Fitoterapia最新文献_第8页

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

Hai-Peng Tang , En-Lin Zhu , Qian-Xiang Bai , Shuang Wang , Zhi-Bin Wang , Meng Wang , Hai-Xue Kuang

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

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

Shouyuan Wu , Xianqiang Chen , Jingling Ren , Peilian Liu , Qing Yan , Ziming Chen

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

Nurdan Yazici , Seçkin Engin , Elif Nur Barut , Fadıl Kaan Kuran , Gozde Hasbal-Celikok , Tugba Yilmaz-Ozden , Mahmut Miski

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

Csilla Zsuzsanna Dávid , Zuhao Cui , Katalin Veres , Annamária Kincses , Norbert Kúsz , Anita Barta , Tamara Sápi , László Bakacsy , Judit Hohmann , Andrea Vasas

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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引用次数: 0

Pegaharolines A − I, structurally novel indole alkaloids with anti-HSV-2 virus activities from Peganum harmala L. seeds Pegaharolines A - I，从 Peganum harmala L. 种子中提取的具有抗 HSV-2 病毒活性的结构新颖的吲哚生物碱。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106237

Zhong-Nan Wu , Yu-Bo Zhang , Guo-Cai Wang , Qing Tang , Yao-Lan Li , Wen Cheng

Leading by the antiviral activities against HSV-2 virus, bioactivity-guided the fraction of crude alkaloids from seeds of Peganum harmala led to the isolation of nine structurally novel indole alkaloids, pegaharolines A − I (1–9), and 11 known ones (10−20). Compound 3 was an unusual 6/5/5/5 spirotetracyclic indole-derived alkaloids featuring a classic bicyclic indole unit fused with an additional pyrrolizine ring via a spiral atom (C-3). Compound 4 was determined as a novel indole alkaloid, characterized with a rare hexacyclic 6/5/6/5–6/6 ring system, by a single-crystal X-ray diffraction. Compounds 5 and 6 were peculiar indole dimers featuring with the rare carbon skeleton of an octacyclic scaffold. Compounds 1–6 were six racemates. Most compounds exhibited different levels of antiviral activities against HSV-2. Especially, the anti-HSV-2 activity of compound 1 (IC₅₀ = 0.90 ± 0.10 μM) was much better than that of the positive control (acyclovir, IC₅₀ = 1.12 ± 0.15 μM). In this study, the discovery of anti-HSV-2 components from the seeds of P. harmala, could benefit development and utilization of this plant in antiviral medicinal products.

在对 HSV-2 病毒的抗病毒活性的引领下，以生物活性为指导，从 Peganum harmala 种子中分离出了 9 种结构新颖的吲哚生物碱，即 pegaharolines A - I（1-9）和 11 种已知的生物碱（10-20）。化合物 3 是一种不寻常的 6/5/5/5 双环吲哚生物碱，其特征是一个经典的双环吲哚单元通过一个螺旋原子（C-3）与另一个吡咯烷环融合。化合物 4 通过单晶 X 射线衍射被确定为一种新型吲哚生物碱，具有罕见的六环 6/5/6/5-6/6 环系统。化合物 5 和 6 是奇特的吲哚二聚体，具有罕见的八环支架碳骨架。化合物 1-6 共有六个外消旋体。大多数化合物对 HSV-2 具有不同程度的抗病毒活性。特别是化合物 1 的抗 HSV-2 活性（IC50 = 0.90 ± 0.10 μM）远远优于阳性对照（阿昔洛韦，IC50 = 1.12 ± 0.15 μM）。在这项研究中，从哈密瓜种子中发现抗HSV-2成分将有利于开发和利用这种植物的抗病毒药物产品。

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引用次数: 0

Exploring the molecular mechanism of Toddalia asiatica (L.) lam on the treatment of thrombosis based on zebrafish models, network pharmacology and experimental verification 基于斑马鱼模型、网络药理学和实验验证，探讨川芎治疗血栓形成的分子机理。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106224

Songqin Yang , Mao Zhao , Yuhan Feng , Xia Zhang , Qiuhong Li , Wenwen Jiang , Daoping Wang

