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Natural Products in Prevention and Treatment of Metabolic Syndrome
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Natural Products in Prevention and Treatment of Metabolic Syndrome

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

Deadline for manuscript submissions: closed (31 December 2019) | Viewed by 80207

Special Issue Editors

Dr. Jianbo Wan

E-Mail Website
Guest Editor
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
Interests: metabolic syndrome; alcoholic liver disease; nonalcoholic liver disease; atherosclerosis; metabolomics; LC-MS
Special Issues, Collections and Topics in MDPI journals
Dr. Ligen Lin

E-Mail Website
Guest Editor
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, China
Interests: natural products chemistry; obesity and diabetes; adipose tissue and skeletal muscle remodeling; hunger and satiety regulation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Metabolic syndrome is a complex cluster of metabolic disorders, which increase a patient's risk of developing diabetes mellitus and cardiovascular diseases, the main causes of morbidity and mortality in the world. Despite the availability of many pharmacotherapies, new classes of pharmacological agents capable of reducing overall risk are needed. An accumulating number of studies have indicates that some natural products or moleules are able to modulate metabolic syndrome and its risk factors. This Special Issue aims to identify and review the latest natural products or moleules that can prevent and treat metabolic syndrome and its risk factors.

Prof. Dr. Jianbo Wan
Dr. Ligen Lin
Guest Editors

Manuscript Submission Information

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Keywords

  • Metabolic Syndrome
  • Cardiovascular Diseases
  • Alcoholic Liver Disease
  • Non-alcoholic Liver Disease
  • Obesity
  • Insulin Resistance and Diabetes
  • Dyslipidemia
  • Pancreatic β-cell failure

Published Papers (16 papers)

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Research

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12 pages, 1074 KiB  
Article
Simultaneous Determination of α-Glucosidase Inhibitory Triterpenoids in Psidium guajava Using HPLC–DAD–ELSD and Pressurized Liquid Extraction
by In-Cheng Chao, Ying Chen, Mei-Hua Gao, Li-Gen Lin, Xiao-Qi Zhang, Wen-Cai Ye and Qing-Wen Zhang
Molecules 2020, 25(6), 1278; https://doi.org/10.3390/molecules25061278 - 11 Mar 2020
Cited by 7 | Viewed by 3124
Abstract
Psidium guajava, a popular food and medicine dual purposes plant cultivated in tropical and subtropical regions, has been widely used as food crop and folk medicine, such as anti-diabetes agent, around the world. Triterpenoids have been considered as the major active ingredients [...] Read more.
Psidium guajava, a popular food and medicine dual purposes plant cultivated in tropical and subtropical regions, has been widely used as food crop and folk medicine, such as anti-diabetes agent, around the world. Triterpenoids have been considered as the major active ingredients of P. guajava. In the present study, a high-performance liquid chromatography coupled with diode array and evaporative light scattering detectors (HPLC–DAD–ELSD) method was developed for simultaneous determination of nine triterpenoids in P. guajava. Pressurized liquid extraction (PLE) was performed for sample preparation, and the analysis was achieved on a Cosmosil 5C18-MS-II (Nacalai Tesque, Kyoto, Japan) column eluted with gradient 0.1% aqueous formic acid-methanol system. The drift tube temperature of ELSD was set at 40 °C, and nitrogen flow-rate was at 1.6 L/min. All calibration curves for the analytes showed good linear regression (R2 > 0.9992) within test ranges. The established method was validated for intra-day and inter-day precisions (RSDs < 5%) and accuracy (recovery 94.23–106.87%). The validated method was successfully applied to determinate nine triterpenoids in 15 samples from the leave or fruit of P. guajava. In addition, the α-glucosidase inhibition assay showed good α-glucosidase inhibition activity in almost all the determined triterpenoids. The present study suggested that triterpenoids should be the quality control markers for P. guajava and HPLC–DAD–ELSD was an effective tool for the quality control of P. guajava. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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17 pages, 56177 KiB  
Article
Beneficial Metabolic Effects of Chitosan and Chitosan Oligosaccharide on Epididymal WAT Browning and Thermogenesis in Obese Rats
by Jin Wang, Wanping He, Di Yang, Hua Cao, Yan Bai, Jiao Guo and Zhengquan Su
Molecules 2019, 24(24), 4455; https://doi.org/10.3390/molecules24244455 - 05 Dec 2019
Cited by 21 | Viewed by 3718
Abstract
Many anti-obesity chemicals have been withdrawn from the market due to serious adverse reactions, and the researchers have turned their attention to low-toxic natural products. Previous studies have demonstrated that chitosan (CTS) and chitosan oligosaccharide (COS) were low-toxic natural products for the use [...] Read more.
