Fitoterapia最新文献_第5页

Antitrypanosomal activity of Crossopteryx febrifuga and phytochemical profiling using LC-MS/MS analysis coupled to molecular network and SIRIUS 利用与分子网络和 SIRIUS 相结合的 LC-MS/MS 分析方法，研究 Crossopteryx febrifuga 的抗红斑狼疮活性和植物化学成分分析。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-12 DOI: 10.1016/j.fitote.2024.106255

Esaïe Tchetan , Sergio Ortiz , Pascal Abiodoun Olounladé , Erick Virgile Bertrand Azando , Claire Avril , Dominique Demblon , Sylvie Mawule Hounzangbe-Adote , Fernand Ahokanou Gbaguidi , Joëlle Quetin-Leclercq

Crossopteryx febrifuga (Rubiaceae) is a plant widely used in traditional African medicine to treat tryapnosomiasis. The aim of our study was to evaluate the antitrypanosomal activity of C. febrifuga extracts and to identify the compounds responsible for this activity. We prepared 4 extracts by successive maceration of plant leaf powder in n-hexane, dichloromethane, methanol and water. The antitrypanosomal activity of the extracts was assessed on Trypanosoma brucei brucei and their selectivity on Leishmania mexicana mexicana and human non cancer WI38 fibroblast cells. The dichloromethane extract, the most antitrypanosomal (IC₅₀ of 9.3 ± 0.8 μg/mL) was fractionated on an Open Column Chromatography to give 14 fractions. Fractions 6–9 were the most active with an IC₅₀ ranging from 1.3 to 2.1 μg/mL. All fractions were analyzed by UPLC-ZenoTOFHRMS, followed by manual dereplication of metabolites detected in the most active fractions. Manual dereplication was aided by the Molecular Network (MN) and SIRIUS. Metabolic profiling of fractions 6–9 has enabled us to identify 33 compounds, most of which were reported for the first time in C. febrifuga. These include buddlenol C (6), naringenin (7), maslinic acid (22), corosolic acid or isomer (24), asperphenamate (25), hydroxyoctadecenoic acid (29), sumaresinolic acid or isomer I and II (30 and 31), glycyrrhetinic acid (32) and oleanolic acid (36). The bioactivity-based approach identified maslinic (22), corosolic (24), and oleanolic (36) acids as linked to the antitrypanosomal activity. The data obtained support the traditional use of C. febrifuga in the traditional treatment of trypanosomiasis. Further studies are required to verify the activity observed in vivo.

在非洲传统医学中，Crossopteryx febrifuga（茜草科）被广泛用于治疗锥虫病。我们研究的目的是评估 C. febrifuga 提取物的抗锥虫病活性，并确定产生这种活性的化合物。我们用正己烷、二氯甲烷、甲醇和水连续浸泡植物叶粉，制备了 4 种提取物。我们评估了这些提取物对布氏锥虫的抗锥虫活性，以及它们对墨西哥利什曼原虫和人类非癌症 WI38 成纤维细胞的选择性。二氯甲烷提取物的抗盘虫能力最强（IC50 为 9.3 ± 0.8 μg/mL），经开放柱色谱法分馏后得到 14 个馏分。馏分 6-9 的活性最强，IC50 在 1.3 至 2.1 μg/mL 之间。所有馏分均通过 UPLC-ZenoTOFHRMS 进行分析，然后对活性最强的馏分中检测到的代谢物进行人工去复制。手动去复制由分子网络（MN）和 SIRIUS 协助完成。通过对馏分 6-9 进行代谢分析，我们确定了 33 种化合物，其中大部分是首次在 C. febrifuga 中发现。其中包括佛手酚 C（6）、柚皮苷（7）、马斯林酸（22）、科罗索酸或异构体（24）、天门冬氨酸（25）、羟基十八碳烯酸（29）、苏木精酸或异构体 I 和 II（30 和 31）、甘草次酸（32）和齐墩果酸（36）。基于生物活性的方法确定了马斯林酸（22）、科罗索酸（24）和齐墩果酸（36）与抗锥虫活性有关。获得的数据支持了 C. febrifuga 在锥虫病传统治疗中的传统用途。要验证在体内观察到的活性，还需要进一步的研究。

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引用次数: 0

Ginseng fruit rare saponins (GFRS) improved inflammatory response: In vitro and in vivo assessment 人参果稀有皂甙（GFRS）可改善炎症反应：体外和体内评估

