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Special Issue "Biological Activity of Natural Substances and Their Derivatives"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 May 2020).

Special Issue Editors

Dr. Olga Pecháňová
Website
Guest Editor
Institute of Normal and Pathological Physiology, Centre of Experimental Medicine, Slovak Academy of Sciences, Sienkiewiczova 1, 813 71 Bratislava, Slovakia
Interests: polyphenolic compounds; nitric oxide; cardiovascular system; hypertension; metabolic syndrome
Dr. Martina Cebova
Website
Assistant Guest Editor
Institute of Normal and Pathological Physiology, Centre of Experimental Medicine, Slovak Academy of Sciences, Sienkiewiczova 1, 813 71 Bratislava, Slovakia
Interests: myocardial infarction; heart failure; obesity; gasotransmitters; morphological analysis

Special Issue Information

Dear Colleagues,

Although several so-called non-essential substances found in food have been shown not to be absolutely necessary to maintain basic life processes, they are useful to the human body in many critical situations and thus improve the quality of human life. Many biologically active natural substances, e.g., natural polyphenols, have a synergistic effect with different drugs, and can even alleviate the consequences of disease in pharmacotherapy intolerant individuals. In view of the current nutritional habits and prevalence of morbidity and mortality in the industrial world (cardiovascular diseases, cancer, metabolic syndrome, osteoporosis, etc.), supplements containing essential nutrients are more than desirable. In this Special Issue, we invite researchers and clinicians to contribute original research and review articles that analyze and describe new mechanisms of actions of different natural substances, and their derivatives and secondary metabolite products. Special interest is devoted to new natural products with pleiotropic effects for the prevention and treatment of cardiovascular diseases, metabolic syndrome, diabetes, nervous system disorders, inflammatory diseases, and others. Potential topics include, but are not limited to the following:

  • Preventive and curative effects of natural substances and their mechanisms of actions.
  • Pleiotropic and synergic effects of polyphenolic bioactive compounds.
    • Nanoparticles using natural substances and extracts.
    • Bioactive essential oil components: isolation, analysis, and underlying mechanisms.
    • Derivatives and secondary metabolite products.
  • Natural substances that mimic the effects of hibernation and other protective processes under extreme conditions.

Dr. Olga Pechanova
Dr. Martina Cebova
Guest Editors

Manuscript Submission Information

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Published Papers (18 papers)

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Research

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Open AccessArticle
Decorin Protects Cardiac Myocytes against Simulated Ischemia/Reperfusion Injury
Molecules 2020, 25(15), 3426; https://doi.org/10.3390/molecules25153426 - 28 Jul 2020
Abstract
Search for new cardioprotective therapies is of great importance since no cardioprotective drugs are available on the market. In line with this need, several natural biomolecules have been extensively tested for their potential cardioprotective effects. Previously, we have shown that biglycan, a member [...] Read more.
Search for new cardioprotective therapies is of great importance since no cardioprotective drugs are available on the market. In line with this need, several natural biomolecules have been extensively tested for their potential cardioprotective effects. Previously, we have shown that biglycan, a member of a diverse group of small leucine-rich proteoglycans, enhanced the expression of cardioprotective genes and decreased ischemia/reperfusion-induced cardiomyocyte death via a TLR-4 dependent mechanism. Therefore, in the present study we aimed to test whether decorin, a small leucine-rich proteoglycan closely related to biglycan, could exert cardiocytoprotection and to reveal possible downstream signaling pathways. Methods: Primary cardiomyocytes isolated from neonatal and adult rat hearts were treated with 0 (Vehicle), 1, 3, 10, 30 and 100 nM decorin as 20 h pretreatment and maintained throughout simulated ischemia and reperfusion (SI/R). In separate experiments, to test the mechanism of decorin-induced cardio protection, 3 nM decorin was applied in combination with inhibitors of known survival pathways, that is, the NOS inhibitor L-NAME, the PKG inhibitor KT-5823 and the TLR-4 inhibitor TAK-242, respectively. mRNA expression changes were measured after SI/R injury. Results: Cell viability of both neonatal and adult cardiomyocytes was significantly decreased due to SI/R injury. Decorin at 1, 3 and 10 nM concentrations significantly increased the survival of both neonatal and adult myocytes after SI/R. At 3nM (the most pronounced protective concentration), it had no effect on apoptotic rate of neonatal cardiac myocytes. No one of the inhibitors of survival pathways (L-NAME, KT-5823, TAK-242) influenced the cardiocytoprotective effect of decorin. MYND-type containing 19 (Zmynd19) and eukaryotic translation initiation factor 4E nuclear import factor 1 (Eif4enif1) were significantly upregulated due to the decorin treatment. In conclusion, this is the first demonstration that decorin exerts a direct cardiocytoprotective effect possibly independent of NO-cGMP-PKG and TLR-4 dependent survival signaling. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Dehydrozingerone, a Curcumin Analog, as a Potential Anti-Prostate Cancer Inhibitor In Vitro and In Vivo
Molecules 2020, 25(12), 2737; https://doi.org/10.3390/molecules25122737 - 12 Jun 2020
Abstract
Curcumin (Cur) exhibits biological activities that support its candidacy for cancer treatment. However, there are limitations to its pharmacological effects, such as poor solubility and bioavailability. Notably, the use of Cur analogs has potential for addressing these limitations. Dehydrozingerone (DZG) is a representative [...] Read more.
