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A Feasible Approach for Natural Products to Treatment of Diseases

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

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 36438

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Guest Editor
School of Dentistry and Medical Sciences, Charles Sturt University, Panorama Avenue, Bathurst, NSW 2795, Australia
Interests: evidence-based practice; bee venom; nutrition; reproduction; cancer; natural medicine
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
School of Dentistry and Medical Sciences, Charles Sturt University, Panorama Avenue, Bathurst, NSW 2795, Australia
Interests: evidence-based complementary medicine; nutrition; naturopathy; phytotherapy; natural medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

A natural product is a compound or substance that originated from living beings. Natural products from both plant and animal sources have been used to treat diseases and illnesses since ancient times. Roots, leaves, rhizomes, or barks of medicinal plants are commonly featured in the herbal preparations of many traditional medicinal systems. Similarly, hooves, skins, bones, feathers, and tusks can be essential ingredients in the preparation of Indigenous curative or protective remedies. Many natural products, such as curcumin from turmeric, catechin from green tea, and astaxanthin from shellfish, are consumed as herbal remedies, functional foods, nutritional supplements, or wellness products to improve health and wellbeing, especially among many with underlying chronic conditions.

Modern medicine has also benefited from the characterisation of lead compounds from natural products. Acetylsalicylic acid, or more commonly known as aspirin, is a synthetic derivative of salicylic acid naturally found in willow bark, a traditional pain remedy. Quinine, a medication used to treat malaria, is a bitter compound that comes from the cinchona tree bark. Furthermore, Taxanes, a class of diterpenes initially identified from plants of the genus Taxus, are the mainstay chemotherapy today in the form of paclitaxel and docetaxel. In fact, over 60% of the current anticancer drugs were derived from natural sources, in one way or another.

The potential of natural products for the treatment of diseases remains enormous as our understanding so far is just the tip of an iceberg. Much preclinical and clinical research is required to uncover the active constituents, mechanisms of actions, pharmacokinetics, safety, and toxicity of natural products for therapeutic use. Other issues to address include extraction, isolation, and standardisation of any naturally derived compounds and their effective mode of therapeutic delivery. Hence, much research is needed before any natural products can be feasibly applied in treatment.

In this Special Issue, we invite researchers to contribute recent original research and review articles that will strengthen knowledge of not only the therapeutic or preventative utilities of natural products but also the mechanisms, methods or processes of treatment.   

Dr. Sokcheon Pak
Dr. Soo Liang Ooi
Guest Editors

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Keywords

  • traditional medicine
  • flavonoids
  • anti-inflammatory agents
  • chemotherapy
  • active compounds
  • nanotechnology

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Published Papers (14 papers)

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Editorial

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4 pages, 192 KiB  
Editorial
Editorial: A Feasible Approach for Natural Products to Treatment of Diseases
by Soo Liang Ooi and Sok Cheon Pak
Molecules 2023, 28(9), 3791; https://doi.org/10.3390/molecules28093791 - 28 Apr 2023
Cited by 1 | Viewed by 748
Abstract
The potential of natural products from both plant and animal sources to treat diseases remains enormous, as our understating forms just the tip of the iceberg [...] Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)

