Recent advances and structure-activity relationship studies of DPP-4 inhibitors as anti-diabetic agents.

Diabetes mellitus (DM) is one of the largest public health problems worldwide and in the last decades various therapeutic targets have been investigated. For the treatment of type-2 DM (T2DM), dipeptidyl peptidase-4 (DPP-4) is one of the well reported target and has established safety in terms of cardiovascular complexicity. Preclinical and clinical studies using DPP-4 inhibitors have demonstrated its safety and effectiveness and have lesser risk of associated hypoglycaemic effect making it suitable for elderly patients. FDA has approved a number of structurally diverse DPP-4 inhibitors for clinical use. The present manuscript aims to focus on the well reported hybrid and non-hybrid analogues and their structural activity relationship (SAR) studies. It aims to provide structural insights for this class of compounds pertaining to favourable applicability of selective DPP-4 inhibitors in the treatment of T2DM.

Nutraceuticals and phytotherapeutics for holistic management of amyotrophic lateral sclerosis.

Amyotrophic lateral sclerosis" (ALS) is a progressive neuronal disorder that affects sensory neurons in the brain and spinal cord, causing loss of muscle control. Moreover, additional neuronal subgroups as well as glial cells such as microglia, astrocytes, and oligodendrocytes are also thought to play a role in the aetiology. The disease affects upper motor neurons and lowers motor neurons and leads to that either lead to muscle weakness and wasting in the arms, legs, trunk and periventricular area. Oxidative stress, excitotoxicity, programmed cell death, altered neurofilament activity, anomalies in neurotransmission, abnormal protein processing and deterioration, increased inflammation, and mitochondrial dysfunction may all play a role in the progression of ALS. There are presently hardly FDA-approved drugs used to treat ALS, and they are only beneficial in slowing the progression of the disease and enhancing functions in certain individuals with ALS, not really in curing or preventing the illness. These days, researchers focus on understanding the pathogenesis of the disease by targeting several mechanisms aiming to develop successful treatments for ALS. This review discusses the epidemiology, risk factors, diagnosis, clinical features, pathophysiology, and disease management. The compilation focuses on alternative methods for the management of symptoms of ALS with nutraceuticals and phytotherapeutics.

Drug Repurposing Strategies for Non-cancer to Cancer Therapeutics.

Global efforts invested in the prevention and treatment of cancer need to be repositioned to develop safe, effective, and economic anticancer therapeutics by adopting rational approaches of drug discovery. Drug repurposing is one of the established approaches to reposition old, clinically approved off-patent noncancer drugs with known targets into newer indications. The literature review suggests a key role of drug repurposing in the development of drugs intended for cancer as well as noncancer therapeutics. A wide category of noncancer drugs such as, drugs acting on CNS, anthelmintics, cardiovascular drugs, antimalarial drugs, anti-inflammatory drugs, have come out with interesting outcomes during preclinical and clinical phases. In the present article, a comprehensive overview of the current scenario of drug repurposing for the treatment of cancer has been focused. The details of some successful studies along with examples have been included followed by associated challenges.

A systematic review on use of aminoquinolines for the therapeutic management of COVID-19: Efficacy, safety and clinical trials.

Recent global outbreak of the pandemic caused by coronavirus (COVID-19) emphasizes the urgent need for novel antiviral therapeutics. It can be supplemented by utilization of efficient and validated drug discovery approaches such as drug repurposing/repositioning. The well reported and clinically used anti-malarial aminoquinoline drugs (chloroquine and hydroxychloroquine) have shown potential to be repurposed to control the present pandemic by inhibition of COVID-19. The review elaborates the mechanism of action, safety (side effects, adverse effects, toxicity) and details of clinical trials for chloroquine and hydroxychloroquine to benefit the clinicians, medicinal chemist, pharmacologist actively involved in controlling the pandemic and to provide therapeutics for the treatment of COVID-19 infection.

Comparative analysis of enzyme-linked immunosorbent assay and direct microscopy for the diagnosis of Giardia intestinalis in fecal samples.

CONTEXT: Giardiasis is one of the most common nonviral infections causing diarrheal illness worldwide. In this prospective cross-sectional study, we evaluated the RIDASCREEN ® Giardia kit for detection of Giardia intestinalis in stool samples and compared the results with direct microscopy. MATERIALS AND METHODS: A total of 360 fecal samples were collected. They were then processed by wet film, iodine preparation and an enzyme-linked immunosorbent assay (ELISA) kit to determine the presence of Giardia trophozoites and cysts. Statistical analysis was performed by sensitivity, specificity, positive predictive value, negative predictive value and diagnostic accuracy. RESULTS AND CONCLUSION: Of the 360 cases, 17.2% samples were positive for Giardia by direct microscopy and 23.6% were found to be positive by ELISA (sensitivity ~97%), but specificity was ~92% only. Because of less specificity, we need to perform ELISA in congruence with direct microscopy, etc. Further studies need to be performed on a larger sample size using other molecular tests in order to get more accurate estimations.

Hematological parameters in patients of cleft lip and cleft palate with special reference to eosinophil counts.

INTRODUCTION: Birth abnormalities like cleft lip and cleft palate account for about 1.4 per 1000 live births in India. These are seen to be associated with a high incidence of eosinophilia which delays the surgical management of these patients. AIMS: The aim of this paper is to study the hematological parameters in patients of cleft lip and cleft palate. PATIENTS AND METHODS: A total of 223 cases of cleft lip and cleft palate were taken up for the study. Hematological parameters including hemoglobin, total leukocyte count, differential leukocyte count, absolute eosinophil count, and red cell indices were studied. RESULTS: Anemia was found in 182/223 (81.63%) cases which was most commonly of microcytic hypochromic type. Eosinophilia was seen in 46/223 (20.60%) cases. CONCLUSIONS: Many cleft lip and cleft palate patients show high eosinophil counts. Absolute eosinophil count was found to be a better parameter for assessment of eosinophils.