Search Results (86)

The sorghum aphid (Melanaphis sacchari (Zehntner, 1897)), a globally destructive pest, severely compromises sorghum yield and quality. This study compared aphid-resistant (HX133) and aphid-susceptible (HX37) sorghum (Sorghum bicolor (L.) Moench) cultivars, revealing that HX133 significantly suppressed aphid proliferation through repellent and antibiotic effects, while aphid populations increased continuously in HX37. Transcriptome analysis identified 2802 differentially expressed genes (DEGs, 45.9% upregulated) in HX133 at 24 h post-infestation, in contrast with only 732 DEGs (21% upregulated) in HX37. Pathway enrichment highlighted shikimate-mediated phenylpropanoid/flavonoid biosynthesis and glutathione metabolism as central to HX133’s defense response, alongside photosynthesis-related pathways common to both cultivars. qRT-PCR validation confirmed activation of the shikimate pathway in HX133, driving the synthesis of dhurrin—a cyanogenic glycoside critical for aphid resistance—and other tyrosine-derived metabolites (e.g., benzyl isoquinoline alkaloids, tocopherol). These findings demonstrate that HX133 employs multi-layered metabolic regulation, particularly dhurrin accumulation, to counteract aphid infestation, whereas susceptible cultivars exhibit limited defense induction. This work provides molecular targets for enhancing aphid resistance in sorghum breeding programs. Full article

Syringin is a phenylpropanoid glycoside isolated from the bark of Syringa vulgaris. Phillygenin is a lignan obtained mainly from the fruits and flowers of Forsythia intermedia. Both compounds have shown potent anti-inflammatory and antioxidant properties. We investigated the potential role of syringin and phillygenin in preventing lipid deposition in macrophages. Syringin and phillygenin significantly (p < 0.001) reduced lipid deposition in macrophages in a dose-dependent manner. For syringin, the greatest reduction in CD36 receptor expression was found to be over 80% (50 μg/mL) compared to the cholesterol-stimulated control (p < 0.001). Phillygenin inhibited CD36 receptor expression by approximately 25% (50 μg/mL), compared to the stimulated control (p < 0.05). For syringin, the CD36 receptor regulation pathway was PPAR-γ dependent. Phillygenin showed a statistically significant (p < 0.001) increase in the expression of the ABCA1 transporter: 2.5-fold (10 μg/mL), 3-fold (20 μg/mL) and 4-fold (50 μg/mL) compared to the cholesterol-stimulated control. Syringin did not significantly increase ABCA1 expression. For phillygenin, the activation pathway of the ABCA1 transporter was HO-1dependent. Our study showed that syringin inhibits the cholesterol-induced differentiation of macrophages into foam cells. Moreover, phillygenin increased cholesterol efflux from macrophages. Therefore, syringin and phillygenin may be valuable agents in the prevention of early and late atherosclerosis. Full article

Soil salinization hinders plant growth and agricultural production, so breeding salt-tolerant crops is an economical way to exploit saline–alkali soils. However, the specific metabolites and associated pathways involved in salt tolerance of the dandelion have not been clearly elucidated so far. Here, we compared the transcriptome and metabolome responses of 0.7% NaCl-stressed dandelion ‘BINPU2’ (variety A) and ‘TANGHAI’ (variety B). Our results showed that 222 significantly altered metabolites mainly enriched in arginine biosynthesis and pyruvate metabolism according to a KEGG database analysis in variety A, while 147 differential metabolites were predominantly enriched in galactose metabolism and the pentose phosphate pathway in variety B. The transcriptome data indicated that the differentially expressed genes (DEGs) in variety A were linked to secondary metabolite biosynthesis, phenylpropanoid biosynthesis, and photosynthesis–antenna proteins. Additionally, KEGG annotations revealed the DEGs had functions assigned to general function prediction only, post-translation modification, protein turnover, chaperones, and signal transduction mechanisms in variety A. By contrast, the DEGs had functions assigned to variety B as plant–pathogen interactions, phenylpropanoid biosynthesis, and photosynthesis–antenna proteins, including general function prediction, signal transduction mechanisms, and secondary metabolite biosynthesis from the KOG database functional annotation. Furthermore, 181 and 162 transcription factors (TFs) expressed under saline stress conditions specifically were detected between varieties A and B, respectively, representing 36 and 37 TF families. Metabolomics combined with transcriptomics revealed that salt stress induced substantial changes in terpenoid metabolites, ubiquinone biosynthesis metabolites, and pyruvate metabolites, mediated by key enzymes from the glycoside hydrolase family, adenylate esterases family, and P450 cytochrome family at the mRNA and/or metabolite levels. These results may uncover the potential salt-response mechanisms in different dandelion varieties, providing insights for breeding salt-tolerant crop plants suitable for saline–alkali land cultivation. Full article