Research

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13 pages, 2795 KiB  
Article
Oxalactam A, a Novel Macrolactam with Potent Anti-Rhizoctonia solani Activity from the Endophytic Fungus Penicillium oxalicum
by Ruizhen Zhang, Yingrun Ma, Ming-Ming Xu, Xinyi Wei, Cheng-Bin Yang, Fei Zeng, Jin-Ao Duan, Chun-Tao Che, Junfei Zhou and Ming Zhao
Molecules 2022, 27(24), 8811; https://doi.org/10.3390/molecules27248811 - 12 Dec 2022
Cited by 2 | Viewed by 1498
Abstract
A novel macrolactam named oxalactam A (1), three known dipeptides (24) as well as other known alkaloids (57) were obtained from the endophytic fungus Penicillium oxalicum, which was derived from the tuber [...] Read more.
A novel macrolactam named oxalactam A (1), three known dipeptides (24) as well as other known alkaloids (57) were obtained from the endophytic fungus Penicillium oxalicum, which was derived from the tuber of Icacina trichantha (Icacinaceae). All chemical structures were established based on spectroscopic data, chemical methods, ECD calculations, and 13C-DP4+ analysis. Among them, oxalactam A (1) is a 16-membered polyenic macrolactam bearing a new skeleton of 2,9-dimethyl-azacyclohexadecane core and exhibited potent anti-Rhizoctonia solani activity with a MIC value of 10 μg/mL in vitro. The plausible biosynthetic pathway of 1 was also proposed via the alanyl protecting mechanism. Notably, three dipeptides (24) were first identified from the endophytic fungus P. oxalicum and the NMR data of cyclo(L-Trp-L-Glu) (2) was reported for the first time. In addition, the binding interactions between compound 1 and the sterol 14α-demethylase enzyme (CYP51) were studied by molecular docking and dynamics technologies, and the results revealed that the 16-membered polyenic macrolactam could be a promising CYP51 inhibitor to develop as a new anti-Rhizoctonia solani fungicide. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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13 pages, 2817 KiB  
Article
Effect of Holoptelea integrifolia (Roxb.) Planch. n-Hexane Extract and Its Bioactive Compounds on Wound Healing and Anti-Inflammatory Activity
by Kanokwan Somwong, Pattawika Lertpatipanpong, Wutigri Nimlamool, Aussara Panya, Yingmanee Tragoolpua, Rujipas Yongsawas, Wandee Gritsanapan, Hataichanok Pandith and Seung Joon Baek
Molecules 2022, 27(23), 8540; https://doi.org/10.3390/molecules27238540 - 04 Dec 2022
Cited by 2 | Viewed by 1719
Abstract
The stem bark of Holoptelea integrifolia (Roxb.) Planch. has been applied for the treatment of human cutaneous diseases as well as canine demodicosis in several countries. However, no detailed mechanistic studies have been reported to support their use. In this study, thin-layer chromatography [...] Read more.
The stem bark of Holoptelea integrifolia (Roxb.) Planch. has been applied for the treatment of human cutaneous diseases as well as canine demodicosis in several countries. However, no detailed mechanistic studies have been reported to support their use. In this study, thin-layer chromatography and gas chromatography were used to screen phytochemicals from the fresh stem bark extract of H. integrifolia. We found the two major bioactive compounds, friedelin and lupeol, and their activity on wound healing was further investigated in keratinocytes. Both bioactive compounds significantly reduced wound area and increased keratinocyte migration by increasing matrix metalloproteinases-9 production. Subsequently, we found that the mRNA gene expressions of cadherin 1 and desmoglobin 1 significantly decreased, whereas the gene expression involved in keratinocyte proliferation and homeostasis (keratin-17) increased in compound-treated human immortalized keratinocytes cells. The expression of inflammatory genes (cyclooxygenase-2 and inducible nitric oxide synthase) and pro-inflammatory cytokine genes (tumor necrosis factor-alpha and interleukin-6) was reduced by treatment with n-hexane extract of H. integrifolia and its bioactive compounds. Our results revealed that H. integrifolia extract and its bioactive compounds, friedelin and lupeol, exhibit wound-healing activity with anti-inflammatory properties, mediated by regulating the gene expression involved in skin re-epithelialization. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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18 pages, 3423 KiB  
