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19 pages, 1604 KiB

Open AccessArticle

Eucommiae cortex Comprehensive Phytochemical Analysis Connected with Its In Vitro Anti-Inflammatory Activity in Human Immune Cells

by Małgorzata Kołtun-Jasion, Marta Katarzyna Dudek and Anna Karolina Kiss

Molecules 2025, 30(6), 1364; https://doi.org/10.3390/molecules30061364 - 18 Mar 2025

Viewed by 409

Abstract

Eucommia ulmoides Oliv., commonly known as “plant gold”, is a species of the Eucommiaceae family, native to East Asia and widely utilized in medicine, food, and the chemical industry. In Traditional Chinese Medicine, the bark of E. ulmoides plays a special role, used [...] Read more.

Eucommia ulmoides Oliv., commonly known as “plant gold”, is a species of the Eucommiaceae family, native to East Asia and widely utilized in medicine, food, and the chemical industry. In Traditional Chinese Medicine, the bark of E. ulmoides plays a special role, used to nourish the liver and kidneys and to strengthen tendons and bones. Due to its extensive pharmacological profile, including anti-inflammatory, antioxidant, hypoglycemic, hypotensive, and cardio- and neuroprotective effects, there has been growing interest in elucidating the molecular mechanisms underlying its biological effects. However, many of these mechanisms remain poorly understood to date. This study analyzed the phytochemical composition of E. ulmoides bark infusions and tinctures and their dominant compounds using the HPLC-DAD-MS/MS method, and evaluated their anti-inflammatory effects in human immune cell models. The analysis identified lignans, iridoids, and caffeic acid derivatives as the dominant constituents of the tested samples. The extracts significantly inhibited the secretion of pro-inflammatory cytokines (TNF-α, IL-6, IL-8, MCP-1) in neutrophils, PBMC-derived monocytes/macrophages, and THP-1 cells. The results presented herein offer significant insights into the detailed phytochemical composition of E. ulmoides bark, and contribute to a deeper understanding of its anti-inflammatory mechanisms in human immune cells. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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21 pages, 4151 KiB

Open AccessArticle

Antifungal Properties of Bioactive Compounds Isolated from Fucus vesiculosus Supercritical Carbon Dioxide Extract

by Katarzyna Tyśkiewicz, Felix Rüttler, Renata Tyśkiewicz, Artur Nowak, Marcin Gruba, Anita Wziątek, Agnieszka Dębczak, Michał Sandomierski and Walter Vetter

Molecules 2024, 29(24), 5957; https://doi.org/10.3390/molecules29245957 - 17 Dec 2024

Viewed by 884

Abstract

The exploration of natural antifungal substances from algal origins is significant due to the increasing resistance of pathogens to conventional antifungal agents and the growing consumer demand for natural products. This manuscript represents the inaugural investigation into the antifungal attributes of bioactive compounds [...] Read more.

The exploration of natural antifungal substances from algal origins is significant due to the increasing resistance of pathogens to conventional antifungal agents and the growing consumer demand for natural products. This manuscript represents the inaugural investigation into the antifungal attributes of bioactive compounds extracted from Fucus vesiculosus via supercritical carbon dioxide (scCO₂) extraction utilizing contemporary countercurrent chromatography (CCC). In aligning with the prospective utilization of this extract within the agricultural sector, this study also serves as the preliminary report demonstrating the capability of Fucus vesiculosus scCO₂ extract to enhance the activity of plant resistance enzymes. The fractions obtained through CCC were subjected to evaluation for their efficacy in inhibiting the macrospores of Fusarium culmorum. The CCC methodology facilitated the successful separation of fatty acids (reaching up to 82.0 wt.% in a given fraction) and fucosterol (attaining up to 79.4 wt.% in another fraction). All CCC fractions at the concentration of 1.0% were found to inhibit 100% of Fusarium culmorum growth. Moreover, Fucus vesiculosus scCO₂ extract was able to activate plant resistance enzymes (Catalase, Ascorbic Peroxidase, Guaiacol Peroxidase, Phenylalanine Ammonia-Lyase, and Phenylalanine Ammonia-Lyase Activity). Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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16 pages, 4948 KiB

Open AccessArticle

Ultra-Performance Liquid Chromatography and Mass Spectrometry Characterization, and Antioxidant, Protective, and Anti-Inflammatory Activity, of the Polyphenolic Fraction from Ocimum basilicum

by Magdalena Wójciak, Roman Paduch, Piotr Drozdowski, Magdalena Żuk, Weronika Wójciak, Katarzyna Tyszczuk-Rotko, Marcin Feldo and Ireneusz Sowa

Molecules 2024, 29(21), 5043; https://doi.org/10.3390/molecules29215043 - 25 Oct 2024

Cited by 2 | Viewed by 994

Abstract

Ocimum basilicum is a valuable plant widely consumed worldwide and considered a rich source of polyphenols. This study examined the impact of the polyphenolic fraction isolated from basil (ObF) on human normal colon epithelial cells and human colorectal adenocarcinoma cells, evaluating its anti-inflammatory [...] Read more.

