Flavonoids Catechin Research Articles

Sorbitol induces flavonoid accumulation as a secondary signal via the nanoencapsulated SPc/lncRNA809-MmNAC17 module against Alternaria alternata in Malus micromalus

Sorbitol is an important primary metabolite that serves as both a carbon source and signal to pathogens. The leaf diseases caused by Alternata alternata are particularly serious in crabapple (Malus micromalus). Here, we found that sorbitol can enhance the resistance of crabapple to A. alternata R1 by increasing the content of flavonoid catechin. Nanomaterials as an emerging technology tool can efficiently deliver lncRNA to target cells. Here, we found nanoencapsulated lncRNA809 (SPc/lncRNA809) exhibits significant resistance to R1strain. To elucidate the effect of SPc/lncRNA809 on flavonoids catechin synthesis, we observed the expression of lncRNA809 was consistent with that of MmNAC17 which regulates the synthesis of catechin and both could jointly respond to sorbitol. MmNAC17 induced the accumulation of catechin in vivo by directly activating the expression of catechin synthase genes MmF3H and MmLAR. Correspondingly, overexpression of lncRNA809 significantly upregulated the expression of MmNAC17 and enhanced the disease resistance. This study reveals for the first time that sorbitol positively regulates the expression of MmNAC17 through lncRNA809, promoting the accumulation of catechin via the expression of MmF3H and MmLAR, ultimately improving the defense response of M. micromalus. This research provides a crucial foundation for the establishment and application of sorbitol-based signaling regulatory networks.

In vitro Bioaccesibility of Phenolic Compounds from the Halophytes Suaeda Edulis and Suaeda Esteroa: Opportunity for the Development of Novel Foods

Halophytic plants grow in high salinity environments and present phytochemicals with antioxidant properties, such as phenolic compounds; due to the uncertain availability of healthy foods, there is a growing interest in their nutritional potential. However, their bioactive compounds with beneficial health effects are limited in their bioaccessibility. The objective of this study was to subject S. edulis and S. esteroa to an in vitro digestion process to evaluate the bioaccessibility and total antioxidant capacity of phenolic compounds during three phases of digestion. We determined phenolic compounds, flavonoids, and antioxidant capacity by colorimetric methods and phenolic composition by UHPLC-DAD. Total phenols, total flavonoids, and total antioxidant capacity by DPPH and TEAC in the three phases of digestion (oral, gastric, and intestinal) of S. esteroa were higher than in S. edulis, founding 4.84 % higher in total phenol content, and 0.05 % in total flavonoid content; also, and 28.94 and 23.93 % higher in total antioxidant capacity by DPPH and TEAC, respectively in the intestinal digestion phase. The bioaccessibility of S. edulis was higher than in S. esteroa; the intestinal was the phase reflecting more bioaccessible compounds. The bioaccessibility percentages of total phenols and flavonoids were 590.16 and 1012.93 %, and the percentage recovery of total antioxidant capacity by DPPH and TEAC were 181.37 and 139.74 %. We identified phenolic acids ferulic, p-Coumaric, and synaptic (hydroxycinnamic), gallic and protocatechuic (hydroxybenzoic), the flavonoids catechin (flavan-3-oles), myricetin and ruthin (flavonols), naringenin and naringin (flavonones). S. esteroa presented bioactive compounds in higher concentrations than S. edulis due to the stress imposed by its habitat; nevertheless, the determined bioactive compounds of S. edulis showed a higher bioaccessibility because it was managed under local improvement.

