使用 FOD 提取物或化合物 2 进行预处理不会改变给予葡萄糖溶液后的 BGLs。在 STZ 诱导的糖尿病小鼠模型中，经 FOD 提取物（200 毫克/千克）或化合物 2（100 毫克/千克）处理的糖尿病小鼠与糖尿病对照组小鼠相比，BGLs 没有明显差异。这些实验研究都表明，东方鱼腥草提取物对参与 DM 的酶系统有明显的影响，因此应该计划进一步研究复方 FT 和 FOD 提取物的生物利用度、剂量不足和给药持续时间等可能存在的问题。

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引用次数: 0

Phytochemical and pharmacological investigation of the non-volatile compounds of Lepidium cartilagineum (J. C. Mayer) Thell. and determination of the essential oil composition of its flowers and fruits Lepidium cartilagineum (J. C. Mayer) Thell.非挥发性化合物的植物化学和药理学研究及其花和果实精油成分的测定

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106236

Eighteen compounds, among them phenylpropanoids (1–2), neolignans (3–9), a megastigmane (10), a phenyl glucoside (11), flavonoids (12–14), and N-containing compounds (15–18) were isolated from the methanolic extract of the whole plant of L. cartilagineum. The structures of the compounds were determined by NMR and MS measurements. The composition of the essential oils prepared from the flowers and fruits of L. cartilagineum was investigated using GC and GC–MS measurements. The essential oils were rich in aliphatic aldehydes and hydrocarbons, but low in sulfur-containing compounds, e.g., isothiocyanates. The extracts prepared from the aerial parts and roots of the plant, the essential oil, and the isolated compounds (1–9) were tested for antiproliferative activity against COLO 205 and COLO 320 cell lines and antibacterial activity on Lactobacillus rhamnosus. Dehydrodiconiferyl alcohol γ’-methyl ether (5) possessed marked antiproliferative activity against both human tumor cell lines. Neither the extracts nor the compounds affected the growth of the bacteria and did not influence the biofilm formation of L. rhamnosus. Based on the results, it can be concluded that L. cartilagineum is non-toxic to the human gut microbiome forming L. rhamnosus.

从软骨草全草的甲醇提取物中分离出了 18 种化合物，其中包括苯丙酸类化合物（1-2）、新木脂素类化合物（3-9）、巨木脂素类化合物（10）、苯基葡萄糖苷类化合物（11）、黄酮类化合物（12-14）和含 N 的化合物（15-18）。通过核磁共振和质谱测定确定了这些化合物的结构。利用气相色谱和气相色谱-质谱测量法研究了从软骨草花和果实中制备的精油的成分。精油富含脂肪醛和碳氢化合物，但含硫化合物（如异硫氰酸盐）含量较低。从该植物的气生部分和根部制备的提取物、精油和分离出的化合物（1-9）对 COLO 205 和 COLO 320 细胞系进行了抗增殖活性测试，并对鼠李糖乳杆菌进行了抗菌活性测试。脱氢二烯醇 γ'-甲醚（5）对两种人类肿瘤细胞株都具有明显的抗增殖活性。提取物和化合物都不影响细菌的生长，也不影响鼠李糖杆菌生物膜的形成。根据上述结果，可以得出结论：软骨草对形成鼠李糖的人体肠道微生物群无毒性。

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