Planta medica最新文献

Possibility and potential intervention targets of saffron extract in the treatment of atopic dermatitis: A Review.

IF 2.1 4区医学

Planta medica Pub Date : 2025-02-13 DOI: 10.1055/a-2538-5769

Huiyang Shi, Xuan Liu, Peiyi Zhao, Wei Huang, Hebin Wang, Heying Jin, Junyou Zhu, Jianwu Wang, Tianjiao Li

{"title":"Possibility and potential intervention targets of saffron extract in the treatment of atopic dermatitis: A Review.","authors":"Huiyang Shi, Xuan Liu, Peiyi Zhao, Wei Huang, Hebin Wang, Heying Jin, Junyou Zhu, Jianwu Wang, Tianjiao Li","doi":"10.1055/a-2538-5769","DOIUrl":"https://doi.org/10.1055/a-2538-5769","url":null,"abstract":"Atopic dermatitis (AD) is a chronic, recurrent inflammatory skin disorder characterized by dry skin, eczema-like lesions, and severe itching. The multifaceted etiology of AD, which is not yet fully understood, includes genetic predispositions, immune dysfunctions(such as an impaired skin barrier and abnormal immune regulation), imbalances in the skin microbiota, and environmental factors, among others. In the field of AD treatment, the combination of traditional Chinese medicine and modern medicine is becoming an emerging trend. Given the potential side effects and reduced efficacy of conventional therapeutic drugs, Chinese herbal medicines offer patients new treatment options because of their unique efficacy and low toxicity. Some saffron extracts derived from saffron and gardenia , such as crocin, crocetin, and safranal, have shown promising potential in the treatment of AD. These natural ingredients not only possess anti-inflammatory and immunomodulatory properties similar to those of traditional Chinese medicines but also demonstrate excellent effects in promoting the repair of damaged skin barriers. Therefore, this article reviews the therapeutic potential of saffron extract in the treatment of AD, with a special focus on its mechanisms and potential interventions, while emphasizing the importance of herbal medicines as alternatives to traditional treatments, providing AD patients with safer and more effective treatment options.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-02-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Real-World Data to Document the Use of Herbal Medicinal Products in Children - Report of a Workshop in Krakow.

IF 2.1 4区医学

Planta medica Pub Date : 2025-02-11 DOI: 10.1055/a-2523-3856

Nico Symma, Andreas Hensel, Bernd Roether, Barbara Steinhoff, Rudolf Bauer

{"title":"Real-World Data to Document the Use of Herbal Medicinal Products in Children - Report of a Workshop in Krakow.","authors":"Nico Symma, Andreas Hensel, Bernd Roether, Barbara Steinhoff, Rudolf Bauer","doi":"10.1055/a-2523-3856","DOIUrl":"https://doi.org/10.1055/a-2523-3856","url":null,"abstract":"The workshop \"Real-world data to document the use of phytopharmaceuticals in children\" was organized by the GA Foundation Plants for Health in collaboration with multiple international scientific societies on July 14, 2024, during the International Congress on Natural Products Research in Kraków, Poland. The event focused on leveraging real-world data and real-world evidence to support the use of herbal medicinal products (syn. phytopharmaceuticals) in pediatric care. The workshop aimed to discuss the current state and future approaches for utilizing real-world data/real-world evidence in expanding the use of herbal medicinal products in children and adolescents. Therefore, the workshop highlighted the unmet needs and challenges in documenting the effectiveness and safety of herbal medicinal products in children and emphasized the coordinated exchange and collaboration among academia, industry, and regulatory authorities. After an e-symposium in May 2022 with more than 300 participants and an in-person workshop on this topic in Bonn in June 2023, this workshop in Krakow was the third event of its kind hosted by the Foundation Plants for Health. Participants concluded that interdisciplinary collaboration is highly needed to establish qualified methods of data collection and assessment of real-world data, e.g., establishing requirements to incorporate nonprescription herbal medicinal products into electronic patient records and registries that can be accessed by all stakeholders.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399577","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Combating Inflammation and Oxidative Stress: Exploring the Cellular Effects of Lonicera caerulea var. kamtschatica Extract. 抗炎症和氧化应激：探索金银花提取物的细胞作用。

