PMID: 

Planta Med. 2012 Mar ;78(4):341-8. Epub 2012 Jan 13. PMID: 22399273

Abstract Title: 

Paeoniae radix reduces PDGF-stimulated hepatic stellate cell migration.

Abstract: 

Hepatic stellate cells (HSCs) play a key role in the pathogenesis of liver fibrosis. In chronic liver injury, HSCs undergo transdifferentiation to an activated myofibroblastic phenotype and migrate to injured areas in response to chemotactic factors, producing extracellular matrix proteins such as collagen type I to repair the damage as well as overexpression ofα-smooth muscle actin (α-SMA). Paeoniae Radix, the root of Paeonia lactiflora Pall, was investigated for PDGF-BB-induced HSC chemotaxis. Rat HSCs and LX-2, a human HSC cell line, were used for the in vitro experiments. Cell migration was analyzed by wound-healing and transwell assays. An ELISA anda Sircol collagen assay kit were used to detect the expressions of α-SMA and of collagen, respectively. Phosphorylations of mitogen-activated protein kinases, including ERK 1/2, p38, and JNK, were evaluated with immunoblotting. Results indicated that PDGF-BB increased migration as well as α-SMA and collagen expression in HSCs. Paeoniae Radix extracts and its active components, paeonol and 1,2,3,4,6-penta- O-galloyl- β-D-glucose (PGG), inhibited PDGF-BB-induced HSC migration and α-SMA and collagen expressions in a concentration-dependent manner. The inhibitory effects were associated withdownregulation of PDGF receptor- α, ERK, p38, and JNK activation. Both paeonol and PGG participate in HSC migration, but via differential mechanisms.

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PMID: 

Oncol Lett. 2016 Aug ;12(2):904-910. Epub 2016 Jun 9. PMID: 27446367

Abstract Title: 

Anti-tumor effect of Radix Paeoniae Rubra extract on mice bladder tumors using intravesical therapy.

Abstract: 

Radix Paeoniae Rubra (RPR) is the dried root ofPallas andLynch, and is a herbal medicine that is widely used in traditional Chinese medicine for the treatment of blood-heat and blood-stasis syndrome, similarly to Cortex Moutan. The present study identified the same three components in RPR and Cortex Moutan extracts. In addition, it has been reported that RPR has an anti-cancer effect. Bladder cancer is the seventh most common type of cancer worldwide. Due to the high recurrence rate, identifying novel drugs for bladder cancer therapy is essential. In the present study, RPR extract was evaluated as a bladder cancer therapyand. The present results revealed that RPR extract reduced the cell viability of bladder cancer cells with a half maximal inhibitory concentration of 1-3 mg/ml, and had an extremely low cytotoxic effect on normal urothelial cells. Additionally, RPR decreased certain cell cycle populations, predominantly cells in the G1 phase, and caused a clear sub-G increase. In a mouse orthotopic bladder tumor model, intravesical application of RPR extract decreased the bladder tumor size without altering the blood biochemical parameters of the mice. In summary, the present results demonstrate the anti-proliferative properties of RPR extract on bladder cancer cells, and its anti-bladder tumor effect. Compared to Cortex Moutan extract, RPR extract may provide a more effective alternative therapeutic strategy for the intravesical therapy of superficial bladder cancer.

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PMID: 

J Ethnopharmacol. 2020 Feb 17:112671. Epub 2020 Feb 17. PMID: 32081739

Abstract Title: 

Anti-influenza virus phytochemicals from Radix Paeoniae Alba and characterization of their neuraminidase inhibitory activities.