Many anti-obesity chemicals have been withdrawn from the market due to serious adverse reactions, and the researchers have turned their attention to low-toxic natural products. Previous studies have demonstrated that chitosan (CTS) and chitosan oligosaccharide (COS) were low-toxic natural products for the use of weight loss. However, it is still unclear whether CTS and COS have positive effects on the thermogenesis. In this study, CTS and COS significantly reduced the weight gain of rats without affecting food intake and effectively inhibited adipose tissue hypertrophy and hyperplasia. Consistently, CTS and COS significantly increased the thermogenic capacity of obese rats induced by high-fat diet (HFD) and increased the expression of browning genes and proteins (UCP1, PGC1α, PRMD16, and ATF2) in white adipose tissue (WAT) and brown adipose tissue (BAT). In vitro, COS inhibited the formation of mature adipocytes and increased the expression of browning genes. In conclusion, COS and CTS was used to explore the function and mechanism on thermogenesis, and CTS and COS can increase the browning of WAT and the thermogenesis of BAT to inhibit obesity. This effect may be achieved by promoting the expression of browning and thermogenic genes, providing new ideas for the utilization of COS and CTS. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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15 pages, 5397 KiB  
Article
20(S)-Protopanaxadiol Saponins Mainly Contribute to the Anti-Atherogenic Effects of Panax notoginseng in ApoE Deficient Mice
by Conghui Liu, Ruibing Feng, Jian Zou, Fangbo Xia and Jian-Bo Wan
Molecules 2019, 24(20), 3723; https://doi.org/10.3390/molecules24203723 - 16 Oct 2019
Cited by 17 | Viewed by 3491
Abstract
Atherosclerosis mainly contributes to cardiovascular disease, a leading cause of global morbidity and mortality. Panax notoginseng saponins (PNS) are proved to therapeutically attenuate the formation of atherosclerotic lesions. According to different sapogenin, PNS are generally classified into 20(S)-protopanaxadiol saponins (PDS) and [...] Read more.
Atherosclerosis mainly contributes to cardiovascular disease, a leading cause of global morbidity and mortality. Panax notoginseng saponins (PNS) are proved to therapeutically attenuate the formation of atherosclerotic lesions. According to different sapogenin, PNS are generally classified into 20(S)-protopanaxadiol saponins (PDS) and 20(S)-protopanaxatriol saponins (PTS). It was reported that PDS and PTS might exert diverse or even antagonistic bioactivities. In this study, the probable effects of PTS and PDS on atherosclerotic development were investigated and compared in ApoE-deficient mice (ApoE−/−). Male mice were gavaged daily by PNS (200 mg/kg/d), PTS (100 mg/kg/d), or PDS (100 mg/kg/d), respectively for eight weeks. The treatments of PNS and PDS, but not PTS, showed decreased atherosclerotic lesions in the entire aorta by 45.6% and 41.3%, respectively, as evaluated by an en-face method. Both PNS and PDS can improve the plaque vulnerability, as evidenced by the increased collagen fiber, increased expression of α- smooth muscle actin (α-SMA), and decreased Cluster of differentiation 14 (CD14). Additionally, PDS also inhibit the nuclear factor kappa B (NF-κB)-mediated vascular inflammation in the aorta. In conclusion, PDS, but not PTS, might mainly contribute to the anti-atherosclerosis of P. notoginseng. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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14 pages, 1752 KiB  
Article
Constituents and Anti-Hyperuricemia Mechanism of Traditional Chinese Herbal Formulae Erding Granule
by Wugang Zhang, Wendi Du, Guofeng Li, Chen Zhang, Wuliang Yang, Shilin Yang, Yulin Feng and Haifang Chen
Molecules 2019, 24(18), 3248; https://doi.org/10.3390/molecules24183248 - 06 Sep 2019
Cited by 13 | Viewed by 3290
Abstract
Erding granule (EDG) is a traditional Chinese medicine that has recently been identified as having anti-hypouricemic effects. However, the active components and underlying mechanism for this new indication have not been elucidated. Therefore, we compared the effects of different EDG extracts (water, 50% [...] Read more.