Curcumin (Cur) exhibits biological activities that support its candidacy for cancer treatment. However, there are limitations to its pharmacological effects, such as poor solubility and bioavailability. Notably, the use of Cur analogs has potential for addressing these limitations. Dehydrozingerone (DZG) is a representative of the half-chemical structure of Cur, and many reports have indicated that it is anticancer in vitro. We, therefore, have hypothesized that DZG could inhibit prostate cancer progression both in vitro and in vivo. Results revealed that DZG decreased cell proliferation of rat castration-resistant prostate cancer, PLS10 cells, via induction of the cell cycle arrest in the G1 phase in vitro. In the PLS10 xenograft model, DZG significantly decreased the growth of subcutaneous tumors when compared to the control via the inhibition of cell proliferation and angiogenesis. To prove that DZG could improve the limitations of Cur, an in vivo pharmacokinetic was determined. DZG was detected in the serum at higher concentrations and remained up to 3 h after intraperitoneal injections, which was longer than Cur. DZG also showed superior in vivo tissue distribution than Cur. The results suggest that DZG could be a candidate of the Cur analog that can potentially exert anticancer capabilities in vivo and thereby improve its bioavailability. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Cell Death Effects Induced by Sulforaphane and Allyl Isothiocyanate on P-Glycoprotein Positive and Negative Variants in L1210 Cells
Molecules 2020, 25(9), 2093; https://doi.org/10.3390/molecules25092093 - 30 Apr 2020
Cited by 1
Abstract
Variants of L1210 leukemia cells-namely, parental P-glycoprotein-negative S cells and R and T cells expressing P-glycoprotein, due to selection with vincristine and transfection with the human p-glycoprotein gene, respectively-were used. The responses of these cell variants to two naturally occurring isothiocyanates-sulforaphane (SFN, from [...] Read more.
Variants of L1210 leukemia cells-namely, parental P-glycoprotein-negative S cells and R and T cells expressing P-glycoprotein, due to selection with vincristine and transfection with the human p-glycoprotein gene, respectively-were used. The responses of these cell variants to two naturally occurring isothiocyanates-sulforaphane (SFN, from cruciferous vegetables) and allyl isothiocyanate (AITC, from mustard, radish, horseradish and wasabi)-were studied. We obtained conflicting results for the cell death effects induced by isothiocyanates, as measured by i. cell counting, which showed inhibited proliferation, and ii. cell metabolic activity via an MTS assay, which showed an increased MTS signal. These results indicated the hyperactivation of cell metabolism induced by treatment with isothiocyanates. In more detailed study, we found that, depending on the cell variants and the isothiocyanate used in treatment, apoptosis and necrosis (detected by annexin-V cells and propidium iodide staining), as well as autophagy (detected with monodansylcadaverine), were involved in cell death. We also determined the cell levels/expression of Bcl-2 and Bax as representative anti- and pro-apoptotic proteins of the Bcl-2 family, the cell levels/expression of members of the canonical and noncanonical NF-κB pathways, and the cell levels of 16 and 18 kDa fragments of LC3B protein as markers of autophagy. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Beneficial Effects of Cornelian Cherries on Lipid Profile and NO/ROS Balance in Obese Zucker Rats: Comparison with CoQ10
Molecules 2020, 25(8), 1922; https://doi.org/10.3390/molecules25081922 - 21 Apr 2020
Cited by 2
Abstract
Cornelian cherries (CCs) belong to promising anti-obesity substances. We aimed to study effects of coenzyme Q10 (CoQ10) and two varieties of CCs on lipid profile, ROS, and nitric oxide (NO) production in obese rats. Male Zucker rats were divided into the control group [...] Read more.
