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Orthosiphon stamineus Benth. (OSB) is a popular plant used for making "Shen tea" or "Java tea". It has been demonstrated with antioxidant, anti-inflammatory, and hepatoprotective activities. However, its potential beneficial effects and bioactive material basis for nonalcoholic fatty liver disease (NAFLD) has not been convincingly studied. In the present work, we conducted dual phytochemical/activity-guided extraction optimization and component fractionation of OSB, and evaluated its beneficial effects on NAFLD. Flavonoids and polyphenols (caffeic acid/protocatechuic acid derivatives) were determined as the dominant phytochemicals in OSB. The extraction process for these phytochemicals was optimized by using response surface methodology. Noticeably, flavonoids showed a stronger correlation with the antioxidant activities of OSB than polyphenols. Likewise, the flavonoid-rich fraction of OSB exerted antioxidant activities stronger than those of other fractions. As expected, in vitro and in vivo studies demonstrated that the flavonoid-rich fraction effectively attenuated weight increase, improved lipid metabolism, alleviated hepatic steatosis, and reversed hepatic inflammation. Importantly, this fraction showed equivalent beneficial effects to the total extract of OSB, suggesting that flavonoids were the main bioactive constituents of OSB. The action mechanism was indicated as direct antioxidant effect through chemical interaction with free radicals and indirect mitochondria-mediated antioxidant defense. Our research offers bioactive substances for further exploitation and expands the potential application of OSB.

Forsythiae Fructus (FF) is a widely used folk medicine in China, Japan, and Korea. The distribution of bioactive constituents throughout the fruit segments has rarely been addressed, although mounting evidence suggests that plant secondary metabolites are synthesized and distributed regularly. The phytochemical profiles of three segments of FF (pericarp, stalk and seed) were firstly revealed by liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based quantitative analysis of twenty-one bioactive constituents, including three phenylethanoid glycosides, five lignans, eight flavonoids, and five phenolic acids to explore the spatial distribution of bioactive constituents. Furthermore, the hierarchical clustering analysis (HCA) and one-way analysis of variance (one-way ANOVA) were conducted to visualize and verify the distribution regularity of twenty-one analytes among three segments. The results showed that phytochemical profiles of the three segments were similar, i.e., phenylethanoid glycosides covering the most part were the predominant compounds, followed by lignans, flavonoids and phenolic acids. Nevertheless, the abundance of twenty-one bioactive constituents among three segments was different. Specifically, phenylethanoid glycosides were highly expressed in the seed; lignans were primarily enriched in the stalk; flavonoids were largely concentrated in the pericarp, while the contents of phenolic acids showed no much difference among various segments. The research improves our understanding of distribution patterns for bioactive constituents in FF, and also complements some scientific data for further exploring the quality formation mechanism of FF., Competing Interests: The authors declare no conflicts of interest.

The demand for licorice and its natural product derivatives in domestic and foreign market is considerably huge. The core production areas of licorice are covered with salinity and drought land in northwestern China. Studies have shown that suitable environmental stress can promote the accumulation of glycyrrhizin and liquiritin to improve its quality as medicinal materials. However, there are few reports on other bioactive constituents of licorice, not to mention their dynamic accumulation under stressed conditions. To explore the quality formation of licorice from the perspective of salt influence, a reliable method based on ultra-fast liquid chromatography tandem triple quadrupole mass spectrometry (UFLC-MS/MS) was established for simultaneous determination of sixteen bioactive constituents, including triterpenoids, flavonoids, chalcones and their glycosides. Physiological experiments were performed to investigate salt tolerance of licorice under different salinity treatments. The expressions of crucial genes (bAS and CHS), key enzymes of triterpenoid and flavonoid synthesis, were also tested by qRT-PCR. Our study found that 50 mM NaCl treatment (low stress) was the most favorable to promote the accumulation of bioactive constituents in the long term, without harming the plants. Flavonoid accumulation of non-stressed and low-stressed groups became different in the initial synthesis stage, and glycosyltransferases may have great influence on their downstream synthesis. Furthermore, bAS and CHS also showed higher levels in low-stressed licorice at harvest time. This work provides valuable information on dynamic variations in multiple bioactive constituents in licorice treated by salt and insight into its quality formation under stressed conditions.