Erding granule (EDG) is a traditional Chinese medicine that has recently been identified as having anti-hypouricemic effects. However, the active components and underlying mechanism for this new indication have not been elucidated. Therefore, we compared the effects of different EDG extracts (water, 50% ethanol and 95% ethanol) on serum uric acid concentrations in the hyperuricemia model mouse. We also analyzed the constituents of different extracts by ultra-high performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS) to observe the variation between the active and inactive products. Extract activity and target site were evaluated by assessing uric acid- and inflammation-suppressing effects along with evaluating ability to regulate the uric acid transporter. The results showed that the 50% ethanol extract (EDG-50) had an obvious serum uric acid concentration lowering effect compared with water (EDG-S) and the 95% ethanol extract (EDG-95). UHPLC-Q-TOF-MS/MS analysis showed that EDG-50 was compositionally different to EDG-S and EDG-95. EDG-50 showed dose-dependent effects on reducing uric acid, suppressing inflammation and regulating uric acid transporters. Moreover, western blot analysis showed that EDG-50 down-regulated GLUT9 and URAT1 expression, and up-regulated OAT1 expression. Therefore, our findings enable the preliminarily conclusion that EDG-50 lowers serum uric acid concentrations, mainly by down-regulating the expression of GLUT9 and URAT1 proteins and up-regulating the expression of OAT1 proteins. This provides a research basis for clinical use of EDG as an anti-hyperuricemic agent. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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14 pages, 2523 KiB  
Article
A Limonoid, 7-Deacetoxy-7-Oxogedunin (CG-1) from Andiroba (Carapa guianensis, Meliaceae) Lowers the Accumulation of Intracellular Lipids in Adipocytes via Suppression of IRS-1/Akt-Mediated Glucose Uptake and a Decrease in GLUT4 Expression
by Chihiro Matsumoto, Atsushi Koike, Reiko Tanaka and Ko Fujimori
Molecules 2019, 24(9), 1668; https://doi.org/10.3390/molecules24091668 - 28 Apr 2019
Cited by 15 | Viewed by 3535
Abstract
Limonoids are phytochemicals with a variety of biological properties. In the present study, we elucidated the molecular mechanism of suppression of adipogenesis in adipocytes by a limonoid, 7-deacetoxy-7-oxogedunin (CG-1) from Carapa guianensis (Meliaceae), known as andiroba. CG-1 reduced the accumulation of intracellular triglycerides [...] Read more.