The genus Clinopodium L. (Lamiaceae) comprises perennial herbaceous plants known for their diverse pharmacological properties. Clinically, these plants are mainly used for the treatment of various hemorrhagic disorders. This review systematically summarizes the research progress on the chemical composition, pharmacological activity, quality control, toxicity, and pharmacokinetics of the genus Clinopodium by searching Google Scholar, Scopus-Elsevier, Wiley, Springer, Taylor & Francis, Medline, Web of Science, CNKI, Weipu, Wanfang, and other academic databases over the last decade (March 2015–February 2025). To date, more than one hundred and thirty structurally diverse secondary metabolites have been isolated and identified from this genus, including flavonoids, triterpenoid saponins, diterpenoid glycosides, lignans, and phenylpropanoids. In addition, numerous volatile oil constituents have been identified in over forty species of the genus Clinopodium. Crude extracts and purified compounds exhibit a variety of pharmacological activities, including hemostatic, anti-myocardial cell injury, cardiovascular protective, anti-inflammatory, antimicrobial, antitumor, hypoglycemic, and insecticidal properties. However, current quality assessment protocols in the genus Clinopodium are limited to flavonoid- and saponin-based evaluations in C. chinense (Benth.) O. Kuntze and C. gracile (Benth.) O. Matsum. Further research is needed to elucidate the pharmacological mechanisms, toxicity, and possible interactions with other drugs. Therefore, the genus Clinopodium has a wide range of biologically active compounds with potential applications in drug development for hemostasis and cardiovascular protection. Nevertheless, there is also an urgent need to establish standardized methodologies to address uncertainties concerning the safety and efficacy of injectable extracts or compounds. Full article