IF 2.1 4区医学

Planta medica Pub Date : 2025-02-11 DOI: 10.1055/a-2520-0013

Katarzyna Zima, Laura Banaszkiewicz, Mateusz Kacper Woźniak, Barbara Khaidakov, Krzysztof Lemke, Paulina Kowalczyk

{"title":"Combating Inflammation and Oxidative Stress: Exploring the Cellular Effects of Lonicera caerulea var. kamtschatica Extract.","authors":"Katarzyna Zima, Laura Banaszkiewicz, Mateusz Kacper Woźniak, Barbara Khaidakov, Krzysztof Lemke, Paulina Kowalczyk","doi":"10.1055/a-2520-0013","DOIUrl":"10.1055/a-2520-0013","url":null,"abstract":"Lonicera caerulea var. kamtschatica, known as blue honeysuckle or haskap berry, is rich in bioactive compounds such as polyphenols, flavonoids, and anthocyanins, which are linked to various health benefits, including anti-inflammatory and antioxidant properties. The research specifically investigates the effects of an L. caerulea var. kamtschatica extract that has been standardized to contain a minimum of 15% anthocyanins on inflammation and oxidative stress at the cellular level. In vitro studies using A549 human lung epithelial cells and peripheral blood mononuclear cells demonstrated the extract's anti-inflammatory and antioxidant properties. L. caerulea var. kamtschatica extract significantly inhibited the nuclear translocation of NF-κB p65 and reduced the production of IL-8 in A549 cells. It also downregulated the expression of proinflammatory genes (RELA and PTGS2) while upregulating antioxidant genes (CAT, HMOX1, and SOD2). In peripheral blood mononuclear cells, L. caerulea var. kamtschatica extract decreased the phosphorylation of NF-κB p65 and reduced the levels of proinflammatory cytokines IL-1β and IL-6 following lipopolysaccharide stimulation. Additionally, the extract inhibited reactive oxygen species formation and nitric oxide production, demonstrating its potential to modulate oxidative stress. Furthermore, in vitro assays indicated that L. caerulea var. kamtschatica extract could hinder the binding of SARS-CoV-2 spike protein to the hACE2 receptor, suggesting antiviral potential.These findings suggest that L. caerulea var. kamtschatica extract exerts significant anti-inflammatory and antioxidant effects, indicating its potential as a functional food ingredient or dietary supplement to combat inflammation and oxidative stress.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143009344","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pseudopeptides of Marine Vibrio spp. from Taiwan and their Combined-Treatment Effects with Commercial Antibiotics.

IF 2.1 4区医学

Planta medica Pub Date : 2025-02-11 DOI: 10.1055/a-2536-8292

Mao-Xuan Hong, Bo-Wei Wang, Li-Hua Lo, Gamaralalage Eranga Dilshan Jayalath, Wei-Tsen Lin, Yu-Liang Yang, Sung-Pin Tseng, Yen-Hsu Chen, Wan-Chi Tsai, Wei-Chieh Cheng, Chih-Chuang Liaw

