• Journal of Pharmacopuncture
• /
• v.26 no.1
• /
• pp.27-37
• /
• 2023

Objectives: Moroccan Arbutus unedo is an essential medicinal plant; however, little is known about the biological properties of its leaves mentioned in Moroccan traditional medicine. Methods: Various standard experiments were performed to evaluate the phytochemical, antidiabetic, antioxidant, antibacterial, and acute and sub-chronic toxicity characteristics of A. unedo leaves. Results: Phytochemical screening led to the identification of several phytochemical classes, including tannins, flavonoids, terpenoids, and anthraquinones, with high concentrations of polyphenols (31.83 ± 0.29 mg GAEs/g extract) and flavonoids (16.66 ± 1.47 mg REs/g extract). Further, the mineral analysis revealed high levels of calcium and potassium. A. unedo extract demonstrated significant antioxidant and anti-diabetic activities by inhibiting α-amylase (1.350 ± 0.32 g/mL) and α-glucosidase (0.099 ± 1.21 g/mL) compared to the reference drug Acarbose. Also, the methanolic extract of the plant exhibited significantly higher antibacterial activity than the aqueous extract. Precisely, three of the four examined bacterial strains exhibited substantial susceptibility to the methanolic extract . Minimum bactericidal concentration (MBC)/minimum inhibitory concentration (MIC) values indicated that A. unedo harbor abundant bactericidal compounds. For toxicological studies, mice were administered with A. unedo aqueous extract at single doses of 2,000 and 5,000 mg/kg. They did not exhibit significant abnormal behavior, toxic symptoms, or death during the 14-day acute toxicity test and the 90-day sub-chronic toxicity test periods. The general behavior, body weight, and hematological and biochemical status of the rats were assessed, revealing no toxicological symptoms or clinically significant changes in biological markers observed in the mice models, except hypoglycemia, after 90 days of daily dose administration. Conclusion: The study highlighted several biological advantages of A. unedo leaves without toxic effects in short-term application. Our findings suggest that conducting more comprehensive and extensive in vivo investigations is of utmost importance to identify molecules that can be formulated into pharmaceuticals in the future.

• Korean Journal of Clinical Laboratory Science
• /
• v.55 no.3
• /
• pp.174-183
• /
• 2023

Antioxidant, cytotoxic, and anti-inflammatory assays were conducted to determine the commercial viability of Brachythecium populeum. The antioxidant activity was assessed by performing the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. This was followed by the quantification of polyphenols and flavonoids. Results of the DPPH and ABTS assay showed that antioxidant activities of the ethanol extract of B. populeum were 3.7 and 3.6 times higher than water extract, respectively. The polyphenol concentration was also determined to be 4.1 times higher and the flavonoid concentration was 5.3 times higher than the water extract. The cell-based experiments, 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT) assay and nitric oxide assay, were performed using RAW 264.7. Results of the MTT assay revealed that both extracts exerted no cytotoxicity on the cells (based on 80% viability). In the nitric oxide (NO) production inhibition experiment, inhibition of NO production was determined to be 15.42% more when exposed to ethanol extract as compared to water extract. Furthermore, the ethanol extract exerted greater inhibition of inflammatory cytokines interleukin (IL)-1β, IL-6, and tumor necrosis factor-α production (9.39%, 11.87%, and 14.49% more, respectively) when compared to the water extract. Due to the good antioxidant activity and potential for inhibiting NO and inflammatory cytokine production, B. populeum ethanol extracts are prospective sources of anti-inflammatory compounds.

