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14 pages, 309 KiB

Open AccessArticle

Tea as a Source of Biologically Active Compounds in the Human Diet

by Joanna Klepacka, Elżbieta Tońska, Ryszard Rafałowski, Marta Czarnowska-Kujawska and Barbara Opara

Molecules 2021, 26(5), 1487; https://doi.org/10.3390/molecules26051487 - 09 Mar 2021

Cited by 24 | Viewed by 3604

Abstract

Due to the different levels of bioactive compounds in tea reported in the literature, the aim of this study was to determine whether commercially available leaf teas could be an important source of phenolics and selected minerals (copper, manganese, iron, zinc, magnesium, calcium, [...] Read more.

Due to the different levels of bioactive compounds in tea reported in the literature, the aim of this study was to determine whether commercially available leaf teas could be an important source of phenolics and selected minerals (copper, manganese, iron, zinc, magnesium, calcium, sodium, potassium) and if the differences in the content of these components between various types of tea are significant. It was found that both the amount of these compounds in tea and the antioxidant activity of tea infusions were largely determined by the origin of tea leaves as well as the processing method, which can modify the content of the studied components up to several hundred-fold. The group of green teas was the best source of phenolic compounds (110.73 mg/100 mL) and magnesium (1885 µg/100 mL) and was also characterised by the highest antioxidant activity (59.02%). This type of tea is a great contributor to the daily intake of the studied components. The average consumption of green tea infusions, assumed to be 3–4 cups (1 L) a day, provides the body with health-promoting polyphenol levels significantly exceeding the recommended daily dose. Moreover, drinking one litre of an unfermented tea infusion provides more than three times the recommended daily intake of manganese. Tea infusions can be a fairly adequate, but only a supplementary, source of potassium, zinc, magnesium, and copper in the diet. Moreover, it could be concluded that the antioxidant activity of all the analysed types of tea infusions results not only from the high content of phenolic compounds and manganese but is also related to the presence of magnesium and potassium. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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14 pages, 3001 KiB

Open AccessArticle

Betulinic Acid Protects DOX-Triggered Cardiomyocyte Hypertrophy Response through the GATA-4/Calcineurin/NFAT Pathway

by Jung Joo Yoon, Chan Ok Son, Hye Yoom Kim, Byung Hyuk Han, Yun Jung Lee, Ho Sub Lee and Dae Gill Kang

Molecules 2021, 26(1), 53; https://doi.org/10.3390/molecules26010053 - 24 Dec 2020

Cited by 19 | Viewed by 3119

Abstract

Cardiac hypertrophy is a major risk factor for heart failure and leads to cardiovascular morbidity and mortality. Doxorubicin (DOX) is regarded as one of the most potent anthracycline antibiotic agents; however, its clinical usage has some limitations because it has serious cardiotoxic side [...] Read more.

Cardiac hypertrophy is a major risk factor for heart failure and leads to cardiovascular morbidity and mortality. Doxorubicin (DOX) is regarded as one of the most potent anthracycline antibiotic agents; however, its clinical usage has some limitations because it has serious cardiotoxic side effects such as dilated cardiomyopathy and congestive heart failure. Betulinic acid (BA) is a pentacyclic-cyclic lupane-type triterpene that has been reported to have anti-bacterial, anti-inflammatory, anti-vascular neogenesis, and anti-fibrotic effects. However, there is no study about its direct effect on DOX induced cardiac hypertrophy and apoptosis. The present study aims to investigate the effect of BA on DOX-induced cardiomyocyte hypertrophy and apoptosis in vitro in H9c2 cells. The H9c2 cells were stimulated with DOX (1 µM) in the presence or absence of BA (0.1–1 μM) and incubated for 24 h. The results of the present study indicated that DOX induces the increase cell surface area and the upregulation of hypertrophy markers including atrial natriuretic peptide (ANP), B-type natriuretic peptide (BNP), beta-myosin heavy chain (β-MHC), and Myosin Light Chain-2 (MLC2) in H9c2 cells. However, the pathological hypertrophic responses were downregulated after BA treatment. Moreover, phosphorylation of JNK, ERK, and p38 in DOX treated H9c2 cells was blocked by BA. As a result of measuring the change in ROS generation using DCF-DA, BA significantly inhibited DOX-induced the production of intracellular reactive oxygen species (ROS) when BA was treated at a concentration of over 0.1 µM. DOX-induced activation of GATA-4 and calcineurin/NFAT-3 signaling pathway were remarkably improved by pre-treating of BA to H9c2 cells. In addition, BA treatment significantly reduced DOX-induced cell apoptosis and protein expression levels of Bax and cleaved caspase-3/-9, while the expression of Bcl-2 was increased by BA. Therefore, BA can be a potential treatment for cardiomyocyte hypertrophy and apoptosis that lead to sudden heart failure. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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10 pages, 2461 KiB