Cornelian cherries (CCs) belong to promising anti-obesity substances. We aimed to study effects of coenzyme Q10 (CoQ10) and two varieties of CCs on lipid profile, ROS, and nitric oxide (NO) production in obese rats. Male Zucker rats were divided into the control group and groups treated with CoQ10 (30mg/kg/day), or CC varieties: Koralovij Marka (KM) and Wild Type (WT) (5 g/kg/day, n = 6 in each group) for 6 weeks. Blood pressure (BP), bodyweight, relative heart weight, and plasma lipid profile were determined. NOS activity and expressions of eNOS, SOD, and NADPH oxidase were determined in the left ventricle (LV) and aorta. Among CC groups, KM decreased bodyweight and WT relative heart weight. Neither CoQ10 nor CCs affected BP. CoQ10 did not affect lipid profile and NOS activity either in the LV or aorta. On the other hand, WT decreased cholesterol and LDL levels. KM and WT increased NOS activity in the aorta, while not affecting the activity in the LV. KM increased eNOS expression and did not affect ROS production, while WT increased SOD and decreased NADPH oxidase without affecting eNOS expressions in both tissues. In conclusion, CCs showed better beneficial effects than CoQ10 in all parameters studied. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Induction of Apoptosis by Gluconasturtiin-Isothiocyanate (GNST-ITC) in Human Hepatocarcinoma HepG2 Cells and Human Breast Adenocarcinoma MCF-7 Cells
Molecules 2020, 25(5), 1240; https://doi.org/10.3390/molecules25051240 - 09 Mar 2020
Abstract
Gluconasturtiin, a glucosinolate present in watercress, is hydrolysed by myrosinase to form gluconasturtiin-isothiocyanate (GNST-ITC), which has potential chemopreventive effects; however, the underlying mechanisms of action have not been explored, mainly in human cell lines. The purpose of the study is to evaluate the [...] Read more.
Gluconasturtiin, a glucosinolate present in watercress, is hydrolysed by myrosinase to form gluconasturtiin-isothiocyanate (GNST-ITC), which has potential chemopreventive effects; however, the underlying mechanisms of action have not been explored, mainly in human cell lines. The purpose of the study is to evaluate the cytotoxicity of GNST-ITC and to further assess its potential to induce apoptosis. GNST-ITC inhibited cell proliferation in both human hepatocarcinoma (HepG2) and human breast adenocarcinoma (MCF-7) cells with IC50 values of 7.83 µM and 5.02 µM, respectively. Morphological changes as a result of GNST-ITC-induced apoptosis showed chromatin condensation, nuclear fragmentation, and membrane blebbing. Additionally, Annexin V assay showed proportion of cells in early and late apoptosis upon exposure to GNST-ITC in a time-dependent manner. To delineate the mechanism of apoptosis, cell cycle arrest and expression of caspases were studied. GNST-ITC induced a time-dependent G2/M phase arrest, with reduction of 82% and 93% in HepG2 and MCF-7 cell lines, respectively. The same treatment also led to the subsequent expression of caspase-3/7 and -9 in both cells demonstrating mitochondrial-associated cell death. Collectively, these results reveal that GNST-ITC can inhibit cell proliferation and can induce cell death in HepG2 and MCF-7 cancer cells via apoptosis, highlighting its potential development as an anticancer agent. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Antibacterial Activity and Pharmacokinetic Profile of a Promising Antibacterial Agent: 22-(2-Amino-phenylsulfanyl)-22-Deoxypleuromutilin
Molecules 2020, 25(4), 878; https://doi.org/10.3390/molecules25040878 - 17 Feb 2020
Cited by 1
Abstract
A new pleuromutilin derivative, 22-(2-amino-phenylsulfanyl)-22-deoxypleuromutilin (amphenmulin), has been synthesized and proved excellent in vitro and in vivo efficacy than that of tiamulin against methicillin-resistant Staphylococcus aureus (MRSA), suggesting this compound may lead to a promising antibacterial agent to treat MRSA infections. In this [...] Read more.
