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Pharmaceuticals, Volume 15, Issue 12

December 2022 - 147 articles

Cover Story: The design of drugs for multifactorial diseases is one of the most significant challenges for medicinal chemistry today. In this scenario, multitarget drugs appear attractive as they can simultaneously affect several biological mechanisms. In this work, we present the molecular docking-directed optimization of 5-aminoanthranilic acid derivatives, their in vitro evaluation, and the determination of their effects in an in vivo model of metabolic syndrome induced by a hypercaloric diet. The optimized compound simultaneously lowered glucose, triglyceride, and cholesterol levels after 14 days of oral administration. The evidence suggests that the mechanisms related to the biological effects of these new compounds result from an orchestrated and balanced activation between different PPAR subtypes and HMG-CoA inhibitory properties. View this paper
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Articles (147)

  • Article
  • Open Access
1 Citations
3,047 Views
8 Pages

Real-World Comparative Evaluation of Add-On Glucagon-like Peptide 1 Receptor Agonist in Type 2 Diabetes Treated with or without Insulin

  • Hsuan-Wen Chou,
  • Kai-Pi Cheng,
  • An-Chi Lin,
  • Hao-Chang Hung,
  • Ching-Han Lin,
  • Chih-Chen Wang,
  • Hung-Tsung Wu and
  • Horng-Yih Ou

15 December 2022

Glucagon-like peptide 1 receptor agonist (GLP-1 RA) is a potent antidiabetic agent with cardiorenal and weight-losing benefits in patients with type 2 diabetes (T2D). The combination of GLP-1 RA with basal insulin has been suggested in several clinic...

  • Article
  • Open Access
4 Citations
2,823 Views
19 Pages

Component Characterization, In Vitro Activities and Molecular Mechanism of Cydonia oblonga Mill. against Diabetic

  • Bingqing Chi,
  • Xilong Liang,
  • Lihua Wang,
  • Yifei Bian,
  • Meng Zhang,
  • Zhixin Tang,
  • Danyang Wang and
  • Zhenhua Tian

15 December 2022

Cydonia Oblonga Mill. is widely distributed in Turkey, Uzbekistan and China and commonly used by the food industry to produce jam, jelly and candies. The aim of this study was to investigate the in vitro antidiabetic activity and anti-diabetic mechan...

  • Article
  • Open Access
2 Citations
2,894 Views
18 Pages

Isotopic Radiolabeling of Crizotinib with Fluorine-18 for In Vivo Pet Imaging

  • Malvika Sardana,
  • Louise Breuil,
  • Sébastien Goutal,
  • Maud Goislard,
  • Mikhail Kondrashov,
  • Etienne Marchal,
  • Florent L. Besson,
  • Christophe Dugave,
  • Gail Wrigley and
  • Anna C. Jonson
  • + 5 authors

15 December 2022

Crizotinib is a tyrosine kinase inhibitor approved for the treatment of non-small-cell lung cancer, but it is inefficient on brain metastases. Crizotinib is a substrate of the P-glycoprotein, and non-invasive nuclear imaging can be used to assess the...

  • Article
  • Open Access
5 Citations
2,804 Views
11 Pages

Safety Investigations of Two Formulations for Vaginal Use Obtained from Eugenia uniflora L. Leaves in Female Rats

  • Guilherme Donadel,
  • Mariana Dalmagro,
  • João Antonio Berta de Oliveira,
  • Giuliana Zardeto,
  • Mariana Moraes Pinc,
  • Jaqueline Hoscheid,
  • Odair Alberton,
  • Salviano Tramontin Belettini,
  • Ezilda Jacomassi and
  • Arquimedes Gasparotto Junior
  • + 1 author

15 December 2022

Medicinal plants have great prominence in research into the development of new medicines. Eugenia uniflora L. (Myrtaceae) is an edible and medicinal plant with economic value in the northeast region of Brazil. Several preparations from E. uniflora le...

  • Review
  • Open Access
2 Citations
3,314 Views
18 Pages

15 December 2022

Thyroid disorders are among the most common endocrinological conditions. As the prevalence of thyroid diseases increases annually, the exploration of thyroid disease mechanisms and the development of treatments are also gradually improving. With the...

  • Article
  • Open Access
6 Citations
3,381 Views
9 Pages

Characterization of Sigma-2 Receptor—Specific Binding Sites Using [3H]DTG and [125I]RHM-4

  • Chi-Chang Weng,
  • Aladdin Riad,
  • Brian P. Lieberman,
  • Kuiying Xu,
  • Xin Peng,
  • John L. Mikitsh and
  • Robert H. Mach

15 December 2022

The sigma-2 receptor/transmembrane protein 97 (σ2R/TMRM97) is a promising biomarker of tumor proliferation and a target for cancer therapy. [3H]DTG has been used to evaluate σ2R/TMEM97 binding affinity in compound development studies. How...

  • Article
  • Open Access
18 Citations
5,263 Views
17 Pages

14 December 2022

Cancer chemotherapy is known to cause cognitive defects in patients. Our study investigated the effect of piracetam (PIRA; 200 or 400 mg/kg) against doxorubicin (DOX)-induced cognitive deficits in a rat model. The cognitive parameters were analyzed u...

  • Article
  • Open Access
4 Citations
2,655 Views
12 Pages

14 December 2022

The advancement of high-throughput sequencing and genomic analysis revealed that acute lymphoblastic leukemia (ALL) is a genetically heterogeneous disease. The abundance of such genetic data in ALL can also be utilized to identify potential targets f...

  • Article
  • Open Access
8 Citations
3,519 Views
19 Pages

Human Lung Cancer (A549) Cell Line Cytotoxicity and Anti-Leishmania major Activity of Carissa macrocarpa Leaves: A Study Supported by UPLC-ESI-MS/MS Metabolites Profiling and Molecular Docking

  • Mohamed A. A. Orabi,
  • Omaish Salman Alqahtani,
  • Bandar A. Alyami,
  • Ahmed Abdullah Al Awadh,
  • El-Shaymaa Abdel-Sattar,
  • Katsuyoshi Matsunami,
  • Dalia I. Hamdan and
  • Mohamed E. Abouelela

14 December 2022

Lung cancer and cutaneous leishmaniasis are critical diseases with a relatively higher incidence in developing countries. In this research, the activity of Carissa macrocarpa leaf hydromethanolic extract and its solvent-fractions (n-hexane, EtOAc, n-...

  • Article
  • Open Access
14 Citations
3,426 Views
24 Pages

Protective Effects of Naringin–Dextrin Nanoformula against Chemically Induced Hepatocellular Carcinoma in Wistar Rats: Roles of Oxidative Stress, Inflammation, Cell Apoptosis, and Proliferation

  • Eman E. Mohamed,
  • Osama M. Ahmed,
  • Adel Abdel-Moneim,
  • Khairy M. A. Zoheir,
  • Basem H. Elesawy,
  • Ahmad Al Askary,
  • Ahmed Hassaballa and
  • Ahmed A. G. El-Shahawy

14 December 2022

Nanotechnology holds great promise for the development of treatments for deadly human diseases, such as hepatocellular carcinoma (HCC). In the current study, we compared the hepatoprotective effects of naringin–dextrin nanoparticles (NDNPs) aga...

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Pharmaceuticals - ISSN 1424-8247