Open AccessArticle

Activity of Pterostilbene Metabolites against Liver Steatosis in Cultured Hepatocytes

by Jenifer Trepiana, Stéphanie Krisa and María Puy Portillo

Molecules 2020, 25(22), 5444; https://doi.org/10.3390/molecules25225444 - 20 Nov 2020

Cited by 6 | Viewed by 2496

Abstract

Pterostilbene is a dimethyl ether derivative of resveratrol, less metabolized than its analogue, due to the substitution of two hydroxyl groups with methoxyl groups. Nevertheless, the amounts of pterostilbene phase II metabolites found in plasma and tissues are higher than those of the [...] Read more.

Pterostilbene is a dimethyl ether derivative of resveratrol, less metabolized than its analogue, due to the substitution of two hydroxyl groups with methoxyl groups. Nevertheless, the amounts of pterostilbene phase II metabolites found in plasma and tissues are higher than those of the parent compound. The first aim of this study was to assess whether pterostilbene-4′-O-glucuronide (PT-G) and pterostilbene-4′-O-sulfate (PT-S) were able to prevent triglyceride accumulation in AML12 (alpha mouse liver 12) hepatocytes. This being the case, we aimed to analyze the mechanisms involved in their effects. For this purpose, an in vitro model mimicking the hepatocyte situation in fatty liver was developed by incubating mouse AML12 hepatocytes with palmitic acid (PA). For cell treatments, hepatocytes were incubated with 1, 10 or 25 µM of pterostilbene, pterostilbene-4′-O-glucuronide or pterostilbene-4′-O-sulfate for 18 h. Triglycerides and cell viability were assessed by a commercial kit and crystal violet assay, respectively. Protein expression of enzymes and transporters involved in triglyceride metabolism was analyzed by immunoblot. The results showed for the first time the anti-steatotic effect of pterostilbene metabolites and thus, that they contribute to the preventive effect induced by pterostilbene on steatosis in in vivo models. This anti-steatotic effect is mainly due to the inhibition of de novo lipogenesis. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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11 pages, 2979 KiB

Open AccessArticle

Rose (Rosa gallica) Petal Extract Suppress Proliferation, Migration, and Invasion of Human Lung Adenocarcinoma A549 Cells through via the EGFR Signaling Pathway

by Won-Chul Lim, Hyo-Kyung Choi, Kyung-Tack Kim and Tae-Gyu Lim

Molecules 2020, 25(21), 5119; https://doi.org/10.3390/molecules25215119 - 04 Nov 2020

Cited by 9 | Viewed by 2862

Abstract

We sought to investigate the effect of rose petal extract (RPE) on the proliferation, migration, and invasion of cancer cells. RPE significantly inhibited the growth of lung and colorectal cancer cell lines, with rapid suppression of A549 lung cancer cells at low concentrations. [...] Read more.

We sought to investigate the effect of rose petal extract (RPE) on the proliferation, migration, and invasion of cancer cells. RPE significantly inhibited the growth of lung and colorectal cancer cell lines, with rapid suppression of A549 lung cancer cells at low concentrations. These effects occurred concomitantly with downregulation of the cell proliferation mediators PCNA, cyclin D1, and c-myc. In addition, RPE suppressed the migration and invasion of A549 cells by inhibiting the expression and activity of matrix metalloproteinase-2 and matrix metalloproteinase-9 (MMP-2 and -9). We hypothesize that the suppressive activity of RPE against lung cancer cell proliferation and early metastasis occurs via the EGFR-MAPK and mTOR-Akt signaling pathways. These early results highlight the significant potency of RPE, particularly for lung cancer cells, and warrant further investigation. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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11 pages, 1472 KiB