{"title":"Pseudopeptides of Marine Vibrio spp. from Taiwan and their Combined-Treatment Effects with Commercial Antibiotics.","authors":"Mao-Xuan Hong, Bo-Wei Wang, Li-Hua Lo, Gamaralalage Eranga Dilshan Jayalath, Wei-Tsen Lin, Yu-Liang Yang, Sung-Pin Tseng, Yen-Hsu Chen, Wan-Chi Tsai, Wei-Chieh Cheng, Chih-Chuang Liaw","doi":"10.1055/a-2536-8292","DOIUrl":"https://doi.org/10.1055/a-2536-8292","url":null,"abstract":"Vibrio strains, identified by 16S rDNA, were isolated from the marine environment surrounding Taiwan, revealing diverse bioactive effects, such as iron-chelating and antimicrobial activities. Notably, the hierarchical clustering dendrogram of mass spectrum profiles (MSP) of the Vibrio strains using MALDI-TOF, in contrast to the phylogenetic tree based on 16S rDNA sequencing analysis, exhibited a strong correlation with their observed bioactivities. Within this set, GNPS molecular network analysis by LC-HRMS/MS highlighted that three strains, Vibrio tubiashii DJW05-1, V. japonicas DJW05-8, and V. fortis DJW21-4 shared similar bioactive pseudopeptides in the same cluster. Subsequent chromatographical isolation and purification yield an unprecedented unsaturated diketopiperazine, (Z)-3-(2-methylpropylidene)-2,3-dihydropyrrolo[1,2-a]pyrazine-1,4-dione (1), along with a series of diketopiperazines, and a potential new annotated pseudopeptide 2, as well as three pseudopeptides, including andrimid (10), moiramide B (11), and moiramide C (12), and several alkaloids from V. tubiashii DJW05-1. Further investigation into the combined applications of the major antimicrobial compound and commercial antibiotics revealed that andrimid (10) displayed significant inhibitory effects against Gram-positive Staphylococcus aureus, and Gram-negative Escherichia coli, Salmonella typhimurium, and Acinetobacter baumannii, except for Pseudomonas aeruginosa. Nevertheless, the potential for synergistic and additive effects of andrimid (10) with certain antibiotics remains, presenting valuable prospects for medicinal applications.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Galactomannan and vicilin from fenugreek seeds (Trigonella foenum-graecum) impair pathogen-host interaction of Campylobacter jejuni with intestinal cells via JlpA.

IF 2.1 4区医学

Planta medica Pub Date : 2025-02-10 DOI: 10.1055/a-2536-8392

Leon Kemper, Fabian Herrmann, Simone König, Franco F Falcone, Andreas Hensel

{"title":"Galactomannan and vicilin from fenugreek seeds (Trigonella foenum-graecum) impair pathogen-host interaction of Campylobacter jejuni with intestinal cells via JlpA.","authors":"Leon Kemper, Fabian Herrmann, Simone König, Franco F Falcone, Andreas Hensel","doi":"10.1055/a-2536-8392","DOIUrl":"https://doi.org/10.1055/a-2536-8392","url":null,"abstract":"Campylobacter jejuni is the leading cause of severe enteritis worldwide. Identification of natural products against C. jejuni, inhibiting early-stage host-pathogen interactions is a promising strategy, particularly by blocking bacterial adhesion to and invasion into the host cells. This should help to reduce bacterial load in the vector animals. From the seeds of Trigonella foenum-graecum an aqueous extract (FHM) of high-molecular compounds (polysaccharides, proteins) was obtained. The polysaccharide was characterized as galactomannan (1,4-mannose backbone, substituted at O-6 with single galactose residues and galactose oligosaccharide chains). The protein part consisted of 50 kDa vicilin as main compound. FHM did not influence proliferation of C. jejuni and viability of Caco-2 cells (1-1000 μg/mL). FHM reduced bacterial adhesion to Caco-2 significantly (500-1000 μg/mL), which was due to interaction with the bacterial adhesin JlpA, preventing the interaction of this outer membrane protein to its ligand HSP90α (IC50 23.4 µg/mL). Bacterial invasion was reduced significantly. Both, polysaccharides as well as vicilin contribute to the observed antiadhesive effect. As vicilin-like proteins are widely found in plants from Fabaceae family a vicilin-enriched protein preparation from Pisum sativum was investigated for antiadhesive activity. These findings suggest that fenugreek seeds or vicilin-rich plant extracts could be used to develop novel strategies to control C. jejuni infections in food-producing animals, ultimately helping to decrease the prevalence of campylobacteriosis in humans.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143391503","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The Characteristics and Functions of Orally Absorbed Herbal Decoction-borne Plant MicroRNAs.

