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Topic Review
Biography
Topic Review
Diabetic Retinopathy Treatment
Diabetic retinopathy (DR) is one of the leading matters of vision-loss globally. Even though there have been extensive efforts to reduce vision loss, the prevalence of DR is still uprising. There are several pharmacological and surgical therapies currently used in clinics, but none of them has not been used as effective therapies at the early stage of DR.
565
01 Nov 2021
Topic Review
Diarylureas
The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties.
727
25 Jan 2021
Topic Review
Diet-Induced Insulin Resistance
Insulin resistance (IR) is defined as the decreased ability of insulin to insert the glucose transporter (glut4) on the cell membrane facilitating glucose entry into body cells. IR in the hepatocytes is associated with increased de novo lipogenesis and gluconeogenesis, leading to hypertriglyceridemia and hyperglycemia.
266
06 Nov 2023
Topic Review
Diet, Obesity, and Depression
Obesity and depression co-occur in a significant proportion of the population. Mechanisms linking the two disorders include the immune and the endocrine system, psychological and social mechanisms.
400
12 May 2021
Topic Review
Differential Inhibitors of Aldose Reductase
Aldose reductase, classified within the aldo-keto reductase family as AKR1B1, is an NADPH dependent enzyme that catalyzes the reduction of hydrophilic as well as hydrophobic aldehydes. AKR1B1 is the first enzyme of the so-called polyol pathway that allows the conversion of glucose into sorbitol, which in turn is oxidized to fructose by sorbitol dehydrogenase. The activation of the polyol pathway in hyperglycemic conditions is generally accepted as the event that is responsible for a series of long-term complications of diabetes such as retinopathy, cataract, nephropathy and neuropathy. The role of AKR1B1 in the onset of diabetic complications has made this enzyme the target for the development of molecules capable of inhibiting its activity.
690
11 Apr 2022
Topic Review
Digalloyl Glycoside: A Potential Inhibitor of Trypanosomal PFK
Human African trypanosomiasis is an endemic infectious disease caused by Trypanosoma brucei via the bite of tsetse-fly. Most of the drugs used for the treatment, e.g., Suramin, have shown several problems, including the high level of toxicity. A phytochemical investigation of the methanolic extract of E. abyssinica was carried out. Twelve compounds, including two triterpenes (1, 2); one sterol-glucoside (4); three ellagic acid derivatives (3, 9, 11); three gallic acid derivatives (5, 6, 10); and three flavonoids (7, 8, 12), were isolated. Compound (10) was obtained for the first time from genus Euphorbia while all other compounds except compound (4), were firstly reported in E. abyssinica. Consequently, an in silico study was used to estimate the anti-trypanosomal activity of the isolated compounds. Several compounds displayed interesting activity where 1,6-di-O-galloyl-d-glucose (10) appeared as the most potent inhibitor of trypanosomal phosphofructokinase (PFK). Moreover, molecular dynamics (MD) simulations and ADMET calculations were performed for 1,6-di-O-galloyl-d-glucose. In conclusion, 1,6-di-O-galloyl-d-glucose revealed high binding free energy, desirable molecular dynamics, and pharmacokinetic properties; therefore, it could be suggested for further in vitro and in vivo studies for trypanosomiasis.
436
04 Mar 2022
Topic Review
Dihydropyrimidine Dehydrogenase (DPD) Pharmacogenetics
The dihydropyrimidine dehydrogenase (DPD), encoded by the DPYD gene, is the enzyme mainly involved in the catabolism of fluoropyrimidines (FP). DPYD polymorphisms increase the risk of severe FP-related toxicity and DPYD-pharmacogenetics (DPYD-PGx) is recommended before starting the FP-based chemotherapy. Other factors influence FP safety, therefore phenotyping methods, such as measurement of plasmatic 5-fluorouracil (5-FU) clearance and DPD activity, could complement the DPYD-PGx. Here, authors reported eleven clinical cases in whom a combined genotyping/phenotyping approach, together with careful clinical monitoring was used to optimise the FP-based treatment. In addition, authors performed a systematic review of the literature concerning the use of DPYD-PGx, together with phenotyping methods to personalise such a chemotherapy.
540
23 Mar 2021
Topic Review
Dinoflagellate Phycotoxins
Dinoflagellates are single-celled eukaryotes constitute an important group of phytoplanktons, characterized by two dissimilar flagella and distinctive features of both plants and animals.
610
30 Dec 2020
Topic Review
Dipeptidyl Peptidase 4 Inhibitors
Information on absorption, metabolism and excretion of drugs is necessary to support the studies on their pharmacokinetics and potential drug–drug interactions. Moreover, the knowledge on drug metabolism is one of the crucial factors used to assess their pharmacokinetic profile in patients with some dysfunctions. It is especially important in diabetic patients with higher incidence of chronic liver and kidney problems.
256
27 Jul 2023
Topic Review
Discovering Amino Acid Transporter Inhibitors
Amino acid transporters are abundant amongst the solute carrier family and have an important role in facilitating the transfer of amino acids across cell membranes. Because of their impact on cell nutrient distribution, they also appear to have an important role in the growth and development of cancer. Naturally, this has made amino acid transporters a novel target of interest for the development of new anticancer drugs.
96
05 Mar 2024
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