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Search Results (113)

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Keywords = apigenin-7-glycoside

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19 pages, 2617 KB  
Review
Insights into the Therapeutic Use of Kalanchoe pinnata Supplement in Diabetes Mellitus
by Felix Omoruyi, Lauren Tatina, Lizette Rios, Dewayne Stennett and Jean Sparks
Pharmaceuticals 2025, 18(10), 1518; https://doi.org/10.3390/ph18101518 - 10 Oct 2025
Viewed by 123
Abstract
Kalanchoe pinnata, commonly known as the “miracle plant” or “life plant”, is a succulent species traditionally used for various health conditions. Recent research investigations have intensified interest in this species due to its diverse repertoire of bioactive constituents, including flavonoids, alkaloids, triterpenes, [...] Read more.
Kalanchoe pinnata, commonly known as the “miracle plant” or “life plant”, is a succulent species traditionally used for various health conditions. Recent research investigations have intensified interest in this species due to its diverse repertoire of bioactive constituents, including flavonoids, alkaloids, triterpenes, and glycosides. These compounds have been associated with multiple therapeutic effects, notably antioxidant, anti-inflammatory, and antidiabetic activities. Although several studies have highlighted the positive effects of the extracts of K. pinnata on key factors contributing to the pathophysiology and complications of diabetes mellitus, a systematic overview focusing on the use of these extracts and their bioactive constituents in the management of the disease is lacking. This literature review summarizes the phytochemical composition, traditional uses, and recent scientific data supporting the antidiabetic potential of K. pinnata, with a particular focus on its effects on glycemic control, as well as inflammatory and oxidative homeostasis, toxicity, safety, and potential clinical implications. The phytochemical constituents discussed include quercetin, kaempferol, apigenin, epigallocatechin gallate (EGCG), avicularin, and bufadienolides, along with a presentation of representative structures. The review also covers the potential mechanisms of action in diabetes mellitus. The survey of available literature highlights the effects of K. pinnata on indices of diabetes mellitus, including enhancing insulin sensitivity, mitigating oxidative stress and inflammation, lowering blood glucose levels, and the potential adverse effects. These results point to the promising prospect for K. pinnata use in the management of diabetes mellitus and its associated complications, while underscoring the need for more rigorous investigations, including well-controlled clinical trials. Full article
(This article belongs to the Special Issue Natural Products in Diabetes Mellitus: 2nd Edition)
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16 pages, 2458 KB  
Communication
Machine Learning and UHPLC–MS/MS-Based Discrimination of the Geographical Origin of Dendrobium officinale from Yunnan, China
by Tao Lin, Yanping Ye, Jiao Zhang, Jing Wang, Zhengxu Hu, Khine Zar Linn, Xinglian Chen, Hongcheng Liu, Zhenhuan Liu and Qinghua Yao
Foods 2025, 14(19), 3442; https://doi.org/10.3390/foods14193442 - 8 Oct 2025
Viewed by 262
Abstract
A rapid targeted screening method for 22 compounds, including flavonoids, glycosides, and phenolics, in Dendrobium officinale was developed using UHPLC–MS/MS, demonstrating good linear correlation coefficients, precision, repeatability, and stability. D. officinale from the Guangnan and Maguan regions can be effectively classified into two [...] Read more.
A rapid targeted screening method for 22 compounds, including flavonoids, glycosides, and phenolics, in Dendrobium officinale was developed using UHPLC–MS/MS, demonstrating good linear correlation coefficients, precision, repeatability, and stability. D. officinale from the Guangnan and Maguan regions can be effectively classified into two distinct categories using PCA. In addition, OPLS-DA discriminant analysis enables clear separation between groups, with samples forming well-defined clusters. The 22 chemical components provide valuable origin-related information for D. officinale. The compounds with VIP values of >1 included eriodictyol, vanillic acid, protocatechuic acid, gentisic acid, and naringenin. The difference in naringenin content between D. officinale from the two production areas was minimal. By contrast, eriodictyol and