Ocimum basilicum is a valuable plant widely consumed worldwide and considered a rich source of polyphenols. This study examined the impact of the polyphenolic fraction isolated from basil (ObF) on human normal colon epithelial cells and human colorectal adenocarcinoma cells, evaluating its anti-inflammatory and protective activity against oxidative stress. The phytochemical characterization of the fraction was performed using ultra-performance liquid chromatography (UPLC) with a photodiode detector (DAD) and mass spectrometry (MS). UPLC-DAD-MS revealed that ObF predominantly contains caffeic acid derivatives, with rosmarinic acid and chicoric acid being the most abundant. The fraction demonstrated high antioxidant potential, as shown by DPPH assays, along with significant reducing power (FRAP). Furthermore, it prevented the depletion of antioxidant enzymes, including superoxide dismutase and catalase, and decreased malonylodialdehyde (MDA) in induced oxidative stress condition. Additionally, it exhibited a significant protective effect against H₂O₂-induced cytotoxicity in human normal colon epithelial cells. Although it had no impact on the viability of adenocarcinoma cells, it significantly reduced IL-1β levels in the neoplastic microenvironment. Our study demonstrated that basil polyphenols provide significant health benefits due to their antioxidant and protective activities. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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30 pages, 6392 KiB

Open AccessArticle

Evaluating the Root Extract of Reynoutria ciliinervis (Nakai) Moldenke: An Analysis of Active Constituents, Antioxidant Potential, and Investigation of Hepatoprotective Effects in Rats

by Zheng Xing, Yang Han, Hao Pang, Li Li, Guangqing Xia, Junyi Zhu, Jing Han and Hao Zang

Molecules 2024, 29(19), 4701; https://doi.org/10.3390/molecules29194701 - 4 Oct 2024

Cited by 2 | Viewed by 1149

Abstract

Reynoutria ciliinervis (Nakai) Moldenke (R. ciliinervis) root, a traditional Chinese medicine, was found to exhibit remarkable pharmacological properties through a series of comprehensive investigations. Our study commenced with a qualitative phytochemical analysis that identified 12 bioactive compounds within the plant. Subsequently, [...] Read more.

Reynoutria ciliinervis (Nakai) Moldenke (R. ciliinervis) root, a traditional Chinese medicine, was found to exhibit remarkable pharmacological properties through a series of comprehensive investigations. Our study commenced with a qualitative phytochemical analysis that identified 12 bioactive compounds within the plant. Subsequently, utilizing ultraviolet-visible spectrophotometry, the methanol extract emerged as the optimal solvent extract, which was abundant in diverse classes of compounds such as carbohydrates, phenolics, steroids, alkaloids, phenolic acids, and tannins. In vitro antioxidant assays underscored the exceptional free radical scavenging, metal ion chelation, hydrogen peroxide scavenging, singlet oxygen quenching, and β-carotene bleaching capabilities of the methanol extract, significantly outperforming other solvent extracts. Further ultra high-performance liquid chromatography–electrospray ionization–quadrupole time of flight–mass spectrometry analysis revealed the presence of 45 compounds, predominantly anthraquinones and phenolics, in the methanol extract. The extract demonstrated robust stability under various conditions, including high temperatures, varying pH levels, and simulated gastrointestinal digestion as well as efficacy in inhibiting the oxidation in edible oils. Acute toxicity tests in mice confirmed the safety of the methanol extract and provided a valuable dosage reference for future studies. Importantly, high-dose methanol extract exhibited a significant pre-protective effect against D-galactosamine-induced liver injury in rats, as evidenced by reduced alanine aminotransferase, aspartate aminotransferase, γ-glutamyl transpeptidase, malondialdehyde levels, and elevated catalase and albumin levels. These findings suggest a potential role for the methanol extract of R. ciliinervis root in treating oxidative stress-related disorders, highlighting the plant’s immense medicinal potential. Our research offers a thorough evaluation of the bioactive components, antioxidant properties, stability, and liver-protecting effects of the methanol extract, setting the stage for deeper investigation and potential clinical applications. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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30 pages, 5007 KiB