Article
Angelica sinensis Polysaccharide and Astragalus membranaceus Polysaccharide Accelerate Liver Regeneration by Enhanced Glycolysis via Activation of JAK2/STAT3/HK2 Pathway
by Xu-Dong Wen, Yao-Lei Zhang, Ling Yang, Zhen Ye, Guo-Chuan Fu, Yong-He Hu, Tao Pan and Qiao-Bo Ye
Molecules 2022, 27(22), 7890; https://doi.org/10.3390/molecules27227890 - 15 Nov 2022
Cited by 8 | Viewed by 2037
Abstract
The promotion of liver regeneration is crucial to avoid liver failure after hepatectomy. Angelica sinensis polysaccharide (ASP) and Astragalus membranaceus polysaccharide (AMP) have been identified as being associated with hepatoprotective effects. However, their roles and specific mechanisms in liver regeneration remain to be [...] Read more.
The promotion of liver regeneration is crucial to avoid liver failure after hepatectomy. Angelica sinensis polysaccharide (ASP) and Astragalus membranaceus polysaccharide (AMP) have been identified as being associated with hepatoprotective effects. However, their roles and specific mechanisms in liver regeneration remain to be elucidated. In the present study, it suggested that the respective use of ASP or AMP strikingly promoted hepatocyte proliferation in vitro with a wide range of concentrations (from 12.5 μg/mL to 3200 μg/mL), and a stronger promoting effect was observed in combined interventions. A significantly enhanced liver/body weight ratio (4.20%) on day 7 and reduced serum transaminase (ALT 243.53 IU/L and AST 423.74 IU/L) and total bilirubin (52.61 IU/L) levels on day 3 were achieved by means of ASP-AMP administration after partial hepatectomy in mice. Metabonomics showed that differential metabolites were enriched in glycolysis with high expression of beta-d-fructose 6-phosphate and lactate, followed by significantly strengthened lactate secretion in the supernatant (0.54) and serum (0.43) normalized to control. Upon ASP-AMP treatment, the knockdown of hexokinase 2 (HK2) or inhibited glycolysis caused by 2-deoxy-d-glucose decreased hepatocyte proliferation in vitro and in vivo. Furthermore, pathway analysis predicted the role of JAK2/STAT3 pathway in ASP-AMP-regulated liver regeneration, and phosphorylation of JAK2 and STAT3 was proven to be elevated in this promoting process. Finally, downregulated expression of HK2, an attenuated level of lactate secretion, and reduced hepatocyte proliferation were displayed when STAT3 was knocked out in vitro. Therefore, it can be concluded that ASP-AMP accelerated liver regeneration and exerted a hepatoprotective effect after hepatectomy, in which the JAK2/STAT3/HK2 pathway was actively involved in activating glycolysis. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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26 pages, 5197 KiB  
Article
Walnut Prevents Cognitive Impairment by Regulating the Synaptic and Mitochondrial Dysfunction via JNK Signaling and Apoptosis Pathway in High-Fat Diet-Induced C57BL/6 Mice
by Jong Hyun Moon, Jong Min Kim, Uk Lee, Jin Yong Kang, Min Ji Kim, Hyo Lim Lee, Hye Rin Jeong, Min Ji Go, Hyun-Jin Kim, Hye Won Park, Chul-Woo Kim, Sung Jin Park and Ho Jin Heo
Molecules 2022, 27(16), 5316; https://doi.org/10.3390/molecules27165316 - 20 Aug 2022
Cited by 4 | Viewed by 2436
Abstract
This study was conducted to evaluate the protective effect of Juglans regia (walnut, Gimcheon 1ho cultivar, GC) on high-fat diet (HFD)-induced cognitive dysfunction in C57BL/6 mice. The main physiological compounds of GC were identified as pedunculagin/casuariin isomer, strictinin, tellimagrandin I, ellagic acid-O-pentoside, and [...] Read more.