Limonoids are phytochemicals with a variety of biological properties. In the present study, we elucidated the molecular mechanism of suppression of adipogenesis in adipocytes by a limonoid, 7-deacetoxy-7-oxogedunin (CG-1) from Carapa guianensis (Meliaceae), known as andiroba. CG-1 reduced the accumulation of intracellular triglycerides in a concentration-dependent manner. The expression levels of the adipogenic, lipogenic, and lipolytic genes were decreased by CG-1 treatment, whereas the glycerol release level was not affected. When CG-1 was added into the medium during days 0-2 of 6-days-adipogenesis, the accumulation of intracellular lipids and the mRNA levels of the adipogenesis-related genes were decreased. In addition, the phosphorylation level of insulin receptor substrate-1 (IRS-1) and Akt in the early phase of adipocyte differentiation (within 1 day after initiating adipocyte differentiation) was reduced by CG-1. Furthermore, insulin-activated translocation of glucose transporter 4 to the plasma membranes in adipocytes was suppressed by CG-1, followed by decreased glucose uptake into the cells. These results indicate that an andiroba limonoid CG-1 suppressed the accumulation of intracellular lipids in the early phase of adipocyte differentiation through repression of IRS-1/Akt-mediated glucose uptake in adipocytes. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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16 pages, 4882 KiB  
Article
Therapeutic Effect of Chitooligosaccharide Tablets on Lipids in High-Fat Diets Induced Hyperlipidemic Rats
by Di Yang, Canji Hu, Xiaoyi Deng, Yan Bai, Hua Cao, Jiao Guo and Zhengquan Su
Molecules 2019, 24(3), 514; https://doi.org/10.3390/molecules24030514 - 31 Jan 2019
Cited by 44 | Viewed by 3989
Abstract
Chitooligosaccharide is beneficial for inhibiting dyslipidemia and reducing atherosclerotic and hyperlipidemic risk. The purpose of this study was to investigate the cholesterol-regulating effects and potential mechanisms of Chitooligosaccharide tablets (CFTs) in high-fat diet-induced hyperlipidemic rats. The results revealed that CFTs can regulate serum [...] Read more.
Chitooligosaccharide is beneficial for inhibiting dyslipidemia and reducing atherosclerotic and hyperlipidemic risk. The purpose of this study was to investigate the cholesterol-regulating effects and potential mechanisms of Chitooligosaccharide tablets (CFTs) in high-fat diet-induced hyperlipidemic rats. The results revealed that CFTs can regulate serum lipid levels in hyperlipidemic rats in a dosage-dependent manner. Synchronously, gene expressions related to cholesterol excretion were upregulated in a dosage-dependent manner, including cholesterol 7α-hydroxylase (CYP7A1), liver X receptor α (LXRA), peroxisome proliferation-activated receptor-α (PPARα) and low-density lipoprotein receptor (LDLR), whereas cholesterol synthetic gene expressions including 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGCR) and sterol-responsive element binding protein-2 (SREBP2) were reduced. This work highlights that CFTs have potential as natural products to prevent and treat metabolic hyperlipidemia syndrome, probably due to the reduction of cholesterol biosynthesis and through cholesterol elimination; they also improve the pathological changes of liver tissue in rats, alleviate liver damage, maintain normal lipid metabolism in the liver, ameliorate hepatic glycolipid disorders and accelerate TC operation, and reduce blood lipid levels. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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14 pages, 1812 KiB  
Article
Triterpenoids from Cyclocarya paliurus that Enhance Glucose Uptake in 3T3-L1 Adipocytes
by Zhu-Jun Fang, Sheng-Nan Shen, Jia-Min Wang, Yong-Jiang Wu, Chang-Xin Zhou, Jian-Xia Mo, Li-Gen Lin and Li-She Gan
Molecules 2019, 24(1), 187; https://doi.org/10.3390/molecules24010187 - 06 Jan 2019
Cited by 30 | Viewed by 4879
Abstract
Four previously undescribed compounds, including three rarely occurring seco-dammarane triterpenoid glycosides and a pentacyclic triterpenic acid, were isolated from a 70% ethanol extract of the leaves of Cyclocarya paliurus (Juglandaceae), along with eleven known triterpenoids. Their structures were determined by spectroscopic techniques, [...] Read more.