A new pleuromutilin derivative, 22-(2-amino-phenylsulfanyl)-22-deoxypleuromutilin (amphenmulin), has been synthesized and proved excellent in vitro and in vivo efficacy than that of tiamulin against methicillin-resistant Staphylococcus aureus (MRSA), suggesting this compound may lead to a promising antibacterial agent to treat MRSA infections. In this study, the effectiveness and safety of amphenmulin were further investigated. Amphenmulin showed excellent antibacterial activity against MRSA (minimal inhibitory concentration = 0.0156~8 µg/mL) and performed time-dependent growth inhibition and a concentration-dependent postantibiotic effect (PAE). Acute oral toxicity test in mice showed that amphenmulin was a practical non-toxic drug and possessed high security as a new drug with the 50% lethal dose (LD50) above 5000 mg/kg. The pharmacokinetic properties of amphenmulin were then measured. After intravenous administration, the elimination half-life (T1/2), total body clearance (Clβ), and area under curve to infinite time (AUC0→∞) were 1.92 ± 0.28 h, 0.82 ± 0.09 L/h/kg, and 12.23 ± 1.35 μg·h/mL, respectively. After intraperitoneal administration, the T1/2, Clβ/F and AUC0→∞ were 2.64 ± 0.72 h, 4.08 ± 1.14 L/h/kg, and 2.52 ± 0.81 μg·h/mL, respectively, while for the oral route were 2.91 ± 0.81 h, 6.31 ± 2.26 L/h/kg, 1.67 ± 0.66 μg·h/mL, respectively. Furthermore, we evaluated the antimicrobial activity of amphenmulin in an experimental model of MRSA wound infection. Amphenmulin enhanced wound closure and promoted the healing of wound, which inhibited MRSA bacterial counts in the wound and decreased serum levels of the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
The Possible Role of the Nitroso-Sulfide Signaling Pathway in the Vasomotoric Effect of Garlic Juice
Molecules 2020, 25(3), 590; https://doi.org/10.3390/molecules25030590 - 29 Jan 2020
Cited by 1
Abstract
The beneficial cardiovascular effects of garlic have been reported in numerous studies. The major bioactive properties of garlic are related to organic sulfides. This study aimed to investigate whether garlic juice works exclusively due to its sulfur compounds or rather via the formation [...] Read more.
The beneficial cardiovascular effects of garlic have been reported in numerous studies. The major bioactive properties of garlic are related to organic sulfides. This study aimed to investigate whether garlic juice works exclusively due to its sulfur compounds or rather via the formation of new products of the nitroso-sulfide signaling pathway. Changes in isometric tension were measured on the precontracted aortic rings of adult normotensive Wistar rats. We evaluated NO-donor (S-nitrosoglutathione, GSNO)-induced vasorelaxation and compare it with effects of hydrogen sulfide (H2S)/GSNO and garlic/GSNO. Incubation with garlic juice increased the maximal GSNO-induced relaxation and markedly changed the character of the relaxant response. Although incubation with an H2S donor enhanced the maximal vasorelaxant response of GSNO, neither the absolute nor the relative relaxation changed over time. The mixture of GSNO with an H2S donor evoked a response similar to GSNO-induced relaxation after incubation with garlic juice. This relaxation of the H2S and GSNO mixture was soluble guanylyl cyclase (sGC) dependent, partially reduced by HNO scavenger and it was adenosine triphosphate-sensitive potassium channels (KATP) independent. In this study, we demonstrate for the first time the suggestion that H2S itself is probably not the crucial bioactive compound of garlic juice but rather potentiates the production of new signaling molecules during the GSNO-H2S interaction. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Quercetin Exerts Age-Dependent Beneficial Effects on Blood Pressure and Vascular Function, But Is Inefficient in Preventing Myocardial Ischemia-Reperfusion Injury in Zucker Diabetic Fatty Rats
Molecules 2020, 25(1), 187; https://doi.org/10.3390/molecules25010187 - 02 Jan 2020
Cited by 4
Abstract
Background: Quercetin (QCT) was shown to exert beneficial cardiovascular effects in young healthy animals. The aim of the present study was to determine cardiovascular benefits of QCT in older, 6-month and 1-year-old Zucker diabetic fatty (ZDF) rats (model of type 2 diabetes). [...] Read more.