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-11 DOI: 10.1016/j.fitote.2024.106244

Yifei Zheng , Hongyan Tan , Jiayi Chai , Linlin Han , Changzhen Zhai , Jungjoon Lee , Xiaomin Li , Yuqing Zhao

Inflammation is the body's protective immune response to tissue damage. Ginseng has a long history of medicinal use, and its active ingredient ginsenosides have anti-inflammatory effects. Ginseng fruit rare saponins (GFRS) is a transformation product of ginseng saponins and rich in a variety of rare saponins. We used HPLC-DAD method to study GFRS rare saponins with ginsenoside F4, R-Rg₃, SRg₃, Rk₁, Rg₆, Rg₅, Rk₃ and Rh₄. However, there is no study on the use of GFRS to reduce skin inflammation. This study enriched the action pathway of GFRS through network pharmacology and revealed the anti-inflammatory effect of GFRS for the first time. In vitro experiments showed that GFRS could significantly reduce the release of NO in lipopolysaccharide (LPS) -induced RAW264.7 cells and HaCaT cells, and reduce the secretion and expression of inflammation-related factors Interleukin-6 (IL-6), Tumor necrosis factor-α (TNF-α) and Interleukin-17 A (IL-17 A), thereby reducing cell inflammatory damage. In the imiquimod (IMQ) -induced mouse inflammatory model, the therapeutic effect of GFRS on the pathogenesis of psoriasis-like dermatitis was studied. In vivo experiments showed that the skin erythema, scales, thickness and inflammatory infiltration of GFRS-treated mice were reduced, and the psoriasis area severity index score was significantly lower than that of IMQ group. GFRS restored IMQ-induced spleen size and reduced the secretion and expression of TNF-α, IL-6, Interferon-γ (IFN-γ) and IL-17 A in serum. In summary, our results demonstrate that GFRS alleviates IMQ-induced dermatitis symptoms, effectively reduces the secretion of inflammatory factors, and inhibits IL-17 A expression.

炎症是人体对组织损伤的保护性免疫反应。人参的药用历史悠久，其有效成分人参皂苷具有抗炎作用。人参果稀有皂甙（GFRS）是人参皂甙的转化产物，富含多种稀有皂甙。我们采用 HPLC-DAD 方法研究了人参果稀有皂苷，包括人参皂苷 F4、R-Rg3、SRg3、Rk1、Rg6、Rg5、Rk3 和 Rh4。然而，目前还没有关于使用 GFRS 减少皮肤炎症的研究。这项研究通过网络药理学丰富了 GFRS 的作用途径，并首次揭示了 GFRS 的抗炎作用。体外实验表明，GFRS能显著减少脂多糖（LPS）诱导的RAW264.7细胞和HaCaT细胞中NO的释放，降低炎症相关因子白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）和白细胞介素-17 A（IL-17 A）的分泌和表达，从而减轻细胞炎症损伤。在咪喹莫特（IMQ）诱导的小鼠炎症模型中，研究了 GFRS 对银屑病样皮炎发病机制的治疗作用。体内实验表明，GFRS 治疗组小鼠的皮肤红斑、鳞屑、厚度和炎症浸润均减轻，银屑病面积严重性指数评分明显低于 IMQ 组。GFRS可恢复IMQ诱导的脾脏大小，减少血清中TNF-α、IL-6、干扰素-γ（IFN-γ）和IL-17 A的分泌和表达。总之，我们的研究结果表明，GFRS 可减轻 IMQ 引起的皮炎症状，有效减少炎症因子的分泌，并抑制 IL-17 A 的表达。

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引用次数: 0

Lignans and phenols with potential anti-inflammatory effect from the stems of Mallotus paxii Pamp 具有潜在抗炎作用的山苍子茎木酚素和酚类物质

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-11 DOI: 10.1016/j.fitote.2024.106253

Yan Huang , Ping Hou , Liwei Pan , Jian Li , Xiaoqin Liang , Chenyang Ren , Liuting Peng , Chunqiu Gan , Weifeng Xu , Ruiyun Yang , Jun Li , Xinlan Guan

Phytochemical investigation of the stems of Mallotus paxii Pamp. led to the isolation and identification of four new compounds, including three neolignans (1–3) and one phenol (13), along with eight known neolignans (4–12) and one known phenol (14). Their structures were determined by spectroscopic methods, including NMR, MS and ECD analyses. Bioassay demonstrated that malloapelin A (4) exhibited a most potent anti-inflammatory activity to NO release with IC₅₀ value of 21.32 μM. Furthermore, malloapelin A (4) markedly decreased the secretion of TNF-α, iNOS, and NF-κB and inhibited the expression of COX-2 and NF-κB/p65 in LPS-induced RAW264.7 cells in a dose-dependent manner.