Four previously undescribed compounds, including three rarely occurring seco-dammarane triterpenoid glycosides and a pentacyclic triterpenic acid, were isolated from a 70% ethanol extract of the leaves of Cyclocarya paliurus (Juglandaceae), along with eleven known triterpenoids. Their structures were determined by spectroscopic techniques, including 2D NMR and HRESIMS, as well as chemical methods. Among them, several triterpenoids enhanced insulin stimulated glucose uptake in both 3T3-L1 adipocytes and C2C12 myotubes. Furthermore, compound 1 dose-dependently increased glucose uptake through activating AMP-activated protein kinase (AMPK)-p38 pathway. Collectively, triterpenoids from C. paliurus could be developed as insulin sensitizers, which might have therapeutic potential for insulin resistance and hyperglycemia. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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11 pages, 2174 KiB  
Article
A New Strategy for Rapidly Screening Natural Inhibitors Targeting the PCSK9/LDLR Interaction In Vitro
by Li Li, Chen Shen, Ya-Xuan Huang, Ya-Nan Li, Xiu-Feng Liu, Xu-Ming Liu and Ji-Hua Liu
Molecules 2018, 23(9), 2397; https://doi.org/10.3390/molecules23092397 - 19 Sep 2018
Cited by 9 | Viewed by 5074
Abstract
The interaction between proprotein convertase subtilisin/kexin type 9 (PCSK9) and the low-density lipoprotein receptor (LDLR) is a promising target for the treatment of hyperc-holesterolemia. In this study, a new method based on competitive affinity and tag detection was developed, which aimed to evaluate [...] Read more.
The interaction between proprotein convertase subtilisin/kexin type 9 (PCSK9) and the low-density lipoprotein receptor (LDLR) is a promising target for the treatment of hyperc-holesterolemia. In this study, a new method based on competitive affinity and tag detection was developed, which aimed to evaluate potent natural inhibitors preventing the interaction of PCSK9/LDLR directly. Herein, natural compounds with efficacy in the treatment of hypercholesterolemia were chosen to investigate their inhibitory activities on the PCSK9/LDLR interaction. Two of them, polydatin (1) and tetrahydroxydiphenylethylene-2-O-glucoside (2), were identified as potential inhibitors for the PCSK9/LDLR interaction and were proven to prevent PCSK9-mediated LDLR degradation in HepG2 cells. The results suggested that this strategy could be applied for evaluating potential bioactive compounds inhibiting the interaction of PCSK9/LDLR and this strategy could accelerate the discovery of new drug candidates for the treatment of PCSK9-mediated hypercholesterolemia. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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12 pages, 1189 KiB  
Article
Daily Consumption of Chocolate Rich in Flavonoids Decreases Cellular Genotoxicity and Improves Biochemical Parameters of Lipid and Glucose Metabolism
by Aldo Leyva-Soto, Rocio Alejandra Chavez-Santoscoy, Linda Ramona Lara-Jacobo, Ana Vianey Chavez-Santoscoy and Lina Natalia Gonzalez-Cobian
Molecules 2018, 23(9), 2220; https://doi.org/10.3390/molecules23092220 - 01 Sep 2018
Cited by 36 | Viewed by 9675
Abstract
In recent years, the incidence of atherosclerotic cardiovascular disease, obesity, and diabetes has increased largely worldwide. In the present work, we evaluated the genoprotective effect of the consumption of flavonoids-rich chocolate on 84 young volunteers. Biochemical indicators related to the prevention and treatment [...] Read more.
In recent years, the incidence of atherosclerotic cardiovascular disease, obesity, and diabetes has increased largely worldwide. In the present work, we evaluated the genoprotective effect of the consumption of flavonoids-rich chocolate on 84 young volunteers. Biochemical indicators related to the prevention and treatment of cardiovascular risk and metabolic syndrome were also determined. A randomized, placebo-controlled, double-blind study was performed in the Autonomous University of Baja California. The treatments comprised the daily consumption of either 2 g of dark chocolate containing 70% cocoa, or 2 g of milk chocolate, for 6 months. The total amount of phenolic compounds and flavonoids was determined in both types of chocolate. Anthropometrical and Biochemical parameters were recorded prior to and after the study. The evaluation of the genotoxicity in buccal epithelial cells was performed throughout the duration of the study. Flavonoids from cocoa in dark chocolate significantly prevented DNA damage, and improved the nucleus integrity of cells. This effect could be related to the antioxidant capacity of the dark chocolate that decreased cellular stress. Biochemical parameters (total cholesterol, triglycerides, and LDL-cholesterol level in blood) and anthropometrical parameters (waist circumference) were improved after six months of daily intake of 2 g of dark chocolate with a 70% of cocoa. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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15 pages, 2108 KiB  
Article
Effects of Rhizome Extract of Dioscorea batatas and Its Active Compound, Allantoin, on the Regulation of Myoblast Differentiation and Mitochondrial Biogenesis in C2C12 Myotubes
by Junnan Ma, Seok Yong Kang, Xianglong Meng, An Na Kang, Jong Hun Park, Yong-Ki Park and Hyo Won Jung
Molecules 2018, 23(8), 2023; https://doi.org/10.3390/molecules23082023 - 13 Aug 2018
Cited by 31 | Viewed by 5819
Abstract
With the aging process, a loss of skeletal muscle mass and dysfunction related to metabolic syndrome is observed in older people. Yams are commonly use in functional foods and medications with various effects. The present study was conducted to investigate the effects of [...] Read more.