Long-lasting brain fatigue is a consequence of stroke or traumatic brain injury associated with emotional, psychological, and physical overload, distress in hypertension, atherosclerosis, viral infection, and aging-related chronic low-grade inflammatory disorders. The pathogenesis of brain fatigue is linked to disrupted neurotransmission, the glutamate-glutamine cycle imbalance, glucose metabolism, and ATP energy supply, which are associated with multiple molecular targets and signaling pathways in neuroendocrine-immune and blood circulation systems. Regeneration of damaged brain tissue is a long-lasting multistage process, including spontaneously regulating hypothalamus-pituitary (HPA) axis-controlled anabolic–catabolic homeostasis to recover harmonized sympathoadrenal system (SAS)-mediated function, brain energy supply, and deregulated gene expression in rehabilitation. The driving mechanism of spontaneous recovery and regeneration of brain tissue is a cross-talk of mediators of neuronal, microglia, immunocompetent, and endothelial cells collectively involved in neurogenesis and angiogenesis, which plant adaptogens can target. Adaptogens are small molecules of plant origin that increase the adaptability of cells and organisms to stress by interaction with the HPA axis and SAS of the stress system (neuroendocrine-immune and cardiovascular complex), targeting multiple mediators of adaptive GPCR signaling pathways. Two major groups of adaptogens comprise (i) phenolic phenethyl and phenylpropanoid derivatives and (ii) tetracyclic and pentacyclic glycosides, whose chemical structure can be distinguished as related correspondingly to (i) monoamine neurotransmitters of SAS (epinephrine, norepinephrine, and dopamine) and (ii) steroid hormones (cortisol, testosterone, and estradiol). In this narrative review, we discuss (i) the multitarget mechanism of integrated pharmacological activity of botanical adaptogens in stress overload, ischemic stroke, and long-lasting brain fatigue; (ii) the time-dependent dual response of physiological regulatory systems to adaptogens to support homeostasis in chronic stress and overload; and (iii) the dual dose-dependent reversal (hormetic) effect of botanical adaptogens. This narrative review shows that the adaptogenic concept cannot be reduced and rectified to the various effects of adaptogens on selected molecular targets or specific modes of action without estimating their interactions within the networks of mediators of the neuroendocrine-immune complex that, in turn, regulates other pharmacological systems (cardiovascular, gastrointestinal, reproductive systems) due to numerous intra- and extracellular communications and feedback regulations. These interactions result in polyvalent action and the pleiotropic pharmacological activity of adaptogens, which is essential for characterizing adaptogens as distinct types of botanicals. They trigger the defense adaptive stress response that leads to the extension of the limits of resilience to overload, inducing brain fatigue and mental disorders. For the first time, this review justifies the neurogenesis potential of adaptogens, particularly the botanical hybrid preparation (BHP) of Arctic Root and Ashwagandha, providing a rationale for potential use in individuals experiencing long-lasting brain fatigue. The review provided insight into future research on the network pharmacology of adaptogens in preventing and rehabilitating long-lasting brain fatigue following stroke, trauma, and viral infections. Full article

Lantana camara L., commonly known as pigeon berry, is a herbaceous plant of growing scientific interest due to the high medicinal value. In fact, despite being categorized as an invasive species, it has been used for a long time to treat different diseases thanks to the many biological activities. Triterpenes, flavonoids, phenylpropanoids, and iridoid glycosides are the bioactive compounds naturally occurring in L. camara that have demonstrated anticancer, antifilarial, nematocidal, antibacterial, insecticidal, antileishmanial, antifungal, anti-inflammatory, and antioxidant properties. The aim of this review is to update the information concerning the chemistry and biological activity of L. camara extracts and their constituents, including semisynthetic derivatives, revising the literature until June 2024. We believe that the data reported in this review clearly demonstrate the importance of the plant as a promising source of medicines and will therefore stimulate further investigations. Full article

Cinnamomum osmophloeum, commonly known as indigenous cinnamon, is a tree species native to Taiwan’s hardwood forests. It has been extensively investigated for its chemical composition and bioactivities. Several reports have shown that C. osmophloeum leaves are rich in aromatic oils, which are grouped into various chemotypes based on their major constituents. Components of the volatile oils included phenylpropanoids, monoterpenoids, sesquiterpenoids, phenols, coumarins, and other miscellaneous compounds. In addition, other secondary metabolites previously identified in this species included flavonol glycosides, phenolic acids, lignans, proanthocyanidins, and cyclopropanoids. C. osmophloeum is widely recognized for its medicinal and industrial applications, particularly its essential oils. In general, essential oils exhibit remarkable anti-inflammatory and antioxidant actions, enabling them to modulate key inflammatory mediators and neutralize free radicals. This review explored the phytochemical composition of the essential oils and extracts from C. osmophloeum as well as therapeutic potential of this species, focusing on the action mechanisms and clinical potential. We hope that this review will contribute to a better understanding of the biological effects of this plant and its potential applications in the management of conditions associated with inflammation and oxidative stress. Full article