vanillic acid were relatively abundant in D. officinale from Guangnan, while gentisic acid and protocatechuic acid were more prevalent in D. officinale from Maguan. The pathways with higher Kyoto Encyclopedia of Genes and Genomes enrichment were primarily associated with lipid metabolism and atherosclerosis, fluid shear stress and atherosclerosis, and nonalcoholic fatty liver disease. These findings suggest that D. officinale exhibits promising lipid-balancing properties and potential cardiovascular health benefits. Seven machine learning algorithms—Random Forest, XGBoost, Support Vector Machine, k-Nearest Neighbor, Backpropagation Neural Network, Random Tree, and CatBoost—demonstrated superior accuracy and precision in distinguishing D. officinale from the Guangnan and Maguan regions. The key compounds with higher weights—vanillic acid, chrysoeriol, trigonelline, isoquercitrin, gallic acid, 4-hydroxybenzaldehyde, eriodictyol, sweroside, apigenin, and homoeriodictyol—play a crucial role in model construction and the identification of D. officinale from the Guangnan and Maguan regions. The quantification of 22 compounds using UHPLC–MS/MS, combined with PCA, OPLS-DA, and machine learning, enables effective discrimination of D. officinale from these two Yunnan production areas. Full article
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10 pages, 1320 KB  
Communication
Chemical Constituents from the Vietnamese Mangrove Avicennia marina: Two New Iridoid Glycosides and Their Cytotoxicity Against Cancer Cell Lines
by Ngo Van Hieu, Le Ba Vinh, Pham Thi Mai, Le Ngoc Hung, Nguyen Tien Dat, Lai Ha Phuong, Tran Phương Anh, Do Thanh Tuan, Nguyen Viet Phong, Truong Thi Thu Hien and Hoang Le Tuan Anh
Int. J. Mol. Sci. 2025, 26(19), 9694; https://doi.org/10.3390/ijms26199694 - 5 Oct 2025
Viewed by 287
Abstract
Avicennia marina, commonly known as the grey mangrove, is a salt-tolerant species widely distributed in coastal and estuarine ecosystems. Traditionally, it has been used in folk medicine to treat skin diseases, rheumatism, and ulcers due to its anti-inflammatory and antimicrobial properties. However, [...] Read more.
Avicennia marina, commonly known as the grey mangrove, is a salt-tolerant species widely distributed in coastal and estuarine ecosystems. Traditionally, it has been used in folk medicine to treat skin diseases, rheumatism, and ulcers due to its anti-inflammatory and antimicrobial properties. However, comprehensive studies on the chemical constituents and their pharmacological effects remain limited. The dried powder of the aerial parts of A. marina (3.6 kg) was successfully extracted three times with methanol (20 L × 3, each for 2 h) using a multifunctional ultrasonic cleaner operated at 25 °C with a 50% amplitude setting. In this study, the methanolic extract of the aerial parts of A. marina led to the isolation of eight compounds, including two previously unreported iridoid glycosides—avicenosides A and B (1 and 2)—and six known compounds: techtochrysin (3), 7,4′-di-O-methyl-apigenin (4), luteolin (5), kaempferol (6), trans-caffeic acid (7), and 3,4-dihydroxybenzoic acid (8). Their chemical structures were elucidated using nuclear magnetic resonance (NMR) spectroscopy and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) and compared with previously published data. Moreover, the absolute configuration of the sugar moieties in the new compounds was also identified. All isolated compounds were evaluated for their cytotoxicity against HepG2 and A549 cancer cell lines. The results indicate potential cytotoxicity of the secondary metabolites from A. marina and provide evidence of their promising role as lead compounds for the development of novel anticancer agents. Full article
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22 pages, 5424 KB  
Article
Integrated Transcriptome and Metabolome Analysis Reveals Molecular Mechanisms of Flavonoid Biosynthesis During Camphora officinarum Leaf Development
by Xiaofeng Peng, Peiwu Xie, Bing Li, Yonglin Zhong, Boxiang He, Yingli Wang, Yiqun Chen, Ning Li and Chen Hou
Forests 2025, 16(9), 1490; https://doi.org/10.3390/f16091490 - 19 Sep 2025
Viewed by 292
Abstract
Camphora officinarum Nees is a significant economic tree because of its aromatic, medicinal, and ornamental attributes. The diverse flavonoids present within the leaves of C. officinarum have been neglected for an extended period, hindering a comprehensive understanding of the molecular mechanisms responsible for [...] Read more.