This study was conducted to evaluate the protective effect of Juglans regia (walnut, Gimcheon 1ho cultivar, GC) on high-fat diet (HFD)-induced cognitive dysfunction in C57BL/6 mice. The main physiological compounds of GC were identified as pedunculagin/casuariin isomer, strictinin, tellimagrandin I, ellagic acid-O-pentoside, and ellagic acid were identified using UPLC Q-TOF/MS analysis. To evaluate the neuro-protective effect of GC, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), 2′,7′-dichlorodihydrofluorecein diacetate (DCF-DA) analysis were conducted in H2O2 and high glucose-induced neuronal PC12 cells and hippocampal HT22 cells. GC presented significant cell viability and inhibition of reactive oxygen species (ROS) production. GC ameliorated behavioral and memory dysfunction through Y-maze, passive avoidance, and Morris water maze tests. In addition, GC reduced white adipose tissue (WAT), liver fat mass, and serum dyslipidemia. To assess the inhibitory effect of antioxidant system deficit, lipid peroxidation, ferric reducing antioxidant power (FRAP), and advanced glycation end products (AGEs) were conducted. Administration of GC protected the antioxidant damage against HFD-induced diabetic oxidative stress. To estimate the ameliorating effect of GC, acetylcholine (ACh) level, acetylcholinesterase (AChE) activity, and expression of AChE and choline acetyltransferase (ChAT) were conducted, and the supplements of GC suppressed the cholinergic system impairment. Furthermore, GC restored mitochondrial dysfunction by regulating the mitochondrial ROS production and mitochondrial membrane potential (MMP) levels in cerebral tissues. Finally, GC ameliorated cerebral damage by synergically regulating the protein expression of the JNK signaling and apoptosis pathway. These findings suggest that GC could provide a potential functional food source to improve diabetic cognitive deficits and neuronal impairments. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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20 pages, 4314 KiB  
Article
Molineria recurvata Ameliorates Streptozotocin-Induced Diabetic Nephropathy through Antioxidant and Anti-Inflammatory Pathways
by Prasanta Dey, Amit Kundu, Ha Eun Lee, Babli Kar, Vineet Vishal, Suvakanta Dash, In Su Kim, Tejendra Bhakta and Hyung Sik Kim
Molecules 2022, 27(15), 4985; https://doi.org/10.3390/molecules27154985 - 05 Aug 2022
Cited by 6 | Viewed by 2850
Abstract
Molineria recurvata (MR) has been traditionally used to manage diabetes mellitus in India. However, the molecular mechanism of MR on the diabetic-induced nephropathy has not been clearly investigated. Thus, this study investigates the protective effects of the MR extract on nephropathy in streptozotocin [...] Read more.
Molineria recurvata (MR) has been traditionally used to manage diabetes mellitus in India. However, the molecular mechanism of MR on the diabetic-induced nephropathy has not been clearly investigated. Thus, this study investigates the protective effects of the MR extract on nephropathy in streptozotocin (STZ)-induced diabetic rats. Diabetes was instigated by a single intraperitoneal injection of STZ (45 mg/kg) in male Sprague-Dawley rats. Once the diabetes was successfully induced, the MR extract (200 mg/kg/day) or metformin (200 mg/kg/day) was orally administered for 14 days. Renal function, morphology changes and levels of inflammatory cytokines were measured. Blood glucose concentrations were considerably reduced in STZ-induced diabetic rats following treatment with the MR extract. The administration of the MR extract substantially restored the abnormal quantity of the oxidative DNA damage marker 8-hydroxy-2′-deoxy-guanosine (8-OHdG), malondialdehyde, glutathione, oxidized glutathione, superoxide dismutase, catalase, interleukin (IL)-1β, IL-6, IL-10, and transforming growth factor-β (TGF-β). The urinary excretion of kidney injury molecule-1 (KIM-1), neutrophil gelatinase-associated lipocalin (NGAL), selenium binding protein 1 (SBP1), and pyruvate kinase M2 (PKM2) was significantly reduced in diabetes rats after administration of the MR extracts. In the kidneys of STZ-induced diabetic rats, the MR extracts markedly downregulated the expression of fibronectin, collagen-1, and α-smooth muscle actin (α-SMA). In particular, the MR extracts markedly increased the level of SIRT1 and SIRT3 and reduced claudin-1 in the kidney. These results suggest that the MR extracts exhibits therapeutic activity in contrast to renal injury in STZ-induced diabetic rats through repressing inflammation and oxidative stress. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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13 pages, 5897 KiB  