Rehmannia glutinosa Libosch., which belongs to the Orobanchaceae family, is a perennial herb found in China, Japan, and Korea. In traditional medicine, it is used to cool the body, improve water metabolism in the kidney, and provide protection from metabolic diseases such as type 2 diabetes mellitus (T2DM) and obesity. In this study, three new compounds were isolated from the roots of R. glutinosa, along with eighteen known compounds. Structure elucidation was performed with spectroscopic analyses including nuclear magnetic resonance (NMR) and circular dichroism (CD) spectroscopy. As the AMP-activated protein kinase (AMPK) signaling pathway is reportedly related to metabolic diseases, AMPK activation studies were conducted using in silico simulations and in vitro assays. Among the isolated compounds, 1 showed a potential as an AMPK activator in both in silico simulations and in vitro experiments. Our findings expand the chemical profiles of the plant R. glutinosa and suggest that one newly found compound (1) activates AMPK. Full article

A comprehensive phytochemical investigation of the twigs/leaves and flower buds of Kolkwitzia amabilis, a rare deciduous shrub native to China, led to the isolation of 39 structurally diverse compounds. These compounds include 11 iridoid glycosides (1–4 and 7–13), 20 triterpenoids (5, 6, and 14–31), and 8 phenylpropanoids (32–39). Among these, amabiliosides A (1) and B (2) represent previously undescribed bis-iridoid glycosides, while amabiliosides C (3) and D (4) feature a unique bis-iridoid-monoterpenoid indole alkaloid scaffold with a tetrahydro-β-carboline-5-carboxylic acid moiety. Amabiliacids A (5) and B (6) are 24-nor-ursane-type triterpenoids characterized by an uncommon ∆^11,13(18) transannular double bond. Their chemical structures and absolute configurations were elucidated through spectroscopic data and electronic circular dichroism analyses. Compound 2 exhibited a moderate inhibitory effect against acetyl CoA carboxylase 1 (ACC1), with an IC₅₀ value of 9.6 μM. Lonicejaposide C (8), 3β-O-trans-caffeoyl-olean-12-en-28-oic acid (29), and (23E)-coumaroylhederagenin (31) showed notable inhibitory effects on ATP-citrate lyase (ACL), with IC₅₀ values of 3.6, 1.6, and 4.7 μM, respectively. Additionally, 3β-acetyl-ursolic acid (17) demonstrated dual inhibitory activity against both ACC1 and ACL, with IC₅₀ values of 10.3 and 2.0 μM, respectively. The interactions of the active compounds with ACC1 and ACL enzymes were examined through molecular docking studies. From a chemotaxonomic perspective, the isolation of bis-iridoid glycosides in this study may aid in clarifying the taxonomic relationship between the genera Kolkwitzia and Lonicera within the Caprifoliaceae family. These findings highlight the importance of conserving plant species with unique and diverse secondary metabolites, which could serve as potential sources of new therapeutic agents for treating ACC1/ACL-associated diseases. Full article

Deep eutectic solvents (DESs) are mixtures of organic compounds displaying excellent solvent properties while keeping an ecofriendly character. In this study, DESs have been applied to the extraction of phenylpropanoid glycosides from Pedicularis oederi Vahl, successively separated by means of counter-current chromatography. Firstly, the ultrasonic-assisted extraction conditions were optimized by response surface methodology, and the results showed phenylpropanoid glycosides could be well extracted under the optimized extraction conditions with deep eutectic solvents. Then, the sample was separated by counter-current chromatography using ethyl acetate/aqueous solution of choline chloride and glycerol (6:6, v/v) as the solvent system. In about 360 min, four phenylpropanoid glycosides, including 31.6 mg of echinacoside, 65.3 mg of Jionoside A1, 28.9 mg of Forsythoside B, 74.1 mg of verbascoside, and 21.2 mg of kaempferol-3-O-rutinoside were obtained from about 900 mg of the sample. It revealed deep eutectic solvents could be well employed as a green solvent for the extraction and counter-current separation of natural products. Full article

