Flavonoid Components Research Articles

Novel insights on acetylcholinesterase inhibition by Convolvuluspluricaulis, scopolamine and their combination in zebrafish

Acetylcholinesterase (AChE) inhibitors increase the retention of acetylcholine (ACh) in synapses. Although they alleviate cognitive deficits in Alzheimer’s disease, their limited benefits warrant investigations of plant extracts with similar properties. We studied the anti-AChE activity of Convolvulus pluricaulis (CP) in a zebrafish model of cognitive impairment induced by scopolamine (SCOP). CP is a perennial herb with anti-amnesiac and anxiolytic properties. It contains alkaloid, anthocyanin, coumarin, flavonoid, phytosterol and triterpenoid components. Isoxazole (ISOX) was used as a positive control for AChE inhibition. CP-treated 168 hpf larvae showed a similar pattern of AChE inhibition (in the myelencephalon and somites) as that of ISOX-treated larvae. CP was superior to ISOX as evidenced by the retention of avoidance response behavior in adult zebrafish. Molecular docking studies indicated that ISOX binds Ser203 of the catalytic triad on the human AChE. The active components of CP—scopoletin and kaempferol—were bound by His447 of the catalytic triad, the anionic subsite of the catalytic center, and the peripheral anionic site. This suggested the ability of CP to mediate both competitive and non-competitive modes of inhibition. Surprisingly, SCOP showed AChE inhibition in larvae, possibly mediated via the choline-binding sites. CP + SCOP induced a concentration-dependent increase in AChE inhibition and ACh depletion. Abnormal motor responses were observed with ISOX, CP, ISOX + SCOP, and CP + SCOP, indicative of undesirable effects on the peripheral cholinergic system. Our study proposes the examination of CP, SCOP, and CP + SCOP as potential AChE inhibitors for their ability to modulate cognitive deficits.

Alkaloids, Flavonoids, Tannins and Saponins Contents in Moringa Oleifera Leaves

Various studies have shown that Moringa oleifera leaves have benefits in preventing disease. It also has the potential to solve environmental problems as mosquito larvasides. This is presumably because Moringa leaves contain potentially beneficial compounds. Objective: The aim of this study was to analyze the content of bioactive compounds in Moringa oleifera leaf extract qualitatively and quantitatively. This study was an descriptive study. The study was conducted in Kupang East Nusa Tenggara at September 2019. Moringa leaf extraction was carried out using maceration method with 96% ethanol solvent. The identification of compounds was qualitatively carried out using Thin Layer Chromatography (TLC) methods, while quantitative using spectrophotometric methods. Data was analyzed descriptively to describe the content of flavonoid, tannin, alkaloid, saponin. Study results showed that Moringa leaf extract had flavonoid, alkaloid, tannin and saponin components which were measured qualitatively. Quantitative measurement results showed that Moringa leaves have compounds Total alkaloid Equivalent Quinine 0,3% b/b, Total Flavonoid Equivalent Quercetin17,40 % b/b, Tannin Total Equivalent Tannic Acid 14,68 % b/b, Saponin 7,41% b/b. It is concluded that Moringa oleifera leaf extract has compounds that are beneficial for many things, both in disease prevention, larvasides and other benefits.

Dynamic Metabolomics and Transcriptomics Analyses for Characterization of Phenolic Compounds and Their Biosynthetic Characteristics in Wheat Grain.

