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Role of Bioactive Phytochemicals in Metabolic Diseases

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (20 January 2023) | Viewed by 9204

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Special Issue Editors

Dr. Malgorzata Zakłos-Szyda

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Guest Editor

Institute of Molecular and Industrial Biotechnology, Faculty of Biotechnology and Food Sciences, Lodz University of Technology, Stefanowskiego 2/22, 90-537 Lodz, Poland
Interests: phytocompounds; phenolic compounds; animal cell culture; cell signaling; nuclear receptors; apoptosis; cytoprotection; lipid and carbohydrates metabolism
Special Issues, Collections and Topics in MDPI journals

Dr. Edyta Gendaszewska-Darmach

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Guest Editor

Institute of Molecular and Industrial Biotechnology, Faculty of Biotechnology and Food Sciences, Lodz University of Technology, Stefanowskiego 2/22, 90-537 Lodz, Poland
Interests: antidiabetic activity in the group of GPCR ligands; inhibitors of small GTPases prenylation; molecular mechanism of action of phytochemicals (fatty acids and their derivatives)

Special Issue Information

Dear Colleagues,

The constant increase in the incidence of metabolic diseases, including cardiovascular disease, obesity and type 2 diabetes, prompts scientists to search for new therapeutics that have the ability to improve the metabolism of lipids and carbohydrates. What is more, epidemiologic evidence suggests that people with diabetes are at a significantly greater risk of many forms of cancer. In spite of the great progress in the field of medicinal chemistry that has allowed for the synthesis of a huge amount of novel potential drug molecules, the variety of complications resulting from their prolonged usage encouraged the search for less harmful plant-derived substitutes. There is growing evidence that bioactive phytocompounds present in our diet, mainly secondary metabolites, can prevent multiple pathologies with different mechanisms, i.e., by the reduction in oxidative stress, modulation of cell signaling responses, regulation of certain genes expression, or even direct interaction with some proteins. Therefore, plant-derived natural products are significant as ingredients of functional foods or sources of medicinal agents and as models for the design of new remedies. While phenolic compounds deserve a special attention, more so than other bioactive phytocomponents, the regulatory effects of other plant metabolites, i.e., lipids, are still partially known. Thus, the aim of this Special Issue is to highlight recent achievements in the field of dietary bioactive phytochemicals, their specific mechanisms of action, and their use in the prevention of chronic diseases.

Dr. Malgorzata Zakłos-Szyda
Dr. Edyta Gendaszewska-Darmach
Guest Editors

Manuscript Submission Information

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Keywords

bioactive phytochemicals
phenolic compounds
bioactive lipids
biological activity
mechanism of action
chronic diseases
functional foods ingredients.

Published Papers (4 papers)

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Research

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14 pages, 2122 KiB

Open AccessArticle

Identification of Genipin as a Potential Treatment for Type 2 Diabetes

by Yajun Wu, Yao Wang and Dongmin Liu

Int. J. Mol. Sci. 2023, 24(3), 2131; https://doi.org/10.3390/ijms24032131 - 21 Jan 2023

Viewed by 1779

Abstract

The prevalence of type 2 diabetes (T2D) has been rising dramatically in many countries around the world. The main signatures of T2D are insulin resistance and dysfunction of β-cells. While there are several pharmaceutical therapies for T2D, no effective treatment is available for reversing the functional decline of pancreatic β-cells in T2D patients. It has been well recognized that glucagon-like peptide-1 (GLP-1), which is an incretin hormone secreted from intestinal L-cells, plays a vital role in regulating glycemic homeostasis via potentiating glucose-stimulated insulin secretion and promoting β-cell function. We found that genipin, a natural compound from Elli, can directly target intestinal L-cells, leading to the secretion of GLP-1. Incubation of the cells with genipin elicited a rapid increase in intracellular Ca²⁺. Inhibition of PLC ablated genipin-stimulated Ca²⁺ increase and GLP-1 secretion, suggesting that genipin-induced GLP-1 release from cells is dependent on the PLC/Ca²⁺ pathway. In vivo, acute administration of genipin stimulated GLP-1 secretion in mice. Chronically, treatment with genipin via oral gavage at 50 mg/kg/day for 6 weeks reversed hyperglycemia and insulin resistance in high-fat-diet (HFD)-induced obese mice. Moreover, genipin alleviated the impaired lipid metabolism and decreased lipid accumulation in the liver of obese mice. These results suggest that naturally occurring genipin might potentially be a novel agent for the treatment of T2D and diet-induced fatty liver disease. Full article

(This article belongs to the Special Issue Role of Bioactive Phytochemicals in Metabolic Diseases)

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17 pages, 3050 KiB

Open AccessArticle

Cirsium Setidens Water Extracts Containing Linarin Block Estrogen Deprivation-Induced Bone Loss in Mice

by Moon-Sik Oh, Soo-Il Kim, Young Eun Sim, Sin-Hye Park, Min-Kyung Kang, Il-Jun Kang, Soon Sung Lim and Young-Hee Kang

Int. J. Mol. Sci. 2023, 24(2), 1620; https://doi.org/10.3390/ijms24021620 - 13 Jan 2023