Background: Thesium chinense Turcz. (Named as Bai Rui Cao in Chinese) and its preparations (e.g., Bairui Granules) have been used to treat inflammatory diseases, such as acute mastitis, lobar pneumonia, tonsillitis, coronavirus disease 2019 (COVID-19), and upper respiratory tract infection. However, the material basis, pharmacological efficiency, and safety have not been illustrated. Methods: Anti-inflammatory activity-guided isolation of constituents has been performed using multiple column chromatography, and their structures were elucidated by NMR spectroscopy and ECD calculations. The inhibitory effects on lung inflammation and safety of the crude ethanol extract (CE), Bairui Granules (BG), and the purified active constituents were evaluated using lipopolysaccharide (LPS)-stimulated acute lung inflammation (ALI) mice model or normal mice. Results: Seven new compounds (1–7) and fifty-six known compounds (8–63) were isolated from T. chinense, and fifty-four were reported from this plant for the first time. The new flavonoid glycosides 1–2, new fatty acids 4–5, new alkaloid 7 as well as the known constituents including flavonoid aglycones 8–11, lignans 46–54, alkaloids 34 and 45, coumarins 57, phenylpropionic acids 27, and simple aromatic compounds 39, 44 and 58 exhibited anti-inflammatory activity. Network pharmacology analysis indicated that anti-inflammation of T. chinense was attributed to flavonoids and alkaloids by regulating inflammation-related proteins (e.g., TNF, NF-κB, TGF-β). Furthermore, constituents of T. chinense including kaempferol-3-O-glucorhamnoside (KN, also named as Bairuisu I, 19), astragalin (AG, Bairuisu II, 12), and kaempferol (KF, Bairuisu III, 8), as well as CE and BG could alleviate lung inflammation caused by LPS in mice by preventing neutrophils infiltration and the expression of the genes for pro-inflammatory cytokines NLRP3, caspase-1, IL-1β, and COX-2. After a 28-day subacute toxicity test, BG at doses of 4.875 g/kg and 9.750 g/kg (equivalent to onefold and twofold the clinically recommended dose) and CE at a dose of 11.138 g/kg (equivalent to fourfold the clinical dose of BG) were found to be safe and non-toxic. Conclusions: The discovery of sixty-three constituents comprehensively illustrated the material basis of T. chinense. T. chinense and Bairui Granules could alleviate lung inflammation by regulating inflammation-related proteins and no toxicity was observed under the twofold of clinically used doses. [ABSTRACT FROM AUTHOR]