With the aging process, a loss of skeletal muscle mass and dysfunction related to metabolic syndrome is observed in older people. Yams are commonly use in functional foods and medications with various effects. The present study was conducted to investigate the effects of rhizome extract of Dioscorea batatas (Dioscoreae Rhizoma, Chinese yam) and its bioactive compound, allantoin, on myoblast differentiation and mitochondrial biogenesis in skeletal muscle cells. Yams were extracted in water and allantoin was analyzed by high performance liquid chromatography (HPLC). The expression of myosin heavy chain (MyHC) and mitochondrial biogenesis-regulating factors, peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), sirtuin-1 (Sirt-1), nuclear respiratory factor-1 (NRF-1) and transcription factor A, mitochondrial (TFAM), and the phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC) were determined in C2C12 myotubes by reverse transcriptase (RT)-polymerase chain reaction (RT-PCR) or western blot. The glucose levels and total ATP contents were measured by glucose consumption, glucose uptake and ATP assays, respectively. Treatment with yam extract (1 mg/mL) and allantoin (0.2 and 0.5 mM) significantly increased MyHC expression compared with non-treated myotubes. Yam extract and allantoin significantly increased the expression of PGC-1α, Sirt-1, NRF-1 and TFAM, as well as the phosphorylation of AMPK and ACC in C2C12 myotubes. Furthermore, yam extract and allantoin significantly increased glucose uptake levels and ATP contents. Finally, HPLC analysis revealed that the yam water extract contained 1.53% of allantoin. Yam extract and allantoin stimulated myoblast differentiation into myotubes and increased energy production through the upregulation of mitochondrial biogenesis regulators. These findings indicate that yam extract and allantoin can help to prevent skeletal muscle dysfunction through the stimulation of the energy metabolism. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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13 pages, 725 KiB  
Article
Isolation, Structural Elucidation, and α-Glucosidase Inhibitory Activities of Triterpenoid Lactones and Their Relevant Biogenetic Constituents from Ganoderma resinaceum
by Xian-Qiang Chen, Li-Gen Lin, Jing Zhao, Ling-Xiao Chen, Yu-Ping Tang, De-Lun Luo and Shao-Ping Li
Molecules 2018, 23(6), 1391; https://doi.org/10.3390/molecules23061391 - 08 Jun 2018
Cited by 6 | Viewed by 3610
Abstract
Ganoderma resinaceum has been used as an ethnomedicine for lowering blood sugar. To clarify the bioactive chemical constituents contributing to lower blood sugar, chemical investigation on the fruiting bodies of Ganoderma resinaceum was conducted by chromatographic techniques, and led to the isolation of [...] Read more.