Open AccessArticle

Phytochemical Analysis and Antioxidant Activities of Various Extracts from the Aerial Part of Anemone baicalensis Turcz.: In Vitro and In Vivo Studies

by Shuang Sun, Guangqing Xia, Hao Pang, Junyi Zhu, Li Li and Hao Zang

Molecules 2024, 29(19), 4602; https://doi.org/10.3390/molecules29194602 - 27 Sep 2024

Cited by 3 | Viewed by 1581

Abstract

Anemone baicalensis Turcz., a botanical species with a rich historical background in traditional medicine for detoxification and insecticidal applications, possesses a vast, yet largely unexplored, therapeutic potential. This study primarily focused on conducting a qualitative phytochemical analysis of the plant, determining the active [...] Read more.

Anemone baicalensis Turcz., a botanical species with a rich historical background in traditional medicine for detoxification and insecticidal applications, possesses a vast, yet largely unexplored, therapeutic potential. This study primarily focused on conducting a qualitative phytochemical analysis of the plant, determining the active ingredient content and antioxidant activity of various solvent extracts. The qualitative phytochemical analysis revealed the presence of 12 different types of phytochemicals within the plant. Utilizing ultraviolet-visible spectrophotometry, we identified 11 active ingredients in 4 solvent extracts. Notably, the methanol extract was found to contain high concentrations of total carbohydrate, total monoterpenoid, total phenolic, total tannin, and total triterpenoid. In the antioxidant experiment, the methanol extract demonstrated superior scavenging abilities against 1,1-diphenyl-2-picrylhydrazyl radical, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid) diammonium salt, superoxide anion radical, and hydrogen peroxide, outperforming other extracts in chelation experiments aimed at reducing iron and metal ions. Consequently, the methanol extract was selected for further investigation. Subsequent ultrahigh-performance liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry analysis revealed that the methanol extract contained 39 compounds, primarily phenolic compounds and triterpenoid saponins. Three stability assessments confirmed the extract’s stability under high temperatures, varying pH levels, and simulated gastrointestinal processes. Additionally, oil stability testing demonstrated its antioxidant capacity in extra virgin olive oil and cold-pressed sunflower seed oil media. An oral acute toxicity experiment conducted on mice not only confirmed the absence of acute toxicity in the methanol extract but also provided a dose reference for subsequent gastric protection experiments. Notably, the methanol extract exhibited significant gastroprotective effects against ethanol-induced gastric lesions in rats, as evidenced by histopathological and biochemical analyses. Specifically, the extract reduced levels of malondialdehyde, alanine aminotransferase, and aspartate aminotransferase while increasing glutathione, nitric oxide, and catalase, indicating its gastroprotective mechanism. These findings suggest that the methanol extract from the aerial part of Anemone baicalensis could be a promising therapeutic agent for conditions associated with oxidative imbalances. They underscore the plant’s potential therapeutic benefits and offer valuable insights into its antioxidant properties, thereby broadening our understanding of its medicinal potential. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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14 pages, 3144 KiB

Open AccessArticle

Towards the Use of Lichens as a Source of Bioactive Substances for Topical Applications

by Izabela Baczewska, Barbara Hawrylak-Nowak, Martyna Zagórska-Dziok, Aleksandra Ziemlewska, Zofia Nizioł-Łukaszewska, Grzegorz Borowski and Sławomir Dresler

Molecules 2024, 29(18), 4352; https://doi.org/10.3390/molecules29184352 - 13 Sep 2024

Cited by 3 | Viewed by 1864

Abstract

The increasing incidence of dermatological diseases prompts the search for new natural methods of treatments, and lichens, with their special symbiotic structure, are a little-known and promising source of biologically active substances. Seven lichen species, Cladonia unicialis (L.) Weber ex F.H. Wigg. (Cladoniaceae) [...] Read more.