Toddalia asiatica (L.) Lam. (TA) is a traditional folk medicine of ethnic minorities in the southwest of China. It is widely used in the treatment of dispersing blood stasis and activating blood. However, the effective substance and pharmacological mechanism have not been fully elucidated. The zebrafish larvae were treated with Phenylhydrazine (PHZ) to establish a thrombus model, and the staining intensity of zebrafish red blood cells was analyzed. The antithrombotic activity of TA was verified for the first time, and it was found that the inhibition rate of TA on thrombosis was up to 60.85 %. The chemical ingredients of TA were collected by combining UPLC-HRMS analysis and the literature research. Network pharmacology revealed that six key targets were obtained, which including TNF, AKT1, EGFR, PTGS2, PPARG, and IFNG. It showed that the PI3K-Akt pathway was a core signaling pathway. Coagulation factor III(TF), playing an important role in the process of hemostasis and thrombosis, which ranks high in the PPI network. Moreover, the results of molecular docking showed that the active components had a strong binding force with TF, which indicated that TF might be the key target of TA in treating thrombosis. In vitro experiments showed that TA could inhibit TNF-α-induced high expression of TF in EA.hy926 cells. In addition, TA could inhibit TNF-α-activated expression of Akt, IκBα and P65 protein phosphorylation in PI3K-Akt pathway. The results showed that TA had antithrombotic activity and exerted an antithrombotic effect by inhibiting the expression of TF through the PI3K-Akt-NF-κB signaling pathway.

虎杖（Toddalia asiatica (L.) Lam.(TA）是中国西南少数民族的传统民间药材。它被广泛用于散瘀活血的治疗。然而，其有效物质和药理机制尚未完全阐明。本研究以斑马鱼幼体为研究对象，用苯肼（PHZ）处理斑马鱼幼体，建立血栓模型，分析斑马鱼红细胞的染色强度。首次验证了 TA 的抗血栓活性，发现 TA 对血栓形成的抑制率高达 60.85%。结合UPLC-HRMS分析和文献研究，收集了TA的化学成分。网络药理学发现，TA有6个关键靶点，包括TNF、AKT1、EGFR、PTGS2、PPARG和IFNG。结果表明，PI3K-Akt通路是核心信号通路。凝血因子 III（TF）在止血和血栓形成过程中发挥着重要作用，在 PPI 网络中排名靠前。此外，分子对接结果表明，活性成分与TF有很强的结合力，这表明TF可能是TA治疗血栓形成的关键靶点。体外实验表明，TA能抑制TNF-α诱导的TF在EA.hy926细胞中的高表达。此外，TA还能抑制PI3K-Akt通路中TNF-α激活的Akt、IκBα和P65蛋白的磷酸化表达。结果表明，TA具有抗血栓活性，通过PI3K-Akt-NF-κB信号通路抑制TF的表达，从而发挥抗血栓作用。

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引用次数: 0

Cardenolides; calotropin and gomphogenin from Calotropis procera (Aiton) mitigate bone turnover in ovariectomized osteoporotic rats: Targeting RANKL/OPG axis and estrogen receptor-alpha Calotropis procera (Aiton) 中的 Cardenolides、calotropin 和 gomphogenin 可减轻卵巢切除骨质疏松大鼠的骨质流失：靶向 RANKL/OPG 轴和雌激素受体-α

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-23 DOI: 10.1016/j.fitote.2024.106226

Walaa S.A. Mettwally , Rehab A. Hussein , Gehad A. Abdel Jaleel , Azza Hassan , Dalia O. Saleh , Ahmed A. El-Beih

The present study aimed to examine the effect of Calotropis procera (Aiton) and its major cardenolides; calotropin and gomphogenin on ovariectomy-induced osteoporosis in rats. Osteoporotic rats were orally treated with C. procera alcoholic extract (100 mg/kg), calotropin (CLT; 100 μg/kg) and gomphogenin (GPG; 100 μg/kg) for 14 consecutive days. Bone resorption/formation biomarkers; bone specific alkaline phosphatase (BALP), osteoprotegerin (OPG) and nuclear factor-κβ ligand (RANKL) as well as serum calcium and phosphorus were assessed 24 h after last doses of treatments. Serum levels of estradiol (E2) and catalase were also measured.

Oral treatment with C. procera extract, CLT and GPG caused E2 restoration to normal level with a marked regulation in the RANKL/OPG axis. Serum phosphorus and calcium were up-leveled whereas BALP was downregulated. Histopathological examination, bone histomorphometric analysis and immunohistochemical staining for osteopontin (OPN) inspection further emphasized the aforementioned outcomes. The results revealed the superiority of CLT and to a lesser extent GPG osteoporotic effect over C. procera extract. Molecular docking of the two compounds on ER-α and RANKL/OPG complex showed noteworthy binding affinities which also confirmed the supremacy of CLT due to the additional hydrogen bonding of the hydroxyl groups of the sugar moiety with RANKL/OPG complex. Finally, it is concluded that CLT and GPG from C. procera hinder bone turnover by decreasing osteoclastic bone cells activity and increasing calcium mineralization thus suppressing bone remodeling and preventing bone infirmity in OVX osteoporotic rats directly via binding to RANKL/OPG complex and ER-α and indirectly through elevating level of E2.