Managing Esca in Susceptible ‘Sauvignon Blanc’ Wine Grapes Through Trunk Renewal

Trunk renewal was evaluated as a treatment for highly susceptible ‘Sauvignon blanc’ wine grapes with moderate leaf and wood symptoms of the trunk disease Esca in a 17-year-old vineyard 7 years after symptoms first appeared. The trunk was cut above the graft union, removing all woody parts of the vine above it, including infected wood. A new trunk was retrained from a shoot off presumably healthy wood at the base of the trunk. Prior to trunk renewal, we detected Esca pathogens from 26% of 97 symptomatic vines. Five years after trunk renewal, 72 retrained vines were still asymptomatic, 24 were replanted (i.e., did not produce a shoot after trunk renewal), and one had leaf and fruit symptoms. Chemical composition of asymptomatic fruit from asymptomatic-retrained vines (RV-AF) was compared to that of vines that were not retrained, the latter of which included asymptomatic fruit from asymptomatic vines (AV-AF) and both asymptomatic fruit (SV-AF) and symptomatic fruit (SV-SF) from the same symptomatic vines. Given the high proportion of asymptomatic retrained vines after five growing seasons, trunk renewal was an effective cultural practice. Although there were no differences in chemistry parameters used to make harvest decisions (total soluble solids, pH, and titratable acidity), SV-SF was unique in having the highest concentrations of the flavonoids catechin and epicatechin and the lowest concentrations of the volatile-aroma compounds hexanal and 2-hexanal. These findings in all three blocks among fruit with visible spots may reflect a host-defense response and/or the effect of Esca on fruit ripening.

COI1 dependent jasmonic acid signalling positively modulates ROS scavenging system in transgenic hairy root culture of tomato

Reactive oxygen species (ROS) production is a routine event in plants. ROS function as signalling molecules in regulating plant development and defence. However, their accumulation beyond threshold leads to toxicity. Hence, plants are evolved with specialized ROS scavenging system involving phytohormones (synthesis and signalling), enzymes and metabolites. To understand the role of phytohormone jasmonic acid (JA) signalling in ROS scavenging, tomato coronatine insensitive 1 (SlCOI1), a key gene in JA signalling, was silenced and overexpressed in tomato transgenic hairy roots (HR) under the constitutive promoter. Targeted metabolomics of transgenic HR revealed accumulation of phenolic acids including ferulic acid, coumaric acid, vanillic acid, and flavonoid catechin in SlCOI1 overexpressed line. Moreover, osmolyte amino acids proline, asparagine, and glutamine showed a positive co-relation with transgenic overexpression of SlCOI1. Ascorbic acid-glutathione, a crucial antioxidant system was found to be influenced by COI1-mediated JA signalling. The expression of genes encoding enzymes superoxide dismutase 1, ascorbate peroxidase 1, and dehydroascorbate reductase 2 was found to be down and upregulated in SlCOI1 silenced and overexpressed lines, respectively. Methyl jasmonate and Fusarium oxysporum f.sp. lycopersici crude extract treatment further confirmed the regulatory role of COI1-mediated JA signalling in regulation of enzymatic components involved in ROS scavenging. The COI1-mediated JA signalling could also elevate the expression of RESPIRATORY BURST OXIDASE HOMOLOG-B gene which is involved in ROS wave signal generation. The present study underscores the role of COI1-mediated JA signalling in modulating enzymatic and non-enzymatic components of ROS scavenging system and pathogen associated molecular pattern triggered immunity.

Adaptive advantage of Sesbania virgata (Cav.) Pers. in the phytochemical production: the influence on fungi occurring in seeds

Sesbania virgata is a native Brazilian plant species. It exhibits rapid growth, a high soil cover potential, and efficient soil seed bank formation and is used in environmental restoration projects. The soil seed bank is susceptible to fungal infection and other biotic factors. However, only a few studies have reported on the fungi on the surface of S. virgata seeds. Moreover, little is known about how substances present in the seed integument affect fungal communities and their role in adapting to and thriving in new environments. Herein, S. virgata seeds were collected from populations that produce or do not produce the flavonoid catechin in the seed coat. These seeds were subjected to laboratory tests to identify and quantify the fungal populations in the integument. We selected and subjected three genera to irrigation and inoculation tests with S. virgata extracts and seeds from both populations. We observed that the aqueous seed coat extracts inhibited Alternaria sp. micellar and augmented Phoma sp. growth. Phoma sp. also caused post-germinated seed lethality. Our data indicate that the seed coat of S. virgata contains antifungal substances that endow this species with an adaptive advantage.