IF 2.1 4区医学

Planta medica Pub Date : 2025-01-28 DOI: 10.1055/a-2527-2127

Yating Zhu, Yao Jia, Yicheng Yu, Ziqi Lin, Jinyue Lei, Diyao Wu, Tielong Xu, Longxue Li, Bin Zheng

{"title":"The Characteristics and Functions of Orally Absorbed Herbal Decoction-borne Plant MicroRNAs.","authors":"Yating Zhu, Yao Jia, Yicheng Yu, Ziqi Lin, Jinyue Lei, Diyao Wu, Tielong Xu, Longxue Li, Bin Zheng","doi":"10.1055/a-2527-2127","DOIUrl":"https://doi.org/10.1055/a-2527-2127","url":null,"abstract":"Herbal decoctions always contain numerous plant microRNAs (miRNAs), and some of these can be absorbed orally to exert cross-kingdom gene regulation. However, little is known about which specific types of herbal decoction-borne plant miRNAs are more likely to be absorbed. Thus, two antiviral herbal decoctions, Qingfei Paidu (QFPD) and Qingre Huashi Kangdu (QRHS), were administered to human volunteers and rats, respectively, to investigate the characteristics of orally absorbed decoction-borne plant miRNAs. MIR-6240-3p was identified as an absorbed plant miRNA in humans and is most highly expressed in QFPD decoction. Therefore, the kinetics of MIR-6240-3p were monitored in humans following the administration of the QFPD decoction, and its antiviral effect on human coronavirus type 229E (HCoV-229E) was examined in vitro. 586,176 small RNAs (sRNAs) were identified in QFPD decoction, of which 100,276 were orally absorbed by humans. In the QRHS decoction, 124,026 sRNAs were detected, with 7484 being orally absorbed by rats. Logistical repression analysis revealed that absorbable plant sRNAs in both humans and rats presented higher expression levels, greater minimum free energy, and increased AU/UA frequencies compared to non-absorbable plant sRNAs. The amount of MIR-6240-3p in humans increased between 1- and 3-hours after the administration of the QFPD decoction. In addition, MIR-6240-3p significantly reduced the RNA copy number and TCID50 of HCoV-229E in vitro. These results suggest that herbal decoction-borne plant sRNAs with higher expression level, greater minimum free energy or an increased AU/UA frequency are more likely to be orally absorbed and could potentially mediate cross-kingdom gene regulation.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143060102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Roseoglobuloside A, a Novel Nonanolide, and Identification of Specialized Metabolites as hPTP1B1 - 400 Inhibitors from Mangrove-Dwelling Aspergillus spp.

IF 2.1 4区医学

Planta medica Pub Date : 2025-01-27 DOI: 10.1055/a-2515-9491

Carlos A Fajardo-Hernández, Ángeles G Zavala-Sierra, Verenice I Merlin-Lucas, Jesús I Morales-Jiménez, José Rivera-Chávez