Background: Quercetin (QCT) was shown to exert beneficial cardiovascular effects in young healthy animals. The aim of the present study was to determine cardiovascular benefits of QCT in older, 6-month and 1-year-old Zucker diabetic fatty (ZDF) rats (model of type 2 diabetes). Methods: Lean (fa/+) and obese (fa/fa) ZDF rats of both ages were treated with QCT for 6 weeks (20 mg/kg/day). Isolated hearts were exposed to ischemia-reperfusion (I/R) injury (30 min/2 h). Endothelium-dependent vascular relaxation was measured in isolated aortas. Expression of selected proteins in heart tissue was detected by Western blotting. Results: QCT reduced systolic blood pressure in both lean and obese 6-month-old rats but had no effect in 1-year-old rats. Diabetes worsened vascular relaxation in both ages. QCT improved vascular relaxation in 6-month-old but worsened in 1-year-old obese rats and had no impact in lean controls of both ages. QCT did not exert cardioprotective effects against I/R injury and even worsened post-ischemic recovery in 1-year-old hearts. QCT up-regulated expression of eNOS in younger and PKCε expression in older rats but did not activate whole PI3K/Akt pathway. Conclusions: QCT might be beneficial for vascular function in diabetes type 2; however, increasing age and/or progression of diabetes may confound its vasculoprotective effects. QCT seems to be inefficient in preventing myocardial I/R injury in type 2 diabetes and/or higher age. Impaired activation of PI3K/Akt kinase pathway might be, at least in part, responsible for failing cardioprotection in these subjects. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Optimization of Antioxidant Hydrolysate Produced from Tibetan Egg White with Papain and Its Application in Yak Milk Yogurt
Molecules 2020, 25(1), 109; https://doi.org/10.3390/molecules25010109 - 27 Dec 2019
Abstract
The objective of the present study was to produce antioxidant hydrolysate from Tibetan egg white protein hydrolyzed with papain, and to investigate the effect of added papain egg white hydrolysate (PEWH) on the quality characteristics and amino acid profiles of yak milk yogurt. [...] Read more.
The objective of the present study was to produce antioxidant hydrolysate from Tibetan egg white protein hydrolyzed with papain, and to investigate the effect of added papain egg white hydrolysate (PEWH) on the quality characteristics and amino acid profiles of yak milk yogurt. A response surface methodology (RSM) was utilized to analyze the effects of hydrolysis time (X1), the ratio of enzymes to substrates, and enzyme dosage (X3) on the superoxide anion radical (O2) scavenging activity of hydrolysates. The predicted maximum value of O2 scavenging activity (89.06%) was obtained an X1 of 2.51 h, X2 of 4.13%, and X3 of 4500 U/g of substrate, almost approaching the experimental value (88.05 ± 1.2%). Furthermore, it was found that the addition of PEWH to yak milk can enhance acidification, sensory score, the number of lactic acid bacteria (LAB), and the amino acid content in yak milk yogurt. The results suggested that PEWH displayed an exceptional potential to be developed as a functional food ingredient that could be applied during the manufacturing process of yak milk yogurt. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Sequential Response of Sage Antioxidant Metabolism to Chilling Treatment
Molecules 2019, 24(22), 4087; https://doi.org/10.3390/molecules24224087 - 12 Nov 2019
Abstract
Chilling influences the growth and metabolism of plants. The physiological response and acclimatization of genotypes in relation to stress stimulus can be different. Two sage cultivars: ‘Icterina’ and ‘Purpurascens’ were subjected to 4 °C and 18 °C (control), and sampled between the 5th [...] Read more.