Article
Phytochemical Discrimination, Biological Activity and Molecular Docking of Water-Soluble Inhibitors from Saussurea costus Herb against Main Protease of SARS-CoV-2
by Hajo Idriss, Babeker Siddig, Pamela González Maldonado, H. M. Elkhair, A. I. Alakhras, Emad M. Abdallah, Pablo Hernán Sotelo Torres and Amin O. Elzupir
Molecules 2022, 27(15), 4908; https://doi.org/10.3390/molecules27154908 - 01 Aug 2022
Cited by 9 | Viewed by 2393
Abstract
Siddha medicine is one of the oldest medical systems in the world and is believed to have originated more than 10,000 years ago and is prevalent across ancient Tamil land. It is undeniable that inhibitor preferences rise with increasing solubility in water due [...] Read more.
Siddha medicine is one of the oldest medical systems in the world and is believed to have originated more than 10,000 years ago and is prevalent across ancient Tamil land. It is undeniable that inhibitor preferences rise with increasing solubility in water due to the considerations pertaining to the bioavailability and the ease of which unabsorbed residues can be disposed of. In this study, we showed the phytochemical discrimination of Saussurea costus extracted with water at room temperature as a green extraction procedure. A total of 48 compounds were identified using gas chromatography-mass spectrometry (GC-MS). The fatty acids had a high phytochemical abundance at 73.8%, followed by tannins at 8.2%, carbohydrates at 6.9%, terpenoids at 4.3%, carboxylic acids at 2.5%, hydrocarbons at 2.4%, phenolic compounds at 0.2%, and sterols at 1.5%. Of these compounds, 22 were docked on the active side and on the catalytic dyad of His41 and Cys145 of the main protease of SARS-CoV-2 (Mpro). Eight active inhibitors were carbohydrates, five were fatty acids, three were terpenoids, two were carboxylic acids, one was a tannin, one was a phenolic compound, and one was a sterol. The best inhibitors were 4,8,13-Cyclotetradecatriene-1,3-diol, 1,5,9-trimethyl-12-(1-methylethyl), Andrographolide, and delta.4-Androstene-3.beta.,17.beta.-diol, with a binding affinity that ranged from −6.1 kcal/mol to −6.5 kcal/mol. The inhibitory effect of Saussurea costus of SARS-CoV-2 entry into the cell was studied using a pseudovirus with Spike proteins from the D614G variant and the VOC variants Gamma and Delta. Based on the viral cycle of SARS-CoV-2, our results suggest that the Saussurea costus aqueous extract has no virucidal effect and inhibits the virus in the events after cell entry. Furthermore, the biological activity of the aqueous extract was investigated against HSV-1 virus and two bacterial strains, namely Staphylococcus aureus ATCC BAA 1026 and Escherichia coli ATCC 9637. According to this study, an enormous number of water-soluble inhibitors were identified from Saussurea costus against the Mpro, and this is unprecedented as far as we know. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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15 pages, 3698 KiB  
Article
Steroidal Antimetabolites Protect Mice against Trypanosoma brucei
by Minu Chaudhuri, Ujjal K. Singha, Boden H. Vanderloop, Anuj Tripathi and W. David Nes
Molecules 2022, 27(13), 4088; https://doi.org/10.3390/molecules27134088 - 25 Jun 2022
Cited by 2 | Viewed by 1367
Abstract
Trypanosoma brucei, the causative agent for human African trypanosomiasis, is an emerging ergosterol-dependent parasite that produces chokepoint enzymes, sterol methyltransferases (SMT), not synthesized in their animal hosts that can regulate cell viability. Here, we report the lethal effects of two recently described [...] Read more.