The increasing incidence of dermatological diseases prompts the search for new natural methods of treatments, and lichens, with their special symbiotic structure, are a little-known and promising source of biologically active substances. Seven lichen species, Cladonia unicialis (L.) Weber ex F.H. Wigg. (Cladoniaceae), Evernia prunastri (L.) Ach. (Parmeliaceae), Hypogymnia physodes (L.) Nyl. (Parmaliaceae), Parmelia sulcata (Taylor) (Parmeliaceae), Physcia adscendens (Fr.) H. Olivier (Physciaceae), Pseudoevernia furfuracea (L.) Zopf (Parmeliaceae), and Xanthoria parietina (L.) Th. Fr. (Teloschistaceae), were used in our experiment. We identified different metabolites in the acetone extracts of all the lichen species. Based on the high-performance liquid chromatography analysis, the content of lichen substances in the extracts was evaluated. The impact of the individual lichen-specific reference substances, compared to the lichen extracts, on the viability of keratinocytes (HaCaT cell line) and fibroblasts (BJ cell line) and on the activity of selected skin-related enzymes was investigated. Our results revealed that only emodin anthrone at a concentration of 200 mg/L was cytotoxic to keratinocytes and fibroblasts in both cell viability assays. In turn, the C. uncialis extract was only cytotoxic to keratinocytes when used at the same concentration. The other tested treatments showed a positive effect on cell viability and no cytotoxicity or indeterminate cytotoxicity (shown in only one of the tests). Elastase and collagenase activities were inhibited by most of the lichen extracts. In turn, the individual lichen compounds (with the exception of evernic acid) generally had an undesirable stimulatory effect on hyaluronidase and collagenase activity. In addition, almost all the tested compounds and extracts showed anti-inflammatory activity. This suggests that some lichen compounds hold promise as potential ingredients in dermatological and skincare products, but their safety and efficacy require further study. The high cytotoxicity of emodin anthrone highlights its potential use in the treatment of hyperproliferative skin diseases such as psoriasis. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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20 pages, 11881 KiB

Open AccessArticle

Investigation of the Structural Properties and Antioxidant Potency of Pectic Polysaccharides Derived from Rohdea japonica (Thunb.) Roth

by Su Yan, Zhiying Lin, Kuo Cui, Hao Zang, Yifa Zhou, Lihui Zhang and Duo Liu

Molecules 2024, 29(17), 4135; https://doi.org/10.3390/molecules29174135 - 31 Aug 2024

Cited by 2 | Viewed by 1005

Abstract

This study investigated the structural composition and antioxidant properties of pectic polysaccharides extracted from Rohdea japonica (Thunb.) Roth. Pectins, which belong to a complex category of acidic polysaccharides, possess a wide range of biological effects stemming from their distinctive structural domains. The polysaccharides [...] Read more.

This study investigated the structural composition and antioxidant properties of pectic polysaccharides extracted from Rohdea japonica (Thunb.) Roth. Pectins, which belong to a complex category of acidic polysaccharides, possess a wide range of biological effects stemming from their distinctive structural domains. The polysaccharides were extracted using water, and were subsequently purified through ion exchange and gel permeation chromatography. In order to elucidate their structural features, Fourier Transform Infrared Spectroscopy and Nuclear Magnetic Resonance techniques were applied. Two specific polysaccharides, WRJP-A2a and WRJP-A3b, with molecular weights of 42.7 kDa and 64.1 kDa, respectively, were identified to contain varying proportions of homogalacturonan, rhamnogalacturonan I, and rhamnogalacturonan II domains. Regarding antioxidant capacity, WRJP-A3b exhibited superior scavenging capabilities against DPPH, ABTS, and hydroxyl radicals, potentially attributed to its higher galacturonic acid content and abundance of homogalacturonan domains. These results enhance our comprehension of the structure–activity interplay of pectic polysaccharides sourced from Rohdea japonica (Thunb.) Roth and their potential utility in the healthcare and functional food sectors. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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15 pages, 1815 KiB

Open AccessArticle

Antioxidant Properties of Green Plants with Different Vitamin K Contents

by Iryna Bryshten, Łukasz Paprotny, Małgorzata Olszowy-Tomczyk and Dorota Wianowska

Molecules 2024, 29(15), 3655; https://doi.org/10.3390/molecules29153655 - 1 Aug 2024

Cited by 4 | Viewed by 1801

Abstract

Vitamin K, as a natural protector of our blood, bones, kidneys, and brain, is essential for human health. It is also considered an effective anti-aging agent with comprehensive biological effects, including antifungal, antibacterial, anti-inflammatory, analgesic, and even antioxidant properties. Of these, the least [...] Read more.