本研究的目的是探讨普鲁卡因（Calotropis procera，Aiton）及其主要贲门醇内酯--卡洛托品（calotropin）和鹅掌揪素（gomphogenin）对卵巢切除术诱发的大鼠骨质疏松症的影响。对骨质疏松症大鼠连续 14 天口服普鲁卡因酒精提取物（100 毫克/千克）、卡洛托品（CLT；100 微克/千克）和 gomphogenin（GPG；100 微克/千克）。在最后一次给药 24 小时后，对骨吸收/形成生物标志物、骨特异性碱性磷酸酶（BALP）、骨保护素（OPG）和核因子κβ配体（RANKL）以及血清钙和磷进行评估。雌二醇（E2）和过氧化氢酶的血清水平也进行了测定。口服普鲁卡因提取物、CLT和GPG可使E2恢复到正常水平，并显著调节RANKL/OPG轴。血清磷和钙的水平有所提高，而 BALP 则有所降低。组织病理学检查、骨组织形态学分析和骨生成素（OPN）免疫组化染色检查进一步证实了上述结果。结果显示，CLT 的骨质疏松效果优于 C. procera 提取物，GPG 的骨质疏松效果次之。这两种化合物在 ER-α 和 RANKL/OPG 复合物上的分子对接显示了值得注意的结合亲和力，这也证实了 CLT 的优越性，因为糖分子的羟基与 RANKL/OPG 复合物有额外的氢键结合。最后，我们得出的结论是，白花蛇舌草中的 CLT 和 GPG 能降低破骨细胞的活性，增加钙矿化，从而抑制骨重塑，通过与 RANKL/OPG 复合物和 ER-α 直接结合，以及通过提高 E2 水平间接地防止 OVX 骨质疏松症大鼠的骨质疏松。

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引用次数: 0

Genus Castanopsis: A review on phytochemistry and biological activities 栲属：植物化学和生物活性综述。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-18 DOI: 10.1016/j.fitote.2024.106216

Bing-Yuan Yang, Ya-Feng Wang, Gui-Qin Li, Rui-Jie He, Yong-Lin Huang

Genus Castanopsis are native to tropical and subtropical Asia, comprising about 120 species. Some species from Castanopsis have been used as folk medicines in Asia. Phytochemistry investigations of the different plant parts of Genus Castanopsis have disclosed the presences of natural products including phenolics, terpenoids, steroids, and essential oils. Phenolics exist in Castanopsis species widely, particularly, triterpene ellagitannins were found to be potential chemotaxonomic marks of this geuns. The crude extracts and chemical constituents from Castanopsis have extensive biological activities, such as anti-inflammatory, anti-oxidative, antimicrobial, etc. In conclusion, the phytochemistry and biological activities of genus Castanopsis make it a promising source of natural products for drug discovery and development. This review collected the literatures published prior to 2023 on the traditional medicinal uses, phytochemistry, and bioactivties of the genus Castanopsis by searching from several scientific databases, such as Elsevier, Sci-finder, PubMed, Web of Science, CNKI, and Baidu Scholar. The main purpose of this systematic review is to provide the available information for relevant scholars to understand the progress in phytochemistry and biological activies of the genus Castanopsis and help the further development of this genus.

栲属原产于亚洲热带和亚热带地区，约有 120 个品种。Castanopsis 的一些种类在亚洲被用作民间药物。对栲属植物不同部分进行的植物化学研究发现，其中存在酚类、萜类、甾体和精油等天然产品。酚类物质广泛存在于栲属植物中，尤其是三萜类鞣花丹宁被认为是该属植物潜在的化学分类标志。栲胶的粗提取物和化学成分具有广泛的生物活性，如抗炎、抗氧化、抗菌等。总之，拟南芥属的植物化学和生物活性使其成为药物发现和开发的一个很有前景的天然产品来源。本综述通过检索 Elsevier、Sci-finder、PubMed、Web of Science、CNKI 和百度学术等多个科学数据库，收集了 2023 年之前发表的有关栲属植物传统药用、植物化学和生物活性的文献。本系统综述的主要目的是为相关学者提供现有信息，以了解栲属植物化学和生物活性方面的进展，帮助该属植物的进一步发展。

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引用次数: 0

Bioactive abietenolide diterpenes from Suregada procera 来自 Suregada procera 的具有生物活性的 Abietenolide 二萜。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-18 DOI: 10.1016/j.fitote.2024.106217