Trypanosoma brucei, the causative agent for human African trypanosomiasis, is an emerging ergosterol-dependent parasite that produces chokepoint enzymes, sterol methyltransferases (SMT), not synthesized in their animal hosts that can regulate cell viability. Here, we report the lethal effects of two recently described natural product antimetabolites that disrupt Acanthamoeba sterol methylation and growth, cholesta-5,7,22,24-tetraenol (CHT) and ergosta-5,7,22,24(28)-tetraenol (ERGT) that can equally target T. brucei. We found that CHT/ERGT inhibited cell growth in vitro, yielding EC50 values in the low nanomolar range with washout experiments showing cidal activity against the bloodstream form, consistent with their predicted mode of suicide inhibition on SMT activity and ergosterol production. Antimetabolite treatment generated altered T. brucei cell morphology and death rapidly within hours. Notably, in vivo ERGT/CHT protected mice infected with T. brucei, doubling their survival time following daily treatment for 8–10 days at 50 mg/kg or 100 mg/kg. The current study demonstrates a new class of lead antibiotics, in the form of common fungal sterols, for antitrypanosomal drug development. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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13 pages, 2514 KiB  
Article
Anti-Obesity and Anti-Adipogenic Effects of Administration of Arginyl-Fructose-Enriched Jeju Barley (Hordeum vulgare L.) Extract in C57BL/6 Mice and in 3T3-L1 Preadipocytes Models
by Soo-Young Lee, Tae-Yang Kim, Ji-Yoon Hong, Gi-Jung Kim, Jung-Bae Oh, Min-Joo Kim, Emmanouil Apostolidis, Jung-Yun Lee and Young-In Kwon
Molecules 2022, 27(10), 3248; https://doi.org/10.3390/molecules27103248 - 19 May 2022
Cited by 6 | Viewed by 1965
Abstract
In our previous study, we reported that arginyl-fructose (AF), one of the Amadori rearrangement compounds (ARCs) produced by the heat processing of Korean ginseng can reduce carbohydrate absorption by inhibiting intestinal carbohydrate hydrolyzing enzymes in both in vitro and in vivo animal models. [...] Read more.
In our previous study, we reported that arginyl-fructose (AF), one of the Amadori rearrangement compounds (ARCs) produced by the heat processing of Korean ginseng can reduce carbohydrate absorption by inhibiting intestinal carbohydrate hydrolyzing enzymes in both in vitro and in vivo animal models. This reduced absorption of carbohydrate might be helpful to control body weight gain due to excessive carbohydrate consumption and support induced calorie restriction. However, the weight management effect, except for the effect due to anti-hyperglycemic action, along with the potential mechanism of action have not yet been determined. Therefore, the efforts of this study are to investigate and understand the possible weight management effect and mechanism action of AF-enriched barley extracts (BEE). More specifically, the effect of BEE on lipid accumulation and adipogenic gene expression, body weight gain, body weight, plasma lipids, body fat mass, and lipid deposition were evaluated using C57BL/6 mice and 3T3-L1 preadipocytes models. The formation of lipid droplets in the 3T3-L1 treated with BEE (500 and 750 µg/mL) was significantly blocked (p < 0.05 and p < 0.01, respectively). Male C57BL/6 mice were fed a high-fat diet (30% fat) for 8 weeks with BEE (0.3 g/kg-body weight). Compared to the high fat diet control (HFD) group, the cells treated with BEE significantly decreased in intracellular lipid accumulation with concomitant decreases in the expression of key transcription factors, peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer-binding protein alpha (CEBP/α), the mRNA expression of downstream lipogenic target genes such as fatty acid binding protein 4 (FABP4), fatty acid synthase (FAS), and sterol regulatory element-binding protein 1c (SREBP-1c). Supplementation of BEE effectively lowered the body weight gain, visceral fat accumulation, and plasma lipid concentrations. Compared to the HFD group, BEE significantly suppressed body weight gain (16.06 ± 2.44 g vs. 9.40 ± 1.39 g, p < 0.01) and increased serum adiponectin levels, significantly, 1.6-folder higher than the control group. These results indicate that AF-enriched barley extracts may prevent diet-induced weight gain and the anti-obesity effect is mediated in part by inhibiting adipogenesis and increasing adiponectin level. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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11 pages, 1605 KiB  