Evaluation of proximate compositions and profiling of nutritional aspects in pupae of tasar silkworm Antheraea mylitta (Drury) as potential for food and feed resources

Aim: To investigate the proximate compositions, amino acids profile, phenols, flavonoids, fatty acids and minerals in Tasar silkworm pupae and assessment of biological potential of pupae extracts. Methodology: Biochemical composition such as proteins, fat, carbohydrate, chitin, ash, moisture and minerals were analyzed in Tasar silkworm pupae. The amino acid, vitamins, phenolics and flavonoid, fatty acids and free radical scavenging assay were evaluated. Results: The pupae powder contained 11.23% moisture, 60.67% crude protein, 23.83% fat, 3.29% carbohydrate, 5.1% ash and 3.87% chitin on a dry matter basis. Further, the pupae protein contained 19 amino acids, including all of the essential amino acids. Similarly, the pupae powder contained both water and fat soluble vitamins with higher content of tocopherol (13.23 µg 100 gm-1), phenolics compounds majorly ferulic acid (1317.5 µg gm-1) and p-coumaric acid (730.96 µg gm-1), flavonoids catechin (40.771 µg gm-1) and myricetin (12.466 µg gm-1) at higher levels and fatty acid with higher palmitic acid content (6.565 mg g-1). Mineral analysis indicated higher magnesium (208 mg 100 gm-1), calcium (47.79 mg 100gm-1) and iron (37.72 mg 100 gm-1) contents. Further, pupae extract exhibited free radical scavenging potential in a concentration-dependent manner. Interpretation: The results of the study indicate tasar pupae as a renewable and sustainable source for preparation of animal feeds. Key words: Antheraea mylitta, Antioxidants, Tasar pupae

The impact of varying doses of moringa leaf methanolic extract supplementation in the cryopreservation media on sperm quality, oxidants, and antioxidant capacity of frozen-thawed ram sperm

To increase rams’ post-thaw semen quality following cryopreservation, this study used enriched Tris-based diluent with varying amounts of moringa leaf methanolic extract (MLME). The antioxidant activity, total phenolic, and total flavonoid content were all assessed in MLME. The sperm of five healthy Awassi rams were collected, divided into 4 equal aliquots, and diluted [1:5; (v/v)] in Tris-citrate-glucose extender supplemented with 0.48, 0.56, and 0.64 mg MLME/ml or without MLME supplementation (control). The percentages of sperm total motility (STM, %), sperm progressive motility (SPM, %) and viability (V, %), abnormal morphology (AM, %), membrane functional integrity (MFI, %), and acrosome integrity (AI %) were measured. Malondialdehyde (MDA), nitric oxide (NO), ascorbic acid (AA), superoxide dismutase (SOD), glutathione peroxidase (GPx), total cholesterol (TC), low-density lipoproteins (LDL), lactate dehydrogenase (LDH), alkaline phosphatase (ALP), zinc (Zn), and copper (Cu) were measured. The total phenolic gallic acid and flavonoid catechin (equivalent) contents were 19.78 mg/g and 11.94 mg/g, respectively. 2,2-Diphenyl-1-picrylhydrazyl (34.37 mM TE/g) and 2,2′-azino-bis/3-ethylbenzothiazoline-6-sulfonic acid (53.47 mM TE/g) were found in MLME. MLME had a 64.59 mM TE/g ferric-reducing power. In comparison to control, the addition of 0.64 mg/ml MLME to Tris-based extender resulted in the highest (P < 0.001) STM (55.22 ± 0.98), SPM (45.41 ± .70), SV (60.01 ± 1.05), MFI (75.23 ± 0.77), and AI (73.13 ± 0.72) and the lowest (P < 0.001) AM (21.34 ± 0.72) values. In comparison to the control, the addition of 0.56 mg/ml semen extender resulted in lower STM, SPM, SV, MFI, and AI with higher AM percentages. MDA (P = 0.03), NO (P = 0.012), CHO (P = 0.0001), and LDL (P = 0.004) were reduced by 0.64 mg/ml MLME, while AA (P = 0.017) and SOD (P = 0.0001) were elevated. In conclusion, the highest copper (P = 0.006) and lowest zinc concentrations in MLME (0.48 mg/ml extender) deteriorated the post-thaw semen quality, prompting us to suggest the addition of 0.64 mg MLME to rams’ Tris-based semen extender.

Combined Water Extracts from Oxidation-Treated Leaves and Branches of Hovenia dulcis Has Anti-Hangover and Liver Protective Effects in Binge Alcohol Intake of Male Mice.