Phenolic compounds are important bioactive phytochemicals with potential health benefits. In this study, integrated metabolomics and transcriptomics analysis was used to analyze the metabolites and differentially expressed genes in grains of two wheat cultivars (HPm512 with high antioxidant activity, and ZM22 with low antioxidant activity) during grain development. A total of 188 differentially expressed phenolic components, including 82 phenolic acids, 81 flavonoids, 10 lignans, and 15 other phenolics, were identified in the developing wheat grains, of which apigenin glycosides were identified as the primary flavonoid component. The relative abundance of identified phenolics showed a decreasing trend with grain development. Additionally, 51 differentially expressed phenolic components were identified between HPm512 and ZM22, of which 41 components, including 23 flavonoids, were up-regulated in HPm512. In developing grain, most of the identified differentially expressed genes involved in phenolic accumulation followed a similar trend. Integrated metabolomics and transcriptomics analysis revealed that certain genes encoding structural proteins, glycosyltransferase, and transcription factors were closely related to metabolite accumulation. The relatively higher accumulation of phenolics in HPm512 could be due to up-regulated structural and regulatory genes. A sketch map was drawn to depict the synthetic pathway of identified phenolics and their corresponding genes. This study enhanced the current understanding of the accumulation of phenolics in wheat grains. Besides, active components and their related genes were also identified, providing crucial information for the improvement of wheat's nutritional quality.

One-step purification and immobilization of thermostable β-glucosidase on Na-Y zeolite based on the linker and its application in the efficient production of baohuoside I from icariin

Baohuoside I, a minor flavonoid component of Herba Epimedii, has better bioactivities than its precursor compound icariin. In this work, we have fused the linker (4LP) to thermostable β-glucosidase (Tpebgl3) and successfully prepared the immobilized enzyme (4LP-Tpebgl3@Na-Y) to produce baohuoside I from icariin. The activity recovery and maximum load of 4LP-Tpebgl3@Na-Y were 95.4% and 50.3 mg/g, respectively. Moreover, it exhibited four-fold improved adsorption selectivity (80.5%) with respect to native enzyme after immobilization. The maximum activity of 4LP-Tpebgl3@Na-Y was exhibited at 85 °C, pH 5.0, and it retained>80% of its initial activity after incubation at 75 °C for 2 h . It showed enhanced tolerance of organic solvent and glucose as compared to free enzymes. Kcat/Km value for 4LP-Tpebgl3@Na-Y was 1616.0 s−1•mM−1, which was 61.0% higher than that of free enzyme. Under suitable conditions (75 °C, pH 5.0, 0.1 U/mL enzyme and 120 min), 2000 mg/L icariin was transformed into baohuoside I with a molar conversion of 97.6%. 4LP-Tpebgl3@Na-Y retained 85.2% of its original activity after 10 cycles of reuse and the 768.8 mg/L/h total productivity of baohuoside I was obtained. This is the first research on one-step purification and immobilization of thermostable β-glucosidase based on the linker and its application in the efficient production of baohuoside I from icariin.

Evaluation of the Phytochemical and Pharmacological Potential of Taif's Rose (Rosa damascena Mill var. trigintipetala) for Possible Recycling of Pruning Wastes.

This study investigated the phytochemical contents of Taif’s rose pruning wastes and their potential application as phytomedicine, thereby practicing a waste-recycling perspective. In the Al-Shafa highland, four Taif rose farms of various ages were chosen for gathering the pruning wastes (leaves and stems) for phytochemical and pharmacological studies. The leaves and stems included significant amounts of carbohydrates, cardiac glycosides, alkaloids, flavonoids, and other phenolic compounds. The cardiac glycoside and flavonoid contents were higher in Taif rose stems, while the phenolic and alkaloid contents were higher in the plant leaves. Cardiovascular glycosides (2.98–5.69 mg g−1), phenolics (3.14–12.41 mg GAE g−1), flavonoids (5.09–9.33 mg RUE g −1), and alkaloids (3.22–10.96 mg AE g−1) were among the phytoconstituents found in rose tissues. According to the HPLC analysis of the phenolic compounds, Taif’s rose contains flavonoid components such as luteolin, apigenin, quercetin, rutin, kaempferol, and chrysoeriol; phenolics such as ellagic acid, catechol, resorcinol, gallic acid, and phloroglucinol; alkaloids such as berbamine, jatrorrhizine, palmatine, reticuline, isocorydine, and boldine. Warm water extract was highly effective against Bacillus subtilis, Escherichia coli, and Proteus vulgaris, whereas methanol and cold water extracts were moderately effective against Aspergillus fumigatus and Candida albicans. The study’s findings suggested that Taif’s rose wastes could be used for varied medical purposes.