Article
Antiproliferative Properties of Triterpenoids by ECIS Method—A New Promising Approach in Anticancer Studies?
by Anna Hordyjewska, Monika Prendecka-Wróbel, Łukasz Kurach, Anna Horecka, Anna Olszewska, Dominika Pigoń-Zając, Teresa Małecka-Massalska and Jacek Kurzepa
Molecules 2022, 27(10), 3150; https://doi.org/10.3390/molecules27103150 - 14 May 2022
Cited by 4 | Viewed by 1878
Abstract
Electric cell–substrate impedance sensing is an advanced in vitro impedance measuring system which uses alternating current to determine behavior of cells in physiological conditions. In this study, we used the abovementioned method for checking the anticancer activities of betulin and betulinic acid, which [...] Read more.
Electric cell–substrate impedance sensing is an advanced in vitro impedance measuring system which uses alternating current to determine behavior of cells in physiological conditions. In this study, we used the abovementioned method for checking the anticancer activities of betulin and betulinic acid, which are some of the most commonly found triterpenes in nature. In our experiment, the threshold concentrations of betulin required to elicit antiproliferative effects, verified by MTT and LDH release methods, were 7.8 µM for breast cancer (T47D), 9.5 µM for lung carcinoma (A549), and 21.3 µM for normal epithelial cells (Vero). The ECIS results revealed the great potential of betulin and betulinic acid’s antitumor properties and their maintenance of cytotoxic substances to the breast cancer T47D line. Moreover, both substances showed a negligible toxic effect on healthy epithelial cells (Vero). Our investigation showed that the ECIS method is a proper alternative to the currently used assay for testing in vitro anticancer activity of compounds, and that it should thus be introduced in cellular routine research. It is also a valuable tool for live-monitoring changes in the morphology and physiology of cells, which translates into the accurate development of anticancer therapies. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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17 pages, 11028 KiB  
Article
Immunomodulatory Properties of Polysaccharide-Rich Young Green Barley (Hordeum vulgare) Extract and Its Structural Characterization
by Marta Kinga Lemieszek, Iwona Komaniecka, Michał Chojnacki, Adam Choma and Wojciech Rzeski
Molecules 2022, 27(5), 1742; https://doi.org/10.3390/molecules27051742 - 07 Mar 2022
Cited by 5 | Viewed by 2166
Abstract
Young green barley (YGB) water extract has revealed a beneficial impact on natural killer (NK) cells’ ability to recognize and eliminate human colon cancer cells, without any side effects for normal colon epithelial cells. The direct anticancer effect of the tested compounds has [...] Read more.
Young green barley (YGB) water extract has revealed a beneficial impact on natural killer (NK) cells’ ability to recognize and eliminate human colon cancer cells, without any side effects for normal colon epithelial cells. The direct anticancer effect of the tested compounds has been also shown. The mixture of oligosaccharides found in this extract was characterized by chemical analyses and via FT-IR spectroscopy and MALDI-TOF MS techniques. The YGB preparation contained 26.9% of proteins and 64.2% of sugars, mostly glucose (54.7%) and fructose (42.7%), with a small amount of mannose (2.6%) and galactose (less than 0.5%). Mass spectrometry analysis of YGB has shown that fructose oligomers contained from 3 to 19 sugar units. The number of fructans was estimated to be about 10.2% of the dry weight basis of YGB. The presented results suggest the beneficial effect of the consumption of preparations based on young barley on the human body, in the field of colon cancer prevention. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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Review