Camphora officinarum Nees is a significant economic tree because of its aromatic, medicinal, and ornamental attributes. The diverse flavonoids present within the leaves of C. officinarum have been neglected for an extended period, hindering a comprehensive understanding of the molecular mechanisms responsible for color transformation and resistance to adverse environmental conditions. In this study, multi-omics analyses were conducted to systematically compare the relative contents of flavonoid metabolites and the expression profiles of flavonoid-related genes across three developmental stages of C. officinarum leaves. A total of 175 flavonoid compounds were detected via metabolomics, with flavonols being the most abundant. Through weighted gene co-expression network analysis, 25 key DEGs encoding CHS, DFR, FLS, ANS, F3′H, and LAR genes are predicted to be involved in anthocyanin biosynthesis for color change during leaf development. Notably, ten MYB, seven bHLH, and three ERF factors are potentially implicated in the regulation of key genes, underscoring their significant contributions to the color mechanisms underlying flavonoid biosynthesis. Other flavonoids, e.g., apigenin, isorhamnetin glycosides, sakuranetin, and sakuranin, may facilitate the adaptation of C. officinarum for protective purposes against adverse environmental conditions. These findings lay a theoretical foundation for resource exploration and the ornamentation improvement of C. officinarum. Full article
(This article belongs to the Section Genetics and Molecular Biology)
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27 pages, 3962 KB  
Article
Optimization of Conventional and Ultrasound-Assisted Extraction to Maximize Recovery of Total Phenolic Content and In Vitro Antioxidant Activity from Crataegus almaatensis Leaves
by Zhanar Nabiyeva, Akerke Kulaipbekova, Serena Carpentieri, Yuliya Pronina, Abdyssemat Samadun, Elmira Assembayeva and Giovanna Ferrari
Antioxidants 2025, 14(8), 1003; https://doi.org/10.3390/antiox14081003 - 16 Aug 2025
Viewed by 909
Abstract
Background: Crataegus almaatensis, an endemic hawthorn species from Kazakhstan, is known for its rich content of phenolic compounds and flavonoids with significant pharmacological potential. This study aimed to optimize and compare conventional solid–liquid extraction (SLE) and ultrasound-assisted extraction (UAE) processes for maximizing [...] Read more.
Background: Crataegus almaatensis, an endemic hawthorn species from Kazakhstan, is known for its rich content of phenolic compounds and flavonoids with significant pharmacological potential. This study aimed to optimize and compare conventional solid–liquid extraction (SLE) and ultrasound-assisted extraction (UAE) processes for maximizing the extractability of bioactive compounds from hawthorn leaves powder. Methods: The effects of temperature, extraction time, ethanol concentration, and solid-to-liquid ratio (or ultrasound power in the case of UAE) on total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity (FRAP, DPPH, and ABTS assays) were systematically evaluated. Results: The UAE method yielded higher concentrations of TPC and TFC, with up to 16% improvement in TPC and reduced ethanol usage (40% (v/v)) compared to SLE (75% (v/v)), demonstrating its efficiency and sustainability. Optimal extraction conditions were identified as 70 °C, 75% ethanol, 34 min, and an S/L ratio of 0.05 g/mL for SLE, 70 °C, 40% ethanol, 44 min, and 100 W US power for UAE. High-resolution HPLC-DAD and LC-Q/TOF-MS analyses confirmed the presence of key phenolic acids and flavonoid glycosides, including chlorogenic acid and apigenin-8-C-glucoside-2′-rhamnoside as the most abundant compounds identified. Conclusions: These findings validate UAE as an innovative, eco-friendly method for extracting bioactive compounds from hawthorn leaves and highlight its potential for developing natural antioxidants for pharmaceutical and nutraceutical applications. Full article
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19 pages, 1768 KB  
Article
Pomegranate Peels: A Promising Source of Biologically Active Compounds with Potential Application in Cosmetic Products
by Yulian Tumbarski, Ivan Ivanov, Radka Vrancheva, Nadezhda Mazova and Krastena Nikolova
Cosmetics 2025, 12(4), 169; https://doi.org/10.3390/cosmetics12040169 - 11 Aug 2025
Viewed by 2879
Abstract
As a rich source of biologically active compounds, pomegranate peel is a valuable by-product with applications in the food, pharmaceutical and cosmetic sectors. The present study aimed to investigate the phytochemical composition, antioxidant and antimicrobial activity, photoprotective activity and application in a cosmetic [...] Read more.