Decomposition of the interaction energy of several flavonoids with Escherichia coli DNA Gyr using the SAPT (DFT) method: The relation between the interaction energy components, ligand structure, and biological activity

In this study, the SAPT (DFT) method is used to determine the components of the electronic interaction energies (electrostatic (Eele), exchange (Eex), induction (Eind), exchange-induction (Eex-ind), dispersion (Edisp), and exchange-dispersion (Eex-disp)) between the several selected flavonoids and the important residues of the active site of Escherichia coli DNA Gyr determined by molecular docking. A significant linear correlation between the calculated SAPT (DFT) interaction energies of flavonoids and their experimental pIC50 values is found, which is not observed for the free binding energies (ΔGb) of flavonoids obtained from molecular docking. The variation of the interaction energy components of flavonoids with their structural differences is investigated to find the relation between the flavonoids structures and their biological activity based on the interaction energy components.

Integrated Analysis of Metabolome and Transcriptome Data for Uncovering Flavonoid Components of Zanthoxylum bungeanum Maxim. Leaves Under Drought Stress.

Zanthoxylum bungeanum Maxim. leaves (ZBLs) are rich in flavonoids and have become popular in nutrition, foods and medicine. However, the flavonoid components in ZBLs and the mechanism of flavonoid biosynthesis under drought stress have received little attention. Here, we performed an integrative analysis of the metabolome and transcriptome of ZBLs from HJ (Z. bungeanum cv. “Hanjiao”) and FJ (Z. bungeanum cv. “Fengjiao”) at four drought stages. A total of 231 individual flavonoids divided into nine classes were identified and flavones and flavonols were considered the most abundant flavonoid components in ZBLs. The total flavonoid content of ZBLs was higher in FJ; it increased in FJ under drought stress but decreased in HJ. Nine-quadrant analysis identified five and eight differentially abundant flavonoids in FJ and HJ leaves, respectively, under drought stress. Weighted gene correlation network analysis (WGCNA) identified nine structural genes and eight transcription factor genes involved in the regulation of flavonoid biosynthesis. Moreover, qRT-PCR results verified the accuracy of the transcriptome data and the reliability of the candidate genes. Taken together, our results reveal the flavonoid components of ZBLs and document changes in flavonoid metabolism under drought stress, providing valuable information for nutrition value and food utilization of ZBLs.

Systems pharmacology-based drug discovery and active mechanism of natural products for coronavirus pneumonia (COVID-19): An example using flavonoids

BackgroundRecently, the value of natural products has been extensively considered because these resources can potentially be applied to prevent and treat coronavirus pneumonia 2019 (COVID-19). However, the discovery of nature drugs is problematic because of their complex composition and active mechanisms. MethodsThis comprehensive study was performed on flavonoids, which are compounds with anti-inflammatory and antiviral effects, to show drug discovery and active mechanism from natural products in the treatment of COVID-19 via a systems pharmacological model. First, a chemical library of 255 potential flavonoids was constructed. Second, the pharmacodynamic basis and mechanism of action between flavonoids and COVID-19 were explored by constructing a compound–target and target–disease network, targets protein-protein interaction (PPI), MCODE analysis, gene ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment. ResultsIn total, 105 active flavonoid components were identified, of which 6 were major candidate compounds (quercetin, epigallocatechin-3-gallate (EGCG), luteolin, fisetin, wogonin, and licochalcone A). 152 associated targets were yielded based on network construction, and 7 family proteins (PTGS, GSK3β, ABC, NOS, EGFR, and IL) were included as central hub targets. Moreover, 528 GO items and 178 KEGG pathways were selected through enrichment of target functions. Lastly, molecular docking demonstrated good stability of the combination of selected flavonoids with 3CL Pro and ACEⅡ. ConclusionNatural flavonoids could enable resistance against COVID-19 by regulating inflammatory, antiviral, and immune responses, and repairing tissue injury. This study has scientific significance for the selective utilization of natural products, medicinal value enhancement of flavonoids, and drug screening for the treatment of COVID-19 induced by SARS-COV-2.