Ganoderma resinaceum has been used as an ethnomedicine for lowering blood sugar. To clarify the bioactive chemical constituents contributing to lower blood sugar, chemical investigation on the fruiting bodies of Ganoderma resinaceum was conducted by chromatographic techniques, and led to the isolation of 14 compounds. Their structures were elucidated as triterpenoid lactones (1–4 and 8) and ganoderma acids (5–7 and 9–14) based on the analysis of extensive spectroscopy (mass spectrometry (MS), nuclear magnetic resonance (NMR), infrared (IR), and ultraviolet (UV)) and comparison with literature data. Compounds 3, 5, 6, and 9–14 were evaluated for α-glucosidase inhibitory activity. Compounds 1–7 are new compounds. Compounds 1–4 and 8 were characteristic of an oxaspirolactone moiety, consisting of a five-membered ether ring, a five-membered lactone ring, and a characteristic C-23 spiro carbon. It is rare for natural products that such an oxaspirolactone moiety occurred in the lanostane-type triterpenoids. Compounds 5–7 and 9–14 may be important intermediates of the biosynthetic pathways of 1–4 and 8. Compounds 1 and 2 showed more potent inhibitory activity against α-glucosidase compared with the positive control drug acarbose with IC50 value of 0.75 ± 0.018 mM and 1.64 ± 0.022 mM, respectively. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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Review

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17 pages, 2074 KiB  
Review
Xanthones, A Promising Anti-Inflammatory Scaffold: Structure, Activity, and Drug Likeness Analysis
by Zheling Feng, Xiuqiang Lu, Lishe Gan, Qingwen Zhang and Ligen Lin
Molecules 2020, 25(3), 598; https://doi.org/10.3390/molecules25030598 - 30 Jan 2020
Cited by 52 | Viewed by 6276
Abstract
Inflammation is the body’s self-protective response to multiple stimulus, from external harmful substances to internal danger signals released after trauma or cell dysfunction. Many diseases are considered to be related to inflammation, such as cancer, metabolic disorders, aging, and neurodegenerative diseases. Current therapeutic [...] Read more.
Inflammation is the body’s self-protective response to multiple stimulus, from external harmful substances to internal danger signals released after trauma or cell dysfunction. Many diseases are considered to be related to inflammation, such as cancer, metabolic disorders, aging, and neurodegenerative diseases. Current therapeutic approaches include mainly non-steroidal anti-inflammatory drugs and glucocorticoids, which are generally of limited effectiveness and severe side-effects. Thus, it is urgent to develop novel effective anti-inflammatory therapeutic agents. Xanthones, a unique scaffold with a 9H-Xanthen-9-one core structure, widely exist in natural sources. Till now, over 250 xanthones were isolated and identified in plants from the families Gentianaceae and Hypericaceae. Many xanthones have been disclosed with anti-inflammatory properties on different models, either in vitro or in vivo. Herein, we provide a comprehensive and up-to-date review of xanthones with anti-inflammatory properties, and analyzed their drug likeness, which might be potential therapeutic agents to fight against inflammation-related diseases. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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25 pages, 295 KiB  
Review
The Potential of South African Herbal Tisanes, Rooibos and Honeybush in the Management of Type 2 Diabetes Mellitus
by Olawale R. Ajuwon, Ademola O. Ayeleso and Gbenga A. Adefolaju
Molecules 2018, 23(12), 3207; https://doi.org/10.3390/molecules23123207 - 05 Dec 2018
Cited by 34 | Viewed by 4844
Abstract
Diabetes mellitus is a metabolic disease that can lead to high morbidity, mortality and long-term complications. Available treatment strategies, which are mainly based on treating hyperglycemia, with insulin and other pharmacological agents are not completely efficient and can even lead to development of [...] Read more.
Diabetes mellitus is a metabolic disease that can lead to high morbidity, mortality and long-term complications. Available treatment strategies, which are mainly based on treating hyperglycemia, with insulin and other pharmacological agents are not completely efficient and can even lead to development of unwanted side effects. Scientific evidence suggests that bioactive compounds from teas and other plant-based foods, which are known source of natural antioxidants, could be an attractive strategy to preferentially treat and manage type 2 diabetes mellitus (T2DM) and thus, have significant therapeutic implications. In this review, we attempt an in-depth analysis and discussion of the current progress in our understanding of the antidiabetic potential of two commercialized South Africa herbal tisanes—Rooibos and Honeybush and their polyphenols. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
29 pages, 2873 KiB  
Review
Intestinal Saturated Long-Chain Fatty Acid, Glucose and Fructose Transporters and Their Inhibition by Natural Plant Extracts in Caco-2 Cells
by Katharina Schreck and Matthias F. Melzig
Molecules 2018, 23(10), 2544; https://doi.org/10.3390/molecules23102544 - 06 Oct 2018
Cited by 17 | Viewed by 8448 | Correction
Abstract
The intestinal absorption of fatty acids, glucose and fructose is part of the basic requirements for the provision of energy in the body. High access of saturated long-chain fatty acids (LCFA), glucose and fructose can facilitate the development of metabolic diseases, particularly the [...] Read more.
