Main Flavonoid Compounds Research Articles

Anti-Neuroinflammatory Effect of Ombuin from Rhamnus erythroxylon Pall. Leaves in LPS-Induced BV-2 Microglia by Targeting Src and Suppressing the PI3K-AKT/NF-κB Signaling Pathway.

The leaves of Rhamnus erythroxylon Pall. are widely used as tea substitutes in northwest China for their fragrant aroma, anti-irritability, and digestion-enhancing properties. Ombuin, a main flavonoid compound found in the leaves, exhibited notable anti-inflammatory and antioxidant effects. However, its potential role in treating neuroinflammatory-related diseases remains unexplored. Thus, this study aims to evaluate the anti-neuroinflammatory effects of ombuin and to explore the underlying molecular mechanisms. According to our findings, ombuin dramatically reduced the release of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), IL-1β, nitric oxide (NO), and reactive oxygen species (ROS) in lipopolysaccharide (LPS)-stimulated BV-2 microglia. Further analysis, including transcriptomics, network pharmacology, molecular docking, and cellular heat transfer assays, revealed that Src was a direct target of ombuin. Western blot analysis showed that ombuin effectively suppressed Src phosphorylation and inhibited the downstream expressions of p-PI3K p85, p-AKT1, p-IKKα/β, p-IκBα, and nuclear factor κB (NF-κB). Meanwhile, the repression of Src significantly reversed the anti-neuroinflammatory activity of ombuin. Our results identified Src as a direct target of ombuin and implied that ombuin exerted an anti-neuroinflammatory effect by inhibiting Src phosphorylation and suppressing the activation of the PI3K-AKT and NF-κB pathways, which might provide an alternative therapeutic strategy for neurodegenerative diseases.

Anti-diabetes and neuroprotection potential and primary safety studies of Isatis tinctoria L. hydroalcoholic leaf extract

PurposeNatural plant raw materials, previously underestimated in therapeutics, are becoming the subject of research for new applications in medicine. In our research, the hydroalcoholic extract of Isatis tinctoria leaf, rich in flavonoid compounds such as vicenin-2 and quercetin, was examined as a potential antidiabetic and neuroprotective agent. MethodsThe effect of the extract and its main flavonoid compounds on protein glycation, alpha-glucosidase activity, and acetylcholinesterase activity was tested. In vitro, in the mouse hippocampal neuronal cell line and in vivo, using a mouse model, the safety of the extract was screened for. ResultsOur experiments demonstrated significant inhibition of protein glycation, alpha-glucosidase activity, acetylcholinesterase activity, and β-amyloid aggregation by the extract, in a concentration-dependent manner. The extract had a strong reducing effect and did not exhibit cytotoxicity up to a concentration of 25 mg/mL. Intraperitoneal administration of the extract to mice did not have negative effects on body mass, locomotor activity, coordination, and liver cell integrity. ConclusionsOur research sheds new light on this raw material and deepens knowledge of its activity. This may result in the recognition of its therapeutic effects and even in its introduction in the modern treatment of diseases characterized by pathological changes associated with hyperglycemia, oxidation, and inflammation.

Extraction of phenolic and flavonoid compounds and evaluation of their antioxidant activity in saffron anthers (Crocus sativus L.)

Saffron (Crocus sativus L.) is the most expensive spice in the world and rich in a variety of bioactive compounds including phenolic acids, flavonoids, and vitamins. Saffron is used in food, cosmetics, perfumery, and dye industries due to its color, taste, aroma, and medicinal properties. The extraction of bioactive compounds imposes a constant search for economically and environmentally viable extraction strategies for higher yields including the solvent type. The research was carried out to evaluate total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity of C. sativus L. anthers using different extraction solvents including ethanol, methanol, and distilled water. The results showed that ethanol was the most effective extraction solvent type exhibiting the highest TPC (7.29 mg GAE g-1 DW), TFC (3.77 mg QE g-1 DW), and antioxidant activity of flavonoids (88%) and ascorbic acid (76.07%). Flavonoids proved to be stronger antioxidants than ascorbic acid, irrespective of solvent type, however the ethanolic extracts showed significantly higher antioxidant activity. A Reverse Phase High-Performance Liquid Chromatography method revealed that gallic acid (3.1 mg g-1), syringic acid (0.2 mg g-1), and vanillic acid (0.13 mg g-1) were the main phenolic compounds detected in the dried anther ethanolic extracts, while quercetin (2.13 mg g-1), pyrogallol (1.73 mg g-1), kaempferol (1.2 mg g-1), rutin (0.2 mg g-1), and tricin (0.1 mg g-1) the main flavonoid compounds. Thus, apart from the spice, constituted by the red stigmas, the production of other flower parts such as the anthers, so far considered agricultural waste can constitute a rich source of bioactive compounds of high antioxidant potential by setting quality standards for new products’ development and ensuring better valorization of saffron’s bioresidues in Mashhad region of Iran.