通过对 Mallotus paxii Pamp.茎进行植物化学研究，分离并鉴定了四种新化合物，包括三种新木质素（1-3）和一种酚（13），以及八种已知的新木质素（4-12）和一种已知的酚（14）。这些化合物的结构是通过光谱方法确定的，包括 NMR、MS 和 ECD 分析。生物测定表明，毛果芸香素 A（4）对 NO 的释放具有最强的抗炎活性，IC50 值为 21.32 μM。此外，在 LPS 诱导的 RAW264.7 细胞中，毛果芸香素 A (4) 能以剂量依赖的方式显著降低 TNF-α、iNOS 和 NF-κB 的分泌，并抑制 COX-2 和 NF-κB/p65 的表达。

引用次数: 0

Effects of morroniside isolated from Cornus officinalis fruits on functional gastrointestinal disorders and gastric ulcer in mice 从山茱萸果实中分离出的山茱萸苷对小鼠功能性胃肠功能紊乱和胃溃疡的影响

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-11 DOI: 10.1016/j.fitote.2024.106249

Yoshiyuki Kimura , Masahiko Taniguchi

The dried fruits of Cornus officinalis (Cornaceae) are used in Kampo medicine (e.g. Hachimigan and Goshajinkigan) to treat senile osteoporosis, diabetes, gastric atony, frequent urination, and diarrhea/constipation associated with aging. The present study investigated the effects of a C. officinalis fruit extract and morroniside, an iridoid compound from isolated these fruits, on the reduction in gastric emptying small intestinal motility caused by 5-hydroxytryptamine (5-HT) and 1-(3-chlorophenyl) biguanide (5-HT₃ receptor agonist), and gastric ulcers induced by 150 or 75 mM HCl/90 % EtOH (HCl-EtOH) and/or 5-HT in mice. C. officinalis extract (500 mg/kg) and morroniside (20 and 50 mg/kg) suppressed the reduction in gastric emptying induced by 5-HT- and 5-HT₃ agonist. C. officinalis extract, morroniside and 5-HT₃ receptor antagonist (ramosetron) attenuated 5-HT-induced diarrhea. Furthermore, morroniside (20 and 50 mg/kg) prevented EtOH/HCl-induced gastric ulcers and those caused by 5-HT. Morroniside (20 and 50 mg/kg) attenuated elevations in the plasma levels of corticosterone, corticotropin-releasing factor (CRF), and adrenocorticotropic hormone (ACTH) in 75 mM HCl/90 % EtOH- and 5-HT-treated mice. The results obtained herein suggest the potential of morroniside as an effective treatment for irritable bowel syndrome, such as diarrhea and functional dyspepsia (reductions in gastric emptying and small intestinal motility), caused by 5-HT. The present study suggests a role for morroniside in the regulation of elevations in CRF, ACTH, and corticosterone levels through hypothalamic-pituitary-adrenal axis activity induced by stress loading, such as a 5-HT treatment and/or HCl/EtOH stimulation.

