Evidence mapPaperPMID 37628991Full record

ArticleInternational journal of molecular sciences2023

Anti-Diabetic Activity of Glycyrrhetinic Acid Derivatives FC-114 and FC-122: Scale-Up, In Silico, In Vitro, and In Vivo Studies.

Samuel Álvarez-Almazán, Luz Cassandra Solís-Domínguez, Paulina Duperou-Luna, Teresa Fuerte-Gómez, Martin González-Andrade, María E Aranda-Barradas, Juan Francisco Palacios-Espinosa, Jaime Pérez-Villanueva, Félix Matadamas-Martínez, Susana Patricia Miranda-Castro and 2 more

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
3.4field-weighted citation impact, top 7% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

10 citing papers in PubMed, 14 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Review
  7. Article
  8. Special Issue "Advances in Drug Discovery and Synthesis".International journal of molecular sciences · 2025
    Article
  9. Article
  10. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors at 3 institutions in 1 country.

Samuel Álvarez-AlmazánLaboratory of Biotechnology, Unidad de Posgrado, Facultad de Estudios Superiores Cuautitlán Campus 1, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54740, Mexico.ORCID 0000-0001-7346-8251
Luz Cassandra Solís-DomínguezLaboratory of Biotechnology, Unidad de Posgrado, Facultad de Estudios Superiores Cuautitlán Campus 1, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54740, Mexico.
Paulina Duperou-LunaLaboratory of Synthesis and Isolation of Bioactive Substances, Departamento de Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco (UAM-X), Mexico City 04960, Mexico.
Teresa Fuerte-GómezLaboratory of Biotechnology, Unidad de Posgrado, Facultad de Estudios Superiores Cuautitlán Campus 1, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54740, Mexico.
Martin González-AndradeLaboratory of Biosensors and Molecular Modelling, Departamento de Bioquímica, Facultad de Medicina, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico.ORCID 0000-0002-8910-3035
María E Aranda-BarradasLaboratory of Biotechnology, Unidad de Posgrado, Facultad de Estudios Superiores Cuautitlán Campus 1, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54740, Mexico.ORCID 0000-0001-5182-5684
Juan Francisco Palacios-EspinosaLaboratory of Synthesis and Isolation of Bioactive Substances, Departamento de Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco (UAM-X), Mexico City 04960, Mexico.ORCID 0000-0001-9650-004X
Jaime Pérez-VillanuevaLaboratory of Synthesis and Isolation of Bioactive Substances, Departamento de Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco (UAM-X), Mexico City 04960, Mexico.ORCID 0000-0001-5777-2536
Félix Matadamas-MartínezLaboratory of Synthesis and Isolation of Bioactive Substances, Departamento de Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco (UAM-X), Mexico City 04960, Mexico.
Susana Patricia Miranda-CastroLaboratory of Biotechnology, Unidad de Posgrado, Facultad de Estudios Superiores Cuautitlán Campus 1, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54740, Mexico.ORCID 0000-0002-2178-1112
Crisóforo Mercado-MárquezIsolation and Animal Facility Unit, Facultad de Estudios Superiores Cuautitlán 28, Universidad Nacional Autónoma de México, Cuautitlán Izcalli 54714, Mexico.
Francisco Cortés-BenítezLaboratory of Synthesis and Isolation of Bioactive Substances, Departamento de Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco (UAM-X), Mexico City 04960, Mexico.ORCID 0000-0002-3954-8220
Universidad de Cuautitlán Izcalli · MXUniversidad Autónoma Metropolitana · MXUniversidad Nacional Autónoma de México · MX

Funding

Consejo Nacional de Ciencia y Tecnología CF-2023-I-186
6 · The paper itself

Abstract

Type 2 diabetes (T2D) is one of the most common diseases and the 8th leading cause of death worldwide. Individuals with T2D are at risk for several health complications that reduce their life expectancy and quality of life. Although several drugs for treating T2D are currently available, many of them have reported side effects ranging from mild to severe. In this work, we present the synthesis in a gram-scale as well as the in silico and in vitro activity of two semisynthetic glycyrrhetinic acid (GA) derivatives (namely FC-114 and FC-122) against Protein Tyrosine Phosphatase 1B (PTP1B) and α-glucosidase enzymes. Furthermore, the in vitro cytotoxicity assay on Human Foreskin fibroblast and the in vivo acute oral toxicity was also conducted. The anti-diabetic activity was determined in streptozotocin-induced diabetic rats after oral administration with FC-114 or FC-122. Results showed that both GA derivatives have potent PTP1B inhibitory activity being FC-122, a dual PTP1B/α-glucosidase inhibitor that could increase insulin sensitivity and reduce intestinal glucose absorption. Molecular docking, molecular dynamics, and enzymatic kinetics studies revealed the inhibition mechanism of FC-122 against α-glucosidase. Both GA derivatives were safe and showed better anti-diabetic activity in vivo than the reference drug acarbose. Moreover, FC-114 improves insulin levels while decreasing LDL and total cholesterol levels without decreasing HDL cholesterol.

Indexed as

Diabetes Mellitus, ExperimentalDiabetes Mellitus, Type 2Glycyrrhetinic Acidalpha-GlucosidasesAnimalsHumansMolecular Docking SimulationQuality of LifeRatsalpha-GlucosidasesGlycyrrhetinic Acidacute oral toxicityglycyrrhetinic acidmolecular dockingmolecular dynamicsprotein tyrosine phosphatase 1Bsemisynthesistype 2 diabetes mellitusα-glucosidase

Identifiers

PMID37628991
PMCPMC10454726
OpenAlexW4385835505

What Socratic holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.