The intestinal absorption of fatty acids, glucose and fructose is part of the basic requirements for the provision of energy in the body. High access of saturated long-chain fatty acids (LCFA), glucose and fructose can facilitate the development of metabolic diseases, particularly the metabolic syndrome and type-2 diabetes mellitus (T2DM). Research has been done to find substances which decelerate or inhibit intestinal resorption of these specific food components. Promising targets are the inhibition of intestinal long-chain fatty acid (FATP2, FATP4), glucose (SGLT1, GLUT2) and fructose (GLUT2, GLUT5) transporters by plant extracts and by pure substances. The largest part of active components in plant extracts belongs to the group of polyphenols. This review summarizes the knowledge about binding sites of named transporters and lists the plant extracts which were tested in Caco-2 cells regarding uptake inhibition. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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16 pages, 1423 KiB  
Review
Morphological Characteristics, Nutrients, and Bioactive Compounds of Zizania latifolia, and Health Benefits of Its Seeds
by Ning Yan, Yongmei Du, Xinmin Liu, Cheng Chu, John Shi, Hongbo Zhang, Yanhua Liu and Zhongfeng Zhang
Molecules 2018, 23(7), 1561; https://doi.org/10.3390/molecules23071561 - 28 Jun 2018
Cited by 45 | Viewed by 7304
Abstract
Zizania latifolia (tribe Oryzeae Dum., subfamily Oryzoideae Care, family Gramineae) is native to East Asian countries. The seeds of Z. latifolia (Chinese wild rice) have been consumed as a cereal in China for >3000 years. Z. latifolia forms swollen culms when infected with [...] Read more.
Zizania latifolia (tribe Oryzeae Dum., subfamily Oryzoideae Care, family Gramineae) is native to East Asian countries. The seeds of Z. latifolia (Chinese wild rice) have been consumed as a cereal in China for >3000 years. Z. latifolia forms swollen culms when infected with Ustilago esculenta, which is the second most-cultivated aquatic vegetable in China. The current review summarizes the nutrients and bioactive compounds of Z. latifolia, and health benefits of its seeds. The seeds of Z. latifolia contain proteins, minerals, vitamins, and bioactive compounds, the activities of which—for example, antioxidant activity—have been characterized. Various health benefits are associated with their consumption, such as alleviation of insulin resistance and lipotoxicity, and protection against cardiovascular disease. Chinese wild rice may be used to prevent and treat metabolic disease, such as diabetes, obesity, and cardiovascular diseases. Various compounds were isolated from the swollen culm, and aerial parts of Z. latifolia. The former suppresses osteoclast formation, inhibits growth of rat glioma cells, and may act as antioxidants and immunomodulators in drugs or foods. The latter exerts anti-fatigue, anti-inflammatory, and anti-allergic effects. Thus, Z. latifolia may be used to produce nutraceuticals and functional foods. Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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3 pages, 1445 KiB  
Correction
Correction: Schreck, K. and Melzig, M.F. Intestinal Saturated Long-Chain Fatty Acid, Glucose and Fructose Transporters and their Inhibition by Natural Plant Extracts in Caco-2 Cells. Molecules, 2018, 23, 2544
by Katharina Schreck and Matthias F. Melzig
Molecules 2018, 23(12), 3290; https://doi.org/10.3390/molecules23123290 - 11 Dec 2018
Cited by 2 | Viewed by 2115
Abstract
The authors wish to make the following correction to their paper [...] Full article
(This article belongs to the Special Issue Natural Products in Prevention and Treatment of Metabolic Syndrome)
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