山茱萸（山茱萸科）的干燥果实在堪布医药（如 Hachimigan 和 Goshajinkigan）中被用于治疗老年性骨质疏松症、糖尿病、胃失弛缓症、尿频以及与衰老有关的腹泻/便秘。本研究调查了欧当归果实提取物和morroniside（一种从这些果实中分离出来的鸢尾类化合物）对5-羟色胺（5-HT）和1-（3-氯苯基）双胍（5-HT3受体激动剂）引起的胃排空减少、150或75 mM HCl/90 % EtOH（HCl-EtOH）和/或5-HT诱发的小鼠胃溃疡的影响。欧当归提取物（500 毫克/千克）和吗罗尼苷（20 和 50 毫克/千克）可抑制 5-HT 和 5-HT3 激动剂引起的胃排空减少。欧当归提取物、吗罗尼苷和 5-HT3 受体拮抗剂（雷莫司琼）减轻了 5-HT 引起的腹泻。此外，莫罗尼甙（20 和 50 毫克/千克）还能预防乙醇/HCl 引起的胃溃疡和 5-HT 引起的胃溃疡。莫罗尼甙（20 和 50 毫克/千克）可减轻 75 mM HCl/90 % EtOH 和 5-HT 处理的小鼠血浆中皮质酮、促肾上腺皮质激素释放因子（CRF）和促肾上腺皮质激素（ACTH）水平的升高。本研究的结果表明，吗罗尼甙有可能成为治疗肠易激综合征的有效药物，如 5-HT 引起的腹泻和功能性消化不良（胃排空和小肠蠕动减少）。本研究表明，莫罗尼苷可通过应激负荷（如 5-HT 治疗和/或 HCl/EtOH 刺激）诱导的下丘脑-垂体-肾上腺轴活动，在调节 CRF、ACTH 和皮质酮水平升高方面发挥作用。

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引用次数: 0

Acremochlorin S and other prenylated chlorophenol antimicrobial metabolites from the fungus Acremonium sp. Strain MNA-F-1 来自 Acremonium sp. Strain MNA-F-1 真菌的 Acremochlorin S 和其他前炔化氯苯酚抗菌代谢物

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-11 DOI: 10.1016/j.fitote.2024.106254

Mohamed S. Elnaggar , Nada M. Mostafa , Ahmed M. Elissawy , Kunthida Phutthacharoen , Paul Eckhardt , Birthe Sandargo , Lasse van Geelen , Sherif S. Ebada , Till Opatz , Abdel Nasser B. Singab , Rainer Kalscheuer

Chemical prospection for the mycelial extract of the fungus Acremonium sp. Strain MNA-F-1, derived from the inner tissue of anise roots (Pimpnella anisum L., family Apiaceae), led to the isolation and characterization of one previously undescribed natural product, acremochlorin S (1), together with five related derivatives (2–6) and an alkaloidal metabolite, ilicicolin H (7). Structure elucidation of the isolated compounds was determined through comprehensive 1D/2D NMR spectroscopic analyses and HR-ESI-MS measurements. The absolute configuration of acremochlorin S (1) was concluded based on the comparison of its experimental and calculated electronic circular dichroism (ECD) spectra implementing Time-dependent density functional theory (TDDFT). All isolated compounds were assessed for their antibacterial activity against Staphylococcus aureus, Escherichia coli and Mycobacterium tuberculosis, where several compounds revealed potent activities against tested Gram-positive strains.

从八角根（Pimpnella anisum L.，芹科）内部组织中提取的真菌 Acremonium sp. 菌株 MNA-F-1 的菌丝体提取物进行了化学研究，分离并鉴定了一种以前未曾描述过的天然产物 acremochlorin S (1)，以及五种相关衍生物 (2-6) 和一种生物碱代谢物 ilicicolin H (7)。通过全面的 1D/2D NMR 光谱分析和 HR-ESI-MS 测量，确定了这些分离化合物的结构。根据实验光谱与采用时间相关密度泛函理论（TDDFT）计算得出的电子圆二色性（ECD）光谱的对比结果，确定了 acremochlorin S（1）的绝对构型。评估了所有分离化合物对金黄色葡萄球菌、大肠杆菌和结核分枝杆菌的抗菌活性，其中几个化合物显示出对测试的革兰氏阳性菌株具有强效活性。

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引用次数: 0

Bioactivities of Sargassum elegans, Bryopsis myosuroides, Callophyllis variegata seaweeds on diabetes and obesity-related biochemical parameters: A comparative in vitro study Sargassum elegans、Bryopsis myosuroides 和 Callophyllis variegata 海藻对糖尿病和肥胖相关生化指标的生物活性：体外比较研究

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-11 DOI: 10.1016/j.fitote.2024.106252

S'thandiwe N. Magwaza , Kolawole A. Olofinsan , Almahi I. Mohamed , Balaji Meriga , Md. Shahidul Islam