Miquelianin, a main functional flavonoid of lotus leaf, induces thermogenic signature via p38‐PINK1‐PARKIN‐mediated mitophagy and mimicking NRF2 signaling during brown adipocyte differentiation

AbstractAdipocytes thermogenesis is an important mechanism for increasing energy expenditure. Here, screening of thermogenic activators (Sirt1 and Ucp1) investigated in C3H10T1/2 cells revealed ethanol extract of lotus leaf (LLE) may exert higher activity compared with that of the other 11 ingredients. UPLC‐MS/MS analysis showed that miquelianin was identified as the main flavonoid compounds in LLE (12.8%) and therefore deserves further investigation. The results in C3H10T1/2 cells revealed miquelianin promoted lipolysis, enhanced thermogenic programming (Sirt1, Ppargc1a, Prdm16, Cox7a, Nrf1, Cox2, and Ucp1), and induced brown‐like adipocyte formation (Fgf21, Cd137, Tmem26, Tbx1, Cd40, and Cited1). Moreover, miquelianin increased mitochondrial abundance, mitochondrial membrane potential, and NAD+/NADH ratio, suggesting its potential in mitochondria activity. We also observed that miquelianin improved mitochondrial quality by the establishment of mitochondrial dynamics (Mfn1, Mfn2, Opa1, Drp1, and Fis1) and subsequent suppression of autophagy. Chemical inhibition experiment revealed miquelianin may trigger browning via p38‐PINK1‐PARKIN‐mediated mitophagy. Furthermore, in ML385‐treated cells, NRF2, HMOX1, TFAM, and UCP1 were compromised by miquelianin treatment, suggesting that NRF2 signaling is necessary during miquelianin‐induced mitochondria biogenesis. Together, our findings demonstrate that miquelianin may induce browning and mitochondria thermogenic programing by suppressing mitophagy via p38‐PINK1‐PARKIN and mimicking NRF2 signaling.

Baicalin Alleviates Silica-Induced Lung Inflammation and Fibrosis by Inhibiting TLR4/NF-κB Pathway in Rats

Silicosis is an occupational lung disease caused by inhaling silica dust. The disease is characterized by early lung inflammation and late irreversible pulmonary fibrosis. Here we report the effect of Baicalin, a main flavonoid compound from the roots of Chinese herbal medicine Huang Qin on silicosis in a rat model. Results showed Baicalin (50 or 100 mg/kg/day) can mitigate the silica-induced lung inflammation and reduce the harm of alveolar structure and the blue region of collagen fibers in rat lung at 28 days after administration. At the same time, Baicalin also diminished the level of interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and transforming growth factor-β1 (TGF-β1) in lung tissues. The protein expression of collagen I (Col-1), α-smooth muscle actin (α-SMA) and vimentin were down-regulated while E-cadherin (E-cad) was increased in Baicalin-treated rats. In addition, the Toll Like Receptor 4 (TLR4)/ nuclear factor kappaB (NF-κB) pathway was enabled at 28 days after silica infusion, and the treatment of Baicalin diminished the expression of TLR4 and NF-κB in the lungs of rat with silicosis. These results suggested that Baicalin inhibited the pulmonary inflammatory and fibrosis in a rat model of silicosis, which could be attributed to inhibition of the TLR4/NF-κB pathway.