As a rich source of biologically active compounds, pomegranate peel is a valuable by-product with applications in the food, pharmaceutical and cosmetic sectors. The present study aimed to investigate the phytochemical composition, antioxidant and antimicrobial activity, photoprotective activity and application in a cosmetic emulsion of extracts obtained from pomegranate peel by different solvents. The analysis of phenolic compounds was determined by high-performance liquid chromatography (HPLC); the total phenolic content (TPC) and the total flavonoid content (TFC) were evaluated using standard spectrophotometric methods; the antioxidant activity was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging, ferric-reducing antioxidant power (FRAP) and 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays; antimicrobial screening was performed against twenty test microorganisms; the ultraviolet (UV) protection effect of extracts and cosmetic emulsion was assessed spectrophotometrically in the wavelength range of 290–320 nm. HPLC analysis revealed fourteen phenolic compounds, including four phenolic acids (ellagic, gallic, p-coumaric, and ferulic), two tannins (pedunculagin and punicalagin), six flavonoids (myricetin, hesperidin, quercetin, luteolin, kaempferol, and apigenin), and two quercetin glycosides (rutin and hyperoside). The four pomegranate peel extracts demonstrated high TPC, TFC and antioxidant potential (DMSO > 70% ethanolic > methanolic > aqueous), and significant antimicrobial activity. The four extracts showed a remarkable UV protection effect. When applied in a cosmetic emulsion, the ethanolic extract showed sun protection factor (SPF) values from 13.59 (0.5 mg/g) to 50.65 (5 mg/g). Based on the results obtained, we can conclude that pomegranate peel is a promising source of bioactive compounds, which can be successfully utilized by integration into various pharmaceutical and value-added skin health products. Full article
(This article belongs to the Special Issue Feature Papers in Cosmetics in 2025)
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13 pages, 1010 KB  
Article
Valorization of Flourensia cernua Foliage Through a Multiproduct Fungal Solid-State Bioprocess and Its Effect on In Vitro Digestibility
by Juan López-Trujillo, Juan Alberto Ascacio-Valdés, Miguel Mellado-Bosque, Cristóbal N. Aguilar, Antonio Francisco Aguilera-Carbó and Miguel Á. Medina-Morales
Fermentation 2025, 11(8), 433; https://doi.org/10.3390/fermentation11080433 - 29 Jul 2025
Viewed by 661
Abstract
Biotechnological valorization of Flourensia cernua foliage was carried out using fungal solid-state fermentation; several outcomes of this bioprocess were identified which added value to the plant material. F. cernua leaves placed in aluminum trays were inoculated with Aspergillus niger; extracts of this [...] Read more.
Biotechnological valorization of Flourensia cernua foliage was carried out using fungal solid-state fermentation; several outcomes of this bioprocess were identified which added value to the plant material. F. cernua leaves placed in aluminum trays were inoculated with Aspergillus niger; extracts of this plant were evaluated and the foliage was tested for in vitro digestibility. The solid bioprocess was carried out at 75% humidity for 120 h and after the fermentation, β-glucosidase activity; phenolics and in vitro digestibility were quantified and measured. Two high β-glucosidase production levels were detected at 42 and 84 h with 3192 and 4092 U/L, respectively. Several phenolics of industrial importance were detected with a HPLC-ESI-MS, such as glycosides of luteolin and apigenin. The other outcome was a substantial improvement in anaerobic digestibility. The unfermented sample registered a 30% in vitro degradability, whereas samples subjected to 84 h of fungal fermentation increased degradability by up to 51%. This bioprocess was designed to detect more than one product, which can contribute to an increase in the added value of F. cernua foliage. Full article
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32 pages, 722 KB  
Article
Nutritional and Bioactive Characterization of Unconventional Food Plants for Sustainable Functional Applications
by Izamara de Oliveira, José Miguel R. T. Salgado, João Krauspenhar Lopes, Marcio Carocho, Tayse F. F. da Silveira, Vitor Augusto dos Santos Garcia, Ricardo C. Calhelha, Celestino Santos-Buelga, Lillian Barros and Sandrina A. Heleno
Sustainability 2025, 17(15), 6718; https://doi.org/10.3390/su17156718 - 23 Jul 2025
Viewed by 933
Abstract
Unconventional food plants (UFPs) are increasingly valued for their nutritional composition and bioactive potential. This study proposes a comprehensive characterization of the chemical and bioactive properties of Pereskia aculeata Miller (Cactaceae) (PA); Xanthosoma sagittifolium (L.) Schott (Araceae) (XS); Stachys byzantina K. Koch (Lamiaceae) [...] Read more.