Diabesity’ is the occurrence of diabetes in the presence of obesity. Numerous reports have shown that seaweeds possess beneficial biological activities. This study assessed the effects of three seaweeds Bryopsis myosuroides (green), Callophyllis variegata (red), and Sargassum elegans (brown), on diabetes and obesity-related parameters in vitro. The antioxidant potential, carbohydrate and lipid digestive enzyme inhibitory activity, and glucose uptake activities of ethanolic and sulphated polysaccharides (SPs) rich extracts were evaluated. The SP-rich or ethanolic extracts of S. elegans showed the greater inhibition of 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC₅₀ 46.6 ± 1.00 g/mL), hydroxyl radical (OH) (IC₅₀ 353.70 ± 2.01 μg/mL), and nitric oxide (NO) (IC₅₀ 407.5 ± 0.95 μg/mL) compared to other seaweeds. Moreover, the SP-rich extract of S. elegans exhibited higher inhibition of α- glucosidase (IC₅₀ 123.8 ± 1.69 μg/mL), whereas B. myosuroides SP-rich extract had better α-amylase (IC₅₀ 55.7 ± 0.98 μg/mL) and pancreatic lipase inhibitory activities (IC₅₀ 481.1 ± 0.9 μg/mL) compared to other seaweeds. Liquid Chromatography Mass Spectroscopy (LC-MS) was used to identify the compounds present in the seaweed extracts. These include Taxifolin, Amentoflavone-7,4′,4″‘-Trimethyl Ether, Chrysophenol, and Glucotropaeolin, which have been previously reported to possess biological activities beneficial to human health. Although all three seaweeds evaluated in this study demonstrated antioxidant, digesting enzyme inhibitory and glucose uptake activity to different extents, S. elegans (brown) depicted the highest activity in most assays compared to the other seaweeds. However, further research is required to assess the effects of these seaweed extracts on diabetes and obesity via ex vivo and in vivo experimental animal models.

肥胖症 "是指在肥胖的情况下出现糖尿病。大量报告显示，海藻具有有益的生物活性。本研究评估了三种海藻 Bryopsis myosuroides（绿色）、Callophyllis variegata（红色）和 Sargassum elegans（棕色）在体外对糖尿病和肥胖相关参数的影响。评估了乙醇提取物和富含硫酸化多糖（SPs）提取物的抗氧化潜力、碳水化合物和脂质消化酶抑制活性以及葡萄糖摄取活性。与其他海藻相比，秀丽海藻的富含 SP 或乙醇提取物对 2,2-二苯基-1-苦基肼（DPPH）（IC50 46.6 ± 1.00 g/mL）、羟自由基（OH）（IC50 353.70 ± 2.01 μg/mL）和一氧化氮（NO）（IC50 407.5 ± 0.95 μg/mL）的抑制作用更强。此外，与其他海藻相比，S. elegans 的富 SP 提取物对α-葡萄糖苷酶（IC50 123.8 ± 1.69 μg/mL）有更高的抑制作用，而 B. myosuroides 的富 SP 提取物对α-淀粉酶（IC50 55.7 ± 0.98 μg/mL）和胰脂肪酶（IC50 481.1 ± 0.9 μg/mL）有更好的抑制作用。液相色谱质谱法（LC-MS）用于鉴定海藻提取物中的化合物。这些化合物包括 Taxifolin、Amentoflavone-7,4',4″'-Trimethyl Ether、Chrysophenol 和 Glucotropaeolin。虽然本研究中评估的三种海藻都在不同程度上表现出抗氧化、抑制消化酶和葡萄糖吸收的活性，但与其他海藻相比，秀丽海藻（棕色）在大多数测定中表现出最高的活性。不过，还需要进一步研究，通过体内外实验动物模型评估这些海藻提取物对糖尿病和肥胖症的影响。

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引用次数: 0

DMOA-derived polycyclic meroterpenoids with antiviral activities from the deep-sea-derived fungus Penicillium pancosmium A6A 来自深海源真菌青霉 A6A 的具有抗病毒活性的 DMOA 衍生多环美拉皮素。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-10 DOI: 10.1016/j.fitote.2024.106248

Ziming Chen , Yinghui Lv , Zhuhua Luo , Bihong Hong , Siwen Niu

Two undescribed 3,5-dimethylorsellinic acid (DMOA) derived meroterpenoids, namely pancosterpenoids A (1) and B (2), were discovered from the EtOAc extract of the deep-sea sediment-derived fungus Penicillium pancosmium A6A. The gross structures were established by detailed analysis of the spectroscopic data (NMR and HRESIMS spectra), while their absolute configurations were resolved by comparing the experimental and calculated ECD data as well as X-ray single crystal diffraction analysis. Pancosterpenoid A (1) was the first representative of DMOA-derived meroterpenoids possessing a 6/6/6/5/5 pentacyclic system, while pancosterpenoid B (2) belongs to a class of rare 13-nor-citreohybridone meroterpenoids. Two metabolites were evaluated the antiviral effects against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) trVLP pseudovirus. As a result, compounds 1 and 2 showed moderately inhibitory activities with IC₅₀ values of 22.37 and 18.12 μM, respectively.