Vitamin K, as a natural protector of our blood, bones, kidneys, and brain, is essential for human health. It is also considered an effective anti-aging agent with comprehensive biological effects, including antifungal, antibacterial, anti-inflammatory, analgesic, and even antioxidant properties. Of these, the least is known about the antioxidant properties of natural vitamin K. To fill this gap, this study compared the antioxidant properties of extracts obtained from commonly consumed green plants with different vitamin K contents with the activity of vitamin K standard solutions at concentrations corresponding to the vitamin K contents in the extracts. Various measurement methods were used in the research (i.e., DPPH, FRAP, CUPRAC, and the β-carotene bleaching test). Among the tested methods, the β-carotene bleaching test is the most sensitive in the assessment of this unusual compound. In light of the data presented, the antioxidant response of vitamin K alone is dose-dependent. However, in extracts, the activity of this compound is modulated by other constituents present in them. As a result, the activity does not always correlate with vitamin K content. The presented data supplement the knowledge about the antioxidant properties with the contribution resulting from the presence of vitamin K in green plant extracts. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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17 pages, 10731 KiB

Open AccessArticle

Anti-Tumor Activity and Mechanism of Silibinin Based on Network Pharmacology and Experimental Verification

by Peihai Li, Dexu Wang, Xueliang Yang, Changyu Liu, Xiaobin Li, Xuanming Zhang, Kechun Liu, Yun Zhang, Mengqi Zhang, Changyun Wang and Rongchun Wang

Molecules 2024, 29(8), 1901; https://doi.org/10.3390/molecules29081901 - 22 Apr 2024

Cited by 6 | Viewed by 2524

Abstract

Silibinin is a flavonoid compound extracted from the seeds of Silybum marianum (L.) Gaertn. It has the functions of liver protection, blood-lipid reduction and anti-tumor effects. However, the potential molecular mechanism of silibinin against tumors is still unknown. This study aimed to assess [...] Read more.

Silibinin is a flavonoid compound extracted from the seeds of Silybum marianum (L.) Gaertn. It has the functions of liver protection, blood-lipid reduction and anti-tumor effects. However, the potential molecular mechanism of silibinin against tumors is still unknown. This study aimed to assess the anti-tumor effects of silibinin in adenoid cystic carcinoma (ACC2) cells and Balb/c nude mice, and explore its potential mechanism based on network pharmacology prediction and experimental verification. A total of 347 targets interacting with silibinin were collected, and 75 targets related to the tumor growth process for silibinin were filtrated. Based on the PPI analysis, CASP3, SRC, ESR1, JAK2, PRKACA, HSPA8 and CAT showed stronger interactions with other factors and may be the key targets of silibinin for treating tumors. The predicted target proteins according to network pharmacology were verified using Western blot analysis in ACC2 cells and Balb/c nude mice. In the pharmacological experiment, silibinin was revealed to significantly inhibit viability, proliferation, migration and induce the apoptosis of ACC2 cells in vitro, as well as inhibit the growth and development of tumor tissue in vivo. Western blot analysis showed that silibinin affected the expression of proteins associated with cell proliferation, migration and apoptosis, such as MMP3, JNK, PPARα and JAK. The possible molecular mechanism involved in cancer pathways, PI3K-Akt signaling pathway and viral carcinogenesis pathway via the inhibition of CASP3, MMP3, SRC, MAPK10 and CDK6 and the activation of PPARα and JAK. Overall, our results provided insight into the pharmacological mechanisms of silibinin in the treatment of tumors. These results offer a support for the anti-tumor uses of silibinin. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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18 pages, 7796 KiB

Open AccessArticle

Involvement of Bile Acid Metabolism and Gut Microbiota in the Amelioration of Experimental Metabolism-Associated Fatty Liver Disease by Nobiletin

by Hongling Xu, Mingming Yuan, Kailin Niu, Wei Yang, Maoyuan Jiang, Lei Zhang and Jing Zhou

Molecules 2024, 29(5), 976; https://doi.org/10.3390/molecules29050976 - 23 Feb 2024

Cited by 3 | Viewed by 3027

Abstract

Metabolism-associated fatty liver disease (MAFLD), a growing health problem worldwide, is one of the major risks for the development of cirrhosis and liver cancer. Oral administration of nobiletin (NOB), a natural citrus flavonoid, modulates the gut microbes and their metabolites in mice. In [...] Read more.