Scrophulariae Radix (SR), the dried root of Scrophularia ningpoensis Hemsl (S. ningpoensis), has been extensively used as traditional Chinese medicine for thousands of years. However, since the mid-20th century, the traditional processing technology of S. ningpoensis has been interrupted. Therefore, ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry technology, together with a Global Natural Product Social Molecular Networking (GNPS) method, was applied to comprehensively analyze the characteristic changes and mutual transformation of chemical constituents in the differently processed roots of S. ningpoensis, as well as to scientifically elucidate the processing mechanism of differently processed SR. As a result, a total of 149 components were identified. Notably, with the help of the GNPS data platform and MS² fragment ions, the possible structures of four new compounds (47, 48, 50, and 73) were deduced in differently processed SR samples, in which 47, 48, and 50 are iridoid glycosides, and 73 is a phenylpropanoid glycoside. Five cyclopeptides (78, 86, 97, 99, and 104) derived from leucine (isoleucine) were identified in SR for the first time. The heatmaps analysis results indicated that leucine or isoleucine may be converted to cyclopeptides under the prolonged high-temperature conditions. Moreover, it is found that short-time steaming can effectively prevent the degradation of glycosides by inactivating enzymes. This study provides a new and efficient technical strategy for systematically identifying the chemical components, rapidly discovering the components, and preliminarily clarifying the processing mechanism of S. ningpoensis, as well as also providing a scientific basis for the improvement of the quality standards and field processing of S. ningpoensis. Full article

Herbal teas are used in South Africa as digestives to lower glycaemia and for other indications. However, the chemical composition of the infusions and their effect on enzymes related to metabolic syndrome is poorly known. The composition of infusions and methanol extracts of B. saligna (Scrophulariaceae), Lippia javanica, L. scaberrima, and Phyla dulcis (Verbenaceae) was assessed and the effect of the infusions and extract was determined towards α-glucosidase, α-amylase, and pancreatic lipase. The commercial herbal products were extracted separately with MeOH or hot water to obtain the extract/infusion for comparative studies. Total phenolic, total flavonoid and antioxidant capacity were assessed. The fingerprints of the MeOH extracts and infusions were compared by HPLD-DAD. The extract constituents were tentatively identified by HPLC-MS/MS and NMR analyses. From the extracts/infusions, 57 compounds were identified, including iridoids, phenylpropanoid glycosides, flavonoids, and caffeic acid derivatives, among others. The MeOH extracts and infusions showed strong inhibition towards α-glucosidase with IC₅₀ in the range of 0.13–0.84 µg/mL for the phenolic-enriched infusion extract (PEI) and 0.47–0.50 µg/mL for the MeOH extracts, respectively. The P. dulcis PEI showed higher inhibition towards α-glucosidase, and the MeOH extract of L. scaberrima was better than the PEI. At 100 µg/mL, the PEI from the four herbal teas reduces the activity of α-amylase by 23.03–28.61%, with L. javanica as the most active tea. Three of the species are high in phenylpropanoid glycosides, while P. dulcis contains rosmarinic acid. Some 26 compounds were identified in the infusion from B. saligna, 28 from L. scaberrima, and 21 from P. dulcis. Four of them are common in all the teas, namely decaffeoylverbascoside, verbascoside, isoverbascoside, and tuberonic acid hexoside. Ten compounds occur in two of the teas and seventeen, fifteen, and eleven compounds were detected only in B. saligna, L. scaberrima, and P. dulcis, respectively. Most of the compounds are reported for the first time from the crude drug infusions. The results give some support for the traditional use of herbal teas as digestives and/or indications for diabetes. The chemical fingerprints set the basis for quality control of the crude drugs, based on the main constituents and differential compounds occurring in the samples. Full article