从源于深海沉积物的真菌青霉 A6A 的乙酸乙酯提取物中发现了两种未曾描述过的 3,5-二甲基月桂酸（DMOA）衍生美拉皮素，即泛醇类 A (1) 和 B (2)。通过对光谱数据（核磁共振和 HRESIMS 光谱）的详细分析，确定了它们的总体结构，同时通过比较实验和计算的 ECD 数据以及 X 射线单晶衍射分析，确定了它们的绝对构型。Pancosterpenoid A（1）是第一个具有 6/6/6/5/5 五环体系的 DMOA 衍生经并萜类化合物的代表，而 Pancosterpenoid B（2）则属于罕见的 13-nor-citreohbridyone 经并萜类化合物。研究人员评估了这两种代谢物对严重急性呼吸系统综合征冠状病毒-2（SARS-CoV-2）trVLP 伪病毒的抗病毒作用。结果表明，化合物 1 和 2 显示出中等程度的抑制活性，IC50 值分别为 22.37 和 18.12 μM。

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引用次数: 0

Apocarotenoids from the fresh roots of Rehmannia glutinosa and their anti-pulmonary fibrosis activity 地黄鲜根中的类胡萝卜素及其抗肺纤维化活性

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-10 DOI: 10.1016/j.fitote.2024.106247

Xiang-Da Li , Yan-Gang Cao , Yu-Han Zhang , Ying-Jie Ren , Meng-Nan Zeng , Yan-Ling Liu , Xu Chen , Xin-Yi Ma , Bing-Xian Zhao , Xiao-Ke Zheng , Wei-Sheng Feng

Six undescribed compounds (1–6) and twenty-three known analogues (7–29) were isolated from the fresh roots of Rehmannia glutinosa. The structures of the compounds (1–29) were established through the application of spectroscopic analysis. Compounds 3, 4, 6, 8, 13, 18, 21, 22, 25, and 28 exhibited excellent anti-pulmonary fibrosis activity. The potential mechanistic pathway of 3 was also investigated, whose results indicate that compound 3 ameliorate TGF-β1 induced BEAS-2B cell injury via PI3K/AKT/NF-κB signaling pathway.

从地黄的新鲜根中分离出了六种未曾描述过的化合物（1-6）和二十三种已知的类似物（7-29）。化合物（1-29）的结构是通过光谱分析确定的。化合物 3、4、6、8、13、18、21、22、25 和 28 表现出卓越的抗肺纤维化活性。研究人员还对化合物 3 的潜在机制途径进行了研究，结果表明化合物 3 可通过 PI3K/AKT/NF-κB 信号通路改善 TGF-β1 诱导的 BEAS-2B 细胞损伤。

引用次数: 0

Three undescribed isosteroidal alkaloids from the bulbs of Fritillaria ussuriensis maxim: Anti-inflammatory activities, docking studies and molecular dynamic 从 Fritillaria ussuriensis maxim 的鳞茎中提取的三种未被描述的异甾体生物碱：抗炎活性、对接研究和分子动力学

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-10 DOI: 10.1016/j.fitote.2024.106246

Dong-Xv Lu , Lei-Xin Zhuang , Peng Jiang , Yan-Ying Li , Yi-Qiang Zhang , Yu-Meng Luo , Juan Pan , Zhi-Chao Hao , Wei Guan , Qing-Shan Chen , Li-Li Zhang , Hai-Xue Kuang , Yan Liu , Bing-You Yang

Three undescribed isosteroidal alkaloids (1–3), along with two known ones (4, 5) were isolated from the bulbs of Fritillaria ussuriensis Maxim, their structures were established by comprehensive analyses of the 1D, 2D-NMR and HR-ESI-MS data. Meanwhile, LPS-activated RAW 264.7 macrophages were used to determine the potential anti-inflammatory activity of all the alkaloids in vitro. Among them, compounds 1 and 4 showed significant inhibitory effects against LPS-induced NO production with IC₅₀ values of 7.79 μM and 11.22 μM, respectively. Compounds 1 and 4 were performed between molecular docking with TLR4/MD2. Based on the results of cell experiments and binding affinities, compound 1 (UG) was chosen for molecular dynamic analysis together with the TLR4/MD2 protein.