Open AccessArticle

Influence of Nanoencapsulation Using High-Pressure Homogenization on the Volatile Constituents and Anticancer and Antioxidant Activities of Algerian Saccocalyx satureioides Coss. et Durieu

by Abdelhakim Aouf, Hatem Ali, Abdel Rahman Al-Khalifa, Khaled Fahmy Mahmoud and Amr Farouk

Molecules 2020, 25(20), 4756; https://doi.org/10.3390/molecules25204756 - 16 Oct 2020

Cited by 14 | Viewed by 2373

Abstract

The nanoencapsulation of essential oils enhances their applicability in several areas, such as pharmaceuticals and food biopreservation. This study focuses on the encapsulation of Saccocalyx satureioides Coss. et Durieu essential oil into nanoemulsions by high-pressure homogenization (HPH) and its effect on the volatile [...] Read more.

The nanoencapsulation of essential oils enhances their applicability in several areas, such as pharmaceuticals and food biopreservation. This study focuses on the encapsulation of Saccocalyx satureioides Coss. et Durieu essential oil into nanoemulsions by high-pressure homogenization (HPH) and its effect on the volatile constituents and the antioxidant and anticancer activities of the essential oil. The analysis of hydrodistilled (HD) S. satureioides essential oil using gas chromatography–mass spectrometry revealed a total of 28 constituents, representing 99.80%, while only 13 constituents were identified in nanoemulsions, representing 98.65% of the total volatile material. The use of HPH led to qualitative and quantitative differences between the volatile profiles of the HD and the nanoemulsion of S. satureioides essential oil. Whereas borneol, α-terpineol, and thymol were the predominant constituents in the HD oil, carvacrol, thymol, and γ-terpinene were the major constituents in the nanoemulsion. The antioxidant activity of the S. satureioides essential oil nanoemulsion displayed was lower as compared to that of HD oil using DPPH free radical–scavenging, CUPRAC, and ABTS assays. This is consistent with the differences in total flavonoid, total phenolic, and volatiles detected in both HD oil and its nanoemulsion. Meanwhile, the cytotoxicity on liver cancer cells (Hep-G2) was stronger using nanoemulsions (106 μg/mL) than using HD oil (274.8 μg/mL). Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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21 pages, 1211 KiB

Open AccessArticle

Protective Effects of Eicosapentaenoic Acid Plus Hydroxytyrosol Supplementation Against White Adipose Tissue Abnormalities in Mice Fed a High-Fat Diet

by Paola Illesca, Rodrigo Valenzuela, Alejandra Espinosa, Francisca Echeverría, Sandra Soto-Alarcon, Cristian Campos, Alicia Rodriguez, Romina Vargas, Thea Magrone and Luis A. Videla

Molecules 2020, 25(19), 4433; https://doi.org/10.3390/molecules25194433 - 27 Sep 2020

Cited by 17 | Viewed by 2630

Abstract

Objective: Obesity induced by high-fat diet (HFD) elicits white adipose tissue dysfunction. In this study, we have hypothesized that the metabolic modulator eicosapentaenoic acid (EPA) combined with the antioxidant hydroxytyrosol (HT) attenuates HFD-induced white adipose tissue (WAT) alterations. Methods: C57BL/6J mice were administered [...] Read more.

Objective: Obesity induced by high-fat diet (HFD) elicits white adipose tissue dysfunction. In this study, we have hypothesized that the metabolic modulator eicosapentaenoic acid (EPA) combined with the antioxidant hydroxytyrosol (HT) attenuates HFD-induced white adipose tissue (WAT) alterations. Methods: C57BL/6J mice were administered with a HFD (60% fat, 20% protein, 20% carbohydrates) or control diet (CD; 10% fat, 20% protein, 70% carbohydrates), with or without EPA (50 mg/kg/day), HT (5 mg/kg/day), or both for 12 weeks. Determinations in WAT include morphological parameters, EPA and docosahexaenoic acid content in phospholipids (gas chromatography), lipogenesis, oxidative stress (OS) and inflammation markers, and gene expression and activities of transcription factors, such as sterol regulatory element-binding protein-1c (SREBP-1c), peroxisome proliferator-activated receptor-gamma (PPAR-γ), nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) (p65 subunit) and nuclear factor erythroid 2-related factor 2 (Nrf2) (quantitative polymerase chain reaction and enzyme linked immunosorbent assay). Results: HFD led to WAT hypertrophy in relation to PPAR-γ downregulation. WAT metabolic dysfunction was characterized by upregulation of lipogenic SREBP-1c system, mitochondrial energy metabolism depression, loss of the antioxidant Nrf2 signaling with OS enhancement, n-3 long-chain polyunsaturated fatty acids depletion and activation of the pro-inflammatory NF-κB system. EPA and HT co-supplementation diminished HFD-dependent effects additively, reaching values close or similar to controls. Conclusion: Data presented strengthen the importance of combined protocols such as EPA plus HT to attenuate metabolic-inflammatory states triggered by obesity. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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12 pages, 998 KiB