Hovenia dulcis, known as the oriental raisin tree, is used for food supplements and traditional medicine for the liver after alcohol-related symptoms. However, little information exists about the use of its leaves and branches. In this study, we established a method to use the leaves and branches to develop anti-hangover treatment and elucidated the underlying mechanisms. Oxidation-treated leaves (OL) exhibited high antioxidant content comparable to that of the peduncles and showed an anti-hangover effect in male mice. The branch extract (BE) was enriched in the flavonoid catechin, approximately five times more than OL extract. The mixture of OL and BE (OLB) was formulated in a 2:1 ratio with frozen-dried extract weight and was tested for anti-hangover effects and protective properties against binge alcohol-induced liver injury. OLB showed better anti-hangover effect than OL. In addition to this anti-hangover effect, OLB protected the liver from oxidative/nitrosative damage induced by binge alcohol intake.

Effects of Sargassum virgatum extracts on the testicular measurements, genomic DNA and antioxidant enzymes in irradiated rats

Background Oxidative stress and reactive oxygen species (ROS) are primarily responsible for the development of male infertility after exposure to γ-irradiation. The present work aimed to assess the ameliorative and therapeutic roles of the aqueous and ethanolic extracts of the edible seaweed Sargassum virgatum (S. virgatum) on spermatogenesis and infertility in γ-irradiated Wistar rats. Materials and methods Induction of infertility was performed by exposing the rats to 137Cs-gamma rays, using a single dose of 3.5 Gy. γ-irradiated rats were given the S. virgatum ethanolic (S. virgatum-EtOH) and aqueous extracts intraperitoneally on a daily base for two consecutive weeks at doses of 100 and 400 mg/kg body weight (b.wt.) for each seaweed extract. Morphometric data of the testes, semen quality indices, antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), and glutathione peroxidase (GPx), and deoxyribonucleic acid (DNA) fragmentation were assessed. The results obtained were taken during two-time intervals of 15 and 60 days from the commencement of the algal treatments. In vitro antioxidant assays and polyphenolic compounds of S. virgatum were characterized. Results Significant negative changes in the semen quality and morphometric data of the testes, as well as remarkable DNA fragmentation, were detected in the irradiated rats compared to the control. The levels of the endogenous antioxidant enzymes (SOD, CAT, GSH, and GPx) were also significantly diminished. Nonetheless, treatments of γ-irradiated rats with the S. virgatum-EtOH and aqueous extracts significantly improved the above-mentioned enzymes, in addition to noteworthy amendments in the dimensions of the testes, the semen quality, as well as the DNA structure. Conclusions The ameliorative potency of S. virgatum to cure γ-irradiation-induced male infertility, particularly 400 mg/kg ethanolic extract for 60 days, is the result of the consistent therapeutic interventions of its potent antioxidant and anti-apoptotic polyphenols, particularly protocatechuic, p-hydroxybenzoic, rosmarinic, chlorogenic, cinnamic and gentisic acids, as well as the flavonoids catechin, hesperidin, rutin and quercetin. Besides its high-value nutraceutical importance, S. virgatum could be a natural candidate for developing well-accepted radioprotectant products capable of treating γ-irradiation-induced male infertility.

Biochemical characterization of Peumus boldus fruits: Insights of its antioxidant properties through a theoretical approach

Peumus boldus is an endemic tree species from Chile whose leaves have been the focus of study for decades given that their infusions are reported to relieve rheumatic symptoms, headache, dyspepsia, urinary tract inflammation, and symptoms of other illnesses. These health properties have been studied mainly using leaves and bark, then it is relevant to know more about these properties in different parts of the plant. Considering the importance of P. boldus fruits in the diet of some rural populations, we analyzed their properties to explore its impact on the Chilean population health. Liquid chromatography and mass spectrometry analysis confirmed the presence of alkaloids such as boldine, although aporphine N-methyl-laurotetanine was the most abundant. In addition, flavonoids catechin, chrysin and quercetin were also found in the extract. Cytotoxicity and anti-inflammatory activities of the fruit extract were invitro tested by using a murine macrophage cell model, observing that a diluted fraction of the extract was not cytotoxic, but showed anti-inflammatory activity, which is likely attributed to antioxidants activities. By means of quantum chemical calculations, we calculated the redox potential of the respective alkaloids and flavonoids found in the extract. Results suggest a synergistic effect between alkaloids and flavonoids, where boldine and N-methyl-laurotetanine showed similar antioxidant properties. Finally, we present a description of the oxidation mechanisms for both groups of molecules which will sustain P. boldus fruit biological properties, in order to give this kind of fruits scientific value focusing on human health.