Unconventional food plants (UFPs) are increasingly valued for their nutritional composition and bioactive potential. This study proposes a comprehensive characterization of the chemical and bioactive properties of Pereskia aculeata Miller (Cactaceae) (PA); Xanthosoma sagittifolium (L.) Schott (Araceae) (XS); Stachys byzantina K. Koch (Lamiaceae) (SB); and inflorescences from three cultivars of Musa acuminata (Musaceae) var. Dwarf Cavendish, var. BRS Platina, and var. BRS Conquista (MAD, MAP, and MAC), including the assessment of physical, nutritional, phytochemical, and biological parameters. Notably, detailed phenolic profiles were established for these species, many of which are poorly documented in the literature. XS was characterized by a unique abundance of C-glycosylated flavones, especially apigenin and luteolin derivatives, rarely described for this species. SB exhibited high levels of phenylethanoid glycosides, particularly verbascoside and its isomers (up to 21.32 mg/g extract), while PA was rich in O-glycosylated flavonols such as quercetin, kaempferol, and isorhamnetin derivatives. Nutritionally, XS had the highest protein content (16.3 g/100 g dw), while SB showed remarkable dietary fiber content (59.8 g/100 g). Banana inflorescences presented high fiber (up to 66.5 g/100 g) and lipid levels (up to 7.35 g/100 g). Regarding bioactivity, PA showed the highest DPPH radical scavenging activity (95.21%) and SB the highest reducing power in the FRAP assay (4085.90 µM TE/g). Cellular antioxidant activity exceeded 2000% in most samples, except for SB. Cytotoxic and anti-inflammatory activities were generally low, with only SB showing moderate effects against Caco-2 and AGS cell lines. SB and PA demonstrated the strongest antimicrobial activity, particularly against Yersinia enterocolitica, methicillin-resistant Staphylococcus aureus (MRSA), and Enterococcus faecalis, with minimum inhibitory concentrations ranging from 0.156 to 0.625 mg/mL. Linear discriminant analysis revealed distinctive chemical patterns among the species, with organic acids (e.g., oxalic up to 7.53 g/100 g) and fatty acids (e.g., linolenic acid up to 52.38%) as key discriminant variables. Overall, the study underscores the nutritional and functional relevance of these underutilized plants and contributes rare quantitative data to the scientific literature regarding their phenolic signatures. Full article
(This article belongs to the Section Sustainable Food)
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22 pages, 1665 KB  
Review
Molecular Mechanisms of Vitexin: An Update on Its Anti-Cancer Functions
by Liyun Lu, Yinhua Deng, Junnan Li, Xing Feng and Hui Zou
Int. J. Mol. Sci. 2025, 26(12), 5853; https://doi.org/10.3390/ijms26125853 - 18 Jun 2025
Cited by 1 | Viewed by 1704
Abstract
Cancer remains a leading global health challenge, necessitating the exploration of novel therapeutic strategies. Vitexin (apigenin-8-C-β-D-glucopyranoside), a natural flavonoid glycoside with a molecular weight of 432.38 g/mol, is derived from plants such as mung bean, beetroot, and hawthorn. This compound features a distinctive [...] Read more.
Cancer remains a leading global health challenge, necessitating the exploration of novel therapeutic strategies. Vitexin (apigenin-8-C-β-D-glucopyranoside), a natural flavonoid glycoside with a molecular weight of 432.38 g/mol, is derived from plants such as mung bean, beetroot, and hawthorn. This compound features a distinctive C-glycosidic bond at the 8-position of its apigenin backbone, contributing to its enhanced metabolic stability compared to O-glycosidic flavonoids. Preclinical studies demonstrate that vitexin modulates critical cellular processes such as cell cycle progression, apoptosis, autophagy, metastasis, angiogenesis, epigenetic modifications, and tumor glycolysis inhibition. It exerts its effects by targeting key signaling pathways, including phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/Akt/mTOR), nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), and signal transducer and activator of transcription 3 (STAT3), and shows potential for combination therapies to enhance efficacy and overcome resistance. Advances in nanotechnology further enhance its bioavailability and delivery potential. This review comprehensively examines the current evidence on vitexin’s anticancer mechanisms, highlighting its multi-target therapeutic potential and future research directions. Full article
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14 pages, 892 KB  
Article
Metabolomic Analysis Provides Insights into Bud Paradormancy in Camellia sinensis cv. Huangdan
by Mingjie Chen, Zhenghua Du, Wenjie Yue, Xiangrui Kong, Quanming Xu, Dongsheng Fang and Changsong Chen
Int. J. Mol. Sci. 2025, 26(11), 5094; https://doi.org/10.3390/ijms26115094 - 26 May 2025
Viewed by 563
Abstract
Bud paradormancy has been widely studied in perennial deciduous woody species, but little attention has been paid to paradormancy set and release in perennial evergreen tree species. Here, shoot bud paradormancy in Camellia sinensis cv. Huangdan was studied by untargeted metabolomics. We found [...] Read more.
