Current knowledge and development of hederagenin as a promising medicinal agent: a comprehensive review

Jia, Zeng; Huang, Ting; Xue, Man; Chen, Jianxing; Feng, Liang; Du, Ruofei; Feng, Yi

doi:10.1039/c8ra03666g

Cited by 49 publications

(19 citation statements)

References 59 publications

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“…, is an oxidized derivative of oleanolic acid ( 115 ). This compound has been attracting a great deal of attention, due to its wide range of biological activities, including multidrug resistance reversal properties [ 140 , 141 ]. Main chemical modifications explored so far on hederagenin ( 120 ) scaffold are mostly focused at the C-3 and C-23 hydroxyl groups, the carboxylic acid group at C-28 and at the double bound between C-12 and C-13.…”

Section: Terpenesmentioning

confidence: 99%

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

2020

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Multidrug resistance (MDR) in cancer is one of the main limitations for chemotherapy success. Numerous mechanisms are behind the MDR phenomenon wherein the overexpression of the ATP-binding cassette (ABC) transporter proteins P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance protein 1 (MRP1) is highlighted as a prime factor. Natural product-derived compounds are being addressed as promising ABC transporter modulators to tackle MDR. Flavonoids and terpenoids have been extensively explored in this field as mono or dual modulators of these efflux pumps. Nitrogen-bearing moieties on these scaffolds were proved to influence the modulation of ABC transporters efflux function. This review highlights the potential of semisynthetic nitrogen-containing flavonoid and terpenoid derivatives as candidates for the design of effective MDR reversers. A brief introduction concerning the major role of efflux pumps in multidrug resistance, the potential of natural product-derived compounds in MDR reversal, namely natural flavonoid and terpenoids, and the effect of the introduction of nitrogen-containing groups are provided. The main modifications that have been performed during last few years to generate flavonoid and terpenoid derivatives, bearing nitrogen moieties, such as aliphatic, aromatic and heterocycle amine, amide, and related functional groups, as well as their P-gp, MRP1 and BCRP inhibitory activities are reviewed and discussed.

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Section: Terpenesmentioning

confidence: 99%

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

2020

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“…It also has the potential for neuro-protection and improves motor degeneration. [24] The initial PPI network has 220 targets, occupying twothirds of the AM-related targets. SRC, MAPK1, JUN, TP53, and HSP90AA1 are the top 5 targets based on the degree value.…”

Section: Discussionmentioning

confidence: 99%

Exploring the mechanism of astragalus membranaceus in the treatment of multiple system atrophy based on network pharmacology and molecular docking

Yang

et al. 2023

Medicine

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Multiple system atrophy (MSA) is a fatal neurodegenerative disease, it causes functional degradation of multiple organs and systems throughout the body. Astragalus membranaceus (AM), a well-known traditional Chinese medicine, has been used to improve muscle wasting-related disorders for a long history. In this study, we used network pharmacology and molecular docking to predict the mechanism underlying AM for the treatment of MSA. We screened the active compounds of AM and its related targets, as well as the target proteins of MSA. We made a Venn diagram to obtain the intersecting targets and then constructed a protein-protein interaction network to find the core targets and build an active ingredient-target network map. After subjecting the intersecting targets to gene ontology and Kyoto encyclopedia of genes and genomes analysis, the binding ability of core compounds and core target proteins were validated by molecular docking. A total of 20 eligible compounds and 274 intersecting targets were obtained. The core components of treatment are quercetin, kaempferol, and isorhamnetin, and the core targets are TP53, RELA, and TNF. The main biological processes are related to cellular responses and regulation. Molecular functions are mainly associated with apoptosis, inflammation, and tumorigenesis. Molecular docking results show good and standard binding abilities. This study illustrates that AM treats MSA through multiple targets and pathways, and provides a reference for subsequent research.

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“…It has also been shown to have hypoglycemic effects, mediated via the regulation of hepatic glycogen metabolism, in diabetic mice [ 36 , 37 , 38 ]. Hederagenin (4), a pentacyclic triterpenoid, is present in several plants and possesses various pharmacological properties, including anti-inflammatory, anti-viral, and anti-hyperlipidemic activities [ 39 ]. Furthermore, hederagenin (4) possesses anti-diabetic activity mediated via the inhibition of the glycogen phosphorylase enzyme [ 40 ].…”

Section: Discussionmentioning

confidence: 99%

Bioactive Phytochemicals Isolated from Akebia quinata Enhances Glucose-Stimulated Insulin Secretion by Inducing PDX-1

Lee

Sezirahiga

et al. 2020

Plants

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Chocolate vine (Akebia quinata) is consumed as a fruit and is also used in traditional medicine. In order to identify the bioactive components of A. quinata, a phytosterol glucoside stigmasterol-3-O-β-d-glucoside (1), three triterpenoids maslinic acid (2), scutellaric acid (3), and hederagenin (4), and three triterpenoidal saponins akebia saponin PA (5), hederacoside C (6), and hederacolchiside F (7) were isolated from a 70% EtOH extract of the fruits of A. quinata (AKQU). The chemical structures of isolates 1–7 were determined by analyzing the 1D and 2D nuclear magnetic resonance (NMR) spectroscopic data. Here, we evaluated the effects of AKQU and compounds 1–7 on insulin secretion using the INS-1 rat pancreatic β-cell line. Glucose-stimulated insulin secretion (GSIS) was evaluated in INS-1 cells using the GSIS assay. The expression levels of the proteins related to pancreatic β-cell function were detected by Western blotting. Among the isolates, stigmasterol-3-O-β-d-glucoside (1) exhibited strong GSIS activity and triggered the overexpression of pancreas/duodenum homeobox protein-1 (PDX-1), which is implicated in the regulation of pancreatic β-cell survival and function. Moreover, isolate 1 markedly induced the expression of extracellular signal-regulated protein kinases 1 and 2 (ERK1/2), insulin receptor substrate-2 (IRS-2), phosphoinositide 3-kinase (PI3K), and Akt, which regulate the transcription of PDX-1. The results of our experimental studies indicated that stigmasterol-3-O-β-d-glucoside (1) isolated from the fruits of A. quinata can potentially enhance insulin secretion, and might alleviate the reduction in GSIS during the development of T2DM.

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Current knowledge and development of hederagenin as a promising medicinal agent: a comprehensive review

Abstract: Hederagenin (HG) is a pentacyclic triterpenoid that exists in many plants in the form(s) of sapogenin or saponins.

Cited by 49 publications

References 59 publications

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

Exploring the mechanism of astragalus membranaceus in the treatment of multiple system atrophy based on network pharmacology and molecular docking

Bioactive Phytochemicals Isolated from Akebia quinata Enhances Glucose-Stimulated Insulin Secretion by Inducing PDX-1

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