A Study of Polyphenolic Compounds and in vitro Antioxidant Activity of Trianthema portulacastrum Linn. Extracts

Background: Trianthema portulacastrum Linn. is an exotic plant growing as weed in Africa, Southeast Asia and tropical America. Chemical fingerprinting under the present study was undertaken to characterize the polyphenolic compounds and antioxidant activities present in the plant. Methods: Several in vitro antioxidant assays were performed to evaluate the antioxidant activities in aqueous, alcoholic and hydro-alcoholic extracts. Characterization of polyphenolic compounds was done by HPLC and GCMS analyses. Result: Total phenols, flavonoids and total antioxidant activity as assessed by DPPH, ABTS and total antioxidant capacity assays was found to be maximum in hydroethanolic extract of the plant. HPLC analysis confirmed the presence of gallic acid, protocatechuic acid, catechin hydrate, vanillic acid, epicatechin, p-coumaric acid, rutin, salicylic acid, myricetin, quercetin and trans-cinnamic acid in plant extracts being maximum in hydroethanolic followed by aqueous, hydromethanolic, ethanolic and then methanolic extracts. Catechin, epicatechin, rutin, myricetin and quercetin were main flavonoid compounds in most of the plant extracts. GCMS analysis also confirmed the presence of several other antioxidants. Based on the findings of the phytochemical analyses and in vitro antioxidative studies, it can be clearly established that Trianthema portulacastrum has rich amounts of potent polyphenolic and flavonoid compounds having antioxidant properties.

Effect of Skin Melinjo Extract (Gnetum Gnemon) On Expression URAT1 and GLUT9 Genes In Hyperuricemia

Hyperuricemia is defined as a metabolic syndrome disease with markers characteristic of uric acid production that exceed normal limits. Normal uric acid levels range from 3.4-7.0 mg/dl in adult men and 2.4 -6.0 mg/dl in adult women. So if uric acid levels exceed the normal limit, it will cause uric acid can not be fully metabolized and cause hyperuricemia. About 70% of uric acid is excreted through the kidneys. The kidneys are therefore organs that have an important role in maintaining uric acid levels and uric acid homeostasis in general, through complex molecular mechanisms. Reabsorption of uric acid that occurs in the kidneys by URAT1 and GLUT9 has an important role in uric acid levels in the human body, where uric acid is reabsorbed by the kidneys will then be flowed back into the blood so that it affects the levels of uric acid in the human body. Preliminary data showed that ethanol extract of melinjo skin contains 3 main Flavonoid compounds that have a higher Binding affinity value compared to allopurinol, so it has a higher effect in overcoming uric acid levels.

Honey and Alzheimer's Disease-Current Understanding and Future Prospects.

Alzheimer's disease (AD), a leading cause of dementia, has been a global concern. AD is associated with the involvement of the central nervous system that causes the characteristic impaired memory, cognitive deficits, and behavioral abnormalities. These abnormalities caused by AD is known to be attributed by extracellular aggregates of amyloid beta plaques and intracellular neurofibrillary tangles. Additionally, genetic factors such as abnormality in the expression of APOE, APP, BACE1, PSEN-1, and PSEN-2 play a role in the disease. As the current treatment aims to treat the symptoms and to slow the disease progression, there has been a continuous search for new nutraceutical agent or medicine to help prevent and cure AD pathology. In this quest, honey has emerged as a powerful nootropic agent. Numerous studies have demonstrated that the high flavonoids and phenolic acids content in honey exerts its antioxidant, anti-inflammatory, and neuroprotective properties. This review summarizes the effect of main flavonoid compounds found in honey on the physiological functioning of the central nervous system, and the effect of honey intake on memory and cognition in various animal model. This review provides a new insight on the potential of honey to prevent AD pathology, as well as to ameliorate the damage in the developed AD.

Molecular mechanisms and promising role of dihydromyricetin in cardiovascular diseases

Vine tea, a Chinese herbal medicine, is widely used in traditional Asian medicine to treat common health problems. Dihydromyricetin (DMY) is the main functional flavonoid compound extracted from vine tea. In recent years, preclinical studies have focused on the potential beneficial effects of dihydromyricetin, including glucose metabolism regulation, lipid metabolism regulation, neuroprotection, and anti-tumor effects. In addition, DMY may play a role in cardiovascular disease by resisting oxidative stress and participating in the regulation of inflammation. This review is the first review that summaries the applications of dihydromyricetin in cardiovascular diseases, including atherosclerosis, myocardial infarction, myocardial hypertrophy, and diabetic cardiomyopathy. We also clarified the underlying mechanisms and signaling pathways involved in the above process. The aim of this review is to provide a better understanding and quick overview for future researches of dihydromyricetin in the field of cardiovascular diseases, and more detailed and robust researches are needed for evaluation and reference.

Pectolinarigenin shows lipid-lowering effects by inhibiting fatty acid biosynthesis in vitro and in vivo.