Cited by 1 | Viewed by 1682

Abstract

Osteoporosis is evident in postmenopausal women and is an osteolytic disease characterized by bone loss that further increases the susceptibility to bone fractures and frailty. The use of complementary therapies to alleviate postmenopausal osteoporosis is fairly widespread among women. Edible Cirsium setidens contains various polyphenols of linarin, pectolinarin, and apigenin with antioxidant and hepatoprotective effects. This study aimed to determine whether Cirsium setidens water extracts (CSEs), the component linarin, and its aglycone acacetin blocked ovariectomy (OVX)-induced bone loss. This study employed OVX C57BL/6 female mice as a model for postmenopausal osteoporosis. CSEs, acacetin, or linarin was orally administrated to OVX mice at a dose of 20 mg/kg for 8 weeks. Surgical estrogen loss in mice for 8 weeks reduced bone mineral density (BMD) of mouse femur and serum 17β-estradiol level and enhanced the serum receptor activator of NF-κB ligand/osteoprotegerin ratio with uterine atrophy. CSEs and linarin reversed such adverse effects and enhanced femoral BMD in OVX mice. Oral administration of CSEs and linarin attenuated tartrate-resistant acid phosphate activity and the induction of αvβ3 integrins and proton suppliers in resorption lacunae in femoral bone tissue of OVX mice. In addition, CSEs and linarin curtailed the bone levels of cathepsin K and matrix metalloproteinase-9 responsible for osteoclastic bone resorption. On the other hand, CSEs and linarin enhanced the formation of trabecular bones in estrogen-deficient femur with increased induction of osteocalcin and osteopontin. Further, treatment with CSEs and linarin enhanced the collagen formation-responsive propeptide levels in the circulation along with the increase in the tissue non-specific alkaline phosphatase level in bone exposed to OVX. Supplementing CSEs, acacetin, or linarin to OVX mice elevated the formation of collagen fibers in OVX trabecular bone, evidenced using Picrosirius red staining. Accordingly, CSEs and linarin were effective in retarding osteoclastic bone resorption and promoting osteoblastic bone matrix mineralization under OVX conditions. Therefore, linarin, which is abundant in CSEs, may be a natural compound for targeting postmenopausal osteoporosis and pathological osteoresorptive disorders. Full article

(This article belongs to the Special Issue Role of Bioactive Phytochemicals in Metabolic Diseases)

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20 pages, 8172 KiB

Open AccessArticle

Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases

by Natalia Rosiak, Kamil Wdowiak, Ewa Tykarska and Judyta Cielecka-Piontek

Int. J. Mol. Sci. 2022, 23(23), 15198; https://doi.org/10.3390/ijms232315198 - 2 Dec 2022

Cited by 11 | Viewed by 2248

Abstract

The present study reports amorphous solid dispersions (ASDs) of hesperidin (Hes) prepared by ball milling to improve its solubility and apparent solubility over the unmodified compound. The carriers were Soluplus^® (Sol), alginate sodium (SA), and hydroxypropylmethylcellulose (HPMC). XRPD analysis confirmed full amorphization of all binary systems in 1:5 w/w ratio. One glass transition (T_g) observed in DSC thermograms of hesperidin:Soluplus^® (Hes:Sol) and hesperidin:HPMC (Hes:HPMC) 1:5 w/w systems confirmed complete miscibility. The mathematical model (Gordon–Taylor equation) indicates that the obtained amorphous systems are characterized by weak interactions. The FT-IR results confirmed that hydrogen bonds are responsible for stabilizing the amorphous state of Hes. Stability studies indicate that the strength of these bonds is insufficient to maintain the amorphous state of Hes under stress conditions (25 °C and 60 °C 76.4% RH). HPLC analysis suggested that the absence of degradation products indicates safe hesperidin delivery systems. The solubility and apparent solubility were increased in all media (water, phosphate buffer pH 6.8 and HCl (0.1 N)) compared to the pure compound. Our study showed that all obtained ASDs are promising systems for Hes delivery, wherein Hes:Sol 1:5 w/w has the best solubility (about 300-fold in each media) and apparent solubility (about 70% in phosphate buffer pH 6.8 and 63% in HCl). Full article

(This article belongs to the Special Issue Role of Bioactive Phytochemicals in Metabolic Diseases)

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Review

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19 pages, 1427 KiB

Open AccessReview

Glycyrrhizic Acid and Its Derivatives: Promising Candidates for the Management of Type 2 Diabetes Mellitus and Its Complications

by Dechao Tan, Hisa Hui Ling Tseng, Zhangfeng Zhong, Shengpeng Wang, Chi Teng Vong and Yitao Wang

Int. J. Mol. Sci. 2022, 23(19), 10988; https://doi.org/10.3390/ijms231910988 - 20 Sep 2022

Cited by 16 | Viewed by 2910

Abstract

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease, which is characterized by hyperglycemia, chronic insulin resistance, progressive decline in β-cell function, and defect in insulin secretion. It has become one of the leading causes of death worldwide. At present, there is no cure for T2DM, but it can be treated, and blood glucose levels can be controlled. It has been reported that diabetic patients may suffer from the adverse effects of conventional medicine. Therefore, alternative therapy, such as traditional Chinese medicine (TCM), can be used to manage and treat diabetes. In this review, glycyrrhizic acid (GL) and its derivatives are suggested to be promising candidates for the treatment of T2DM and its complications. It is the principal bioactive constituent in licorice, one type of TCM. This review comprehensively summarized the therapeutic effects and related mechanisms of GL and its derivatives in managing blood glucose levels and treating T2DM and its complications. In addition, it also discusses existing clinical trials and highlights the research gap in clinical research. In summary, this review can provide a further understanding of GL and its derivatives in T2DM as well as its complications and recent progress in the development of potential drugs targeting T2DM. Full article

(This article belongs to the Special Issue Role of Bioactive Phytochemicals in Metabolic Diseases)

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