Jackson Obegi Matundura , Jackson T. Mollel , Masum Miah , Joanna Said , Leonidah K. Omosa , Thobias M. Kalenga , Yannik T. Woordes , Vaderament-Alexe Nchiozem-Ngnitedem , Andreas Orthaber , Jacob O. Midiwo , Wouter Herrebout , Edward Trybala , Tomas Bergström , Luis Apaza Ticona , Mate Erdelyi , Abiy Yenesew

The phytochemical investigation of the leaves and the roots of Suregada procera afforded the new ent-abietane diterpenoid sureproceriolide A (1) along with the known secondary metabolites 8,14β:11,12α-diepoxy-13(15)-abietane-16,12-olid (2), jolkinolide A (3), jolkinolide E (4), ent-pimara-8(14),15-dien-19-oic acid (5), sitosterol (6), oleana-9(11):12-dien-3β-ol (7), and oleic acid (8). Their structures were elucidated by NMR spectroscopic and mass spectrometric analyses, and the structure of jolkinolide A (3) was confirmed by single-crystal X-ray diffraction analysis. Sureproceriolide A (1) showed modest activity against the Gram-positive bacterium Staphylococcus lugdunensis (MIC = 31.44 μM), and sitosterol (6) against the Gram-negative bacterium Porphyromonas gingivalis (IC₅₀ = 45.37 μM). Jolkinolide A (3) and E (4) as well as sitosterol (6) inhibited the release of NOS (IMR-90 cells), TNF-α (HaCaT cells) and NF-κB (HaCaT cells), with IC₅₀ values of 0.43, 3.21, and 10.32 μM, respectively. Compound 6 showed antitumoral activity against SK-MEL-28 (IC₅₀ = 20.66 μM) and CCD-13Lu (IC₅₀ = 24.70 μM) cell lines, with no cytotoxic effect against the prostate cells PrEC (CC₅₀ > 300 μM).

对 Suregada procera 的叶和根进行的植物化学研究发现了新的内阿比坦二萜类物质 sureproceriolide A (1)，以及已知的次生代谢物 8,14β：11,12α-diepoxy-13(15)-abietane-16,12-olid (2)、jolkinolide A (3)、jolkinolide E (4)、ent-pimara-8(14),15-dien-19-oic acid (5)、sitosterol (6)、oleana-9(11):12-dien-3β-ol (7) 和 oleic acid (8)。核磁共振光谱和质谱分析阐明了它们的结构，单晶 X 射线衍射分析证实了金丝桃内酯 A（3）的结构。Sureproceriolide A（1）对革兰氏阳性菌卢格杜氏葡萄球菌（MIC = 31.44 μM）显示出适度的活性，而 sitosterol（6）对革兰氏阴性菌牙龈卟啉单胞菌（IC50 = 45.37 μM）显示出适度的活性。Jolkinolide A（3）和 E（4）以及西坦醇（6）可抑制 NOS（IMR-90 细胞）、TNF-α（HaCaT 细胞）和 NF-κB （HaCaT 细胞）的释放，其 IC50 值分别为 0.43、3.21 和 10.32 μM。化合物 6 对 SK-MEL-28 细胞株（IC50 = 20.66 μM）和 CCD-13Lu 细胞株（IC50 = 24.70 μM）具有抗肿瘤活性，而对前列腺细胞 PrEC（CC50 > 300 μM）没有细胞毒性作用。

{"title":"Bioactive abietenolide diterpenes from Suregada procera","authors":"Jackson Obegi Matundura , Jackson T. Mollel , Masum Miah , Joanna Said , Leonidah K. Omosa , Thobias M. Kalenga , Yannik T. Woordes , Vaderament-Alexe Nchiozem-Ngnitedem , Andreas Orthaber , Jacob O. Midiwo , Wouter Herrebout , Edward Trybala , Tomas Bergström , Luis Apaza Ticona , Mate Erdelyi , Abiy Yenesew","doi":"10.1016/j.fitote.2024.106217","DOIUrl":"10.1016/j.fitote.2024.106217","url":null,"abstract":"<div><div>The phytochemical investigation of the leaves and the roots of Suregada procera afforded the new ent-abietane diterpenoid sureproceriolide A (1) along with the known secondary metabolites 8,14β:11,12α-diepoxy-13(15)-abietane-16,12-olid (2), jolkinolide A (3), jolkinolide E (4), ent-pimara-8(14),15-dien-19-oic acid (5), sitosterol (6), oleana-9(11):12-dien-3β-ol (7), and oleic acid (8). Their structures were elucidated by NMR spectroscopic and mass spectrometric analyses, and the structure of jolkinolide A (3) was confirmed by single-crystal X-ray diffraction analysis. Sureproceriolide A (1) showed modest activity against the Gram-positive bacterium Staphylococcus lugdunensis (MIC = 31.44 μM), and sitosterol (6) against the Gram-negative bacterium Porphyromonas gingivalis (IC50 = 45.37 μM). Jolkinolide A (3) and E (4) as well as sitosterol (6) inhibited the release of NOS (IMR-90 cells), TNF-α (HaCaT cells) and NF-κB (HaCaT cells), with IC50 values of 0.43, 3.21, and 10.32 μM, respectively. Compound 6 showed antitumoral activity against SK-MEL-28 (IC50 = 20.66 μM) and CCD-13Lu (IC50 = 24.70 μM) cell lines, with no cytotoxic effect against the prostate cells PrEC (CC50 > 300 μM).</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"179 ","pages":"Article 106217"},"PeriodicalIF":2.5,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142282618","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chemical constituents of five Saxifraga species and their virucidal activities 五种 Saxifraga 品种的化学成分及其杀病毒活性。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-09-14 DOI: 10.1016/j.fitote.2024.106215