Open AccessArticle

Ethanolic Extract of Salvia hispanica L. Regulates Blood Pressure by Modulating the Expression of Genes Involved in BP-Regulatory Pathways

by Gerardo I. Arredondo-Mendoza, Zacarías Jiménez-Salas, Francisco Javier Guzmán-de la Garza, Elizabeth Solís-Pérez, Manuel López-Cabanillas-Lomelí, Blanca Edelia González-Martínez and Eduardo Campos-Góngora

Molecules 2020, 25(17), 3875; https://doi.org/10.3390/molecules25173875 - 26 Aug 2020

Cited by 4 | Viewed by 2781

Abstract

Hypertension (HT) is considered to be a potential risk factor for cardiovascular diseases and has been directly related to pathologies such as obesity and dyslipidemias. Angiotensin-converting enzyme inhibitors (ACEIs) blocked the renin-angiotensin-aldosterone cascade diminishing the production of angiotensin II and the level of [...] Read more.

Hypertension (HT) is considered to be a potential risk factor for cardiovascular diseases and has been directly related to pathologies such as obesity and dyslipidemias. Angiotensin-converting enzyme inhibitors (ACEIs) blocked the renin-angiotensin-aldosterone cascade diminishing the production of angiotensin II and the level of bradykinin, produced by the kallikrein-kinin system. Although ACEIs are effective therapeutics in regulating HT, they present several side-effects that can be due to their mechanism of action (as hypotension, cough, dizziness, light-headedness or hyperkalemia) to specific drug molecular structure (skin rash, neutropenia and tasting disorders) or due to associated pathologies in the patients (it has been considered a possible nephrotoxic effect when ACEIs are administered in combination with angiotensin receptor blockers, in patients that present comorbidities as diabetes, acute kidney injury or chronic kidney disease). Therefore, it is necessary the searching for new products with ACEI activity that do not produce side effects. Interestingly, species of the plant genus Salvia have been found to possess hypotensive effects. In the present study, we analyzed the effects of the ethanolic extract of Salvia hispanica L. seeds (EESH) on the expression of genes involved in pathways regulating HT. Administration of EESH to hypertensive rats inhibited the angiotensin-converting enzyme (ACE) activity along with a decrease in Ace and elevation of Agtr1a and Nos3 gene expression, as compared to that in healthy rats. Moreover, these results were similar to those observed with captopril, an antihypertensive drug used as a control. No significant change in the expression of Bdkrb2 gene was observed in the different groups of rats. To conclude, our results demonstrate that EESH regulates blood pressure (BP) in hypertensive rats through transcriptionally regulating the expression of genes that participate in different pathways involving ACE. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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16 pages, 1361 KiB

Open AccessArticle

EPA/DHA Concentrate by Urea Complexation Decreases Hyperinsulinemia and Increases Plin5 in the Liver of Mice Fed a High-Fat Diet

by Alejandra Espinosa, Andrés Ross, Gretel Dovale-Rosabal, Francisco Pino-de la Fuente, Ernesto Uribe-Oporto, Camila Sacristán, Paulina Ruiz, Rodrigo Valenzuela, Nalda Romero, Santiago P. Aubourg and Alicia Rodríguez

Molecules 2020, 25(14), 3289; https://doi.org/10.3390/molecules25143289 - 20 Jul 2020

Cited by 8 | Viewed by 2985

Abstract

Dietary intake of eicosapentaenoic/docosahexaenoic acid (EPA/DHA) reduces insulin resistance and hepatic manifestations through the regulation of metabolism in the liver. Obese mice present insulin resistance and lipid accumulation in intracellular lipid droplets (LDs). LD-associated proteins perilipin (Plin) have an essential role in both [...] Read more.