• Asia-pacific Journal of Multimedia Services Convergent with Art, Humanities, and Sociology
• /
• v.7 no.1
• /
• pp.395-405
• /
• 2017

To confirm potential anti-cancer activities of ethylacetate (EtOAc) fraction from Orostachys japonicus on the A549 human lung cancer cells, this study examined. As a result of conducting MTS assay for measuring cell viability, the EtOAc fraction inhibited the proliferation of A549 cells in a dose-dependent manner. To investigate whether the inhibiting A549 cell viability was caused by apoptosis, this study analyzed chromatin condensation in A549 cells using DAPI staining. The morphological changes such as the formation of nuclear condensation were formed in a dose-dependent manner. Also, this study performed Annexin V-FITC staining for detecting phosphatidylinositol (PS). As a result of Annexin V-FITC staining to investigate level of early and late apoptosis, the apoptosis level treated with EtOAc fraction was higher than that of control. RT-PCR was performed to study the correlation between G2/M cell cycle arrest and cell cycle control genes. The anti-cancer activity of EtOAc fraction was accompanied by inhibition of CDK1, 4, cyclin B1 and D1 mRNA. This study also examined the expression of various marker proteins: p53, Bax, Bcl-2 and pro-caspase 3. Western blotting revealed that p53 and Bax proteins were up-regulated, and Bcl-2 and pro-caspase 3 proteins down-regulated in a time and dose-dependent manner.

• Animal Bioscience
• /
• v.35 no.10
• /
• pp.1461-1478
• /
• 2022

The maintenance of poultry gut health is complex depending on the intricate balance among diet, the commensal microbiota, and the mucosa, including the gut epithelium and the superimposing mucus layer. Changes in microflora composition and abundance can confer beneficial or detrimental effects on fowl. Antibiotics have devastating impacts on altering the landscape of gut microbiota, which further leads to antibiotic resistance or spread the pathogenic populations. By eliciting the landscape of gut microbiota, strategies should be made to break down the regulatory signals of pathogenic bacteria. The optional strategy of conferring dietary fibers (DFs) can be used to counterbalance the gut microbiota. DFs are the non-starch carbohydrates indigestible by host endogenous enzymes but can be fermented by symbiotic microbiota to produce short-chain fatty acids (SCFAs). This is one of the primary modes through which the gut microbiota interacts and communicate with the host. The majority of SCFAs are produced in the large intestine (particularly in the caecum), where they are taken up by the enterocytes or transported through portal vein circulation into the bloodstream. Recent shreds of evidence have elucidated that SCFAs affect the gut and modulate the tissues and organs either by activating G-protein-coupled receptors or affecting epigenetic modifications in the genome through inducing histone acetylase activities and inhibiting histone deacetylases. Thus, in this way, SCFAs vastly influence poultry health by promoting energy regulation, mucosal integrity, immune homeostasis, and immune maturation. In this review article, we will focus on DFs, which directly interact with gut microbes and lead to the production of SCFAs. Further, we will discuss the current molecular mechanisms of how SCFAs are generated, transported, and modulated the pro-and anti-inflammatory immune responses against pathogens and host physiology and gut health.

• Research in Plant Disease
• /
• v.29 no.4
• /
• pp.390-398
• /
• 2023

Apple white rot, caused by Botryosphaeria dothidea, is one of the important diseases in Korea. B. dothidea can cause pre- and postharvest decay on apple fruit as well as canker and dieback of apple trees. In this study, we isolated bacteria from the trunk of apple trees and tested their antagonistic activity against B. dothidea. Five bacterial isolates (23-168, 23-169, 23-170, 23-172, and 23-173) were selected that were most effective at inhibiting the mycelial growth of the pathogens. The isolate 23-172 was identified as Bacillus amyloliquefaciens and four isolates 23-168, 23-169, 23-170, and 23-173 were identified as Bacillus velezensis by RNA polymerase beta subunit (rpoB) and DNA gyraseA subunit (gyrA) gene sequencing. All isolates showed strong antagonistic activity against B. dothidiea as well as Colletotrichum fructicola and Diaporthe eres. All isolates exhibited cellulolytic, proteolytic and phosphate solubilizing activities. In particular, two isolates 23-168, 23-169 were shown to significantly reduce the size of white rot lesions in pretreated apple fruits. These results will provide the basis for the development of a fungicide alternative for the control of white rot of apple.