Metabolism-associated fatty liver disease (MAFLD), a growing health problem worldwide, is one of the major risks for the development of cirrhosis and liver cancer. Oral administration of nobiletin (NOB), a natural citrus flavonoid, modulates the gut microbes and their metabolites in mice. In the present study, we established a mouse model of MAFLD by subjecting mice to a high-fat diet (HFD) for 12 weeks. Throughout this timeframe, NOB was administered to investigate its potential benefits on gut microbial balance and bile acid (BA) metabolism using various techniques, including 16S rRNA sequencing, targeted metabolomics of BA, and biological assays. NOB effectively slowed the progression of MAFLD by reducing serum lipid levels, blood glucose levels, LPS levels, and hepatic IL-1β and TNF-α levels. Furthermore, NOB reinstated diversity within the gut microbial community, increasing the population of bacteria that produce bile salt hydrolase (BSH) to enhance BA excretion. By exploring further, we found NOB downregulated hepatic expression of the farnesoid X receptor (FXR) and its associated small heterodimer partner (SHP), and it increased the expression of downstream enzymes, including cholesterol 7α-hydroxylase (CYP7A1) and cytochrome P450 27A1 (CYP27A1). This acceleration in cholesterol conversion within the liver contributes to mitigating MAFLD. The present findings underscore the significant role of NOB in regulating gut microbial balance and BA metabolism, revealing that long-term intake of NOB plays beneficial roles in the prevention or intervention of MAFLD. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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14 pages, 8518 KiB

Open AccessArticle

Hypolipidemic and Antithrombotic Effect of 6′-O-Caffeoylarbutin from Vaccinium dunalianum Based on Zebrafish Model, Network Pharmacology, and Molecular Docking

by Boxiao Wu, Churan Li, Huan Kan, Yingjun Zhang, Xiaoping Rao, Yun Liu and Ping Zhao

Molecules 2024, 29(4), 780; https://doi.org/10.3390/molecules29040780 - 8 Feb 2024

Cited by 4 | Viewed by 2091

Abstract

Vaccinium dunalianum leaf buds make one of the most commonly used herbal teas of the Yi people in China, which is used to treat articular rheumatism, relax tendons, and stimulates blood circulation in the body. In addition, 6′-O-caffeoylarbutin (CA) is a [...] Read more.

Vaccinium dunalianum leaf buds make one of the most commonly used herbal teas of the Yi people in China, which is used to treat articular rheumatism, relax tendons, and stimulates blood circulation in the body. In addition, 6′-O-caffeoylarbutin (CA) is a standardized extract of V. dunalianum, which has been found in dried leaf buds, reaching levels of up to 31.76%. Because of the uncommon phenomenon, it is suggested that CA may have a potential therapeutic role in hyperlipidemia and thrombosis. This study was designed to study the efficacy of CA on treating hyperlipidemia and thrombosis and the possible mechanisms behind these effects. Hyperlipidemia and thrombosis zebrafish models were treated with CA to observe variations of the integrated optical density within the vessels and the intensity of erythrocyte staining within the hearts. The possible mechanisms were explored using network pharmacology and molecular docking. The results demonstrate that CA exhibits an excellent hypolipidemic effect on zebrafish at concentrations ranging from 3.0 to 30.0 μg/mL and shows thrombosis inhibitory activity in zebrafish at a concentration of 30.0 μg/mL, with an inhibition rate of 44%. Moreover, network pharmacological research shows that MMP9, RELA, MMP2, PRKCA, HSP90AA1, and APP are major targets of CA for therapy of hyperlipidemia and thrombosis, and may relate to pathways in cancer, chemical carcinogenesis-receptor activation, estrogen signaling pathway, and the AGE–RAGE signaling pathway in diabetic complications. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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20 pages, 4512 KiB

Open AccessArticle

Uncovering the Anti-Angiogenic Mechanisms of Centella asiatica via Network Pharmacology and Experimental Validation

by Bingtian Zhao, Yuanyuan Li, Binya Wang, Jing Liu, Yang Yang, Qianghua Quan, Quan An, Rong Liang, Chunhuan Liu and Cheng Yang

Molecules 2024, 29(2), 362; https://doi.org/10.3390/molecules29020362 - 11 Jan 2024

Cited by 5 | Viewed by 3610

Abstract

Background: Centella asiatica (CA) has been used to address cancer for centuries in traditional Chinese medicine (TCM). Previous studies demonstrated its anti-angiogenesis efficacy, but the underlying mechanism of its action remains to be further clarified. This study aims to investigate the underlying mechanisms [...] Read more.