通过一维、二维核磁共振和 HR-ESI-MS 数据的综合分析，从 Fritillaria ussuriensis Maxim 的鳞茎中分离出了三种未被描述的异甾体生物碱（1-3）和两种已知生物碱（4、5），并确定了它们的结构。同时，利用 LPS 激活的 RAW 264.7 巨噬细胞来测定所有生物碱的体外潜在抗炎活性。其中，化合物 1 和 4 对 LPS 诱导的 NO 生成有显著的抑制作用，IC50 值分别为 7.79 μM 和 11.22 μM。化合物 1 和 4 与 TLR4/MD2 进行了分子对接。根据细胞实验结果和结合亲和力，选择化合物 1（UG）与 TLR4/MD2 蛋白一起进行分子动力学分析。

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引用次数: 0

A greener side of health care: Revisiting phytomedicine against the human fungal pathogen Malassezia 医疗保健更环保的一面：重新审视针对人类真菌病原体马拉色菌的植物药。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2024-10-09 DOI: 10.1016/j.fitote.2024.106243

Jayaprakash Sasikumar, Keerthana P.P., Bharati Naik, Shankar Prasad Das

Malassezia species are commensal fungi residing on the skin and in the gut of humans and animals. Yet, under certain conditions, they become opportunistic pathogens leading to various clinical conditions including dermatological disorders. The emergence of drug resistance and adverse effects associated with conventional antifungal agents has propelled the search for alternative treatments, among which phytomedicine stands out prominently. Phytochemicals, including phenolic acids, flavonoids, and terpenoids, demonstrate potential antifungal activity against Malassezia by inhibiting its growth, adhesion, and biofilm formation. Furthermore, the multifaceted therapeutic properties of phytomedicine (including anti-fungal and, antioxidant properties) contribute to its efficacy in alleviating symptoms associated with Malassezia infections. Despite these promising prospects, several challenges hinder the widespread adoption of phytomedicine in clinical practice mostly since the mechanistic studies and controlled experiments to prove efficacy have not been done. Issues include standardization of herbal extracts, variable bioavailability, and limited clinical evidence. Hence, proper regulatory constraints necessitate comprehensive research endeavors and regulatory frameworks to harness the full therapeutic potential of phytomedicine. In conclusion, while phytomedicine holds immense promise as an alternative or adjunctive therapy against Malassezia, addressing these challenges is imperative to optimize its efficacy and ensure its integration into mainstream medical care. In this review we provide an update on the potential phytomedicines in combating Malassezia-related ailments, emphasizing its diverse chemical constituents and mechanisms of action.

马拉色菌是人类和动物皮肤和肠道中的共生真菌。然而，在某些条件下，它们会成为机会性病原体，导致包括皮肤病在内的各种临床症状。传统抗真菌药物的耐药性和不良反应的出现，推动了人们寻找替代治疗方法，其中植物药的作用尤为突出。包括酚酸、类黄酮和萜类化合物在内的植物化学物质通过抑制马拉色菌的生长、粘附和生物膜形成，对马拉色菌具有潜在的抗真菌活性。此外，植物药的多方面治疗特性（包括抗真菌和抗氧化特性）也有助于其有效缓解马拉色菌感染的相关症状。尽管前景广阔，但植物药在临床实践中的广泛应用仍面临一些挑战，主要是因为尚未开展机理研究和对照实验来证明其疗效。这些问题包括草药提取物的标准化、生物利用度的可变性以及有限的临床证据。因此，适当的监管约束需要全面的研究努力和监管框架，以充分发挥植物药的治疗潜力。总之，虽然植物药作为马拉色菌的替代或辅助疗法前景广阔，但要优化其疗效并确保其融入主流医疗保健，解决这些挑战势在必行。在本综述中，我们介绍了植物药在防治马拉色菌相关疾病方面的最新潜力，并强调了其不同的化学成分和作用机制。

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