The roots and rhizomes of Glycyrrhiza uralensis Fisch. represent the oldest and most frequently used herbal medicines in Eastern and Western countries. However, the quality of cultivated G. uralensis has not been adequate to meet the market demand, thereby exerting increased pressure on wild G. uralensis populations. Nitrogen, vital for plant growth, potentially influences the bioactive constituents of plants. Yet, more information is needed regarding the effect of different forms of nitrogen on G. uralensis. G. uralensis seedlings were exposed to a modified Hoagland nutrient solution (HNS), varying concentrations of nitrate (KNO3), or ammonium (NH4)2SO4. We subsequently obtained the roots of G. uralensis for physiology, transcriptomics, and metabolomics analyses. Our results indicated that medium-level ammonium nitrogen was more effective in promoting G. uralensis growth compared to nitrate nitrogen. However, low-level nitrate nitrogen distinctly accelerated the accumulation of flavonoid ingredients. Illumina sequencing of cDNA libraries prepared from four groups--treated independently with low/medium NH4+ or NO3- identified 364, 96, 103, and 64 differentially expressed genes (DEGs) in each group. Our investigation revealed a general molecular and physiological metabolism stimulation under exclusive NH4+ or NO3- conditions. This included nitrogen absorption and assimilation, glycolysis, Tricarboxylic acid (TCA) cycle, flavonoid, and triterpenoid metabolism. By creating and combining putative biosynthesis networks of nitrogen metabolism, flavonoids, and triterpenoids with related structural DEGs, we observed a positive correlation between the expression trend of DEGs and flavonoid accumulation. Notably, treatments with low-level NH4+ or mediumlevel NO3- positively improved primary metabolism, including amino acids, TCA cycle, and glycolysis metabolism. Meanwhile, low-level NH4+ and NO3- treatment positively regulated secondary metabolism, especially the biosynthesis of flavonoids in G. uralensis. Our study lays the foundation for a comprehensive analysis of molecular responses to varied nitrogen forms in G. uralensis, which should help understand the relationships between responsive genes and subsequent metabolic reactions. Furthermore, our results provide new insights into the fundamental mechanisms underlying the treatment of G. uralensis and other Glycyrrhiza plants with different nitrogen forms. [ABSTRACT FROM AUTHOR]

Tea is the second-most drank and refreshing beverage after water since the time immemorial. Tea harbours more than 700 bioactive compounds viz, different classes of polyphenols, unique amino acid L-Theanine, alkaloids (Caffeine, Theobromine), and Volatile Flavor Compounds (VFC). Tea's polyphenols make its inherent therapeutic potential unlimited. Tea's significance in managing cancer, diabetes, stomach ulcer, influenza, neurological diseases, etc. is well-documented. However, advantageous biochemical capabilities of tea have yet to be fully utilised. Hence, this review aims at to examine tea's variety, drinking habits, biochemistry, and therapeutic qualities. A number of significant online resources, including Google Scholar, Pub Med, Science Direct, and others, were searched for various research works on tea and its healthpromoting qualities by using keywords like tea, health benefits, bioactive components against diseases, etc. Current review highlighted that drinking a cup or more green tea is recommended for improving antioxidant status and to manage diabetes and obesity related problem. However after detailed review work on tea it become clear that not only green tea but also other varies of tea like black, white tea are also harbour lots of bioactive molecules since they are processed from same plant. Tea improves antioxidant status and manages diabetes and obesity. It also helps prevent and cure heart disease, malignancy, digestive dysfunction, and metabolic disorders including obesity and diabetes. Epigallocatechin Gallate (EGCG), found in tea, has been shown to reduce complications from Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-COV 2) infection. When taken in its traditional form to manage ailments, tea is sometimes controversialdue to a lack of confirming evidence of its benefits. The paper covers the numerous health advantages of tea, focusing on the specific components contributing to such benefits, and stresses the value of diverse brewing processes. [ABSTRACT FROM AUTHOR]

In our quest to discover advanced glycation end products (AGEs) inhibitors from Clinacanthus nutans (Burm.f.) Lindau leaves, we conducted a bioactivity-based molecular networking. This approach integrates LC-MS2 profiling and in vitro antiglycation data to predict bioactive compounds. We began by screening three extracts: 100% ethanol, 70% ethanol and 100% water alongside the in vitro antioxidant activity, total phenolics content (TPC) and schaftoside content. Among these extracts, 100% ethanol extract exhibited the highest total AGEs inhibition effects (IC 50 = 80.18 ± 11.6 μg/mL), DPPH scavenging activity (IC 50 = 747.40 ± 10.30 μg/mL) and TPC (26.54 ± 2.09 μg GAE /mg extract). Intriguingly, 100% ethanol extract contained the lowest amount of schaftoside, suggesting the involvement of other phytochemicals in the antiglycation effects. The molecular networking and in silico structural annotations of 401 LC-MS features detected in the fractions from 100% ethanol extract predicted 21 bioactive compounds (p < 0.05, r > 0.90), including several C 40 carotenoids, alkaloids containing tetrapyrrole structures and fatty acids. On the contrary, all phenolics showed weak correlations with antiglycation effects. These predictions were further validated in vitro, where carotenoid lutein showed half maximal inhibitory concentration, IC 50 = 96 ± 8 μM and selected flavonoid- C -glycosides exhibited weaker inhibitions (IC 50 between 568 and 1922 μM). Notably, lutein content was higher in freeze-dried leaves (12.42 ± 0.82 mg/100 g) than oven-dried, although the former was associated with elevated mercury levels. In summary, C. nutans exhibited potential antiglycation and antioxidant activity, and lutein was identified as the main bioactive principle. [Display omitted] [ABSTRACT FROM AUTHOR]