Jump to: Editorial, Research

37 pages, 2238 KiB  
Review
Terpenoids: Natural Compounds for Non-Alcoholic Fatty Liver Disease (NAFLD) Therapy
by Pengyu Yao and Yajuan Liu
Molecules 2023, 28(1), 272; https://doi.org/10.3390/molecules28010272 - 29 Dec 2022
Cited by 12 | Viewed by 3798
Abstract
Natural products have been the most productive source for the development of drugs. Terpenoids are a class of natural active products with a wide range of pharmacological activities and therapeutic effects, which can be used to treat a variety of diseases. Non-alcoholic fatty [...] Read more.
Natural products have been the most productive source for the development of drugs. Terpenoids are a class of natural active products with a wide range of pharmacological activities and therapeutic effects, which can be used to treat a variety of diseases. Non-alcoholic fatty liver disease (NAFLD), a common metabolic disorder worldwide, results in a health burden and economic problems. A literature search was conducted to obtain information relevant to the treatment of NAFLD with terpenoids using electronic databases, namely PubMed, Web of Science, Science Direct, and Springer, for the period 2011–2021. In total, we found 43 terpenoids used in the treatment of NAFLD. Over a dozen terpenoid compounds of natural origin were classified into five categories according to their structure: monoterpenoids, sesquiterpenoids, diterpenoids, triterpenoids, and tetraterpenoids. We found that terpenoids play a therapeutic role in NAFLD, mainly by regulating lipid metabolism disorder, insulin resistance, oxidative stress, and inflammation. The AMPK, PPARs, Nrf-2, and SIRT 1 pathways are the main targets for terpenoid treatment. Terpenoids are promising drugs and will potentially create more opportunities for the treatment of NAFLD. However, current studies are restricted to animal and cell experiments, with a lack of clinical research and systematic structure–activity relationship (SAR) studies. In the future, we should further enrich the research on the mechanism of terpenoids, and carry out SAR studies and clinical research, which will increase the likelihood of breakthrough insights in the field. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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19 pages, 2006 KiB  
Review
Mechanism of Citri Reticulatae Pericarpium as an Anticancer Agent from the Perspective of Flavonoids: A Review
by Li Song, Peiyu Xiong, Wei Zhang, Hengchang Hu, Songqi Tang, Bo Jia and Wei Huang
Molecules 2022, 27(17), 5622; https://doi.org/10.3390/molecules27175622 - 31 Aug 2022
Cited by 8 | Viewed by 4164
Abstract
Citri Reticulatae Pericarpium (CRP), also known as “chenpi”, is the most common qi-regulating drug in traditional Chinese medicine. It is often used to treat cough and indigestion, but in recent years, it has been found to have multi-faceted anti-cancer effects. This article reviews [...] Read more.
Citri Reticulatae Pericarpium (CRP), also known as “chenpi”, is the most common qi-regulating drug in traditional Chinese medicine. It is often used to treat cough and indigestion, but in recent years, it has been found to have multi-faceted anti-cancer effects. This article reviews the pharmacology of CRP and the mechanism of the action of flavonoids, the key components of CRP, against cancers including breast cancer, lung cancer, prostate cancer, hepatic carcinoma, gastric cancer, colorectal cancer, esophageal cancer, cervical cancer, bladder cancer and other cancers with a high diagnosis rate. Finally, the specific roles of CRP in important phenotypes such as cell proliferation, apoptosis, autophagy and migration–invasion in cancer were analyzed, and the possible prospects and deficiencies of CRP as an anticancer agent were evaluated. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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19 pages, 2753 KiB  
Review
Health-Promoting Properties of Medicinal Mushrooms and Their Bioactive Compounds for the COVID-19 Era—An Appraisal: Do the Pro-Health Claims Measure Up?
by Jennifer Mary Phillips, Soo Liang Ooi and Sok Cheon Pak
Molecules 2022, 27(7), 2302; https://doi.org/10.3390/molecules27072302 - 01 Apr 2022
Cited by 7 | Viewed by 6025
Abstract
Many mushroom species are consumed as food, while significant numbers are also utilised medicinally. Mushrooms are rich in nutrients and bioactive compounds. A growing body of in vitro, in vivo, and human research has revealed their therapeutic potentials, which include such properties as [...] Read more.
Many mushroom species are consumed as food, while significant numbers are also utilised medicinally. Mushrooms are rich in nutrients and bioactive compounds. A growing body of in vitro, in vivo, and human research has revealed their therapeutic potentials, which include such properties as anti-pathogenic, antioxidant, anti-inflammatory, immunomodulatory, gut microbiota enhancement, and angiotensin-converting enzyme 2 specificity. The uses of medicinal mushrooms (MMs) as extracts in nutraceuticals and other functional food and health products are burgeoning. COVID-19 presents an opportunity to consider how, and if, specific MM compounds might be utilised therapeutically to mitigate associated risk factors, reduce disease severity, and support recovery. As vaccines become a mainstay, MMs may have the potential as an adjunct therapy to enhance immunity. In the context of COVID-19, this review explores current research about MMs to identify the key properties claimed to confer health benefits. Considered also are barriers or limitations that may impact general recommendations on MMs as therapy. It is contended that the extraction method used to isolate bioactive compounds must be a primary consideration for efficacious targeting of physiological endpoints. Mushrooms commonly available for culinary use and obtainable as a dietary supplement for medicinal purposes are included in this review. Specific properties related to these mushrooms have been considered due to their potential protective and mediating effects on human exposure to the SARS CoV-2 virus and the ensuing COVID-19 disease processes. Full article
(This article belongs to the Special Issue A Feasible Approach for Natural Products to Treatment of Diseases)
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