• Biomolecules & Therapeutics
• /
• v.32 no.3
• /
• pp.329-340
• /
• 2024

Mangiferin is a kind of natural xanthone glycosides and is known to have various pharmacological activities. However, since the beneficial efficacy of this compound has not been reported in retinal pigment epithelial (RPE) cells, this study aimed to evaluate whether mangiferin could protect human RPE ARPE-19 cells from oxidative injury mimicked by hydrogen peroxide (H₂O₂). The results showed that mangiferin attenuated H₂O₂-induced cell viability reduction and DNA damage, while inhibiting reactive oxygen species (ROS) production and preserving diminished glutathione (GSH). Mangiferin also antagonized H₂O₂-induced inhibition of the expression and activity of antioxidant enzymes such as manganese superoxide dismutase and GSH peroxidase, which was associated with inhibition of mitochondrial ROS production. In addition, mangiferin protected ARPE-19 cells from H₂O₂-induced apoptosis by increasing the Bcl-2/Bax ratio, decreasing caspase-3 activation, and blocking poly(ADP-ribose) polymerase cleavage. Moreover, mangiferin suppressed the release of cytochrome c into the cytosol, which was achieved by interfering with mitochondrial membrane disruption. Furthermore, mangiferin increased the expression and activity of heme oxygenase-1 (HO-1) and nuclear factor-erythroid-2 related factor 2 (Nrf2). However, the inhibition of ROS production, cytoprotective and anti-apoptotic effects of mangiferin were significantly attenuated by the HO-1 inhibitor, indicating that mangiferin promoted Nrf2-mediated HO-1 activity to prevent ARPE-19 cells from oxidative injury. The results of this study suggest that mangiferin, as an Nrf2 activator, has potent ROS scavenging activity and may have the potential to protect oxidative stress-mediated ocular diseases.

• Journal of Applied Biological Chemistry
• /
• v.66
• /
• pp.369-378
• /
• 2023

Smilax sieboldii is one of the Smilax species. A number of Smilax plants have multiple physiologically-active components and anti-inflammatory/anti-oxidant effects. Antiobesity effects induced by Smilax sieboldii have not been reported. In this study, we investigated the effects and molecular mechanisms of anti-obesity activity of 70% ethanol Smilax sieboldii extract (SSE). The anti-obesity effect of SSE was determined using 3T3-L1 adipocytes. We confirmed that SSE was not cytotoxic to murine 3T3-L1 preadipocytes, we evaluated SSE dose-dependently decreased the accumulation of lipids via an Oil Red O assay and triglyceride assay. These anti-obesity activities of SSE were mediated by the inhibition of adipogenesis-related marker genes (peroxisome proliferator activated receptor-γ, CCAAT-enhancer-binding protein α, and SREBP1c) and lipogenesis-related marker genes (fatty acid synthase and aP2). These results suggest that SSE has the potential to exert anti-obesity and anti-hyperlipidemia effects by regulating adipogenic transcription factors and inhibiting the expression of adipogenic markers.

• Journal of Life Science
• /
• v.34 no.9
• /
• pp.656-665
• /
• 2024

Enzymes, as proteins that regulate various metabolic processes within the human body, play a crucial role in maintaining health. However, the overexpression of certain enzymes can disrupt metabolic balance, leading to various diseases. Enzyme inhibitors are vital in treating these diseases or conditions by inhibiting the action of these enzymes, making them indispensable in the development of effective therapies for a wide array of diseases. Quercetin, a natural product derived from plants, is a type of flavonoid that belongs to the polyphenol family. Quercetin, a natural flavonoid from the polyphenol family, has emerged as a potent enzyme inhibitor. This low-molecular-weight secondary metabolite is known for its inhibitory effects on enzymes such as α-glucosidase, acetylcholinesterase, bacterial neuraminidase, and xanthine oxidase due to its structural advantages. Quercetin is isolated from biomaterials and can be classified into glycosylated, methoxylated, and alkylated derivatives based on its structural variations. These natural quercetin derivatives possess unique substituents that enable specific binding patterns with catalytic residues in enzyme active sites. Therefore, quercetin derivatives can be expected to have better enzyme inhibitory activity than basic quercetin. Due to their specificity and enhanced activity, quercetin and its derivatives hold promise as candidates for developing potent enzyme inhibitors to treat diseases resulting from enzyme imbalances.