{"title":"Roseoglobuloside A, a Novel Nonanolide, and Identification of Specialized Metabolites as hPTP1B1 - 400 Inhibitors from Mangrove-Dwelling Aspergillus spp.","authors":"Carlos A Fajardo-Hernández, Ángeles G Zavala-Sierra, Verenice I Merlin-Lucas, Jesús I Morales-Jiménez, José Rivera-Chávez","doi":"10.1055/a-2515-9491","DOIUrl":"https://doi.org/10.1055/a-2515-9491","url":null,"abstract":"An approach combining enzymatic inhibition and untargeted metabolomics through molecular networking was employed to search for human recombinant full-length protein tyrosine phosphatase 1B (hPTP1 B1 - 400) inhibitors from a collection of 66 mangrove-associated fungal taxa. This strategy prioritized two Aspergillus strains (IQ-1612, section Circumdati, and IQ-1620, section Nigri) for further studies. Chemical investigation of strain IQ-1612 resulted in the isolation of a new nonanolide derivative, roseoglobuloside A (1: ), along with two known metabolites (2: and 3: ), whereas strain IQ-1620 led to the isolation of four known naphtho-γ-pyrones and one known diketopiperazine (4: -8: ). Of all isolates, compounds 2, 3: , and 7: showed a marked inhibitory effect on hPTP1B1 - 400 with an IC50 value < 20 µM, while 6: showed moderate inhibition with IC50 of 65 µM. Compounds 1: and 8: were inactive at a concentration of 100 µM, whereas 4: and 5: demonstrated significant inhibition at 20 µM. The structure of 1: was established by comprehensive spectroscopic analysis, and its relative and absolute configuration was assigned based on NOE correlations and by comparison of calculated and experimental ECD curves. Molecular docking indicated that these molecules primarily bind to two different allosteric sites, thereby inducing conformational changes that impact enzymatic activity.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143053194","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Eleutherococcus senticosus Alleviates Aristolochic-Acid-Induced Acute Kidney Damage by Inhibiting the NLRP3/IL-1β Signaling Pathway in Mice.

IF 2.1 4区医学

Planta medica Pub Date : 2025-01-24 DOI: 10.1055/a-2517-9234

Jian-Hui Zhang, Mei-Zhu Gao, Qian Chen, Ting Chen, Dan-Dan Ruan, Min Wu, Fang-Meng Huang, Jie-Wei Luo, Yao-Bin Zhu, Li Chen

{"title":"Eleutherococcus senticosus Alleviates Aristolochic-Acid-Induced Acute Kidney Damage by Inhibiting the NLRP3/IL-1β Signaling Pathway in Mice.","authors":"Jian-Hui Zhang, Mei-Zhu Gao, Qian Chen, Ting Chen, Dan-Dan Ruan, Min Wu, Fang-Meng Huang, Jie-Wei Luo, Yao-Bin Zhu, Li Chen","doi":"10.1055/a-2517-9234","DOIUrl":"https://doi.org/10.1055/a-2517-9234","url":null,"abstract":"Eleutherococcus senticosus (ES) exerts various pharmacological effects, including renoprotection in a rat model of renal ischemia-reperfusion injury. However, the mechanisms of these effects remain unclear. Therefore, we investigated the effects and mechanisms of ES on aristolochic acid (AA)-induced acute kidney injury in mice. The experimental mice were divided into the control group, the model group (AA-induced acute kidney injury model), the model + ES group (Eleutherococcus senticosus boiled-free granules treated by gavage for two weeks), the model + fasudil group (fasudil administered intraperitoneally for three days), and the model + ES + fasudil group. After AA intervention in normal mice, the expression of ASC and NLRP3 and the levels of IL-1β, IL-18, and TNF-α were significantly elevated in mouse renal tissues (P < 0.05). However, AA-induced renal dysfunction was ameliorated by both ES and fasudil, which was confirmed by the decrease in serum creatinine and blood urea nitrogen levels, as well as by renal histopathological abnormalities such as renal tubule dilation and tubular formation. In addition, the inflammatory response of AA-induced renal inflammation was inhibited by both ES and fasudil, and the expression of ASC and NLRP3 and the levels of IL-1β, IL-18, and TNF-α were significantly higher in mouse renal tissues after the treatment of either ES or fasudil (P < 0.05). ES may be a potential treatment agent for aristolochic-acid-triggered nephropathy, with inhibition of the NLRP3/IL-1β as one plausible underlying mechanism.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143040977","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Characterization of lipophilicity and blood partitioning of pyrrolizidine alkaloids and their N-oxides in vitro and in silico for toxicokinetic modeling.