Optimization of extraction and purification processes of six flavonoid components from Radix Astragali using BP neural network combined with particle swarm optimization and genetic algorithm

BackgroundRadix Astragali (RA), as food and traditional Chinese medicine, has been used for a long history in China. However, few studies on the extraction and purification of the active components from RA have been reported. Thus, the optimal extraction and purification conditions of six flavonoid components (calycosin, calycosin-7-glucoside, formononetin, ononin, 7,2′-dihydroxy-3′,4′- dimethoxyisoflav −7-O-glucoside, and 9,10-dimethoxyptercarpan-3-O-β-D-glucoside) from RA were investigated in this study. MethodsBP neural network combined with particle swarm optimization and genetic algorithm (PSO-GA-BPNN) was used to analyze the relations between the extraction/purification conditions and the response value, and search the optimal extraction/purification conditions. Response surface methodology (RSM) was performed simultaneously as a comparison. Furthermore, the DPPH·radical scavenging activity and hydroxyl radical scavenging activity of crude extract and purified extract were detected. ResultA three-layer PSO-GA-BPNN containing 3 input neurons, 3 hidden layer neurons and 1 output neuron was established to investigate the relationship between the extraction/purification conditions and the response value. For extraction, the optimal condition by PSO-GA-BPNN was as follow: ethanol concentration 54%, extraction time 254 min, and solid-to-liquid ratio 18 mL/g. Using the optimal condition, the yield of six components was 2.084 mg/g, which was greater than 1.915 mg/g optimized by RSM. For purification, among nine types of macroporou resins, CAD-40 with higher adsorption ratio and desorption ratio was selected to purify the extract. The optimal adsorption condition by PSO-GA-BPNN was as follow: pH 6.9, adsorption flow rate 1.6 mL/min and solution concentration 0.22 g/mL, while the optimal desorption condition by PSO-GA-BPNN was as follow: ethanol concentration 55%, desorption flow rate 1.5 mL/min and elution volume 8.5 BV. Under the optimal condition, the adsorption capacity and desorption capacity were 1.465 mg/g and 1.259 mg/g, respectively, which were better than 1.381 mg/g and 1.156 mg/g optimized by RSM. These optimal values obtained by PSO-GA-BPNN were significant increased compared with these by RSM according statistical analysis. The antioxidant test showed that the purified extract has better antioxidant activity. ConclusionThese results indicate that PSO-GA-BPNN model was more appropriate and has better indicative value for extraction than RSM, while the same as for purification. Consequently, PSO-GA-BPNN model combined with MPR purification enhanced the antioxidant potential of the RA from this medicinal species.

Pharmacological Effects and Underlying Mechanisms of Licorice-Derived Flavonoids.

Glycyrrhizae Radix et Rhizoma is the most frequently prescribed natural medicine in China and has been used for more than 2,000 years. The flavonoids of licorice have garnered considerable attention in recent decades due to their structural diversity and myriad pharmacological effects, especially as novel therapeutic agents against inflammation and cancer. Although many articles have been published to summarize different pharmacological activities of licorice in recent years, the systematic summary for flavonoid components is not comprehensive. Therefore, in this review, we summarized the pharmacological and mechanistic data from recent researches on licorice flavonoids and their bioactive components.