Chilling influences the growth and metabolism of plants. The physiological response and acclimatization of genotypes in relation to stress stimulus can be different. Two sage cultivars: ‘Icterina’ and ‘Purpurascens’ were subjected to 4 °C and 18 °C (control), and sampled between the 5th and 14th day of the treatment. Ascorbate peroxidase (APX) activity was up-regulated in chilled ‘Purpurascens’ on the 14th day, while guaiacol peroxidase (GPX) activity increased on the 10th and 12th day in relation to the control. GPX activity of the control ‘Icterina’ was frequently higher than chilled plants, and chilling did not affect APX activity of that cultivar. Catalase activity remained stable in both sage cultivars. Chilled ‘Purpurascens’ showed a significant increase in total phenolics contents on the 5th, 7th, and 12th day and in total antioxidant capacity on the 5th and 10th day as compared to the control for respective sampling days. Higher malondialdehyde content was found in chilled plants on the 12th, or 14th day, differences reached 26–28% of the controls. Chilling caused significant decrease in dry matter content. The stress response was more stable and effective in ‘Icterina’, while more dynamic changes were found for ‘Purpurascens’. Based on our results, we propose to use ‘Purpurascens’ for targeted stress-induced studies and ‘Icterina’ for field applications. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Modulation of Adipogenesis and Oxidative Status by Quercetin and Ochratoxin A: Positive or Negative Impact on Rat Adipocyte Metabolism?
Molecules 2019, 24(20), 3726; https://doi.org/10.3390/molecules24203726 - 16 Oct 2019
Cited by 2
Abstract
(1) Background: Impaired adipose tissue function leads to the development of metabolic disorders. Reactive oxygen species play a key role in the regulation of adipogenesis and insulin-stimulated glucose uptake by adipocytes. Quercetin (QCT) regulates adipogenesis by affecting the redox state of preadipocytes. Ochratoxin [...] Read more.
(1) Background: Impaired adipose tissue function leads to the development of metabolic disorders. Reactive oxygen species play a key role in the regulation of adipogenesis and insulin-stimulated glucose uptake by adipocytes. Quercetin (QCT) regulates adipogenesis by affecting the redox state of preadipocytes. Ochratoxin A (OTA) is one of the most prevalent mycotoxins contaminating food. It has cytotoxic, genotoxic, pro-inflammatory, and anti-adipogenic effects. Antioxidants are believed to protect cells from the cytotoxicity and genotoxicity induced by OTA. The aim of this study was to investigate the effect of QCT and OTA application on preadipocyte differentiation, oxidative status, and adipocyte metabolism. (2) Methods: Primary rat preadipocytes were isolated from subcutaneous adipose tissue of Wistar rats. Gene expressions were determined by qPCR. Cell viability, reactive oxygen species (ROS) production, glucose uptake, and lipid accumulation were determined using commercially available kits. (3) Results: A dose-dependent inhibitory effect of QCT on adipogenic differentiation was observed, which was accompanied by a decrease in ROS production. Reduced ROS formation is closely related to impaired glucose uptake by adipocytes. (4) Conclusions: The results of this study indicate a key role of ROS in regulating adipogenesis and metabolic pathways, which is affected by the application of QCT and/or OTA. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessArticle
Auriculatone Sulfate Effectively Protects Mice Against Acetaminophen-Induced Liver Injury
Molecules 2019, 24(20), 3642; https://doi.org/10.3390/molecules24203642 - 09 Oct 2019
Abstract
Acetaminophen (APAP) overdose is very common worldwide and has been widely recognized as the leading cause of drug-induced liver injury in the Western world. In our previous investigation, auriculatone, a natural product firstly obtained from Aster auriculatus, has demonstrated a potent protective [...] Read more.
Acetaminophen (APAP) overdose is very common worldwide and has been widely recognized as the leading cause of drug-induced liver injury in the Western world. In our previous investigation, auriculatone, a natural product firstly obtained from Aster auriculatus, has demonstrated a potent protective effect against APAP-induced hepatotoxicity in HL-7702 cells. However, the poor water solubility and low bioavailability restrict its application. Auriculatone sulfate (AS) is a sulfated derivative of auriculatone with highly improved water-solubility. Hepatoprotective effects against APAP-induced liver injury (AILI) showed that intragastric pretreatment with AS at 50 mg/kg almost completely prevented mice against APAP-induced increases of serum alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase and ATPase. Histological results showed that AS could protect the liver tissue damage. In addition, AS pretreatment not only significantly retained hepatic malondialdehyde and the activities of glutathione, superoxide dismutase, and glutathione peroxidase at normal levels, but also markedly suppressed the increase of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 levels in mouse liver caused by overdose APAP. Immunohistochemical analysis showed that AS obviously attenuated the expression of CD45 and HNE in liver tissue. Further mechanisms of action investigation showed that inhibition of cytochrome P450 3A11 (CYP 3A11) and CYP2E1 enzymatic activities (but not that of CYP1A2) was responsible for APAP bioactivation. In conclusion, AS showed a hepatoprotective effect against AILI through alleviating oxidative stress and inflammation and inhibiting CYP-mediated APAP bioactivation. It may be an effective hepatoprotective agent for AILI and other forms of human liver disease. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Review

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Open AccessReview
Protective Effects of Polyphenols against Ischemia/Reperfusion Injury
Molecules 2020, 25(15), 3469; https://doi.org/10.3390/molecules25153469 - 30 Jul 2020
Abstract
Myocardial infarction (MI) is a leading cause of morbidity and mortality across the world. It manifests as an imbalance between blood demand and blood delivery in the myocardium, which leads to cardiac ischemia and myocardial necrosis. While it is not easy to identify [...] Read more.