The aerial part of Artemisia absinthium, collected in Almaty region of Kazakhstan, investigated for chemical constituent with sufficiently completed quantitative and qualitative analysis. Biological active constituents such as organic acid (1.08%) and flavonoids (0.52%) together with the moisture content (7.14%), total ash (6.4%), and extractives (12.82%) of plant A. absinthium were determined. In the ash of the plant was found 8 macro-micro elements, main of them was K (417.930 μg/ml), Ca (116.0225 μg/ml), Mg (26.2250 μg/ml), Na (15.9825 μg/ml) by using the method of multi-element atomic emission spectral analysis at the Institute of Combustion Problems. Additionally, twenty amino acids and eight fatty acids were identified from A. absinthium. As the results showed that the major contents of amino acids were glutamate (2380 mg/100g), aspartate (1200 mg/100g) and alanine (712 mg/100g), and main contents of fatty acids were linoleic (44.8%) and oleic (30%) acids, relatively. [ABSTRACT FROM AUTHOR]

• Tibet sea buckthorn is a valuable source of natural functional ingredients. • Antioxidant activity of leaf extracts was higher than that of fruit extracts. • Contents of flavonoids, phenolics, and polysaccharides varied monthly. • Meteorological factors affected polysaccharide and flavonoid contents. • The best harvest month differed for different target components. Sea buckthorn, a medicinal and edible plant, is rich in flavonoids, phenolics, and polysaccharides. We detected monthly variations in the contents of three types of active compounds and the antioxidant activity of leaf and fruit extracts, and explored the effects of meteorological factors on active component contents. The highest flavonoid content in leaves and fruits was in July, and this did not coincide with the maximum contents of phenolics and polysaccharides. Compared with fruit extracts, leaf extracts showed higher antioxidant activity in the DPPH radical scavenging assay, the ferric ion reducing antioxidant power assay, and the total radical trapping antioxidant parameter assay. We detected significant correlations between some meteorological factors and the contents of bioactive components. The results reveal variations in the contents of bioactive components in sea buckthorn throughout the growing season in southeastern Tibet, and reveal the best time to harvest materials for optimum resource use. [Display omitted] [ABSTRACT FROM AUTHOR]

A novel quantitative method using high-performance liquid chromatography coupled to electrospray ionization tandem mass spectrometry was developed for simultaneous determination of the 16 important bioactive constituents including nine coumarins, and seven flavonoids in Common cnidium fruit samples from different regions. The separation was performed on a C 18 column with linear gradient elution of acetonitrile and 0.1% acetic acid at a flow rate of 1.0 ml/min in 15 min. Quantification of the analytes was achieved by use of a hybrid quadrupole linear ion-trap mass spectrometer. Multiple-reaction monitoring scanning was employed with switching electrospray ion source polarity between positive and negative modes in a single run. The validation results of the method indicated that the method was simple, rapid, specific, and reliable. The results demonstrated that the quantitative difference in content of 16 bioactive constituents was useful not only for chemotaxonomy of many samples from different sources but also for the standardization and differentiation of many similar samples. Simultaneous quantification of bioactive components by high performance liquid chromatography–tandem mass spectrometric method would be a well acceptable strategy to comprehensively control the quality of C. cnidium fruit . [ABSTRACT FROM AUTHOR]