Gas Chromatographic Analysis of the Phyto-Constituents and the Assessment of the Anti-Microbial Properties of the Leave Extracts of Nigeria-Grown Gingko biloba

Purpose: Gingko biloba (GB) leaves have been recognized for their therapeutic effects, dating back to traditional Chinese medicine where the ground leaves were used to treat several health problems. GB extracts are renowned for their medicinal properties in Asia, Europe and South America. However, GB leaves are rarely grown and used in Nigeria. In this study, we screened the phytochemical constituents and antimicrobial activities of GB leaves (aqueous and ethanol extracts) grown in Enugu, Enugu State, South East Nigeria. Study Design: Experimental Materials and Methods: Quantitative analyses of phytochemicals were done using gas chromatography while disk diffusion and broth dilution methods were used to determine the antimicrobial activities. Results: The phytochemical analysis of aqueous and ethanol extracts showed high quantity of flavonoids (anthocyanin, rutin, epicatechin, kaemferol and catechin), alkaloids (lunamarine and ribalindine) and saponin while the moderate quantity of steroids and terpenes, tannin and phenols were also observed. The phytochemical analysis also showed very little concentration of antinutrients (phytate and oxalate) in both extracts. The ethanol extract showed some degree of antibacterial and antifungal activities as observed from their zones of inhibition (mm). Activity was observed on gram-positive bacteria; Staphylococcusaureus (15.5+0.71mm) and less activity on gram-negative bacteria; Escherichia coli (10.5+1.41mm) and Pseudomonasaeruginosa (no activity). Also there was an activity on yeast; Candida albicans (16.5+0.71mm) and less activity on moulds; Penicilliumcyclopium (9+1.41mm) and Aspergillus fumigatus (no activity). The aqueous extract showed no antimicrobial activity on both bacteria and fungi. Conclusion: This study revealed the medicinal potentials of Ginkgo biloba leaves grown in Nigeria. The findings, therefore, will be useful for pharmaceutical industries and medical practice in Nigeria and beyond for the provision of good health to individuals.

Influence of pectinase–assisted extraction time on the antioxidant capacity of Spent Coffee Ground (SCG)

Spent Coffee Ground (SCG) comprises a range of functional components with high antioxidant potential and health benefits. Although SCG has many advantages, antioxidant values obtained using enzymes is still scarce. Several studies reported that the use of enzyme-assisted extraction techniques could improve the detection of antioxidant compounds in samples of by-products. In this study, SCG was extracted using enzymeassisted techniques for different periods (0, 20, 40, 60, 80 and 100 mins). The total antioxidant capacity was measured using Peroxidase, Catalase, Ferric reducing antioxidant power (FRAP), Superoxide radical scavenging assay (SRSA) and 2,2-diphenyl-2- picrylhydrazyl (DPPH) analysis. 60 mins extraction was found to exhibit antioxidant activity in DPPH, SRSA, Catalase and Peroxidase of 84.18±7.01%, 32.83±6.75%, 76.65±5.52% and 75.01±7.67%, respectively. Besides that, the extraction also gave a high amount of content with 267.17±26.69 mg TAE/mL and 58.30±2.36 mg QE/g in total phenolic content and total flavonoid content respectively. Flavonoids such as quercetin, kaempferol, rutin, gallic acid, catechin, epigallocatechin, p-Coumaric acid and myricetin were found to be present in SCG extract. A high amount of catechin was found in all periods of extraction, whereby 60 mins had the highest concentration of 1741.65 mg/L, while 40 mins had the lowest concentration which was 389.85 mg/L. In conclusion, 60 mins extraction using a pectinase-assisted method was the best extraction period. Additionally, the individual flavonoid catechin in SCG showed that it has potential as an antioxidant. Finally, there is a strong correlation between antioxidative activity and both phenolic and flavonoid content

Epigallocatechin gallate and theaflavin gallate interaction in SARS-CoV-2 spike-protein central channel with reference to the hydroxychloroquine interaction: Bioinformatics and molecular docking study.