An environmental approach for the photodegradation of toxic pollutants from wastewater using Pt–Pd nanoparticles: Antioxidant, antibacterial and lipid peroxidation inhibition applications

BackgroundGreen synthesis is an effective and friendly method for the environment, especially in recent years has been used in many areas. It finds application opportunities in many fields such as physics, chemistry, electronics, food, and especially health and is the subject of intensive studies in this field. ObjectivesThe synthesized Pt–Pd NPs were aimed to be used as a bio-based photocatalyst under sunlight to prevent wastewater pollution. In addition, it is aimed to use Pt–Pd NPs as biological agents in different applications in the future. MethodsIn this study, the platinum-palladium nanoparticles were synthesized by the extract of Hibiscus sabdariffa, the characterization of the nanoparticles was carried out by different methods (ultraviolet–visible spectroscopy (UV–vis), transmission electron microscopy (TEM), infrared transform spectroscopy atomic force microscopy (AFM), and ray diffraction (XRD) analysis). And we discussed several different parameters related to human health by obtaining platinum-palladium bimetallic nanoparticles (Pt–Pd NPs) with a green synthesis method. These parameters are antioxidant properties (total phenolic, flavonoid, and DPPH scavenging activity), antibacterial activity, and lipid peroxidation inhibition activity. Gallic acid was used as standard phenolic, and quercetin was used as standard flavonoid reagents. The newly synthesized Hibiscus sabdariffa mediated green synthesized Pt–Pd NPs were compared with gram-positive and gram-negative bacteria, the high antibacterial activity was shown by gram-positive bacteria. The photodegradation of Pt–Pd NPs was carried out against MB dye for 180 min. ResultsTEM results show that the average size of Pt–Pd NPs is around 4.40 nm. The total amount of phenolic compounds contained in 0.2 mg/ml of Pt-Pd NPs was equivalent to 14.962 ± 7.890 μg/ml gallic acid and the total amount of flavonoid component was found to be equal to 28.9986 ± 0.204 μg/ml quercetin. Hibiscus sabdariffa mediated green synthesized Pt–Pd NPs was found to have very effective for lipid peroxidation inhibition activity in the FeCl2–H2O2 system. The maximum DPPH scavenging activity was determined as 97.35% at 200 μg/ml. The photocatalytic activity of Pt–Pd NPs was analysed against Methylene blue (MB) and the maximum degradation percentage was observed to be 83.46% at 180 min. ConclusionsThe biogenic Pt–Pd NPs showed a high effective photocatalytic and biological activity.

Phytochemical Screening and in vitro Antibacterial Activity of Typhonium trilobatum Methanolic extract

Typhoniumtrilobatum (Family: Araceae) is a common vegetable and a useful perennial herb in traditional medicine found all over Bangladesh. The purpose of this study was to evaluate thephytochemical screening,totalphenoliccontent, total flavonoid content and antibacterial activity of Typhoniumtrilobatum species. The phytochemical analysis revealed the presence of alkaloids, carbohydrates, flavonoids,phenoliccompounds and reducing sugar. Theantibacterialstudy resultconfirmed that the crude methanolic extract ofTyphoniumtrilobatumhas the ability to inhibit bacterial growth. The higher antibacterial activity was foundagainst Gram-negative bacteria Shigella bodydiiwhere the zone of inhibition wasfound 12 mm for1000µg/disc extract. The lowest inhibitory activity was found against Salmonella paratyphi with 8 mm zone of inhibition. The presence of total phenolic and flavonoid contents was found10.8mg gallic acid equivalent (GAE/gm) and 6.5 mg quercetin equivalent (QE/gm), respectively in each gram of Typhoniumtrilobatum methanolic extract.The antibacterial effects of the Typhoniumtrilobatumleaves extract may be linked to the presence of phenolic and flavonoid components. However, further studies are required to obtain more reliable information.