Dietary intake of eicosapentaenoic/docosahexaenoic acid (EPA/DHA) reduces insulin resistance and hepatic manifestations through the regulation of metabolism in the liver. Obese mice present insulin resistance and lipid accumulation in intracellular lipid droplets (LDs). LD-associated proteins perilipin (Plin) have an essential role in both adipogenesis and lipolysis; Plin5 regulates lipolysis and thus contributes to fat oxidation. The purpose of this study was to compare the effects of deodorized refined salmon oil (DSO) and its polyunsaturated fatty acids concentrate (CPUFA) containing EPA and DHA, obtained by complexing with urea, on obesity-induced metabolic alteration. CPUFA maximum content was determined using the Box–Behnken experimental design based on Surface Response Methodology. The optimized CPUFA was administered to high-fat diet (HFD)-fed mice (200 mg/kg/day of EPA + DHA) for 8 weeks. No significant differences (p > 0.05) in cholesterol, glycemia, LDs or transaminase content were found. Fasting insulin and hepatic Plin5 protein level increased in the group supplemented with the EPA + DHA optimized product (38.35 g/100 g total fatty acids) compared to obese mice without fish oil supplementation. The results suggest that processing salmon oil by urea concentration can generate an EPA+DHA dose useful to prevent the increase of fasting insulin and the decrease of Plin5 in the liver of insulin-resistant mice. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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13 pages, 3394 KiB

Open AccessArticle

Rosmarinic Acid as a Candidate in a Phenotypic Profiling Cardio-/Cytotoxicity Cell Model Induced by Doxorubicin

by Qiao Zhang, Jing Li, Sha Peng, Yanling Zhang and Yanjiang Qiao

Molecules 2020, 25(4), 836; https://doi.org/10.3390/molecules25040836 - 14 Feb 2020

Cited by 9 | Viewed by 2918

Abstract

Advances in cancer treatment have led to significant improvements in long-term survival in many types of cancer, but heart dysfunction and heart failure, associated with cancer treatment, have also increased. Anthracyclines are the main cause of this type of cardiotoxicity. In this study, [...] Read more.

Advances in cancer treatment have led to significant improvements in long-term survival in many types of cancer, but heart dysfunction and heart failure, associated with cancer treatment, have also increased. Anthracyclines are the main cause of this type of cardiotoxicity. In this study, we describe a combined experimental and cell morphology analysis approach for the high-throughput measurement and analysis of a cardiomyocyte cell profile, using partial least square linear discriminant analysis (PLS-LDA) as the pattern recognition algorithm. When screening a small-scale natural compound library, rosmarinic acid (RosA), as a candidate drug, showed the same cardioprotective effect as the positive control. We investigated the protective mechanism of RosA on a human cardiomyocyte cell line (AC16) and human induced pluripotent stem-cell-derived cardiomyocytes (hiPSC-CMs). We showed that RosA pretreatment suppressed doxorubicin (Dox)-induced cell apoptosis and decreased the activity of caspase-9. RosA promotes the expression of Heme oxygenase-1 (HO-1) and reduces the production of reactive oxygen species (Ros), which is induced by Dox. Meanwhile, it can also promote the expression of cardiac-development-related protein, including histone deacetylase 1 (HDAC1), GATA binding protein 4 (GATA4) and troponin I3, cardiac type (CTnI). Collectively, our data support the notion that RosA is a protective agent in hiPSC-CMs and has the potential for therapeutic use in the treatment of cancer therapy-related cardiac dysfunction and heart failure. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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9 pages, 1176 KiB

Open AccessArticle

Amelioration of Hyperglycemia-Induced Nephropathy by 3,3′-Diindolylmethane in Diabetic Mice

by Kyeong-Mi Choi and Hwan-Soo Yoo

Molecules 2019, 24(24), 4474; https://doi.org/10.3390/molecules24244474 - 06 Dec 2019

Cited by 11 | Viewed by 3180

Abstract

Type 1 diabetes mellitus (insulin-dependent diabetes) is characterized by hyperglycemia caused by an insulin deficiency. Diabetic nephropathy is a major complication of hyperglycemia. 3,3′-diindolylmethane (DIM)-a natural compound produced from indole-3-carbinol, found in cruciferous vegetables-enhances glucose uptake by increasing the activation of the insulin [...] Read more.