Abstract: 

ETHNOPHARMACOLOGICAL RELEVANCE: Bai Shao (Radix Paeoniae Alba, BS) is the root of Paeonia lactiflora Pall. in ancient China for Wen Bing (Warm Disease) treatment. Wen Bing has the symptoms of influenza. Ethanol extract of the root has recently been shown to possess anti-influenza activity. However, the active compounds have not yet been identified.AIM: We showed that BS aqueous extract was potent in inhibiting influenza A virus in infected cells. We aimed to isolate the bioactive compounds and characterize the anti-influenza mechanism.MATERIALS AND METHODS: Plaque reduction bioassay-guided assay was performed for fractions isolated from BS. Hemagglutination inhibition assay and neuraminidase inhibition assay were performed to find the target protein. Molecular docking and reverse genetics were used to confirm the action site of gallic acid on the neuraminidase protein.RESULTS: We identified three tannin compounds gallic acid (GA), methyl gallate (MG) and pentagalloylglucose (PGG) in BS aqueous extract that could inhibit the replication of influenza A virus in MDCK cells. While only PGG was found to inhibit the influenza virus-induced hemagglutination of chicken red blood cells, all three compounds significantly reduced the activity of the neuraminidase. The results from molecular docking and reverse genetics showed that GA interacted with Arg152 of neuraminidase protein.CONCLUSION: Three compounds GA, MG and PGG isolated from Bai Shao were found to inhibit influenza A virus in MDCK cells. GA interacts with aa Arg152 of the viral neuraminidase. Our study identified anti-influenza compounds of BS and demonstrated their antiviral mechanism, thus providing scientific evidence for using this herb for clinical treatment.

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PMID: 

Exp Gerontol. 2020 Feb 18:110881. Epub 2020 Feb 18. PMID: 32084535

Abstract Title: 

Oral gallic acid improve liver steatosis and metabolism modulating hepatic lipogenic markers in obese mice.

Abstract: 

INTRODUCTION: Gallic acid (GA) is a natural endogenous polyphenol found in a variety of fruits, vegetables and wines, with beneficial effects on the energetic homeostasis.AIM: The present study aimed to investigate oral gallic acid effects on liver steatosis and hepatic lipogenesis markers in obese mice evaluating new possible molecular related mechanisms.METHODS: Twenty-four Swiss male mice were divided into four groups and fed for 60 days with standard diet (ST), standard diet plus gallic acid (ST + GA), high-fat diet (HFD), and high-fat diet plus gallic acid (HFD + GA). We evaluated the relationship between body weight, food intake and serum levels of total cholesterol, triglycerides, insulin, aspartate and alanine transaminases. Liver histology was analyzed by hematoxylin and eosin staining. These results were accompanied by bioinformatics analyses. The acetyl-CoA carboxylase (ACC), sterol regulatory element binding protein-1 (SREBP-1) and fatty acid synthase (FAS) expression was assessed by quantitative real-time reverse transcriptase PCR (qRT-PCR).RESULTS: The main findings of the present study showed that GA reduced liver steatosis, body weight and plasma insulin levels. Analyzes of hepatic steatosis related genes expression showed that ACC and FAS mRNA were significantly suppressed in liver of HFD + GA mice. These data was corroborated by bioinformatics analysis.CONCLUSION: These data suggest an important clinical application of GA in the prevention of liver diseases.

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PMID: 

Pharmacol Res. 2011 Jul ;64(1):31-5. Epub 2011 Feb 22. PMID: 21349333

Abstract Title: 

Soluble fiber-enriched diets improve inflammation and oxidative stress biomarkers in Zucker fatty rats.

Abstract: 

In this study we evaluated the effect of the administration of different soluble fiber enriched-diets on inflammatory and redox state of Zucker fatty rats. Four groups of ten 8 week-old female Zucker fatty rats were used. The four groups were respectively fed the following diets until the 15th week of life: standard diet (obese control), 10% high methoxylated apple pectin (HMAP)-, 5% soluble cocoa fiber (SCF)-, and 10%β-glucan-enriched diets. A group of Zucker lean rats fed the standard diet was also used as control for normal values of this rat strain. The plasma levels of tumoral necrosis factor-α (TNF-α), adiponectin, and malondialdehyde (MDA) were measured at the end of treatment. The reduced glutathione liver levels were also obtained at that moment. TNF-α plasma levels decreased somewhat in Zucker fatty rats fed the different fibers, and MDA plasma levels significantly decreased in these animals. Nevertheless, adiponectin plasma levels increased in the Zucker fatty rats fed the SCF enriched diet,but did not change in the HMAP and the β-glucan group. The Zucker fatty rats fed the different fiber showed a trend towards increased the reduced glutathione liver levels, but significant differences with obese control rats were only obtained in the β-glucan group. The results obtained in this study suggest that the intake of the different soluble fiber-enriched diets that we have evaluated could prevent and/or attenuate the inflammatory and/or the prooxidative state of the metabolic syndrome.