Since ancient times, herbs have been used as natural remedies for curing many physiological disorders. Traditional medicinal literature appreciated their value as nature's gift to mankind for the healing of illnesses. Some of the herbs have also been used for culinary purposes, and few of them have been used in cheese manufacture both as coagulating agents and flavor ingredients. Scientific investigations regarding biological activity and toxicity of chemical moieties present in many herbs have been carried out over a period of time. Consequently, literature related to the use of herbs or their functional ingredients in foods and their interaction with food constituents has been appearing in recent times. This article presents the information regarding some biologically active constituents occurring in commonly used herbs, viz., alkaloids, anthraquinones, bitters, flavonoids, saponins, tannins, and essential oils, their physiological functionalities, and also the description of few herbs of importance, viz., Asparagus racemosus, Withania somnifera, Bacopa monniera, Pueraria tuberose, Emblica officinalis, Terminalia chebula, Terminalia belerica, Terminalia arjuna, and Aloe vera, in terms of their chemical composition, biological functionality, and toxicity. This article also reviews the use of herbs and their active ingredients in foods and their interactions with different food constituents. [ABSTRACT FROM AUTHOR]

Hypericum perforatum(Hp) extracts contain many different classes of constituents including flavonoids and biflavonoids, phloroglucinols, naphthodianthrones, caffeic acid derivatives, and unknown and/or unidentified compounds. Many constituents may be responsible for the anti-inflammatory activity of Hp including quercetin and derivatives, hyperforin, pseudohypericin, and amentoflavone. In line with antidepressant data, it appears that the interactions of constituents may be important for the anti-inflammatory activity of Hp. Interactions of constituents, tested in bioavailability models, may explain why synergistic mechanisms have been found to be important for antidepressant and antiproliferative bioactivities. This review highlights the relationship among individual constituents and the anti-inflammatory activity of Hp extracts and proposes that interactions of constituents may be important for the anti-inflammatory activity of botanical extracts, although the exact mechanisms of the interactions are still unclear. [ABSTRACT FROM PUBLISHER]

As the largest jujube cultivating areas of the world, the market price and quality of Chinese jujube are obviously affected by its producing regions in China. Therefore, traceability of Chinese jujube has become an important issue. To search the suitable geographical labels of Chinese jujube, 26 major cultivars from five geographical regions of China were investigated by evaluating their bioactive compounds and antioxidant activity profiling. Multivariate statistical techniques (e,g., PCA, PLS, VIP value) applied to the above-obtained data were further used to identify geographical origin in different areas of Chinese jujube. The results indicated that the highest median contents of total phenols (TP) and flavonoids (TF) of Chinese jujube were originated from Ningxia and Henan provinces, both of which also exhibited the stronger bioactivity. p -Hydroxybenzoic acid and rutin exhibited the highest contents among the all detected individual phenolic compounds. The highest median contents of cyclic adenosine monophosphate (cAMP), cyclic guanosine monophosphate (cGMP) and polysaccharides were all found in Chinese jujube samples of Xinjiang province. In particular, p -hydroxybenzoic acid, rutin, cAMP, cGMP and polysaccharides can be regarded as the potential biomarkers in distinguishing the geographical origin of Chinese jujube. Additionally, the high altitude and latitude might be benefit for the accumulation of cAMP, cGMP and polysaccharides (primary metabolites), and high longitude and annual precipitation maybe improve the contents of TP and TF (secondary metabolites). These information could provide an effective methods in distinguishing the geographical features of Chinese jujube, and also be benefit for the products development. • Five bioactive compounds could be regarded as the biomarkers of Chinese jujube. • High altitude and latitude was benefit for primary metabolites accumulation. • High longitude and annual precipitation improve secondary metabolites contents. [ABSTRACT FROM AUTHOR]