SARS‐CoV‐2 or COVID‐19 pandemic global outbreak created the most unstable situation of human health–economy. In the past two decades different parts of the word experienced smaller or bigger outbreak related to human coronaviruses. The spike glycoproteins of the COVID‐19 (similar to SARS‐CoV) attach to the angiotensin‐converting enzyme (ACE2) and transit over a stabilized open state for the viral internalization to the host cells and propagate with great efficacy. Higher rate of mutability makes this virus unpredictable/less sensitive to the protein/nucleic acid based drugs. In this emergent situation, drug‐induced destabilization of spike binding to RBD could be a good strategy. In the current study we demonstrated by bioinformatics (CASTp: computed atlas of surface topography of protein, PyMol: molecular visualization) and molecular docking (PatchDock and Autodock) experiments that tea flavonoids catechin products mainly epigallocatechin gallate or other like theaflavin gallate demonstrated higher atomic contact energy (ACE) value, binding energy, Ki value, ligand efficiency, surface area and more amino acid interactions than hydroxychloroquine (HCQ) during binding in the central channel of the spike protein. Moreover, out of three distinct binding sites (I, II and III) of spike core when HCQ binds only with site III (farthest from the nCoV‐RBD of ACE2 contact), epigallocatechin gallate and theaflavin gallate bind all three sites. As sites I and II are in closer contact with open state location and viral–host contact area, these drugs might have significant effects. Taking into account the toxicity/side effects by chloroquine/HCQ, present drugs may be important. Our laboratory is working on tea flavonoids and other phytochemicals in the protection from toxicity, DNA/mitochondrial damage, inflammation and so on. The present data might be helpful for further analysis of flavonoids in this emergent pandemic situation.

Control of Reactive Oxygen Species for the Prevention of Parkinson's Disease: The Possible Application of Flavonoids.

Oxidative stress reflects an imbalance between the production of reactive oxygen species (ROS) and antioxidant defense systems, and it can be associated with the pathogenesis and progression of neurodegenerative diseases such as multiple sclerosis, stroke, and Parkinson’s disease (PD). The application of antioxidants, which can defend against oxidative stress, is able to detoxify the reactive intermediates and prevent neurodegeneration resulting from excessive ROS production. There are many reports showing that numerous flavonoids, a large group of natural phenolic compounds, can act as antioxidants and the application of flavonoids has beneficial effects in the adult brain. For instance, it is well known that the long-term consumption of the green tea-derived flavonoids catechin and epigallocatechin gallate (EGCG) can attenuate the onset of PD. Also, flavonoids such as ampelopsin and pinocembrin can inhibit mitochondrial dysfunction and neuronal death through the regulation of gene expression of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. Additionally, it is well established that many flavonoids exhibit anti-apoptosis and anti-inflammatory effects through cellular signaling pathways, such as those involving (ERK), glycogen synthase kinase-3β (GSK-3β), and (Akt), resulting in neuroprotection. In this review article, we have described the oxidative stress involved in PD and explained the therapeutic potential of flavonoids to protect the nigrostriatal DA system, which may be useful to prevent PD.

Molecular Docking, Physicochemical Properties, Pharmacokinetics and Toxicity of Flavonoids Present in Euterpe oleracea Martius.

Euterpe oleracea Martius, popularly known as açaí, is a fruit rich in α- tocopherols, fibers, lipids, mineral ions, and polyphenols. It is believed that the high content of polyphenols, especially flavonoids, provides several health-promoting effects to the açaí fruit, including anti-inflammatory, immunomodulatory, antinociceptive and antioxidant properties. Most of the flavonoids are antioxidant molecules of plant origin that act as a trap for free radicals, reacting and neutralizing them, thus offering perspectives in preventing oxidative damage. In this study, we aim to perform an in silico evaluation of flavonoids present in the pulp and the oil of Euterpe oleracea Martius, evaluating their potential to serve as antioxidant agents. Firstly, we selected 16 flavonoids present in Euterpe oleracea Martius pulp and oil, and then their physicochemical properties were analyzed concerning the Lipinski's Rule of Five. Moreover, we evaluated their pharmacokinetic properties using the QikProp module of the Schrödinger software as well as their toxicity profile, using the DEREK software. Docking simulations, using the GOLD 4.1 software, as well as pharmacophoric hypotheses calculation of molecules were also performed. Flavonoids present in the açaí pulp including catechin, epicatechin, luteolin, chrisoeriol, taxifolin, apigenin, dihydrokaempferol, isovitexin, and vitexin presented good oral bioavailability. Regarding the pharmacokinetic properties, the compounds catechin, epicatechin, isovitexin, luteolin, chrisoeriol, taxifolin, and isorhamnetin rutinoside presented the best results, besides high human oral absorption. Regarding the prediction of toxicological properties, compounds isorhamnetin rutinoside and rutin presented mutagenicity for hydroxynaphthalene or derivate, and regarding the docking simulations, all the compounds investigated in this study presented key interactions with the corresponding targets. The flavonoids catechin, chrysoeriol, and taxifolin presented the best results according to the evaluation conducted in this study. These computational results can be used as a theoretical basis for future studies concerning the development of drug candidates, as well as to enlighten biological tests in vitro and in vivo, which can contribute to the treatment of neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease, and Huntington's disease.