Nanami Kurosawa , Yohei Takeda , Yoshimi Ichimaru , Dulamjav Jamsransuren , Sachiko Matsuda , Yoshinobu Ishikawa , Minori Yamaguchi , Haruko Ogawa , Kenroh Sasaki , Toshihiro Murata

The chemical constituents of Saxifraga stolonifera, S. fortunei, S. nipponica, S. cortusifolia, and S. rebunshirensis were investigated for structure and virucidal activity. In addition to the Saxifraga species-derived tannins, 30 compounds (1−30) were isolated from the five species. 5-Hydroxy-4-methoxy-3-O-(6-O-caffeoyl)-β-D-glucopyranosyl benzoic acid (1) and kaempferol 3-O-β-d-xylopyranosyl-(1 → 2)-β-D-xylopyranoside (2) were identified as undescribed compounds. Although 1 was isolated as the (E)-isomer of its caffeoyl moiety, under light it became over time a mixture of the (Z)-isomer (1a) and (E)-isomer (1). Kaempferol 3-O-β-d-xylopyranosyl-(1 → 2)-β-D-glucopyranoside (3) was an analog of 2 and a known compound, whose NMR assignment was reconsidered and described. 6-Isopropyl-5,5-dimethyldihydropyrimidine-2,4(1H,3H)-dione (30) was expected to be a racemic mixture based on its optical rotation and X-ray crystallography data. The virucidal activities of the isolated compounds (1–30) against influenza A virus, severe acute respiratory syndrome coronavirus 2, feline calicivirus, and murine norovirus were evaluated to identify the presence of compounds other than the Saxifraga species-derived tannins, which exhibited virucidal activities. Although the isolated compound activities were relatively weak compared to those of Saxifraga species-derived tannins, the potential virucidal activity of the compounds with galloyl groups was confirmed.

研究了 Saxifraga stolonifera、S. fortunei、S. nipponica、S. cortusifolia 和 S. rebunshirensis 的化学成分结构和杀病毒活性。除了从 Saxifraga 物种中提取的单宁外，还从这五个物种中分离出了 30 种化合物（1-30）。5-羟基-4-甲氧基-3-O-(6-O-咖啡酰基)-β-D-吡喃葡萄糖基苯甲酸（1）和山柰酚 3-O-β-D-吡喃木糖基-(1→2)-β-D-吡喃木糖苷（2）被鉴定为未描述的化合物。虽然 1 是作为其咖啡酰基的 (E) -异构体分离出来的，但在光照下，随着时间的推移，它变成了 (Z) -异构体 (1a) 和 (E) -异构体 (1) 的混合物。堪非醇 3-O-β-d-xylopyranosyl-(1 → 2)-β-D-glucopyranoside (3) 是 2 的类似物，也是一种已知化合物，对其 NMR 赋值进行了重新考虑和描述。根据 6-异丙基-5,5-二甲基二氢嘧啶-2,4(1H,3H)-二酮（30）的光学旋转和 X 射线晶体学数据，预计它是一种外消旋混合物。评估了分离出的化合物（1-30）对甲型流感病毒、严重急性呼吸系统综合征冠状病毒 2、猫犊牛病毒和小鼠诺沃克病毒的杀病毒活性，以确定除西夏属物种衍生的单宁酸外，还存在其他具有杀病毒活性的化合物。虽然分离出的化合物活性相对于西番莲萃取的单宁较弱，但带有五倍子基团的化合物的潜在杀病毒活性得到了证实。

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引用次数: 0