Bud paradormancy has been widely studied in perennial deciduous woody species, but little attention has been paid to paradormancy set and release in perennial evergreen tree species. Here, shoot bud paradormancy in Camellia sinensis cv. Huangdan was studied by untargeted metabolomics. We found that after removing the axillary floral buds for one day, the paradormancy of the axillary shoot buds was released. The paradormant shoot buds had lower glucose-1-phosphate, fructose, and D-(-)-tagatofuranose content but higher trehalose, raffinose, galactinol, and α-D-xylopyranose content. Meanwhile, high levels of asparagine were accumulated. Flavonoids were differentially accumulated, and higher levels of three flavone glycosides (C-diglucosylapigenin, apigenin 6-C-glucoside 8-C-arabinoside, and prunin) and four proanthocyanidins (Procyanidin trimer isomer 1, Galloylprocyanidin dimer, Procyanidin trimer isomer 3, and Galloylated trimeric proanthocyanidin) were accumulated in paradormant shoot buds. During the paradormancy-to-growth transition, all these metabolites were reversed. These data suggest that the reconfiguration of carbon, nitrogen, and flavonoid metabolism could be an important aspect for the paradormancy set and release of tea axillary shoot buds. This study provided novel insights into shoot bud paradormancy set and release in a perennial evergreen tree species. Full article
(This article belongs to the Special Issue Advances in Tea Tree Metabolism and Genetics)
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48 pages, 8000 KB  
Review
A Comprehensive Review of the Phenolic Compounds in Dracocephalum Genus (Lamiaceae) Related to Traditional Uses of the Species and Their Biological Activities
by Izabela Weremczuk-Jeżyna and Izabela Grzegorczyk-Karolak
Molecules 2025, 30(9), 2017; https://doi.org/10.3390/molecules30092017 - 30 Apr 2025
Cited by 1 | Viewed by 1369
Abstract
The genus Dracocephalum (family Lamiaceae) comprises approximately 70 species, many of which have been traditionally used in various ethnomedical systems. The plants exhibit a broad distribution across steppe, semi-deserts, deserts, and alpine zones of temperate Eurasia, with isolated endemic species occurring in North [...] Read more.
The genus Dracocephalum (family Lamiaceae) comprises approximately 70 species, many of which have been traditionally used in various ethnomedical systems. The plants exhibit a broad distribution across steppe, semi-deserts, deserts, and alpine zones of temperate Eurasia, with isolated endemic species occurring in North America and North Africa. The traditional medicinal uses of the Dracocephalum species encompass the treatment of respiratory diseases, colds and fever, gastrointestinal disorders, liver and gallbladder ailments, musculoskeletal conditions, cardiovascular diseases, diabetes, gynecological and urological disorders, as well as ailments of the ears, throat, mouth, and eyes, as well as various dermatological conditions. The plants are rich sources of polyphenolic compounds, including flavonoids and phenolic acids, which contribute to their diverse pharmacological activities. The flavonoid profile of the Dracocephalum species is dominated by luteolin and apigenin derivatives, supplemented by mono-, di-, tri-, tetra-, and pentamethoxylated flavones. The predominant phenolic acids are chlorogenic acid, coumaric acid, rosmarinic acid, and their derivatives. Other phenolic compounds have also been identified in the genus: anthocyanins, lignans, phenylethanoids, phenylacetamide glycosides, flavonoid alkaloids, gingerols, coumarins, furanocoumarins, and cyanogenic glucosides. Despite growing scientific interest in this genus, a comprehensive review of its polyphenolic constituents, their structures, and associated biological activities remains lacking. To bridge this gap, this review presents an analysis of the polyphenolic profile of the Dracocephalum species, their ethnomedicinal uses, and the latest findings on their biological potential. Full article
(This article belongs to the Special Issue Biological Activity of Plant Extracts)
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18 pages, 10631 KB  
Article
Integrated Transcriptomic and Metabolomic Analysis Reveals Tissue-Specific Flavonoid Biosynthesis and MYB-Mediated Regulation of UGT71A1 in Panax quinquefolius
by Yumeng Wang, Jiaxin Zhang, Ping Wang, Yongkang Li, Yihan Wang, Yan Yan, Junwen Chi, Jiankang Chen, Junmei Lian, Xiangmin Piao, Xiujuan Lei, Ying Xiao, Jeremy Murray, Micheal K. Deyholos, Yingping Wang, Peng Di and Jian Zhang
Int. J. Mol. Sci. 2025, 26(6), 2669; https://doi.org/10.3390/ijms26062669 - 16 Mar 2025
Cited by 2 | Viewed by 1469
Abstract
Panax quinquefolius is a globally valued medicinal plant rich in bioactive flavonoids, yet the molecular mechanisms underlying their biosynthesis remain poorly understood. In this study, we integrated transcriptomic and metabolomic analyses to investigate tissue-specific flavonoid accumulation and regulatory networks in roots, leaves, and [...] Read more.