Effects of Gambir leaves extract (Uncaria gambir Roxb.) in preventing the aging process inducted D-galactose on pancreas mice

Increasing level of reactive oxygen species (ROS) can damage the cell membrane and composition of DNA, leading to organ degeneration. Pancreas is among the organs that is sensitive to oxidative damage. Consumption of flavonoid-rich stuffs such as herbs, fruits and vegetables are believed to strengthen antioxidant capacity in the body in neutralizing free radicals. Gambir leaves have been used traditionally as remedies of various diseases. The most prominent active compounds in Gambir is flavonoid catechin which belongs to flavan-3-ols group. D-galactose is monosaccharide thatin high concentration can increase ROS generationand induce senescence in animal models. In this study, we aimed to observe the effect of Gambir leaves extract (GLE) in preventing ROS production and pancreas damage in galactose-induced mice model. Twenty-four female mice were divided into 4 groups amd injectedwith D-galactose 150 mg/kgBW intraperitoneally for 6 weeks. Three groups were supplemented with GLE 100; 200 and 400 mg/kgBW, respectively. Serum MDA, blood glucose and pancreas histopatology were analyzed. There is no significant difference among GLE-treated groups compared to control in the level of serum MDA (p=0,286), blood glucose fasting (p=0,051) and random (p=0,626), and pancreas histopathology: area of Langerhans islet (p=0,589) and perimeter of Langerhans islet (p=0,634). We did not found the histological damage in panreas. Interestingly, we found a trend increase in area, perimeter and cell number in Langerhans islet. Our data suggested a potential effect of GLE in increasing the growth of panreatic cells. Further study is necessary to elucidate the regenerative effect of GLE in damage pancreas such as streptozotocin-induced diabetes model.

Pharmacological actions of Tridax procumbens L.: A Scientific Review

Tridax procumbens L. (Asteraceae) is. known for several potential therapeutic activ'ities like antiviral, antibiotic efficacies, wound healing activity, insecticidal and anti-int'lammatory activity. The medicinal plants are the rich sources of natural remedies to treat the pathogenic and other diseases. Plant Tridax procumbens belongs to family Asteraceae one off. Plant is native of tropical America and naturalized in tropical Africa, Asia, and Australia. Local people known it as “Ghamara”, in English popularly called ‘coat buttons’ and is dispensed for “Bhringraj” by some of the practitioners of Ayurveda. The phytochemical screening revealed the presence of alkaloids, carotenoids, flavonoids (catechin and flavones), fumeric acid, fl-sitosterol, saponins and tannins. It is richly endowed with carotenoids, saponins, oleanolic acid and ions like calcium, magnesium, potassium, sodium and selenium. The extracts of Tridax procumbens have been used as indigenous medicine for a variety of ailments. It has been extensively used in Indian traditional medicine for wound healing, as anticoagulant, antifungal and insect repellent, in diarrhea and dysentery.