In Vitro Antioxidant and Antimicrobial Activity of Isolated Flavonoid from the Methanolic Extract of Spermacoce hispida Leaves

The purpose of this research was to separate the flavonoid component of the Spermacoce hispida plant that is responsible for its medicinal effects. A methanolic extract of Spermacoce hispida leaves was used to study the separation of flavonoids from a plant component. Phytochemical analysis of methanol extract confirmed the presence of flavonoid compounds. The extracted flavonoid component was refined using thin-layer chromatography and column chromatography. The structures of the isolated compounds were characterised using UV-Visible, FT-IR, 13C, 1H NMR, and Mass spectroscopy. Therefore, 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3-[-Lrhamnopyranosyl-(16)—D-glucopyranosyloxy] was given as the name for the isolated molecule. There has to be further biological investigation of this plant's isolated flavonoid. Flavonoids are a distinct class of plant secondary metabolites having pharmacological benefits that have been used for centuries in traditional medicine. They support a diverse array of medical procedures that may provide novel and therapeutic medication discoveries. Flavonoids' potential as antioxidants in the face of oxidative stress has been the subject of a lot of recent research. To what extent flavonoids may serve as antioxidants and as antimicrobials is explored in this study.

Troxerutin affects nephropathy signaling events in the kidney of type-1 diabetic male rats.

Objective:Nephropathy is known to be the leading cause of kidney failure in diabetic patients. Troxerutin, as a flavonoid component, could provide a novel protective strategy in the prevention of diabetic nephropathy. A large number of reports on the salutary effects of troxerutin inspired us to investigate its effect on the nephropathy signaling events (i.e., expression of TGF-β, miRNA192, and SIP1) in type-1 induced diabetic rats.Materials and Methods:50 male Wistar rats were divided into 5 groups including control group, sham group treated with troxerutin for 4 weeks, diabetic group induced by streptozotocin (STZ) injection, DI group including insulin-treated diabetic animals and DT group treated with troxerutin. Ultimately, rat kidneys were extracted, and the level of miR-192 (using qPCR), transforming growth factor-beta (TGF-β), and smad interacting protein 1 (SIP1) using an ELISA kit, was measured.Results:The level of TGF-β and miRNA192 significantly increased in the diabetic group. However, their expression levels decreased following the administration of troxerutin and insulin (p<0.05) compared to control group. SIP1 was down-regulated in the diabetic group, whereas a spike in the expression levels was observed after troxerutin administration compared to control and troxerutin groups (p<0.05). However, no significant difference was found in the effects of insulin and troxerutin on the level of miR-192, SIP1, and TGF- β. Conclusion:According to the previous literatures, during the progression of nephropathy, TGF-β represses SIP1 (the repression region in the collagen gene) by increasing the expression of miR-192. Ultimately, in this study, diabetes led to up-regulation of TGF-β while troxerutin proved to have a protective effect on the kidney by increasing SIP and lowering miR-192 levels.

Oroxin A ameliorates the oleic acid-induced A549 cell injury through the suppression of pyroptosis and degradation of alveolar surfactant

The destruction of the pulmonary epithelial barrier in acute respiratory distress syndrome is caused by the damage of the alveolar epithelial cells. Oroxin A is an effective flavonoid component derived from the medicinal plant Oroxylum indicum (L.) Kurz. In this study, the oleic acid (OA)-induced A549 cell injury model was established in vitro to explore the protective mechanism of Oroxin A. The experiment was divided into the following groups: control, OA and OA + Oroxin A group. The OA-induced A549 cell injury was dose (time)-dependent and was detected by the CCK-8 assay. The protein and mRNA expression levels associated with pyroptosis are detected by Western blotting and RT-qPCR. After Oroxin A treatment, the levels of IL-1β, IL-18 and LDH released were significantly lower than the OA group. In terms of pyroptosis, Oroxin A can inhibit the expression of pyroptosis-related protein and mRNA. Significantly, the surfactant protein C (SPC) level in the OA + Oroxin A group was significantly higher than that in the OA group. The treatment with Oroxin A alleviates the OA-induced injury in the A549 cells, and its mechanism may be related to the inhibition of A549 cells pyroptosis and prevention of the degradation of the SPC.