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PMID: 

Eur J Nutr. 2013 Oct ;52(7):1743-53. Epub 2012 Dec 11. PMID: 23229409

Abstract Title: 

Consumption of a highβ-glucan barley flour improves glucose control and fatty liver and increases muscle acylcarnitines in the Zucker diabetic fatty rat.

Abstract: 

PURPOSE: The soluble fiberβ-glucan, a natural component of barley, has been shown to lower the postprandial glucose response and is thought to improve insulin resistance.METHODS: This study examined the effect of chronic consumption of the highβ-glucan barley flour on glucose control, liver lipids and markers of muscle fatty acid oxidation in the Zucker diabetic fatty (ZDF) rat. Two groups of ZDF rats were fed diets containing either 6% β-glucan in the form of barley flour or cellulose as a control for 6 weeks. A group of Zucker lean rats served as a negative control.RESULTS: The barley flour group had an increased small intestinal contents viscosity compared to the obese control group. After 6 weeks, the barley flour group had reduced glycated hemoglobin, lower relative kidney weights and a reduced area under the curve during a glucose tolerance test, indicating improved glucose control. Fasting plasma adiponectin levels increased in the barley flour group and were not different than the lean control group. ZDF rats on the barley flour diet had lower relative epididymal fat pad weights than the obese control and a greater food efficiency ratio. The barley flour group also had reduced liver weights and a decreased concentration of liver lipids. The barley flour group had significantly higher concentrations of muscle acylcarnitines, a metabolite generated during fatty acid oxidation.CONCLUSION: These results show that chronic consumption ofβ-glucans can improve glucose control and decrease fatty liver in a model of diabetes with obesity.

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PMID: 

Nutr Rev. 2019 Oct 22. Epub 2019 Oct 22. PMID: 31638148

Abstract Title: 

Effects of oats on gastrointestinal health as assessed by in vitro, animal, and human studies.

Abstract: 

Oats are uniquely nutritious, owing to their composition of bioactive compounds, lipids, andβ-glucan. Scientific research has established that oats can improve diet quality, reduce cholesterol, regulate satiety, and protect against carcinogenesis in the colon; however, determining the effects of oats on gastrointestinal health and the gut microbiome is a newer, evolving area of research.To better understand the effects of oats on gastrointestinal health in humans, a literature review with predefined search criteria was conducted using the PubMed database and keywords for common gastrointestinal health outcomes. Moreover, to examine the gastrointestinal effects of oats across the scientific spectrum, a similar search strategy was executed to identify animal studies. In vitro studies were identified from the reference lists of human and animal studies. A total of 8 human studies, 19 animal studies, and 5 in vitro studies met the inclusion criteria for this review. The evidencein humans shows beneficial effects of oats on gastrointestinal health, with supportive evidence provided by in vitro and animal studies. The effective dose of oats varies by type, although an amount providing 2.5 to 2.9 g of β-glucan per day was shown to decrease fecal pH and alter fecal bacteria.For oat bran, 40 to 100 g/d was shown to increase fecal bacterial mass and short-chain fatty acids in humans. Differences in study design, methodology, and type of oats tested make valid comparisons difficult. The identification of best practices for the design of oat studies should be a priorityin future research, as the findings will be useful for determining how oats influence specific indices of gastrointestinal health, including the composition of the human gut microbiome.

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PMID: 

Front Nutr. 2019 ;6:171. Epub 2019 Nov 27. PMID: 31828074

Abstract Title: 

The Cholesterol-Lowering Effect of Oats and Oat Beta Glucan: Modes of Action and Potential Role of Bile Acids and the Microbiome.