Background: Centella asiatica (CA) has been used to address cancer for centuries in traditional Chinese medicine (TCM). Previous studies demonstrated its anti-angiogenesis efficacy, but the underlying mechanism of its action remains to be further clarified. This study aims to investigate the underlying mechanisms of CA and its triterpenes in anti-angiogenesis for cancer therapeutics through network pharmacology and experimental validation. Methods: Cytoscape was used to construct a network of compound–disease targets and protein–protein interactions (PPIs) from which core targets were identified. GO and KEGG analyses were performed using Metascape, and the AutoDock-Vina program was used to realize molecular docking for further verification. Then, VEGF165 was employed to establish an induced angiogenesis model. The anti-angiogenic effects of CA were evaluated through assays measuring cell proliferation, migration, and tubular structure formation. Results: Twenty-five active ingredients in CA had potential targets for anti-angiogenesis including madecassoside, asiaticoside, madecassic acid, asiatic acid, and asiaticoside B. In total, 138 potential targets for CA were identified, with 19 core targets, including STAT3, SRC, MAPK1, and AKT1. A KEGG analysis showed that CA is implicated in cancer-related pathways, specifically PD-1 and AGE-RAGE. Molecular docking verified that the active components of CA have good binding energy with the first four important targets of angiogenesis. In experimental validation, the extracts and triterpenes of CA improved VEGF165-induced angiogenesis by reducing the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs). Conclusions: Our results initially demonstrate the effective components and great anti-angiogenic activity of CA. Evidence of the satisfactory anti-angiogenic action of the extracts and triterpenes from CA was verified, suggesting CA’s significant potential as a prospective agent for the therapy of cancer. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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Review

Jump to: Research

23 pages, 919 KiB

Open AccessReview

Potential Use of Marine Plants as a Source of Bioactive Compounds

by Maria del Mar Ribas-Taberner, Pere Miquel Mir-Rossello, Lorenzo Gil, Antoni Sureda and Xavier Capó

Molecules 2025, 30(3), 485; https://doi.org/10.3390/molecules30030485 - 22 Jan 2025

Cited by 1 | Viewed by 1465

Abstract

The search for bioactive natural compounds, traditionally focused on terrestrial environments, has increasingly expanded to the seas and oceans, opening new frontiers for exploration. Among the diverse organisms inhabiting these ecosystems, marine phanerogams have emerged as a promising source of health-promoting bioactive compounds. [...] Read more.

The search for bioactive natural compounds, traditionally focused on terrestrial environments, has increasingly expanded to the seas and oceans, opening new frontiers for exploration. Among the diverse organisms inhabiting these ecosystems, marine phanerogams have emerged as a promising source of health-promoting bioactive compounds. This review highlights the distinctive chemical diversity of seagrasses including species such as Posidonia oceanica, Zostera marina, and Cymodocea nodosa, among others, and focusses on the growing interest in natural therapies as alternatives to conventional pharmaceuticals. Compounds such as polysaccharides or secondary metabolites such as polyphenol and flavonoids produced by marine plants exhibit a broad range of beneficial properties, including anti-inflammatory, antibacterial, antioxidant, and antidiabetic qualities. This review describes how these compounds can mitigate inflammation, promote skin health, and combat oxidative stress. Moreover, certain marine extracts have demonstrated potential to inhibit cancer cell growth and improve metabolic disorders like obesity and diabetes. The manuscript also discusses the potential of marine plant extracts in the development of novel therapeutic agents to address various illnesses, including infections, chronic diseases, and metabolic disorders. It emphasizes the need for further research to fully elucidate the mechanisms underlying the activity of these bioactive compounds and their potential therapeutic applications. In summary, this study highlights marine plants as a valuable reservoir for identifying organic molecules, paving the way for innovative advancements in medical and healthcare interventions. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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35 pages, 3101 KiB

Open AccessReview

A Comprehensive Review of Traditional Medicinal Uses, Geographical Distribution, Botanical Characterization, Phytochemistry, and Pharmacology of Aralia continentalis Kitag.

by Luyun Zhang, Huri Piao and Hao Zang

Molecules 2024, 29(15), 3529; https://doi.org/10.3390/molecules29153529 - 26 Jul 2024

Cited by 1 | Viewed by 1816

Abstract

Aralia continentalis Kitag. (A. continentalis) holds significant medicinal value among the Aralia genus. It has traditionally been employed in ethnomedicine to address a wide range of conditions, including wind–cold–dampness arthralgia; rheumatic pain in the waist and lower extremities; lumbar muscular strain; [...] Read more.