• Molecular Medicine Reports
• /
• v.20 no.4
• /
• pp.3709-3718
• /
• 2019

Chronic pancreatitis (CP) is characterized by recurrent pancreatic injury, resulting in inflammation and fibrosis. Currently, there are no drugs for the treatment of pancreatic fibrosis associated with CP. Piperine, a natural alkaloid found in black pepper, has been reported to show anti-inflammatory, anti-oxidative, and antitumor activities. Although piperine exhibits numerous properties in regards to the regulation of diverse diseases, the effects of piperine on CP have not been established. To investigate the effects of piperine on CP in vivo, we induced CP in mice through the repetitive administration of cerulein (50 ㎍/kg) six times at 1-h intervals, 5 times per week, for a total of 3 weeks. In the pre-treatment groups, piperine (1, 5, or 10 mg/kg) or corn oil were administrated orally at 1 h before the first cerulein injection, once a day, 5 times a week, for a total of 3 weeks. In the post-treatment groups, piperine (10 mg/kg) or corn oil was administered orally at 1 or 2 week after the first cerulein injection. Pancreases were collected for histological analysis. In addition, pancreatic stellate cells (PSCs) were isolated to examine the anti-fibrogenic effects and regulatory mechanisms of piperine. Piperine treatment significantly inhibited histological damage in the pancreas, increased the pancreatic acinar cell survival, reduced collagen deposition and reduced pro-inflammatory cytokines and chemokines. In addition, piperine treatment reduced the expression of fibrotic mediators, such as α-smooth muscle actin (α-SMA), collagen, and fibronectin 1 in the pancreas and PSCs. Moreover, piperine treatment reduced the production of transforming growth factor (TGF)-β in the pancreas and PSCs. Furthermore, piperine treatment inhibited TGF-β-induced pSMAD2/3 activation but not pSMAD1/5 in the PSCs. These findings suggest that piperine treatment ameliorates pancreatic fibrosis by inhibiting TGF-β/SMAD2/3 signaling during CP.

• Journal of Nutrition and Health
• /
• v.42 no.1
• /
• pp.14-22
• /
• 2009

This study was conducted to investigate the effects of powdered young barley leaf and its water extract on body weight and lipid metabolism in high-fat fed mice. Male mice were divided into normal group, high-fat (HF) group, high-fat group supplemented with powdered young barley leaf (HF-YBL) and high-fat group supplemented with water extract of the powdered young barley leaf (HF-WYBL). The powdered young barley leaf or its water extract was added to a standard diet based on 1% dried young barley leaf (1 g YBL/100 diet and 0.28 g WYBL/100 g diet) for 8 weeks. Supplementation of YBL and WYBL significantly reduced body weight and epididymal adipose tissue weight in high-fat fed mice. Food intake and daily energy intake were significantly lower in the YBL group than in the HF group. After 8 weeks, plasma triglyceride and cholesterol concentrations were significantly higher in the HF group than in the Normal group; however, both YBL and WYBL significantly lowered those of the high-fat fed mice. The ratio of HDL-cholesterol/total cholesterol of the YBL and WYBL groups were significantly elevated compared to that of HF group. Both YBL and WYBL significantly increased fecal excretion of triglyceride in high-fat fed mice, whereas they did not affect fecal cholesterol concentration. The triglyceride levels of liver, adipose tissue and heart were significantly lower in the YBL and WYBL groups than in the HF group. Supplementation of WYBL also lowered the kidney triglyceride and heart cholesterol concentrations compared to those of HF group. Hepatic lipid regulating enzyme activities, fatty acid synthase, HMG-CoA reductase and acyl-coenzyme A: cholesterol acyltransferase, were significantly lower in the YBL and WYBL groups than in the HF group. Accordingly, these results suggest that YBL and WYBL improve plasma and organ lipid levels partly by increasing fecal lipid excretion and inhibiting fatty acid and cholesterol biosynthesis in the liver.