Abstract: 

Consumption of sufficient quantities of oat products has been shown to reduce host cholesterol and thereby modulate cardiovascular disease risk. The effects are proposed to be mediated by the gel-forming properties of oatβ-glucan which modulates host bile acid and cholesterol metabolism and potentially removes intestinal cholesterol for excretion. However, the gut microbiota has emerged as a major factor regulating cholesterol metabolism in the host. Oat β-glucan has been shown to modulate the gut microbiota, particularly those bacterial species that influence host bile acid metabolism and production of short chain fatty acids, factors which are regulators of host cholesterol homeostasis. Given a significant role for the gut microbiota in cholesterol metabolism it is likely that the effects of oat β-glucanon the host are multifaceted and involve regulation of microbe-host interactions at the gut interface. Here we consider the potential for oat β-glucan to influence microbial populations in the gut with potential consequences for bile acid metabolism, reverse cholesterol transport (RCT), short-chainfatty acid (SCFA) production, bacterial metabolism of cholesterol and microbe-host signaling.

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PMID: 

Molecules. 2019 Dec 23 ;25(1). Epub 2019 Dec 23. PMID: 31877995

Abstract Title: 

Effect of the Modifications on the Physicochemical and Biological Properties ofβ-Glucan-A Critical Review.

Abstract: 

β-Glucan exhibits many biological activities and functions such as stimulation of the immune system and anti-inflammatory, anti-microbial, anti-infective, anti-viral, anti-tumor, anti-oxidant, anti-coagulant, cholesterol-lowering, radio protective, and wound healing effects. It has a wide variety of uses in pharmaceutical, cosmetic, and chemical industries as well as in food processing units. However, due to its dense triple helix structure, formed by the interaction of polyhydroxy groups in the β-d-glucan molecule, it features poor solubility, which not only constrains its applications, butalso inhibits its physiological function in vivo. One aim is to expand the applications for modified β-glucan with potential to prevent disease, various therapeutic purposes and as health-improving ingredients in functional foods and cosmetics. This review introduces the major modification methodsrequired to understand the bioactivity of β-glucan and critically provides a literature survey on the structural features of this molecule and reported biological activity. We also discuss a new method to create novel opportunities to exploit maximally various properties of β-glucan, namely ultrasound-assisted enzymatic modification.

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PMID: 

Pharmaceutics. 2019 Dec 20 ;12(1). Epub 2019 Dec 20. PMID: 31861805

Abstract Title: 

Utilizing Liposomal Quercetin and Gallic Acid in Localized Treatment of VaginalInfections.

Abstract: 

Vulvovaginal candidiasis (VVC) is a widely spread fungal infection that causes itching, pain and inflammation at the vaginal site. Although common, currently available treatment suffers from limited efficacy and high recurrence. In addition, the growing problem of resistance to azole drugs used in current treatments emphasizes the need for superior treatment options. Antimicrobial polyphenols are an attractive approach offering multitargeting therapy. We aimed to develop novel liposomes for simultaneous delivery of two polyphenols (quercetin, Q, and gallic acid, GA) that, when released within the vaginal cavity, act in synergy to eradicate infection while alleviating the symptoms of VVC. Q was selected for its anti-itching and anti-inflammatory properties, while GA for its reported activity against. Novel liposomes containing only Q (LP-Q), only GA (LP-GA) or both polyphenols (LP-Q+GA) were in the size range around 200 nm. Q was efficiently entrapped in both LP-Q and in LP-Q+GA (85%) while the entrapment of GA was higher in LP-Q+GA (30%) than in LP-GA (25%). Liposomes, especially LP-Q+GA, promoted sustained release of both polyphenols. Q and GA acted in synergy, increasing the antioxidant activities of a single polyphenol. Polyphenol-liposomes were not cytotoxic and displayed stronger anti-inflammatory effects than free polyphenols. Finally, LP-GA and LP-Q+GA considerably reducedgrowth.

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