Pectolinarigenin is the main flavonoid compound and presents in Linaria vulgaris and Cirsium chanroenicum. In this study, RNA sequencing (RNA-seq) was applied to dissect the effect of pectolinarigenin on the transcriptome changes in the high lipid Huh-7 cells induced by oleic acid. RNA-seq results revealed that 15 pathways enriched by downregulated genes are associated with cell metabolism including cholesterol metabolism, glycerophospholipid metabolism, steroid biosynthesis, steroid hormone biosynthesis, fatty acid biosynthesis, etc. Moreover, 13 key genes related to lipid metabolism were selected. Among them, PPARG coactivator 1 beta (PPARGC1B) and carnitine palmitoyltransferase 1A (CPT1A) were found to be upregulated, solute carrier family 27 member 1(SLC27A1), acetyl-CoA carboxylase alpha (ACACA), fatty-acid synthase (FASN), 3-Hydroxy-3-Methylglutaryl-CoA Reductase (HMGCR), etc. were found to be downregulated. Glycolysis/gluconeogenesis, steroid hormone biosynthesis, and fatty acid biosynthesis were all significantly downregulated, according to gene set variation analysis and gene set enrichment analysis. Besides, protein levels of FASN, ACACA, and SLC27A1 were all decreased, whereas PPARγ and CPT1A were increased. Docking models showed that PPARγ may be a target for pectolinarigenin. Furthermore, pectolinarigenin reduced serum TG and hepatic TG, and improved insulin sensitivity in vivo. Our findings suggest that pectolinarigenin may target PPARγ and prevent fatty acid biosynthesis.

DETERMINATION OF TOTAL CARBOHYDRATES, FLAVONOIDS, ORGANIC ACIDS, MACRO-AND MICROELEMENTS IN WOLFBERRY (LYCIUM BARBARUM L.) FRUIT CULTIVATED IN ALBANIA

Objective: The purpose of the study is to determine the biological activity components content of wolfberry (Lycium Barbarum L.) fruit originating from Albania. To unify the requirements for quality control of medicinal plant raw materials, it is advisable to study the qualitative composition and quantitative content of the components of this plant that determine the complexity of biological action-anti-inflammatory, neuroprotective, anti-cancer, vision-improving, and reproduction-enhancing effects. Methods: Lycium barbarum L. fruits were analyzed for the content of total carbohydrates and fructans by spectrophotometry method. The organic acids, one flavonoid, and one scopoletin were identified and quantified by the HPLC method. Macro-and microelements were analyzed by ICP-OES. Results: The results of the spectrophotometric analysis showed that total carbohydrate content and fructans content lie in the range of 21.763%-70.384% and 19.90-20.25%. Rutin, the main flavonoid compound in Lycium barbarum L. fruits, and scopoletin, a coumarin compound, contents lie respectively in the range of 2.10–5.48 mg/g and 0.48-0.76 mg/g. Potassium (K) is the predominant element in fruits, the content of which was 6740.75 μg/g. Conclusion: Lycium barbarum L. fruit is a rich source of important biologically active substances. Further, the resulting data are going to be used to establish a monograph for Lycium barbarum L. fruits.

The effect of Melissa officinalis L. extract on learning and memory: Involvement of hippocampal expression of nitric oxide synthase and brain-derived neurotrophic factor in diabetic rats