Aralia continentalis Kitag. (A. continentalis) holds significant medicinal value among the Aralia genus. It has traditionally been employed in ethnomedicine to address a wide range of conditions, including wind–cold–dampness arthralgia; rheumatic pain in the waist and lower extremities; lumbar muscular strain; injuries resulting from falls, fractures, contusions, and strains; headache; toothache; and abscesses. Modern pharmacological research has validated its therapeutic potential, encompassing anti-inflammatory, analgesic, antioxidant, antimicrobial, insecticidal, hepatoprotective, anti-diabetic, and cytotoxic properties, among other pharmacological effects. To compile comprehensive knowledge on A. continentalis, a rigorous literature search was undertaken utilizing databases like SciFinder, PubMed, and Web of Science. This review seeks to delve into the plant’s traditional applications, geographical distribution, botanical characteristics, phytochemistry, and pharmacology. The objective is to lay a foundation and propose novel research directions for exploring the plant’s potential applications. Currently, one hundred and fifty-nine compounds have been isolated and identified from A. continentalis, encompassing diterpenoids, steroids, triterpenoids, volatile components, phenolics, vitamins, trace elements, and other compounds. Notably, diterpenoids, steroids, triterpenoids, volatile components, and phenolics have exhibited pronounced pharmacological effects, such as anti-inflammatory, analgesic, antioxidant, hepatoprotective, antidiabetic, and antimicrobial activities. However, despite the extensive research conducted, further studies are imperative to unravel new components and mechanisms of action, necessitating more in-depth investigations. This comprehensive exploration could pave the way for advancing and harnessing the potential of A. continentalis. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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Open AccessReview

Ethnomedicinal Uses, Geographical Distribution, Botanical Description, Phytochemistry, Pharmacology, and Quality Control of Laportea bulbifera (Sieb. et Zucc.) Wedd.: A Review

by Jiaxin Feng, Guangqing Xia, Junyi Zhu, Li Li and Hao Zang

Molecules 2024, 29(1), 42; https://doi.org/10.3390/molecules29010042 - 20 Dec 2023

Cited by 1 | Viewed by 1652

Abstract

Laportea bulbifera (Sieb. et Zucc.) Wedd. (L. bulbifera) is a significant plant in the Laportea genus. Traditionally, it has been used in ethnomedicine for treating various conditions such as rheumatic arthralgia, fractures, falling injuries, nephritis dropsy, limb numbness, pruritus, fatigue-induced internal [...] Read more.

Laportea bulbifera (Sieb. et Zucc.) Wedd. (L. bulbifera) is a significant plant in the Laportea genus. Traditionally, it has been used in ethnomedicine for treating various conditions such as rheumatic arthralgia, fractures, falling injuries, nephritis dropsy, limb numbness, pruritus, fatigue-induced internal imbalances, and irregular menstruation. Modern pharmacological studies have confirmed its therapeutic potential, including anti-inflammatory, immunosuppressive, analgesic, and anti-rheumatoid arthritis properties. To gather comprehensive information on L. bulbifera, a thorough literature search was conducted using databases like Web of Science, PubMed, ProQuest, and CNKI. This review aims to provide a comprehensive understanding of L. bulbifera, covering various aspects such as ethnomedicinal uses, geographical distribution, botanical description, phytochemistry, pharmacology, and quality control. The goal is to establish a solid foundation and propose new research avenues for exploring and developing potential applications of L. bulbifera. So far, a total of one hundred and eighty-nine compounds have been isolated and identified from L. bulbifera, including flavonoids, phenolics, nitrogen compounds, steroids, terpenoids, coumarins, phenylpropanoids, fatty acids and their derivatives, and other compounds. Notably, flavonoids and fatty acids have demonstrated remarkable antioxidant and anti-inflammatory properties. Additionally, these compounds show promising potential in activities such as analgesia, hypoglycemia, and hypolipidemia, as well as toxicity. Despite extensive fundamental studies on L. bulbifera, further research is still needed to enhance our understanding of its mechanism of action and improve quality control. This requires more comprehensive investigations to explore the specific material basis, uncover new mechanisms of action, and refine quality control methods related to L. bulbifera. By doing so, we could contribute to the further development and utilization of this plant. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts II)

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