IF 2.1 4区医学

Planta medica Pub Date : 2025-01-23 DOI: 10.1055/a-2523-3987

Anja Lehmann, Manuel Haas, Julian Taenzer, Gerd Hamscher, Charlotte Kloft, Anja These, Christoph Hethey

{"title":"Characterization of lipophilicity and blood partitioning of pyrrolizidine alkaloids and their N-oxides in vitro and in silico for toxicokinetic modeling.","authors":"Anja Lehmann, Manuel Haas, Julian Taenzer, Gerd Hamscher, Charlotte Kloft, Anja These, Christoph Hethey","doi":"10.1055/a-2523-3987","DOIUrl":"https://doi.org/10.1055/a-2523-3987","url":null,"abstract":"Lipophilicity and blood partitioning are important determinants for predicting toxicokinetics using physiologically-based toxicokinetic (PBTK) modeling. In this study, the logarithm of the n-octanol:water partition coefficient (logP) and the blood-to-plasma concentration ratio (Rb ) were for the first time experimentally determined for the pyrrolizidine alkaloids (PAs) intermedine, lasiocarpine, monocrotaline, retrorsine and their N-oxides (PANOs). Validated in vitro assays for logP (miniaturized shake-flask method) and Rb (LC-MS/MS-based depletion assay) determination were compared to an ensemble of in silico models. Experimentally determined logP indicate a higher affinity of PAs and PANOs to the aqueous compared to the organic phase. Depending on the method, in silico determined logP overpredicted the experimental values by ≥ 1 log unit for 3 out of 4 PAs (SPARC), 4 out of 6 PAs and PANOs (CLOGP), 5 out of 8 PAs and PANOs (KowWIN) and 3 out of 8 PAs and PANOs (S+logP). Rb obtained in vitro suggested a low binding affinity of PAs and PANOs towards red blood cells. For all 8 PAs and PANOs, in silico predicted Rb deviated from experimental values by less than 50%. In conclusion, for PBTK modeling of PAs and PANOs, experimental logP should be preferred, while Rb predicted by the acid/base classification model is a suitable surrogate for experimental data.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143029261","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Phytoestrogens and Sirtuin Activation for Renal Protection: A Review of Potential Therapeutic Strategies. 植物雌激素和Sirtuin激活对肾脏保护：潜在治疗策略的综述。

IF 2.1 4区医学

Planta medica Pub Date : 2025-01-22 DOI: 10.1055/a-2464-4354

Debojyoti Mandal, Nahid Akhtar, Sana Shafi, Jeena Gupta

{"title":"Phytoestrogens and Sirtuin Activation for Renal Protection: A Review of Potential Therapeutic Strategies.","authors":"Debojyoti Mandal, Nahid Akhtar, Sana Shafi, Jeena Gupta","doi":"10.1055/a-2464-4354","DOIUrl":"10.1055/a-2464-4354","url":null,"abstract":"Significant health and socio-economic challenges are posed by renal diseases, leading to millions of deaths annually. The costs associated with treating and caring for patients with renal diseases are considerable. Current therapies rely on synthetic drugs that often come with side effects. However, phytoestrogens, natural compounds, are emerging as promising renal protective agents. They offer a relatively safe, effective, and cost-efficient alternative to existing therapies. Phytoestrogens, being structurally similar to 17-β-estradiol, bind to estrogen receptors and produce both beneficial and, in some cases, harmful health effects. The activation of sirtuins has shown promise in mitigating fibrosis and inflammation in renal tissues. Specifically, SIRT1, which is a crucial regulator of metabolic activities, plays a role in protecting against nephrotoxicity, reducing albuminuria, safeguarding podocytes, and lowering reactive oxygen species in diabetic glomerular injury. Numerous studies have highlighted the ability of phytoestrogens to activate sirtuins, strengthen antioxidant defense, and promote mitochondrial biogenesis, playing a vital role in renal protection during kidney injury. These findings support further investigation into the potential role of phytoestrogens in renal protection. This manuscript reviews the potential of phytoestrogens such as resveratrol, genistein, coumestrol, daidzein, and formononetin in regulating sirtuin activity, particularly SIRT1, and thereby providing renal protection. Understanding these mechanisms is crucial for designing effective treatment strategies using naturally occurring phytochemicals against renal diseases.","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.1,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142771386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0