Myocardial infarction (MI) is a leading cause of morbidity and mortality across the world. It manifests as an imbalance between blood demand and blood delivery in the myocardium, which leads to cardiac ischemia and myocardial necrosis. While it is not easy to identify the first pathogenic cause of MI, the consequences are characterized by ischemia, chronic inflammation, and tissue degeneration. A poor MI prognosis is associated with extensive cardiac remodeling. A loss of viable cardiomyocytes is replaced with fibrosis, which reduces heart contractility and heart function. Recent advances have given rise to the concept of natural polyphenols. These bioactive compounds have been studied for their pharmacological properties and have proven successful in the treatment of cardiovascular diseases. Studies have focused on their various bioactivities, such as their antioxidant and anti-inflammatory effects and free radical scavenging. In this review, we summarized the effects and benefits of polyphenols on the cardiovascular injury, particularly on the treatment of myocardial infarction in animal and human studies. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessReview
Therapeutic Potential of Polyphenols-Loaded Polymeric Nanoparticles in Cardiovascular System
Molecules 2020, 25(15), 3322; https://doi.org/10.3390/molecules25153322 - 22 Jul 2020
Abstract
Numerous studies document an increased production of reactive oxygen species (ROS) with a subsequent decrease in nitric oxide (NO) bioavailability in different cardiovascular diseases, including hypertension, atherosclerosis, and heart failure. Many natural polyphenols have been demonstrated to decrease ROS generation and/or to induce [...] Read more.
Numerous studies document an increased production of reactive oxygen species (ROS) with a subsequent decrease in nitric oxide (NO) bioavailability in different cardiovascular diseases, including hypertension, atherosclerosis, and heart failure. Many natural polyphenols have been demonstrated to decrease ROS generation and/or to induce the endogenous antioxidant enzymatic defense system. Moreover, different polyphenolic compounds have the ability to increase the activity/expression of endothelial nitric oxide synthase (eNOS) with a subsequent enhancement of NO generation. However, as a result of low absorption and bioavailability of natural polyphenols, the beneficial effects of these substances are very limited. Recent progress in delivering polyphenols to the targeted tissues revealed new possibilities for the use of polymeric nanoparticles in increasing the efficiency and reducing the degradability of natural polyphenols. This review focuses on the effects of different natural polyphenolic substances, especially resveratrol, quercetin, curcumin, and cherry extracts, and their ability to bind to polymeric nanoparticles, and summarizes the effects of polyphenol-loaded nanoparticles, mainly in the cardiovascular system. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessReview
Natural Psychoplastogens As Antidepressant Agents
Molecules 2020, 25(5), 1172; https://doi.org/10.3390/molecules25051172 - 05 Mar 2020
Cited by 1
Abstract
Increasing prevalence and burden of major depressive disorder presents an unavoidable problem for psychiatry. Existing antidepressants exert their effect only after several weeks of continuous treatment. In addition, their serious side effects and ineffectiveness in one-third of patients call for urgent action. Recent [...] Read more.