Panax quinquefolius is a globally valued medicinal plant rich in bioactive flavonoids, yet the molecular mechanisms underlying their biosynthesis remain poorly understood. In this study, we integrated transcriptomic and metabolomic analyses to investigate tissue-specific flavonoid accumulation and regulatory networks in roots, leaves, and flowers. Metabolomic profiling identified 141 flavonoid metabolites, with flavones, flavonols, and C-glycosylflavones predominantly enriched in aerial tissues (leaves and flowers), while specific glycosides like tricin 7-O-acetylglucoside showed root-specific accumulation. Transcriptome sequencing revealed 15,551–18,946 DEGs across tissues, and the reliability of the transcriptomic data was validated by qRT-PCR. KEGG and GO annotation analyses suggested that these DEGs may play a crucial role in the biosynthesis and metabolism of secondary metabolites. From the DEGs, UGTs and MYB TFs were identified and subjected to correlation analysis. Functional validation through in vitro enzymatic assays confirmed that PqUGT71A1 catalyzes apigenin and naringenin glycosylation at the 7-OH position. Additionally, subcellular localization and yeast one-hybrid assays demonstrated that PqMYB7 and PqMYB13 interact with the PqUGT71A1 promoter and activate its expression.. This study unveils the spatial dynamics of flavonoid metabolism in P. quinquefolius and establishes a MYB-UGT regulatory axis, providing critical insights for metabolic engineering and bioactive compound optimization in medicinal plants. Full article
(This article belongs to the Special Issue Advances in Plant Genomics and Genetics: 2nd Edition)
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19 pages, 2563 KB  
Article
Insulin-Sensitizing Properties of Decoctions from Leaves, Stems, and Roots of Cucumis prophetarum L.
by Zewdie Mekonnen, Giuseppe Petito, Getasew Shitaye, Gianluca D’Abrosca, Belete Adefris Legesse, Sisay Addisu, Maurizio Ragni, Antonia Lanni, Roberto Fattorusso, Carla Isernia, Lara Comune, Simona Piccolella, Severina Pacifico, Rosalba Senese, Gaetano Malgieri and Solomon Tebeje Gizaw
Molecules 2025, 30(1), 98; https://doi.org/10.3390/molecules30010098 - 30 Dec 2024
Viewed by 1610
Abstract
Type 2 diabetes mellitus (T2DM) is a chronic disease characterized by insulin resistance and impaired beta-cell secretory function. Since existing treatments often present side effects based on different mechanisms, alternative therapeutic options are needed. In this scenario, the present study first evaluates the [...] Read more.
Type 2 diabetes mellitus (T2DM) is a chronic disease characterized by insulin resistance and impaired beta-cell secretory function. Since existing treatments often present side effects based on different mechanisms, alternative therapeutic options are needed. In this scenario, the present study first evaluates the cytotoxicity of decoctions from the leaves, stems, and roots of Cucumis prophetarum L. on HepG2 and L6C5 cells. The extracts were chemically investigated by UV–Vis and ATR-FTIR spectroscopic techniques and by ultra high-performance chromatographic techniques, coupled with high-resolution mass spectrometry. Briefly, decoctions from the leaves and stems were mainly composed of apigenin C-glycosides, while the root decoction was rich in raffinose and cucumegastigmane II. To evaluate the insulin-sensitizing properties of the extracts in insulin-resistant L6 myoblasts, an evaluation by Western blot analysis of the proteins in the insulin signaling pathway was then performed. Particularly, key proteins of insulin signaling were investigated, i.e., insulin receptor substrate (IRS-1), protein kinase B (PKB/AKT), and glycogen synthase kinase-3 (GSK-3β), which have gained considerable attention from scientists for the treatment of diabetes. Under all conditions tested, the three decoctions showed low cytotoxicity. The stem and root decoction (300 μg/mL) resulted in a significant increase in the levels of p-IRS-1 (Tyr612), GSK3β (Ser9), and p-AMPK (Thr172) compared to those of the palmitic acid-treated group, and the leaf decoction resulted an increase in the level of p-IRS-1 (Tyr612) and p-AMPK (Thr172) and a decrease in p-GSK3β (Ser9) compared to the levels for the palmitic acid-treated group. The root decoction also reduced the level of p-mToR (Ser2448). Overall, the acquired data demonstrate the effect of reducing insulin resistance induced by the investigated decoctions, opening new scenarios for the evaluation of these effects aimed at counteracting diabetes and related diseases in animal models. Full article
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18 pages, 2581 KB  
Article
Relationship Between the Structure of the Flavone C-Glycosides of Linseed (Linum usitatissimum L.) and Their Antioxidant Activity
by Imen Ghozzi, Jean-Xavier Fontaine, Roland Molinié, Redouan Elboutachfaiti, Lylia Akkouche, Khaled Sebei, David Mathiron, Christophe Hano, Laurine Garros, Elodie Choque, Romain Roulard, Laurent Petit, Cédric Delattre, Emmanuel Petit and Anthony Quéro
Molecules 2024, 29(24), 5829; https://doi.org/10.3390/molecules29245829 - 10 Dec 2024
Cited by 3 | Viewed by 2680
Abstract
Flavonoids have been documented to have good antioxidant activities in vitro. In recent years, reports on the antioxidant activities of flavone C-glycosides, a subclass of flavonoids, have attracted great attention. Despite the wealth of information on this subject, the correlation between structure [...] Read more.
