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Keywords = geniposide (GP)

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19 pages, 4441 KiB  
Article
In Silico and In Vivo Pharmacological Evaluation of Iridoid Compounds: Geniposide and Asperuloside Profile Study Through Molecular Docking Assay and in the Caenorhabditis elegans Model
by Mariana Uczay, Péterson Alves Santos, Pricila Pflüger, Gilsane von Poser, José Brea, Maria Isabel Loza, Patrícia Pereira and José Angel Fontenla
Biomolecules 2025, 15(8), 1105; https://doi.org/10.3390/biom15081105 - 31 Jul 2025
Viewed by 259
Abstract
Iridoids are compounds recognized for their neuroprotective properties and their potential application in the treatment of neurodegenerative diseases. Geniposide (GP) and asperuloside (ASP) are iridoids that have demonstrated some biological activities. In this study, the potential neuroprotective effects of these iridoids were evaluated [...] Read more.
Iridoids are compounds recognized for their neuroprotective properties and their potential application in the treatment of neurodegenerative diseases. Geniposide (GP) and asperuloside (ASP) are iridoids that have demonstrated some biological activities. In this study, the potential neuroprotective effects of these iridoids were evaluated through in silico and in vivo assays, using Caenorhabditis elegans (C. elegans) strains CF1553 (sod-3::GFP), GA800 (cat::GFP), and CL2166 (gst-4::GFP). The results suggested that neither compound appears to have good passive permeability through the blood–brain barrier (BBB). However, an active transport mechanism involving the glucose transporter GLUT-1 may be present, as both compounds contain glucose in their molecular structure. In addition, they can inhibit the activity of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). GP at 1 and 2 mM reversed the H2O2-induced increase in sod-3 expression, while ASP at 1 and 2 mM reversed the increase in gst-4 expression. Worm survival was more adversely affected by higher concentrations of GP than ASP, although both similarly reduced acetylcholinesterase activity. These findings suggest that GP and ASP exhibit very low toxicity both in silico and in vivo in C. elegans, and positively modulate key enzymes involved in antioxidant pathways, highlighting their potential for neuroprotective applications. Full article
(This article belongs to the Section Natural and Bio-derived Molecules)
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15 pages, 3339 KiB  
Article
Combination of a Deep Eutectic Solvent and Macroporous Resin for Green Recovery of Iridoids, Chlorogenic Acid, and Flavonoids from Eucommia ulmoides Leaves
by Yunhui Liao, Feng Chen, Haishan Tang, Wubliker Dessie and Zuodong Qin
Molecules 2024, 29(3), 737; https://doi.org/10.3390/molecules29030737 - 5 Feb 2024
Cited by 6 | Viewed by 2156
Abstract
To increase the effectiveness of using typical biomass waste as a resource, iridoids, chlorogenic acid, and flavonoids from the waste biomass of Eucommia ulmoides leaves (EULs) were extracted by deep eutectic solvents (DESs) in conjunction with macroporous resin. To optimize the extract conditions, [...] Read more.
To increase the effectiveness of using typical biomass waste as a resource, iridoids, chlorogenic acid, and flavonoids from the waste biomass of Eucommia ulmoides leaves (EULs) were extracted by deep eutectic solvents (DESs) in conjunction with macroporous resin. To optimize the extract conditions, the experiment of response surface was employed with the single-factor of DES composition molar ratio, liquid–solid ratio, water percentage, extraction temperature, and extraction time. The findings demonstrated that the theoretical simulated extraction yield of chlorogenic acid (CGA), geniposidic acid (GPA), aucubin (AU), geniposide (GP), rutin (RU), and isoquercetin (IQU) were 42.8, 137.2, 156.7, 5.4, 13.5, and 12.8 mg/g, respectively, under optimal conditions (hydrogen bond donor–hydrogen bond acceptor molar ratio of 1.96, liquid–solid ratio of 28.89 mL/g, water percentage of 38.44%, temperature of 317.36 K, and time of 55.59 min). Then, 12 resins were evaluated for their adsorption and desorption capabilities for the target components, and the HPD950 resin was found to operate at its optimum. Additionally, the HPD950 resin demonstrated significant sustainability and considerable potential in the recyclability test. Finally, the hypoglycemic in vitro, hypolipidemic in vitro, immunomodulatory, and anti-inflammatory effects of EUL extract were evaluated, and the correlation analysis of six active components with biological activity and physicochemical characteristics of DESs by heatmap were discussed. The findings of this study can offer a theoretical foundation for the extraction of valuable components by DESs from waste biomass, as well as specific utility benefits for the creation and development of natural products. Full article
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18 pages, 1616 KiB  
Review
Natural Products Targeting PI3K/AKT in Myocardial Ischemic Reperfusion Injury: A Scoping Review
by Syarifah Aisyah Syed Abd Halim, Norhashima Abd Rashid, Choy Ker Woon and Nahdia Afiifah Abdul Jalil
Pharmaceuticals 2023, 16(5), 739; https://doi.org/10.3390/ph16050739 - 12 May 2023
Cited by 13 | Viewed by 3251
Abstract
This scoping review aimed to summarize the effects of natural products targeting phosphoinositide-3-kinases/serine/threonine kinase (PI3K/AKT) in myocardial ischemia-reperfusion injury (MIRI). The review details various types of natural compounds such as gypenoside (GP), gypenoside XVII (GP-17), geniposide, berberine, dihydroquercetin (DHQ), and tilianin which identified [...] Read more.