Petit vert (scientific name: Brassica oleracea var. gemmifera DC. × Brassica oleracea var. acephala DC.) is a new variety of vegetable created by crossbreeding kale and brussel sprouts (Brassica oleracea species). The present study aimed to identify biologically active compounds in extracts of the outer leaves of Petit vert by purification and to examine their biological activities. The dried and powdered outer leaves of Petit vert were extracted, fractionated, and purified to isolate active compounds. Mass spectrometry (MS) was used to identify the compounds, and nuclear magnetic resonance (NMR) spectroscopy was performed to elucidate their structures. The compounds isolated from Petit vert leaves were glycosides that contained kaempferol, quercetin (flavonol), or sinapic acid (phenylpropanoid). Glucose uptake in cultured C2C12 murine myoblasts in the absence of insulin was significantly increased by these compounds, kaempferol, sinapic acid, and ferulic acid, while uptake in the presence of insulin was also significantly increased by compounds 3 and 4, kaempferol, and sinapic acid. The effect was not necessarily concentration-dependent, and some agents decreased the glucose uptake at higher concentrations. The present study reports for the first time the isolation of five compounds containing sinapic acid from the outer leaves of Petit vert and their stimulation of glucose uptake in cultured C2C12 murine myoblasts. The results obtained herein suggest the potential of these compounds to effectively attenuate hyperglycemia and maintain muscle strength by promoting glucose metabolism in muscle cells. Full article

About one-third of the global food supply is wasted. Brewers’ spent grain (BSG), being produced in enormous amounts by the brewery industry, possesses an eminence nutritional profile, yet its recycling is often neglected for multiple reasons. We employed integrated metagenomics and metabolomics techniques to assess the effects of enzyme treatments and Lactobacillus fermentation on the antioxidant capacity of BSG. The biotreated BSG revealed improved antioxidant capability, as evidenced by significantly increased (p < 0.05) radical scavenging activity and flavonoid and polyphenol content. Untargeted metabolomics revealed that Lactobacillus fermentation led to the prominent synthesis (p < 0.05) of 15 novel antioxidant peptides, as well as significantly higher (p < 0.05) enrichment of isoflavonoid and phenylpropanoid biosynthesis pathways. The correlation analysis demonstrated that Lactiplantibacillus plantarum exhibited strong correlation (p < 0.05) with aucubin and carbohydrate-active enzymes, namely, glycoside hydrolases 25, glycosyl transferases 5, and carbohydrate esterases 9. The fermented BSG has potential applications in the food industry as a culture medium, a functional food component for human consumption, and a bioactive feed ingredient for animals. Full article

Abiotic stress, especially drought stress, poses a significant threat to terrestrial plant growth, development, and productivity. Although mulberry has great genetic diversity and extensive stress-tolerant traits in agroforestry systems, only a few reports offer preliminary insight into the biochemical responses of mulberry leaves under drought conditions. In this study, we performed a comparative metabolomic and transcriptomic analysis on the “drooping mulberry” (Morus alba var. pendula Dippel) under PEG-6000-simulated drought stress. Our research revealed that drought stress significantly enhanced flavonoid accumulation and upregulated the expression of phenylpropanoid biosynthetic genes. Furthermore, the activities of superoxide dismutase (SOD), catalase (CAT) and malondialdehyde (MDA) content were elevated. In vitro enzyme assays and fermentation tests indicated the involvement of flavonol synthase/flavanone 3-hydroxylase (XM_010098126.2) and anthocyanidin 3-O-glucosyltransferase 5 (XM_010101521.2) in the biosynthesis of flavonol aglycones and glycosides, respectively. The recombinant MaF3GT5 protein was found to recognize kaempferol, quercetin, and UDP-glucose as substrates but not 3-/7-O-glucosylated flavonols and UDP-rhamnose. MaF3GT5 is capable of forming 3-O- and 7-O-monoglucoside, but not di-O-glucosides, from kaempferol. This implies its role as a flavonol 3, 7-O-glucosyltransferase. The findings from this study provided insights into the biosynthesis of flavonoids and could have substantial implications for the future diversified utilization of mulberry. Full article