In the current work, some 1,3,4-oxadiazole-naphthalene hybrids were designed and synthesised as VEGFR-2 inhibitors. The synthesised compounds were evaluated in vitro for their antiproliferative activity against two human cancer cell lines namely, HepG-2 and MCF-7. Compounds that exhibited promising cytotoxicity (5, 8, 15, 16, 17, and 18) were further evaluated for their VEGFR-2 inhibitory activities. Compound 5 showed good antiproliferative activity against both cell lines and inhibitory effect on VEGFR-2. Besides, it induced apoptosis by 22.86% compared to 0.51% in the control (HepG2) cells. This apoptotic effect was supported by a 5.61-fold increase in the level of caspase-3 compared to the control cells. Moreover, it arrested the HepG2 cell growth mostly at the Pre-G1 phase. Several in silico studies were performed including docking, ADMET, and toxicity studies to predict binding mode against VEGFR-2 and to anticipate pharmacokinetic, drug-likeness, and toxicity of the synthesised compounds.

Diabetic complications are among the most pressing health issues currently. Cardiovascular problems, particularly diabetic cardiomyopathy (DCM), are responsible for almost 80% of diabetic deaths. Because of the increasing prevalence of diabetes and the increased threat of death from its consequences, researchers are searching for new pharmaceutical targets to delay or cure it. Currently, there are a few medicines available for the treatment of DCM, some of which have serious side effects. To address this issue, researchers are focusing on natural products. Thus, in this review, we discuss the prevalence, incidence, risk factors, histological spectrum, diagnosis, pathogenic pathways of DCM, genetic and epigenetic mechanisms involved in DCM, the current treatments, and the beneficial effects of natural product–based therapeutics. Natural treatments range from single doses to continuous regimens lasting weeks or months. Flavonoids are the largest class of natural compounds reported for the treatment of DCM. Natural regimens may cover the way for new treatment strategies for DCM for being multi-target agents in the treatment of DCM, with the ability to play a variety of functions via distinct signaling pathways.

The use of angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) in coronavirus disease 2019 (COVID-19) patients has been claimed as associated with the risk of COVID-19 infection and its subsequent morbidities and mortalities. These claims were resulting from the possibility of upregulating the expression of angiotensin-converting enzyme 2 (ACE2), facilitation of SARS-CoV-2 entry, and increasing the susceptibility of infection in such treated cardiovascular patients. ACE2 and renin-angiotensin-aldosterone system (RAAS) products have a critical function in controlling the severity of lung injury, fibrosis, and failure following the initiation of the disease. This review is to clarify the mechanisms beyond the possible deleterious effects of angiotensin II (Ang II), and the potential protective role of angiotensin 1–7 (Ang 1–7) against pulmonary fibrosis, with a subsequent discussion of the latest updates on ACEIs/ARBs use and COVID-19 susceptibility in the light of these mechanisms and biochemical explanation.

Aim: To investigate the change in a serum level of copeptin, a neuroendocrine biomarker, in differentiating grades of COVID-19 severity on admission time and to find its diagnostic potential. Mater... Plain language summary We conducted a biochemical study on the role of copeptin – a biomarker of acute stress due to COVID-19 infection – in classification of COVID-19 severity on admission over 16...