This scoping review aimed to summarize the effects of natural products targeting phosphoinositide-3-kinases/serine/threonine kinase (PI3K/AKT) in myocardial ischemia-reperfusion injury (MIRI). The review details various types of natural compounds such as gypenoside (GP), gypenoside XVII (GP-17), geniposide, berberine, dihydroquercetin (DHQ), and tilianin which identified to reduce MIRI in vitro and in vivo by regulating the PI3K/AKT signaling pathway. In this study, 14 research publications that met the inclusion criteria and exclusion criteria were shortlisted. Following the intervention, we discovered that natural products effectively improved cardiac functions through regulation of antioxidant status, down-regulation of Bax, and up-regulation of Bcl-2 and caspases cleavage. Furthermore, although comparing outcomes can be challenging due to the heterogeneity in the study model, the results we assembled here were consistent, giving us confidence in the intervention’s efficacy. We also discussed if MIRI is associated with multiple pathological condition such as oxidative stress, ERS, mitochondrial injury, inflammation, and apoptosis. This brief review provides evidence to support the huge potential of natural products used in the treatment of MIRI due to their various biological activities and drug-like properties. Full article
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13 pages, 4853 KiB  
Article
Effects of Geniposide and Geniposidic Acid on Fluoxetine-Induced Muscle Atrophy in C2C12 Cells
by Shang-Ming Huang, Shuan-Ying Lin, Ming-Kai Chen, Chiung-Chi Peng and Chiu-Lan Hsieh
Processes 2021, 9(9), 1649; https://doi.org/10.3390/pr9091649 - 13 Sep 2021
Cited by 3 | Viewed by 3386
Abstract
Fluoxetine, an antidepressant known as a selective 5-hydroxytryptamine reuptake inhibitor (SSRI), can cause side effects such as muscle atrophy with long-term use, but the mechanism is not fully understood. Geniposide (GPS) and geniposidic acid (GPSA), the main components of Gardenia jasminoides fruit, have [...] Read more.
Fluoxetine, an antidepressant known as a selective 5-hydroxytryptamine reuptake inhibitor (SSRI), can cause side effects such as muscle atrophy with long-term use, but the mechanism is not fully understood. Geniposide (GPS) and geniposidic acid (GPSA), the main components of Gardenia jasminoides fruit, have been shown to have biological activity in disease prevention, but their role in preventing FXT-related side effects such as muscle atrophy remains unclear. The process of muscle atrophy is a complex physiological mechanism involving the balance of protein synthesis and catabolism. In this study, we hypothesized that FXT may suppress hypertrophy signaling and activate the atrophy mechanisms, resulting in proteolysis and reduced protein synthesis, while geniposide (GPS) and geniposide acid (GPSA) may be beneficial in improving muscle weakness caused by FXT. The C2C12 cell model was used to examine the expression of hypertrophy signaling (PI3K, Akt, and mTOR) and protein break signals (FOXO, MuRF-1, and MyHC). Our data indicated that FXT inhibited MyHC and promoted MuRF-1 protein expression by downregulating the signaling pathways of p-ERK1/2, p-Akt, p-mTOR, and p-FOXO, resulting in a decrease in differentiation and myotube formation in C2C12 muscle cells, which further resulted in muscle atrophy. However, GPS and GPSA can positively regulate the atrophy mechanism induced by FXT in muscle cells, thereby ameliorating the imbalance in muscle synthesis. In conclusion, GPS and GPSA have the potential to attenuate the muscle loss caused by long-term FXT administration, diseases, or the aging process. Full article
(This article belongs to the Special Issue Food Safety Management and Quality Control Techniques)
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11 pages, 317 KiB  
Article
Effects of Fructus Psoraleae Extract on the Intestinal Absorption Kinetics of Geniposide and Geniposidic Acid in Rat
by Yan Huo, Yuxing Huang, Xiangmei Hou, Lifeng Han, Lei Wang, Erwei Liu and Xiumei Gao
Molecules 2014, 19(6), 7557-7567; https://doi.org/10.3390/molecules19067557 - 6 Jun 2014
Cited by 6 | Viewed by 6135
Abstract
Cortex Eucommia has been used as a kidney-tonifying herbal medicine with a long history of compatibility with Fructus Psoraleae. Geniposide (GP) and geniposidic acid (GPA) are the two main chemical components in Cortex Eucommia. In the present study, the effects of [...] Read more.
Cortex Eucommia has been used as a kidney-tonifying herbal medicine with a long history of compatibility with Fructus Psoraleae. Geniposide (GP) and geniposidic acid (GPA) are the two main chemical components in Cortex Eucommia. In the present study, the effects of Fructus Psoraleae extract (FPE) on intestinal absorption kinetics of GP and GPA in rat were investigated. Twenty four male Sprague-Dawley rats were randomly assigned into four groups which were treated with GP, GPA, GP mixed with FPE and GPA mixed with FPE, respectively, by in situ intestinal perfusion for 3 h. The samples of intestinal perfusion solutions were collected every 30 min, and analyzed by ultra high performance liquid chromatography (UPLC). The curves of time and residual quantities of GP and GPA (lnx) in the intestinal perfusion solution and the cumulative absorption rate were obtained. The results showed that FPE exhibited different effects on the intestinal absorption of GP and GPA in rat: it increased the intestinal absorption of GP (p < 0.05), while demonstrated no significant effect on the absorption of GPA. Full article
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