Ethnopharmacological relevanceDiabetes is a systemic disease, which can cause synaptic defects in the hippocampus. Hippocampus plays a crucial role in learning and memory. Melissa officinalis L. has been used as for memory enhancement in Persian Medicine. Aim of the studyThe aim of this study was to evaluate the impact of the hydroalcoholic extract of Melissa officinalis L. on learning and memory, considering its impact on nitric oxide synthase and brain-derived neurotrophic factor expression in the hippocampus of diabetic rats. Materials and methodsMelissa officinalis L. extract was obtained by maceration method. To evaluate phenolic and flavonoid compounds of the extract, the samples were analyzed by HPLC. The animals were randomly divided into 6 groups: vehicle-treated control, Melissa officinalis-treated control (50 mg/kg), vehicle-treated diabetic, and M. officinalis-treated diabetic (25, 50, or 100 mg/kg). Diabetes was induced by streptozotocin And Melissa officinalis L. was administered for 2 weeks once diabetes was induced. Passive avoidance and Y-maze tasks were performed for learning and memory assessment. At the end of learning and memory tasks, rats were sacrificed and their hippocampus removed, lysed, and homogenized. The RNA contents were purified and then used as the template for cDNA synthesis. Real-time PCR was used to evaluate nitric oxide synthase and brain-derived neurotrophic factor genes expression. ResultsRutin was main flavonoid compound and rosmarinic acid was the main phenolic compound of the Melissa officinalis extract. Streptozotocin induced diabetes and impaired learning and memory in diabetic rats. Melissa officinalis treated-control group showed a higher alternation score in the Y-maze task and step-through latency in the passive avoidance task compared to the vehicle treated diabetic group. Melissa officinalis-treated rats showed a higher alternation score in the Y-maze task in all doses compared to the vehicle treated diabetic group (P < 0.05). In addition, in the passive avoidance task Melissa officinalis increased step-through latency (P < 0.05) but not initial latency, in all doses. Furthermore, in diabetic rats, the expression of brain-derived neurotrophic factor and nitric oxide synthase genes decreased. However, hippocampal brain-derived neurotrophic factor and nitric oxide synthase gene expression was increased in Melissa officinalis-treated rats compared to diabetic rats (P < 0.05). ConclusionsMelissa officinalis improved learning and memory in diabetic rats, which may have occurred by increasing brain-derived neurotrophic factor and nitric oxide synthase gene expression.

Ecofriendly Bioagents, Parthenocissus quinquefolia, and Plectranthus neochilus Extracts to Control the Early Blight Pathogen (Alternaria solani) in Tomato

Background: early blight disease caused by Alternaria solani is one of the most destructive diseases of the tomato, reducing tomato production globally. Methods: four fungal isolates were collected from four tomato cultivars and identified through morphological characterization and polymerase chain reaction (PCR) amplification of the internal transcript spacer (ITS) region. Plectranthus neochilus and Parthenocissus quinquefolia methanol extracts and the bioagents Trichoderma viride and Pseudomonas fluorescens were used as antifungal agents in vitro and in vivo and compared with chlorothalonil, a reference chemical fungicide. HPLC analysis of the plant extracts was used to identify the main flavonoid compounds, namely, rutin and myricetin. Results: molecular characterization showed that the fungal isolates belonged to A. solani. The results of in vitro antifungal activity studies revealed that chlorothalonil, at a concentration of 2500 mg/L, showed the highest inhibition percentage of fungal growth (IPFG) against A. solani (84.4%), followed by the bioagents T. viride and P. fluorescens, with IPFG values of 72.9% and 67.9%, respectively. Moderate to weak activity was found against A. solani when P. neochilus and P. quinquefolia extracts were applied at a concentration of 2500 mg/L, with an IPFG value of 54% for both extracts. The results of in vivo spray application showed that T. viride and chlorothalonil, as well as P. fluorescens, significantly reduced the disease index of early blight, and followed by the P. neochilus and P. quinquefolia extracts. By HPLC, the flavonoid compounds rutin and myricetin were identified in P. neochilus (leaf) with amounts of 2429.60 and 75.92 mg/100 g of extract, and in P. quinquefolia (fruit), with amounts of 1891.60 and 241.06 mg/100 g of extract, respectively. Conclusions: the results of the bioactivity of plant extracts and the bioagents indicate a vital role as antifungal activity against A. solani.

Determining the adsorption and desorption properties of flavonoids found in Eucommia ulmoides Oliv. leaves using macroporous resin and acetylcholinesterase inhibitor screening

The adsorption and desorption properties of 12 resins containing flavonoid compounds found in Eucommia ulmoides Oliv. leaves (EUOL) extracts were investigated. The static adsorption and desorption, kinetic, adsorption, and thermodynamic properties of the adsorption of the flavonoids onto macroporous resins were determined. The HPD-300, NKA-9, and AB-8 resins exhibited a greater adsorption capacity and desorption characteristics. A pseudo-second-order kinetic model was suitable to characterize the kinetics of the adsorption of flavonoids onto the resins selected, and the diffusion of flavonoids was divided into three stages, with the boundary layer diffusion and intra-particle diffusion being the rate-controlling factors. The Langmuir model was found to be the best description of the adsorption behavior of flavonoids. Thermodynamic studies indicated that the adsorption of flavonoids was a physical, exothermic, and spontaneous process. The 60% ethanol eluted fraction from the NKA-9 resin column not only had the highest flavonoid content, but also possessed the strongest inhibitory effect on acetylcholinesterase. In addition, the degree of binding of the main flavonoid compounds found in the EUOL to acetylcholinesterase compounds was investigated via molecular docking technology. The results showed that the docking total score of isoquercetin and enzyme proteins were the highest, followed by kaempferol-3-O-rutinoside.