Phytochemical Analysis, Estimation of Quercetin, and in Vitro Anti-Diabetic Potential of Stevia Leaves Samples Procured from Two Geographical Origins

The current study used RP-HPLC to compare phytochemicals and estimate the bioactive constituents found in Stevia rebaudiana Bert. (SRB) leaves collected from two different geographical sources. SRB leaves were collected from Bangalore, Karnataka, India, and Reduit, Mauritius. Extracts were prepared using ethanol and aqueous solvents. Proximate analysis was used to evaluate moisture content, ash values, crude fibers, and extractive values. Following that, preliminary phytochemical screening was done on both ethanol leaves extracts, and subsequently total flavonoid content was determined. In addition, TLC chromatograms and RP-HPLC studies were performed on both plant extracts to determine the presence of flavonoid components in both leaves extracts, followed by in vitro anti-diabetic activity was performed with alpha amylase and alpha glucosidase enzymes against Acarbose as standard. Results revealed that both the extracts from two different geographical sources varied significantly with the yield, content of chemicals, and presence of quercetin (flavonoid) content when estimated through the RP-HPLC standardized method. Glycosides, flavonoids, proteins, steroids, saponins, terpenoids, and phenols were found in various concentrations during phytochemical screening. Among both zones, the ethanol leaves extract of SRB taken from Mauritius had a greater content of phytochemicals and a higher yield than other extracts due to the soil nature. The Mauritius sample had greater total flavonoid levels as well as more quercetin (0.92 ± 0.011) than the other extracts. Following that, ethanol extract inhibited enzymes (alpha amylase, alpha glucosidases) more than aqueous extract, and this inhibition was dose dependent. Among them, the Mauritius ethanol sample showed higher anti-diabetic efficacy than the Indian sample, but this difference was not significant. Overall, SRB ethanol leaves extracts outperformed other leaves extracts in terms of yield, phytoconstituents, and total flavonoids. Overall, both SRB samples had high quercetin levels and possessed anti-diabetic potential, but they were greater in the Mauritius sample, demonstrating that plant traits are influenced by geographic location.

Comparison of Functional Flavonoid Components and Contents from Domestic Propolis Extracts

프로폴리스에 함유된 다양한 플라보노이드 성분은 생산 지역에 따라 함량이 다르기 때문에 그 표준화가 어렵다. 본 연구에서는 먼저 프로폴리스의 추출방법을 최적화하고, 두 번째로 프로폴리스 추출물의 지역별 플라보노이드 함량의 차이를 비교하고 주요 성분의 효능을 비교하였다. 지역별 프로폴리스의 총 폴리페놀 함량을 측정하고 DPPH assay를 통해 항산화 효능을 확인하였다. HPLC 분석을 통하여, 주요 플라보노이드 성분인 quercetin, caffeic acid, p-coumaric acid, pinocembrin, kaempferol, galangin 및 chrysin의 프로폴리스 내 함유량을 정량하였다. 마지막으로 β-hexosaminidase release assay를 통해 quercetin의 항알레르기 효능을 확인하였다. 경상북도 안동, 봉화, 군위에서 생산된 프로폴리스 추출물의 항산화 효과는 각각 80.2%, 72.4%, 54.5%였다. 프로폴리스 추출물의 플라보노이드 함량은 지역별로 차이가 있었으며 quercetin, pinocembrin, galangin, chrysin의 함량이 공통적으로 가장 높았다. Quercetin의 β-hexosaminidase 방출이 양성대조군의 약 25%로 나타나 알레르기 억제 효능을 확인하였다. 본 연구에서 프로폴리스 추출법의 표준화와 더불어 지역별 프로폴리스 추출물의 플라보노이드 함량과 각 성분별 효능을 비교하였으며, 플라보노이드에 의한 천연 항알레르기제의 활용 가능성을 제시하였다.