Increasing prevalence and burden of major depressive disorder presents an unavoidable problem for psychiatry. Existing antidepressants exert their effect only after several weeks of continuous treatment. In addition, their serious side effects and ineffectiveness in one-third of patients call for urgent action. Recent advances have given rise to the concept of psychoplastogens. These compounds are capable of fast structural and functional rearrangement of neural networks by targeting mechanisms previously implicated in the development of depression. Furthermore, evidence shows that they exert a potent acute and long-term positive effects, reaching beyond the treatment of psychiatric diseases. Several of them are naturally occurring compounds, such as psilocybin, N,N-dimethyltryptamine, and 7,8-dihydroxyflavone. Their pharmacology and effects in animal and human studies were discussed in this article. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessReview
In Vitro and In Vivo Effects of Flavonoids on Peripheral Neuropathic Pain
Molecules 2020, 25(5), 1171; https://doi.org/10.3390/molecules25051171 - 05 Mar 2020
Cited by 6
Abstract
Neuropathic pain is a common symptom and is associated with an impaired quality of life. It is caused by the lesion or disease of the somatosensory system. Neuropathic pain syndromes can be subdivided into two categories: central and peripheral neuropathic pain. The present [...] Read more.
Neuropathic pain is a common symptom and is associated with an impaired quality of life. It is caused by the lesion or disease of the somatosensory system. Neuropathic pain syndromes can be subdivided into two categories: central and peripheral neuropathic pain. The present review highlights the peripheral neuropathic models, including spared nerve injury, spinal nerve ligation, partial sciatic nerve injury, diabetes-induced neuropathy, chemotherapy-induced neuropathy, chronic constriction injury, and related conditions. The drugs which are currently used to attenuate peripheral neuropathy, such as antidepressants, anticonvulsants, baclofen, and clonidine, are associated with adverse side effects. These negative side effects necessitate the investigation of alternative therapeutics for treating neuropathic pain conditions. Flavonoids have been reported to alleviate neuropathic pain in murine models. The present review elucidates that several flavonoids attenuate different peripheral neuropathic pain conditions at behavioral, electrophysiological, biochemical and molecular biological levels in different murine models. Therefore, the flavonoids hold future promise and can be effectively used in treating or mitigating peripheral neuropathic conditions. Thus, future studies should focus on the structure-activity relationships among different categories of flavonoids and develop therapeutic products that enhance their antineuropathic effects. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessReview
Pleiotropic Biological Effects of Dietary Phenolic Compounds and their Metabolites on Energy Metabolism, Inflammation and Aging
Molecules 2020, 25(3), 596; https://doi.org/10.3390/molecules25030596 - 29 Jan 2020
Cited by 1
Abstract
Dietary phenolic compounds are considered as bioactive compounds that have effects in different chronic disorders related to oxidative stress, inflammation process, or aging. These compounds, coming from a wide range of natural sources, have shown a pleiotropic behavior on key proteins that act [...] Read more.
Dietary phenolic compounds are considered as bioactive compounds that have effects in different chronic disorders related to oxidative stress, inflammation process, or aging. These compounds, coming from a wide range of natural sources, have shown a pleiotropic behavior on key proteins that act as regulators. In this sense, this review aims to compile information on the effect exerted by the phenolic compounds and their metabolites on the main metabolic pathways involved in energy metabolism, inflammatory response, aging and their relationship with the biological properties reported in high prevalence chronic diseases. Numerous in vitro and in vivo studies have demonstrated their pleiotropic molecular mechanisms of action and these findings raise the possibility that phenolic compounds have a wide variety of roles in different targets. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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Open AccessReview
Iridoids: Research Advances in Their Phytochemistry, Biological Activities, and Pharmacokinetics
Molecules 2020, 25(2), 287; https://doi.org/10.3390/molecules25020287 - 10 Jan 2020
Cited by 4
Abstract
Iridoids are a class of active compounds that widely exist in the plant kingdom. In recent years, with advances in phytochemical research, many compounds with novel structure and outstanding activity have been identified. Iridoid compounds have been confirmed to mainly exist as the [...] Read more.
Iridoids are a class of active compounds that widely exist in the plant kingdom. In recent years, with advances in phytochemical research, many compounds with novel structure and outstanding activity have been identified. Iridoid compounds have been confirmed to mainly exist as the prototype and aglycone and Ι and II metabolites, by biological transformation. These metabolites have been shown to have neuroprotective, hepatoprotective, anti-inflammatory, antitumor, hypoglycemic, and hypolipidemic activities. This review summarizes the new structures and activities of iridoids identified locally and globally, and explains their pharmacokinetics from the aspects of absorption, distribution, metabolism, and excretion according to the differences in their structures, thus providing a theoretical basis for further rational development and utilization of iridoids and their metabolites. Full article
(This article belongs to the Special Issue Biological Activity of Natural Substances and Their Derivatives)
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