In Vitro Evaluation of Antidiabetic and Anti-Inflammatory Activities of Polyphenolic-Rich Extracts from Anchusa officinalis and Melilotus officinalis.

This study was focused on the phytochemical composition and biological activities of Anchusa officinalis and Melilotus officinalis polyphenolic-rich extracts obtained by nanofiltration. The high-performance liquid chromatography–mass spectrometry analysis showed that chlorogenic acid and rosmarinic acid were the main phenolic acids in both extracts. The main flavonoid compound from A. officinalis extracts is luteolin, whereas rutin and isoquercitrin are the main flavonoids in M. officinalis. M. officinalis polyphenolic-rich extract had the highest α-amylase (from hog pancreas) inhibitory activity (IC50 = 1.30 ± 0.06 μg/mL) and α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity (IC50 = 92.18 ± 1.92 μg/mL). However, both extracts presented a significant α-glucosidase inhibitory activity. Furthermore, the hyaluronidase inhibition of polyphenolic-rich extracts also proved to be stronger (IC50 = 11.8 ± 0.1 μg/mL for M. officinalis and 36.5 ± 0.2 μg/mL for A. officinalis), but there was moderate or low lipoxygenase inhibition. The studies on the fibroblast cell line demonstrated that both A. officinalis and M. officinalis polyphenolic-rich extracts possess the cytotoxic effect at a concentration higher than 500 μg/mL. The experimental data suggest that both extracts are promising candidates for the development of natural antidiabetic and anti-inflammatory food supplements.

Liquiritin, a novel inhibitor of TRPV1 and TRPA1, protects against LPS-induced acute lung injury

TRPV1 and TRPA1 are cation channels that play key roles in inflammatory signaling pathways. They are co-expressed on airway C-fibers, where they exert synergistic effects on causing inflammation and cough. Licorice, the root of Glycyrrhiza uralensis, has been widely used in China as an anti-inflammatory and anti-coughing herb. To learn if TRPV1 and TRPA1 might be key targets of the anti-inflammatory and antitussive effects of licorice, we examined liquiritin, the main flavonoid compound and active ingredient of licorice, on agonist-evoked TRPV1 and TRPA1 activation. Liquiritin inhibited capsaicin- and allyl isothiocyanate-evoked TRPV1 and TRPA1 whole-cell currents, respectively, with a similar potency and maximal inhibition. In a mouse acute lung injury (ALI) model induced by the bacterial endotoxin lipopolysaccharide, which involves both TRPV1 and TRPA1, an oral gavage of liquiritin prevented tissue damage and suppressed inflammation and the activation of NF-κB signaling pathway in the lung tissue. Liquiritin also suppressed LPS-induced increase in TRPV1 and TRPA1 protein expression in the lung tissue, as well as TRPV1 and TRPA1 mRNA levels in cells contained in mouse bronchoalveolar lavage fluid. In cultured THP-1 monocytes, liguiritin, or TRPV1 and TRPA1 antagonists capsazepine and HC030031, respectively, diminished not only cytokine-induced upregulation of NF-κB function but also TRPV1 and TRPA1 expression at both protein and mRNA levels. We conclude that the anti-inflammatory and antitussive effects of liquiritin are mediated by the dual inhibition of TRPV1 and TRPA1 channels, which are upregulated in nonneuronal cells through the NF-κB pathway during airway inflammation via a positive feedback mechanism.

Radix Tetrastigma extract from different origins protect RAW264.7 macrophages against LPS-induced inflammation.

Radix Tetrastigma (RT) is a medicinal plant and functional food in China, distributed in various places in the south of China. Radix Tetrastigma extract (RTE) from different origins were collected and analyzed for their anti-inflammatory effects. Different RTEs showed different abilities to suppress shape deformation, decrease the nitric oxide (NO) production, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in RAW 264.7 cells. Subsequently, their bioactive components were compared, and results showed RTEs are rich in flavonoid (85.25-436.70mg RE/g DW), polysaccharides (100.45-349.26mg glucose/g DW), phenolic (12.92-225.40mg GAE/g DW) and protein contents (4.429-7.719mg/g DW). Principal component analysis (PCA) and correlation studies indicated that anti-inflammatory capacity could be more associated with total flavonoid contents. High-performance liquid chromatography (HPLC) and Ultraperformance liquid chromatography-time-of flight mass spectrometry (UPLC-TOF/MS) analysis were conducted, and results showed that rutin, isoquercitrin, kaempferol-3-O-rutinoside and astragalin were main flavonoid compounds, among them astragalin exhibited a prior protective effect, suggesting it might be responsible for RTE's excellent anti-inflammatory capacity.