Comparative study on the main active components of Baoyuan decoction in plasma and urine of normal and heart failure rats.

The global morbidity and mortality of heart failure has been increasing in recent years. Traditional Chinese medicine (TCM) was increasingly used to treat cardiovascular diseases. Baoyuan decoction (BYD) was a famous classical prescription in China. Modern pharmacological studies showed that it had obvious therapeutic effects on cardiovascular diseases, but its pathological pharmacokinetic studies were unclear. In this research, the absorption of 16 bioactive components in plasma and the excretion of 9 representative components in urine of control rats and isoproterenol (ISO)-induced heart failure rats were studied using the large-volume direct-injection LC-MS method established by our research group. The results indicated that flavonoid constituents exhibited quicker absorption and elimination than saponin constituents after oral administration of BYD. The half-life period of some bioactive compounds in the model group was increased, which contributed to the longer therapeutic effect. The cumulative excretion rate of major flavonoid components of BYD decreased significantly in the ISO-induced heart failure rats.

Simultaneous Determination of Four Marker Compounds in Lobelia chinensis Lour. Extract by HPLC-PDA

Lobelia chinensis Lour. (L. chinensis) has traditionally been used as a treatment for snake bites, high fever, jaundice, edema, and diarrhea, and modern studies have reported its anti-inflammatory, antioxidant, and antiviral activities. L. chinensis contains various compounds, such as flavonoids and coumarins, and its flavonoid components have been identified in many studies. In this study, a high-performance liquid chromatograph equipped with a photodiode array (PDA) detector and an Aegispak C18-L reverse-phase column (4.6 mm × 250 mm i.d., 5 μm) was used to simultaneously analyze four marker components in L. chinensis for standardization purposes. HPLC-PDA (detection at 340 nm), performed using a 0.1% formic acid-water/0.1% formic acid-acetonitrile gradient, separated the four marker compounds: luteolin-7-O-β-d-glucuronopyranosyl (1→2)-O-β-d-glucuronopyranoside, clerodendrin, chrysoeriol-7-O-diglucuronide, and diosmin. The developed analytical method showed excellent linearity values (r2 &gt; 0.9991), limits of detection (LODs: 0.376–2.152 μg/mL), limits of quantification (LOQs: 1.147–6.521 μg/mL), intra- and inter-day precisions (RSD &lt; 1.96%), and analyte recoveries (96.83–127.07%; RSD &lt; 1.73%); thus, it was found to be suitable for the simultaneous analysis of these four marker compounds in L. chinensis.

Antioxidant Activity and Cytotoxicity Against WiDR Cell and Vero Cell of The Karamunting (Rhonomyrtus tomentosa L.) Leaves Ethanol Extract

Karamunting (Rhodomyrtus tomentosa L.), a plant used as a traditional medicine, is widely distributed throughout Indonesia. Karamuting has the potential as an antioxidant and anticancer agents because of its phenolic and flavonoid components. This study aimed to determine total phenolic level, antioxidant activity and cytotoxic of karamunting leaves extract. The simplisia of karamunting leaves were extracted by maceration method using 96% ethanol, tested for its antioxidant activity using DPPH and its citotoxic by MTT method (3- (4,5-dimethyltiazol-2-il) -2,5-diphenyl tetrazolium bromide) on WiDr cells and Vero cells. The results of this study showed that the yield of karamunting extract were 15.635% with a total phenolic level of 0.76%, antioxidant activity (IC50 values) of 15,330 μg / mL and cytotoxicity (IC50 values) of 205.7069 μg / mL for WiDr cells and 44.87703 μg / mL for Vero cells. Ethanol extract of karamunting leaves possessed a very strong antioxidant activity while it showed a weak cytotoxic effect on WiDr cells and toxic effect on Vero cells.Keywords: Antioxidant, Anticancer, Karamunting