Flavonoids have been documented to have good antioxidant activities in vitro. In recent years, reports on the antioxidant activities of flavone C-glycosides, a subclass of flavonoids, have attracted great attention. Despite the wealth of information on this subject, the correlation between structure and function is not well understood. In this work, the relationship between the structure and the antioxidant activity of 12 flavone C-glycosides extracted from the aerial part of winter linseed (Linum usitatissimum L.) was studied to fill the current gaps. Orientin, isoorientin, vitexin, isovitexin, swertisin, swertiajaponin, carlinoside, schaftoside, lucenin-1, lucenin-2, vicenin-1, and vicenin-2 were purified by preparative HPLC and by the drowning-out crystallization method. Then, the control of the purity and the confirmation of the chemical structures were assessed by LC-MS and NMR analyses. The antioxidant activity was evaluated using ABTS, CUPRAC, FRAP, and iron chelating activity in vitro assays. Luteolin and its flavone C-glycoside derivatives exhibited higher antioxidant activity than apigenin and its flavone C-glycosides derivatives. This could be attributed to the ortho-dihydroxyl groups at C-3′ and C-4′ of the B ring in the flavonoid skeleton, which seemed to play an important role in antioxidant behavior. These results indicate that the antioxidant activity of these compounds, derived from apigenin and luteolin, can be closely related to their structural characteristics, including the position and nature of the sugars, the number of hydroxyl groups, and the presence of methyl group. Full article
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Article
Improved Skin Barrier Function Along with Hydration Benefits of Viola yedoensis Extract, Aesculin, and Schaftoside and LC-HRMS/MS Dereplication of Its Bio-Active Components
by Sreelatha Thonthula, Sandra De Sousa, Alexis Dubuis, Samia Boudah, Richa Mehta, Akanksha Singh, Joan Eilstein, Jean-Claude Tabet, Sherluck John, Dhimoy Roy and Steve Thomas Pannakal
Int. J. Mol. Sci. 2024, 25(23), 12770; https://doi.org/10.3390/ijms252312770 - 27 Nov 2024
Cited by 2 | Viewed by 3632
Abstract
The skin hydration level is a key factor that influences the physical and mechanical properties of the skin. The stratum corneum (SC), the outermost layer of the epidermis, is responsible for the skin’s barrier function. In this study, we investigated the role of [...] Read more.
The skin hydration level is a key factor that influences the physical and mechanical properties of the skin. The stratum corneum (SC), the outermost layer of the epidermis, is responsible for the skin’s barrier function. In this study, we investigated the role of a unique composition of Viola yedoensis extract for its ability to activate CD44, a cell-surface receptor of hyaluronic acid, and aquaporin-3, a water-transporting protein, in human keratinocytes (HaCaT). An ELISA assay evaluating the protein expression levels of CD44, aquaporin-3 (AQP3), filaggrin, and keratin-10 revealed that V. yedoensis extract upregulated the levels of CD44 and AQP3 by 15% and 78%, respectively. Additionally, V. yedoensis extract demonstrated a comparative effect on water vapor flux in TEWL and lipid perturbation in DSC versus the reference, glycerin. In light of this new biological efficacy, a detailed phytochemical characterization was undertaken using an integrated LC-HRMS/MS-based metabolomics approach, which provided further insights on the chemistry of V. yedoensis. This led to the identification of 29 secondary metabolites, 14 of which are reported here for the first time, including esculetin, aesculin, apigenin and kaempferol C-glycosides, megastigmane glycosides, roseoside, platanionoside B, and an eriojaposide B isomer, along with the rare, calenduloside F and esculetin diglucoside, which are reported for the first time from the genus, Viola. Notably, two active components identified in the V. yedoensis extract, namely, aesculin and schaftoside, showed an upregulation of the protein expression of CD44 in HaCaT cells by 123% and 193% within 24 h of treatment, respectively, while aesculin increased AQP3 levels by 46%. Aesculin and schaftoside also significantly upregulated the expression of K-10 levels by 299% and 116%, which was considerably higher than sodium hyaluronate, the positive control. The rationale used to characterize the new structures is outlined along with the related biosynthetic pathways envisioned to generate roseoside and Eriojaposide B. These findings provide new molecular insights to deepen the understanding of how V. yedoensis extract, along with the biomarkers aesculin and schaftoside, restores the skin barrier and skin hydration benefits. Full article
(This article belongs to the Special Issue Recent Advances in Medicinal Plants and Natural Products)
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