Type 1 diabetes mellitus (insulin-dependent diabetes) is characterized by hyperglycemia caused by an insulin deficiency. Diabetic nephropathy is a major complication of hyperglycemia. 3,3′-diindolylmethane (DIM)-a natural compound produced from indole-3-carbinol, found in cruciferous vegetables-enhances glucose uptake by increasing the activation of the insulin signaling pathway in 3T3-L1 adipocytes. In this study, we investigated whether DIM could improve insulin-dependent diabetes and nephropathy in streptozotocin (STZ)-induced diabetic mice. In mice, STZ induced hyperglycemia, hunger, thirst, and abnormally increased kidney weight and serum creatinine, which is a renal functional parameter. DIM decreased STZ-increased high blood glucose levels and food and water intake in diabetic mice. DIM also improved diabetic nephropathy by inhibiting the expression of PKC-α, the marker of albuminuria, and TGF-β1, an indicator of renal hypertrophy, in diabetic mice. Our findings suggest that DIM may ameliorate hyperglycemia and diabetic nephropathy through the inhibition of PKC-α and TGF-β1 signaling. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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10 pages, 3863 KiB

Open AccessArticle

Aucubin, An Active Ingredient in Aucuba japonica, Prevents N-methyl-N-nitrosourea-induced Retinal Degeneration in Mice

by Eunsoo Jung, Su-Bin Park, Woo Kwon Jung, Hyung Rae Kim and Junghyun Kim

Molecules 2019, 24(24), 4437; https://doi.org/10.3390/molecules24244437 - 04 Dec 2019

Cited by 8 | Viewed by 2726

Abstract

In the present study, we examined the potent retinoprotective effects of an ethanol-based extract of Aucuba japonica (AJE) and its active ingredient, aucubin, on N-methyl-N-nitrosourea (MNU)-induced retinal degeneration in mice. Retinal degeneration was induced by an intraperitoneal injection of MNU [...] Read more.

In the present study, we examined the potent retinoprotective effects of an ethanol-based extract of Aucuba japonica (AJE) and its active ingredient, aucubin, on N-methyl-N-nitrosourea (MNU)-induced retinal degeneration in mice. Retinal degeneration was induced by an intraperitoneal injection of MNU (60 mg/kg). AJE (250 mg/kg) and aucubin (15 mg/kg) were orally administered for 1 week after the MNU injection. Electroretinography (ERG) and histological examinations were performed. Retinal apoptosis and oxidative DNA damage were also quantified. The retinoprotective abilities of AJE and aucubin were also assessed in primary cultured retinal cells. Morphologically, MNU induced a remarkable decrease in the outer nuclear layer, which contains photoreceptor cells. However, this layer was well preserved in the AJE- and aucubin-administered mice. The ERG responses significantly decreased in both a- and b-wave amplitudes in the MNU-injected mice. In the AJE and aucubin-treated mice, ERG responses were significantly increased. In addition, a terminal deoxynucleotidyl transferase dUTP nick end-labeling (TUNEL) assay and immunohistochemical staining for 8-hydroxydeoxyguanosine (8-OHdG) revealed that both AJE and aucubin attenuated MNU-induced photoreceptor cell apoptosis and oxidative DNA damage. Furthermore, the in vitro assay also showed that AJE and aucubin have potent anti-oxidative and anti-apoptotic activities in primary cultured retinal cells. These results indicate that AJE and aucubin have potent retinoprotective effects, and that this retinoprotective activity is as a result of the potency of the bioactive compound, aucubin. These pharmacological characteristics suggest the additional application of AJE or aucubin in the treatment of patients with retinal degenerative diseases. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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Review

Jump to: Research

13 pages, 1208 KiB

Open AccessReview

Pharmacological Extracts and Molecules from Virola Species: Traditional Uses, Phytochemistry, and Biological Activity

by María González-Rodríguez, Clara Ruiz-Fernández, Vera Francisco, Djedjiga Ait Eldjoudi, Yousof Ramadan Farrag AbdElHafez, Alfonso Cordero-Barreal, Jesus Pino, Francisca Lago, Manuel Campos-Toimil, Glaucimeire Rocha Carvalho, Thiago Melo Costa Pereira and Oreste Gualillo

Molecules 2021, 26(4), 792; https://doi.org/10.3390/molecules26040792 - 03 Feb 2021

Cited by 5 | Viewed by 3230

Abstract

Virola is the largest genus of Myristicaceae in America, comprising about 60 species of medium-sized trees geographically spread from Mexico to southern Brazil. The plant species of this genus have been widely used in folk medicine for the treatment of several ailments, such [...] Read more.