Campomanesia genus – a literature review of nonvolatile secondary metabolites, phytochemistry, popular use, biological activities, and toxicology

The genus Campomanesia belongs to the Myrtaceae family and has about 30 species. It is characterized by citrus-flavored fruits. Several articles describe the extensive use of its fruit, such as in the food industry, however, other parts of the plants are also used for food or pharmacological purposes such as the leaves, flowers, seeds, and roots. Analyzing works published on the genus in the period 2005-2019, we observed that the classes of main flavonoid compounds present are anthocyanins, chalcones, coumarins, tannins, and saponins. Species of this genus are also used as a medicine in the treatment of wounds, toothaches, fractures, and bruises. Therapeutic activities have also been detected for Campomanesia, such as antimicrobial, antiulcerogenic, antiprotozoal, anti-inflammatory, and antidiarrheal activity, antiproliferative and antioxidant potential, antiplatelet, antithrombotic, and fibrinolytic activities, as well as hypotensive effects. There are a small number of works demonstrating the low toxic potential of plant extracts. Thus, the Campomanesia genus presents pharmacological potential to be explored.

Vitexin attenuates myocardial ischemia/reperfusion injury in rats by regulating mitochondrial dysfunction induced by mitochondrial dynamics imbalance

Vitexin (VT) is a main bioactive flavonoid compound derived from the dried leaf of hawthorn (Crataegus pinnatifida), a widely used Chinese traditional folk medicine. Recent studies have shown that vitexin presents cardioprotective effects in vivo and in vitro. Mitochondrial dysfunction is a salient feature of myocardial ischemia/reperfusion (I/R) injury (MIRI), but the potential mechanism is still unclear. This study investigated the cardioprotective effect of vitexin against MIRI and its possible mechanism. Isolated SD rat hearts were subjected to MIRI in a Langendorff perfusion system, and H9c2 cells were subjected to hypoxia/reoxygenation (H/R) in vitro. Ex vivo experiments showed improved left ventricular function and reduced infarct size in the vitexin group. Transmission electron microscopy showed that I/R caused outer mitochondrial membrane rupture, cristae disappearance and vacuolation, while vitexin reduced mitochondrial damage and ultimately reduced cardiomyocyte apoptosis. In vitro, vitexin protected H9c2 cells from H/R-induced mitochondrial dysfunction, significantly reducing ROS levels; improving mitochondrial activity, mitochondrial membrane potential and ATP content; markedly increasing MFN2 expression and reducing the recruitment of Drp1 in mitochondria. These results suggest a new protective mechanism of vitexin for ischemic heart disease treatment.

Effects of high pressure extraction on the extraction yield, phenolic compounds, antioxidant and anti-tyrosinase activity of Djulis hull.

The hulls of Djulis (Chenopodium formosanum) are a type of agricultural waste. Using 70% ethanol as the extraction solvent, this study compared the extraction yields of high-pressure-assisted extraction (HPE) and conventional oscillation extraction (CE) for Djulis hulls (DH). The total phenolic and flavonoid contents, and antioxidant, anti-inflammatory and anti-tyrosinase activities were also compared. Our findings indicated that 600MPa/5min of HPE resulted in higher total phenolic (567-642mgGAE/g) and flavonoid (47.2-57.2mgQU/g) concentrations; gallic acid (44.5-53.2μg/g) and rutin (26.8-34.2μg/g) were the main phenolic and flavonoid compounds. When the extraction pressure was greater than 450MPa, HPE extracts showed stronger antioxidant capacity and anti-tyrosinase activity than CE extracts. In a LPS-induced RAW 264.7 cell model of inflammation, HPE extracts had significant inhibitory effects on the cumulative concentrations of nitric oxide and prostaglandin E2. These results indicate that HPE had a better extraction yield, and required a shorter time for the extraction of functional ingredients from DH. Hence, DH could be a potential source for natural antioxidants for the food and biotechnology industries.