HPLC-DAD and HPLC-ESI-MS Analysis of Polyphenol-rich Extracts from Mango (&amp;lt;i&amp;gt;Mangifera indica&amp;lt;/i&amp;gt; L.), Tommy Atkins and Haden Varieties, Cultivated in Dominican Republic

Background: Antioxidant, anti-inflammatory, and analgesic effects of mango stem bark extracts (MSBE) have been reported. A previous published report described the identification of several components (polyphenols, polyols, and sugars) by HPLC, MS, and NMR. Mangiferin (2-β-D-glucopyranosyl-1,3,6,7-tetrahydroxyl-9H- xanthen-9-one) was identified as the major bioactive component of MSBE. However, MSBE has shown more potent effects than model mangiferin solutions in several in vitro experiments at different concentrations. Therefore, there are other extract components which contribute to the observed pharmacological effects. Objective: The identification of other polyphenolic components in MSBE, which may contribute to the observed pharmacological effects through a synergic pathway. Method: Polyphenol-rich extracts from mango stem bark and branch trees from two varieties (Haden and Tommy Atkins), cultivated in Dominican Republic, were analyzed by HPLC-DAD. Butanol MSBE extract from Haden mango stem bark was analyzed by HPLC-MS-ESI. Results: The mangiferin content in Haden mango extracts by HPLC-DAD was considerably high as compared to previous reports in the literature from other mango varieties. The identification of Haden mango stem bark butanolic extract components by HPLC-ESI-MS led to the unambiguous identification of 20 components: 2 benzoic acid derivatives, gallic acid and 8 gallate derivatives, 2 benzophenones (maclaurin and iriflophenone types), 3 flavonoids (catechin, epicatechin, and quercetin), mangiferin, isomangiferin, homomangiferin, and noratyriol. Conclusion: HPLC-ESI-MS analysis of the Haden mango SB extract showed the presence of many polyphenolic components, not previously reported, which may correlate to the antioxidant, anti-inflammatory, and/or analgesic effects of this extract mostly through a synergistic effect of its components. The potential exploitation of mango by-products from the Haden variety would be the best option for obtaining polyphenol-rich extracts from mango agricultural by-products to be used as bioactive ingredients in nutraceutical, cosmeceutical, and/or pharmaceutical formulations.

Structure of the flavonoid catechin in solution: NMR and quantum chemical investigations

DFT-PCM statistical index scan curves and 1H-NMR profiles reveal conformational changes when a solid catechin sample is dissolved in acetone solvent.

IN-VITRO AND IN-VIVO STUDIES OF THE POSSIBLE CHEMOPREVENTIVE FUNCTIONS OF SOYBEAN ISOFLAVONE AND FLAVONOIDS ON BREAST CANCER

Objectives: In this study, we assess the possible influence of soybean isoflavone (genistein) and other flavonoids (quercetin and catechin) on breast cancer chemoprevention. We design in-vitro and in-vivo experiments to analyze the effect of genistein, quercetin and catechin on cell proliferation, cell migration, and angiogenesis of breast cancer cells. Methods: In cell proliferation experiment, MCF-7 cells, SKBR-3 cells, and HUVEC cells were treated with genistein and other flavonoids (catechin and/or quercetin) for 48[Formula: see text]h to assess the influence on cell growth of normal and breast cancer cells. In cell motility test, we analyze the effect of isoflavone and flavonoids on migration ability of MCF-7 cells by 16[Formula: see text]h and SKBR-3 cells by 24[Formula: see text]h in two different concentrations (1.25[Formula: see text][Formula: see text]g/ml and 2.5[Formula: see text][Formula: see text]g/ml). In the in-vivo experiment, SKBR-3 cells mixed with PBS and catechin, respectively, were injected subcutaneously into nude mice, then we investigated the effect of catechin on cell growth by observing subcutaneous tumor size changes after 15 days. Results: The results suggest that genistein and quercetin can significantly inhibit proliferation of breast cancer cells, and their inhibitory effects are independent of estrogen receptor. In cell motility tests, all of the three phytochemicals were effective in the inhibition of cell migration on two breast cancer cell lines, except for quercetin on cell migration of SKBR-3 cell line. In the in-vitro experiment, catechin showed stimulatory effect on cell proliferation of HUVEC cell line, which may consider positive effect on angiogenesis, rather than inhibitory effect. However, in the in-vivo experiment, it showed no significant change in tumor size between the groups of with and without catechin treatment. Conclusions: According to our study, the results suggest that isoflavone and flavonoids tend to inhibit cell growth and metastasis of breast cancer cells. Our in-vivo experiment does not reach a significant result, and it may be due to lower catechin concentration. Under in-vivo environment, we should also consider the possible metabolic forms of catechin that cause different result from the in-vitro study.