Virola is the largest genus of Myristicaceae in America, comprising about 60 species of medium-sized trees geographically spread from Mexico to southern Brazil. The plant species of this genus have been widely used in folk medicine for the treatment of several ailments, such as rheumatic pain, bronchial asthma, tumors in the joints, intestinal worms, halitosis, ulcers, and multiple infections, due to their pharmacological activity. This review presents an updated and comprehensive summary of Virola species, particularly their ethnomedicinal uses, phytochemistry, and biological activity, to support the safe medicinal use of plant extracts and provide guidance for future research. The Virola spp.’s ethnopharmacology, including in the treatment of stomach pain and gastric ulcers, as well as antimicrobial and tryponosomicidal activities, is attributable to the presence of a myriad of phytoconstituents, such as flavonoids, tannins, phenolic acids, lignans, arylalkanones, and sitosterol. Hence, such species yield potential leads or molecular scaffolds for the development of new pharmaceutical formulations, encouraging the elucidation of not-yet-understood action mechanisms and ascertaining their safety for humans. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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20 pages, 2933 KiB

Open AccessFeature PaperReview

Natural Flavonoids as Potential Angiotensin-Converting Enzyme 2 Inhibitors for Anti-SARS-CoV-2

by Muchtaridi Muchtaridi, M. Fauzi, Nur Kusaira Khairul Ikram, Amirah Mohd Gazzali and Habibah A. Wahab

Molecules 2020, 25(17), 3980; https://doi.org/10.3390/molecules25173980 - 01 Sep 2020

Cited by 75 | Viewed by 14629

Abstract

Over the years, coronaviruses (CoV) have posed a severe public health threat, causing an increase in mortality and morbidity rates throughout the world. The recent outbreak of a novel coronavirus, named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) caused the current Coronavirus Disease [...] Read more.

Over the years, coronaviruses (CoV) have posed a severe public health threat, causing an increase in mortality and morbidity rates throughout the world. The recent outbreak of a novel coronavirus, named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) caused the current Coronavirus Disease 2019 (COVID-19) pandemic that affected more than 215 countries with over 23 million cases and 800,000 deaths as of today. The situation is critical, especially with the absence of specific medicines or vaccines; hence, efforts toward the development of anti-COVID-19 medicines are being intensively undertaken. One of the potential therapeutic targets of anti-COVID-19 drugs is the angiotensin-converting enzyme 2 (ACE2). ACE2 was identified as a key functional receptor for CoV associated with COVID-19. ACE2, which is located on the surface of the host cells, binds effectively to the spike protein of CoV, thus enabling the virus to infect the epithelial cells of the host. Previous studies showed that certain flavonoids exhibit angiotensin-converting enzyme inhibition activity, which plays a crucial role in the regulation of arterial blood pressure. Thus, it is being postulated that these flavonoids might also interact with ACE2. This postulation might be of interest because these compounds also show antiviral activity in vitro. This article summarizes the natural flavonoids with potential efficacy against COVID-19 through ACE2 receptor inhibition. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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22 pages, 2149 KiB

Open AccessReview

Plants as Sources of Anti-Inflammatory Agents

by Clara dos Reis Nunes, Mariana Barreto Arantes, Silvia Menezes de Faria Pereira, Larissa Leandro da Cruz, Michel de Souza Passos, Luana Pereira de Moraes, Ivo José Curcino Vieira and Daniela Barros de Oliveira

Molecules 2020, 25(16), 3726; https://doi.org/10.3390/molecules25163726 - 15 Aug 2020

Cited by 142 | Viewed by 10926

Abstract

Plants represent the main source of molecules for the development of new drugs, which intensifies the interest of transnational industries in searching for substances obtained from plant sources, especially since the vast majority of species have not yet been studied chemically or biologically, [...] Read more.

Plants represent the main source of molecules for the development of new drugs, which intensifies the interest of transnational industries in searching for substances obtained from plant sources, especially since the vast majority of species have not yet been studied chemically or biologically, particularly concerning anti-inflammatory action. Anti-inflammatory drugs can interfere in the pathophysiological process of inflammation, to minimize tissue damage and provide greater comfort to the patient. Therefore, it is important to note that due to the existence of a large number of species available for research, the successful development of new naturally occurring anti-inflammatory drugs depends mainly on a multidisciplinary effort to find new molecules. Although many review articles have been published in this regard, the majority presented the subject from a limited regional perspective. Thus, the current article presents highlights from the published literature on plants as sources of anti-inflammatory agents. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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20 pages, 1640 KiB

Open AccessReview

The Intrinsic Virtues of EGCG, an Extremely Good Cell Guardian, on Prevention and Treatment of Diabesity Complications

by Maria Assunta Potenza, Dominga Iacobazzi, Luca Sgarra and Monica Montagnani

Molecules 2020, 25(13), 3061; https://doi.org/10.3390/molecules25133061 - 04 Jul 2020

Cited by 19 | Viewed by 4730

Abstract

The pandemic proportion of diabesity—a combination of obesity and diabetes—sets a worldwide health issue. Experimental and clinical studies have progressively reinforced the pioneering epidemiological observation of an inverse relationship between consumption of polyphenol-rich nutraceutical agents and mortality from cardiovascular and metabolic diseases. With [...] Read more.

The pandemic proportion of diabesity—a combination of obesity and diabetes—sets a worldwide health issue. Experimental and clinical studies have progressively reinforced the pioneering epidemiological observation of an inverse relationship between consumption of polyphenol-rich nutraceutical agents and mortality from cardiovascular and metabolic diseases. With chemical identification of epigallocatechin-3-gallate (EGCG) as the most abundant catechin of green tea, a number of cellular and molecular mechanisms underlying the activities of this unique catechin have been proposed. Favorable effects of EGCG have been initially attributed to its scavenging effects on free radicals, inhibition of ROS-generating mechanisms and upregulation of antioxidant enzymes. Biologic actions of EGCG are concentration-dependent and under certain conditions EGCG may exert pro-oxidant activities, including generation of free radicals. The discovery of 67-kDa laminin as potential EGCG membrane target has broaden the likelihood that EGCG may function not only because of its highly reactive nature, but also via receptor-mediated activation of multiple signaling pathways involved in cell proliferation, angiogenesis and apoptosis. Finally, by acting as epigenetic modulator of DNA methylation and chromatin remodeling, EGCG may alter gene expression and modify miRNA activities. Despite unceasing research providing detailed insights, ECGC composite activities are still not completely understood. This review summarizes the most recent evidence on molecular mechanisms by which EGCG may activate signal transduction pathways, regulate transcription factors or promote epigenetic changes that may contribute to prevent pathologic processes involved in diabesity and its cardiovascular complications. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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Open AccessReview

Production and Potential Applications of Bioconversion of Chitin and Protein-Containing Fishery Byproducts into Prodigiosin: A Review

by San-Lang Wang, Van Bon Nguyen, Chien Thang Doan, Thi Ngoc Tran, Minh Trung Nguyen and Anh Dzung Nguyen

Molecules 2020, 25(12), 2744; https://doi.org/10.3390/molecules25122744 - 13 Jun 2020

Cited by 28 | Viewed by 4553

Abstract

The technology of microbial conversion provides a potential way to exploit compounds of biotechnological potential. The red pigment prodigiosin (PG) and other PG-like pigments from bacteria, majorly from Serratia marcescens, have been reported as bioactive secondary metabolites that can be used in [...] Read more.

The technology of microbial conversion provides a potential way to exploit compounds of biotechnological potential. The red pigment prodigiosin (PG) and other PG-like pigments from bacteria, majorly from Serratia marcescens, have been reported as bioactive secondary metabolites that can be used in the broad fields of agriculture, fine chemicals, and pharmacy. Increasing PG productivity by investigating the culture conditions especially the inexpensive carbon and nitrogen (C/N) sources has become an important factor for large-scale production. Investigations into the bioactivities and applications of PG and its related compounds have also been given increased attention. To save production cost, chitin and protein-containing fishery byproducts have recently been investigated as the sole C/N source for the production of PG and chitinolytic/proteolytic enzymes. This strategy provides an environmentally-friendly selection using inexpensive C/N sources to produce a high yield of PG together with chitinolytic and proteolytic enzymes by S. marcescens. The review article will provide effective references for production, bioactivity, and application of S. marcescens PG in various fields such as biocontrol agents and potential pharmaceutical drugs. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds in the Prevention and Treatment of Chronic Diseases)

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